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Purpose: To compare pharmacokinetics and bioavailability of saquinavir (SQV) and ritonavir (RTV) and their optimized cyclodextrin complexes of anti-retro viral drugs after oral administration into rats. Methods: Rats were fasted overnight and dose equivalent to 10 mg/kg was administered orally via feeding tubes. Serial blood samples were collected, and plasma concentrations of both drugs and their complexes were determined using liquid chromatography tandem mass spectrometry, LCMS/MS. Results: After oral administration, half-life, apparent volume of distribution, total body clearance and bioavailabilities were calculated for both drugs and their optimized cyclodextrin complexes. The cyclodextrin complexes of both saquinavir (3860.93±138.50 ng.h/ml) and ritonavir (2300.19±118.21 ng.h/ml) had shown higher AUC0-∞ values compared to pure drugs, saquinavir (2293.04±82.13 ng.h/ml) and ritonavir (1636.07±162.51 ng.h/ml). Conclusion: Orally administered cyclodextrin complexes of SQV and RTV had shown higher bioavailabilities and higher peak plasma concentrations compared to SQV and RTV.

indian journal of pharmaceutical education

Comparative Single Dose Pharmacokinetics and Bioavailability Studies of Saquinavir, Ritonavir and their Optimized Cyclodextrin Complexes after Oral Administration into Rats using LC-MS/MS.