采用多条溶出曲线评价国产盐酸普罗帕酮片的内在质量

目的：利用光纤药物溶出度实时测定仪，研究国产盐酸普罗帕酮片在不同pH介质中的溶出曲线，评价制剂质量。方法：采用浆法，转速50 r·min^-1，以pH 1.2盐酸溶液、pH 4.0醋酸盐缓冲液、pH 6.8磷酸盐缓冲液和水为溶出介质，采用光纤药物溶出度实时测定仪测定国产盐酸普罗帕酮片与进口制剂的溶出曲线，并用AV值法与日本橙皮书公布的溶出曲线进行比较。结果：国产样品在4种介质中溶出行为差异很大，溶出曲线与橙皮书参比曲线全部不相似。结论：国产盐酸普罗帕酮片制剂工艺与国外有较大差异，各厂家产品质量参差不齐。

Objective: To study dissolution curve profiles of domestic propafenone hydrochloride tablets in different pH media by the fiber-optic real time dissolution test system and evaluate the drug quality. Methods: The paddle method was used at a rate of 50 r·min^-1,the dissolution curves of domestic and imported propafenone hydrochloride tablets were detected in the following four media including water,pH 1.2 hydrochloric acid solution,pH 4.0 acetate buffer solution,and pH 6.8 phosphate buffer solution by the fiber-optic real time dissolution test system,and the results were compared with the dissolution curves published in the Japanese Orange Book by method of AV value. Results: The comparison indicated that the dissolution process of domestic products were quite different in the four media,the dissolution curves were all distinctly dissimilar with the reference curves in the Orange Book. Conclusion: There is significant difference in the quality of domestic products from several manufacturers and a pronounced gap exists as compared between the domestic manufacturing technique and the abroad.

[1] CHEN Xin-qian(陈新谦), JIN You-yu(金有豫), TANG Guang(汤光).New Materia Medica (新编药物学)[M].Beijing(北京):People's Medical Publishing House(人民卫生出版社), 2003:343
[2] Clarot F, Goullé JP, Horst M, et al.Fatal propafenone overdoses:caserepots and a review of the literature[J].J Ana1 Toxicol, 2003, 27(8):595
[3] CHEN Xiao-yan(陈笑艳), HUANG Hai-hua(黄海华), ZHONG Da-fang(钟大放), et al.Characterization of hydroxylated metabolites of propafenone in healthy Chinese volunteers(普罗帕酮在中国健康受试者体内的羟基化代谢产物研究)[J].Acta Pharm Sin(药学学报), 1999, 34(10):776
[4] Zhou Q, Yao TW, Yu YN, et al.Stereoselective metabolism of propafenone by human liver CYP3A4 expressed in transgenic Chinese hamster CHL cells lines[J].Acta Pharmacol Sin, 2001, 22(10):944
[5] LIU Jun-ting(刘俊亭), GAO Li-na(高利娜), WANG Yan(王妍).Determination of propafenone and its metabolites with GC-MS(体内普罗帕酮及其代谢物的GC-MS检验)[J].J Instrum Anal(分析测试学报), 2007, 26(81):44
[6] ChP 2010.Vol Ⅱ(中国药典2010年版.二部)[S].2010:790
[7] ZHANG Qi-ming(张启明), XIE Mu-feng(谢沐风), NING Bao-ming(宁保明), et al.Evaluation of solid oral products by dissolution profiles in different mediums(采用多条溶出曲线评价口服固体制剂的内在质量)[J].Chin J Pharm(中国医药工业杂志), 2009, 40(12):946
[8] 財団法人日本公定書協會編.医療用医薬品品質情報集(オレンジブック)と品質再評価日本薬局方外医薬品規格[S].第三部.薬事日報社
[9] JIANG Xiong-ping(姜雄平), WEI Li-ping(魏立平).New comparative evaluation for dissolution profiles(一种新的溶出曲线比较方案)[J].Chin J Pharm Anal(药物分析杂志), 2010, 30(6):1026
[10] Annotationof ChP 1990 VolⅡ(中国药典1990年版二部药典注释)[M].Beijing(北京):Chemical Industry Press(化学工业出版社), 1993:599
[11] PAN Guo-zong(潘国宗), CAO Shi-zhen(曹世帧).Modern gastroenterology(现代胃肠病学)[M].Beijing(北京):Science Press(科学出版社), 1994:150