王浩,温梦,刘俊鹏,张亚秋
WANG Hao1,WEN Meng2,LIU Jun-peng1,ZHANG Ya-qiu2(1.School of Pharmaceutical Science

• 1:辽宁医学院药学院
• 2:辽宁医学院药学实验中心

摘要(Abstract)：

目的考察水不溶高分子乙基纤维素薄膜中具有两亲性质的壬苯醇醚的释放行为,考察水微溶阳离子表面活性剂三甲基十六烷基溴化铵的添加对壬苯醇醚释放的影响。方法以刮板法制备5种乙基纤维素载药薄膜,使壬苯醇醚载药量与乙基纤维素质量比为1.5∶10.0、5.0∶10.0、10.0∶10.0、20.0∶10.0、40.0∶10.0,同样以刮板法制备6种添加有三甲基十六烷基溴化铵的薄膜,使壬苯醇醚,三甲基十六烷基溴化铵与乙基纤维素质量比1.5∶0.5∶10.0、1.5∶1.0∶10.0、5.0∶0.5∶10.0、5.0∶1.0∶10.0、10.0∶0.5∶10.0、10.0∶1.0∶10.0。以去离子水为释放介质,37℃,120 r.min-1条件下考察药物的释放,采用HPLC法测定释放介质中药物的量,绘制8 h内的药物累计释放曲线并进行拟合。结果乙基纤维素薄膜中壬苯醇醚载药量的高低,可以使得其8 h内的释放行为从没有释放到30 min内完全突释,2个系列的样品具有缓释能力,并且载药量越大同一时间点乙基纤维素薄膜中壬苯醇醚的释放量越大。添加三甲基十六烷基溴化铵能促进壬苯醇醚的释放。具有缓释行为的样品的释药曲线对Higuchi's和1级释放方程拟合均较好。结论在乙基纤维素薄膜中,壬苯醇醚的载药量可以影响其自身的释放行为,三甲基十六烷基溴化铵的添加和增多可加速壬苯醇醚的释放,为研究其它类型乙基纤维素/壬苯醇醚共混系统药物释放行为提供了参考。
Objective To investigate release behavior of amphiphilic polyethylene glycol mono-4-nonylphenyl ether from water-insoluable polymer ethyl cellulose,and the effect on release behavior when water semi-soluable cationic surfactant hexadecyltrimethyl ammonium bromide was added.Methods Five kinds of drug-loaded ethyl cellulose film were prepared by casting method with mass ratio of polyethylene glycol mono-4-nonylphenyl ether/ethyl cellulose at 1.5∶ 10.0,5.0∶ 10.0,10.0∶ 10.0,20.0∶ 10.0,40.0∶ 10.0,respectively.Another 3 kinds film with hexadecyltrimethyl ammonium bromide were prepared wiht the ratio of polyethylene glycol mono-4-nonylphenyl ether/hexadecyltrimethyl ammonium bromide /ethyl cellulose at 1.5∶ 0.5∶ 10.0,1.5∶ 1.0∶ 10.0,5.0∶ 0.5∶ 10.0,5.0∶ 1.0∶ 10.0,10.0∶ 0.5∶ 10.0,10.0∶ 1.0∶ 10.0.Drug release test was carried out at 37 ℃,120 r · min-1 in deionized water,release amount was determined by HPLC before accumulative release profiles were prepared and regressed within 8 h.Results Loading amount of polyethylene glycol mono-4-nonylphenyl ether in ethyl cellulose film could lead no drug release within 8h or total burst release after 30 min,2 series of films had the ability of sustained release and as the loading amount of drug lifted,drug release amount became bigger at the same sampling time.Addition of trimethylhexadecyl ammonium bromide favored the release of the drug.Drug release profiles of films which release drug sustainably fitted the regress of Higuchi′s equation and 1st order release equation well.Conclusions Loading amount of polyethylene glycol mono-4-nonyl phenyl ether in ethyl cellulose can affect the release behavior of itself and addition of trimethylhexadecyl ammonium bromide can accelerate the release of the drug.This research provides some references of release behavior for other polyethylene glycol mono-4-nonylphenyl ether/ethyl cellulose hybrid systems.

关键词(KeyWords)： 薄膜;壬苯醇醚;乙基纤维素;三甲基十六烷基溴化铵;药物释放
film;polyethylene glycol mono-4-nonylphenyl ether;ethyl cellulose;hexadecyltrimethyl ammonium bromide;drug release

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 王浩,温梦,刘俊鹏,张亚秋
WANG Hao1,WEN Meng2,LIU Jun-peng1,ZHANG Ya-qiu2(1.School of Pharmaceutical Science

DOI: 10.14066/j.cnki.cn21-1349/r.2012.08.011

参考文献(References)：

• [1]陈慧云,王建华,徐世荣,等.高分子材料纤维素醚类衍生物在缓释制剂辅料中的应用[J].材料导报,2005,19(7):48-60.
• [2]罗明生,高天慧.药剂辅料大全[M].成都:四川科学技术出版社,2006:771-772.
• [3]姬静,郭圣荣,方晓玲.乙基纤维素在药物制剂中的应用[J].中国医药工业杂志,2000,31(2):89-92.
• [4]李杰,任麒,孙冠男,等.乙基纤维素在缓控释制剂中的应用概况[J].中国药房,2008,19(16):1257-1259.
• [5]李汉蕴.膜剂的进展概况[J],南京药学院学报,1979,2:74-86.
• [6]张蕴晖,丁训诚,徐晋勋.表面活性剂———一类新型的阴道用避孕药[J].中国计划生育学杂志,2001,9(1):57-59.
• [7]吴莹,陈庆华.女性外用避孕技术的研究应用进展[J].世界临床药物,2008,29(7):414-417.
• [8]张文红,朱伟杰.杀精子剂壬苯醇醚-9的研究现状[J].中国男科学杂志,2001,15(3):276-278.
• [9]韩锦标,曹美玉,陈幼亭,等.高效外用避孕及预防性病传播药物———壬苯醇醚[J].药物不良反应杂志,2000,2(4):268-270.
• [10]王成伟,唐星,姚家荣.壬苯醇醚阴道用缓释凝胶的研制[J].沈阳药科大学学报,2004,21(4):245-249.
• [11]邵长凤,陈坚,张颖,等.长效避孕栓溶出度试验研究[J].中国计划生育学杂志,1999,7(9):390-392.
• [12]陈坚,邵长凤,张颖,等.低剂量复方壬苯醇醚-9阴道避孕制剂体外杀精子作用的研究[J].天津药学,1999,11(2):30-31.
• [13]沈丽琳,崔志娟,邵长风.壬苯醇醚栓的研制及体外溶出度的测定[J].中国药学杂志,1997,32(12):744-746.
• [14]姚丹,谢成国.正交设计法优选壬苯醇醚膜剂的制备工艺[J].数理医药学杂志,2007,20(6):878-879.
• [15]TAEPAIBOON P,RUNGSARDTHONG U,SUPAPHOLP.Vitamin-loaded electrospun cellulose acetate nanofi-ber mats as transdermal and dermal therapeutic agentsof vitamin A aicd and vitamin E[J].European Journalof Pharmaceutics and Biopharmaceutics,2007,67(2):387-397.
• [16]王浩,邓英杰,焦自学,等.聚L-乳酸与聚乙醇酸-b-聚L-乳酸电纺纤维中布洛芬的释放[J].沈阳药科大学学报,2010,27(9):686-694.
• [17]LEE J,GO A,OH S,et al.Tissue anti-adhesion poten-tial of ibuprofen-loaded PLLA-PEG diblock copolymerfilms[J].Biomaterials,2005,26(36):671-678.
• [18]崔福德.药剂学[M].北京:中国医药科技出版社,2002:517-519.