Formulation and evaluation of saquinavir injection
Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar-470 003, India
N K Jain Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar-470 003 India E-mail: [email protected]
Acquired immunodeficiency syndrome (AIDS) pandemic is one of the biggest challenges of the 21st century. With the development of antiretroviral therapy, the count of human immunodeficiency virus (HIV)-infected people may decrease to a certain extent. Presently available formulations for this disease are found not to be very useful due to poor bioavailability, leading to poor efficacy, various side effects and high cost. In the present investigation, it was proposed to formulate the aqueous injection of saquinavir, which should definitely be more effective, economical, safe and with the least side effects as compared to its existing dosage forms, e.g., hard and soft gelatin capsule. The solubilization of saquinavir (antiHIV drug), practically insoluble in water, by means of physiologically active hydrotropes and cosolvents has been investigated. The results indicate that enhancement in solubility of saquinavir in the presence of hydrotrope at low concentration is due to weak ionic interaction. At higher concentrations (>0.4 M), complexation is found to be the probable mechanism for solubility enhancement by nicotinamide but nature of complex formed is not clear; whereas for ascorbic acid, self-association is the probable mechanism at these concentrations. Using these two approaches, various formulations of saquinavir were developed, and haemolysis study and dilution study of these formulations were carried out. Formulation containing nicotinamide as hydrotrope showed promising results.