微波炮附子“液封减毒-干燥膨化”两阶段炮制工艺设计及药效评价  

“Liquid seal to detoxification–drying and puffing”of two stage processing technology design and pharmacodynamic study of aconite(Aconiti Lateralis Radix Praeparata)processed by microwave

作　　者：贺亚男[1] 杨欣 吴京 侯寓森 胡琦 许润春[1] 黄勤挽[1] 杨明 张定堃[1] HE Ya-nan;YANG Xin;WU Jing;HOU Yu-sen;HU Qi;XU Run-chun;HUANG Qin-wan;YANG Ming;ZHANG Ding-kun(State Key Laboratory of Southwestern Chinese Medicine Resources,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Guiyang Xinqi Microwave Industry company with limited liability,Guiyang 550000,China;State Key Laboratory of Innovation Medicine and High Efficiency and Energy Saving Pharmaceutical Equipment,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China)

机构地区：[1]成都中医药大学药学院,西南特色中药资源国家重点实验室,四川成都611137 [2]贵阳新奇微波工业有限责任公司,贵州贵阳550000 [3]江西中医药大学,创新药物与高效节能降耗制药设备国家重点实验室,江西南昌330004

出　　处：《药学学报》2023年第5期1328-1337,共10页Acta Pharmaceutica Sinica

基　　金：国家中医药管理局交叉创新团队项目(ZYYCXTD-D-202209);四川省中医药管理局科学技术研究专项(2021MS016)。

摘　　要：建立过程可控、智能化程度高的生产线,有助于提升微波炮附子的品质及生产效率,促进微波炮附子的转化与应用。本研究根据附子减毒原理及工业化微波设备特点,以双酯型生物碱及单酯型生物碱为指标,建立微波炮附子工业化生产线,并进行中试生产。同时与附子主流炮制品生附片、白附片以及黑顺片的有效成分含量及药效进行对比。结果表明,微波炮附子工业化生产主要分为“液封减毒-干燥膨化”两阶段。中试生产10批微波炮附子的单酯型生物碱含量为0.071%~0.166%;双酯型生物碱含量为0.004%~0.016%,均符合2020年版《中华人民共和国药典》相关要求。与黑顺片和白附片相比,微波炮附子的有效成分保留率更高。药理实验表明,微波炮附子不仅保留了黑顺片、白附片的抗炎、镇痛活性,同时可显著提高肝癌化疗小鼠的白细胞、淋巴细胞的水平,增强小鼠脾脏细胞中CD4/CD8比值(P<0.05),调节机体免疫,而白附片的这种作用较弱,黑顺片和生附片则无该作用。通过以上研究,建立了过程可控、智能化程度高的微波炮附子生产线,并用优化工艺生产出了毒性低、质量稳定、疗效确切的微波炮附子,为微波炮附子的工业化连续生产和临床应用奠定了基础,为微波技术在中医药领域的发展和应用提供了科学支撑。本研究中所有动物实验在开展前经过成都中医药大学实验动物伦理委员会审查批准(批准号:2020-28)。Establish a production line with controllable process and high intelligence,contribute to improve the quality and production efficiency of aconite processed by microwave,and promote the transformation and application of aconite processed by microwave.According to the principle of aconite detoxification and the characteristics of industrial microwave equipment,an industrial production line of aconite processed by microwave was established with diester alkaloids and monoester alkaloids as indicators,and pilot production was carried out.At the same time,the content of active constituents and efficacy were compared with that of the main processed products,such as Shengfupian,Baifupian and Heishunpian.The results showed that the industrial production of aconite processed by microwave can be divided into two stages:"Liquid seal to detoxification-drying and puffing".The content of monoester alkaloids in 10 batches of aconite processed by microwave was 0.071%-0.166%and the content of diester alkaloids was 0.004%-0.016%,which met the relevant requirements of the Chinese Pharmacopoeia in 2020.Compared with Heishunpian and Baifupian,the retention rate of the effective components of aconite processed by microwave was higher.Pharmacological experiments showed that aconite processed by microwave not only retained the anti-inflammatory and analgesic activities of Heishunpian and Baifupian,but also significantly increased the levels of leukocytes and lymphocytes in mice with liver cancer chemotherapy,enhanced the CD4/CD8 ratio in spleen cells of mice(P<0.05),thus regulating the body's immunity.However,this effect of Baifupian was weak,while Heishunpian and Shengfupian had no such effect.Through the above research,this study established microwave processing line with controllable process and high intelligence,as well produced the aconite processed by microwave with low toxicity and stable quality.It laid a foundation for the industrialized continuous production and clinical positioning of aconite by microwave processed,and provid

关 键 词：微波炮制 生物碱含量 中试生产 抗炎镇痛 免疫调节 

分 类 号：R917[医药卫生—药物分析学]