直肠用美沙拉嗪温敏凝胶的制备及质量评价
Preparation and quality evaluation of mesalazine thermosensitive gel for rectal use
潘娇娇 1李娇 1丁杨 2刘彤 3杨瑞 4桂双英 2王淑君5
作者信息
- 1. 安徽中医药大学药学院,合肥 230012;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. 安徽中医药大学药学院,合肥 230012;药物制剂技术与应用安徽省重点实验室,合肥 230012
- 3. 辽宁省药品检验检测院,沈阳 110034
- 4. 辽宁中医药大学附属第二医院,沈阳 110034
- 5. 沈阳药科大学药学院,沈阳 110016
- 折叠
摘要
目的 制备一种具有缓释和保留性能,用于直肠给药的美沙拉嗪温敏凝胶(MZ-Gel).方法 以胶凝温度为评价指标,采用星点设计-响应面法对泊洛沙姆407和泊洛沙姆188的用量进行优化.以Franz扩散池法进一步考察体外释药行为,得到最佳处方并对其进行质量评价.结果 MZ-Gel优化处方为P40722.56％,P188 3.34％,胶凝温度为(32.8±0.3)℃;MZ-Gel的体外释药符合一级动力学特征,具有缓释效果;胶凝时间平均值为38.3 s,pH平均值为4.07,膨胀系数平均值为4.81％,持水率平均值为99.78％;红外表征表明,美沙拉嗪的加入并没有破坏温敏凝胶结构.结论 此方法制备工艺简单,性质稳定且具有良好的体外释药特征.
Abstract
Objective To prepare a mesalazine thermosensitive gel(MZ-Gel)with sustained release for rectal administration.Methods The dosage of Porloxam 407 and Porloxam 188 was optimised with star point design-response surface methodology using gelling temperature as the evaluation index.The in vitro drug release behavior was further determined by Franz diffusion cell method to obtain the optimal formula and evaluate its quality.Results The optimal formula of MZ-Gel was P407 22.56％,and P188 3.34％,with gelling temperature at(32.8±0.3)℃.The in vitro drug release of MZ-Gel was in accordance with the first-order kinetic characteristics,with sustained release.The average value of the gelation time was 38.3 s,the average value of pH was 4.07,and the coefficient of expansion was 4.81％,with a water-holding capacity of 99.78％.The infrared ray(IR)characterization showed that the addition of mesalazine did not destroy its thermosensitivegel structure.Conclusion This preparation method is simple and stable,and has good in vitro drug release characteristics.
关键词
美沙拉嗪/温敏凝胶/星点设计-响应面法/Franz扩散池法/体外释药Key words
mesalazine/thermosensitive gel/star point design-response surface methodology/Franz diffusion cell method/in vitro drug release引用本文复制引用
基金项目
安徽省高等学校自然科学研究项目(KJ2021A0541)
出版年
2024
NETL
NSTL
万方数据