Absorption important [Design Issues]

posted by Helmut Homepage – Vienna, Austria, 2010-04-14 21:38 (5920 d 04:58 ago) – Posting: # 5141
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Dear Heema,

❝ [...] overall extent of absorption is of importance for such NTIs.


No, in BE we are interested in the difference of absorption between formulations. Elimination is specific for the drug. After 2-4× tmax the AUC-ratio does not change any more, only variability increases (just saw Kamal Midha walking 'round the corner ;-)). In other words AUC72(T)/AUC72(R) ~ AUC504(T)/AUC504(R) ~ AUCinf(T)/AUCinf(R), but AUC's CVintra,72<CVintra,504<CVintra,inf. Please search the forum for examples and references.

Above said is only true for immediate relase formulations (elimination = slowest phase). For some MR formulations (CR, but not DR) the slowest phase is absorption - the one we are interested in: in such a case truncation does not make sense. Luckily there are only a few stupid controlled release formulations of drug with a long half-life on the market.

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