米诺地尔搽剂体外透皮一致性研究
Study on in vitro transdermal consistency of minoxidil solution
吕晨羲 1游蓉丽 2刘艳之 3罗钢 2杨戎 2沈悦 2孙艳玉 2陆洋 4李建伟5
作者信息
- 1. 北京中医药大学中药学院,北京 102488;北京振东光明药物研究院有限公司,北京 100085
- 2. 北京振东光明药物研究院有限公司,北京 100085
- 3. 北京中医药大学中药学院,北京 102488;山西振东安欣生物制药有限公司,山西晋中 030619
- 4. 北京中医药大学中药学院,北京 102488
- 5. 北京振东光明药物研究院有限公司,北京 100085;长治医学院药学系,山西长治 046013
- 折叠
摘要
目的:比较5％米诺地尔搽剂试验制剂和参比制剂透皮作用的一致性.方法:以巴马香猪皮肤作为透皮渗透的材料,选用立式改良Franz扩散池测定米诺地尔搽剂的渗透规律,采用液相色谱-串联质谱法(LC-MS/MS)分别测定接收液中药物的渗透总量和猪皮中药物的滞留量随时间的变化关系.结果:试验制剂和参比制剂在巴马香猪皮肤中24 h米诺地尔的累积渗透量分别为(49 721±29 707)ng·cm-2和(45 372±23 755)ng·cm-2;平均渗透速率分别为(2 352±1 309)ng·cm-2·h-1和(2 182±1 080)ng·cm-2·h-1;皮肤滞留量分别为(218 276±137 675)ng·g-1 和(188 040±49 523)ng·g-1;试验制剂与参比制剂在累积渗透量约为总透过量一半时(12h)的平均渗透速率分别为(2172±1 330)ng·cm-2·h-1和(1 947±1 037)ng·cm-2·h1.结论:5％米诺地尔搽剂试验制剂与参比制剂的透皮渗透程度和速率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.
Abstract
OBJECTIVE To compare the consistency of transdermal effect of 5％minoxidil solution test product versus refer-ence product.METHODS Bama miniature pig skin was utilized as a material for transdermal penetration and vertical modified Franz diffusion cell for determining the penetration of minoxidil solution.Liquid chromatography/tandem mass spectrometry(LC-MS/MS)was employed for determining the relationship between total amount of drug permeation in receiving solution and reten-tion of drug in skin with time.RESULTS Test and reference products in skin for 24 h cumulative permeation were(49 721± 29 707)and(45 372±23 755)ng·cm-2;Average permeation rates were(2 352±1 309)and(2 182±1 080)ng·cm-2·h-1;24 h skin retention(218 276±137 675)and(188 040±49 523)ng·g-1;Average permeation rates of test and reference products at a cumulative permeation of about half total permeation(12 h)were(2 172±1 330)and(1 947±1 037)ng·cm-2·h-1.CONCLUSION Degree and rate of transdermal penetration of 5％minoxidil solution test/reference formulation fulfill the consis-tency requirements for topical formulations.And drug retention characteristics of minoxidil solution are similar in Bama miniature pig skin.
关键词
米诺地尔搽剂/液相色谱-串联质谱法/体外透皮/Franz扩散池Key words
minoxidil solution/LC-MS/MS/in vitro transdermal permeation/Franz diffusion cell引用本文复制引用
出版年
2024
NETL
NSTL
万方数据