Abstract

DEVELOPMENT AND IN VITRO EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF NICORANDIL

Paikra C. P. S.*, Ojha Sunil, Dr. Agrawal Amit, Mishra T. S.

ABSTRACT

Nicorandil is a drug of choice in the treatment of Angina Pectoris. Though it is a potent drug, it suffers from drawbacks like short half-life (1hr), high water solubility and good permeability. In this study Different matrix tablet formulations prepared by using wet granulation method (Eudragit RLPO, HPMC K4M) were used as a matrixing polymer. PVP K30 is used as a dry binder to give proper binding property to tablets. Lactose was used as a diluent. Results of preformulation study revealed that majority of the excipients which are going to be used in formulation development were found to be compatible with Nicorandil and give good binding and flow property. Directly compressible sustained-release (SR) Nicorandil tablet formulations of different concentration of Eudragit RLPO was used but tablet of eudragit alone was seems to rupture within 3-4 hrs so HPMC K4M was combined with it which gave proper binding property. Tablet of this combination of polymers gave extended release upto 22-24 hrs. So Eudragit RLPO and HPMC K4M selected as a polymers of choice for formulation development. It was demonstrated that the release of Nicorandil from matrix tablets can be modified by changing the type and amount of polymer in the matrix tablets. A comparison between experimental data (observed value) and theoretical data (predicted value) was performed and there was no significant difference. Mathematical modeling of Best batch indicate Weibull model showed the least value of sum of square of residuals (SSR) and F value. Thus, it may be concluded that drug release from batch can best explained by the Weibull model. So the sustained release formulation for Nicorandil was developed which was able to release the drug in controlled manner up to 24hrs. The drug remains within the effective concentration (therapeutic window) throughout the day without the subsequent dosing. The developed formulation also complied with the all In-vitro characterization parameters. Though, further In Vivo studies are needed for the assurance of clinical efficacy of the formulation.

Keywords: Nicorandil, Eudragit RLPO, HPMC K4M, PVP K30, Directly compressible sustained-release (DCSR).