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使用乳糖酸微球实现吲哚美辛的pH敏感释放。

pH-sensitive release of indomethacin using lactan-acetate microspheres.

作者信息

Na K, Lee K Y

机构信息

Department of Chemical Technology, Chonnam National University, Kwangju, Korea.

出版信息

Drug Dev Ind Pharm. 1998 Jun;24(6):563-8. doi: 10.3109/03639049809085659.

Abstract

Hydrophobic lactan acetate was prepared from hydrophilic lactan gum by chemical modification and it was used for a pH-sensitive drug delivery system. Lactan acetate microspheres were prepared by the solvent evaporation method. The size of the microspheres prepared from lactan acetate was below 5 microns. The drug loading efficiencies of microspheres were approximately 70 and 80% at the initial amount of drug 40 and 80 mg, respectively. The microsphere showed pH-sensitive swelling behavior. The swelling capacity of microspheres at pH 7.4 was much greater than that at pH 1.2. The pH of the medium significantly influenced the in vitro release rate; the rate at pH 7.2 was approximately 10 times faster than that at pH 1.2. A pH-sensitive drug release pattern was due to the escape of drug from the microsphere that disintegrated after swelling.

摘要

通过化学改性由亲水性乳糖胶制备了疏水性醋酸乳糖,并将其用于pH敏感药物递送系统。采用溶剂蒸发法制备了醋酸乳糖微球。由醋酸乳糖制备的微球尺寸小于5微米。在药物初始量分别为40毫克和80毫克时,微球的载药效率分别约为70%和80%。微球表现出pH敏感的溶胀行为。微球在pH 7.4时的溶胀能力远大于在pH 1.2时的溶胀能力。介质的pH值显著影响体外释放速率;在pH 7.2时的释放速率约为在pH 1.2时的10倍。pH敏感的药物释放模式是由于药物从溶胀后崩解的微球中逸出所致。

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