复方蒿甲醚分散片的溶出度研究及其方法学验证  

A Method for Determining the Dissolution of Artemether and Lumefantrine Dispersible Tablets and Methodology Study

作　　者：鲁素雅 邢海艳 金鹏[1] 袁耀佐 金华[1] LU Su-ya;XING Hai-yan;JIN Peng;YUAN Yao-zuo;JIN Hua(Huai′an Institute for Food and Drug Control,Jiangsu Huai′an 223305,China;Jiangsu Institute for Food and Drug Control,Jiangsu Nanjing 210019,China)

机构地区：[1]淮安市食品药品检验所,江苏淮安223005 [2]江苏省食品药品监督检验研究院,江苏南京210019

出　　处：《中国药物评价》2019年第1期15-20,共6页Chinese Journal of Drug Evaluation

摘　　要：目的:建立并验证复方蒿甲醚分散片中蒿甲醚和苯芴醇的溶出度测定方法。方法:蒿甲醚的溶出以水1 000 mL为溶出介质,桨法,转速为100 r·min^(-1),于1 h和3 h取样测定,用十八烷基硅烷键合硅胶为填充剂(Macherey-Nagel,Nucleosil 100-5,12.5cm×40 mm),以水-乙腈-正丙醇-三氟乙酸(400∶500∶100∶1)为流动相,检测波长为210 nm,流速为1mL·min^(-1);蒿甲醚检测波长为210 nm。苯芴醇的溶出以1%氯化苄基二甲基烷基胺的0.1 mol·L^(-1)盐酸溶液1 000 mL为介质,桨法,转速为100 r·min^(-1),45 min时取样测定,按吸收系数法(E11%cm)在342 nm波长处测定吸光度。结果:蒿甲醚在1 h和3 h的溶出分别为58.5%和85.9%以上;苯芴醇在45 min溶出82.8%以上。结论:该方法分别测定分散片中蒿甲醚和苯芴醇的溶出度,稳定性高,专属性强。Objective:To establish and validate the method for determining the dissolution of artemether and lumefantrinein the artemether and lumefantrinedispersible tablets.Methods:For artemether,using 1 000 mL of degassed water as the dissolution medium,and rotating the paddle at 100 revolutions per minute.At 60 minutes and 180 minutes withdraw a sample of 10 mL of the medium through an in-line filter as test solutions.Using a stainless steel column(12.5 cm×40 mm)packed withparticles of silica gel which has been modified with chemically bonded octadeylsilyl groups(Macherey-Nagel,Nucleosil 100-5 was recommended).As the mobile phase,use a mixture of 400 volumes of water,500 volumes of acetonitrile 100 volumes of 1-propanol and 1 volume of trifluoroacetic acid.Operate with a flow rate of 1 mL per minute.As a detector using an ultraviolet spectrophotometer was set at a wavelength of about 210 nm.For lumefantrine,using 1000 ml of hydrochloric acid(~3.6 g·L^-1)TS,1%benzalkonium chloride Ras the dissolution medium,and rotating the paddle at 100 revolutions per minute.At 45 minutes withdraw a sample of 10 ml of the medium through an in-line filter.Allow the filtered sample to cool to room temperature.Measure the absorbance of a 1 cm layer of the resulting solution,suitably diluted if necessary,at the maximum at about 342 nm.For each of the six tablets tested,calculate the total amount of lumefantrine(C 30 H 32 Cl 3 NO)in the medium,using the absorptivity value of 300.8(A 1%1 cm=300.8).Results:The dissolution of artemether at 1 hour and 3 hours wasabove58.5%and 85.9%,respectively;Lumefantrinewas dissolved above 82.8%at 45 minutes.Conclusion:The methods to determine the dissolution of artemether and lumefantrinein the artemether and lumefantrine dispersible tablets,and which is accurate,high in stability and strong in specificity.

关 键 词：蒿甲醚 苯芴醇 分散片 溶出度 

分 类 号：R927.2[医药卫生—药学]