benzofurans and paeonol

To study the relationship between deposition content and time of the active ingredients in rat skin, and investigate the dermatopharmacokinetics of Liangfu Cream.. The contents of paeonol, dictamnine, fraxinellone and glycyrrhetinic acid in rat skin were determined by HPLC. The dermatopharmacokinetics parameters were calculated by DAS software.. The dermatopharmacokinetics of paeonol and glycyrrhetinic acid were two compartment model, while that of dictamnine and fraxinellone were one compartment model: T(1/2Ka) of four active ingredients were 0.307, 0.112, 0.146, 0.216 h, respectively; T(lag) of them were 0.006, 0.123, 0.136, 0.109 h, respectively; all the Tmax of them was 0.5 h; the Cmax, were 40.163, 1.607, 6.725, 100.553 microg x cm(-3), respectively; the t(1/2beta), were 14.719, 1.262, 0.838, 234.807 h, respectively; the AUC(0-infinity), were 16.987, 2.713, 9.345, 697.000 microg x cm(-3) x h(-1), respectively; and the MRT(0-infinity) were 3.662, 1.67, 1.585, 10.897, respectively.. The skin pharmacokinetics characteristic of four ingredients in Liangfu cream is lined with the cataplasm long time.

Topics: Acetophenones; Administration, Cutaneous; Animals; Benzofurans; Drugs, Chinese Herbal; Glycyrrhetinic Acid; Male; Mice; Quinolines; Skin

To study the effects of different penetration enhancers on the in vitro percutaneous absorption and amount retained in skin of active ingredients in Liangfu cream and to screen out the effective accelerator.. Using improved Franz-type difusion cell and excised small mouse skin in vitro as transdermal barrier, the amount retained in skin and kinetics parameters of active ingredients such as cumulative permeation quantity, permeation rate and permeation lagged time were determined by HPLC. The enhancement ability of four different enhancers such as azone, oleic acid, transcutol P and isopropyl myristate were investigated.. 3% IPM enhanced the cumulative permeation quantity better than other penetration enhancers. The enhancive permeation multiples of paeonol, dictamnine, fraxinellone and glycyrrhetinic acid were 1.52, 1.24, 1.73 and 3.21 times (P < 0.05). The enhancive amount retained in skin multiple of glycyrrhetinic acid was 1.96 times (P < 0.05), but for other components there were no significant impacts.. The effects of penetration enhancers on the in vitro percutaneous absorption and amount retained in skin of components in Liangfu cream are different. 3% IPM which can enhance the cumulative permeation quantity of four components and amount retained in skin of glycyrrhetinic acid is the most suitable penetration enhancer for Liangfu cream.

Topics: Acetophenones; Administration, Cutaneous; Animals; Benzofurans; Drug Carriers; Drugs, Chinese Herbal; Glycyrrhetinic Acid; Male; Mice; Quinolines; Skin; Skin Absorption