天然产物研究与开发 ›› 2025, Vol. 37 ›› Issue (增刊1): 83-91.

• 开发研究 • 上一篇    下一篇

山香圆鼻用温敏凝胶制备及药动学研究

梅陈松1,刘入菲1,关志宇1*,王香珍1,张紫霞1,刘  巍2,刘  婧1   

  1. 1江西中医药大学;2江中药业股份有限公司,南昌 330004
  • 出版日期:2025-09-25 发布日期:2025-09-22
  • 基金资助:
    国家重点研发计划中医药现代化研究重点专项(2018 ZX09721002);江西省人事厅博士后科研项目(2020KY51);江西省研究生创新专项(YC2022-S849);江西省教育厅科学技术研究项目(GJJ211239);江西中医药大学中药学一流学科科研项目(JXSYLXK-ZHYAO049)

Preparation and pharmacokinetic study of Turpinia arguta (Lindl.) Seem. temperature-sensistive nasal gel

MEI Chen-song1,LIU Ru-fei1,GUAN Zhi-yu1*,WANG Xiang-zhen1,ZHANG Zi-xia1,LIU Wei2,LIU Jing1   

  1. 1Jiangxi University of Chinese Medicine;2Jiangzhong Pharmaceutical Co.,Ltd.,Nanchang 330004,China
  • Online:2025-09-25 Published:2025-09-22

摘要:

为了提升山香圆的生物利用度,首先以女贞苷和野漆树苷含量、得膏率为指标,考察山香圆最佳提取工艺,并制备山香圆鼻用温敏凝胶(Turpinia aguta (Lindl.) Seem. temperature-sensistive nasal gel,Tup-Gel),对Tup-Gel的pH值、胶凝温度、流变学性质和体外释放进行考察,最后选用雄性大鼠对山香圆和Tup-Gel进行药动学研究。结果显示最佳提取工艺为料液比1∶14(g/mL),乙醇浓度70%,提取时间1.5 h,提取次数3次。Tup-Gel的pH值为5.54±0.03、胶凝温度为32.93±0.31 ℃,体外释放研究结果证实,Tup-Gel可以有效结合凝胶的优势,具有较好的缓释作用;药动学研究结果表明,较山香圆原料药组,Tup-Gel中女贞苷和野漆树苷的相对生物利用度分别提高到325.63%、33056%。本研究表明Tup-Gel可以提高女贞苷和野漆树苷的生物利用度,为开发新的山香圆制剂提供实验基础。

关键词: 山香圆, 女贞苷, 野漆树苷, 温敏凝胶, 鼻腔给药, 药动学

Abstract:

To enhance the bioavailability of Turpinia arguta (Lindl.) Seem.,an optimized extraction process was first developed using ligustroflavone and rhoifolin content,along with paste yield,as key evaluation indices.A temperature-sensitive nasal gel formulation of T.arguta (Tup-Gel) was then prepared.The physicochemical properties of Tup-Gel,including pH,gelation temperature,rheological behavior,and in vitro drug release,were systematically characterized.Furthermore,a pharmacokinetic study was conducted in male rats to compare the bioavailability of T.arguta extract in solution and in gel form.The optimal extraction conditions were identified as a solid-to-liquid ratio of 1∶14(μg/mL),ethanol concentration of 70%,extraction time of 1.5 h,and three extraction cycles.Tup-Gel exhibited a pH of 5.54 ± 0.03 and a gelation temperature of 32.93 ± 0.31 ℃.In vitro release studies demonstrated that Tup-Gel effectively harnesses the advantages of gel-based delivery systems,providing a sustained-release profile.Pharmacokinetic analysis revealed that the relative bioavailability of ligustroflavone and rhoifolin from Tup-Gel increased to 325.63% and 330.56%,respectively,compared to the traditional extract.These findings suggest that Tup-Gel significantly enhances the bioavailability of ligustroflavone and rhoifolin,offering a promising platform for the development of novel T.arguta formulations.

Key words:

中图分类号:  R94