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刘婷婷, 郭朋程, 刘婧昕, 等. 柴黄鼻腔即型凝胶剂的制备与评价[J]. koko体育app 学报(医学版), 2021, 52(4): 585-591. DOI:
引用本文: 刘婷婷, 郭朋程, 刘婧昕, 等. 柴黄鼻腔即型凝胶剂的制备与评价[J]. koko体育app 学报(医学版), 2021, 52(4): 585-591. DOI:
LIU Ting-ting, GUO Peng-cheng, LIU Jing-xin, et al. Preparation and Evaluation of Intranasal in situ Gel of Bupleuri Radix Volatile Oil and Baicalin[J]. Journal of Sichuan University (Medical Sciences), 2021, 52(4): 585-591. DOI:
Citation: LIU Ting-ting, GUO Peng-cheng, LIU Jing-xin, et al. Preparation and Evaluation of Intranasal in situ Gel of Bupleuri Radix Volatile Oil and Baicalin[J]. Journal of Sichuan University (Medical Sciences൲), 2021, 52(4): 585-591. DOI:

柴黄鼻腔即型凝胶剂的制备与评价

Preparation and Evaluation of Intranasal in situ Gel of Bupleuri Radix Volatile Oil and Baicalin

  • 摘要:
      目的  制备含有柴胡挥发油与黄芩苷有效组分的鼻腔给药温度/离子双敏感即型凝胶剂。
      方法  以泊洛沙姆407与去乙酰结冷胶为凝胶基质,10%Pharmasolve与2%聚山梨酯-80为增溶剂,0.8%三乙醇胺为pH调节剂,制备柴黄鼻用即型凝胶鼻腔剂,对制剂外观、相转换温度、黄芩苷释放性能等进行研究,并采用大鼠干酵母致热模型和小鼠耳廓肿胀炎症模型进行药效学评价。
      结果  凝胶剂的相转换温度为36 ℃,黄芩苷从中的释放具有明显的缓释特征,符合零级动力学方程。大鼠干酵母高热模型和小鼠二甲苯耳廓肿胀炎症模型实验结果显示凝胶剂具有显著的解热和抗炎效果,且均显著优于空白基质和柴黄颗粒对照组。纤毛毒性实验结果显示凝胶剂对蟾蜍上颚黏膜纤毛无明显毒性。
      结论  所制备的柴黄即型凝胶剂具有速效、高效、长效的特点,具有进一步应用开发的前景。
     
    Abstract:
      Objective  To prepare and evaluate a new formulation of thermosensitive and ion-sensitive in situ gel for nasal administration, using the volatile oil of Bupleuri radix and baicalin, the effective component extracted from Scutellariae radix .
      Methods  Formulation of in situ nasal gel of Bupleuri radix volatile oil and baicalin was prepared by using poloxamer 407 and deacetylated gellan gum as the gel base, 10% pharmasolve and 2% polysorbate 80 as the solubilizer, and 0.8% triethanolamine as the pH regulator. The physical appearance, phase transition temperature, and baicalin release performance of the prepared gel were examined. The pharmacodynamic evaluation was done with the rat fever model developed with dry yeast and the mouse auricle swelling inflammation model.
      Results  The phase transition temperature of the gel was optimized to be 36 ℃. The release of baicalin from the gel showed obvious features of sustained release, which accorded well the zero-order kinetics equation. The results of experiments with the rat dry yeast fever model and the mouse xylene auricle swelling inflammation model showed that the gel had significant antipyretic and anti-inflammatory effects that were significantly better than those of the groups treated with the blank gel base and the Bupleuri radix and Scutellariae radix granule. Results from the cilia toxicity test showed that the gel did not have obvious toxic effect on toad palate mucosal cilia.
      Conclusion  The in situ nasal gel of Bupleuri radix volatile oil and baicalin prepared in the study had a rapid onset time, high efficiency, and prolonged release of active ingredients, thus showing promises for further applicational development.
     
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