低共熔溶剂结合球磨工艺制备MCC及其在片剂中的应用性能研究

Preparation of Microcrystalline Cellulose by Deep Eutectic Solvent Combined with Ball Milling Process and Its Application in Tablets

关键词:  低共熔溶剂  微晶纤维素  片剂  崩解性能

Key Words:deep eutectic solvents  microcrystalline cellulose  tablets  disintegration performance

摘要:采用氯化胆碱/甲酸（ChCl/FA）、氯化胆碱/草酸（ChCl/OA）、氯化胆碱/柠檬酸（ChCl/CA）3种低共熔溶剂（DES）处理杨木溶解浆，结合球磨处理制备微晶纤维素（MCC），探讨了不同DES体系下时间、温度对MCC聚合度、粒径等性能的影响；并以布洛芬为模型药物，将MCC作为药用辅料填充在布洛芬片中，研究了MCC粒径及用量对片剂崩解时间、累积释放率等性能的影响。结果表明，ChCl/FA体系在100 ℃、60 min时制备的MCC流动性最好；在不添加崩解剂的情况下，当MCC填充量为35.0%时，片剂的崩解时间为190 s，60 min内累积释放率可达86.58%，且具有较高的硬度和抗张强度，显示出DES法制备的MCC用作药用辅料具有良好的填充效果。

Abstract:Three deep eutectic solvents （DES） of choline chloride/formic acid （ChCl/FA）， choline chloride/oxalic acid （ChCl/OA）， and choline chloride/citric acid （ChCl/CA） were used to treat poplar wood dissolving pulp， combined with ball milling process to prepare microcrystalline cellulose （MCC）. The effects of time and temperature on the properties of MCC polymerization and particle size under different DES systems were investigated. Using ibuprofen as a model drug， MCC was filled as a pharmaceutical excipient to investigate the effects of particle size and dosage of MCC on the properties of tablets such as disintegration time and dissolution degree. The results showed that the MCC prepared by ChCl/FA system at 100 ℃ for 60 min had the best mobility. Without adding disintegrant， when the filling amount of MCC was 35%， the disintegration time and the dissolution degree of tablets within 60 min could reach 190 s and 86.58%， respectively， with high hardness and tensile strength. It showed that MCC prepared via DES method had a better filling effect as a pharmaceutical excipient.