摘要
目的探讨pH值对酮洛芬理化性质及经皮渗透性能的影响,为其制备微乳凝胶研究提供实验依据。方法使用高效液相色谱(HPLC)法测定酮洛芬在水和pH值分别为5.0,6.8,7.4,8.0,9.0下的平衡溶解度(S)、表观油水分配系数(P)、稳态渗透速率(Js)、渗透系数(Ps);采用多元线性回归建立药物的离体透皮参数与pH值、S、P的相关性。结果32℃时,酮洛芬属难溶性药物,在pH值为7.4时,溶解度、Js、Ps均最大,P最小;多元线性回归结果显示pH值、S、P与Js成线性相关性,回归方程为:Js=-0.268pH+1.099 S-0.141 P+92.121。结论通过调节pH值,可以改善酮洛芬的S、P、Js,通过结果分析在pH值为7.4的磷酸盐缓冲液(PBS)溶液中,酮洛芬可获得较高的溶解度、脂溶性及皮肤通透性。
Objective To study the effect of pH value on the physicochemical properties and in-vitro percutaneous permeability of ketoprofen(KP)and to provide experimental basis for the preparation of microemulsion gel.Methods HPLC method was used to determine the equilibrium solubility(S),apparent oil water partition coefficient(P),steady state permeability rate(Js),and permeability coefficient(Ps)of KP in water and phosphate buffer saline(PBS)when pH values was 5.0,6.8,7.4,8.0,and 9.0,respectively.Multiple linear regression was used to establish the correlation between the in vitro transdermal parameters,pH,S and P.Results At 32℃,KP is insoluble in water.In the PBS of pH 7.4,KP showed largest equilibrium solubility,Js and Ps.The multivariate linear regression results showed that pH,S,P and Js are linearly correlated.The regression equation was:Js=-0.268 pH+1.099S-0.141 P+92.121.Conclusion By adjusting the pH,the S,P,and Js of the KP can be improved.According to the results,the KP can obtain higher solubility,lipid solubility,and skin permeability in a PBS solution with a pH of 7.4.
作者
于秋菊
王晓丽
YU Qiuju;WANG Xiaoli(Xuzhou Vocational College of Bioengineering,Xuzhou 221006,China;Department of Pharmacy,Jiangsu Cancer Hospital,Nanjing 210018,China)
出处
《医药导报》
CAS
北大核心
2020年第9期1281-1284,共4页
Herald of Medicine
关键词
酮洛芬
PH值
透皮
多元线性回归
Ketoprofen
pH
Percutaneous permeation
Multiple linear regression
