Wei Z, Yu Z, Bi D
Division of Pharmaceutics, Shenyang Pharmaceutical University, People's Republic of China.
Drug Dev Ind Pharm. 2001 May;27(5):469-74. doi: 10.1081/ddc-100104323.
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.
研制了一种以西沙必利为模型药物的新型双层胃滞留漂浮片(TFTGR)。测定了其体外药物释放情况,并绘制了所得的浮力和时间-浮力曲线。由于在漂浮层中添加了碳酸氢钠,该片剂浸入模拟胃液(SGF)时会膨胀并升至表面,药物在表面逐渐释放。这种双层剂型的体外药物释放受载药层中羟丙基甲基纤维素(HPMC)用量的控制。一般来说,HPMC用量越多,药物释放越慢。由于西沙必利在SGF中的溶解度比模拟肠液(SIF)中的溶解度大,其在SGF中的体外药物溶解速度比在SIF中快。这种片剂的一个显著特点是浮力和药物释放可分别调节。本实验中提出的理念可作为设计其他胃滞留片剂的通用模型。