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对乙酰氨基酚溶液剂及其药物动力学研究

Studies on Paracetamol Liquid and Its Pharmacokinetics in Healthy Volunteers

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【作者】 吕万良屠锡德蒋文蕾王娟Soumana Fofana

【Author】 Lu Wanliang, Tu Xide, Jiang Wenlei, Wang Juan, Soumana Fofana Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009

【机构】 中国药科大学药剂学教研室

【摘要】 研制了对乙酰氨基酚溶液剂(5g/0.1L),建立了高效液相色谱法(HPLC-UV)测定血药浓度。以Tyhenol○R(McNeil,USA)混悬液为对照品,研究了自制对乙酰氨基酚溶液剂在8名健康志愿受试者体内的药物动力学。结果显示,对乙酰氨基酚溶液剂在人体内的动力学以二室线性模型描述为宜,其主要药物动力学参数分别为α=0.6152h-1,β=0.1925h-1,t12=3.62h,Ka=3.8864h-1,AUC0→∞=77.23h·μg/ml,相对于Tylenol○R混悬剂的生物利用度为98.85%。

【Abstract】 Paracetamol liquid (5 g/0.1 L) was developed in the convenient, fast and effective relief of children′s fever and pain. A simple and sensitive high performance liquid chromatographic method (HPLC UV) was establisbed with detection limit of 0.016 μg/ml, and can be used for the analysis of biological samples of paracetamol. Pharmacokinetics of paracetamol(self made) was evaluated in 8 healthy volunteers to assess the disposition in vivo of paracetamol. It was suggested that kinetics of paractetamol in vivo fitted two compartmental model, and that main pharmacokinetics parameters of paracetamol liquid were α =0.6152 h -1 , β =0.1925 h -1 , t 12 =3.62 h, K a=3.8864 h -1 and AUC 0→∞ =77.32 h·μg/ml. The relative bioavailability of paracetamol liquid was 98.85%, compared with the control of Tylenol ○R suspension.

  • 【文献出处】 中国药科大学学报 ,JOURNAL OF CHINA PHARMACEUTICAL UNIVERSITY , 编辑部邮箱 ,1996年03期
  • 【分类号】O657.72
  • 【被引频次】10
  • 【下载频次】385
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