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芍药甘草汤中自组装纳米粒形成对甘草主要成分体外释放和肠

        吸收的影响             Δ


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        沈成英    1,2* ,李小芳 ,朱君君 ,申宝德 ,袁海龙 ,胡建新 (1.江西省人民医院药学部,南昌 330006;2.成都中医
        药大学药学院,成都 611137;3.空军特色医学中心药剂科,北京 100142;4.江西中医药大学现代中药制剂教
        育部重点实验室,南昌 330004)
        中图分类号 R283          文献标志码 A           文章编号 1001-0408(2022)03-0338-06
        DOI   10.6039/j.issn.1001-0408.2022.03.14

        摘   要   目的 研究芍药甘草汤中自组装纳米粒(SGD-SAN)形成对甘草主要成分体外释放和肠吸收的影响。方法 制备甘草单煎
        液(GSD)、芍药单煎液(SSD)、芍药-甘草单煎混合液(MSSGD)和SGD(即芍药、甘草合煎液),并对其中的SAN进行表征。采用高
        效液相色谱法测定甘草中7种主要成分(芹糖甘草苷、甘草苷、芹糖异甘草苷、异甘草苷、甘草素、甘草酸、异甘草素)的含量。采用
        透析袋法,以pH1.2 HCl溶液和pH6.8磷酸盐缓冲液(PBS)为释放介质,考察SGD-SAN形成对甘草中7种主要成分体外释放的影
        响;采用在体单向肠灌流实验考察SGD-SAN形成对甘草中7种主要成分在大鼠肠段吸收的影响。结果 GSD、MSSGD和SGD中
        存在粒径为200~300 nm、多分散性指数为0.3~0.5的SAN;透射电镜观察结果显示,GSD-SAN、MSSGD-SAN呈棒状,SGD-SAN
        呈不规则球形。体外释放实验结果显示,在pH1.2 HCl溶液中,SGD-SAN形成能显著增加甘草素、异甘草素和甘草酸的体外释放,
        对其他成分的释放无明显影响;在pH6.8 PBS中,SGD-SAN形成对甘草中各成分的释放均没有明显影响。在体单向肠灌流实验
        结果显示,SGD-SAN形成能显著促进甘草中各成分在回肠的吸收。结论 SGD-SAN形成能显著改善甘草中难溶性成分的体外释
        放、促进甘草中主要成分的肠吸收,是芍药、甘草配伍增效的物理结构基础。
        关键词 自组装纳米粒;芍药甘草汤;甘草;难溶性成分;体外释放;肠吸收

        Effects of self-assembled nanoparticles from Shaoyao gancao decoction on the in vitro release and intestinal
        absorption of the main components of Glycyrrhiza uralensis
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        SHEN Chengying  1,2 ,LI Xiaofang ,ZHU Junjun ,SHEN Baode ,YUAN Hailong ,HU Jianxin (1. Dept. of
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        Pharmacy,Jiangxi Provincial People’s Hospital,Nanchang 330006,China;2. School of Pharmacy,Chengdu
        University of Traditional Chinese Medicine,Chengdu 611137,China;3. Dept. of Pharmacy,Air Force Medical
        Center,the Chinese People’s Liberation Army,Beijing 100142,China;4. Key Lab of Modern Traditional
        Chinese Medicine Preparation of the Ministry of Education,Jiangxi University of Chinese Medicine,Nanchang
        330004,China)
        ABSTRACT    OBJECTIVE To study the effects of self-assembled nanoparticles from Shaoyao gancao decoction(SGD-SAN)on
        the in vitro release and intestinal absorption of the main components of Glycyrrhiza uralensis. METHODS Gancao single decoction
        (GSD),Shaoyao single decoction(SSD),mixed suspension of Shaoyao and Gancao single decoction(MSSGD)and SGD(i.e.
        Shaoyao-Gancao decoction)were prepared,and SAN was characterized. HPLC method was adopted to determine the contents of 7
        main  components (liquiritin  apioside, liquiritin, isoliquiritin  apioside, isoliquiritin, liquiritigenin, glycyrrhizic  acid,
        isoliquiritigenin)in G. uralensis. The dialysis bag method was used to investigate the effects of the formation of SGD-SAN on in
        vitro release of 7 main components in G. uralensis with pH1.2 HCl solution and pH6.8 phosphate buffered solution (PBS) as
        release media. Single-pass intestinal perfusion study was performed to investigate the effects of the formation of SGD-SAN on the
        intestinal absorption of 7 main components from G. uralensis. RESULTS SAN with particle size of 200-300 nm and polydispersity
        index of 0.3-0.5 was found in GSD,MSSGD and SGD. GSD-SAN and MSSGD-SAN were in rod shape while SGD-SAN was
        irregularly spherical under transmission electron microscope. The results of in vitro release study showed that the formation of
        SGD-SAN could significantly increase in vitro release of liquiritigenin,isoliquiritigenin and glycyrrhizic acid,and had no effect on
        other components of G. uralensis in pH1.2 HCl solution. The formation of SGD-SAN also had no effect on the release of each
                                                            component from G. uralensis in pH6.8 PBS. The results of
            Δ 基金项目:江西省中医药重点研究室-中药制剂临床安全监测
                                                            intestinal perfusion experiments showed that the formation of
        和转化应用重点研究室项目
            *主管中药师,博士。研究方向:中药新型给药系统。电话:                     SGD-SAN could significantly promote the absorption of each
        0791-86891529。E-mail:984075899@qq.com               component from G. uralensis in the ileum. CONCLUSIONS
            # 通信作者:主任药师。研究方向:医院药学。电话:0791-                  The formation of SGD-SAN significantly improves the in vitro
        86895684。E-mail:hjx0108@163.com                     release of poorly soluble components from G. uralensis and


        ·338 ·  China Pharmacy 2022 Vol. 33 No. 3                                    中国药房    2022年第33卷第3期
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