TITLE

FORMULATION DEVELOPMENT AND IN VIVO EVALUATION OF EFAVIRENZ SOLID DISPERSIONS

AUTHOR(S)
Kiran Kumar, V.; Aruna devi, M.; Bhikshapathi, D. V. R. N.
PUB. DATE
November 2012
SOURCE
International Journal of Pharmaceutical Sciences Review & Resear;Nov/Dec2012, Vol. 17 Issue 1, p97
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
The applicability of the solid dispersion technique as a method for enhancing the GI absorption of a drug has been explored in order to achieve better dissolution characteristics and better bioavailability for poorly soluble drugs. Efavirenz is an antiretroviral agent often demonstrates poor gastrointestinal absorption due to inadequate drug solubility in GI fluids. The objective of the present study is to formulate and characterize free flowing efavirenz solid dispersions by short term heating and rapid drying (solvent-melt method) with polyvinyl pyrrolidone and adsorbent Neusilin as anti sticking agent. The release rate of Efavirenz from the resulting complexes was determined from dissolution studies and dissolution characteristics were carried out for solid dispersion formulations, pure drug and physical mixtures. The results indicated that dissolution of optimized formulation (FSD2) showed significantly higher than pure drug and physical mixtures. X-ray diffraction studies of optimized formulation showed no physicochemical interaction. DSC studies revealed that absence of drug peak in the free flowing solid dispersion formulation indicating the drug was in amorphous form. The comparison of in vivo bioavailability studies of optimized formulation and that of a pure drug as reference standard in Wistar rats confirmed that the higher amount of drug concentration in blood indicated better systemic absorption and bioavailability also found to be increased with optimized formulation.
ACCESSION #
87366820

 

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