Abstract

FORMULATION AND EVALUATION OF RITONAVIR β-CYCLODEXTRIN COMPLEX FOR ENHANCED DISSOLUTION

Azmina Tamkin I. Quadri Sayyeda*, Sadek Abukalam Inamdar, Sunil Firangi, Dr. Amol A. Joshi, Khan Walid Sanoon I., Rajmane Ragini B.

Abstract

Ritonavir, a widely prescribed protease inhibitor antiviral drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. It is practically insoluble in water and aqueous fluids and as such it possesses challenging problems in its formulation development. The rational of present work was to enhance the solubility and dissolution of ritonavir by inclusion complexation technology. In present study Ritonavir β-cyclodextrin inclusion complexes was prepared by varying the molar concentrations of drug to β-cyclodextrin and Hydroxy propyl β-cyclodextrin in the molar ratio 1:1, 1:2, 1:3 by Kneading method and physical method. The aim of present work was to prepare and to study the influence of β-cyclodextrin (β-CD) complex on the biopharmaceutical properties of ritonavir by evaluating ritonavir β-cyclodextrin inclusion complex for various parameters viz. FTIR, Drug content, in vitro drug release study, DSC X-ray Diffraction. The present research work concludes that the formulation F12 consisting of ritonavir-hydroxypropyl β-cyclodextrin (1:3) prepared by kneading method showed highest release of ritonavir in a short period of time.

Keywords: Ritonavir, Inclusion complex, ß-cyclodextrin, Solubility enhancement, in vitro drug release.