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一种基于聚天冬酰胺的水凝胶:大鼠体内生物相容性及药物释放的表征与评价

A hydrogel based on a polyaspartamide: characterization and evaluation of in-vivo biocompatibility and drug release in the rat.

作者信息

Giammona G, Pitarresi G, Tomarchio V, Cacciaguerra S, Govoni P

机构信息

Dipartimento di Chimica e Tecnologie Farmaceutiche, Universitá di Palermo, Italy.

出版信息

J Pharm Pharmacol. 1997 Nov;49(11):1051-6. doi: 10.1111/j.2042-7158.1997.tb06040.x.

Abstract

This paper deals with the characterization of a new microparticulate hydrogel obtained by gamma irradiation of alpha, beta-poly[N-(2-hydroxyethyl)-DL-aspartamide] (PHEA). When enzymatic digestion of PHEA hydrogel was evaluated using various concentrations of pepsin and alpha-chymotrypsin no degradation occurred within 24 h. In-vivo studies showed that this new material is biocompatible after oral administration to rats. PHEA hydrogel was also studied as a system for delivery of diflunisal, an anti-inflammatory drug. In-vitro release studies in simulated gastrointestinal juice (pH 1 or 6.8) showed that most of the drug was released at pH 6.8. In-vivo studies indicated that diflunisal-loaded PHEA microparticles significantly improved the gastric tolerance and oral bioavailability of the drug in comparison with free diflunisal. These results suggest the potential application of PHEA hydrogel as a new delivery system for the oral administration of anti-inflammatory drugs.

摘要

本文研究了通过对α,β-聚N-(2-羟乙基)-DL-天冬酰胺进行γ辐射得到的新型微粒水凝胶的特性。当使用不同浓度的胃蛋白酶和α-胰凝乳蛋白酶评估PHEA水凝胶的酶消化情况时,24小时内未发生降解。体内研究表明,这种新材料经大鼠口服给药后具有生物相容性。PHEA水凝胶还被作为一种用于递送抗炎药双氯芬酸的系统进行了研究。在模拟胃肠液(pH 1或6.8)中的体外释放研究表明,大部分药物在pH 6.8时释放。体内研究表明,与游离双氯芬酸相比,负载双氯芬酸的PHEA微粒显著提高了该药物的胃耐受性和口服生物利用度。这些结果表明PHEA水凝胶作为一种新型抗炎药口服给药递送系统具有潜在的应用价值。

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