pharm. practice exam questions- exam 2 Flashcards

Question

Is Stokes' ideal situation realistic? why or why not what does Stokes' law allow for

Answer 1

no, it is not! Because particles are - not necessarily uniform - are irregularly shaped - particle settling results in turbulence and collisions. Stokes law does allow - formulation experts to determine the formulation features that can be changed to achieve an elegant and desired finished product.

Answer 2

1 to 50 μm

Answer 3

Reduction in particle size produces slow and more uniform settling, but not too small. If too small, a compact cake could form. Compact cakes are difficult to break up with shaking

Answer 4

The particle shape of the suspensoid can affect the stability Needle shape versus barrel-shaped particles

Answer 5

: form strong sediment cake on standing that can’t be disturbed upon gentle shaking

Answer 6

do not cake on standing at all

Answer 7

Consider preventing particle agglomeration into crystals or some larger particulate mass of the dispersed phase by using a floc (or floccule)

Answer 8

a mass or collection of things

Answer 9

form a type of lattice that do not completely settle. The ‘flocs’ settle to form a higher sediment volume than non-flocculated particles. The flocculated particles break up easily with a gentle amount of shaking.

Answer 10

- Rapid settling is not ideal, - Suspending agents (i.e., carboxymethyl cellulose- CMC, methylcellulose, bentonite) are used to thicken the medium to suspend the suspensoid. Once suspending agent has been determined, tests must be performed to be certain that agent does not interfere with drug availability.

Answer 11

a system consisting of a suspension of solid particles in a liquid.

Answer 12

enough and should not make suspension too viscous - because these are too difficult to pour.

Answer 13

Density of the suspensoid Amount of material requiring support Whether it is flocculated

Answer 14

relationship between the dispersed phase and continuous phase

Answer 15

dispersed medium (vehicle) and is therefore wetted by it.

Answer 16

when dispersed materials lack any affinity for the medium they clump together or float on the vehicle-- In this case, wetting agents like hydroscopic agent are employed like - Alcohol Glycerin, - Propylene glycol

Answer 17

Displace air in crevices of the particles, permitting dispersed medium to penetrate the particle Preservatives should also be added when possible to safeguard against microbial and mold growth.

Answer 18

Antacid oral suspensions Antibacterial oral suspensions Rectal suspensions Dry powders for suspensions

Answer 19

Intended to combat the effects of gastric hyperactivity (i.e., peptic ulcers of the stomach). Many OTC medications are available for the treatment of patients with gastric indigestions, or to counter acid reflux to the esophagus and throat

Answer 20

water-insoluble material acting within gastrointestinal tract, soothing the irritated or inflamed linings of GI tract.

Answer 21

Ability to neutralize acid effects vary according to the chemical reagents employed

Answer 22

Sodium bicarbonate (SB): Magnesium preparations (MP): Calcium carbonate: Aluminum hydroxide:

Answer 23

Neutralizes acid effectively. However, can produce sodium overload and systemic alkalosis.

Answer 24

Neutralizes acid effectively. However, can cause diarrhea and cause problems for patients with renal impaired function.

Answer 25

Neutralizes acid effectively. However, can also cause hypercalcemia and stimulation of acid secretion (acid rebound).

Answer 26

Neutralizes effects slowly, and not as well as SB or MP. However, excessive use may lead to constipation and phosphate depletion, resulting in muscle weakness, bone resorption and hypercalciuria

Answer 27

absorb faster

Answer 28

Must be reasonably fast acting since gastric emptying is rapid (~1 hr in fasting stomach following administration).

Answer 29

within 10 minutes of simulation gastric conditions.

Answer 30

Pharmacists must caution patients against taking such drugs concomitantly (together) so caution against taking calcium-containing drug with antacid

Answer 31

a suspension that can be administered rectally or orally for diagnostic visualization of GI tract. Do not confuse with sulfite

Answer 32

for oral suspensions, Antibiotics represent the majority of drugs prepared as a dry mix.

Answer 33

The antibiotic drug, colorants flavorants Sweeteners, (e.g.,sucrose, dextrose) Stabilizing agents (e.g., citric acid) Suspending agents (e.g., methylcellulose) Preserving agents (e.g., methylparaben, sodium benzoate) where the water is where contamination could happen All of these excipients must be soluble in the continuous phase—which come into contact with sweeteners

Answer 34

During reconstitution of dry powder or granules, the use of purified water (rather than tap water) will prevent the possibility of any impurities from affecting stability of the preparation.

Answer 35

Pharmacists must realize that oversized containers are to be used to allow for adequate shaking after purified water has been added.– do not want to fill up so much but leave room to be able to shake Note: The amount of water to be added should not be estimated, but should be carefully measured for accuracy. Too much or too little must be avoided.

Answer 36

Cholestyramine (Questran, Par)- for treatment of hyperlipidemia, Barium Sulfate (Barospere, Mallinckrodt)- for visualization of the gastrointestinal tract, used orally or rectally.

Answer 37

“A dispersion in which the dispersed phase is Composed of small globules of a liquid distributed throughout a vehicle in which it is immiscible”– going to globules, oils, vary in size range

Answer 38

Since the external phase of an emulsion is continuous an o/w emulsion may be diluted (or extended) with water or some other aqueous preparation. Similarly, in w/o emulsion it may be diluted with oil-miscible liquid.

Answer 39

Many pharmaceutical preparations that are really emulsions are not classified as such, because they fit another category more appropriately. For e.g., Certain ointments, creams, lotions, commercial vitamin drops

Answer 40

To mask the unpleasant taste of many solid powders The reduced particle size of globules make them more digestible, and more easily absorbed Drugs that are irritating to the skin are less irritating in the internal phase of an emulsified topical preparation when compared to external phase. To healthy skin, a w/o emulsion is preferred because it goes on evenly and is softening to the skin Absorption through the skin is faster with diminished size of internal phase

Answer 41

Should not interfere with the action of the other dosage form ingredients Should be stable and not deteriorate in preparation Should be non-toxic with respect to intended use and amount consumed by patient Should possess little odor, taste or color. Should maintain stability of emulsion for shelf life of product

Answer 42

assigned to emulsifying agents rank the level of hydrophilicity or lipophilicity of an emulsifying agent

Answer 43

Emulsifiers (w/o) 3-6 mostly lipophilic, water is in oil! Emulsifiers (o/w) 8-18 mostly hydrophilic, oil is in water!

Answer 44

a function of emulsifying agents When the liquid is in contact with a second liquid in which it is insoluble (and immiscible), the force causes each liquid to resist breakup into smaller particles. This is called interfacial tension.

Answer 45

A substance that can reduce this tension causing the smaller particles to break up Into smaller drops (or particles) is called a surfactant (or wetting agent). These agents work on the surface of the droplets.

Answer 46

Surface tension theory- Oriented-wedge theory- Interfacial film theory-

Answer 47

Reduces the repellent force between the two liquids, diminishing attraction for its own molecules. Do not want them fusing

Answer 48

Preference for one phase over another depending on the surfactant agent an O/W or W/O emulsion forms depending on the character of the emulsifying agent.

Answer 49

Each drop of the internal phase of the emulsion is covered by an emulsifying agent, preventing contact of the dispersed phase. The tougher the film the more stable the emulsion.

Answer 50

The internal phase forms aggregates of globules Large globules or aggregates of globules rise to the top or fall to bottom of emulsion to form concentrated layers of internal phase—want uniform distribution If all parts of the liquid of the internal phase separates and forms a distinct layer (on top or bottom of the emulsion) Microbial contamination and growth and other chemical and physical alterations

Answer 51

Castor Oil Emulsion:

Answer 52

Used as a laxative for constipation For radiography and endoscopic examination, working directly on small intestines promoting bowel movements. Too much may cause excessive water loss

Answer 53

Amount of castor oil in commercial emulsions varies from 35% to 67%. Amount of oil influences dose required. Better taken on empty stomach followed by one full glass of water

Answer 54

Adult dose is 45 ml (three tablespoonsfuls) Children between 2 and 6 yrs old, 15 ml is sufficient Children less than 2 years of age, 5 ml is sufficient

Answer 55

An O/W emulsion Much more palatable than unemulsified mineral oil Usual dose is 30 mL (unemulsified dose is 15 mL) Both taken 1 hr before bedtime. - Want to make sure that water can support it

Answer 56

Formula: O/W emulsion, lots of water! Mineral Oil 500 mL Syrup 100 mL Vanillin 40 mg Alcohol 60 mL Purified water, to make 1000 mL

Answer 57

Semisolid particles enclosed by, and interpenetrated by, a liquid. Semirigid system, where the movement of the dispersing medium is limited by a network of particles of the dispersed phase Aggregations are controlled Lattice organization makes them thicker

Answer 58

To form Gels, gelling agents are necessary. Amount of Gelling agents used is typically <10% (usually in 0.5% to 2.0% range).

Answer 59

are homogeneous preparations, there is only one phase, cannot be heterogenous

Answer 60

If the gel does not appear to have discrete particles, it is called as a one-phase system. If the gel contains small discrete particles, the gel is called a two-phase system. a two phase gel system with floccules dispersed in gel

Answer 61

5% bentonite + purified water

Answer 62

Describe and demonstrate, How to shake the emulsion and suspension How to measure required doses How to administer a dose How to recap and store bottles containing product How to determine if products are physically unstable and thus not recommended for use

Answer 63

“Ointments, creams and gels are semisolid dosage forms intended for topical application”

Answer 64

Protectants (covers layer of skin, P), emollients (flexible & pliable, E), lubricants (where there is a lot friction, E)

Answer 65

Local or systemic absorption: Dermatologic applications treat the skin

Answer 66

Skin, nose, surface of eye, vagina or rectum

Answer 67

Oleaginous bases Absorption bases Water-removable bases- Water-soluble bases

Answer 68

Have an emollient effect, protecting against moisture escape Effective occlusive dressings One application for an extended period without drying out

Answer 69

Does not wash off easily Petrolatum, USP White Petrolatum, USP Yellow Ointment, USP White Ointment, USP (see textbook)

Answer 70

A purified mixture of semisolid hydrocarbons obtained from petrolatum. Color ranges from yellowish to amber Used alone or in combination with other agents as an ointment base Known as yellow petrolatum and petroleum jelly - Vaseline (Chesbrough-Ponds).

Answer 71

A decolorized purified mixture of semisolid hydrocarbons from petroleum Lighter color compared to yellow petrolatum- Pharmacists prefer this variety in compounding Commercial product ---White vaseline (Chesebrough-Ponds)

Answer 72

The product is all the way to the top so the cover is very close This product implies: it looks like this and is solid from top to bottom, but there could be less in there. But you could have more because we can get rid of air pockets. All depends on the drug product

Answer 73

Yellow wax 50g Petrolatum 950g Purified wax derived from honeycomb of bee Apis mellifera.

Answer 74

Melt yellow wax in a water bath (adding petrolatum until uniform mixture) Cool and stir The viscosity of yellow ointment is greater than plain petrolatum- viscosity is the reason why we have variety and why we want it to be apart of the product

Answer 75

type I type II Type I: permit the incorporation of aqueous solutions, producing water-in-oil (w/o) emulsions (e.g., hydrophilic petrolatum*) Type II: water-in-oil (w/o) that permits additional aqueous solutions (e.g., lanolin). absorption bases are good for incorporating small amounts of aqueous solutions into hydrocarbon bases. the aqueous solutions are incorporated into the absorption base, and then incorporating the mixture into the hydrocarbon base. absorption bases do not wash off well because Because the oil absorbs onto the skin *Hydrophilic Petrolatum, USP Cholesterol 30g Stearyl alcohol 30g White wax 80g White petrolatum. 860g

Answer 76

Lanolin, USP Obtained from sheep wool Cleaned, deodorized (otherwise it would smell) and decolorized No more than 0.25% water– do not need too much water Additional water may be added by mixing

Answer 77

These are oil-in-water (O/W) emulsions closely resemble creams May be diluted with water (aqueous external phase) May absorb serous discharges External phase is water Internal phase is oil If external phase is water, would you want to dilute with oil? No cause they don’t mix but do with water instead

Answer 78

Hydrophilic Ointment, USP (NOT OLEAGINOUS) Ingredient Amount (grams) Methylparaben 0.25 Propylparaben 0.15 Sodium lauryl sulfate 10.00 Propylene glycol 120.00 Stearyl alcohol 250.00 White petrolatum 250.00 Purified water 370.00

Answer 79

Water-soluble bases do not contain oleaginous components (aka~ greaseless) Soften with the addition of water, will compromise dosage form, no need to add more water Large amounts of aqueous solutions are not effectively incorporated in these bases Normally used for the incorporation of solid substances PEG <600: Clear, colorless >600, <1000: Semisolid PEG 1000: Wax-like

Answer 80

Desired release rate of drug from the ointment base? Desirability of topical or percutaneous drug absorption Stability of drug in the ointment base Effect (if any) the drug might have on characteristics of ointment base Desire for a base to be easily removed with water Characteristics of the surface to which the base is applied The base providing the best combination of most desired attributes should be used Creams, applied to weeping or oozing surfaces Lotions, usually applied to where friction may occur (under arm pits, thighs) Ointments, applied to dry and scaly skin surfaces

Answer 81

Mix component until uniform mixture: - use Mortar and pestle - use Spatula and ointment slab or parchment paper

Answer 82

Use stainless steel spatula except when ingredients react with the stainless steel material (i.e., iodine). A Rubber spatula can replace stainless steel in this case – 2 options: Thorough rubbing and working of the components together on solid surface until smooth and make preparation uniform.

Answer 83

Levigation is often used to reduce powder particle size to reduce grittiness prior to incorporation of the solid material into the base. Mineral oil is used for when oil is the external phase Glycerin is used when water is the external phase.

Answer 84

Add solution to minimum amount of hydrophilic base, and then Add this freshly prepared mixture to the hydrophobic base.

Answer 85

alcoholic solutions

Answer 86

By this method, “all or some of the components of an ointment are combined by being melted together and cooled with constant stirring until congealed”

Answer 87

Heat-sensitive or volatile components are added when the temperature of mixture is low enough not to cause decomposition or volatilization. In general, components having the highest melting points are heated to the lowest required temperature to produce a melt. Think of temp.

Answer 88

Melt the component with the lowest melting point first, followed by the addition of the remaining components in order of their melting points. 2) Melt all components simultaneously, increasing the temperature only as needed

Answer 89

Water content is an issue. Staphylococcus aureus often found in dermatologic preparations

Answer 90

Rectal, Urethral, Vaginal Due to the presence of Yeast and Molds at the site of application

Answer 91

packaged in either jars, tubes or syringes

Answer 92

packaged in tubes or syringes

Answer 93

Large mouth containers or metal or plastic tubes Store in cool place in sealed containers Opaque or light sensitive containers used when necessary Labels (for ointments, creams) include type of base (water soluble, water insoluble)

Answer 94

“Semisolid preparations containing one or more drug agents dissolved or dispersed in W/O or O/W emulsion or another water-washable base.” Used topically, rectally and vaginally

Answer 95

Generally when creams evaporate a thin residue film consisting of stearic acid (or other oleaginous components) is left behind. Preferred over ointments by patients and pharmacists since they are easily removed, Still, both options are generally made available.

Answer 96

“Semisolid systems consisting of dispersions of small or large molecules in an aqueous liquid, rendered jellylike by the addition of a gelling agent.” Gelling agent- Carbomers (high MW, water-soluble polymers) Can be prepared to be used with various routes, including skin, eye, nose, vagina and rectum

Answer 97

The polymeric composition of Carbomers determines their viscosity. NF contains monographs of 6, they are 910, 934, 934P, 940*, 941 and 1342. Used as gelling agents at 0.5% to 2.0% in water * 940 has the highest viscosity Gels = Jellies

Answer 98

“Semisolid preparations intended for application to skin. They contain more solid material compared to ointments (~25%).This makes them a little stiffer.” Used to absorb serous secretions, remaining in place after application. A portion of base is softened prior to incorporating the solids, A portion of the base is used rather than a liquid because the liquid will soften the base.

Answer 99

“Solid or semisolid adhesive masses spread on the backing of paper, fabric, moleskin or plastic.” Adhesive tape- Adhesive plaster are used Provide prolonged contact at the site. Unmedicated variety: provide protection or mechanical support at the application site Medicated variety: Concentration of salicylic acid used in commercial plasters (range from 10-40%) for the treatment of corns of feet. examples: hansaplast, corn removal plaster

Answer 100

Plastic masses consisting of the following, gelatin 15% glycerin 40% water 35% medicinal substance 10% (i.e., zinc oxide) Melted and cooled to just above body temperature Fine brush is used to apply the material, and is generally covered with bandage after hardening Applied to skin for long-term. Currently, zinc gelatin is used to treat varicose ulcers (aka~ Zing gelatin boot

Answer 101

Major route of drug transport in the eye is by simple diffusion via the cornea If not efficient, secondary routes are conjunctiva and sclera. Three layered structure of cornea: -Lipophilic epithelial layer - Hydrophilic stromal layer - Less Lipophilic endothelial layer on inside (inner layer) All things considered, lipophilic drugs penetrate these layers better than hydrophilic compounds

Answer 102

Special considerations required- steam sterilization is ineffective because cannot penetrate the ointment base. Dry heat can sterilize but too harsh. So end stage sterilization is not commonly practiced. - Instead, aseptic techniques are used when each component is added, including weighing of the ingredients. Methylparaben, (0.05%) Propylparaben, (0.01%) Benzalkonium chloride, (0.008%) All very small

Answer 103

For nasal delivery ointments and gels are used. Nasal passage is lined with thin layer of mucus produced by epithelial mucus glands. Ciliated epithelium assists with mucus movement Local effects is the primary treatment approach (i.e., nasal decongestants). The nasal passage's vascular region enables general circulation, so systemic absorption does occur. Can be used to deliver insulin, vaccines, polypeptides & proteins.

Answer 104

Drug should both penetrate and be retained in the skin for a specified period Physicochemical properties of the drug Characteristics of the vehicle Concentration of drug in the vehicle Oil-water partition coefficient (PC) And general condition of the skin The skin (like in transdermal delivery systems- TDDS) acts as a natural barrier controlling the rate and extent to which drugs can penetrate it. However, unlike with TDDS, the therapeutic drug concentration delivered by a dermatologic preparation is not known. So, more qualitative measures are used.

Answer 105

Patient must thoroughly clean the affected area with soap and water Dry the area with clean soft cloth Thin layer of medication is applied to skin area, and spread evenly. -- Typically 1 to 3 mg of ointment or cream is applied per square centimeter of skin – thin layer Area of application should remain uncovered unless otherwise stated Clean hands immediately following use

Answer 106

Instruct patient of proper method of administration Explain frequency and duration of use Any special warnings, For e.g., how should it be used during pregnancy? Therapeutic goals and outcomes Signs of an adverse response, and what to do if something goes wrong When should treatment be discontinued?

Answer 107

Only a thin film should be applied Unless otherwise instructed, remove a sufficient quantity from container, apply it, and gently rub into the affected area Use a protective pad to protect area from being removed from the clothing Use of lotions and creams should be avoided Do not rub eyes or touch mouth during handling of application If patient exhibits sensitivity or intolerance contact pharmacist or physician

Answer 108

Largest organ, 1.7 m2, 10% body weight. Primary function (Barrier) 1. UV radiation 2. Chemicals 3. Allergens 4. Microorganisms 5. Loss of moisture, nutrients.

Answer 109

epidermis dermis subcutaneous layer medication for nausea or motion sickness can be placed behind the ear or the thigh thickness behind the ear: 0.084 penetration: 10.0 thickness of thigh: 0.106 penetration: 4.7 behind the ear has a faster rate of penetration because it has a smaller thickness

Answer 110

transcellular route follicular route intercellular route

Answer 111

0.1% of the skin surface area. * May be target site for drug delivery. * Mostly not significant for transdermal pathway.

Answer 112

* intracellular matrix is relative polar in nature. * Intercellular lipid are lipophilic. Permeation requires repeated partitioning (divide into parts) between polar environment and lipophilic domain.

Answer 113

Provide the only continuous route through the stratum corneum. * Diffusion of rate limiting region of very polar permeant is the polar pathway. * Less polar permeant through the lipid pathway

Answer 114

driven by the concentration gradient the vehicle has to pass through SC, which has to pass through epidermis then dermis

Answer 115

flux (J) - the quantity of material (M) flowing through a cross-section of a barrier (A) in unit time (dt) J = (dM)/(Adt) partition coefficient = Ksc Ksc = Csc/Cv J = (D(Co - Ci)/h) = (DKscCv)/h D = diffusion coefficient (area/time) h = thickness of the barrier (cm) C = concentration of drugs

Answer 116

fick's law is at steady state, input rate = output rate input = dM/dt = A x J output rate = eliminatiion rate = Cls x Cpss Cls = systemic clearance (V/time) Cpss = Steady state plasma concentration A * J = Cls * Cpss Cpss = A * J /Cls

Answer 117

Output rate = Cls x Cpss = 5 ng/ml x 10 L/hr =5 μg/L x 10 L/hr = 50 μg/hr Input rate = A J For a patch size usually < 50 cm2, target flux should be > 1 μg/cm2/hr.

Answer 118

Bypass hepatic “first pass” * Bypass gastrointestinal incompatibility * Reduce side effects * Provide predictable and extended duration of activity * Greater patient compliance * Reversibility of drug delivery for removal * Minimize inter- and intrapatient variation Self administration * Can use drugs with short half-life * Administration of drugs with narrow therapeutic window * Zero order release * Controlled release for accurate dosing * Control of plasma levels of potent drugs

Answer 119

Clonidine * Fentanyl * Nicotine * Nitroglycerin. 2.3 ± 0.6 min * Scopolamine * Estradiol The activity of these drugs can be extended through the reservoir of the drugs present in the transdermal delivery devices.

Answer 120

Permeation of drugs through human skin is limited - Stratum corneum is the rate-limiting factor - Only potent drugs that do not require high plasma levels are suitable for delivery Skin irritation from adhesives, API, excipients and enhancers -- Contact allergic dermatitis (involves host immunological activity) -- Contact irritant dermatitis (direct toxic injury to cell membranes, cytoplasm or nuclei) * Poor adhesive of transdermal devices

Answer 121

Polymeric matrix or matrices * Drug (Pharmaceutically Active Ingredient) * Permeation enhancers and other excipients * Adhesives

Answer 122

it supports matrix structure and regulate the release of the drug from the Patch Polymer (polypropylene, polyester) * Cross-linked polymer * Co-polymer Ethylene-vinyl acetate copolymer (EVA) Poly (Vinyl alcohol)-co-(vinyl pyrrolidone) * Polymer blend (PVA-PVP)

Answer 123

Be potent (10 mg to mg per day) * Short half-life * Lipophilicity/Hydrophilicity (predicted by Partition coefficient, K) (logP = 1 - 3.5) * MW and size of molecules (<500) * Extent of skin binding * 1st pass effect is high * Non-irritating to the skin * Clinical necessity for steady state delivery

Answer 124

Pharmacologically inert * Non-toxic, non-irritating, non-allergenic * Reliable and predictable * Immediate recovery of the skin (reversible disruption of the skin) * Compatible with the API

Answer 125

Lipophilic solvents - Dimethylsulfoxide (DMSO) - Dimethylformamide (DMF) 2-Pyrrvolidinone * Surface active agents - Sodium lauryl sulfate (SDS) - Dodecyl methyl sulfoxide * Two component system - Propylene glycol-oleic acid - 1,4 butane diol-linoleic acid

Answer 126

Hydration causes corneocyte swelling and keratin bundle dissociation disrupt the highly ordered structure of the intercellular lipids. * interact with intracellular proteins embedded in the corneocytes to increase the transcellular permeation.

Answer 127

Peripheral adhesive Face adhesive Factors to consider with adhesives - Non-irritating/non-toxic - Adhere to skin aggressively during dosing - Easily removable - Excellent contact with skin

Answer 128

backing film drug reservoir microporous membrane adhesive disc release liner

Answer 129

Polyacrylic copolymer Deponit Glyceryl Trinitrate Polypropylene

Answer 130

"a distinct category of adhesive tapes that in dry form are aggressive and permanently tacky at room temperature.

Answer 131

The measured surface energy of the adhesive must be equal to less than that of the human skin. Kinetic requirement: the material must possess sufficient mobility at room temperature. Under the condition of application, the adhesive must be able to flow sufficiently. * Easily removable Must not leave any residue behind on the skin. examples: PIB-based adhesives (polyisobutylene) * Acylic adhesives (dominates the medical PSA market) A mixture of hard and soft polymers * Silicone-based PSAs long chain polydimethylsiloxane (PDMS) (Tg = -140oC) + benzene- soluble silicate resin.

Answer 132

adhesive device monolithic device reservoir device Membrane-Moderated (Reservoir) - backing - drug reservoir - semipermeable membrane - adhesive - protective peel strip parts of a monolithic device - backing - rate-controlling matrix containing drug - adhesive parts of adhesive - backing - drug - containing adhesive

Answer 133

Skin-controlled drug input system in forearm: rate is 5ug/hr in the chest: rate is 10ug/hr - there is no rate-controlling membrane - example: nitro-disc system-controlled drug input system in forearm: rate is 3ug/hr in the chest: rate is 3ug/hr - system controls the rate - example: transderm-scopolamine

Answer 134

A natural hormone used for the relief of post- menopausal syndromes and osteoporosis. * Oral dosed undergoes significant 1st pass * Short half-life = 1 hr * Not substantially metabolized by skin * Convenient once to twice a week dosing on the trunk (abdomen, buttock) ESTROGENS INCREASE THE RISK OF ENDOMETRIAL CANCER

Answer 135

Vivelle-Dot® contains estradiol in a multipolymeric adhesive. The system is designed to release estradiol continuously upon application to intact skin. 1. A translucent polyolefin film 2. An adhesive formulation containing estradiol, acrylic adhesive, silicone adhesive, oleyl alcohol, povidone, and dipropylene glycol 3. A polyester release liner.

Answer 136

Antimuscarinic drug, natural ingredient found in belladonna plant used for motion sickness 1st transdermal drug device approved by FDA Non-irritating Potent drug: 1 mg/72 hr Short-half life (2.9 ± 1.2 h) anticholinergic side- effects when given orally

Answer 137

(1) Backing layer of tan-colored, aluminized, polyester film (2) Drug reservoir: light mineral oil, and polyisobutylene (3) Rate-controlling microporous polypropylene membrane (4) Adhesive formulation of mineral oil, polyisobutylene, and scopolamine. (5) A protective peel strip of siliconized polyester, which covers the adhesive layer

Answer 138

An antihypertensive agent Oral drug undergoes significant 1st pass Highly lipid soluble Low therapeutic concentration (0.2-2 ng/mL) Once a week 4-layers: backing, reservoir, micro-porous membrane, adhesive formulation

Answer 139

Antianginal drug used for prevention of angina pectoris due to coronary artery disease A Vasodilator Very short-half life (min) Extensive 1st pass Low dose (Cpss 1.2 – 10 ng/mL) Tolerance is common for long term use Side-effects include headache, dizziness, and hypotension, and skin irritation Transderm-Nitro (Novartis) Nitro-Dur (Key) Deponit (Schwarz Pharma)

Answer 140

To provide nicotine replacement therapy to obtain plasma levels of nicotine that would prevent or lessen the severity of the withdrawal symptoms

Answer 141

DURAGESIC® (fentanyl transdermal system) is a transdermal system providing continuous systemic delivery of fentanyl, a potent opioid analgesic, for 72 hours. The amount of fentanyl released from each system per hour is proportional to the surface area (25 μg/h per 10 cm2) 1) a backing layer of polyester film 2) a drug reservoir of fentanyl and alcohol USP gelled with hydroxyethyl cellulose 3) an ethylene-vinyl acetate copolymer membrane that controls the rate of fentanyl delivery to the skin surface 4) a fentanyl containing silicone adhesive. Before use, a protectiv

Answer 142

1. Drug in adhesive Matrix Patch. 2. No rate-controlling membrane.

Answer 143

Layer 1 (Backing Film) is a thin flexible polyester/ethylene-vinyl acetate film that provides the matrix system with occlusivity and physical integrity and protects the adhesive/drug layer. Layer 2 (Adhesive/Drug Layer) is a cast film of acrylic adhesive containing oxybutynin and triacetin. Layer 3 (Release Liner) is two overlapped siliconized polyester strips that are peeled off and discarded by the patient prior to applying the matrix system. 49

Answer 144

OXYTROL is designed to deliver oxybutynin continuously and consistently over a 3- to 4-day interval after application to intact skin Oxybutynin is an antispasmodic, anticholinergic agent

Answer 145

Lidoderm (lidocaine patch 5%) is comprised of an adhesive material containing 5% lidocaine, which is applied to a non-woven polyester felt backing and covered with a polyethylene terephthalate (PET) film release liner. The release liner is removed prior to application to the skin.The size of the patch is 10 cm x 14 cm. Each adhesive patch contains 700 mg of lidocaine in an aqueous base. The Lidoderm® patch is the only topical analgesic indicated to treat the pain of postherpetic neuralgia (PHN)

Answer 146

PHN is the pain after the rash from shingles is gone  Shingles are caused by chicken- pox infection of nerves  Pain can last for 6 months  Zostrix cream  five-six times a day. It will take two to three weeks of use before the cream will start to work

Answer 147

The ORTHO EVRA birth control patch is a highly effective, weekly hormonal birth control patch that is worn on the skin to prevent pregnancy. ORTHO EVRA contains two types of hormones: estrogen (ethinyl estradiol) and progestin (norelgestromin). ORTHO EVRA can be worn in several discreet locations: buttock, abdomen, upper torso, or upper outer arm.

Answer 148

Wash your hands with soap and water before applying the patch. Dry hands completely. * Clean the area chosen with soap and water. Rinse and wipe the area completely dry with a clean tissue. * Apply the patch at the same time of day. * Apply to a non-hairy area of the body. * Do not apply the patch on skin folds or wear under tight clothing. * Do not use the same spot all the time but rotate to different areas. * Do not apply a patch directly after showering, bathing, or swimming. * Open the package and remove and throw away the protective backing. Do not touch the sticky side. * Do not cut the patches. * Attach the patch to the skin and press firmly in place for 10-15 sec. Run your finger along the outside edge of the patch to seal it. * Remove the throwaway patch after the specified time or before applying the next patch. * Repeat the above procedure.

Answer 149

Iontophoresis * Sonophoresis * Microneedle

Answer 150

- Ultrasonic refers to sound waves whose frequency is >20 KHz - the movement of drugs through living skin and into soft tissue under the influence of an ultrasonic perturbation - you have a power supply attached to an ultrasonic transducer attached to the skin and the applied formulation sends sound waves through the skin to allow chemicals to pass through the skin

Answer 151

- a method used to enhance permeability - mechanisms: electrophoresis, electro-osmosis, increased permeability how it works: - put a patch on, this patch is a battery with a + and - end - an electric current is passed from the positive side to the negative side of the patch battery - the ionized drug comes from the positive side and follows the current but gets dropped off into the bloodstream. - the counter ion (which is negative) moves to the negative side E-Trans Fentanyl Patch (Alza, 2004). Indication: post operation pain or cancer chronic pain. Patient self-controllable.

Answer 152

- used for drug deleivery enhancement drug can diffuse through residual holes in skin from a topical formulation (solid MN) drug is absrobed into aqueous layer of the skin (coated MN) microneedles are made of water soluble or biodegradable materials and released into the skin (dissolving MN) hollow microneedles are used to inject liquid formulations into the skin (hollow MN)

Answer 153

What is a capsule? “ A solid dosage form in which medicinal agents and/or inert substances are enclosed within a small shell of gelatin” * When a patient is unable to swallow an intact solid dosage form, chewable tablet, instant dissolving tablets, oral liquids, or suppositories are made available

Answer 154

used to make most capsules the capsule is made of: gelatin, sugar & water they are clear, colorless and tasteless what it consists of - has a long base or body with a small diameter - cap to slide over the base intended to be - swallowed whole - contents should be opened and administered in food or liquid with the acceptance of a pharmacist the gelatin is soluble in hot water & in warm gastric fluids gelatin is digested by proteolytic enzymes and absorbed When gelatin dissolves it exposes its medicinal contents to the gastric (or intestinal) bodily fluids Most are colored with FD&C and D&C dyes and made opaque by adding titanium dioxide. Gelatin is obtained by the partial hydrolysis of collagen obtained from - skin, - white connective tissue, and - bones of animals While stable in air, gelatin is subject to microbial decomposition when moist Hard capsules: contain between 13-16% moisture, but poor storage conditions can increase this level. Not good! size is determined by how much material will go inside sizes: 000 (largest) to 5 (smallest), 8 actual sizes [000,00,0,1,2,3,4 and 5] A pharmacist may compound capsules of a single medicinal agent, or combination of agents at the precise dosage prescribed for the patient pharmacists use the punch method to fill capsules: - Start with the exact number of capsules to be filled - Powder to be encapsulated and placed on a sheet of paper, clean glass, or porcelain plate - Using a spatula powder is formed into a cake - Empty capsule body is held between the thumb and forefinger and “punched” vertically into the powder cake repeatedly until filled

Answer 155

they are pharmaceutically elegant and easily swallowed Prepared to contain liquid, paste & dry fills – Liquids that can easily migrate through the capsule shell cannot be encapsulated into soft gelatin capsules– so if the liquid can easily move through the shell, then it cannot be used When not to be used?: – When water content is > 5% – When low molecular weight water-soluble and organic compounds are employed such as * alcohols, ketones, amines, and esters. Preservatives such as methylparaben and/or propylparaben is used to retard microbial growth – these are antifungal

Answer 156

the size is always determined by the amount of material to be incorporated For human use: 000 (the largest) to 5 (the smallest) are commercially available. There are 8 actual sizes [000,00,0,1,2,3,4 and 5] * Numerical designations are arbitrary, and do not indicate the capsule’s capacity A pharmacist may compound capsules of a single medicinal agent, or combination of agents at the precise dosage prescribed for the patient

Answer 157

they must be: – Harmless (in the quantities used) – Do not exceed the minimum amounts required to provide their intended effect – Do not impair the bioavailability of the product – Do not interfere with assays to evaluate dosage form method 1 to fill capsule: torbial torsion scale - Formulation must be weighed directly to the capsule. It wouldn’t be accurate otherwise. - To compensate for the weight of the empty capsule being filled, the same capsule must be placed on the other side of the balance with a weight equal to the amount to be filled method 2: punch method Pharmacists use the “punch” method – Start with the exact number of capsules to be filled – Powder to be encapsulated and placed on a sheet of paper, clean glass, or porcelain plate – Using a spatula powder is formed into a cake An empty capsule body is held between the thumb and forefinger and “punched” vertically into the powder cake repeatedly until filled. when cleaning and polishing capsules: - Small amounts of powder may adhere to the outside of capsules after filling

Answer 158

Small amounts of powder may adhere to the outside of capsules after filling Must remove before packaging and dispensing, wipe with clean gauze or cloth On large-scale cleaning, a vacuum can remove extraneous materials

Answer 159

– Harmless (in the quantities used) – Do not exceed the minimum amounts required to provide their intended effect – Do not impair the bioavailability of the product – Do not interfere with assays to evaluate dosage form

Answer 160

inspecting counting: handling: capsules are Easier storage and transport

Answer 161

the more food in your stomach, the longer it takes for gastric emptying to occur and for the capsule to be absorbed light objects float on gastric contents heavy objects fall to the base of greater curvature

Answer 162

Often vary in size, shape, hardness, thickness, and in their ability to dissolve In fluids. These tablets are grooved - Are therefore intended to be broken into two parts. - Why? Offers flexibility Patients can swallow them easily or use in divided doses Compressed tablets (C.T.): Usually contain the following in addition to medicinal agents * Diluents or Fillers: Add bulk to prepare a certain size * Binder or Adhesives: Promote adhesion of the particles of the formulation * Disintegrants: Promotes breakup of tablets/drug availability * Antiadherents/ glidants/ or lubricating agents * Miscellaneous Adjuncts: Colorants and flavorants to enhance overall appearance Multiple compressed tablets (M.C.T.): More than a single compression Produces multiple-layered tablet or a tablet within a tablet Each layer may contain diff. medicinal agents. Why? * Separation may be required to avoid chemical and physical incompatibility Staged drug release General appearance of multiple-layered tablet Sugar-coated tablets (S.C.T): Compressed tablet can be covered with a colored or an uncolored sugar layer – The coating is water soluble – The coating is quickly dissolved after swallowing – The coating protects the enclosed drug from the environment – The coating enhances the general appearance of tablets and permits imprinting of identifying manufacturer’s info. – Disadvantages to sugarcoating tablets are, – the time and expertise required in the coating process, – the increase in size, weight, and shipping costs. * May be 50% larger and heavier than uncoated tablets Film-coated tablets (F.C.T.): These compressed tablets are coated with a thin layer of a polymer capable of forming a skin-like film over the tablet Usually colored More durable, less bulky, and less time-consuming to apply than sugar-coatings. Designed to rupture and expose the core tablet at the desired location within the gastrointestinal tract Gelatin-coated tablets: GElCAP, – Capsule-shaped compressed tablets – Facilitates swallowing and compared to unsealed capsules, gelatin tablets are more tamper-evident Enteric-coated tablets (E.C.T.): Have delayed release characteristics Designed to pass unchanged through stomach intestines where the tablets disintegrate and allow drug dissolution. Mainly used when by-passing the stomach to improve drug absorption Buccal or sublingual tablets: These are flat, oval tablets intended to be dissolved in the buccal pouch, or beneath the tongue through absorption through the oral mucosa – An alternative for drugs that are poorly absorbed from the G.I. Tract – Buccal tablets designed to erode slowly – Sublingual tablets designed to provide rapid release Buccal: In direction of the cheek Sublingual: Below or beneath the tongue The dosage form must remain in place Total area of absorption is low compared to other routes- 100 to 170 cm2 – Taste must be bland, or not acceptable for use – must also be a non-irritant – Drug should not discolor or erode teethLining of the epithelium is keratinized for buccal and sublingual, but the epithelium for sublingual is thinner. What does this tell us about drug absorption? chewable: Have a creamy base usually of specially flavored and colored mannitol * Rapid disintegration when chewed or allowed to dissolve in mouth * Ideally suited for children and adults who have difficulty swallowing solid dosage forms. molded tablets ablet triturates (TT) may be prepared by compression and by molding. * In terms of appearance very soft and soluble * Diluent: Lactose and Sucrose usually * Designed for rapid dissolution * Pharmacists may insert TT inside a capsule or dissolved in liquids to provide accurate amounts of potent drugs. Instant Disintegrating/ Dissolving tablets * Extended Release Tablets (E.R.) Vaginal Tablets: Also called vaginal inserts Uncoated and bullet or ovoid shaped tablets * Inserted in vagina for localized effects – Antibacterials for the treatment of Vaginitis caused by Hemophilus vaginalis or – Antifungal for treatment of vulvo vaginitis candidiasis caused by Candida albicans and related species

Answer 163

Solid dosage forms used to administer medicinal substances through the rectum, vagina, or urethra * They melt or dissolve in the body cavity The shape and size should not cause discomfort – Should be retained for a required period of time in order to exert a desired effect. Do not want drugs to be released prematurely bases can either melt or dissolve melting is faster than dissolving

Answer 164

Are inserted with the fingers instead of applicator * Are usually about 32 mm (1.5 inches), and are shaped like a bullet, a torpedo, or the little finger. * The density of base and medication in the suppository determines suppository weight – Adult rectal suppositories weigh about 2 g when cocoa butter (theobroma oil) is employed - larger – Children rectal suppositories weigh half that of adults and assume a pencil shape - smaller

Answer 165

Vaginal suppositories are called pessaries * They are globular, oviform, or cone-shaped * Weigh about 5 g when cocoa butter is the base. – The base used to prepare an individual manufacturer’s product will determine weight * May contain one or more active agents that are compatible and do not form eutectic mixtures * Some excipients used: * diluents, adsorbents, lubricants, or antimicrobial preservatives (so no need to steam sterilize

Answer 166

Urethral suppositories are called bougies, They are slender or pencil-shaped * Intended for insertion into the male or female urethra * This suppository is placed on tip of an applicator and is administered by placing tip into urethra after urination. – Example: MUSE (alprostadil)- single use application *(see article) Drug is suspended in PEG 1450 excipient – Male urethral suppositories: * 4 grams in weight – Female urethral suppositories: * 1/2 that of the male urethral suppository, * 2 grams in weight.

Answer 167

rectal suppositpries are used to relieve constipation or the pain, irritation, itching, and inflammation associated with hemorrhoids * Antihemmorhoidal suppositories typically contain a multitude of different agents (i.e., local anesthetics, vasoconstrictors soothing emollients, astringents, protective agents etc...) – When inserted the suppositories must melt or dissolve and distribute drug substances – Transport from rectal epithelium primarily involves two transport processes: – Paracellular route (between cells) - main route – Transcellular route (through cells) or intracellular

Answer 168

The mucous membranes of the rectum and vagina permits the absorption of many drug agents. – The vagina is NOT used as frequently as the rectum for delivering drug substances; the vagina permits local drug effects only The anal canal is lined by a mucous membrane that covers the internal sphincter. Suppository is inserted with the rounded end first so that it can be pushed in with the flat end. The smooth muscles of the rectum quickly grip the inserted suppository and push it in further. Once inserted, the cold, solid suppository picks heat from the body and then slowly melts to release the active ingredients inside it.

Answer 169

Drugs destroyed or inactivated by the pH, or enzymatic activity of the stomach, are ideal candidates * Drugs irritating to the stomach may be given without irritation * Drugs destroyed by the portal circulation may bypass the liver after rectal absorption * Convenient route for administration of drugs to adult or pediatric patients who prefer not to swallow medication * Convenient, and effective way to administer drugs to patients experiencing vomiting episodes and used as a tranquilizer – Prochloroperazine and chloropromazine

Answer 170

This increases the interaction of drug products with the intended absorbing surface than if fecal matter is there Evacuant Enema may be administered before the administration of the suppository for better absorption - make sure that the pathway is clear Diarrhea, circulation route, colonic obstruction due to tumors, and tissue dehydration can all slow down the rate of drug absorption

Answer 171

Human rectum: – Contains 2 to 3 ml of mucous fluid – No villi or microvilli Abundant vascularization of the submucosal region of the rectum wall with blood and lymphatic vessels – Factors include: Colonic content, pH and lack of buffering capacity of rectal fluids * Drugs absorbed rectally bypass the portal circulation during first pass into the general circulation * Hemorrhoidal veins surrounding the colon receive the absorbed drug, and initiate its circulation throughout the body bypassing the liver * Lymphatic circulation assists with rectal drug absorption 13

Answer 172

Rectal fluids are neutral in pH [no effective buffering capacity] and so drugs will not be changed chemically While cocoa butter melts rapidly at body temperature it does not mix well in fluids, and so does not release fat soluble drugs very well Cocoa butter base should therefore be used with ionized (salt form) of drug to maximize bioavailability drug that has a high affinity for cocoa will not be released because it is very lipophilic can use cocoa butter base for drug with lipo/hydrophilic base

Answer 173

Because the ionized drug form will “maximize bioavailability” when cocoa butter is the base Gelatin and poly-ethylene glycol bases can slow down the rate of releasing un-ionized drugs. gelatin and polyethylene glycol bases can slow down the rate of releasing un-ionized drugs

Answer 174

Relative solubility in lipid and in water – Particle size of dispersed drug – Ability to melt, soften, or dissolve at body temperature – Ability to release the drug substance

Answer 175

Play an essential role in the release of drugs that they hold, and therefore in the availability of the drug for local systemic effects Should remain solid at room temperature but melt or dissolve at body temperature, to make drug fully available soon after insertion

Answer 176

Base must be capable of melting, softening or dissolving to release its drug components for absorption if the base irritates the mucous membrane it might prompt a bowel movement and will prevent complete drug release and absorption but can be prevented with evacuated enema When drug retention time in the bowel is limited to 2 hours absorption is approximately 40%. Not 100% but for local action is good but not good for systemic action * Longer-acting drug effects can be achieved with the use of Alginic acid as a component of the suppository base. Can be used as a stable excipient to increase melting temp. * Research is performed to determine the best formulation for specific purposes

Answer 177

Lipid-water partition coefficient of drug is important consideration in selection of suppository base. A lipophilic drug distributed in a fatty suppository base in low concentrations will not escape to surrounding aqueous fluids as well as a hydrophilic drug. can combine cocoa 100% cocoa has the most melting if I add PEG, and does not have as much melting

Answer 178

For drugs present in suppositories in an undissolved state, the size of the drug particle will influence rate of dissolution and availability for absorption The smaller the particle size the more readily the dissolution of the particle and the greater the chance for rapid absorption larger size -> effects rate of dissolution, makes it slower can control: particle size using mortar suppository base unionized or ionized drug

Answer 179

Fatty or Oleaginous bases * Water-soluble and water-miscible bases * Miscellaneous bases

Answer 180

Because cocoa butter, NF from the roasted seed Theobroma cacao is a member of this class, and was the first base introduced to the market. Hydrogenated fatty acids of vegetable oils such as palm kernel oil and cotton seed oil. – Higher MW fatty acids, such as palmitic & stearic acid. Various combinations are used to, * Achieve a base with desired hardness for shipment & storage * Achieve a base with desired quality for optimal absorption.

Answer 181

Cocoa butter melts between 30 and 36 °C. This is ideal. It’s a solid at room temperature and melts just below body temperature – Given that cocoa butter has a high triglyceride (glycerin + fatty acid) content it exhibits polymorphism (several crystal forms). – When cocoa butter is hastily melted at temperatures well above minimum required, and then quickly chilled, it will form a metastable (alpha) crystal form. Not Good! Why bad?- ----------because Melting point now much lower than cocoa butter, and dosage form may now melt before insertion needle: form cake, skinny barrel: better, larger

Answer 182

You can fix this by allowing the metastable crystal enough time to form a solid. Several days usually required to achieve this. The problem is that this is useless for the patient, because it takes too much time. Cocoa butter should be slowly and evenly melted over a water bath of warm water, to avoid unstable crystal formation, and to ensure ß crystals (the good crystal form) upon chilling of the liquid. Phenol and chloral hydrate can lower melting temperature * Cetyl ester wax (~20%) * Beeswax (~4%) these will not lower temp so use when adding phenol or choral hydrate

Answer 183

Glycerin (or glycerinated gelatin), is a hydroscopic material (attracts moisture) and so when these suppositories are used they must be protected from moisture to maintain shape and consistency Glycerin is slow to soften and dissolve in physiologic fluids Urethra suppositories may be prepared by this base – Gelatin constitutes about 60% of the weight, glycerin about 20% and aqueous drug portion is 20%

Answer 184

PEG (Poly-ethylene glycol) 300 (-15 to -18 °C) 1000 (37 to 40 °C) 8000 (60 to 63 °C) iincrease size comes with increase of temp PEG suppositories will NOT melt at room temperature, will dissolve slowly in body fluids. This lowers the release rate of drug substances. Convenient storage of suppositories too! PEG (poly-ethylene glycol) are polymers of ethylene oxide and water. * Come in a number of molecular weights 300 to 8000 * These are clear and colorless liquids * Hardness of material increases with molecular weight

Answer 185

These consist of mixtures of both oleaginous and water-soluble (or water-miscible) material. * Hydrophilic suppository bases are often used to hold water or aqueous solutions – Example: Poly-oxyl 40 stearate (surface-active agent employed suppositories) * Emulsifying agents (for O/W W/O) can be used to prepare suppositories. because it has oleaginous and water-soluble material like emulsifying agents,

Answer 186

used for individual and large numbers – most used today are made from stainless steel, aluminum, brass, or plastic – scratches to the molding surfaces will make for somewhat rougher surfaces and increase the chances of making imperfect suppositories – plastic molds are prone to scratching

Answer 187

If to be stored at 4 °C suppositories should be warmed to room temperature before insertion * Rub cocoa butter suppositories gently with fingers to melt the surface to provide lubrication for insertion * Glycerinated gelatin or PEG suppositories should be moistened (with water) to enhance lubrication * If PEG formulation does not contain at least 20% water, dipping in water first before insertion will cut down on irritation run gently under H20, will absorb H20 and help with irritation if cold, need to warm for insertion to be comfortable

Answer 188

1 - remove foil wrapper 2- moisten the supposiitory with water or water based lubricatiing jelly 3- lie on your side and bend yur right knee up toward your chest. Gently push the suppository into your rectum so it is deep enough not to come out

Answer 189

Why Vaginal Suppositories? – To combat infections in the female genitourinary area – To restore a normal vaginal mucosal state, – For contraception. – Potential for Long term drug absorption with various intrauterine devices (IUDs) Commonly used base is PEG. Various MWs * Surfactants and preservatives usually added to base * Buffered to an acid pH around 4.5 and this resembles the normal vaginal pH – Acidity discourages pathogenic organisms and provides an environment for colonization of acid-producing bacilli normally present in the vagina – Ex: Progesterone Vaginal Suppositories * Micronized progesterone powder is typically used. * Polyethylene-glycol, cocoa butter bases are used alone or together.

Answer 190

Easier to manufacture, more stable, less messy to handle and use Shape: Ovoid – Plastic inserter designed for proper placement of the tablet in the vagina usually comes with these tablets. – Tablets are intended to disintegrate within the vagina where medication is released

Answer 191

Glycerin based suppositories and glycerinated gelatin suppositories packaged in glass containers and should be closed tightly Cocoa butter based suppositories are wrapped individually to prevent direct contact * Light sensitive materials are wrapped in opaque material ex: metallic foil * Suppositories are adversely affected by heat so store them in a cool place no warm place

Answer 192

Bisacodyl 10 mg Aspirin 300 mg Hydrocortisone acetate 25 mg Prochlorperazine 25 mg

Answer 193

More than a single compression Produces multiple-layered tablet or a tablet within a tablet Each layer may contain diff. medicinal agents. Why? * Separation may be required to avoid chemical and physical incompatibility Staged drug release General appearance of multiple-layered tablet

Answer 194

fecal matter - can decreases the interaction of drug products with the intended absorbing surface, can use an evacuant enema for better absorption diarrhea, circulation route, colonic obstruction due to tumors, and tissue dehydration - these can slow down the rate of drug absorption human rectum - has 2 to 3 ml of mucous fluid - no villi or microvilli Abundant vascularization of the submucosal region of the rectum wall with blood and lymphatic vessels Factors include: Colonic content, pH, and lack of buffering capacity of rectal fluids portal circulation - Drugs absorbed rectally bypass the portal circulation during the first pass into the general circulation Hemorrhoidal veins - surround the colon receive the absorbed drug and initiate its circulation throughout the body bypassing the liver Lymphatic circulation - assists with rectal drug absorption pH and lack of buffering capacity - drugs will not be changed because rectal fluids are neutral in pH cocoa butter: While cocoa butter melts rapidly at body temperature it does not mix well in fluids, and so does not release fat-soluble drugs very well Cocoa butter base should therefore be used with ionized (salt form) drug to maximize bioavailability use an ionized form of drug when using cocoa butter for systemic issues because it will maximize bioavailability

Answer 195

Relative solubility in lipid and in water Particle size of dispersed drug Ability to melt, soften, or dissolve at body temperature Ability to release the drug substance

Answer 196

A & B only

Answer 197

2.2 years 7.5 months

Answer 198

stratum corneum epiderms dermis subcutaneous Stratum Corneum: “The horny outer layer of epidermis consisting of several layers of flat keratinized, non-nucleated dead or peeling cells.”

Answer 199

Non-polar drugs tend to cross the cell barrier through the lipid-rich regions (transcellular route), whereas the polar drug favor transport between the cells (intercellular route) Rate of drug movement depends on: - Concentration in the vehicle - Aqueous solubility - Oil-water partition coefficient between stratum corneum and vehicle * Ideally, the drug should have some aqueous and lipophilic character

Answer 200

Facilitate passage of therapeutic quantities of drug substances through the skin, and into the general circulation for their systemic effect.

Answer 201

Chemical enhancers improve percutaneous absorption -Acetone -Azone -Poly-ethylene glycol -DMSO General considerations: -Efficacy in enhancing skin permeation -Low toxicity -Biocompatibility

Answer 202

Indicators of percutaneous drug absorption -Measurable blood levels of the drug -Detectable excretion of the drug -Clinical response of the patient

Answer 203

In the case of scopolamine, the membrane system (not the skin), controls the rate of absorption. Why? Rate that drug is released is less than the skin’s ability to absorb components: backing drug reservoir semipermeable membrane adhesive protective peel strip

Answer 204

Physical and chemical properties of the skin Molecular weight Solubility and Pka Partitioning coefficient Nature of the carrier vehicle Condition of the skin Age Temperature Site of administration Race (Pigmentation -Dark and white skin) Disease (i.e., Psoriasis)

Answer 205

Monolithic Membrane-controlled transdermal systems Chemical methods Physical methods

Answer 206

Two types: (1) With (2) and without, excess drug inside the matrix With excess drug: Drug reserve is used to ensure continued drug saturation Without excess drug: Used to maintain saturation at the stratum corneum layer, only.

Answer 207

film backing drug/adhesive layer protective liner To prepare a monolithic system: The drug and polymer are both dissolved or blended together, cast as a matrix and dried. Most of these systems are designed to contain an excess of drug, and thus have drug-releasing capacity beyond the time frame recommended for replacement.

Answer 208

Designed to contain a drug reservoir or “pouch”, usually in liquid or gel form, a rate-controlling membrane, and backing, adhesive and protecting layers. an example: scopolamine What is the advantage of this system over the Monolithic systems? As long as the drug in the reservoir system remains saturated, the drug release remains constant

Answer 209

To prepare this system the delivery unit is added to the drug reservoir, and sealed by a process called lamination. Make a note that either the drug delivery system, or the skin, may serve to control drug release.

Answer 210

These are chemicals that increase skin permeability by reversibly damaging or by altering the physicochemical nature of the stratum corneum to reduce its diffusional resistance. How? Increased hydration of the stratum corneum, or Change properties of lipids and proteins Examples include: DMSO (dimethylsulfoxide), ethanol, polyethylene glycol etc…

Answer 211

Iontophoresis An applied electric field is used to deliver chemicals across the skin membrane by following mechanisms, Ionic-electric field interaction Increased permeability Electroosmosis produces bulk motion of solvent Ex: Dexamethasone and verapamil Sonophoresis High frequency ultrasound used to deliver chemicals across the skin membrane Chemical enhancers may not be necessary Ex: hydrocortisone, and salicyclic acid used in gels, creams and in lotions

Answer 212

Charged drug molecules are transported into and through tissues with use of a small direct current Current is passed through a drug-containing “active” electrode in contact with skin Can be used to treat areas of inflammation such as tendonitis Can be used as an alternative to procedures that are more invasive

Answer 213

The advantage that compounds need not be ionized More effective than topical applications alone Cavitation (occurring in keratinocytes) gave rise to better penetration of vitamin A within cells, stimulating mRNA and this produced faster growth of keratinocytes and collagen production.

Answer 214

Used to provide controlled release of nitroglycerin. Used to treat angina. Where applied? Chest and upper arm of shoulder areas Backing: Aluminized plastic Drug reservoir content: Nitroglycerin adsorbed on lactose, colloidal silicon dioxide, and silicone medical fluid

Answer 215

Used to provide controlled release of scopolamine over a 3 day period Used to treat nausea related to travel particularly by sea Where applied? Behind the ear. One patch removed and another can be applied when desirable Backing: Aluminized polyester film Drug reservoir contents: Scopolamine, mineral oil, and polyisobutylene

Answer 216

Dose: 7 to 22 mg of nicotine per/day Treatment: 6-8 wks Should be replaced daily Should be discarded immediately after use Patients are provided with sustained levels of nicotine in blood Where applied? Arm or upper front torso

Answer 217

Dose: 0.05 or 0.1 mg estradiol per/day Treatment: 3 weeks of treatment followed by one without and so forth Patients are provided with 17-β estradiol for conditions associated with menopause, primary ovarian failure etc… Oral delivery a problem, Why? Estradiol Estrone Where applied? lower stomach area, below your waistline

Answer 218

Dose: Fentanyl 25 µg/hr Treatment: 72 hrs Where applied: Apply the patch to a dry, flat skin area on your upper arm, chest, or back. This medicine is a tan, square, transdermal system imprinted with "FENTANYL 25 mcg/hr".

Answer 219

Can avoid difficulties with gastrointestinal drug absorption Can be used as a substitute for oral administration of medication Can avoid first-pass elimination The systems are non-invasive Can provide extended therapy with a single application Drugs having a short half-life can be extended through the reservoir Drug therapy may be terminated by removing the application from the skin surface Ease of rapid identification of the medication in emergency situations

Answer 220

Only potent drugs are considered suitable candidates because only low plasma levels of drug can be maintained Some patients may develop severe response to treatment at the site of application (i.e., dermatitis). In such cases treatments are usually terminated.

Answer 221

Extent of percutaneous absorption may vary according to site of application TDDSs should be applied to clean dry skin areas Use of skin lotions should be avoided TDDS should not be physically altered in any way Be careful not to damage TDDS when removing from package Apply to areas not likely to be rubbed off by clothing Must be worn for the full period of time as discussed in packing insert Use clean hands when applying and removing TDDS Always seek medical advice to sensitivity or any intolerance to the TDDS Remove the patch when finished and discard as recommended. Keep away from children

pharm. practice exam questions- exam 2 Flashcards

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