FORMULATION AND EVALUATION OF S-(-)-AMLODIPINE BESYLATE AND NEBIVOLOL HYDROCHLORIDE TABLETS

• Main Authors: Shaikh S.A, Shaikh S.S, Shahi S.R., Shookur M.A., Reddy L.K, Padalkar A.N, Thube Mahesh
• Format: Article
• Language: English
• Published: Wolters Kluwer Medknow Publications 2010-06-01
• 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/Manuscripts/Formulation%20and%20Evaluation%20of%20S-(-)-Amlodipine%20Besylate%20and%20Nebivolol%20Hydrochloride%20Tablets.pdf

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.