Bioequivalence of indinavir capsules in healthy volunteers

Open access

Background: Indinavir, one component in the HAART regimen, plays an important role in the current treatment of HIV-infection and AIDS. Availability and accessibility of qualified generic indinavir to patients may be the keys for the success of treatment. Objective: Compare the rate and extent of absorption of a generic indinavir formulation with those of an original formulation in healthy Thai volunteers. Method: A randomized, two-period, two-treatment, two-sequence, crossover study with a two-week washout period was performed. A single dose of 2×400 mg indinavir capsules of each formulation was administered to 24 volunteers after an overnight fast. Indinavir plasma concentrations up to 10 hours postdose were determined using high-performance liquid chromatography. Relevant pharmacokinetic parameters were derived and tested for statistically significant differences using ANOVA and criteria of bioequivalence determination were applied. Results: No statistically significant differences were demonstrated for pharmacokinetic parameters including Cmax, Tmax, AUC0-t, and AUC0-∞ derived from the two formulations (n=23, p>0.05). The criteria of bioequivalence determination i.e., the 90% confidence intervals on the mean ratio (generic/original formulation) of natural logarithmtransformed values of Cmax, AUC0-t and AUC0-∞ were 86.3-106.5%, 94.0-108.5%, and 93.9-108.5%, respectively. Conclusion: As the mean ratios of Cmax, AUC0-t and AUC0-∞ of the generic and original formulations were entirely within the guideline range of bioequivalence (80.0-125.0%), the two formulations were considered bioequivalent in terms of rate and extent of absorption.

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