摘要
目的为提高维甲酸的光稳定性、热稳定性及水溶性等而对其进行羟丙 β 环糊精包合物包合条件的研究。方法在单因素考察的基础上 ,采用多因素交叉正交实验对维甲酸的包合条件进行筛选 ,测定包合过程的热力学参数。结果包合的最优条件为 :辅料与药物的投料比 (5∶1 )、包合温度(3 5℃ )、包合时间 (2 4h)、溶剂 (水 )、研磨时间 (1 5min)、离子强度 (无影响 )以及搅拌程度 (低速 )。包合过程的热力学参数为ΔH0 =41 5 8kJ·mol-1,ΔS0 =1 3 8 87J·K-1。结论包合率按包合物中维甲酸的含量与投料的比值计算 ,达到 3 7 5 4% ,优于国内外报道 ,热力学参数数据基本合理。
Objective To raise the stability of tretinoin to light and heat and its solubility in water,including it in HP- β -CD.Methods By the single factors and orthogonal design experiment,we researched on the best conditions of the inclusion.And under the optimizing condition,we studied its thermodynamic constant. Results Being based on the experiment,we definited the best conditions:ratio of the material(5∶1),temperature(35℃),time( 24 h ),solvent(water),grind time(15 min),ion strength(no affect) and extent of stir(low speed).And we also got the initial data of the thermodynamic constant of the including procedure( Δ H 0= 41.58 kJ·mol -1 ,Δ S 0= 138.87 J·K -1 ).Conclusion We confirmed the best conditions of the inclusion and the initial thermodynamics of the procedure.By our methods,the rate (the ratio of tretinoin in the inclusion to the original)of inclusion,which can reach 37.54%,is better than others which were reported before,but these thermodynamical data need a further research to verify them.
出处
《沈阳药科大学学报》
CAS
CSCD
2004年第1期18-21,共4页
Journal of Shenyang Pharmaceutical University
关键词
维甲酸
羟丙-β-环糊精
包合物
正交实验
热力学
tretinoin
hydroxyl propyl beta cyclodextrin
inclusion
orthogonal design experiment
thermodynamics
