多种高分子材料制备氟苯尼考固体分散体及其对比分析

doi:10.13304/j.nykjdb.2017.0232

中国农业科技导报 ›› 2018, Vol. 20 ›› Issue (3): 139-144.DOI: 10.13304/j.nykjdb.2017.0232

多种高分子材料制备氟苯尼考固体分散体及其对比分析

李胜利1,2,刘保光1,赵晓宁1,苑丽1,刘建华1,潘玉善1,吴华1*

1.河南农业大学牧医工程学院, 郑州 450002; 2.济源市动物卫生监督所, 河南济源 454650

收稿日期:2017-04-17 出版日期:2018-03-15 发布日期:2017-08-21
通讯作者: 吴华，高级实验师，博士，主要从事药物新制剂研究及新材料应用研究。E-mail：huatongzhi66@163.com
作者简介:李胜利，兽医师，硕士，主要从事细菌耐药机制研究与新制剂应用研究。E-mail：lslgiant12345@aliyun.com。

Preparation and Comparative Analysis of Florfenicol Solid Dispersions Using Different Polymers for Pharmaceutical

LI Shengli1,2, LIU Baoguang1, ZHAO Xiaoning1, YUAN Li1, LIU Jianhua1,PAN Yushan1, WU Hua1*

1.College of Animal Husbandry and Veterinary Science, Henan Agricultural University, Zhengzhou 450002;2.Jiyuan Animal Health Supervision, Henan Jiyuan 454650, China

Received:2017-04-17 Online:2018-03-15 Published:2017-08-21

摘要/Abstract

摘要： 利用高分子材料制备固体分散体是当前最有效最便捷的改变非水溶性药物的水溶解度和生物利用度的方法之一。为探究临床常见药用高分子材料载体的优越性和差异性，利用聚乙二醇(PEG)6000、PEG4000、聚维酮(PVP)k30、PVPk15、泊洛沙姆188等高分子材料为载体，采用熔融法、溶剂法和溶剂熔融法制备氟苯尼考固体分散体，溶出速率法验证固体分散体，比较氟为尼考原料、物理混合物及固体分散体的溶解度和累积溶出率。结果表明：几种固体分散体均可提高氟苯尼考药物的溶解度和体外溶出速率，其增溶效果为PEG6000>PEG4000>PVPk30>PVPk15>188，氟苯尼考与PEG6000配比在1∶4时溶解度和体外溶出速率均最优，是最佳配比。5种不同高分子材料制备氟苯尼考固体分散体，制备方法简便易操作、质量可控，能提高药物的溶解度，其中PEG6000增溶效果最优，可广泛应用。

关键词: 氟苯尼考, 药用高分子材料, 固体分散体, 溶解度, 累积溶出率

Abstract: Preparation of solid dispersion by polymers for pharmaceuticals is one of the most effective and convenient methods to improve the solubility and bio-availability of many hydrophobic drugs. In order to investigate the differences of several carriers commonly used in clinic practice, this study took polyethyleneglycol (PEG)6000, and PEG4000, polyvinyl pyrrolidone (PVP) k30, PVPk15 and poloxamer 188 as carriers and prepared florfenicol solid dispersions (SDs) by melting method and solvent-melting method with 5 different polymers for pharmace-uticals, and validated the SDs by dissolution rate method. Solubility and cumulative dissolution rate of florfenicol(FF), physical mixture and SDs were measured and analyzed comparatively. The results showed that the solubility of SDs was raised compared with FF itself. Meanwhile, the efficiency of solubilization was PEG6000>PEG4000>PVPk30>PVPk15>188. Especially, PEG6000 polymers could enhance the solubility remarkably. The best matching was FF:PEG6000 (1∶4). Conclusion, these methods for SDs preparation were simple, convenient, and the quality of SDs can be controlled easily. Among them, especially PEG6000 has the best solubilization effect and can be widely applied.

Key words: florfenicol(FF), polymers for pharmaceuticals, solid dispersions(SDs), solubility, cumulative dissolution rate

李胜利1,2,刘保光1,赵晓宁1,苑丽1,刘建华1,潘玉善1,吴华1*. 多种高分子材料制备氟苯尼考固体分散体及其对比分析[J]. 中国农业科技导报, 2018, 20(3): 139-144.

LI Shengli1,2, LIU Baoguang1, ZHAO Xiaoning1, YUAN Li1, LIU Jianhua1,PAN Yushan1, WU Hua1*. Preparation and Comparative Analysis of Florfenicol Solid Dispersions Using Different Polymers for Pharmaceutical[J]. Journal of Agricultural Science and Technology, 2018, 20(3): 139-144.

[1]	姚晓慧§,蔡建星§,苏战强,高超,轩慧勇,夏利宁*. 猪源葡萄球菌中氟苯尼考耐药基因及其移动元件检测分析[J]. 中国农业科技导报, 2018, 20(11): 54-61.
[2]	李诗怡,胡福良*. 蜜蜂丝的微观结构与物理性能研究[J]. 中国农业科技导报, 2016, 18(2): 47-51.

多种高分子材料制备氟苯尼考固体分散体及其对比分析

Preparation and Comparative Analysis of Florfenicol Solid Dispersions Using Different Polymers for Pharmaceutical

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