Exam 3 Flashcards
Why do we need a pharmaceutical carrier?
protect drug from the body
protect body from the drug
Adjust PK, distribution and clearance
Biopharmaceutic Factors in Drug products
Stomach (Food effects)
Small intestine and Transit time (~3h)
Colonic transit (10-20hr)
Large Intestine
Adv Sustained Drug Delivery Tech
Infusion Oral Topical Inhalation Injection Percutaneous Implantation
Advantages of ER/Sustained release products
Sustained therapeutic blood lvls of drug
Improved pt compliance
Reduction in adverse effects and improved tolerability
Reduction in HC costs
Disadvantages of ER products
Dose-dumping
Less flexibility in accurate dose adjustment
less possibility for high dosage
ER drug product definition
dosage form that allows at least a 2fold reduction in dosage frequency as compared to that drug presented as an immediate release dosage form
Delayed release drug product definition
Dosage form that releases a discrete portion/portions of drug at a time other than the promptly release after admin
Targeted release drug products definition
dosage form tat release drug at or near the intended physiological site of action
ODTs definiton
disintegrate rapidly in saliva after oral admin
used without water dispersed in saliva
Enteric coated definiton
type of delayed release designed to release drug in small intestine
Prolonged-action drug product
formulation whose drug activity can continue for a longer time than conventional drugs
Sustained-release drug product
designed to release a drug at predetermined rate for the constant drug conc maintaining during specific period of time
ideal ER drug product
release drug at constant rate
independent of pH, ionic content, other contents within GI tract
Amount of drug needed in sustained-release product to maintain therapeutic drug conc is dependent on both….
Vd and Elim 1/2 life
Five Types of Matrix Tablets
- Hydrophobic matrix (plastic)
- lipid matrix
- hydrophilic matrix
- biodegradable matrix
- mineral matrix
How can matrix be classified?
by porosity situation and also by usage frequency
Ion exchange products
insoluble drug complex containing the resin and drug dissociates in the GI tract in the presence of appropriate counter ions
drug dissolves in GI tract and is rapidly absorbed
Resin needed for anionic drugs?
positively charged
Resin needed for cationic drugs
Negatively charged
Core tablet
Core tablet within a tablet
Inner core suavely slow-release and outer shell is rapid release
Microencapsultion
process of encapsulating microscopic drug particles with a special caution material, making the drug particles more desirable in terms of physical and chemical characteristics
2 Important requirements in development of ER products are….
demonstration of safety and efficacy
demonstration of controlled drug release
Evaluation of modified released products
Dissolution studies
In vitro - In vivo correlations
PK studies
Clinical considerations of modified release drug products
Generic substitution of modified release drug products
Evaluation of invivo bioavailability data
PK profile Steady-state plasma drug conc Rate of drug absorption Occupancy time Bioequiv studies Statistical eval
