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Synthesis and evaluation of chitosan-graft-poly (2-hydroxyethyl methacrylate-co-itaconic acid) as a drug carrier for controlled release of tramadol hydrochloride

机译:壳聚糖-接枝-聚(甲基丙烯酸2-羟乙酯-衣康酸)药物的合成及评价,用于盐酸曲马多的控释

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Chitosan-graft-poly (2-hydroxyethyl methacrylate-co-itaconic acid) has been synthesized for different feed ratios of 2-hydroxyethyl methacrylate and itaconic acid and characterized by FT-IR, thermogravimetry and swelling in simulated biological fluids (SBF) and evaluated as a drug carrier with model drug, tramadol hydrochloride (TRM). Grafting decreased the thermal stability of chitosan. FT-IR spectra of tablet did not reveal any molecular level (i.e. at 100nm level. The observed Korsmeyer-Peppas's power law exponents (0.19-1.21) for the in vitro release profiles of TRM in SBF and other drugs such as 5-fluorouracil (FU), paracetamol (PCM) and vanlafaxine hydrochloride (VNF) with the copolymer carriers revealed an anomalous drug release mechanism. The decreased release rates for the grafted chitosan and the enhanced release rate for the grafts with increasing itaconic acid content in the feed were more likely attributed to the enhanced drug-matrix interaction and polymer-SBF interactions, respectively. The different release profiles of FU, PCM, TRM and VNF with the copolymer matrix are attributed to the different chemical structures of drugs. The above features suggest the graft copolymer's candidature for use as a promising oral drug delivery system.
机译:针对甲基丙烯酸2-羟乙酯和衣康酸的不同进料比,合成了壳聚糖-接枝-聚(甲基丙烯酸2-羟乙酯-衣康酸),并通过FT-IR,热重分析和在模拟生物流体(SBF)中的溶胀进行了表征。作为带有模型药物的盐酸曲马多(TRM)的药物载体。接枝降低了壳聚糖的热稳定性。片剂的FT-IR光谱未显示任何分子水平(即在100nm水平。观察到的Korsmeyer-Peppas的幂定律指数(0.19-1.21),用于SBF和其他药物(如5-氟尿嘧啶)中TRM的体外释放曲线。 FU,聚对乙酰氨基酚(PCM)和盐酸文拉法辛(VNF)与共聚物载体一起揭示了一种异常的药物释放机理,随着饲料中衣康酸含量的增加,接枝壳聚糖的释放速率降低,接枝的释放速率提高。 FU,PCM,TRM和VNF与共聚物基质的不同释放曲线分别归因于药物的不同化学结构,上述特征表明接枝共聚物的结构可能与药物-基质相互作用和聚合物-SBF相互作用增强有关。候选人资格用作有前途的口服药物递送系统。

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