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基于聚乙烯吡咯烷酮的微针体外模拟释放和溶解舒马曲坦琥珀酸盐。

Modelling the in-vitro dissolution and release of sumatriptan succinate from polyvinylpyrrolidone-based microneedles.

机构信息

Otto H. York Department of Chemical, Biological and Pharmaceutical Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USA.

Otto H. York Department of Chemical, Biological and Pharmaceutical Engineering, New Jersey Institute of Technology, Newark, NJ 07102, USA.

出版信息

Eur J Pharm Sci. 2018 Dec 1;125:54-63. doi: 10.1016/j.ejps.2018.09.010. Epub 2018 Sep 14.

DOI:10.1016/j.ejps.2018.09.010
PMID:30223035
Abstract

A mathematical model was developed to predict the transport of sumatriptan molecules across the skin followed by absorption into the bloodstream. The drug was encapsulated in dissolving polyvinylpyrrolidone-based microneedles shaped in the form of pyramids. Mass balance equations were derived to simulate the dissolution and transport of the pharmaceutical ingredient. The theoretical framework made it possible to assess and predict the effects of key parameters on the release profile. The skin concentration increased with the loading dose and the height of the microneedle. An inverse relationship was noted between the amount of drug released in the dermal layer and the pitch width. These results were validated with in-vitro diffusion studies previously conducted using Göttingen minipig skin. The new mathematical approach successfully explained the in-vitro permeation of three different sumatriptan-containing formulations.

摘要

建立了一个数学模型来预测舒马曲坦分子穿过皮肤的传输,然后被吸收到血液中。药物被包裹在溶解的基于聚乙烯吡咯烷酮的微针中,这些微针被制成金字塔的形状。质量平衡方程被推导出来以模拟药物成分的溶解和传输。该理论框架使得评估和预测关键参数对释放曲线的影响成为可能。皮肤中的药物浓度随着加载剂量和微针的高度增加而增加。在皮层层中释放的药物量与节距宽度呈反比关系。这些结果与之前使用哥廷根小型猪皮肤进行的体外扩散研究进行了验证。新的数学方法成功地解释了三种不同的含有舒马曲坦的制剂的体外渗透。

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