Formulation and evaluation of S-(-)-Amlodipine besylate and nebivolol hydrochloride tablets

• Main Authors: S A Shaikh, S S Shaikh, S R Shahi, M A Shookur, L K Reddy, A N Padalkar, Mahesh Thube
• Format: Article
• Language: English
• Published: Wolters Kluwer Medknow Publications 2010-01-01
• Series: Journal of Advanced Pharmaceutical Technology & Research
• Subjects: Tablet; S-(-) - amlodipine besylate; nebivolol hydrochloride; combination therapy; dissolution; wet granulation
• Online Access: http://www.japtr.org/article.asp?issn=2231-4040;year=2010;volume=1;issue=2;spage=199;epage=206;aulast=Shaikh

The objective of the present study was to develop a tablet formulation of S-(-)-amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-)- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity. The study was also carried out to design a suitable dissolution medium for S-(-) - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(-) - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(-) - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.