2 research outputs found
Evaluation of some Methods for Preparing Gliclazide β-Cyclodextrin Inclusion Complexes
Purpose: Gliclazide has been found to form inclusion complexes with
β- cyclodextrin (β-CD) in solution and in solid state. The
present study was undertaken to determine a suitable method for scaling
up gliclazide-β-CD inclusion complex formation and to evaluate the
effect of some parameters on the efficiency of complexation. Method:
The solid inclusion complexes of gliclazide and β-cyclodextrin
were prepared at a molar ratio of 1:1 and 1:2 by mixing, kneading, and
coprecipitation methods both on small and large scales. The effect of
parameters such as kneading time and temperature on complexation was
also studied. Characterization was performed using infrared
spectroscopy, X-ray diffractometry, and dissolution studies. In vitro
release studies were carried out in phosphate buffer (pH 6.8). Result:
All the methods of preparation of complexes were found to be useful in
increasing the solubility of gliclazide except mixing method where the
rise in solubility was not significant. Both kneading and
co-precipitation methods in 1:2 molar ratios were found to be equally
effective in improving the solubility of gliclazide. The formation of
inclusion complexes was evident in these formulations as shown by IR
and XRD studies. But when carried out on a large scale,
co-precipitation method was found to be more tedious and time-consuming
than kneading method. Moreover percent recovery of complexes in the
kneading method was found to be 98.76% as compared to 92.05% in case of
co-precipitation method. Conclusion: Drug content studies, IR
spectroscopic studies, X-Ray diffractometry studies and in vitro
dissolution study data indicated that inclusion complexes prepared by
kneading method in 1:2 molar ratios were suitable for improving the
solubility of gliclazide. The same formulation was prepared at large
scale and optimum formulation conditions were established