目的优化黄芩苷磷脂复合物鼻用原位凝胶的制备工艺。方法采用中心复合设计-效应面优化法,以胶凝温度为评价指标,对黄芩苷磷脂复合物鼻用原位凝胶的制备工艺关键影响因素Poloxamer407(P407)、Poloxamer188(P188)、聚乙二醇6000(PEG 6000)进行研究,利用多元数学统计矩模型,对制备工艺参数和胶凝温度的相关性进行研究,建立工艺参数与胶凝温度的相关方程,确立最佳工艺参数。结果先将黄芩苷磷脂复合物1.0 g溶于0.1%三乙醇胺溶液中,再加入18 gP407、6 g P188、1 g PEG 6000、葡萄糖5 g、苯扎氯胺0.02 g,加去离子水至100 g,于冰浴(4℃)磁力搅拌下使其分散均匀,置4℃冰箱中保存24 h以上,直至聚合物完全溶解得到澄明溶液。结论采用中心复合设计-效应面法优化的黄芩苷磷脂复合物鼻用原位凝胶的制备工艺稳定可行。

Objective To optimize the preparation technology of baicalin-phospholipids complex (BPC) in situ nasal gel. Methods Key factors affecting the preparation technology of BPC in situ nasal gel, Poloxamer407 (P407), Poloxamer188 (P188), and polyethylene glycol 6000 (PEG 6000) were studied using central composite design-response surface method (CCD-RSM) with gelation temperature as evaluation index. The correlation between preparation technology parameters and gelation temperature was analyzed to establish relative equation of preparation technology parameters and gelation temperature and the best preparation technology parameters using multivariate mathematical statistical moment model.Results BPC (1.0 g) was dissolved in 0.1% triethylamine solution, then P407 (18 g), P188 (6 g), PEG 6000 (1 g), glucose (5 g), BKC (0.02 g), and deionized water were added to reach 100 g. The mixture was uniformly dispersed in ice bath (4 ℃) under magnetic stirring and then was stored at 4 ℃ in refrigerator for more than 24 h until polymer was fully dissolved and clear solution was obtained. Conclusion The preparation technology of BPC in situ nasal gel by CCD-RSM is stable and suitable for industry.