Design and development of controlled release floating matrix tablet of Nicorandil using hydrophilic cellulose and pH-independent acrylic polymer: in-vitro and in-vivo evaluations

Abstract

Objectives: The purpose of the study was to develop a floating matrix tablet of Nicorandil using blends of hydrophilic cellulose and pH-independent acrylic polymer to improve the therapeutic effectiveness of the drug in cardiovascular disease.

Methods: Nicorandil tablets were prepared by direct compression and evaluated for drug-excipients compatibility, in-vitro buoyancy and in-vivo γ-scintigraphy study. The selected formulation (FT5) was also evaluated for stability study and the in-vivo absorption in rabbits to compare the pharmacokinetic parameters with the commercially available immediate release tablet of Nicorandil.

Results: DSC and FT-IR studies confirmed the absence of incompatibility and were found stable at refrigerator temperature (2-8°C) and at 25ºC/60% RH. The in-vivo γ-scintigraphy studies revealed that the system was floated for a period of 6 -7 h in the stomach and in-vivo absorption study showed a significant difference (p < 0.05) in the pharmacokinetic parameters (AUC increased by 3 fold and MRT by 2.5 fold) as compared to the marketed formulation.

Conclusion: In conclusion, the developed Nicorandil floating matrix tablet improved the pharmacokinetics parameters (AUC and MRT) in rabbit plasma with expected lowering in side effects potential.

Keywords:

• direct compression
• compatibility
• buoyancy
• in-vivo γ-scintigraphy
• in-vivo absorption

Disclosure statement

No potential conflict of interest was reported by the authors.

Acknowledgement

The authors would like to thank Dr. Aseem Bhattnagar, Department of Nuclear Medicine, Institute of Nuclear Medicine and Allied Sciences (INMAS), Delhi-110054 for providing the facilities and Mr. Raisuddin Ali, Senior Research Fellow of INMAS for successfully carried out the in-vivo gamma scintigraphy study.