Road Map 3 Immediate Release Dosage Forms Flashcards
Immediate release dosage form
designed to release drug immediately; can provide onset within 30 mins
Syrup
concentrated solution of sucrose in water
Elixir
sweetened/flavored solution that contains both water and alcohol
Binders
hold granules and tablet together
Diluents
increase size, can be chosen to improve flow
Disintegrants
draw water into the tablet to promote disintegration
Flow enhancers
prevent sticking of powders to metal parts or reduce friction (aka lubricants, glidants, antiadherents)
Sweeteners
added to help mask the taste or may also increase viscosity (added to chewable tabs and ODT)
Wetting agents
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)
Colorants
make distinctive and protect from light
Goals of designing an immediate release dosage forms
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
methods to maximize disintegration
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
methods to maximize dissolution
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
Solutions
mixture of two components that is homogenous (labeled as “oral solution”)
Suspensions
two phase system consisting of a solid dispersed phase throughout a liquid (labeled as “oral suspension USP”)
Powders for suspension
in powder form that will be suspended when the pharmacist adds water (labeled as “for oral suspension USP”)
Granules
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
IR compressed tablets
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
IR multiple compressed tablets
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)
Effervescent tablets
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
Chewable tablets
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
Rapidly disintegrating tablets
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
Sugar coated tablets
i. Coated with a colored or uncolored sugar layer
ii. Barrier to taste of drug
iii. Water soluble
iv. Bulky compared to film coats
Film coated tablets
i. Coated with a thin, elastic polymer
ii. Barrier to taste
iii. Coat ruptures which exposes the drug
Gelatin coated tablets/gelcaps
i. Capsule shaped compressed tablets coated with gelatin
ii. Smaller than a capsule filled with equivalent dose (allows for easier swallowing)
Counseling on oral liquids
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!
Counseling on IR tablets and capsules
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
Counseling on ODT
i. Preferable not to drink water with ODT (intended to disintegrate in mouth)
ii. Place on tongue until dissolved
Discuss when it is appropriate to split/crush a tablet or open a capsule
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
Hard gelatin capsules
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
Soft gelatin capsules (softgels)
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)
Suspending agents
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
Flocculating agents
added to help minimize caking; loosen the density of the sediment; produce “flocs” or loose aggregations of drug particles
Chelating agents
excipient; minimizes oxidation
Buffers
excipient; maintain pH at max stability or solubility
Antioxidants
excipient; minimizes oxidation
Preservatives
excipient; prevents microbial growth
Dyes
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
Flavors
added to mask the taste of drugs
