Create
Learn
Share

Pharmaceutics III Lect.11 Oral Modified Release Dosage Forms

rename
alchemist04's version from 2016-06-05 17:13

Section

Question Answer
3 things about Monolith/Matrix (1)(1) both 2 types are used for Sustained Release (SR) drug
3 things about Monolith/Matrix (2)(2) drug permeates and diffuse out of the matrix
3 things about Monolith/Matrix (3)(3) The matrix dissolves or erodes from outside to release the drug
memorize

 

Question Answer
One thing about Diffusional Monolith/Matrixdrug diffuse or permeate the matrix from inside and exists.
One thing about the Dissolution Monolith/MatrixThe Matrix/Monolith dissolves or erodes from outside to release the drug
memorize

 

Question Answer
3 things about Reservoir (1)(1) Could be either Delayed Release or Sustained Release
3 things about Reservoir (1)(1) It involves drug Core inside an impervious/hard shell or capsular
3 things about Reservoir (1)(1) Drug could be released by either diffusion or dissolution
memorize

 

Question Answer
One thing about Diffusional ReservoirPermeation of drug from a CORE through a membrane or impervious shell
One thing about Dissolution ReservoirErosion of an impervious shell by the drug CORE
memorize

 

Question Answer
T or F? Delayed Release is only achieved by Dissolution ReservoirTrue
T or F? Dissolution reservoir is used in Sustained ReleaseFalse, Dissolution Reservoir is used in Delayed Released drug
T or F? Diffusion Reservoir is used in Delayed ReleaseFalse, Diffusion Reservoir is used in Sustained Release drug
memorize

 

Question Answer
What are the 3 types of Oral Modified Release of Delivery System (1)(1) Oral Delayed Release Dosage Forms
What are the 3 types of Oral Modified Release of Delivery System (2)(2) Sustained Release Dosage Forms
What are the 3 types of Oral Modified Release of Delivery System (3)(3) Controlled Released or Muti-Mechanism Oral Sustained Release
memorize

 

Question Answer
What are the rationals behind Delayed Release drug? (1)(1) Protect drug from stomach
What are the rationals behind Delayed Release drug? (2)(2) Protect stomach from drug
What are the rationals behind Delayed Release drug? (3)(3) Bc majority of drugs are administered orally as tablets
What are the rationals behind Delayed Release drug? (4)(4) For Patients Convenience and Compliance
What are the rationals behind Delayed Release drug? (5)(5) To reduce SIDE EFFECTS (Controlled Release vs IR)
memorize

 

Question Answer
What are the rationals behind Delayed Release drug? (6)(6) Allow both IR @ 1st dose and follow up release @ 2nd dose from a single tablet
What are the rationals behind Delayed Release drug? (7)(7) Keeps drug from dissolving immediately (delayed release)
What are the rationals behind Delayed Release drug? (8)(8 ) Let drug dissolve after a defined time (Sustained release)
What are the rationals behind Delayed Release drug? (9)(9) Achieved by "Dissolution Release"
memorize

 

 

Question Answer
Dissolution reservoir is employed in "------------ --------------" and "------------- ----------- ----------""Coated Tablet/Capsule" and "Enteric Coated Tablet"
T or F? Release duration or time of dissolution is always longer than the dosing intervalTrue
T or F? CR, XL and HS maybe 24 hrs indicated for dosing intervals (i.e QD, daily or Once a day)True
In Sustained Release (SR) the intervals btw dosings must be ------------ by at least a factor of --------- or at ---------- timesdosings must be increased by atleast a factor of two (i.e 2x) or at multiple times (triple etc)
memorize

 

Question Answer
Rationale for Oral Sustained Release (1)(1) Improved compliance by decreasing frequency of dosing
Rationale for Oral Sustained Release (2)(2) Improved drug therapy by decreasing range in drug plasma levels and decreasing side effects
Limitation for Oral sustained release (1)(1) Not useful for drug that has half life greater than 12 hrs (or long half life)
Limitation for Oral sustained release (2)(2) drug must have high (> 50) oral bioavailability
Limitation for Oral sustained release (3)(3) drug with poor (slow) absorption can't be used
memorize

 

Question Answer
Why temporary adjustment via sustained release (1)(1) increase time of drug release and absorption
Why temporary adjustment via sustained release (2)(2) increase drug concentration to be within "therapeutic window"
Why temporary adjustment via sustained release (3)(3) changing the amount of time plasma concentration of drug is w/n therapeutic window
memorize

 

Question Answer
Reasons for pharmacokinetic adjustments of drug (1)(1) drug Libration must occur before permeation/absorption into the bloodstream can occur
Reasons for pharmacokinetics adjustment of drug (2)(2) the rate constant of DRUG RELEASE MUST BE SLOWER than the rate constant of ABSORPTION
Pharmacokinetics for IR isKabs < Kdist < Klib
Pharmacokinetics for SR isKlib < Kabs < Kdist
What is the most common type of GI Modified Oral Sustained Released tablet?(1) Non-porous insoluble (diffusion monolith) (2) Enteric Coated tablets
memorize

 

Question Answer
One thing about Controlled Released drug (1)(1) Multiple steps is required for libration that cannot be provided by monolith and reservoir
One thing about Controlled Released drug (2)(2) allow adjustment of drug duration
One thing about Controlled Released drug (3)(3) allow adjustment of rate of Release
One thing about Controlled Released drug (4)(4) Provide sustained release of drug for an arbitrarily long period (longer than 12 hrs and even days)
memorize

 

Question Answer
What are the 2 types of Multi-Mechanism Oral sustained delivery technologies(1) Controlled released (2) OROS Controlled release
Adv. of Controlled drugs (1)(1) Wide range of drug release rate possible
Adv. of Controlled drugs (2)(2) Constant Zero order is achievable
Adv. of Controlled drugs (3)(3) Constant drug plasma is achieved
Adv. of Controlled drugs (4)(4) long duration of sustained release in excess of 12 hrs (i.e more than 12 hours)
memorize

 

Question Answer
One thing about OROS (1)(1) It uses Osmotic effects
One thing about OROS (2)(2) Drug is enclosed in a perforated hard shell
One thing about OROS (3)(3) Water percolates the shell
One thing about OROS (4)(4) Drug absorbed the water and causes osmotic pressure
memorize

 

Question Answer
OROS and flow rate (1)(1) Hole diameter determines the flow rate of drug out of the shell
OROS and flow rate (2)(2) Rate of diffusion of water into the shell determines flow rate of drug out of the shell
OROS and flow rate (3)(3) Net drug release is based on diffusion reservoir in reverse (i.e the rate of water penetration + Osmotic pressure)
memorize

 

Question Answer
Adv. of OROS (1)(1) Ability to release drug independent of the GI, pH and pKa
Adv. of OROS (2)(2) Ability to maintain constant and consistent plasma drug concentration for more than 12 hrs
Adv. of OROS (3)(3) Could be designed to so that the rate of ELIMINATION is greater than the rate of RELEASE for a particular drug (this will avoid toxicity)
Adv. of OROS (4)(4) the disadvantage of diffusion reservoir can be incorporated by dissolution reservoir
Adv. of OROS (5)(5) Can provide dose that will enhance plasma concentration for more than 24 hrs.
memorize