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羧甲基栓皮栎胶新型 pH 敏感物理水凝胶。

Novel pH-sensitive physical hydrogels of carboxymethyl scleroglucan.

机构信息

Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, 00185 Rome, Italy.

出版信息

J Pharm Sci. 2012 Jan;101(1):256-67. doi: 10.1002/jps.22766. Epub 2011 Sep 23.

DOI:10.1002/jps.22766
PMID:21953550
Abstract

A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-gel transitions even in the absence of salts. Swelling experiments, performed on freeze-dried samples in different media, showed good affinity of these hydrogels toward the aqueous media and a pH-sensitive behavior. Four nonsteroidal anti-inflammatory drugs (NSAIDs) were loaded into the physical hydrogels obtained from 2.0% (w/v) solutions of the polymer. The results of the release studies carried out in conditions simulating the gastrointestinal tract showed that the new hydrogels could be suggested for the modified oral delivery of NSAIDs, particularly damaging for the gastric mucosa. In vivo studies proved the biocompatibility of the matrix and the absence of any gastric damage for administration of ulcerogenic doses of diclofenac loaded into the hydrogel (DIC/Scl-CM-300). Moreover, DIC/Scl-CM-300 was found to be effective in peripheral analgesia.

摘要

一种羧甲基化程度为 300±10 的支链淀粉(Scl-CM)衍生物通过傅里叶变换红外光谱、电位滴定、粘液粘附研究和流变学测量进行了合成和表征。流变学测量表明,即使在没有盐的情况下,该聚合物也具有进行溶胶-凝胶转变的能力。在不同介质中对冻干样品进行的溶胀实验表明,这些水凝胶对水相具有良好的亲和力,并具有 pH 敏感性。将四种非甾体抗炎药 (NSAIDs) 负载到由聚合物 2.0%(w/v)溶液获得的物理水凝胶中。在模拟胃肠道条件下进行的释放研究结果表明,新的水凝胶可用于 NSAIDs 的改良口服递药,尤其是对胃粘膜有损伤的 NSAIDs。体内研究证明了基质的生物相容性,并且负载致溃疡剂量的双氯芬酸的水凝胶(DIC/Scl-CM-300)给药不会造成任何胃损伤。此外,DIC/Scl-CM-300 在外周镇痛方面也被证明是有效的。

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