吡嘧司特钾眼用原位温度敏感凝胶的制备及其体外释放度的研究  

Preparation and releasing rate in vitro study of pemirolast potassum in situ thermosensitive gel for ophthalmic use

作　　者：闫荟羽[1] 曲晓宇[1] 马洁[1] 张四喜[1] YAN Hui-yu;QU Xiao-yu;MA Jie;ZHANG Si-xi(Department of Pharmacy,the First Hospital of Jilin University,Jilin Changchun 130021,China)

机构地区：[1]吉林大学第一医院

出　　处：《中国医院药学杂志》2019年第22期2304-2308,共5页Chinese Journal of Hospital Pharmacy

基　　金：吴阶平医学基金会临床科研专项资助基金(编号:320.6750.1418)

摘　　要：目的:以吡嘧司特钾为模型药物,制备眼用原位温度敏感凝胶,考察其体外释放度。方法:以泊洛沙姆407/188为基质,筛选最佳处方以达到合适的胶凝温度,建立高效液相色谱法测定吡嘧司特钾含量并以无膜溶出模型考察体外释放度。结果:处方中以5%甘露醇为溶媒,0.1%吡嘧司特钾(w/v)、0.01%苯扎溴铵(v/v)、6%泊洛沙姆188(w/v)和20%泊洛沙姆407(w/v)的组成可以达到最适胶凝温度,经影响因素试验考察证明该制剂性质稳定,体外释放度考察结果表明药物的释放与时间成线性关系。结论:本文制备的吡嘧司特钾眼用原位温度敏感凝胶具有很好的温度敏感性,能够延长药物在眼部停留时间且给药方便,有望开发成为一种新型眼用给药制剂。OBJECTIVE To prepare in situ temperature-sensitive ophthalmic gels using pemirolast potassium as a model drug and investigate its in vitro release.METHODS Poloxamer 188/407 was used as the matrix to screen the best formulation to achieve the appropriate gelation temperature. HPLC method was established to determine the content of pemirolast potassium and the release in vitro was investigated using a membrane-free dissolution model.RESULTS In the formulation, 5% mannitol was used as the vehicle, and the compositions of 0.1% pemirolast potassium(w/v), 0.01% benzalkonium bromide(v/v), 6% poloxamer 188(w/v) and 20% poloxamer 407(w/v) could reach the optimum gelation temperature. The investigation on the influence factors proved that the formulation was stable in nature. The results of in vitro release test indicated that the release of the formulation showed a linear relationship with time.CONCLUSION The in situ thermosensitive gel of pemirolast potassium prepared in this paper has good temperature sensitivity, which can prolong the residence time of the drug in the eye and is easy to administer. It is expected to be developed into a new ophthalmic dosing formulation.

关 键 词：吡嘧司特钾 眼用 原位凝胶 温度敏感 胶凝温度 释放度 

分 类 号：R974[医药卫生—药品]