乙基纤维素膜中壬苯醇醚的释放

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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。 Aim To investigate the release behavior of nonoxynol with amphipathic properties in water-insoluble macromolecule ethyl cellulose (Cellulose) films and investigate the effect of water-soluble cationic surfactant trimethylhexadecyl ammonium bromide on the nonoxynol The impact of release. Methods Five kinds of ethycellulose loaded films were prepared by scraping method. The drug loading of nonoxynol and the mass ratio of ethylcellulose were 1.5: 10.0, 5.0: 10.0, 10.0: 10.0, 20.0:10.0, 40.0:10 10.0, also prepared by the scraping of six kinds of added trimethyl hexadecyl ammonium bromide film, nonoxynol, trimethylhexadecylammonium bromide and ethyl cellulose mass ratio of 1.5: 0.5 : 1.0: 1.0: 10.0, 5.0: 0.5: 10.0, 5.0: 1.0: 10.0, 10.0: 5.0: 10.0, 10.0: 1.0: 10.0. The release of the drug was investigated under the conditions of 37 ℃ and 120 r.min-1 with deionized water as the release medium. The amount of the drug in the release medium was determined by HPLC, and the cumulative release curve within 8 h was drawn and fitted. Results The drug loading of nonoxynol in ethylcellulose film could make the release behavior completely release within 8 h from release to release within 30 min. The two series of samples had sustained release ability, The greater the amount of the same time point ethyl cellulose film, the greater the release of nonoxynol. Addition of trimethylhexadecylammonium bromide can promote the release of nonoxynol. The release curves of the samples with sustained release behavior fitted well to Higuchi’s and the first-order release equation. Conclusion In the ethylcellulose film, the drug loading of nonoxynol can affect its own release behavior. The addition and increase of trimethylhexadecylammonium bromide can accelerate the release of nonoxynol. Other types of ethyl cellulose / nonoxynol blend system drug release behavior provides a reference.
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王左敏,女,医学博士,首都医科大学附属北京朝阳医院口腔科副主任.1998年毕业于北京医科大学口腔医学院,获医学博士学位.1998年~2003年在北京大学口腔医学院工作,任主治医师.期