药学学报, 2016, 51(10): 1622-1628
引用本文:
宋立娜, 李鹤然, 王宏宇, 李贞, 赵文畅, 卢方正, 李三鸣. 珍珠水解液眼用温敏原位凝胶的制备及性质研究[J]. 药学学报, 2016, 51(10): 1622-1628.
SONG Li-na, LI He-ran, WANG Hong-yu, LI Zhen, ZHAO Wen-chang, LU Fang-zheng, LI San-ming. Preparation and properties of thermosensitive in situ gel for ophthalmic formulation containing pearl hydrolyzate[J]. Acta Pharmaceutica Sinica, 2016, 51(10): 1622-1628.

珍珠水解液眼用温敏原位凝胶的制备及性质研究
宋立娜, 李鹤然, 王宏宇, 李贞, 赵文畅, 卢方正, 李三鸣
沈阳药科大学药学院, 辽宁 沈阳 110016
摘要:
珍珠明目滴眼液在眼部作用时间短,影响疗效。本文试图将其制成眼用温度敏感型原位凝胶,期待延长药物在眼部滞留时间。以泊洛沙姆407和泊洛沙姆188为凝胶基质,卡波姆934为生物黏附性材料;以星点设计-效应面法筛选最优处方,并对最优处方进行流变学性质、体外溶蚀及释药机制、离体角膜透过性及滞留时间进行评价。结果表明,在25℃时制剂为牛顿流体,35℃时形成具有一定强度的凝胶,凝胶具有假塑性流体的特征,胶凝时间为13 s;凝胶溶蚀及药物释放均符合零级动力学方程;角膜表观透过系数为5.58 cm·s-1;滞留时间是市售滴眼液的7倍。所得珍珠明目眼用原位凝胶性质良好,可达到延长药物作用时间的目的。
关键词:    珍珠水解液      泊洛沙姆      温敏原位凝胶      流变学      角膜透过性      滞留时间     
Preparation and properties of thermosensitive in situ gel for ophthalmic formulation containing pearl hydrolyzate
SONG Li-na, LI He-ran, WANG Hong-yu, LI Zhen, ZHAO Wen-chang, LU Fang-zheng, LI San-ming
Shool of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China
Abstract:
The study was designed to generate an ophthalmic thermosensitive in situ gel with improved mechanical and mucoadhesive properties that may prolong the retention time to enhance the bioavalability of pearl hydrolyzate. The gene was comprised of poloxamer 407, poloxamer188 and Carbopol 934, which were optimized by central composite design and response surface methodology. The rheological properties, transcorneal permeability, retention time and in vitro release behaviors of the optimal gel formulation were investigated. The gel was Newtonian liquid at 25℃ and performed as a semisolid gel with non-Newtonian liquid property with a gelation time of 13 s at 35℃. Compared with a conventional eye drops, the ophthalmic in situ gel exhibited a sevenfold increase in retention with a sustained release behavior, which was observed with suitable permeability coefficient at 5.58 cm·s-1. In conclusion, the new gel of pearl hydrolyzate prolonged the release duration of drug, which may decrease the frequency of administration of pearl hydrolyzate. kilometers with ecological similarity between 20% and 40%, mainly in Yunnan, Guangxi, Guangdong, Guizhou, Hainan, Sichuan, Fujian and Chongqing. The climate factors mainly affecting the distribution of Panax notoginseng (Burk.) F. H. Chen were precipitation of warmest quarter, SD of temperature seasonality, altitude, isothermality, coefficient of variation of precipitation seasonality, mean temperature of monthly, precipitation of driest month, reference bulk density of soil and soil texture.
Key words:    pearl hydrolyzate    poloxamer    thermosensitive in situ gel    rheology    transcorneal permeability    retention time   
收稿日期: 2016-05-24
DOI: 10.16438/j.0513-4870.2016-0502
基金项目: 国家自然科学基金资助项目(81473161,81273445).
通讯作者: 李三鸣
Email: li_sanming@126.com
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