Preparation, characterization and evaluation of efavirenz inclusion complexes by employing b-cyclodextrin
Journal Title: Journal of Pharmacy Research - Year 2011, Vol 4, Issue 10
Abstract
Efavirenz (EFA) belongs to the class of non nucleoside reverse transcriptase (RT) inhibitors and is indicated in the treatment of HIV infection. Efavirenz is practically insoluble in water having lowest solubility of about 0.01 mg/mL. The objective of the work is to formulate and evaluate inclusion complexes of efavirenz by using ß-cyclodextrin (ßCD) for enhancing the solubility. Phase solubility studies were carried out to evaluate the solubilizing power of cyclodextrin (CD) and to determine the apparent stability constant (k s ) of the complexes. Inclusion complexes were prepared by four methods namely (i) physical mixing (PM) (ii) co evaporation method (CE) (iii) kneading method (KNE) and (iv) freeze drying method (FD). In each case two different proportions of drug and ßCD such as 1:1 and 1:2M ratios were used in the preparation of Inclusion complexes. Characterization of Inclusion complexes was done by means drug content uniformity, Fourier transmitted infrared (FTIR) spectroscopy, differential scanning calorimetry(DSC), powder x-ray diffractometry (X-RD), scanning electron microscopy (SEM) and in vitro dissolution studies. The order of increase in dissolution rate of the drug with different methods were found to be FD > KNE > CE >PM.
Authors and Affiliations
Rama Rao Nadendla*, Yamini Purna Bol lu, Jyothi rmai Val lur i and Manasa Chagant i .
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