阿戈美拉汀离子液体贴片的制备及体外透皮研究  

Preparation and in vitro transdermal research of agomelatine ionic liquid patch

作　　者：杜卓芳 符渝昕 程泽能 DU Zhuo-fang;FU Yu-xin;CHENG Ze-neng(Xiangya School of Pharmaceutical Sciences,Central South University,Changsha 410000;Hunan Huize Bio-pharmaceutical Co.,Ltd.,Changsha 410000)

机构地区：[1]中南大学湘雅药学院,长沙410000 [2]湖南慧泽生物医药科技有限公司,长沙410000

出　　处：《中南药学》2024年第4期908-913,共6页Central South Pharmacy

摘　　要：目的制备阿戈美拉汀离子液体透皮贴片并对其进行质量评价。方法通过药物析晶、体外释放和渗透情况选择处方所用辅料;通过离子交换反应制备阿戈美拉汀-多库酯离子液体,并采用傅里叶变换红外光谱和磁共振波谱对其进行表征;通过溶剂蒸发法制备透皮贴片,对离子液体贴片的含量均匀性、体外释放及体外渗透性能进行质量评价。结果阿戈美拉汀离子液体贴片制备后,表面光滑透明,重量面积比为167 g·m^(-2),单位面积含药量为2.5 mg·cm^(-2);含量均匀度符合药典标准;体外释放速率为(478.31±0.87)μg/(cm^(2)·h^(1/2));体外渗透速率为(24.38±3.93)μg/(cm^(2)·h);24 h的累计透过量为(545.86±93.08)μg·cm^(-2),透过率为(21.78±3.85)%。结论阿戈美拉汀离子液体通过增大贴片的载药量,显著提高贴片的透皮效果,使得透皮贴剂有望成为阿戈美拉汀的新型给药制剂。Objective To prepare transdermal patch of agomelatine ionic liquids and evaluate its quality.Methods The excipients used in the prescription were selected by drug precipitation,in vitro release and in vitro permeation.Agomelatine-docusate ionic liquid was prepared by ion-exchange reaction and the physicochemical properties of this ionic liquid were systematically characterized by FT-IR and NMR.The transdermal patches were prepared by solvent evaporation,and the content uniformity,in vitro release and in vitro permeation of ionic liquid patches were evaluated.Results The prepared agomelatine ionic liquid patch had smooth and transparent surface,the weight area-ratio was 167 g·m^(-2),-and the drug content per unit area was 2.5 mg·cm^(-2).The content uniformity met pharmacopoeia standards.The in vitro release rate was(478.31±0.87)µg/(cm^(2)·h1/2).The permeation rate in vitro was(24.38±3.93)µg/(cm^(2)·h^(1/2)).The cumulative permeation amount was(545.86±93.08)µg·cm^(-2) at 24 h,and the permeability was(21.78±3.85)%.Conclusion The agomelatine ionic liquid significantly improves the transdermal effect of the patch by increasing drug-carrying capacity of the patch,enabling transdermal patches to be a novel delivery formulation for agomelatine.

关 键 词：阿戈美拉汀 离子液体 透皮贴片 体外渗透试验 

分 类 号：R945[医药卫生—微生物与生化药学]