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[尼莫通与尼莫地平片生物利用度的比较]

[Comparison of bioavailability between nimotop and nimodipine tablet].

作者信息

Shi X J, Wang H T, Wei Y, Zhang J H, Zhang L L, Zhong M K

机构信息

Division of Clinical Pharmacy of Huashan Hospital, Shanghai Medical University, Shanghai 200040.

出版信息

Yao Xue Xue Bao. 1997 Sep;32(9):708-10.

Abstract

A new analytical method was established for determining plasma level of nimodipine using HPLC and its application to determine the bioavailability of nimodipine. Experiments were performed on a Waters Model Baseline 810 System instrument. A 3.9 mm x 200 mm stainless steel column was packed with YWG-C18(10 microns) as the stationary phase. The mobile phase was a mixture solution of methanol--water (60/40, v/v) with 1.00 ml.min-1 at 35 degrees C. The detector was set at 358 nm. The plasma samples were extracted with ether--n-hexane (1:1). Calibration curve was linear (gamma = 0.9999) in the concentration range of 5-300 ng.ml-1. The within-day and between-day precision (RSD) were less than 3% and 5%, respectively, with average recoveries of 97.67%-102.3%. The study on bioavailability of numodipine between tablet A (made in China) and nimotop (Bayer, Germany) was carried out in 8 volunteers at the oral dose of 120 mg by cross-over method. Two-compartment open model was suitable for describing the disposition of nimodipine. The main pharmacokinetic parameters were shown in Tab 1 and mean plasma concentration--time curve of nimodipine was shown in Fig 1. The results indicate that tablet A exhibited a lower bioavailability (relative to nimotop). We suggest that the product tablet A must be improved in formula and technology.

摘要

建立了一种用高效液相色谱法测定血浆中尼莫地平含量的新分析方法,并将其应用于尼莫地平生物利用度的测定。实验在Waters Model Baseline 810系统仪器上进行。采用YWG-C18(10微米)填充的3.9毫米×200毫米不锈钢柱作为固定相。流动相为甲醇-水(60/40,v/v)混合溶液,流速为1.00毫升·分钟-1,温度为35℃。检测器设定在358纳米。血浆样品用乙醚-正己烷(1:1)萃取。校准曲线在5-300纳克·毫升-1浓度范围内呈线性(γ = 0.9999)。日内和日间精密度(相对标准偏差)分别小于3%和5%,平均回收率为97.67%-102.3%。采用交叉试验法,对8名志愿者口服120毫克剂量的国产A片和德国拜耳公司的尼莫通进行了生物利用度研究。二室开放模型适用于描述尼莫地平的处置过程。主要药代动力学参数见表1,尼莫地平的平均血药浓度-时间曲线见图1。结果表明,A片的生物利用度较低(相对于尼莫通)。我们建议,A片产品必须在配方和工艺上加以改进。

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