AAPS PharmSciTech

, Volume 11, Issue 2, pp 518–527

Solid Dispersion as an Approach for Bioavailability Enhancement of Poorly Water-Soluble Drug Ritonavir

Authors

  • Shilpi Sinha
    • Department of Analytical Research DevelopmentJubilant Organosys
  • Mushir Ali
    • Department of Pharmaceutics, Faculty of PharmacyHamdard University
  • Sanjula Baboota
    • Department of Pharmaceutics, Faculty of PharmacyHamdard University
  • Alka Ahuja
    • Department of Pharmaceutics, Faculty of PharmacyHamdard University
  • Anil Kumar
    • Department of Pharmaceutics, Faculty of PharmacyHamdard University
    • Department of Pharmaceutics, Faculty of PharmacyHamdard University
Research Article

DOI: 10.1208/s12249-010-9404-1

Cite this article as:
Sinha, S., Ali, M., Baboota, S. et al. AAPS PharmSciTech (2010) 11: 518. doi:10.1208/s12249-010-9404-1

Abstract

Ritonavir is an antiretroviral drug characterized by low solubility and high permeability which corresponds to BCS class II drug. The purpose of the study was to develop solid dispersion by different methods and investigate them for in vitro and in vivo performance for enhancing dissolution and bioavailability, respectively. Since the drug possesses food-related absorption, the effect of biorelevant media (FaSSIF and FeSSIF state) on dissolution behavior was also studied. The solid dispersion was prepared using Gelucire as carrier in 1:4 ratio by different methods and were characterized for differential scanning calorimetry (DSC), X-ray diffractometry, scanning electron microscopy, and FT-IR. Oral bioavailability of 10 mg of ritonavir in solid dispersion prepared by solvent evaporation (SE1) and melt method (MM1) was compared with pure drug after oral administration of solid dispersion and pure drug to Albino Wistar rats of either sex. The results suggested formation of eutectic solid dispersion. In vitro dissolution studies was performed in 0.1 N HCl and biorelevant media showed enhanced dissolution rate as compared to pure drug in both FeSSIF media and 0.1 N HCl. The apparent rate of absorption of ritonavir from SE1 (C max 20221.37 ng/ml, t max 0.5 h) was higher than that of MM1 (C max 2,462.2, t max 1 h) and pure drug (C max 1,354.8 ng/ml, t max 0.5 h). On the basis of the result obtained, it was concluded that solid dispersion is a good approach to enhance solubility and bioavailability of poorly water-soluble ritonavir.

Key words

bioavailability gelucire poorly soluble drug ritonavir solid dispersion

Copyright information

© American Association of Pharmaceutical Scientists 2010