渗透、代谢和行动网站烟酸衍生品的浓度在人类皮肤。与局部相关药理效应。

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穆勒B,卡斯帕米,surb C, Imanidis G

渗透、代谢和行动网站烟酸衍生品的浓度在人类皮肤。与局部相关药理效应。

欧元J制药科学。2003年10月,20 (2):181 - 95。

PubMed ID

14550884 (在PubMed

]

文摘

小说的方法建立烟酸甲酯的药物量效关系,己烟酸和烟酸作为周边皮肤血管舒张药后局部应用研究。这种方法涉及到评估游离药物浓度的水舱现场行动的组织,称为C(*),评估相关浓度负责药理效应。旁边的毛细血管epidermis-dermis边界被假定是行动的相关网站。C(*)从毒品运输参数估计对不同层次的人类尸体的皮肤体外决定。免疫组织化学研究表明,分离的平面皮肤通过热处理是表皮的基底细胞和板之间最亮的星,证实表皮和真皮的完整性用于实验。表皮的渗透速率大大增加,增加药物的亲油性。真皮渗透是大致相同的所有三个化合物。表皮所代表的主要运输屏障体外烟酸甲酯烟酸和烟酸但不己。期间烟酸酯的代谢组织渗透在某种程度上是相当有限的表皮真皮但非常明显。非特异性alpha-naphthylacetate-esterase活动主要位于真皮,在协议与新陈代谢的结果。 The drugs were applied each at three different concentrations in vivo to the ventral forearm of healthy human volunteers and vasodilation was evaluated based on skin erythema which was quantified by measuring colour change of reflected light. Area under the curve of the change of colour co-ordinates as a function of time was used as a measure of pharmacological effect. The pharmacological effect of all three drugs was comparable when similar C(*) values were considered, even though the concentrations applied to the skin differed by orders of magnitude. The effect showed a strong positive dependence on C(*). Methyl and hexyl nicotinate showed identical, nearly sigmoidal effect/C(*)-profiles, while the profile for nicotinic acid was linear, suggesting a possible difference in the intrinsic pharmacological potency between the esters and the acid. These results demonstrate the validity of C(*) as the relevant drug concentration for the cutaneous pharmacological effect of the topically applied drugs and underline the usefulness of the presented methodology for establishing dose-response relationships in dermal therapy and expressing bioavailability.

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药物

烟酸甲酯