What is the role of caffeine in bioequivalence studies? [Dissolution / BCS / IVIVC]

posted by Relaxation  – Germany, 2016-05-18 20:08 (3192 d 11:31 ago) – Posting: # 16328
Views: 6,432

❝ Hello for all!


❝ I would like to confirm an information with experts in BCS....


❝ Best regards.


Hello Mauricio.

I am not saying that I am an expert, but I have an opinion. I am also not quite sure that I got your point, so please do not hesitate to point to my misunderstandings.

I cannot check at the moment, whether caffeine is part of the list of reference standards for permeability experiments, but this could be and I think it is (highly permeable). You can find this list in the FDA-GfI "Waiver of In Vivo Bioavailability and Bioequivalence Studies...". Please note that there is a new version (including BCS-III and I am not quite sure that the title is the same (copy at home)).

However, permeability is nice but not the most important issue in discussing BCS. These are actually solubility and abs. bioavailability.
Just by looking at the first Google match for Caffeine solubility and bioavailability I would say, that solubility is 16 mg/mL at room temperature (increasing with temperature), that is at least 4 g are soluble in 250mL, which should be sufficient for those products I am aware of.
And Blenchard et al. published 1983 that abs. BA is 108.3% in N=6. Hm, admittedly there should be better publications on this, but looks like complete absorption to me.

There you go. BCS-class I. In case some other requirements are fulfilled ... no need for BE for IR products.

Best regards,

Steven

P.S.: to avoid a misunderstanding, the solubility i refer to is in water. That would not be sufficient for a discussion of BCS, but considering the amount and that this is caffeine I would not expect to see the solubility to drop too low over the relevant pH.

Complete thread:

UA Flag
Activity
 Admin contact
23,380 posts in 4,914 threads, 1,661 registered users;
33 visitors (0 registered, 33 guests [including 4 identified bots]).
Forum time: 06:40 CET (Europe/Vienna)

Everything is trivial, if you know the answer.    Thomas Jaki

The Bioequivalence and Bioavailability Forum is hosted by
BEBAC Ing. Helmut Schütz
HTML5