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含有磺胺甲噻二唑的蛋清微球。

Egg albumin microspheres containing sulphamethizole.

作者信息

Brophy M R, Deasy P B

机构信息

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

出版信息

J Microencapsul. 1984 Apr-Jun;1(2):157-68. doi: 10.3109/02652048409038519.

Abstract

Egg albumin microspheres containing sulphamethizole have been prepared by a capillary extrusion procedure. The microspheres were coarse (dvn = 1835 microns) with a narrow size distribution and tended to lose their spherical shape on drying. Scanning electron microscopy revealed that the microspheres were porous with drug concentrated at the periphery of the matrix. This excess surface concentration resulted in a burst effect for drug release in acidic dissolution media with up to 30 per cent drug released in 2 min. This was followed by a more gradual release of drug and finally the release tended to tail off as the matrix became depleted of drug. The average t50 per cent release was 12 min. Variable swelling of the matrix occurred during the first 20-30 min of dissolution which complicated the interpretation of release data. Treatment of the albumin spheres with spermaceti or paraffin wax tended to reduce swelling and increased the t50 per cent release to 33 min and 43 min respectively. Cross-linking of the matrix with aldehydes or by gamma-irradiation proved unsatisfactory.

摘要

通过毛细管挤压法制备了含磺胺甲噻二唑的蛋清白蛋白微球。这些微球较粗(体积平均直径 = 1835微米),粒径分布窄,干燥时往往会失去球形。扫描电子显微镜显示,微球具有多孔性,药物集中在基质的周边。这种表面药物过量集中导致在酸性溶出介质中药物释放出现突释效应,在2分钟内高达30%的药物被释放。随后药物释放更为缓慢,最终随着基质中药物耗尽,释放趋于逐渐减少。药物释放50%的平均时间为12分钟。在溶出的最初20 - 30分钟内基质发生了不同程度的溶胀,这使得对释放数据的解释变得复杂。用鲸蜡油或石蜡处理白蛋白微球往往会减少溶胀,并分别将药物释放50%的时间增加到33分钟和43分钟。用醛类或通过γ射线辐照对基质进行交联效果并不理想。

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