甲氧胺酸透皮贴剂的配方、表征及体外评价。

Journal of drug delivery Pub Date : 2017-01-01 Epub Date: 2017-11-12 DOI:10.1155/2017/7358042
Jirapornchai Suksaeree, Patsakorn Siripornpinyo, Somruethai Chaiprasit
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引用次数: 16

摘要

透皮贴剂中甲氧胺酸的结晶是造成贴剂不稳定和药物释放降低的主要问题。该添加剂用于抑制甲氧胺酸的结晶。在不同类型的添加剂中,研究了聚乙烯吡咯烷酮(PVP) K30和PVP K90对药物结晶的抑制效果较好。PVP在基质贴片中作为甲氧胺酸的增溶剂,在PVP K30和PVP K90的药物与PVP的比例分别为1:2和1:2.5和1:1.5和1:2。表征结果显示基质斑块为均匀斑块,无甲氧胺酸的结晶形态。用Franz扩散池研究了甲氧胺酸在贴片中的释放特性。当PVP作为结晶抑制剂时,在前1 h内甲氧胺酸从斑块中的释放行为明显增加。然而,我们发现药物与PVP K90的比例为1:2时,对增加贴片的药物释放最有效。因此,PVP可以作为甲氧胺酸在基质贴片中的结晶抑制剂,增加药物的释放。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Formulation, Characterization, and In Vitro Evaluation of Transdermal Patches for Inhibiting Crystallization of Mefenamic Acid.

The crystallization of mefenamic acid in transdermal patch is a major problem that makes the patch unstable and decreases the drug release. The additive was used to inhibit crystallization of a mefenamic acid. Among the different types of additives, polyvinylpyrrolidone (PVP) K30 and PVP K90 were studied and found to be highly effective in inhibiting the crystallization of the drug. The PVP presented as a solubilizer agent for mefenamic acid in matrix patches at the different ratio between drug : PVP, 1 : 2 and 1 : 2.5 for using PVP K30 and 1 : 1.5 and 1 : 2 for using PVP K90. The characterizations showed the homogeneous patches without the crystal form of the mefenamic acid in matrix patches. The release profiles of the mefenamic acid from the patches were investigated by Franz diffusion cells. Over the first 1 h, the release behavior of mefenamic acid from the patches obviously increased when PVP was used as a crystallization inhibitor. However, the ratio between drug : PVP K90 at 1 : 2 was found to be the most effective in increasing the drug release from patch. Thus, the PVP could be used as a crystallization inhibitor for mefenamic acid in matrix patches which will increase the drug release.

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Journal of drug delivery
Journal of drug delivery PHARMACOLOGY & PHARMACY-
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