BIO-AVAILABILITY 

 

 


Arrange different dosage forms with deceased bio-availability :

 

Solution > suspention >capsule >tablet >coated tablet

 

* at process of abs. Drug should be in molecular form

*soln :drug in molecular form :abs immediately.

 

*in susp: very small fraction in molecular ,the rest is suspended.

*in capsule (solid drug + inert diluent ) enclosed in a shell made of gelatin-sucrose mix.

#the more steps added to dosage form u expect more difficulty.

*in tablet :should disintegrate first into granules then to drug / soln (add more obstacle ,takes time for drug to be dissolved and be in molecular form.

# there is equilibrium , when drug in soln abs. , shift the drug in solid form to compensate another fraction.

#tablet is the most commom (stable solid ,covered by coat ,transported easily ,easy handle ,economic )

#adjust wt of tablet >const supply of punsh determined by tablet machine >const dose

#u should add disintegrant with granules to abs water from GIT eg starch.

#moistening of pw to make daw > sieve >granules by (starch mu ,gum mu ,sucrose serum which are viscous)

#drying at RT or in vacuum oven

 so tablets contain many additives & many steps

#compression force should be calc otherwise tablet will become as a piece of cement and will overcome the propertue of disint. And pass through GIT without abs.

Due to

1-to much binder

2-high compression

3-poor quality disint.

4-insufficient disint

#some times add colouer sub. For attracrion (certified dye by pharmacopeai)

 

*coated tablet ,coat could be sugar (sucrose serum ) or polymer >thin film around tablet

#film should be proper >as it may abs water and deteriorate the drug.

 

 

 

THE RELATIONSHIP BETWEEN BLOOD CONC& PHARMACOLOGICAL EFFCT :

*AT ZERO TIME OF TAKEN DRUG ORALLY (BY ANY ROUTE EXCEPT IV) durg in blood = zero till mini,um effective conc

increase time  increase drug conc in blood  then decrease drug conc as dose is consumed (completely abs)

*once the dru enter the bl. (dynamic mov) >excreation & metab.

Process of metabolism starts  as soom as drug in blood

*any stepat which drug is subjected is kinetic (1st order)

bell shaped curves

 

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