Huang Y B, Hsu L R, Wu P C, Ko H M, Tsai Y H
School of Pharmacy, Kaohsiung Medical College, Taiwan, Republic of China.
Gaoxiong Yi Xue Ke Xue Za Zhi. 1993 Jul;9(7):392-400.
To improve drug permeation through skin, extracts of crude drugs were evaluated using in vitro and in vivo penetration techniques with rabbit skin as a model membrane. The acetone extract of Amomum cardamomum (ae-AC) and Elettaria cardamomum (ae-EC) had the best effect in enhancing the penetration of Indomethacin (IDM). The flux of IDM for the formulation containing ae-AC from pH 7.4 buffer-alcohol donor solution was 3.6 times higher than that from the 50% alcohol donor solution. In order to confirm enhancer/skin interaction, a microscopic study was carried out in order to determine the presence of physical evidence in the skin caused by enhancers. A pharmacokinetic model of percutaneous absorption of IDM after topical administration was employed on the assumption of a zero-order penetration rate through the stratum corneum followed by absorption into the blood by a first-order process. Good correlation was observed between the experimental data point and simulated plasma concentration. From the results of the study, the in vitro permeability coefficient correlates with the in vivo penetration rate through the stratum corneum.
为提高药物经皮渗透能力，以兔皮为模型膜，采用体外和体内渗透技术对生药提取物进行了评估。小豆蔻丙酮提取物（ae - AC）和白豆蔻丙酮提取物（ae - EC）在增强吲哚美辛（IDM）渗透方面效果最佳。含ae - AC的制剂在pH 7.4缓冲液 - 乙醇供体溶液中IDM的通量比在50%乙醇供体溶液中高3.6倍。为确认促渗剂/皮肤相互作用，进行了微观研究以确定促渗剂在皮肤中引起的物理证据。在假定通过角质层的渗透速率为零级、随后通过一级过程吸收进入血液的前提下，建立了局部给药后IDM经皮吸收的药代动力学模型。实验数据点与模拟血浆浓度之间观察到良好的相关性。从研究结果来看，体外渗透系数与体内通过角质层的渗透速率相关。
