Oral Controlled Release PDF

ORAL CONTROLLED RELEASE Hamid Omidian 2024  Terminology ✓Modified release 1940s and early 1950s Dosage forms having drug-release features based on time (when), path (How), and location (Where) ✓ Extended...

ORAL CONTROLLED RELEASE Hamid Omidian 2024  Terminology ✓Modified release 1940s and early 1950s Dosage forms having drug-release features based on time (when), path (How), and location (Where) ✓ Extended or sustained release (SR) ✓Extended release Allows a reduction in dosing frequency Later ✓Delayed release ✓ Sustained Release (SR) Allows drug release after a lag period ✓ Sustained Action (SA) ✓Repeat action ✓ Prolonged Action (PA) Allows immediate and delayed release of a same ✓ Controlled Release (CR) medication (e.g., bilayer tablets) ✓ Extended Release (ER) ✓Targeted release ✓ Timed Release (TR) Allows drug release at a certain tissue or site in the body ✓ Long Acting (LA) Ansel’s Chapter 9 Conventional versus Controlled Release ✓ Patient inconvenience o 3-4 times administrations a day o Dosing at night-time o Inconvenient to both patients and care-givers ✓ Dosing errors o Fluctuation in drug plasma concentrations o Missed doses (subtherapeutic) o Made-up doses (toxic), severe adverse effects ✓ Patient noncompliance ✓ Drug won’t work as expected Ansel’s Chapter 9 Conventional versus Controlled Release Advantages ✓ Maintain desirable drug blood levels ✓ Minimize number of dosing ✓ Enhance convenience and compliance ✓ Minimize adverse drug side effects ✓ Reduce healthcare costs Disadvantages ✓ Loss of flexibility in adjusting the dose ✓ Risk of sudden and total drug release, dose dumping ✓ Due to abuse or misuse ✓ Due to product failure Ansel’s Chapter 9 Drug Candidates in Extended Release ✓ Should have neither very slow nor very fast rates of absorption and excretion: o Drugs with long half-lives (> 8 hr.) are inherently long-acting, no need for extended release. o Drugs with very short half-lives (