~3H-黄柏,~3H-小檗碱的经皮渗透
PERCUTANEOUS PENETRATION OF ~3H-HUANGBAI EXTRACTS AND H~3-BERBERINE
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摘要: 采用放射性~3H标记黄柏提取物及主要组分小檗碱,利用离体皮肤渗透装置,进行离体皮肤渗透研究。对实验结果作数学模型分析。研究发现黄柏液和小檗碱水溶液或乙二醇溶液在0.99μg/cm~2和0.82μg/cm~2以上剂量组可经豚鼠皮肤和人皮渗透。黄柏水溶液高剂量组33.50μg/cm~2经豚鼠皮肤在10h的渗透速率和渗透率分别为1.30ng/min·cm~2和2.33%.比人皮0.77ng/min·cm~2和1.38为快。小檗碱水溶液高剂量组28.64μg/cm~2在9.5h经豚鼠的渗透速率和渗透率为0.45ng/min·cm和0.89%,比经人皮0.22ng/min·cm~2和0.46%快。用乙二醇作溶剂时,可显著加快黄柏、小檗碱经豚鼠皮肤的穿透。用数学方法分析求得通透常数K_p,发现黄柏、小檗碱乙二醇溶液经豚鼠皮K_p>其相应的水溶液的K_p;黄柏、小檗碱水溶液经人皮的K_p>经豚鼠皮肤的K_p.K_P值与相应的渗透速率、渗透量相一致。黄柏和小檗碱水溶液或乙二醇溶液经人皮吸收的延搁期>经豚鼠的延搁期。Abstract: The percutaneous penetration of ~3H-huangbai extracts and ~3H-berberine through excised guinea pig and human shins was studied using the static diffusion cell technique. The data were treated with mathematical model of skin absorption. The results showed that huangbai extracts and berberine could penetrate the guinea pig and human skins at (above) dose of 8.38 ug/cm~2 and 14.32 ug/cm~2, respectively. The amount and rate of penetration increased linearly with the time of exposure and dose. The permeability of berberine through guinea pig and human skins in two vehicles (water and glycol) was lower than that of huangbai extracts. When Huangbai extracts and berberine were applied in glycol solution, the vehicle greatly enhanced the penetration of the two penetrants. It was found that K_p(perme ability constant) of two penetrants through two kinds of skin decreased in following order: K_p of huangbai in glycol through guinea pig skin >K_p of huangbai in water through guinea pig skin >K_p of huangbai in water through human skin >K_p of berberine in glycol through guinea pig skin >K_p of berberine in water through human skin. The lag time of two penetrants through human skin was longer than that through guinea pig skin.