Design and evaluation of a two-layer floating tablet for gastric retention using cisapride as a model drug.
A new kind of two-layer floating tablet for gastric retention (TFTGR) with cisapride as a model drug was developed. The in vitro drug release was determined, and the resultant buoyancy and the time-buoyancy curve were plotted. Because of the sodium bicarbonate added to the floating layer, when immersed in simulated gastric fluid (SGF) the tablet expands and rises to the surface, where the drug is gradually released. The in vitro drug release of this kind of two-layer dosage was controlled by the amount of hydroxypropylmethylcellulose (HPMC) in the drug-loading layer. Generally, the more HPMC, the slower the drug releases. Because cisapride has greater solubility in SGF than simulated intestinal fluid (SIF), its in vitro drug dissolution in SGF is faster than in SIF. One of the distinguishing characteristics of this kind of tablet is the separate regulation of buoyancy and drug release. The idea developed in this experiment can be used as a general modelfor the design of other tablets for gastric retention.
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Division of Pharmaceutics, Shenyang Pharmaceutical University, People's Republic of China. fxyh@sj-user.he.cninfo.net
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D001826:Body Fluids / Q000378:metabolism; D020117:Cisapride / Q000737:chemistry* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding; D015195:Drug Design; D005750:Gastric Juice / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism*; D005765:Gastrointestinal Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D007785:Lactose / Q000031:analogs & derivatives* / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D010078:Oxazines; D017693:Sodium Bicarbonate; D012995:Solubility; D013608:Tablets, Enteric-Coated / Q000737:chemistry
D003692:Delayed-Action Preparations; D005765:Gastrointestinal Agents; D010078:Oxazines; D013608:Tablets, Enteric-Coated; D017693:Sodium Bicarbonate; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose; D020117:Cisapride