Authors: Tamilvanan, S.¹; Venkatesh Babu, R.²; Nappinai, A.³; Sivaramakrishnan, G.⁴

Source: Drug Development and Industrial Pharmacy, Volume 37, Number 4, April 2011 , pp. 436-445(10)

Publisher: Informa Healthcare

Abstract:

Context: Hydrophilic and hydrophobic polymer-based nicorandil (10 mg)-loaded peroral tablets were prepared using the wet granulation technique. The influence of varying amounts of hydroxypropyl methylcellulose (HPMC) (30--50 mg), ethylcellulose (2--4 mg), microcrystalline cellulose (5--20 mg) and Aerosil^®® (5--12 mg) in conjunction with the constant amounts (3 mg) of glidant and lubricant (magnesium stearate and talc) on the in vitro performances of the tablets (hardness, friability, weight variation, thickness uniformity, drug content, and drug release behavior) were investigated. Objective: The objectives of this study were (i) to select a nicorandil-loaded peroral tablet that matched the in vitro dissolution profile of once-daily commercial sustained-release tablet, and (ii) to compare the in vivo sustaining//controlling efficacy of the selected peroral tablet with that of its commercial counterparts. Results and Discussion: Because the nicorandil (10 mg)-loaded tablet prepared based on F-IX composition (50 mg HPMC, 4 mg ethylcellulose, 10 mg MCC and 3 mg glidant and lubricant) showed a release profile comparable to that of the Nikoran^®® OD SR tablet release profile, the tablet with this composition was considered to be the optimized//selected formulation and, therefore, was subjected to stability study and in vivo study in rabbits. Despite of the higher C_max and AUC values obtained with the optimized tablet, there was no sign of difference between the optimized- and Nikoran^®® OD SR- tablets following a single-dose crossover oral administration into rabbit. Conclusion: The optimized tablet could be used as an alternative to the commercial once-daily tablet.

Keywords: Ethylcellulose; in vivo bioavailability; nicorandil; peroral tablet

Document Type: Original article

DOI: http://dx.doi.org/10.3109/03639045.2010.521161

Affiliations: 1: 1Department of Pharmaceutical Technology, International Medical University (IMU) SDN BHD, Kuala Lumpur, Malaysia 2: 2Department of Pharmaceutics, Arulmigu Kalasalingam College of Pharmacy, Krishnankoil, Tamilnadu, India 3: 4Department of Pharmaceutics, C. L. Baid Metha College of pharmacy, Chennai, Tamilnadu, India 4: 3SaiMirrah Innopharm (P). Ltd., Chennai, Tamilnadu, India

Publication date: 2011-04-01

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