摘要
采用L9(3^4)正交试验设计优选苍艾油传递体贴剂的制备处方,并对优选处方进行影响因素试验及皮肤刺激性考察;同时以丁香酚为指标成分,通过HPLC对苍艾油传递体贴剂的体外释放及经皮渗透规律进行探索。结果显示苍艾油传递体贴剂制备的较优处方为Eudragit E 1000.6 g,丁二酸0.08 g,柠檬酸三乙酯0.25 g,丙三醇0.2 g。通过优选处方制得的苍艾油传递体贴剂外观平整,无明显气泡;初黏力(18.33±2.52)号,持黏力(30.01±2.45)min,剥离强度(5.62±0.95)kN·m^-1。影响因素试验结果显示对其黏附性的影响湿度>温度>光照;皮肤刺激性试验结果显示单次给药24 h后无明显的皮肤刺激性。体外释药行为研究结果显示苍艾油贴剂及苍艾油传递体贴剂体外释放及经皮渗透规律均符合Higuchi方程,72 h时丁香酚的累积释放率分别达80.66%,82.25%,二者差异不显著;72 h丁香酚单位面积的累积渗透量分别达(0.1956±0.0659),(0.1310±0.0455)mg·cm^-2,差异具有显著性(P<0.05)。该制备工艺稳定,制得的贴剂具有良好的黏附性;同时将苍艾油制成传递体贴剂后在一定程度上能减缓并控制药物的释放,为临床儿科用药安全提供一定的实验基础。
L9(3^4)orthogonal experiment design was used to optimize the preparation of the patches,and investigate its affecting factors and skin irritation.Eugenol was taken as the index component to study the release behavior in vitro and percutaneous penetration of Cangai oil transfersomes patches by HPLC.The results showed that the optimal prescription for preparing Cangai oil transfersomes patches were Eudragit E1000.6 g,succinic acid 0.08 g,triethyl citrate 0.25 g,glycerol 0.2 g.Patches prepared by the preferred preparation had a flat appearance without obvious bubbles.The initial adhesion was 18.33±2.52,the stickiness was(30.01±2.45)min,and the peel strength was(5.62±0.95)kN·m^-1.The results of affecting factors experiment showed the order of factors affecting its adhesion was humidity>temperature>lighting,and the skin irritation test results showed no significant skin irritation after 24 h of single administration.The results of drug release behavior in vitro showed that the release and the percutaneous penetration of both Cangai oil patches and Cangai oil transfersomes patches conformed to the Higuchi equation.The release amount of eugenol were 80.66%and 82.25%at 72 h,with no significant difference.The cumulative permeation area of eugenol per unit area reached(0.1956±0.0659),(0.1310±0.0455)mg·cm^-2 at 72 h,with significant differences(P<0.05).The experiment results proved that the preparation process of Cangai oil transfersomes patches was stable,and the prepared patches had a good adhesion.At the same time,the preparation of transfersomes patches could alleviate and control the release of the drug to a certain extent,and provide a certain experimental basis for clinical pediatric drug safety.
作者
张昆
熊磊
李亶烨
高家菊
刘云宽
马云淑
ZHANG Kun;XIONG Lei;LI Dan-ye;GAO Jia-ju;LIU Yun-kuan;MA Yun-shu(School of Chinese Materia Medica,Yunnan University of Chinese Medicine,Kunming 650500,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2020年第4期854-860,共7页
China Journal of Chinese Materia Medica
基金
国家自然科学基金面上项目(81673682)
云南省科技厅中医联合专项重点项目(2018FF001-008).
关键词
苍艾油
传递体
贴剂
丁香酚
质量评价
Cangai oil
transfersomes
patches
eugenol
quality evaluation
作者简介
通讯作者:马云淑,博士,教授,研究方向为新型给药系统,Tel:(0871)65918217,E-mail:yunshuma2@126.com;张昆,硕士研究生,E-mail:2670119925@qq.com
