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本文采用高效液相色谱法对12名男性健康志愿者单剂量口服含100mg无水茶碱的甘氨酸茶碱钠缓释片后血浆中茶碱的浓度进行检测并利用Waguer-Nelson法计算吸收百分率。对体内吸收百分率与体外释放百分率进行相关性研究。结果表明,当采用以浆法,水为溶出介质,转速为100r·min-1,本品体外药物释放与体内药物吸收具有较好的相关性,回归方程为:Y=0.89+1.12x,r=0.9906(n=6),因此,可以通过控制本品在体外的释放,达到控制体内药物吸收的目的。
In this paper, plasma concentrations of theophylline in 12 male healthy volunteers after oral administration of 100 mg anhydrous theophylline glycine theophylline sustained-release tablets were detected by high performance liquid chromatography and the percentage absorption was calculated by Waguer-Nelson method. The correlation between in vivo absorption percentage and in vitro release percentage was studied. The results showed that there was a good correlation between the in vitro drug release and the drug absorption in vivo when using the slurry method and water as the dissolution medium at the speed of 100 r · min-1. The regression equation was Y = 0.89 + 1.12x, r = 0.9906 (n = 6), therefore, can be controlled by the release of the goods in vitro, to achieve the purpose of controlling the absorption of drugs in the body.