Therapeutic Equivalence vs. Pharmaceutical Quality [Design Issues]

posted by Helmut Homepage – Vienna, Austria, 2010-02-07 18:01 (5985 d 22:08 ago) – Posting: # 4726
Views: 8,029

Dear Otto!

❝ Since M1 is the active metabolite that's mainly responsible for the efficacy of Tramadol (strong afinity to the µ-receptor) it is necessary to show BE also for M1. I would be surprised if a study without the BE for M1 would be accepted.


Well, this point of view has clearly shifted from BE seen as surrogate of Therapeutic Equivalence towards a measure of Pharmaceutical Quality (the 'human testtube'-approach) in the past years.
See the new BE-guideline (Section 4.1.5 Characteristics to be investigated / Parent compound or metabolites):

In principle, evaluation of bioequivalence should be based upon measured concentrations of the parent compound. The reason for this is that Cmax of a parent compound is usually more sensitive to detect differences between formulations in absorption rate than Cmax of a metabolite. [...]
The use of a metabolite as a surrogate for an active parent compound is not encouraged.

One exception would be an inactive pro-drug, which is not the case for tramadol.
—
Dif-tor heh smusma 🖖🏼 Довге життя Україна! [image]
Helmut Schütz
[image]

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

Complete thread:

UA Flag
Activity
 Admin contact
23,656 posts in 4,994 threads, 1,570 registered users;
295 visitors (0 registered, 295 guests [including 21 identified bots]).
Forum time: 17:10 CEST (Europe/Vienna)

Most scientists today are devoid of ideas, full of fear, intent on
producing some paltry result so that they can add to the flood
of inane papers that now constitutes “scientific progress”
in many areas.    Paul Feyerabend

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