蒿甲醚贴剂的研制及小鼠体内药效学研究  

Preparation of Artemether Patch and Its Pharmacodynamics in Rats

作　　者：杨华生[1,2] 王乃婕[1] 梁秉文[1] 叶祖光[1] 贺成[1] 薛宝云[1] 

机构地区：[1]中药复方新药开发国家工程研究中心,北京100075 [2]江西中医学院,南昌330004

出　　处：《中国药学杂志》2008年第24期1878-1881,共4页Chinese Pharmaceutical Journal

摘　　要：目的研制蒿甲醚贴剂,并评价其经皮吸收对感染疟原虫小鼠的杀灭及抗复燃作用。方法涂布法制备蒿甲醚贴剂,考察不同促进剂、药物的浓度对透皮速率的影响;首次建立蒿甲醚贴剂体外透皮速率常数的HPLC测定方法;按新药(西药)临床前研究指导原则进行抗疟实验。结果药剂学研究表明,当透皮促进剂丙二醇和月桂氮酮以4%浓度按3∶1比例合用时,贴剂的体外透皮速率常数最大;药效学研究显示,该贴剂能明显减少给药次数,显著降低给药剂量。结论蒿甲醚可以经皮肤给药,达到杀灭疟原虫的作用,并且给药次数及剂量明显减少,患者依从性提高,因此具有良好的开发应用前景。OBJECTIVE To prepare artemether patch and to investigate its antimalaria effects in rats after transdermal absorption. METHODS The patch was prepared through spreading method and the influence of different factors （ enhancers and concentration） was investigated. A HPLC method was developed to determine the permeation rate of artemrther through rat skin in vitro for the first time. The antimalaria test was carried out to evaluate its effect according to the new drug （ western medicine ） preelinical study guide principle. RESULTS The pharmacodynamic study showed that the transdermal system had the largest permeation rate when propylene glycol was mixed with Azone by the ratio of 3：1 at the concentration of 4%. The in vivo pharmacodynamic study in rats demonstrated that the patch evidently minimized administration frequency, markedly reduced dose. CONCLUSION The artemrther patch possessed evident antimalaria effects. It could minimize administration frequency and dose , therefore improve patient compliance. The artemrther-TDDS may have a prosperous future.

关 键 词：蒿甲醚 压敏胶 透皮给药系统 贴剂 促渗剂 抗疟作用 

分 类 号：R944[医药卫生—药剂学]