余甘子软膏的制备及冰片促渗作用考察  

Preparation of Phyllanthus emblica ointment and investigation of the permeation-enhancing effect of borneol

作　　者：崔利利 郝佳旭 查丽春 范晓 梅佳华 普娟 马云淑 CUI Li-li;HAO Jia-xu;ZHA Li-chun;FAN Xiao;MEI Jia-hua;PU Juan;MA Yunshu(School of Chinese Materia Medica,Yunnan University of Chinese Medicine,Yunnan Kunming 650500,China;The Key Laboratory of External Drug Delivery System and Preparation Technology in University of Yunnan Province,Yunnan Kunming 650500,China;Yunnan Provincial Key Laboratory of Molecular Biology for Sinomedicine,Yunnan Kunming 650500,China)

机构地区：[1]云南中医药大学中药学院,云南昆明650500 [2]云南省高校外用给药系统与制剂技术研究重点实验室,云南昆明650500 [3]云南省中医药学分子生物学重点实验室,云南昆明650500

出　　处：《中国医院药学杂志》2022年第18期1862-1867,共6页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金项目(编号:82060723);云南省中医药学分子生物学重点实验室(云南中医药大学)开放基金资助项目(编号:2019DG016)。

摘　　要：目的:制备余甘子软膏并考察冰片对余甘子软膏经皮渗透的影响。方法:采用L_(9)(3^(4))正交试验,以耐寒试验、耐热试验、离心试验及感官评价为指标优选余甘子软膏的制备工艺,并进行皮肤刺激性考察;采用Franz扩散池法,以没食子酸、柯里拉京的体外透皮为指标,通过HPLC考察不同含量冰片对余甘子软膏的促渗作用;并对余甘子软膏经皮渗透及体外释放规律进行探究。结果:余甘子软膏的最佳处方为石蜡油0.5 g,凡士林1 g,羊毛脂5 g,硬脂酸3 g,纯净水1 g,丙三醇1 g,余甘子浸膏4 g;5%的冰片对余甘子软膏中没食子酸和柯里拉京的促渗效果最佳,24 h时的经皮累计渗透量分别为1.1636,0.0738 mg·cm^(-2),经皮吸收速率为0.0463,0.0031 mg·cm^(-2)·h,增渗倍数为1.7380,1.8225;24 h时余甘子软膏中没食子酸和柯里拉京的累计释放率分别为58.91%,45.47%;含5%冰片的余甘子软膏中没食子酸和柯里拉京的经皮渗透均符合一级方程,体外释放分别符合Higuchi方程、Hixson-Crowell方程;单次给药1,24 h后均无明显皮肤刺激性。结论:制得的余甘子软膏具有良好的性状及体外经皮渗透、体外释放性能,无明显皮肤刺激性。OBJECTIVE Prepare Phyllanthus emblica ointment and investigate the effect of borneol on the percutaneous penetration of Phyllanthus emblica ointment.METHODS The L_(9)(3^(4))orthogonal test was used to optimize the preparation process of Phyllanthus emblica ointment with cold tolerance test,heat test,centrifugal test and sensory evaluation as indicators,and to investigate skin irritation.Used the Franz diffusion cell method,in vitro permeation of gallic acid and corilagin as indicators,the penetration enhancement effect of different content of borneol on Phyllanthus emblica ointment was investigated by HPLC.The permeation and in vitro release of Phyllanthus emblica ointment were explored.RESULTS The best prescription for Phyllanthus emblica ointment was 0.5 g of paraffin oil,1 g of petrolatum,5 g of lanolin,3 g of stearic acid,1 g of purified water,1 g of glycerol,and 4 g of phyllanthus emblica extract.Borneol containing 5%had the best penetration promoting effect on gallic acid and corilagin in Phyllanthus emblica ointment,and the cumulative permeation volume at 24 h was 1.1636 and 0.0738 mg·cm^(-2),respectively;The transdermal absorption rate was 0.0463,0.0031 mg·cm^(-2)·h;The osmotic multiples were 1.7380,1.8225.The cumulative release rates of gallic acid and corilagin in Phyllanthus emblica ointment at 24 h were 58.91%and 45.47%,respectively.The transdermal penetration of gallic acid and corilagin in Phyllanthus emblica ointment containing 5%borneol was First-order equation;The in vitro release conforms to the Higuchi equation and the Hixson-Crowell equation respectively.No obvious skin irritation after 1 h,24 h after single administration.CONCLUSIONS The prepared Phyllanthus emblica ointment has good properties,in vitro percutaneous penetration and in vitro release performance,and no obvious skin irritation.

关 键 词：余甘子 软膏 正交试验 冰片 体外透皮 体外释放 

分 类 号：R283.6[医药卫生—中药学]