吡非尼酮亚微乳的制备与评价
Preparation and evaluation of pirfenidone submicroemulsion
王欣茹 1田葳 1孟扬 1徐丽芝 2杨瑞 3刘彤 4王淑君 5叶田田6
作者信息
- 1. 江西中医药大学,南昌 330004;长三角药物高等研究院,江苏 南通 226133;江苏艾迪纳米生物医药有限公司,江苏 南通 226100
- 2. 江西中医药大学,南昌 330004;江苏艾迪纳米生物医药有限公司,江苏 南通 226100;安徽中医药大学,合肥 230012
- 3. 辽宁中医药大学附属第二医院,沈阳 110034
- 4. 辽宁省药品检验检测院,沈阳 110032
- 5. 沈阳药科大学,沈阳 110016
- 6. 江西中医药大学,南昌 330004;沈阳药科大学,沈阳 110016
- 折叠
摘要
目的 制备吡非尼酮亚微乳(pirfenidone submicronemulsion,PFD-SE),优化PFD-SE处方,并研究其体外释药机制.方法 采用高压均质法制备PFD-SE,并以离心稳定常数Ke为评价指标,采用Box-Behnken效应面法优化PFD-SE处方;以透析法考察PFD-SE的体外释药行为.结果 PFD-SE的最优处方为PFD 0.250%,中链甘油三酯 2.500%,大豆卵磷脂S100 0.237%,聚氧乙烯 40 氢化蓖麻油 0.311%,超声时间 8.9 min;PFD-SE体外释药遵从一级动力学方程,与吡非尼酮溶液相比,PFD-SE可延长药物在体内的滞留时间.稳定性结果显示PFD-SE在常温和 4℃条件下稳定性良好.结论 本研究制备的PFD-SE稳定性良好,可达到缓释的目的,为PFD新剂型的开发提供了新思路.
Abstract
Objective To prepare pirfenidone submicroemulsion(PFD-SE),optimize the prescription of PFD-SE,and determine the mechanism of drug release in vitro.Methods PFD-SE was prepared by high pressure homogenization method,and the centrifugal stability constant Ke was used as the evaluation index.The formulation of PFD-SE was optimized by Box-Behnken effect surface method,and the in vitro drug release behavior of PFD-SE was determined by dialysis.Results The optimal prescription of PFD-SE was as follows:PFD 0.250%,medium chain triglyceride 2.500%,soybean lecithin S100 0.237%,polyoxyethylene 40 hydrogenated castor oil 0.311%,and ultrasound for 8.9 min.In vitro release of PFD-SE followed the First order kinetic equation,and PFD-SE prolonged the retention time of the drug in vivo compared with pirfenidone solution.The stability test showed that PFD-SE had good stability at room temperature and 4℃.Conclusion PFD-SE prepared in this study has good stability and sustained release,which provides a new idea for the development of new dosage forms of PFD.
关键词
吡非尼酮/特发性肺纤维化/Box-Behnken效应面法/吸入制剂/亚微乳Key words
pirfenidone/idiopathic pulmonary fibrosis/Box-Behnken response surface methodology/inhaled formulation/submicroemulsion引用本文复制引用
基金项目
军队基础加强计划重点基础研究项目(2021-JCJQ-ZD-077-11)
出版年
2024
NETL
NSTL
万方数据