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102- Science of Medicines > Dosage Forms > Flashcards

Dosage Forms Flashcards

(38 cards)

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1
Q

Sublingual & Buccal

A

Sublingual - under the tongue.
Buccal - between the gum & the cheek.
Rapidly dissolve & absorbed rapidly through the mucous membranes, where they enter the bloodstream, bypassing the stomach & liver.

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2
Q

Effervescent Tablet

A
  • Uncoated tablets which effervesce in water before consumption.
  • Gives rapid tablet dispersion & dissolution, can be pleasant taste & lubricants need to be water soluble.
  • Use sodium bicarbonate to produce effervescence.
  • Sodium bicarbonate can increase rate of tablet disintegration, dissolution & gastric emptying, enabling faster absorption speed.
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3
Q

Oral Granules

A

Solid, dry aggregates of powder particles oft in sachets. Some swallowed, some with water.

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4
Q

Suppositories

A

Via rectum, vagina (pessaries) or urethra (bougies) that melt, soften or dissolve in the body cavity. Useful for targeted or avoiding hepatic first pass.

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5
Q

Oro-dispersible tablets/melts

A

Dissolves or disintegrates in saliva, making solution or suspension. May be absorbed in mouth, pharynx & oesophagus, possibly increasing bioavailability.

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6
Q

Capsules

A

Drug within a gelatine or a sugar-based matrix:
1. Hard-shelled capsules, which are normally used for dry, powdered ingredients,
2. Soft-shelled capsules, primarily used for oils & for APIs dissolved or suspended in oils or emulsions.

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7
Q

Solution: Adv & Dis

A

Clear liquid preparations for oral use containing APIs dissolved in a solvent.
Adv:
* delivery system for low solubility drugs
* avoid large vol of solvent- solution of this drug
* avoid precipitation upon storage when co-solvent is used
* taste masking of drugs
* difficulty in swallowing solid-dosage forms
* controlled drug delivery
Dis:
* Problems - correct dosage
* unstable; formulation to ensure stability over the period of the shelf-life
* difficult aesthetic suspension
* bulky, difficult for patient to carry

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8
Q

Emulsions

A

Oral emulsions are stabilized oil-in-water dispersions, either or both phases of which may contain dissolved solids.
Adv:
* Delivery of drugs with low (aq) solubility:
* Taste masking - sweetening agents
* Administration of oils with therapeutic effect
* reduction of irritation after topical administration: drug in internal phase (o/w)
* ease of swallowing
* total parenteral nutrition
Dis:
* Thermodynamically unstable; appropriate formulation is needed to stabilise the emulsion from separation of the two phases.
* Pharmaceutical emulsions may be difficult to manufacture.

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9
Q

Suspensions

A

One or more APIs suspended in a suitable vehicle, possibly altered with thickening agents.

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10
Q

Syrup

A
  • [Highly] (aq) of sugar or substitute & flavouring agent - masks bad taste
  • unflavoured syrup, mostly sugar
  • drugs: directly incorporated or added as the syrup is being prepared
  • choice of syrup vehicle based on physicochemical properties of drug
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11
Q

Elixir

A

Pleasantly flavoured clear liquid of potent or nauseous drugs. Antimicrobials & ethanol within purified water used to confer stability of the preparation.

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12
Q

Linctus

A

Viscous, liquid usually prescribed for the relief of cough, & reduces inflammation of throat, typically small dose.

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13
Q

Ointments

A

Viscous, semi-solid, greasy preparations for application to the skin, rectum or nasal mucosa. Ointments may be used as emollients or to apply suspended or dissolved medicaments to the skin.

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14
Q

Transdermal Patch

A

Deliver specific dose through the skin & into the bloodstream in a controlled release.

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15
Q

Creams

A

Semi-solid emulsions, which are mixes of oil & water. Divided into two types:
1. Oil-in-water (O/W) creams: less greasy & more easily washed off using water.
2. Water-in-oil (W/O) creams: used many hydrophobic drugs & will be released more readily from a water-in-oil. Are also moisturizing.

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16
Q

Subcutaneous

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A

Injecting fluid into the subcutis, the layer of fatty tissue directly below the dermis & epidermis. Highly effective in administering vaccines & such medications as insulin.

17
Q

Intramuscular Injection

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A

Injection of a substance directly into a muscle. Can be faster or more gradual.

18
Q

Intravenous (IV) injection

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A

Injected in a vein with 100% bioavailability for rapid action.

19
Q

Preformulation

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A

1st step in developing dosage forms using the physiochemical properties of the API

20
Q

Subcutaneous: Adv & Dis

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A

Advantages:
* Slow, sustained delivery
* Self-administration possible
* Implants for long-term delivery
Disadvantages:
* Small doses
* Pain and irritation from repeated injections

21
Q

Intramuscular drug delivery: Adv & Dis

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A

Advantages:
* Relatively large volume
* Sustained release
Disadvantages:
* Professional required
* Erratic absorption

22
Q

Intravenous drug delivery: Adv & Dis

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A

Advantages:
* Rapid effects
* Dose – precise dosing, large volumes possible
* 100% bioavailability
Disadvantages:
* Potential toxicity – rapid Cp elevation (can be controlled by infusion)
* Suitable vein
* Professional required – admin. & monitoring
* Cost
* Duration (infusion can extend dosing)

23
Q

Sublingual & Buccal: Adv & Dis

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A

Advantages
- Possible Hepatic first pass avoidance
- Residence time – sustained delivery possible
- Taste
- Good Compliance – talking, eating, drinking, etc
- Rapid action
Disadvantages
- Irritation – possible, but oral mucosa robust

24
Q

Suppositories: Adv & Dis

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A

Suppositories
Adv:
- good for unconscious or vomiting patients
- avoids poor taste
- Avoidance of possible upper GI tract disease
- Drugs extensively degraded via oral delivery
- Sustained release possible
- Possible protein delivery
Dis:
- compliance

25
Tablets: Adv & Dis
Adv: * Accurate dosage/ minimum variability * Convenience * Greater stability than liquid * Tailored rate of release * Mass production * Simple & cost effective * Good Compliance Dis: * Swallowing * Difficulty in preparing some formulations * Bitter taste &/or bad odour * Oxygen & moisture sensitivity requiring coating of certain tablets
26
Capsules: Adv & Dis
Adv: * No need to compress drugs * Drug uniformity * Dispersed drug stability - oily vehicle protects drugs sensitive to oxidation or hydrolysis. * Drug formulations as self-emulsifying oils increases oral bioavailability. Dis: * Drugs containing high [water] or other gelatine solvents can’t be incorporated. * Surfactants affect the capsule seal * Needs specific pH range * Crosslinking: Gelatine crosslinking may render capsule insoluble. * Water loss or uptake may damage capsule
27
Tablet production requirements:
1) Particles must be sufficiently free flowing 2) Particles, when subjected to a force, cohere to form a compact of adequate strength 3) Adhesion of the tablet must be avoided Few API meet this list, so excipients are ergo required.
28
Liquid Dosage forms: Adv & Dis
Adv: * Better compliance * Faster therapeutic response * Homogeneous system * Reduced irritation; immediate dilution by gastric contents Dis: * Breakage of container * Growth of microorganism * Poorer stability in (aq) than solid dosage form. Stability of excipients. * Shorter shelf-live than solid dosage form. * Dose accuracy (patients uses spoon) * unsuitable for drugs chemically unstable in presence of water
29
Liquid solution Vehicle: Purified Water USP:
Liquid solution Vehicle: Purified Water USP: * Low cost & toxicity * Tap water has chemical incompatibilities * Solid residue after evaporation high * Unsuitable for parenteral formulations as not sterilised
30
Oral administration: Adv & Dis
Adv: * GI tract designed for absorption * Easier, no infection risks * Broad diversity of oral dosage forms * Able to do a variety of release times * Compliance Dis: * Hepatic first pass * Difficulty swallowing * Possible Drug Degradation
31
Nasal drug delivery: Adv & Dis
Adv: - Topical delivery for treatment - Avoidance of first-pass metabolism - Good for Drugs sensitive to intestinal metabolism e.g. Acid-sensitive drugs - Good for Polar compounds with poor oral absorption - Small, lipophilic drugs can diffuse through the nasal epithelium & enter circulation with up to 100% bioavailability. - Ease of administration (drops and sprays) - Little blood brain barrier, drugs enter brain through paracellular diffusion or through olfactory nerves. Promising for drug delivery to CNS Dis: - Nasal physiology differences make absorption inconsistent - Mucus acts as a physical & chemical barrier to drug diffusion.
32
Vaginal Drug Delivery: Adv & Dis
Adv: - Topical delivery - Avoidance of hepatic – first pass effect. - Area has lower enzyme activity Dis: - Many physiochemical factors vary with age and cycle.
33
Ocular drug delivery:
Drugs administered solely for treatment of local conditions, not a viable route for systemic delivery
34
Transdermal Delivery: Adv & Dis Things to increase skin permeability
Adv: - Hydration of Stratum Corneum increase permeability - Control delivery of potent drugs - Reduced dosing frequency - Fewer side-effects are possible - Can be stopped at any time - Good compliance - Hepatic first pass avoidance - Injury & disease reduce barrier action Dis: - Cutaneous first-pass - Varies with age - Varied thickness of skin Things to increase skin permeability: - Iontophoresis – provides active drug reservoir for release - Microneedles – attach to epidermis, then releases substances into it
35
Pulmonary drug delivery: Adv & Dis
Adv: - Topical delivery - Huge potential for systemic delivery - Avoids hepatic first-pass - Reduces dose needed, minimizing side effects Dis: - Large SA, rapid administration possible - Mucus acts a chemical & physical barrier
36
Multi particulate Systems: Adv & Dis
Adv of multi-particulates: * More consistent GI transit than single dose monolithic tablet. * Good stability, flow & bulk density Dis: * Control of membrane characteristics using film-coating can be difficult. * Multi-particulates are difficult to retain in the upper GI tract. Drug-release mechanisms from multi-particulates: * Diffusion: Water diffuses in, the drug dissolves & diffuses across controlled-release coat. * Osmosis: Water enters, osmotic pressure builds, forcing drug solution out. * Erosion: Coating degrades over time, releasing the drug.
37
Water soluble: Adv & Dis (relative to fatty bases):
Adv * Suppository m.pt. can be adjustable to withstand exposure to warmer temp. * Release of drug is independent upon m.pt. * Physical stability on storage is improved. * Suppositories are readily miscible with rectal fluids. Dis: * Chemically more reactive than fats. Incompatible with many drugs. * Care required in processing to avoid inelegant contraction holes in the suppositories. * Greater MW PEG slows release rate. * PEGs tend to be more irritating to mucous membranes than fatty bases.
38
Parenteral Continuous infusion: Adv & Dis
The drug is added to a large volume of parenteral fluid, which is slowly & continuously administered into a vein Adv: * Drug plasma levels are easily controlled by adjusting the infusion rate * Constant drug plasma levels can be achieved * Less problems of irritation/toxicity Dis: * Continuous monitoring * Solubility & stability of some drugs * Fluid-restricted patients

102- Science of Medicines (6 decks)

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