复方利多卡因乳膏体外透皮一致性研究  

Study on in vitro transdermal permeation consistency of compound lidocaine cream

作　　者：刘孟洋 李蒙 王增明 张慧 高静 王汀[1] 郑爱萍 LIU Meng-yang;LI Meng;WANG Zeng-ming;ZHANG Hui;GAO Jing;WANG Ting;ZHENG Ai-ping(College of Medical,Anhui Medical University,Anhui Hefei 230032,China;Institute of Pharmacology and Toxicology,Acad emy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850)

机构地区：[1]安徽医科大学药学院,安徽合肥230032 [2]军事科学院军事医学研究院毒物药物研究所,北京100850

出　　处：《中国医院药学杂志》2022年第12期1186-1191,共6页Chinese Journal of Hospital Pharmacy

基　　金：“十三五”国家重大新药创制科技重大专项资助项目(编号:2018ZX09721003-007)。

摘　　要：目的:比较试验和参比制剂2.5%复方利多卡因乳膏透皮作用的一致性。方法:以大鼠和巴马香猪的皮肤作为透皮渗透的材料,选用立式改良Franz扩散池测定复方利多卡因乳膏的渗透吸收规律,以高效液相色谱法分别测定接收液中药物的吸收总量和猪皮中药物的滞留量随时间的变化关系。结果:复方利多卡因乳膏试验与参比制剂在鼠皮及巴马香猪皮这两种不同透皮材料中5 h利多卡因的单位面积累积渗透量分别为(0.380±0.019)和(0.351±0.017)mg·cm^(-2),(0.228±0.012)和(0.217±0.023)mg·cm^(-2);丙胺卡因的单位面积累积渗透量分别为(0.422±0.022)和(0.382±0.029)mg·cm^(-2),(0.263±0.015)和(0.238±0.008)mg·cm^(-2);试验制剂与参比制剂在巴马香猪皮中5h的利多卡因,丙胺卡因的皮内滞留量分别为(2.021±0.094)和(1.999±0.118)mg·cm^(-2),(2.240±0.115)和(2.208±0.053)mg·cm^(-2);试验和参比制剂的体外释放比较的结果均符合FDA(U.S.Food and Drug Administration)和欧盟的指导原则。结论:2.5%复方利多卡因乳膏试验与参比制剂的透皮渗透程度和速率均符合外用制剂的一致性要求,且在猪皮内药物滞留特征相似。OBJECTIVE To investigate the quality consistency of 2.5%compound lidocaine creambetween a test and reference through the transdermal permeation determination.METHOD The modified Franz diffusion cell was employed for the in vitro transdermal permeation test through skin of rats and Bama pig.The cumulative permeation amounts in the receiving liquids and the drug residue amounts in the pig skin samples were measured by high performance liquid chromatography methods.RESULTS TheCumulative penetration amounts oflidocaine until 5 h of the test and reference compound lidocaine cream preparation in Bama pigskin and rat skin in two different transdermal materials were(0.380±0.019)and(0.351±0.017)mg·cm^(-2),(0.228±0.012)and(0.217±0.023)mg·cm^(-2);The Cumulative penetration amounts of prilocaine were(0.422±0.022)and(0.382±0.029)mg·cm^(-2),(0.263±0.015)and(0.238±0.008)mg·cm^(-2);The Cumulative retention amounts of lidocaine andprilocaine until 5 h of the test and reference preparation in Bama pigskin were(2.021±0.094)and(1.999±0.118)mg·cm^(-2),(2.240±0.115)and(2.208±0.053)mg·cm^(-2);The resultsofthein vitro release comparison of the test and compound lidocaine cream preparation wereinaccordancewith the FDA(U.S.Food and Drug Administration)and European Union guidelines.ConclusionThe degree and rate of transdermal penetration of the test and reference 2.5%compound lidocaine cream preparation were in accordance with the consistency requirements for topical formulations.The characteristics of drug residues in the Bama pig skin was similar.

关 键 词：复方利多卡因乳膏 高效液相色谱 体外透皮吸收 FRANZ扩散池 

分 类 号：R917[医药卫生—药物分析学]