Abstract：
:A dog model was developed to test the capacity of boosters for antiretroviral medication. Two dogs were implanted with a modified constant-flow Codman 3000 infusion pump, adapted to release viscous solutions of darunavir (TMC114) at a constant rate of 25mg/dog/day in the venous blood stream. Booster candidates were given by oral gavage for at least 4 days up to maximum 7 days in cross-over fashion, separated by a wash-out period of minimum 1 week. The booster candidates were tested at doses of 20 and/or 40mg/kg/day: blood sampling for determination of the boosting effect was performed on the last day of booster administration. The model allowed to (1) compare the boosting ratio of these booster candidates based on the exposure (determination of the area under the curve (AUC) of darunavir in presence versus absence of the booster candidate), (2) detect delay in boosting activity by evaluation of the shift of Cmax of darunavir following booster administration versus the Cmax of the booster candidate) and (3) calculate the intrinsic booster capacity, by correcting for the systemic exposure of booster candidate by normalizing the booster ratio for the booster's AUC. The latter parameter (intrinsic booster capacity) allows to determine the booster's metabolic contribution in inhibiting the metabolism of antiretroviral medication (most likely via inhibition of CYP3A4), minimizing the impact of potential effects of the booster at the level of the gastro-intestinal tract.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Schueller L,Baert L,Lachau-Durand S,Borghys H,Clessens E,Van Den Mooter G,Van Gyseghem E,Jonckers TH,Van Remoortere P,Wigerinck P,Rosier Jdoi
10.1016/j.ijpharm.2007.09.025subject
Has Abstractpub_date
2008-05-01 00:00:00pages
45-52issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(07)00768-5journal_volume
355pub_type
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