FORMULATION AND EVALUATION OF CONTROLLED RELEASE OSMOTIC TABLET OF METOPROLOL SUCCINATE
Abstract
Objective: Metoprolol Succinate has a short elimination half- life (3-7 hours) and rapidly absorbed in GIT If it is formulated by conventional tablets requires multiple daily administration with resulting inconvenience to the hypertensive patient and the possibility of reduced compliance with prescribed therapy. Methods: Core tablets were prepared by direct compression technique using fructose and KCl as osmogens and Avicel PH101 as filler. The core tablets were coated by dip coating and used a coating agent cellulose acetate (2%w/v) with PEG400 and PEG6000 as water soluble pore former and dibutyl-pthalate as plasticizer. The optimized formulation was evaluated for Compatibility Study by FTIR, invitro drug release study by USP-II dissolution apparatus and, accelerated stability study. Results: Optimized batch FaC3 was formulated using ratio 3:2 (Fructose : KCl) of osmogent mixture, 20% w/w of pore former(PEG6000) and 4% weight gain. It gave about 97.59 % drug release for 12 hours. The highest r2 value (0.979) through zero order drug release and n≈0.982 indicates case-II transport or typical zero-order. Optimized formulation had no significant effect on pH, agitational intensity and found to be compatible with the excipients and stable. Before contact with the dissolution medium, SEM images revealed that no pores were observed before dissolution and after dissolution had shown the porous nature of the membrane. Conclusion: The present study confirmed that the drug release inversely proportional to membrane weight gain and release increases with mixture of osmogens and system provides a controlled release.
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