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阿拉伯木聚糖的巯基化及其在 pH 敏感的巯基化阿拉伯木聚糖接枝丙烯酸共聚物制备中的应用。

Thiolation of arabinoxylan and its application in the fabrication of pH-sensitive thiolated arabinoxylan grafted acrylic acid copolymer.

机构信息

a Faculty of Pharmacy , University of Sargodha , Sargodha , Pakistan.

b Department of Pharmacy , University of Agriculture , Faisalabad , Pakistan.

出版信息

Drug Dev Ind Pharm. 2019 May;45(5):754-766. doi: 10.1080/03639045.2019.1569041. Epub 2019 Feb 11.

Abstract

Current research work was conducted to synthesize Thiol modified arabinoxylan and its application in fabrication of hydrogel. Thioglycolic acid was esterified with arabinoxylan to prepare Thiolatedarabinoxylan. Appearance of peak at 2533.34 cm in FTIR and thiol content showed successful thiolation. The pH-dependent Thiolatedarabinoxylan/acrylic acid (TAX/AA) hydrogels of perindopril erbumine were prepared via free-radical co-polymerization. Perindopril erbumine (PE) was employed as model drug. Different batches with different feed ratio of TAX, AA, and MBA were prepared and their influence on swelling, solvent penetration, and consequent drug release was investigated. Swelling coefficients increased with increase in pH. TAX/AA hydrogels were characterized by Fourier-transform infrared spectroscopy (FT-IR), Thermal Analysis (TA), X-Ray diffraction (XRD), and scanning electron microscope (SEM). Dissolution studies were performed at pH 1.2 and 7.4 in which drug release showed direct correlation with TAX and AA ratio. In vivo studies showed that C of TAX-co-AA based hydrogel was 81.57 ± 0.35 ng/ml which was maintained for a longer time after its administration. All the results of in vivo studies were significant and TAX-co-AA based hydrogel enhances the bioavailability of perindopril erbumine.

摘要

目前的研究工作旨在合成巯基修饰的阿拉伯木聚糖及其在水凝胶制备中的应用。用硫代乙醇酸对阿拉伯木聚糖进行酯化,制备巯基化阿拉伯木聚糖。傅里叶变换红外光谱(FTIR)中 2533.34cm 处的峰和巯基含量表明成功进行了巯基化。通过自由基共聚制备了依那普利厄贝沙坦的 pH 依赖性巯基化阿拉伯木聚糖/丙烯酸(TAX/AA)水凝胶。依那普利厄贝沙坦(PE)被用作模型药物。制备了不同批次、TAX、AA 和 MBA 不同进料比的水凝胶,并研究了它们对溶胀、溶剂渗透和随后药物释放的影响。溶胀系数随 pH 值的增加而增加。TAX/AA 水凝胶的结构特征通过傅里叶变换红外光谱(FT-IR)、热分析(TA)、X 射线衍射(XRD)和扫描电子显微镜(SEM)进行了表征。在 pH 1.2 和 7.4 下进行了溶出度研究,药物释放与 TAX 和 AA 比例直接相关。体内研究表明,TAX-co-AA 水凝胶的 C 为 81.57±0.35ng/ml,给药后能维持更长时间。体内研究的所有结果均具有统计学意义,TAX-co-AA 水凝胶能提高依那普利厄贝沙坦的生物利用度。

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