甲磺酸伊马替尼片溶出度方法的建立

目的:建立甲磺酸伊马替尼片溶出度的方法。方法:采用紫外-可见分光光度法进行溶出度测定,检测波长为264 nm。按照中国药典2010版(二部)附录XC第二法(桨法),转速为50 r·min^-1,分别以pH 1.0盐酸溶液、pH 4.0醋酸盐缓冲液、pH 6.8磷酸盐缓冲液和纯化水4种溶剂为溶出介质,溶出体积为1000 mL,于不同时间点取样测定溶出曲线,比较4种溶出介质中自制制剂与原研制剂溶出曲线,建立甲磺酸伊马替尼片溶出度的检查方法。结果:在4种溶出介质中,甲磺酸伊马替尼质量浓度在4.8~14.5 μg·mL^-1范围内与吸光度值呈良好的线性关系(r=0.999),精密度试验的RSD分别为0.04%、0.16%、0.08%、0.07%,稳定性试验的RSD分别为0.11%、0.21%、0.32%、0.26%,平均回收率(n=9)分别为99.8%(RSD=0.33%),99.9%(RSD=0.23%),99.9%(RSD=0.32%),99.9%(RSD=0.28%)。自制制剂与原研制剂在4种溶出介质中15 min内溶出度均在90%以上,两者溶出曲线具有相似性。结论:本法经方法学验证,可用于甲磺酸伊马替尼片剂溶出度的检查。

Objective:To establish a dissolution method of imatinib mesylate tablets.Methods:The UV method was adopted and the detection wavelength was set at 264 nm.According to the second dissolution method(paddle method)stated in the appendix of Chinese pharmacopeia(2010 edition),the rotation speed was 50 r·min^-1 with dissolution medium volume of 1 000 mL.The dissolution profiles of imatinib mesylate tablets in 4 kinds of mediums(pH 1.0 hydrochloric acid solution,pH 4.0 acetate buffer,pH 6.8 phosphate buffer and purified water)were determined by UV.The similarity was investigated by the dissolution curves.Based on the dissolution curves,the new method was established.Results:In 4 kinds of mediums,the linear range of imatinib mesylate was 4.8-14.5 μg·mL^-1 (r=0.999); RSDs of precision tests were 0.04%,0.16%,0.08% and 0.07%; RSDs of stability tests were 0.11%,0.21%,0.32% and 0.26%; the average recoveries(n=9)of imatinib mesylate were 99.8%(RSD=0.33%),99.9%(RSD=0.23%),99.9%(RSD=0.32%)and 99.9%(RSD=0.28%),respectively.In 4 kinds of mediums,the dissolution of self-prepared preparations and the reference Glivec were over 90% with in 15 min; the dissolution curves of the self-prepared preparations and the reference were similar.Conclusion:The method was rapid,simple,accurate,and it can be used for determining the dissolution of imatinib mesylate tablets.

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