张娟,徐丽双,张妍,何海冰,徐晖,唐星
ZHANG Juan,XU Li-shuang,ZHANG Yan,HE Hai-bing,XU Hui,TANG Xing

• 1:沈阳药科大学药学院

摘要(Abstract)：

目的应用不同亲水性载体材料制备联苯双酯固体分散体,提高联苯双酯体外溶出。方法应用溶解度参数法初步筛选载体材料,采用热熔挤出法制备联苯双酯固体分散体,采用差示扫描量热法、X射线粉末衍射法和傅立叶变换红外光谱法对所制备的固体分散体进行表征。对固体分散体进行溶出度测定,以体外累积溶出度为主要指标,分别考察不同载体、不同载药量对固体分散体中联苯双酯溶出度的影响。结果应用不同亲水性载体材料制备的固体分散体均可提高联苯双酯溶出度,其中以Soluplus对联苯双酯溶出度的提高最为显著,累积溶出度可达到90%左右。优选Soluplus为固体分散体载体材料,并且当载药量为20%时,溶出度最高。结论应用载体材料Soluplus制备固体分散体可以显著提高联苯双酯溶出度。载体材料的性质及载药量的高低都会影响固体分散体中药物的溶出度。
Objective To improve the dissolution of bifendate by preparing its solid dispersions with different hydrophilic carriers.Methods Solubility parameter method was used to screen the hydrophilic carriers and bifendate solid dispersions were prepared by hot-melt extrusion and characterized by differential scanning calorimetry,X-ray powder diffraction and infrared spectra respectively.Accumulated dissolution of bifendate solid dispersions with different carriers and drug loading was measured.Results It showed that although the dissolution of all bifendate solid dispersions with different carriers was improved,the formulation with Solupluswas better than others and its accumulated dissolution was up to 90%.Thereby Solupluswas chosen as the optimal carrier of bifendate solid dispersions.When drug loading was 20%,the maximum accumulated dissolution of bifendate was reached.Conclusions Dissolution of bifendate is significantly improved by formulating it into solid dispersions with Soluplusas carrier.Properties of carriers and the drug loading were the two main factors affecting the dissolution of solid dispersions.

关键词(KeyWords)： 联苯双酯;亲水性载体;固体分散体;溶出度
bifedate;hydrophilic carriers;solid dispersions;dissolution

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 张娟,徐丽双,张妍,何海冰,徐晖,唐星
ZHANG Juan,XU Li-shuang,ZHANG Yan,HE Hai-bing,XU Hui,TANG Xing

DOI: 10.14066/j.cnki.cn21-1349/r.2017.01.002

参考文献(References)：

• [1]王春江,刘小云,李佐军,等.联苯双酯治疗慢性乙型肝炎的随机对照试验的系统评价[J].国际病理科学与临床杂志,2012,32(2):118-123.
• [2]FENG J,XU L,GAO R,et al.Evaluation of polymer carriers with regard to the bioavailability enhancement of bifendate solid dispersions prepared by hot-melt extrusion[J].Drug Development and Industrial Pharmacy,2012,38(6):735-743.
• [3]杨永刚,王震红.联苯双酯滴丸溶出度的测定与比较[J].中国药事,2010,24(7):698-699.
• [4]陈美婉,陈文荣,陈桐楷,等.热熔挤出技术制备固体分散体的应用研究[J].药学学报,2012,47(2):163-167.
• [5]李平祝,李馨儒,周鹤翔,等.药物与载体材料相容性的预测方法研究[J].中国新药杂志,2009,18(3):262-266.
• [6]李慧,唐星.热熔挤出技术制备联苯双酯固体分散体的研究[D].沈阳:沈阳药科大学,2009:21-22.
• [7]王震红,杨永刚.热分析法对联苯双酯晶型的研究[J].药物分析杂志,2010,30(11):2101-2103.
• [8]HARDUNG D H,DJURIC S A.Combining HME&solubilization:Soluplus-the solid solution[J].Drug Deliver Technology,2010,10(3):20-27.
• [9]王辉.热熔挤出技术优化难溶性药物传递系统的研究进展[J].大家健康(学术版),2014,8(7):328-329.
• [10]TIAN B,ZHANG L,PAN Z,et al.A comparison of the effect of temperature and moisture on the solid dispersions:aging and crystallization[J].International Journal of Pharmaceutics,2014,475(1):385-392.