Road Map 3 Immediate Release Dosage Forms

Question 1

Immediate release dosage form

Answer 1

designed to release drug immediately; can provide onset within 30 mins

Question 2

Syrup

Answer 2

concentrated solution of sucrose in water

Question 3

Elixir

Answer 3

sweetened/flavored solution that contains both water and alcohol

Question 4

Binders

Answer 4

hold granules and tablet together

Question 5

Diluents

Answer 5

increase size, can be chosen to improve flow

Question 6

Disintegrants

Answer 6

draw water into the tablet to promote disintegration

Question 7

Flow enhancers

Answer 7

prevent sticking of powders to metal parts or reduce friction (aka lubricants, glidants, antiadherents)

Question 8

Sweeteners

Answer 8

added to help mask the taste or may also increase viscosity (added to chewable tabs and ODT)

Question 9

Wetting agents

Answer 9

allow hydrophobic powders to wet with water; enhance wettability of powders; important for the dissolution of solids when making solutions and the reconstitution of powders for oral suspensions; common wetting agents include cosolvents (glycerin and alcohol) and surfactants (polysorbates and sorbitan esters)

Question 10

Colorants

Answer 10

make distinctive and protect from light

Question 11

Goals of designing an immediate release dosage forms

Answer 11

a. Provide uniform dose in a manageable size (max is 1 gram in size)
b. Needs to be palatable and accepted by the patient
c. Maximum stability of the drug (chemically, physically, microbial stability)
d. Fast disintegration of the drug
e. Fast dissolution of the drug

Question 12

methods to maximize disintegration

Answer 12

i. Add a disintegrant that will expand upon contact with water to break apart the dosage form
ii. Examples of disintegrants: starch, sodium starch glycolate, crospovidone, croscarmellulose, carboxymethylcellulose, alginic acid/sodium alginate

Question 13

methods to maximize dissolution

Answer 13

i. Decrease particle size
ii. Add a wetting agent (i.e. surfactant)
iii. Improve solubility
1. Use a salt form
2. Use amorphous form rather than crystalline
3. Anhydrous vs. hydrate

Question 14

Solutions

Answer 14

mixture of two components that is homogenous (labeled as “oral solution”)

Question 15

Suspensions

Answer 15

two phase system consisting of a solid dispersed phase throughout a liquid (labeled as “oral suspension USP”)

Question 16

Powders for suspension

Answer 16

in powder form that will be suspended when the pharmacist adds water (labeled as “for oral suspension USP”)

Question 17

Granules

Answer 17

Consists of small particles or grains; can be intended to sprinkle on food, dissolve in solutions or make a suspension (some are effervescent and contain bicarbonate to aid in dissolution); can be coated to make delayed release

Question 18

IR compressed tablets

Answer 18

Mixture of drug, diluents, binders, disintegrants, and lubricants; fed into the cavity (die) of a tableting machine; compressed to remove the air and form a hard solid tablet

Question 19

IR multiple compressed tablets

Answer 19

Tablets are subjected to more than once compression step creating layered dosage forms; may separate drugs that have chemical incompatibilities; can allow for IR release of one layer and ER release of another (e.g. Ambien CR)

Question 20

Effervescent tablets

Answer 20

Designed to be dropped into glass of water before they are taken; contain ingredients that generate carbon dioxide (carbonate or bicarbonate salt / citric or tartaric acid); produce rapid disintegration and dissolution; e.g. alka-seltzer, binosto

Question 21

Chewable tablets

Answer 21

Designed to be chewed prior to being swallowed; compressed tablets made with mannitol and flavors (generally uncoated); useful for children who have trouble swallowing tablets

Question 22

Rapidly disintegrating tablets

Answer 22

Designed to be placed on the tongue and dissolve very quickly; drugs with bad taste cannot be formulated this way; used for patients that are unable to take with water due to N/V and for mental health medications; must protect from moisture

Question 23

Sugar coated tablets

Answer 23

i. Coated with a colored or uncolored sugar layer
ii. Barrier to taste of drug
iii. Water soluble
iv. Bulky compared to film coats

Question 24

Film coated tablets

Answer 24

i. Coated with a thin, elastic polymer
ii. Barrier to taste
iii. Coat ruptures which exposes the drug

Question 25

Gelatin coated tablets/gelcaps

Answer 25

i. Capsule shaped compressed tablets coated with gelatin ii. Smaller than a capsule filled with equivalent dose (allows for easier swallowing)

Question 26

Counseling on oral liquids

Answer 26

i. Show patient where the dose will measure on the dosing spoon or medication cup ii. Specify storage conditions and beyond use date iii. Suspensions: Shake well!

Question 27

Counseling on IR tablets and capsules

Answer 27

i. Take with an 8 ounce glass of water ii. Whether to chew, swallow or crush or open iii. Get the tablet completely wetted before you swallow to prevent sticking in the esophagus (pudding or yogurt can help with dysphagia iv. How often to take and how soon effects will take place: 30 mins to an hour v. Store in humidity controlled environment

Question 28

Counseling on ODT

Answer 28

i. Preferable not to drink water with ODT (intended to disintegrate in mouth) ii. Place on tongue until dissolved

Question 29

Discuss when it is appropriate to split/crush a tablet or open a capsule

Answer 29

a. Tablet splitting needed for tapering or titrating (saves money for the patient) b. Tablet crushing required for enteral feeding tubes c. Most IR tablets that are not coated can be split or crushed d. Ok to split if it contains a score e. Always use a tablet cutter f. Label sig should say “take one-half tablet” rather than “1/2” g. Information about which *capsules* can be opened can be found in package insert

Question 30

Hard gelatin capsules

Answer 30

i. Hard gelatin shell enclosing solid drug and excipients ii. Capsule shell 1. Contains: gelatin, sugar, and water (13-16%) 2. Opaquing agent like titanium oxide to exclude light iii. Capsule contents 1. Drug is diluted with a diluent (lactose, microcrystalline cellulose, starch) 2. Contents may also include disintegrants, flow enhancers, wetting agents

Question 31

Soft gelatin capsules (softgels)

Answer 31

i. Gelatin shell contains glycerin or sorbitol to soften ii. Contents are liquid and contain drug in solution or in a suspension 1. The liquid can be formulated to improve the solubility of a hydrophobic drug 2. Sometimes formulated in oil (can lead to improved bioavailability)

Question 32

Suspending agents

Answer 32

added to help produce a uniform dose that settles slowly; adds viscosity to keep the particles uniformly suspended while the patient pours out the dose; pseudoplastic liquids or “shear-thinning” vehicles are preferred

Question 33

Flocculating agents

Answer 33

added to help minimize caking; loosen the density of the sediment; produce “flocs” or loose aggregations of drug particles

Question 34

Chelating agents

Answer 34

excipient; minimizes oxidation

Question 35

Buffers

Answer 35

excipient; maintain pH at max stability or solubility

Question 36

Antioxidants

Answer 36

excipient; minimizes oxidation

Question 37

Preservatives

Answer 37

excipient; prevents microbial growth

Question 38

Dyes

Answer 38

added to match the color to the flavor; FD&C can be used in foods, drugs and cosmetics; D&C can be used in drugs and cosmetics; External D&C can only be used in externally applied drugs and cosmetics

Question 39

Flavors

Answer 39

added to mask the taste of drugs