基于缓控释技术制备布洛芬双层片的研究及释药机制评价
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摘要
目的基于缓控释技术制备布洛芬双层片,并探讨其释放机制。方法采用高效液相色谱法建立布洛芬体外分析方法,分别以溶出度、释放度为考察指标,优化布洛芬速释缓释双层片的制备工艺;采用数学模型进行拟合,探讨双层片缓释层的释放机制。结果高效液相色谱法测定布洛芬含量稳定可行。通过比较溶出度—时间曲线、释放度—时间曲线评定各辅料对溶出度、释放度的影响,确定各辅料的最佳种类及用量,筛选最优处方;在释药机理研究中,释药行为符合Ritger-Peppas模型方程。结论基于缓控释技术的布洛芬速释缓释双层片制备工艺简单,速释层增加布洛芬的溶解度,缓释层维持了有效的血药浓度,提高生物利用度,减少了服用次数,适合大工业生产。
Objective To prepare ibuprofen bi-layer tablets based on controlled release technology and to explore its release mechanism. Methods The in vitro analysis method of ibuprofen was established by high performance liquid chromatography. The dissolution and release were used as indicators. The preparation process of ibuprofen immediate release slow release double-layer tablets was optimized. The mathematical model was used to fit the release mechanism of the two-layer sustained-release layer. Results The determination of ibuprofen content by high performance liquid chromatography was stable and feasible. By comparing the dissolution-time curve and the releasetime curve, the effects of each excipient on dissolution and release were evaluated. The best type and dosage of each excipient were determined, and the optimal prescription was screened. In the study of drug release mechanism, release behavior conforms to the Ritger-Peppas model equation. Conclusion The preparation process of ibuprofen immediate release slow release bi-layer based on slow release technology is simple, the immediate release layer increases the solubility of ibuprofen, and the sustained release layer maintains an effective blood concentration. Improve bioavailability and reduce the number of doses, suitable for large industrial production.
Objective To prepare ibuprofen bi-layer tablets based on controlled release technology and to explore its release mechanism. Methods The in vitro analysis method of ibuprofen was established by high performance liquid chromatography. The dissolution and release were used as indicators. The preparation process of ibuprofen immediate release slow release double-layer tablets was optimized. The mathematical model was used to fit the release mechanism of the two-layer sustained-release layer. Results The determination of ibuprofen content by high performance liquid chromatography was stable and feasible. By comparing the dissolution-time curve and the releasetime curve, the effects of each excipient on dissolution and release were evaluated. The best type and dosage of each excipient were determined, and the optimal prescription was screened. In the study of drug release mechanism, release behavior conforms to the Ritger-Peppas model equation. Conclusion The preparation process of ibuprofen immediate release slow release bi-layer based on slow release technology is simple, the immediate release layer increases the solubility of ibuprofen, and the sustained release layer maintains an effective blood concentration. Improve bioavailability and reduce the number of doses, suitable for large industrial production.
引文
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[12]王洪珍,张炜煜.益髓通经缓释颗粒成型工艺及释药机理的研究[J].时珍国医国药, 2013, 24(5):1117-1119.
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[15]鱼江,封家福,肖隆祥,等.伊拉地平缓释胶囊的制备工艺及体外释药研究[J].药物分析杂志, 2015, 35(3):512-517.
[16]董峥.人工麝香骨架缓释双层片制剂学研究[D].广州:广州中医药大学, 2005:1-53.
[2]崔久峰,布洛芬缓释微丸的研究[D].沈阳:沈阳药科大学,2005:1-68.
[3]张娟,张娜.脂质类纳米粒在难溶性药物递送中的应用[J].中国新药与临床杂志, 2012, 31(4):188-193.
[4]李先俊,袁弘,周志亮,等.缬沙坦固体脂质纳米粒的研究[J].药物生物技术, 2015, 22(1):29-32.
[5]王敏,谢鹏,杨益民,等.塞来昔布固体脂质纳米粒的制备及其在大鼠体内的药动学[J].中国医院药学杂志, 2015,35(1):31-35.
[6]孙艳冬,张然然,赵源,等.离子交换树脂作为药物载体的应用进展[J].中国医药工业杂志, 2016, 47(6):802-806.
[7]徐斌.离子交换树脂在药物制剂中的研究进展[J].中南药学, 2015, 13(5):512-517.
[8]ELZANFALYES,ZAAZAAHE,SOUDIAT,etal.Development and validation of chromatographic methods for Simultaneous determination of ibuprofen and famotidine in presence of related substances in pharmaceutical formulations[J]. Acta Chimica Slovenica, 2015(62):45-51.
[9]丁盛.盐酸克仑特罗快/慢双相释药系统的研究[D].镇江:江苏大学, 2008:1-95.
[10]尹帮龙.穿心莲总内酯骨架缓释片制备工艺及释药机理的研究[D].成都:成都中医药大学, 2012:1-75.
[11]颜承云,谷继伟,王曦,等. 5-氟尿嘧啶-N-琥珀酰胺壳聚糖纳米粒体外释药机理探讨[J].黑龙江医药科学,2011, 1(2):56-60.
[12]王洪珍,张炜煜.益髓通经缓释颗粒成型工艺及释药机理的研究[J].时珍国医国药, 2013, 24(5):1117-1119.
[13]鱼江,封家福,肖隆祥,等.伊拉地平缓释胶囊的制备工艺及体外释药研究[J].药物分析杂志, 2015, 35(3):512-517.
[14]邓雪,孙敬蒙,张炜煜.叶酸肠溶缓释片制备工艺及体外释药机理的研究[J].华中师范大学报, 2014, 48(3):371-374.
[15]鱼江,封家福,肖隆祥,等.伊拉地平缓释胶囊的制备工艺及体外释药研究[J].药物分析杂志, 2015, 35(3):512-517.
[16]董峥.人工麝香骨架缓释双层片制剂学研究[D].广州:广州中医药大学, 2005:1-53.