Once-daily sustained-release matrix tablets of nicorandil: Formulation and in vitro evaluation |
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Authors: | K Raghuram Reddy Srinivas Mutalik Srinivas Reddy |
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Institution: | (1) College of Pharmaceutical Sciences, 576119 Manipal, Karnataka, India |
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Abstract: | The objective of the present study was to develop once-daily sustained-release matrix tablets of nicorandil, a novel potassium
channel opener used in cardiovascular diseases. The tablets were prepared by the wet granulation method. Ethanolic solutions
of ethylcellulose (EC), Eudragit RL-100, Eudragit RS-100, and polyvinylpyrrolidone were used as granulating agents along with
hydrophilic matrix materials like hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose, and sodium alginate.
The granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The
tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, and in vitro release
studies. The granules showed satisfactory flow properties, compressibility, and drug content. All the tablet formulations
showed acceptable pharmacotechnical properties and complied with in-house specifications for tested parameters. According
to the theoretical release profile calculation, a oncedaily sustained-release formulation should release 5.92 mg of nicorandil
in 1 hour, like conventional tablets, and 3.21 mg per hour up to 24 hours. The results of dissolution studies indicated that
formulation F-I (drug-to-HPMC, 1∶4; ethanol as granulating agent) could extend the drug release up to 24 hours. In the further
formulation development process, F-IX (drug-to-HPMC, 1∶4; EC 4% wt/vol as granulating agent), the most successful formulation
of the study, exhibited satisfactory drug release in the initial hours, and the total release pattern was very close to the
theoretical release profile. All the formulations (except F-IX) exhibited diffusion-dominated drug release. The mechanism
of drug release from F-IX was diffusion coupled with erosion. |
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Keywords: | nicorandil hydroxypropyl methylcellulose ethylcellulose sustained release matrix tablets |
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