[氢化大豆卵磷脂在固体分散体和油性凝胶中的应用及皮肤应用配方研究]。

IF 0.3 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Makiko Fujii
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引用次数: 0

摘要

我一直在研究利用固体分散体和皮肤应用制剂提高药物溶解度的问题。以磷脂酰胆碱(PC)为载体制备固体分散体时,具有氢供体基团的药物会与 PC 相互作用,生成药物含量高的无定形固体分散体,从而改善药物的吸收。药物在用透明卵磷脂形成的油基凝胶中得到溶解和过饱和;这有利于药物通过皮肤的渗透。由于油本身的皮肤渗透性以及随之而来的药物溶解度和在皮肤中的扩散系数的增加,促进作用因所用油的性质而异。在实际用量为 10 µL/cm2 或更小的情况下,吸收性差的药物的皮肤渗透性取决于油的分子量和表面张力。油性载体对上层角质层的渗透影响着药物对角质层的到达;角质层第 7 层附近的高药物浓度会通过增加深层的线性浓度梯度来促进药物在皮肤中的迁移。此外,我们还与毒理学专家合作,对皮肤安全性进行了风险评估,其中包括物质的毒性潜力以及与皮肤转移相关的部分。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Application of Hydrogenated Soya Lecithin in Solid Dispersion and Oily Gel, and the Study of Skin-Applied Formulations].

I have been studying the improvement of drug solubility using solid dispersion and skin-applied formulations. When preparing solid dispersions using phosphatidylcoline (PC) as a carrier, drug with hydrogen-donating groups interacts with PC to produce amorphous solid dispersions with high drug content; this overcomes improves drug absorption. The drug was solubilized and supersaturated in the oil-based gel formed with hyadrogenated lecithin; this facilitates drug permeation through the skin. The promoting effect differs with the nature of the oil used because of the skin penetration of the oil itself and the accompanying increase in drug solubility and diffusion coefficient in the skin. At actual application volumes of 10 µL/cm2 or less, the skin penetration of poorly-absorbable drugs depends on the molecular weight and surface tension of the oil. The penetration of the oil vehicle into the upper stratum corneum influences the reach of the drug into the stratum corneum; a high drug concentration near the 7th layer of the stratum corneum promotes migration through the skin by increasing the linear concentration gradient in deeper layers. In addition, we performed a risk assessment, in collaboration with toxicologists, for dermal safety that included the toxicity potential of substances and the parts related to skin transfer.

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来源期刊
CiteScore
0.60
自引率
0.00%
发文量
169
审稿时长
1 months
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