Tapioca starch blended alginate mucoadhesive-floating beads for intragastric delivery of Metoprolol Tartrate

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• 作者：Nikhil Biswas ; ^{nikhil_ju05@yahoo.co.in" class="auth_mail" title="E-mail the corresponding author} ; Ranjan Kumar Sahoo
• 关键词：Metoprolol Tartrate ; Tapioca starch&ndash ; sodium alginate blending ; Mucoadhesive-floating beads
• 刊名：International Journal of Biological Macromolecules
• 出版年：2016
• 出版时间：February 2016
• 年：2016
• 卷：83
• 期：Complete
• 页码：61-70
• 全文大小：1818 K

文摘

The objective of the study was to develop tapioca starch blended alginate mucoadhesive-floating beads for the intragastric delivery of Metoprolol Tartrate (MT). The beads were prepared by ionotropic gelation method using calcium chloride as crosslinker and gas forming calcium carbonate (CaCO₃) as floating inducer. The alginate gel beads having 51–58% entrapped MT showed 90% release within 45 min in gastric medium (pH 1.2). Tapioca starch blending markedly improved the entrapment efficiency (88%) and sustained the release for 3–4 h. A 12% w/w HPMC coating on these beads extended the release upto 9–11 h. In vitro wash off and buoyancy test in gastric media revealed that the beads containing CaCO₃ has gastric residence of more than 12 h. In vitro optimized multi-unit formulation consisting of immediate and sustained release mucoadhesive-floating beads (40:60) showed good initial release of 42% MT within 1 h followed by a sustained release of over 90% for 11 h. Pharmacokinetic study performed in rabbit model showed that the relative oral bioavailability of MT after administration of oral solution, sustain release and optimized formulation was 51%, 67% and 87%, respectively. Optimized formulation showed a higher percent inhibition of isoprenaline induced heart rate in rabbits for almost 12 h.