Document Detail

Comparative bioavailability of a generic capsule formulation of the reverse transcriptase inhibitor efavirenz and the innovator product.
MedLine Citation:
PMID:  16625987     Owner:  NLM     Status:  MEDLINE    
OBJECTIVE: Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been used successfully for more than a decade to treat human immunodeficiency virus (HIV) infection. The objective of the current study was to determine the bioequivalence between a generic capsule formulation of efavirenz and the innovator product.
MATERIAL AND METHODS: A total of 41 healthy subjects (34 males and 8 females) received a single 200 mg oral dose of efavirenz as the generic (Ranbaxy-Efavirenz, Ranbaxy Laboratories Ltd.) and innovator (Sustiva, Bristol-Myers Squibb) capsule formulations under fasting conditions in a randomized, 2-way crossover study. Multiple blood samples were collected over 72 hours and plasma concentrations of efavirenz were assayed using an LC/MS/MS method. Pharmacokinetic (PK) parameters were calculated using non-compartmental methods.
RESULTS: Plasma concentrations of efavirenz peaked within 2.5 hours and then declined in a multi-exponential manner for both formulations. At 72 hours post dose, all plasma concentrations of efavirenz were above the LOQ of the assay (10 ng/ml). Mean area under the curve from 0 - 72 hours (AUC0-72) and maximum plasma concentrations (Cmax) of efavirenz for the generic capsule formulation were 22,840 ng x h/ml and 1,199 ng/ml, respectively. Ratios and 90% confidence intervals of PK parameters between the two formulations were within 80.0 - 125.0%, suggesting that the two capsule formulations resulted in similar rate and extent of bioavailability under fasting conditions. Adverse events were similar in nature and frequency for the two formulations.
CONCLUSIONS: Based on the above results, the generic capsule formulation of efavirenz developed by Ranbaxy should be as effective as the innovator product.
J F Marier; I Morin; D Al-Numani; M Stiles; G Morelli; S K Tippabhotla; T Vijan; A K Singla; M Garg; M Di Marco; T Monif
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Publication Detail:
Type:  Comparative Study; Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  International journal of clinical pharmacology and therapeutics     Volume:  44     ISSN:  0946-1965     ISO Abbreviation:  Int J Clin Pharmacol Ther     Publication Date:  2006 Apr 
Date Detail:
Created Date:  2006-04-21     Completed Date:  2006-05-03     Revised Date:  2014-02-06    
Medline Journal Info:
Nlm Unique ID:  9423309     Medline TA:  Int J Clin Pharmacol Ther     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  180-4     Citation Subset:  IM    
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MeSH Terms
Administration, Oral
Biological Availability
Cross-Over Studies
Drugs, Generic
HIV Infections / drug therapy
Middle Aged
Oxazines / administration & dosage*,  pharmacokinetics*
Reverse Transcriptase Inhibitors / administration & dosage*,  pharmacokinetics*
Reg. No./Substance:
0/Benzoxazines; 0/Capsules; 0/Drugs, Generic; 0/Oxazines; 0/Reverse Transcriptase Inhibitors; JE6H2O27P8/efavirenz

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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