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芍药甘草汤自组装纳米粒的促吸收作用研究
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| 篇名： | 芍药甘草汤自组装纳米粒的促吸收作用研究 |
| TITLE： | Study on the absorption-enhancing effect of self-assembled nanoparticles from Shaoyao gancao decoction |
| 摘要： | 目的 探讨芍药甘草汤自组装纳米粒（SGD-SAN）形成对其主要活性成分肠吸收行为的影响及机制。方法制备SGD-SAN并进行表征；采用大鼠在体单向肠灌流模型，以吸收速率常数（Ka）和表观渗透系数（Peff）为指标，以游离药物为对照，探讨SGD-SAN中5种活性成分（芍药内酯苷、芍药苷、芹糖甘草苷、甘草苷、甘草酸）在空肠和回肠的吸收特性；在较佳吸收肠段考察药物浓度及外排转运蛋白抑制剂（P糖蛋白抑制剂维拉帕米、多药耐药相关蛋白2抑制剂吲哚美辛、乳腺癌耐药蛋白抑制剂利血平）对上述成分肠吸收特性的影响。结果所得SGD-SAN呈球状且大小均一，平均粒径为（155.57±2.65）nm，多分散性指数为0.34±0.03，Zeta电位为（－9.30±1.12）mV；芍药内酯苷等5种活性成分的平均总含量为12.26%，且不受酶降解和肠道物理吸收的影响。与游离药物组比较，SGD-SAN组中5种成分在回肠段均表现出更高的吸收速率，且在回肠段中的Ka和Peff（回肠段中甘草酸的Peff除外）均显著升高（P＜0.05或P＜0.01），其吸收具有浓度依赖性趋势。游离药物组中，各成分的吸收均受相应抑制剂的调控（P＜0.05或P＜0.01）；而在SGD-SAN组中，除芍药内酯苷和芍药苷外，其余成分均不受抑制剂的影响（P＞0.05）。结论SGD-SAN能够显著改善芍药内酯苷等活性成分的肠道吸收效率，上述促吸收作用可能与规避外排转运蛋白影响、兼具混合吸收模式有关。 |
| ABSTRACT： | OBJECTIVE To investigate the effect and mechanism of self-assembled nanoparticles from Shaoyao gancao decoction （SGD-SAN） on the intestinal absorption behavior of its main active components. METHODS SGD-SAN was prepared and characterized. Using an in-situ single-pass intestinal perfusion model in rats， the absorption characteristics of five active components （albiflorin， paeoniflorin， liquiritin apioside， liquiritin， glycyrrhizic acid） from SGD-SAN in the jejunum and ileum were studied， with the absorption rate constant （ K a ） and apparent permeability coefficient （ P eff ） as indicators， and compared with free drugs. In the intestinal segment with optimal absorption， the effects of drug concentration and efflux transporter inhibitors （P-glycoprotein inhibitor verapamil， multidrug resistance-associated protein 2 inhibitor indomethacin， breast cancer resistance protein inhibitor reserpine） on the intestinal absorption characteristics of these components were examined. RESULTS The obtained SGD-SAN exhibited a spherical shape with uniform sizes， an average particle diameter of （155.57±2.65） nm， a polydispersity index of 0.34±0.03， and a Zeta potential of （－9.30±1.12） mV. The average total content of five active components， including albiflorin， was 12.26%， and remained unaffected by enzymatic degradation and intestinal physical absorption. Compared with the free drug group， the five active components in the SGD-SAN group exhibited higher absorption rates in the ileal segment， with significantly elevated K a and P eff values （except for the P eff value of glycyrrhizic acid in the ileal segment） （ P ＜0.05 or P ＜0.01）. Their absorption demonstrated a concentration-dependent trend. In the free drug groups， the absorption of each component was regulated by corresponding inhibitors （ P ＜0.05 or P ＜0.01）； whereas in the SGD-SAN groups， except for albiflorin and paeoniflorin， the absorption of the remaining components was not affected by the inhibitors （ P ＞0.05）. CONCLUSIONS SGD-SAN significantly enhances the intestinal absorption efficiency of active components. The above absorption-enhancing effect may be related to the avoidance of efflux transporter influence and the presence of a mixed absorption mode. |
| 期刊： | 2026年第37卷第06期 |
| 作者： | 魏欣玲；张双辰；张年战；何沂灿；杜超颖；申宝德；沈成英 |
| AUTHORS： | WEI Xinling， ZHANG Shuangchen，ZHANG Nianzhan，HE Yican，DU Chaoying，SHEN Baode，SHEN Chengying |
| 关键字： | 芍药甘草汤；自组装纳米粒；在体单向肠灌流；吸收速率常数；表观渗透系数；促吸收机制 |
| KEYWORDS： | Shaoyao gancao decoction； self-assembled nanoparticles； in-situ single-pass intestinal perfusion； Ka； Peff； |
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