poorly soluble drugs Flashcards
Why are special formulation methods used for poorly soluble drugs?
- Increased Absorption and Bioavailability
- Overcoming Physiological Barriers
- Consistent Therapeutic Effect:
How does reducing particle size help poorly soluble drugs?
Smaller particles increase the surface area, improving drug dissolution and absorption.
How does esterification affect the bioavailability of a drug, eg phentytoin?
It creates a prodrug form that improved its absorption, as well as its stability and controlled release.
How does esterification affect the bioavailability of hydrophobic drugs like phenytoin?
Esterification can improve bioavailability by converting the drug into a more soluble prodrug, which is later hydrolyzed in the body to release the active drug.
What are the benefits of using carboxymethyl-β-cyclodextrin in drug formulations?
Cyclodextrin complexation improves chemical stability, taste, and bioavailability of drugs like famotidine by enhancing their solubility.
briefly explain the cyclodextrin structure
has a hydrophobic inner centre and and a hydrophilic outer surface.
does the solubility of a drug proportionally improve dependent on cyclodextrin concentration or does it gradually decline?
proportionally improves
what could be a disadvantage of using cyclodextrin?
very expensive
explain the cogrinding technique
- physical mixing and grinding where a drug and exipient are ground together. this reduces particle size and breaks down any crystalline structure.
What advantage does a nanomatrix system of colloidal silica and pH-sensitive polymethylacrylate offer?
It improves the bioavailability of drugs like fenofibrate by providing a controlled release that optimizes dissolution at different pH levels in the GI tract.
Why isn’t there a single solution for all poorly soluble drugs?
Different drugs have unique properties, requiring specific techniques tailored to each drug’s solubility and stability challenges.
