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两种方法制备的水飞蓟宾纳米晶的在体肠吸收及组织分布研究
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| 篇名： | 两种方法制备的水飞蓟宾纳米晶的在体肠吸收及组织分布研究 |
| TITLE： | Study on the in vivo intestinal absorption and tissue distribution of silybin nanocrystals prepared by two methods |
| 摘要： | 目的 研究两种方法制备的水飞蓟宾（Sy）纳米晶在大鼠各肠段的吸收特征和组织分布差异。方法采用高压均质法和反溶剂沉淀法制备粒径相当的Sy纳米晶（即Sy-NS-G、Sy-NS-F）。将大鼠随机分为Sy原料药组、Sy-NS-G组和Sy-NS-F组，每组均设置低、中、高（60、120、180μg/mL）3个质量浓度（以Sy计），每组3只；根据在体单向肠灌流实验，考察Sy原料药、Sy-NS-G和Sy-NS-F在大鼠不同肠段（十二指肠、空肠、回肠）的吸收速率常数（Ka）和表观吸收系数（Papp）。另将大鼠分为Sy原料药组、Sy-NS-G组和Sy-NS-F组，每组20只；各组大鼠单次灌胃剂量均为50mg/kg（以Sy计），分别于给药后0.3、1、4、10、24h处死，考察Sy原料药、Sy-NS-G和Sy-NS-F在心、肝、脾、肺、肾、脑和小肠的组织分布情况。结果Sy-NS-G、Sy-NS-F、Sy原料药在十二指肠、空肠中的Ka、Papp随着Sy质量浓度的增加无明显变化（P＞0.05），Sy-NS-F在十二指肠的吸收高于Sy-NS-G，Sy-NS-G和Sy原料药的吸收部位主要在回肠，Sy-NS-F的吸收部位主要在十二指肠和回肠。Sy-NS-G和Sy-NS-F在大鼠不同组织中的分布不同，Sy-NS-G在大部分组织中1h内达峰，分布浓度由高到低依次为小肠＞脾＞心＞肺＞肝≈脑＞肾；Sy-NS-F在大部分组织中也是1h内达峰，分布浓度由高到低依次为小肠＞脾＞肾＞肺＞心≈肝＞脑。结论Sy纳米晶在十二指肠、空肠中的吸收方式为被动扩散，且在十二指肠中，Sy-NS-F的吸收大于Sy-NS-G；Sy-NS-G和Sy-NS-F在大鼠体内的组织分布有明显区别。 |
| ABSTRACT： | OBJECTIVE To investigate the absorption characteristics and tissue distribution of silybin （Sy） nanocrystals prepared by two methods in different intestinal segments of rats. METHODS Sy nanocrystals （i.e. Sy-NS-G and Sy-NS-F） with comparable particle sizes were prepared using high-pressure homogenization and anti-solvent precipitation methods， respectively. Rats were randomly divided into three groups： Sy raw drug group， Sy-NS-G group， and Sy-NS-F group. Each group was further divided into three subgroups with low， medium， and high （60， 120， 180 μg/mL） mass concentrations （calculated based on Sy）， with 3 rats in each subgroup. The absorption rate constant （Ka） and apparent absorption coefficient （Papp） of Sy raw drug， Sy-NS-G and Sy-NS-F in different intestinal segments were investigated by using the in vivo one-way intestinal perfusion experiment. Additionally， the rats were divided into three groups: Sy raw drug group， Sy-NS-G group， and Sy-NS-F group， with 20 rats in each group. Rats in each group were administered a single intragastric dose of 50 mg/kg （calculated based on Sy）. They were sacrificed at 0.3， 1， 4， 10， and 24 hours post-administration respectively， to investigate the tissue distribution of Sy raw drug， Sy- NS-G， and Sy-NS-F in the heart， liver， spleen， lungs， kidneys， brain and intestines. RESULTS In duodenum and jejunum， the Ka and Papp of the nanocrystals prepared by the two methods remained unchanged with the increase of Sy concentration， and there was no significant difference （P＞0.05）； the absorption of Sy-NS-F in the duodenum was greater than that of Sy-NS-G； the absorption sites of Sy-NS-G and Sy raw drug were mainly in the ileum， while those of Sy-NS-F were mainly in the duodenum and ileum. The concentrations of Sy-NS-G and Sy-NS-F in different tissues of rats were different； Sy-NS-G peaked in most tissues at 1 h， and the distribution concentration was as follows： intestine＞spleen＞heart＞lungs＞liver≈brain＞kidneys. Sy-NS-F reached its peak at 1 h， and the distribution concentration was in the order of intestine＞spleen＞kidney＞lung＞heart≈liver＞brain. CONCLUSIONS The absorption mode of Sy nanocrystals in the duodenum and ileum is mainly passive diffusion. In the duodenum， the absorption of Sy-NS-F is greater than that of Sy-NS-G； there are significant differences in the tissue distribution of Sy-NS-G and Sy-NS-F in rats. |
| 期刊： | 2025年第36卷第11期 |
| 作者： | 王梦颜；孙莹；黄思睿；任娅博；常金花；刘喜纲 |
| AUTHORS： | WANG Mengyan，SUN Ying，HUANG Sirui，REN Yabo，CHANG Jinhua，LIU Xigang |
| 关键字： | 水飞蓟宾；纳米晶；在体单向肠灌流；组织分布；高压均质法；反溶剂沉淀法 |
| KEYWORDS： | silybin； nanocrystals； unidirectional intestinal |
| 阅读数： | 6 次 |
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