厄贝沙坦氨氯地平片溶出度评价

厄贝沙坦氨氯地平片溶出度评价

李国琼1，肖文礼2，杨贵方2， 王俊2，刘启兵3*

(1.海南省药品审核认证管理中心，海口570216；2.海南中济医药科技有限公司，海口570208；3.海南医学院药学院，海口571199)

摘要：目的以国外原研的厄贝沙坦氨氯地平片为参比制剂，考察自研制剂与参比制剂在不同pH条件下溶出行为的相似性。方法依据2010 年版《中国药典( 二部)》和日本《医疗用药品品质情报集》中的溶出度实验条件，采用HPLC法，分别以盐酸溶液(pH=2.0)、醋酸盐缓冲液(pH=4.5)、磷酸盐缓冲液(pH=6.8)和水为溶出介质进行测定，溶出方法为桨法，转速为50 r·min`(-1)，并通过f2相似因子法评价自制与参比厄贝沙坦氨氯地平片溶出曲线的相似性。结果3个批号自制片与原研片在不同溶出介质中溶出度相似因子均大于50%。结论自制片与参比片的溶出曲线相似，提示自制厄贝沙坦氨氯地平片处方合理，生产工艺稳定可靠。

关键词：厄贝沙坦；氨氯地平；溶出度；f2相似因子法

doi:10.3969/j.issn.1004-2407.2015.03.017

中图分类号：R944

文献标志码：A

文章编号：1004-2407(2015)03-0275-04

Abstract:ObjectiveTo investigate the similarity of dissolution behavior between the reference preparation tablets ( the listed abroad Irbesartan and Amlodipine Tablets, and the self-prepared(domestic) preparations in dissolution media with different pH. Methods The HPLC method was adopted to determine the dissolubility according to Chinese Pharmacopoeia (edition 2010) and referring to the dissolution test condition in Japan′s Medical Drugs Quality Informations Set. Water， hydrochloride acid(pH=2)， acetate buffer(pH=4.5) and phosphate buffer (pH=6.8) were sepatately used as the dissolution media and the paddle method was adopted with the rotational speed of 50 r·min`(-1). The similarity of dissolution curve was evaluated by f2 similarity factor method. ResultsThe similarity factor of self-made tablets in different dissolution media to the imported tablets was above 50%．ConclusionThe dissolution curve of self-made and imported Irbesartan and Amlodipine Tablets is similar，which prompts that this test preparation has the rational prescription and the production technology is stable and reliable.

基金项目：海口市2013年科技计划项目(编号：HK2013-17)

作者简介：李国琼，女，主管药师

收稿日期：(2014-10-18)

Dissolution evaluation of Irbesartan and Amlodipine Tablets

LI Guoqiong1， XIAO Wenli2， YANG Guifang2， WANG Jun2， LIU Qibing3*(1. Center for Drug Evaluation and Certification of Hainan Province， Haikou 570216，China； 2. Hainan Zhongji Pharmaceutical Technology Limited Company, Haikou， 570208，China；3.Department of Pharmacy， Hainan Medical College， Haikou 571199，China)

Key words: irbesartan； amlodipine； dissolution；f2similarity factor

*通信作者：刘启兵，男，博士，副教授

厄贝沙坦和苯磺酸氨氯地平组成的复方片剂是由日本住友制药株式会社研发的，于2012年9月在日本上市[1]。其中，厄贝沙坦(irbesartan)为血管紧张素Ⅱ(AngiotensinⅡ，AngⅡ)受体抑制剂，能抑制AngⅠ转化为AngⅡ，特异性地拮抗血管紧张素转换酶1受体(AT1)，对AT1的拮抗作用大于AT2 的8 500倍，通过选择性地阻断AngⅡ与AT1受体的结合，抑制血管收缩和醛固酮的释放，产生降压作用[2]。苯磺……