Pharmacologicsl Factors Affecting Drug Bioavailability- Dose Calculations Flashcards
Principle stages in tablet formation
Drug+excipient-> mixing -> add granulation liquid and binder-> wet granulation-> drying-> lubricant and extragranular disintegratation-> mixing-> compression-> coating
Typical ingredients
Therapeutic agent
Diluent-> main tablet bulk-> lactose, sorbitol
Compression aid-> aids tablet formation-> cellulose
Binder-> binds powders into granules
Glidant-> powder flows into tablet machine
Lubricant-> tablet ejection from dye
Disintegrant-> swells/disrupts tablet on contact with body fluids
Coatings-> organoleptic modification-> enteric/sustained release
Bioequivilance
Identical rate and extent of absorption Assessed by tMax-> time to peak plasma level lMax-> peak plasma level And bioavailability
Acid labile formulations
Enteric coated tablets Non cellulose derivative polymers used Methacyclic acid components-> acid functional group -> pKa 4.66 Omeprazole
Transdermal formulations
Patches
Sustained drug delivery-> longer duration of action
Enhancers such as ethanol improve skin penetration
GTA for angina
Nicotine
Subcutaneous formulations
Control of absorption of insulin from site of injection achieved by differences in physical state of insulin
-> in zine or protein content
-> in pH of suspending buffer
Short acting-> soluble-> rapid onset,short duration
Intermediate-> suspension with procaine-> twice daily
Long acting-> large crystals, high zinc content
I.M formulations
Absorption by use of thick oils that slow diffusion rate
Norethisterine enatate
Percentage solution drug expression
Means grams per 100ml of solution
100%-> 100g per 100ml
1% -> 10mg/ml
Ratios
1: 1000-> 1mg/ml
1: 20,000-> 5mg/ml
Units
A measure of biological activity
Specific to each drug