基于响应面法优选美洲大蠊口腔原位温敏凝胶的制备研究

目的制备美洲大蠊Periplaneta americana口腔原位温敏凝胶。方法采用自由基聚合法首次以N-异丙基丙烯酰胺(NNIPAM)和甲基丙烯酸羟丙酯(HPMA)合成聚(N-异丙基丙烯酰胺-甲基丙烯酸羟丙酯)P(NNIPAM-HPMA)]作为温敏材料;通过冷溶法制备美洲大蠊口腔原位温敏凝胶,采用Box-Behnken设计响应面法,以溶蚀时间、胶凝时间为评价指标,在固定美洲大蠊提取物用量基础上,对羟丙基甲基纤维素(HPMC)、聚乙烯吡咯烷酮(PVP K30)、P(NNIPAM-HPMA)的用量进行优选。结果通过原位聚合法合成了P(NNIPAM-HPMA)温敏材料;并用响应面法优选了可用于口腔的美洲大蠊原位温敏凝胶的处方,优选的处方为美洲大蠊提取物10%、HPMC 3.0%、PVP K30 9.5%、P(NNIPAM-HPMA) 10.0%,其溶蚀时间为2 h,胶凝时间8～9 s。结论优选得到美洲大蠊口腔原位温敏凝胶,为美洲大蠊提取物的口腔原位局部的临床应用奠定了科学依据。

Formation optimization of Periplaneta americana-loaded thermosensitive in situ gel for mouth based on Box-Behnken response surface methodology

Objective To prepare oral Periplaneta americana-loaded thermosensitive in situ gel for mouth. Methods The temperature sensitive material P (NNIPAM-HPMA) was synthesized by radical polymerization with NNIPAM and HPMA as raw materials for the first time. The thermosensitive gel was prepared by cool method, and then the amount of HPMC, PVP K30, and P (NNIPAM-HPMA) was optimized by Box-Behnken design response surface method on the basis of fixing the amount of P. americana extract, taking the dissolution time and gelling time as evaluation indexes. Results The thermosensitive P(NNIPAM-HPMA) was synthesized. The optimized formation of P. Americana-loaded thermosensitive in situ gel for mouth was P. Americana 10%, HPMC 3.0%, PVP K30 9.5%, and P(NNIPAM-HPMA) 10.0%, with 2 h dissolution time and 8-9 s gelation time. Conclusion The formulation of the P. americana-loaded thermosensitive in situ gel for mouth was optimized by Box-Behnken response surface methodology, which provided a scientific basis for the oral local clinical application of extract from P. americana.