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制备和评价用于吡罗昔康透皮给药的 Eudragit 聚合物膜。

Fabrication and evaluation of Eudragit polymeric films for transdermal delivery of piroxicam.

机构信息

a Department of Pharmacy, Faculty of Pharmacy , Mahidol University , Bangkok , Thailand.

b Center of Excellence in Innovative Drug Delivery and Nanomedicine, Faculty of Pharmacy , Mahidol University , Bangkok , Thailand.

出版信息

Pharm Dev Technol. 2018 Oct;23(8):771-779. doi: 10.1080/10837450.2017.1319864. Epub 2017 May 2.

Abstract

The aims of this work were to develop and characterize the prolonged release piroxicam transdermal patch as a prototype to substitute oral formulations, to reduce side effects and improve patient compliance. The patches were composed of film formers (Eudragit) as a matrix backbone, with PVC as a backing membrane and PEG200 used as a plasticizer. Results from X-ray diffraction patterns and Fourier transform-infrared spectroscopy indicated that loading piroxicam into films changed the drug crystallinity from needle to an amorphous or dissolved form. Piroxicam films were prepared using Eudragit RL100 and Eudragit RS100 as film formers at various ratios from 1:0 to 1:3. Films prepared solely by Eudragit RL100 showed the toughest and softest film, while other formulations containing Eudragit RS100 were hard and brittle. Drug release kinetic data from the films fitted with the Higuchi model, and the piroxicam release mechanism was diffusion controlled. Among all formulation tested, Eudragit RL100 films showed the highest drug release rate and the highest drug permeation flux across human epidermal membrane. Increasing drug loading led to an increase in drug release rate. Eudragit can be used as a film former for the fabrication of piroxicam films.

摘要

本工作旨在开发并表征一种吡罗昔康透皮贴片,作为替代口服制剂的原型,以减少副作用并提高患者顺应性。贴片由成膜剂(Eudragit)作为基质骨架、聚氯乙烯(PVC)作为背衬膜、聚乙二醇 200(PEG200)作为增塑剂组成。X 射线衍射图谱和傅里叶变换红外光谱的结果表明,将吡罗昔康载入薄膜会使药物结晶度从针状变为无定形或溶解状态。吡罗昔康薄膜是用 Eudragit RL100 和 Eudragit RS100 以 1:0 至 1:3 的不同比例作为成膜剂制备的。仅由 Eudragit RL100 制备的薄膜显示出最坚韧和最柔软的薄膜,而其他含有 Eudragit RS100 的配方则坚硬易碎。薄膜的药物释放动力学数据符合 Higuchi 模型,药物释放机制为扩散控制。在所有测试的配方中,Eudragit RL100 薄膜显示出最高的药物释放率和最高的药物渗透通量通过人表皮膜。增加药物载药量会导致药物释放率增加。Eudragit 可用作制备吡罗昔康薄膜的成膜剂。

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