阿魏酸乳膏的体外经皮渗透性及大鼠体内药动学  

In vitro Transdermal Permeation and Pharmacokinetics in Rats of Ferulic Acid Cream

作　　者：晏娜 汤湛 王俏 YAN Na;TANG Zhan;WANG Qiao(Dept.of Phamacy,Jin Hua Municipal Maternal and Child Health Care Hospital,Jinhua 321000;School of Pharmacy,Hangzhou Medical College,Hangzhou 310013;Key Lab.of Neuropsychiatric Drug Research of Zhejiang Province,Hangzhou Medical College,Hangzhou310013)

机构地区：[1]浙江省金华市妇幼保健院药剂科,浙江金华321000 [2]杭州医学院药学院,浙江杭州310013 [3]杭州医学院,浙江省神经精神疾病药物研究重点实验室,浙江杭州310013

出　　处：《中国医药工业杂志》2025年第1期73-79,共7页Chinese Journal of Pharmaceuticals

基　　金：金华市科技计划项目(2021-4-305);浙江省神经精神疾病药物研究重点实验室项目(2019E10021)。

摘　　要：该研究采用单因素试验结合Box-Behnken设计-响应面法优化阿魏酸(1)乳膏处方,随后采用离体大鼠皮肤研究了1乳膏的体外渗透行为,及其在大鼠体内的药动学特性。所得优化处方中,1、月桂氮[艹卓]酮、薄荷油、1,2-丙二醇、PEG400的质量分数分别为5.00%、10.68%、10.03%、9.32%、10.00%。体外渗透试验结果显示,以优化处方制备的1乳膏10 h累积渗透量为(470.70±24.54)μg/cm^(2),透皮速率为(57.70±3.09)μg·cm^(-2)·h^(-1)。体内研究表明,大鼠经皮给予1乳膏后,10 h时血浆中AUC即可达到(953.90±175.30)mg·min·L^(-1),与以10 mg/kg剂量灌胃给药相当;且10 h时经皮给药组大鼠的血浆浓度未出现下降趋势。该乳膏制备工艺简单,易于产业化推广,且制成的乳膏经皮吸收性好,可长久、平稳地释放药物,为1的进一步开发和应用提供了参考。In this study,the formulation of ferulic acid(1)cream was optimized by single-factor experiments combined with Box-Behnken design-response surface methodology.Subsequently,the in vitro permeation behavior of the 1 creams was investigated with excised rat skin,and its pharmacokinetics in rats was also explored.The obtained optimal formulation was as follows:the mass fractions of 1,azone,mint oil,1,2-propanediol and PEG400 were 5.00%,10.68%,10.03%,9.32%and 10.00%,respectively.The results of in vitro permeation test showed that the cumulative permeation amount of the 1 cream prepared by the optimal formulation within ten hours was(470.70±24.54)μg/cm~2,and the permeation rate was(57.70±3.09)μg·cm^(-2)·h^(-1).The results of in vivo studies indicated that after transdermal administration of the 1 cream to rats,AUC could reach to(953.90±175.30)mg·min·L^(-1)at 10 h,which was equivalent to that of intragastric administration at a dose of 10 mg/kg.Moreover,the plasma concentration of 1 in rats in the transdermal administration group did not show a decreasing trend within 10 h.This study demonstrated that the preparation process of 1 cream was simple and easy to be industrialized,and the prepared cream had good transdermal absorption and could release the drug stably for a long time,providing a reference for the further development and application of 1.

关 键 词：阿魏酸 抗炎 乳膏 经皮渗透 药物动力学 BOX-BEHNKEN设计 响应面法 

分 类 号：R944.21[医药卫生—药剂学] R283.6[医药卫生—药学]