| 引用本文: | 孙敬蒙,曲晓宇,张四喜.星点设计-效应面法优化贝美前列素眼用温度敏感原位凝胶的处方工艺[J].中国现代应用药学,2021,38(23):2966-2970. |
| SUN Jingmeng,QU Xiaoyu,ZHANG Sixi.Formulation Optimization of the Thermosensitive in Situ Gel System Containing Bimatoprost for Ocular Use by Central Composite Design-Response Surface Methodology[J].Chin J Mod Appl Pharm(中国现代应用药学),2021,38(23):2966-2970. |
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| 摘要: |
| 目的 使用星点设计-效应面法探讨贝美前列素眼用温度敏感原位凝胶的处方组成，并考察其体外释放度。方法 以泊洛沙姆407和188为凝胶基质，用星点设计-效应面法筛选出最佳处方得到合适的胶凝温度，高效液相色谱法测定贝美前列素眼用凝胶的含量，并以无膜溶出模型考察其体外释放度。结果 处方以1%吐温80，0.03%贝美前列素（w/v）、21%泊洛沙姆407（w/v）和2%泊洛沙姆188（w/v）组成能达到最适胶凝温度。体外释放度的考察结果显示药物的释放与时间呈线性关系。结论 本实验制备的贝美前列素眼用温度敏感原位凝胶具有理想的胶凝温度，能够使药物更加持久地附在给药部位，具有给药方便等优点，是一种值得开发并推广使用的眼用制剂。 |
| 关键词: 贝美前列素 温度敏感 星点设计-效应面法 原位凝胶 |
| DOI：10.13748/j.cnki.issn1007-7693.2021.23.009 |
| 分类号:R944 |
| 基金项目:吉林省教育厅科学研究规划项目（JJKH20201123KJ）；吉林大学第一医院科技成果转化基金项目（JDYYZH-1902014） |
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| Formulation Optimization of the Thermosensitive in Situ Gel System Containing Bimatoprost for Ocular Use by Central Composite Design-Response Surface Methodology |
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SUN Jingmeng, QU Xiaoyu, ZHANG Sixi
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Department of Pharmacy, The First Hospital of Jilin University, Changchun 130021, China
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| Abstract: |
| OBJECTIVE To explore the formulation composition of bimatoprost ophthalmic thermosensitive in situ gel by using the central composite design-response surface method and investigate its in vitro release. METHODS Poloxamer 407 and 188 were used as the gel matrix. The central composite design-response surface method was used to screen out the best prescription to obtain the appropriate gelation temperature. HPLC method was established to determine the content of bimatoprost and the release in vitro was investigated using a membrance-free dissolution model. RESULTS In the formulation, 1% tween 80 was used as the solubilizer, and the composition of 0.03% bimatoprost(w/v), 21% poloxamer 407(w/v) and 2% poloxamer 188(w/w) could reach the optimum gelation temperature. 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. |
| Key words: bimatoprost thermosensitive the central composite design-response surface methodology in situ gel |
