increased solubility = different PK profile? [Dissolution / BCS / IVIVC]

posted by Ohlbe – France, 2017-06-08 20:23 (2512 d 00:10 ago) – Posting: # 17469
Views: 14,071

Dear Dr Dan,

❝ The idea behind this question is to develop an oral formulation with a less drug load than the reference product but with the same bioavailability in order to decrease non-systemic adverse events.


There is one (old) example I can think of: fenofibrate. Very low solubility. Started with a 300 mg capsule formulation. Decreased to 200 mg with an improved formulation (if I remember correctly, co-micronisation with sodium laurylsulfate). Decreased further with new formulation improvements: 160 mg and now 145 mg tablets.

I don't know through which type of procedure they were approved, whether BE was demonstrated on both Cmax and AUC, and whether they did any clinical trials in addition to BE. But it may be worth having a look at public assessment reports, if available.
—
Regards
Ohlbe

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