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

  • Bharani S Sogai1Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bangalore, Karnataka, INDIA.
  • Vikram B Narayansetty1Department of Pharmaceutics, Krupanidhi College of Pharmacy, Bangalore, Karnataka, INDIA.
  • Ramana Murthy V Kolapalli2Department of Pharmaceutics, Andhra University, Visakhapatnam, Andhra Pradesh, INDIA.

Volume 52 Issue 4 Pages 587-593

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.

Keywords

  • Oral
  • LCMS/MS
  • Plasma
  • Bioavailability
IJOPP

Loading…