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使用流通扩散池系统评估乙醇酸通过人体皮肤切片的体外经皮吸收情况。

Assessment of in vitro percutaneous absorption of glycolic acid through human skin sections using a flow-through diffusion cell system.

作者信息

Jiang M, Qureshi S A

机构信息

Therapeutic Products Directorate (2202C1), Health Canada, Ottawa, ON.

出版信息

J Dermatol Sci. 1998 Dec;18(3):181-8. doi: 10.1016/s0923-1811(98)00039-5.

Abstract

UNLABELLED

The percutaneous absorption studies were performed using a flow-through diffusion cell system with skin specimens from 24 healthy women to assess the penetration of glycolic acid (GA). Percentages of GA, based on 14C-labelled activity, found in the skin after application of 4% GA at pH 2.0 or pH 3.8, after 24 h were as follows: stratum corneum (SC)= 2.65+/-1.80 versus 1.13+/-1.14 (P<0.05); viable skin (VS)= 13.46+/-7.44 versus 2.23+/-1.51 (P< 0.05) and effluent fraction (EF) = 12.22+/-9.03 versus 1.42+/-0.77 (P < 0.05), respectively. The applications of 4-60%, GA at their native pH resulted in an increased penetration of GA through the skin. For example, application of 20% GA, pH 1.9, resulted in the following values: SC = 2.69+/-2.26 (P > 0.05); VS = 4.88+/-4.05 (P > 0.05) and EF = 30.69+/-13.25 (P < 0.05). Duration of application also affected the extent of penetration of drug. For example, application of 20% GA, pH 1.9, for 6 h resulted in the following levels: SC = 1.16+/-0.80 (P < 0.05); VS = 4.07+/-1.78 (P > 0.05) and EF = 6.12+/-4.95 (P < 0.05).

IN CONCLUSION

(i) absorption of GA in human skin are pH-, strength- and time-dependent; and (ii) the in vitro method appears to provide an appropriate model to reflect in vivo absorption of GA through human skin.

摘要

未标注

采用流通扩散池系统对24名健康女性的皮肤标本进行了透皮吸收研究,以评估乙醇酸(GA)的渗透情况。在pH 2.0或pH 3.8条件下应用4% GA后24小时,基于14C标记活性在皮肤中发现的GA百分比情况如下:角质层(SC)=2.65±1.80与1.13±1.14(P<0.05);活皮肤(VS)=13.46±7.44与2.23±1.51(P<0.05);流出液分数(EF)=12.22±9.03与1.42±0.77(P<0.05)。在其天然pH值下应用4%-60%的GA会导致GA透过皮肤的渗透率增加。例如,应用pH 1.9的20% GA,得到以下数值:SC = 2.69±2.26(P>0.05);VS = 4.88±4.05(P>0.05);EF = 30.69±13.25(P<0.05)。应用持续时间也会影响药物的渗透程度。例如,应用pH 1.9的20% GA 6小时,得到以下水平:SC = 1.16±0.80(P<0.05);VS = 4.07±1.78(P>0.05);EF = 6.12±4.95(P<0.05)。

结论

(i)GA在人体皮肤中的吸收呈pH值、浓度和时间依赖性;(ii)体外方法似乎能提供一个合适的模型来反映GA通过人体皮肤的体内吸收情况。

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