摘要
目的制备温敏型眼用葛根素原位凝胶并评价其质量。方法以泊洛沙姆407和泊洛沙姆188作为凝胶基质、PEG400作为增溶剂,采用冷溶法制备温敏型眼用葛根素原位凝胶;通过单因素实验分别考察了泊洛沙姆407、泊洛沙姆188和PEG400等的用量对胶凝化温度的影响;以凝胶化温度作为评价指标,通过Simplex Lattice实验设计法优化并确定最佳处方组成;并以模拟人工泪液作为释放介质考察其体外释药规律。结果通过实验优化得到温敏型眼用葛根素原位凝胶的处方为:30.0%泊洛沙姆407、5.0%泊洛沙姆188、10.0%PEG400。凝胶溶液在33.6±0.3℃时即可发生凝胶化;温敏性眼用葛根素原位凝胶可延缓药物释放,在420 min内药物可释放完全。结论文中制备的温敏型眼用葛根素原位凝胶在环境温度为33.6±0.3℃时发生凝胶化,具有良好的温度敏感性,可延缓药物释放,增加药物的作用时间,减少患者的用药次数,有望开发成为葛根素的新型眼用给药系统。
OBJECTIVE To prepare in situ thermosensitive ophthalmic gels of puerarin and to evaluate their quality.METHODS In this study,poloxamer 407 and poloxamer 188 were used as gel matrix,PEG400 was used as solubilizer of this in situ thermosensitive ophthalmic gels,and the gels were prepared by cold dissolving method.The effects of poloxamer 407,poloxamer 188 and PEG400 on gelation temperature were investigated by single factor experiments.Finally,the gelation temperature was used as the evaluation index,and the optimal formulation composition was optimized using Simplex Lattice experiment design.The in vitro release behavior was investigated by simulated artificial tears as the release medium.RESULTS The optimal formulation of in situ thermosensitive ophthalmic gels was as follows:Poloxamer 407 concentration was 30.0%,poloxamer 188 concentration was 5.0%,and the polyethylene glycol 400 concentration was 10.0%,respectively.The in situ gels occurred gelation when the temperature was higher than 33.6±0.3℃.The in situ thermosensitive ophthalmic gels of puerarin could delay the drug release and release the drug completely within 420 minutes.CONCLUSION In this study,the in situ thermosensitive ophthalmic gels of puerarin getated at the temperature of 33.6±0.3℃.The in situ gels have suitable temperature sensitivity and can delay drug release,hence increasing the duration of drug action.The in situ thermosensitive ophthalmic gels of puerarin are promising to be developed as a new ophthalmic drug delivery system.
作者
刘媛媛
LIU Yuanyuan(Xianyang Vocational College,Xianyang,Shaanxi,712000 P.R.China)
出处
《华西药学杂志》
CAS
CSCD
2019年第3期230-234,共5页
West China Journal of Pharmaceutical Sciences
