中国药科大学学报2024，Vol.55Issue(2)：209-216,8.DOI:10.11665/j.issn.1000-5048.2023051701
立他司特滴眼液处方工艺优化及对干眼症疗效评价
Optimization of prescription process of lifitegrast eye drops and evaluation of its efficacy for dry eye disease
摘要
Abstract
In order to develop a more effective drug for dry eye disease,the preparation of lifitegrast eye drops was carried out,and the safety and efficacy of lifitegrast eye drops in vitro and in vivo were investigated.First the method for the determination of lifitegrast content was established,and then the composition and preparation process of the preparation were determined by literature review and single factor experiment.Finally,the safety of lifitegrast eye drops was evaluated by Draize eye irritation test and HE staining,and the therapeutic efficacy was evaluated by Schirmer test and ELISA test.The results showed that the final prescription of lifitegrast eye drops consisted of 5%lifitegrast,0.4%sodium chloride,0.3%-0.4%anhydrous disodium hydrogen phosphate,0.3%sodium thiosulfate pentahydrate and 0.3%sodium hydroxide.The appearance of lifitegrast eye drops was transparent and slightly brownish yellow solution,the pH was7.75±0.05,the osmotic pressure was in the range of 200-330 mOsmol/kg and it had good stability at 60℃for 3 months.There was no significant difference in irritation study compared with normal saline.Schirmer test showed that tear secretion was increased and the expression of inflammatory factors IL-6,IL-1β and TNF-α in tears were significantly decreased after treatment with lifitegrast eye drops and compared to the commercially available emulsion cyclosporine eye drops,it takes effect faster.The above results indicate that lifitegrast eye drops are simple to prepare and stable,which is a better choice for the rapid treatment of dry eye disease.关键词
立他司特/制备工艺/方法学/体内外评价/干眼症Key words
lifitegrast/preparation process/methodology/in vivo-in vitro evaluation/dry eye disease分类
医药卫生引用本文复制引用
颜喜,潘宇南,王锴莉,徐千姿,沈雁,陆洋..立他司特滴眼液处方工艺优化及对干眼症疗效评价[J].中国药科大学学报,2024,55(2):209-216,8.基金项目
国家自然科学基金项目(No.82173989) This study was supported by the National Natural Science Foundation of China(No.82173989) （No.82173989）
