title: Tapioca starch blended alginate mucoadhesive-floating beads for intragastric delivery of Metoprolol Tartrate.
abstract: 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 1h 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.
authors.affiliation: Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India. Electronic address: nikhil_ju05@yahoo.co.in.
authors.forename: Nikhil
authors.initials: N
authors.lastname: Biswas
authors.affiliation: Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
authors.forename: Ranjan Kumar
authors.initials: RK
authors.lastname: Sahoo
mesh_terms: D000269:Adhesives / Q000737:chemistry* / Q000378:metabolism; D000464:Alginates / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods; D005753:Gastric Mucosa / Q000378:metabolism*; D005782:Gels / Q000737:chemistry / Q000378:metabolism; D020723:Glucuronic Acid / Q000737:chemistry / Q000378:metabolism; D006603:Hexuronic Acids / Q000737:chemistry / Q000378:metabolism; D008297:Male; D008790:Metoprolol / Q000737:chemistry* / Q000378:metabolism; D011817:Rabbits; D012996:Solutions / Q000737:chemistry / Q000378:metabolism; D013213:Starch / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000269:Adhesives; D000464:Alginates; D003692:Delayed-Action Preparations; D005782:Gels; D006603:Hexuronic Acids; D012996:Solutions; D020723:Glucuronic Acid; D013213:Starch; D008790:Metoprolol
keywords: Metoprolol Tartrate; Mucoadhesive-floating beads; Tapioca starch–sodium alginate blending