基于包合技术的可乐定口腔速溶膜的研制  

Preparation of Clonidine Orodispersible Films Based on Inclusion Technology

作　　者：李慧[1] 吴晓强 方亮[1] LI Hui;WU Xiaoqiang;FANG Liang(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国医药工业杂志》2024年第3期375-384,共10页Chinese Journal of Pharmaceuticals

摘　　要：根据可乐定在不同环糊精衍生物中的相溶解度测定结果,筛选出包合效率高的甲基-β-环糊精。采用旋转蒸发法,制备了甲基-β-环糊精与可乐定包合比为1∶1的包合物,其载药率与包封率分别为(13.45±0.22)%和(88.78±0.56)%。然后采用流延涂布法制备该包合物的口腔速溶膜。经单因素考察法得到的优选处方为:PVA 5-88(80%),包合物(4%),1,2-丙二醇(10%),低取代羟丙纤维素(10%)。测定了优化膜剂的质量属性。结果表明,自制膜剂厚度为(91.72±1.74)μm;含水量为4.71%,表面pH值为6.75±0.09,拉伸强度为(62.44±3.19)N/mm^(2),断裂伸长率为(107.15±7.02)%。使用电子舌技术对自制膜剂的掩味效果进行评价,结果显示包合物的矫味效果优于阿司帕坦,环糊精包合技术能大幅改善药物的苦味。Based on the phase solubility determination results of clonidine in different cyclodextrin derivatives,methyl-β-cyclodextrin was screened out because of the high inclusion efficiency.Then the inclusion complexes with the inclusion ratio of methyl-β-cyclodextrin to clonidine of 1∶1 were prepared by rotary evaporation method.The drug loading and encapsulation rates of the inclusion complexes were(13.45±0.22)%and(88.78±0.56)%,respectively.After that,the orodispersible films based on the obtained inclusion complexes were prepared by cast coating method.The formulation compositions were optimized by single factor tests,and the results were as follows:PVA 5-88(80%),inclusion complex(4%),1,2-propylene glycol(10%),and low-substituted hydroxypropyl cellulose(10%).The quality attributes of the optimized films were determined.The results showed that the thickness,water content,surface pH value,tensile strength and elongation at break of the self-made films were(91.72±1.74)μm,4.71%,6.75±0.09,(62.44±3.19)N/mm^(2),and(107.15±7.02)%,respectively.Finally,the taste masking effect was evaluated by the electronic tongue techniques.The results showed that the taste masking effect of the inclusion complex was better than that of aspartame.In conclusion,cyclodextrin inclusion technology can significantly mask the bitterness of a drug.

关 键 词：可乐定 口腔速溶膜 包合物 掩味 

分 类 号：R944.9[医药卫生—药剂学] R971[医药卫生—药学]