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通过锅包衣法制备的乙酰甲胺磷微胶囊水杨酸钠的体外和体内评价。

In vitro and in vivo evaluation of cellacephate microcapsules of sodium salicylate prepared by pan coating.

作者信息

O'Connell M J, Deasy P B

机构信息

Department of Pharmaceutics, Trinity College, University of Dublin, Ireland.

出版信息

J Microencapsul. 1985 Apr-Jun;2(2):111-21. doi: 10.3109/02652048509031555.

Abstract

Within various organic solvent based coating systems examined, one containing cellacephate and hydrogenated castor oil as cofilm formers was found to produce microcapsules of sodium salicylate by pan coating with optimum enteric properties, as determined by in vitro evaluation by scanning electron microscopy and dissolution studies. Scintiscans showed that such microcapsules packed in an outer hard gelatin capsule shell lodged temporarily in the oesophagus and tended to form aggregates on liberation in the stomach of the dog. Because of their rapid clearance from the stomach, single dosage with these microcapsules only prolonged appearance of the plasma peak by about 1.5 h in comparison to a conventional form. The microcapsules showed no decrease in bioavailability and only slight faecal blood loss during acute toxicity testing for gastrointestinal bleeding.

摘要

在所研究的各种基于有机溶剂的包衣系统中,发现一种含有纤维素醋酸酯和氢化蓖麻油作为共成膜剂的系统,通过锅包衣法制备的水杨酸钠微胶囊具有最佳的肠溶性能,这是通过扫描电子显微镜体外评估和溶出度研究确定的。闪烁扫描显示,装入硬明胶胶囊外壳的此类微胶囊会暂时滞留在狗的食道中,并在狗的胃中释放时倾向于形成聚集体。由于它们能迅速从胃中清除,与传统剂型相比,单次服用这些微胶囊仅使血浆峰出现时间延长约1.5小时。在胃肠道出血急性毒性试验中,微胶囊的生物利用度没有降低,且仅有轻微的粪便失血。

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