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Published on:June 2018
Indian Journal of Pharmaceutical Education and Research, 2018; 52(4):587-593
Original Article | doi:10.5530/ijper.52.4.68

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


Authors and affiliation (s):

Bharani S Sogai, Vikram B Narayansetty, Ramana Murthy V Kolapalli

1Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bangalore, Karnataka, INDIA.

2Department of Pharmaceutics, Andhra University, Visakhapatnam, Andhra Pradesh, INDIA.

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.

Key words: Oral, LCMS/MS, Plasma, Bioavailability.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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