Comparison of in vitro Percutaneous Permeation Characteristics of Glycyrrhizic Acid in 6 Kinds of Glycyrrhetate Creams / 中国药房

OBJECTIVE:To compare in vitro percutaneous permeation characteristics of glycyrrhizic acid in 6 kinds of glycyrrhetate creams,and to provide reference for further development and utilization. METHODS:Modified Franz diffusion cell and isolated rat skin were adopted for in vitro percutaneous permeation test. 24 h accumulative permeation of glycyrrhizic acid in 6 kinds of glycyrrhetate creams(monoammonium glycyrrhizinate,diammonium glycyrrhizinate,monopotassium glycyrrhizinate, dipotassium glycyrrhizate,trisodium glycyrrhizinate,disodium glycyrrhetate)were determined by HPLC. The permeation characteristics of 6 kinds of glycyrrhetate creams were evaluated by calculating percutaneous absorption rate. RESULTS:24 h accumulative permeation of 6 kinds of glycyrrhetate in rat skin in descending order was as follows:trisodium glycyrrhizinate (23.933 μ g/cm2)>dipotassium glycyrrhizinate(22.952 μ g/cm2)>disodium glycyrrhizinate(15.424 μ g/cm2)>monopotassium glycyrrhizinate(10.703 μg/cm2)>diammonium glycyrrhizinate(9.557 μg/cm2)>monoammonium glycyrrhizinate(1.621 μg/cm2). The percutaneous permeation rate in descending order was as follows as trisodium glycyrrhizinate [1.010 2 μ g/(cm2·h)]>dipotassium glycyrrhizinate [0.974 5 μg/(cm2·h)]>disodium glycyrrhizinate [0.641 2 μg/(cm2·h)]>diammonium glycyrrhizinate [0.399 9 μg/(cm2·h)]>monopotassium glycyrrhizinate[0.362 8 μg/(cm2·h)]>monoammonium glycyrrhizinate[0.072 6 μg/(cm2·h)]. CONCLUSIONS:The permeation rate of trisodium glycyrrhizinate is the highest among 6 kinds of glycyrrhetate creams in vitro.

In Vitro Inhibition of Cytochrome P450 in Rats Liver Microsomes by Shuanghuanglian Injection Powder and Its Active Components / 医药导报

Objective To evaluate the inhibition effects of shuanghuanglian injection powder and its active components on the activities of CYP1A,CYP 2D and CYP 3A in rats liver microsomes. Methods Three probe substrates including phenacetin for CYP1A,dextromethorphan for CYP2D and midazolam for CYP3A were incubated with shuanghuanglian injection powder and the active components (baicalin,phillyrin,forsythiaside A,lutin,chlorogenic acid,coffeic acid and lutiolin) in rat liver microsomes. Contents of three probe substrates were simultaneously determined by HPLC to evaluate the metabolic rates. Results Shuanghuanglian injection powder and baicalin inhibited the activities of CYP2D and CYP 3A, but didn 't affect CYP1A. The other active components showed no effect on CYP1A,CYP2D and CYP3A. Conclusion Drug-drug interactions may occur when combining shuanghuanglian powder injection with CYP2D and CYP 3A substrates and baicalin may be the effector substance responsible for the interactions.