Racemate vs. enantiomer? [Regulatives / Guidelines]

posted by Helmut Homepage – Vienna, Austria, 2018-01-17 14:40 (1347 d 14:50 ago) – Posting: # 18190
Views: 2,707

Hi Christian,

» A Clinical study is going to be with an enantiomer (not racemate).

Are you talking about bioequivalence?

» The enantiomers exhibit different pharmacodynamic characteristics but only the active enantiomer is going to be in the formulation.
» There is no in-vivo interconversion.
» The reference standard is going to be the enantiomer (not racemate).

» Is a chiral method required? Can I go with a simple achiral method?

Which regulation? F.i. the FDA’s requirements concerning chiral methods are diametral to the EMA’s (see also here and there). Can’t find anything in the Mexican one.
One of the prerequisites in BE is that same molar doses of the active ingredient are administered. If the enantiomeric ratio* of the reference is 1:1, IMHO, you would have to administer twice the dose of the test and use a chiral method (assessing only the active enantiomer for BE).

Other opinions are welcome.



Dif-tor heh smusma 🖖
Helmut Schütz
[image]

The quality of responses received is directly proportional to the quality of the question asked. 🚮
Science Quotes

Complete thread:

Activity
 Admin contact
21,699 posts in 4,537 threads, 1,542 registered users;
online 4 (0 registered, 4 guests [including 2 identified bots]).
Forum time: Sunday 06:30 CEST (Europe/Vienna)

A central lesson of science is that to understand complex issues
(or even simple ones), we must try to free our minds of dogma and
to guarantee the freedom to publish, to contradict, and to experiment.
Arguments from authority are unacceptable.    Carl Sagan

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