Abstract

DESIGN AND DEVELOPMENT OF ORAL DISINTEGRATING TABLET OF SIMVASTATIN BY USING β-CYCLODEXTRIN

Prof. Dr. S. Z. Chemate and Wagh S. C.*

ABSTRACT

The present study deals with the design and development of oral disintegrating tablet of Simvastatin by using β-cyclodextrin with direct compression technique using various superdisintegrants like Crosprovidone, Croscaramellose sodium and Lactose and Mannitol as diluents. Simvastatin is lipid lowering agent which inhibit the 3- hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Its absolute bioavailability is 5% and coming under the class II of biopharmaceutical classification system. The rate of absorption and/or the extent of bioavailability for such a poorly soluble drug is controlled by rate of dissolution. Hence to enhance the solubility of drug a complex of Simvastatin was prepared with β-cyclodextrin in (1:1) drug: polymer molar ratio by using kneading method and this complex was compressed into tablets. The prepared tablet were evaluated for weight variation, thickness, friability, hardness, wetting time, wetting absorption ratio, disintegration time, invitro dissolution studies, stability study, phase solubility study, DSC study and IR spectroscopy. Among all the formulations, formulation F4 prepared with Crosprovidone (45%) and lactose as diluent showed 97.84% drug release within 30 min and disintegrate within 30 sec and formulation F8 prepared with Crosprovidone (45%) and mannitol as diluent showed 98.54% drug release within 30 min and disintegrate within 28 sec. No chemical interaction between the drug and the excipients was confirmed by FTIR and DSC studies. The stability study conducted as per the ICH guidelines and the formulations were found to be stable. These results revealed that oral disintegrating tablets of poorly soluble drug Simvastatin showed enhanced bioavailability and increased solubility and hence better.

Keywords: Croscaramellose sodium, Crospovidone, Oral disintegrating tablet, Simvastatin.