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基于聚乙烯吡咯烷酮的溶解型微针系统用于琥珀酸舒马普坦的体外给药。

Dissolving polyvinylpyrrolidone-based microneedle systems for in-vitro delivery of sumatriptan succinate.

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 Mar 1;114:84-92. doi: 10.1016/j.ejps.2017.11.031. Epub 2017 Dec 15.

DOI:10.1016/j.ejps.2017.11.031
PMID:29203152
Abstract

In-vitro permeation studies were conducted to assess the feasibility of fabricating dissolving-microneedle-array systems to release sumatriptan succinate. The formulations consisted mainly of the encapsulated active ingredient and a water-soluble biologically compatible polymer, polyvinylpyrrolidone (PVP), approved by the U.S. Food and Drug Administration (FDA). Tests with Franz-type diffusion cells and Göttingen minipig skins showed an increase of the transdermal flux compared to passive diffusion. A preparation, containing 30% by mass of PVP and 8.7mg sumatriptan, produced a delivery rate of 395±31μg/cmh over a 7-hour period after a negligible lag time of approximately 39min. Theoretically, a 10.7cm microneedle-array patch loaded with 118.8mg of the drug would provide the required plasma concentration, 72ng/mL, for nearly 7h.

摘要

进行了体外渗透研究,以评估制造可溶解微针阵列系统以释放舒马曲坦琥珀酸盐的可行性。这些配方主要由包封的活性成分和美国食品和药物管理局 (FDA) 批准的水溶性生物相容聚合物聚乙烯吡咯烷酮 (PVP) 组成。使用 Franz 型扩散池和哥廷根小猪皮进行的测试表明,与被动扩散相比,透皮通量增加。一种制剂,含有 30%质量的 PVP 和 8.7mg 舒马曲坦,在大约 39 分钟的可忽略的滞后时间后,在 7 小时的时间内产生了 395±31μg/cmh 的输送速率。从理论上讲,负载有 118.8mg 药物的 10.7cm 微针阵列贴片将提供所需的血浆浓度 72ng/mL,持续近 7 小时。

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