Abstract

FORMULATION DEVELOPMENT OPTIMIZATION AND CHARACTERIZATION OF NON-EFFERVESCENT SUSTAINED RELEASE FLOATING MATRIX TABLETS OF ATAZANAVIR SULPHATE

Someshwar Komati, Chaganti Sai Sri Rama Chandra Murthy, Donepudi Sri Charan, Sambamoorthy U.*

Abstract

The main objective of the present research was to develop sustained release floating matrix tablets of Atazanavir sulphate (ATZ). This drug has the ability to act as HIV protease inhibitor that exhibits its action by blocking the processing of viral gag-pol proteins in HIV infected cell thereby inhibiting the production of the proteins in HIV infected cell thereby inhibiting the production of the mature virions. ATZ has plasma half-life of about 6.5 hours which needs to be administered frequently for the better therapeutic efficacy. But this frequent administration results in plasma disturbances and also some side effects like cardiac conduction damage, rashes, hyper bilurubinea, nephrolithiasis, nausea, jaundice. ATZ drug shows maximum solubility at pH of acid hence necessary to deliver the drug in stomach is beneficial. ATZ tablets were developed to extend the gastric residence time and to increase drug release after oral administration by utilizing different grades of polymers like MC and HPMC K100M in-order to get the required floating and sustained release over prolonged period of time. All the steps followed in preparation of Atazanavir tablets were extended the drug release up to 24 hours and more and the formulations were optimized to meet the desired release profiles. The drug release and the floating of the drug release depends on the type of polymer and the proportion of polymer used. When the formulation developed using the combination of both the polymers showed more floating time when compared to the formulation developed with EC alone. In vivo radiography study was conducted on this combinational formulary which revealed floating property of about 8hrs. The DSC and FTIR studies showed that there is no interaction between drug and the polymer used. Besides the approach could be a potential alternative for giving information about the preparation of floating drug release system of Atazanavir without use of gas generating agent. Atazanavir is an azapeptide HIV-1 PI that prevents the formation of mature virions through the potent and selective inhibition of viral Gag and Gag–Pol polyprotein processing in HIV-1-infected cells.[1-2]

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