Comparative Single Dose Pharmacokinetics and Bioavailability Studies of Saquinavir, Ritonavir and their Optimized Cyclodextrin Complexes after Oral Administration into Rats using LC-MS/MS.
1, 1, 2
- 1Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bangalore, Karnataka, INDIA.
- 2Department of Pharmaceutics, Andhra University, Visakhapatnam, Andhra Pradesh, INDIA.
CORRESPONDENCE
Bharani S Sogai
Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bangalore, Karnataka, INDIA.
Received: 23-01-2018; Accepted: 17-05-2018.
Volume 52, Issue 4 · pp. 587-593 · 2018 · DOI: 10.5530/ijper.52.4.68
ABSTRACT
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.
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Sogai, B. S., Narayansetty, V. B., & Kolapalli, R. M. V. (2018). Comparative Single Dose Pharmacokinetics and Bioavailability Studies of Saquinavir, Ritonavir and their Optimized Cyclodextrin Complexes after Oral Administration into Rats using LC-MS/MS.. Indian Journal of Pharmaceutical Education and Research, 52(4), 587-593. https://doi.org/10.5530/ijper.52.4.68
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