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中链甘油酯增强罂粟碱的皮肤渗透作用。

Enhanced skin permeation of papaverine by a medium chain glyceride.

作者信息

Okumura M, Nakamori Y, Sugibayashi K, Morimoto Y

机构信息

Omiya Research Laboratory, Nikken Chemicals Co., Ltd, Saitama, Japan.

出版信息

Drug Des Deliv. 1991 Apr;7(2):147-57.

PMID:1910439
Abstract

The mode and mechanism of action of Sefsol-318, a medium chain glyceride and a potent percutaneous absorption enhancer, on the in vitro permeation of papaverine hydrochloride through hairless rat skin were investigated and compared with those of laurocapram (Azone). The total amount of the drug delivered through excised skin over 28 h from aqueous solutions of the drug in which 5% S-318 or Azone was suspended was about 820 or 420 times higher, respectively, than from the solution alone. Experiments using liposomes as models, indicated that both the enhancers markedly increased the fluidity of lipid membranes. Skin conductance measurements in hairless rats indicated that they both also increased in vivo skin moisturizing and water holding capacity. These results suggest that the mechanism of action of Sefsol-318 and Azone in enhancing skin permeation are similar. But following in vitro pretreatment of the excised skin with 5% Sefsol-318 and aqueous emulsion for 2 h, skin permeation of papaverine hydrochloride through the pretreated skin was much lower than through non-treated skin in the presence of Sefsol-318. In contrast, the enhancing effect of Azone on the pretreated skin was similar to that of Azone on the in vitro non-treated skin. We found that, unlike Azone, Sefsol-318 disappeared from skin completely one day after 24 h-in vivo pretreatment of skin with aqueous gels containing each agent. In agreement, drug permeation through skin excised one day after the in vivo pretreatment with Sefsol-318 was almost the same as in non-pretreated controls without Sefsol-318. This difference in the mode of action of Sefsol-318 and Azone may arise from the difference in the residence times of these enhancers in skin.

摘要

研究了中链甘油酯Sefsol - 318(一种强效透皮吸收促进剂)对盐酸罂粟碱经无毛大鼠皮肤体外渗透的作用方式和作用机制,并与月桂氮卓酮(Azone)进行了比较。在含有5% S - 318或Azone的药物水溶液中,28小时内通过离体皮肤递送的药物总量分别比仅药物溶液高出约820倍或420倍。以脂质体为模型的实验表明,两种促进剂均显著增加了脂质膜的流动性。对无毛大鼠的皮肤电导测量表明,它们还增加了体内皮肤的保湿和持水能力。这些结果表明,Sefsol - 318和Azone促进皮肤渗透的作用机制相似。但是,用5% Sefsol - 318和水乳液对离体皮肤进行2小时的体外预处理后,在存在Sefsol - 318的情况下,盐酸罂粟碱通过预处理皮肤的渗透量远低于未处理皮肤。相比之下,Azone对预处理皮肤的增强作用与对体外未处理皮肤的增强作用相似。我们发现,与Azone不同,在用含每种药物的水凝胶对皮肤进行24小时体内预处理后一天,Sefsol - 318从皮肤中完全消失。同样,在用Sefsol - 318进行体内预处理一天后切除的皮肤的药物渗透与未用Sefsol - 318预处理的对照几乎相同。Sefsol - 318和Azone作用方式的这种差异可能源于这些促进剂在皮肤中停留时间的不同。

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