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含对乙酰氨基酚的口服卵清蛋白微球。I. 体外特性研究

Egg albumin microspheres containing paracetamol for oral administration. I. In vitro characterization.

作者信息

Torrado J J, Illum L, Cadorniga R, Davis S S

机构信息

Departamento de Farmacia y Tecnologia Farmaceutica, Facultad de Farmacia, Universidad Compultense, Ciudad Universitaria, Madrid, Spain.

出版信息

J Microencapsul. 1990 Oct-Dec;7(4):463-70. doi: 10.3109/02652049009040468.

Abstract

Different egg albumin microsphere systems for oral administration of paracetamol were prepared by the emulsion and capillary extrusion methods. The size of the microspheres depended on the method used to produce the microcapsules and also the size of the crystals of paracetamol. The effect of the following factors on in vitro dissolution were studied: different denaturation processes, variation in the ratio of paracetamol to albumin, size of microspheres, remnant oil in the microspheres, and the coating of the microspheres with membranes of polymethacrylates (Eudragit). The most important factors to control the release of paracetamol from the microspheres were the denaturation process and the use of waxes and membranes to delay the release of paracetamol from the microspheres. The egg albumin microspheres were very porous and permeable to water and thus the release of the paracetamol from the matrix was usually fast unless the microspheres were suitably coated, with, for example, Eudragit RL or RS.

摘要

采用乳液法和毛细管挤出法制备了用于口服对乙酰氨基酚的不同蛋清蛋白微球系统。微球的大小取决于制备微胶囊所用的方法以及对乙酰氨基酚晶体的大小。研究了以下因素对体外溶出度的影响:不同的变性过程、对乙酰氨基酚与白蛋白比例的变化、微球大小、微球中的残留油以及用聚甲基丙烯酸酯(尤特奇)膜对微球进行包衣。控制对乙酰氨基酚从微球中释放的最重要因素是变性过程以及使用蜡和膜来延缓对乙酰氨基酚从微球中的释放。蛋清蛋白微球孔隙率很高且对水具有渗透性,因此除非用尤特奇RL或RS等对微球进行适当包衣,否则对乙酰氨基酚从基质中的释放通常很快。

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