使用丙烯酸基质的经皮硝酸甘油递送:设计,配方和体外表征。

ISRN Pharmaceutics Pub Date : 2014-01-06 eCollection Date: 2014-01-01 DOI:10.1155/2014/493245
Houman Savoji, Amir Mehdizadeh, Ahmad Ramazani Saadat Abadi
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引用次数: 9

摘要

采用不同的丙烯酸压敏胶(psa)和化学渗透增强剂(cpe)制备了硝酸甘油(TNG)透皮给药系统(TDDSs)。采用溶出法和改良的包套Franz扩散细胞与切除的大鼠腹部皮肤结合,评估了psa和cpe类型和浓度对装置皮肤渗透和体外药物释放的影响。结果表明,药物通过大鼠皮肤的渗透速率或稳态通量(jss)与丙烯酸酯PSA的粘度和类型以及CPE的类型有关。在不同的丙烯酸类ppe中,Duro-Tak 2516和Duro-Tak 2054表现出最高的jss, Duro-Tak 2051表现出最低的jss。在不同的cpe中,丙二醇和十六醇分别表现出最高和最低的TNG皮肤渗透增强作用。得到了器件的粘附性能,如180°剥离强度和探针粘性值。结果表明,CPE浓度的增加会导致PSA的粘附性能降低。此外,经过配方优化,发现在Duro-Tak 2054中使用10% PG作为CPE, 25%硝化甘油负载是一种有效的单片DIAP,用于开发硝酸甘油透皮治疗系统。
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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Transdermal nitroglycerin delivery using acrylic matrices: design, formulation, and in vitro characterization.

Nitroglycerin (TNG) transdermal drug delivery systems (TDDSs) with different acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) were prepared. The effects of PSAs and CPEs types and concentrations on skin permeation and in vitro drug release from devices were evaluated using the dissolution method as well as the modified-jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that the permeation rate or steady state flux (J ss) of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak 2516 and Duro-Tak 2054 showed the highest and Duro-Tak 2051 showed the lowest J ss. Among the various CPEs, propylene glycol and cetyl alcohol showed the highest and the lowest enhancement of the skin permeation of TNG, respectively. The adhesion properties of devices such as 180° peel strength and probe tack values were obtained. It was shown that increasing the concentration of CPE led to reduction in the adhesion property of PSA. Moreover, after optimization of the formulation, it was found that the use of 10% PG as a CPE and 25% nitroglycerin loading in Duro-Tak 2054 is an effective monolithic DIAP for the development of a transdermal therapeutic system for nitroglycerin.

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