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.
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