PDD Exam 2

Immediate release (IR)

— — there is nothing in the drug formulation designed to modify, extend or delay the drug release

Modified release (MR)

— —umbrella category for dosage forms that intentionally delay or modify release of the drug from the dosage form in some way

extended release (ER)

— — this is a formulation designed to allow a drug to be released over an extended amount of time typically to lessen the number of pills that need to be taken in a day to maintain continued plasma levels of the drug

Delayed release

— — the drug is designed not to release after taking it, but drug release begins some time frame significantly after the drug it taken, there is a lag period prior to release

fluctuations

MR pills allow for a decrease in drug dosage — that would typically occur if a patient had to take multiple drugs a day rather than one

Matrix, disintegrants

— system: MR system where the active ingredient is embedded in a matrix of material that slows the release of the drug; — are typically not added to these formulations because it would speed up dissolution

hydrophobic, plastic, hydrophilic

what are the 3 primary types of matrix systems?

slow, into

hydrophobic matrix tablets are typically fatty or waxy and help to — down the diffusion of water — the tablet → causes a much slower rate of tablet dissolution

Carnauba wax, stearyl alcohol, cetyl alcohol, cetostearyl alcohol, glyceryl monostearate

common hydrophobic matrices: (5 two words each)

spray-congealed

— —: used in preparing a hydrophobic matrix tablet by spraying the liquid matrix and then cooling the droplets immediately to congeal them into solid particles that can then be compressed into tablets

inert plastic, organic solvent, evaporated

plastic matrix formulations have the active ingredient encased in an — — matrix; drug formulations are developed by first combining the drug powder with a plastic powder which can then either be wetted for granulation with a small amount of — — OR the plastic and drug powder can be dissolved in more organic solvent and — until a wet mass is achieved for granulation

before

with plastic matrix tablets, demixing is possible UNLESS the drug powder is granulated — mixing with the plastic powder particles

indigestible, polymers, gel

hydrophilic matrix tablets are made up of — hydrophilic — that swell to form a — layer around the entire surface of the tablet which then delays release of the drug

gastric fluid

hydrophilic matrix tablets absorb water from the — — after ingestion and forms the gel layer which slows water emptying the tablet and releasing and dissolving the drug

lactose

for hydrophilic matrix tablets, combining the polymer with — can help to reduce the polymer concentration and increase the rate of drug release

binder

hydrophilic matrix tablets can be formed using the wet granulation method, but you will need a — with enough strength to form the granules

coated

— systems rely on a coating covering the surface of the dosage form

imperfections, color

non-MR coatings may be used for aesthetics, to cover —, taste masking or to add —

slow

MR coatings — the penetration of water into the interior of the dosage form

soluble, pores

coatings are typically formulated from insoluble materials combined with a small amount of — material, the (prev) material can then readily dissolve and form — allowing water to enter and push the drug out of the coating

matrix

coatings are usually used in a — system with smaller particles rather than over an entire tablet

ethylcellulose powder, aqueous EC dispersion, cellulose acetate dispersion, methacrylic-acrylic acid copolymer

common MR coating materials: (4)

short absorption window

— —- — drugs that only have a very small segment of the GIT where they are readily absorbed

gastro-retentive, stomach, acidic

— — forms are drugs that are designed to stay in the stomach longer than typical, they are useful for drugs that are designed to act in the — or forms that are more easily soluble in — gastric fluid

floating, bio-adhesive, swellable, high density

4 types of gastro-retentive forms:

gastric fluid, water

floating systems work by floating on top of the — — to keep it from passing into the small intestine during gastric emptying, patients may be advised to drink —to keep fluid levels in the stomach during the dosage lifespan

gas-forming

floating systems typically use — — ingredients to allow them to float

hydroxypropyl methylcellulose

floating systems use a swellable polymer (ex — — ) that forms CO2 gas using an effervescent mixture creating a floating gel

effervescent

sodium carbonate or bicarbonate + citric acid/tartaric acid are used to form the — mixture in floating systems that then forms CO2

fluid

key limitation of floating system is the need to keep adequate — levels to keep the floating system in the stomach and it cannot be used while sleeping

bio-adhesive

— — systems are designed to adhere to the stomach wall and are commonly used for matrix tablets

non-adhesive, mucus

bio-adhesive systems have a thin — — coating over the top to prevent adhesion in the mouth or throat, it dissolves in the stomach, these systems adhere to the stomach — so (prev) turnover can help prevent prolonged adhesion

swellable

— systems swell in the presence of aqueous fluid into a large size or shape that prevents it from being moved into the small intestine

high density

— — systems contain a very dense ingredient that raises the density of the dosage form as a whole allowing it to sink below the pyloric valve

bismuth subnitrate, barium sulfate, ferrous oxide, titanium dioxide, zinc oxide

commonly used dense excipients: (5)

osmotic

— systems have an inner core or reservoir of drug and then use osmotic agent to pump a drug solution out of the tablet

osmogens

osmotic agents that use osmotic pressure to pump a drug solution out of the tablet, also called osmotic pumps

out, delivery port

osmotic systems have an inner core of drug surrounded by a semi-permeable membrane that allows water in, but does not allow drug —, the drug expands due to water intake creating pressure → drug is then pushed out through a — —

pH

one of the major advantages of the osmotic pump is that their drug release is driven by osmotic pressure rather than — or dynamics of the solvent

elementary osmotic, cellulose acetate, rate

in — — pumps, a tablet is coated with — — and a hole is drilled or cut and the interior is filled with a drug or osmogen, water enters and forms a saturated solution generating pressure that pushes the solution out the tablet at a nearly constant —

push-pull, polymeric

— -- osmotic pumps, unlike elementary pumps, do not need to use water soluble drugs, it has layers where the top has the drug and the osmotic agent and the bottom has a — push compartment that will push out the drug

pulsatile

— drug delivery systems allow drug to be released followed by a lag of drug release followed by another round of drug release creating pulses

GIT, customizable

pulsatile systems can be used to allow drug to be released in different parts of the — or to allow drug to be released at different times, it allows for — drug release schedule

chronotherapy

scheduling drug therapies in coordination with a patients circadian rythm

orally

colonic drugs are given — an release is delayed until the colon

pectin, guar gum, chitoan

colonic drugs are typically coated with polysaccharides such as —, — —, or — that can only be broken down by bacteria in the colon