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用于结肠特异性抗生素药物递送的新型装置——欧车前以及甲基丙烯酸2-羟乙酯与丙烯酰胺的共聚物

Psyllium and copolymers of 2-hydroxylethylmethacrylate and acrylamide-based novel devices for the use in colon specific antibiotic drug delivery.

作者信息

Singh Baljit, Chauhan Nirmala, Kumar S, Bala Ritu

机构信息

Department of Chemistry, Himachal Pradesh University, Shimla 171005, India.

出版信息

Int J Pharm. 2008 Mar 20;352(1-2):74-80. doi: 10.1016/j.ijpharm.2007.10.019. Epub 2007 Oct 24.

Abstract

In order to utilize the psyllium husk, a medicinally important natural polysaccharide, to develop the hydrogels meant for the drug delivery, we have prepared psyllium 2-hydroxylethylmethacrylate (HEMA) and acrylamide (AAm)-based polymeric networks by using N,N'-methylenebisacrylamide (N,N'-MBAAm) as crosslinker and ammonium persulfate (APS) as initiator. The polymeric networks thus formed [psy-cl-poly(HEMA-co-AAm)] were characterized with FTIR and swelling studies which were carried out as a function of crosslinker concentration, time, pH and [NaCl] of the swelling medium. The swelling kinetics of the hydrogels and in vitro release dynamics of model drug (tetracycline hydrochloride) from these hydrogels has been studied for the evaluation of swelling mechanism and drug release mechanism from the hydrogels. The values of the diffusion exponent 'n' have been obtained 0.5 for both swelling kinetics and drug release dynamics. This value shows that the Fickian type diffusion mechanism has occurred for the swelling of the polymers and for the release of drug from the polymers in different release mediums. The values of the initial diffusion coefficients (10.6 x 10(-4), 13.1 x 10(-4), 14.0 x 10(-4))cm(2)/min, average diffusion coefficients (22.2 x 10(-4), 25.7 x 10(-4), 27.0 x 10(-4))cm(2)/min and late diffusion coefficients (1.68 x 10(-4), 2.15 x 10(-4), 2.28 x 10(-4))cm(2)/min for the release of tetracycline HCl respectively in distilled water, pH 2.2 buffer and pH 7.4 buffer from the drug loaded samples shows that in the initial stages, the rate of release of drug from the hydrogels is slow and rate of diffusion of drug increases with time.

摘要

为了利用药用重要天然多糖车前子壳来开发用于药物递送的水凝胶,我们以N,N'-亚甲基双丙烯酰胺(N,N'-MBAAm)为交联剂、过硫酸铵(APS)为引发剂,制备了基于甲基丙烯酸2-羟乙酯(HEMA)和丙烯酰胺(AAm)的车前子聚合物网络。对由此形成的聚合物网络[psy-cl-聚(HEMA-co-AAm)]进行了傅里叶变换红外光谱(FTIR)表征和溶胀研究,溶胀研究是作为交联剂浓度、时间、pH值和溶胀介质的[NaCl]的函数进行的。研究了水凝胶的溶胀动力学以及模型药物(盐酸四环素)从这些水凝胶中的体外释放动力学,以评估水凝胶的溶胀机制和药物释放机制。对于溶胀动力学和药物释放动力学,扩散指数“n”的值均为0.5。该值表明,聚合物的溶胀以及药物在不同释放介质中从聚合物中的释放均发生了菲克型扩散机制。载药样品在蒸馏水、pH 2.2缓冲液和pH 7.4缓冲液中释放盐酸四环素的初始扩散系数值(10.6×10⁻⁴、13.1×10⁻⁴、14.0×10⁻⁴)cm²/min、平均扩散系数值(22.2×10⁻⁴、25.7×10⁻⁴、27.0×10⁻⁴)cm²/min和后期扩散系数值(1.68×10⁻⁴、2.15×10⁻⁴、2.28×10⁻⁴)cm²/min表明,在初始阶段,药物从水凝胶中的释放速率较慢,且药物的扩散速率随时间增加。

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