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千金子脂肪油自组装胶束对 4 种千金子素在大鼠体内肠吸收的

影响研究 Δ

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袁曜晖 ，许晶晶 ，郭 菲 ，张 超 ，王英姿（1.山东中医药大学药学院，济南 250355；2.山东东阿国胶堂阿
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胶药业有限公司，山东 东阿 252201；3.山东中医药大学附属医院检验科，济南 250011；4.北京中医药大学中
药学院，北京 100102）
中图分类号 R284；R94 文献标志码 A 文章编号 1001-0408（2020）04-0435-06
DOI 10.6039/j.issn.1001-0408.2020.04.09

摘 要 目的：研究不同千金子脂肪油用量的自组装胶束对4种千金子素（千金子素L1、L2、L3、L8 ）在大鼠体内肠吸收的影响。方
法：以千金子脂肪油（用量分别为0、0.2、0.4、1、4 g/L）和脱氧胆酸钠为载体，过量加入4种千金子素（40 mg/L），制备包载4种千金
子素的自组装胶束溶液，作为含药肠灌流液。取大鼠60只，建立在体单向肠灌流模型，按不同千金子脂肪油用量的含药肠灌流液
分组进行不同肠段（十二指肠、空肠、回肠、结肠）的灌流实验。采用高效液相色谱法测定灌流前后肠灌流液中4种千金子素的含
量；计算在不同肠段中4种千金子素的吸收速率常数（Ka ）和小肠表观吸收系数（Peff ）；选择吸收效果较好的回肠段为对象，考察并
计算4种千金子素的累积吸收量。结果：不同千金子脂肪油用量的自组装胶束均能使4种千金子素在各肠段的Ka值和Peff值呈现
不同程度的升高。当千金子脂肪油用量为0.4 g/L时，4种千金子素在各肠段均呈现最大吸收，且与不含脂肪油组比较其Peff值均显
著升高（P＜0.05或P＜0.01）。按不同脂肪油用量组各肠段的Ka、Peff值排序，4种千金子素在各肠段的吸收效果总体上呈现空肠最
好、结肠最差的趋势。与不含脂肪油组比较，千金子脂肪油用量为0.2～4 g/L时，4种千金子素在大鼠回肠的累积吸收量均显著升
高（P＜0.05或P＜0.01），且以0.4 g/L脂肪油用量组为最高。结论：不同用量千金子脂肪油与脱氧胆酸盐形成的自组装胶束能不同
程度地增加千金子素L1、L2、L3、L8在大鼠各肠段的吸收量，且空肠为上述千金子素的主要吸收肠段。
关键词 千金子脂肪油；千金子素；自组装胶束；大鼠；肠吸收

Study on the Effects of Self-assembly Micelles of Euphorbiae Semen Fatty Oil on Intestinal Absorption of 4
Kinds of Euphorbia in Rats
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YUAN Yaohui ，XU Jingjing ，GUO Fei ，ZHANG Chao ，WANG Yingzi（1. School of Pharmaceutical Sciences，
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Shandong University of TCM，Jinan 250355，China；2. Shandong Dong’e Guojiaotang E-Jiao Pharmaceutical
Co.，Ltd.，Shangdong Dong’e 252201，China；3. Department of Laboratory，the Affiliated Hospital of Shandong
University of TCM，Jinan 250011，China；4. School of Chinese Materia Medica，Beijing University of TCM，
Beijing 100102，China）
ABSTRACT OBJECTIVE：To study the effects of different amounts of Euphorbiae Semen fatty oil in self-assembly micelles on
intestinal absorption of 4 kinds of euphorbia（euphorbia L1，L2，L3，L8 ）in rats. METHODS：The self-assembled micelle solution
containing 4 kinds of euphorbia was prepared by adding 4 kinds of euphorbia（40 mg/L）in excess，using the fatty oil of Euphorbia
Semen （0.2，0.4，1，4 g/L） and sodium deoxycholate as carriers. Totally 60 rats were collected to establish in-situ one-way
intestinal perfusion model. Different intestinal segments（duodenum，jejunum，ileum，colon）were perfused with drug-containing
intestinal perfusion fluid according to different dosage of Euphorbiae Semen fatty oil. HPLC method was adopted to determine the
contents of 4 kinds of euphorbia in the intestinal perfusate before and after perfusion. The absorption rate constant （Ka ） and
apparent absorption coefficient（Peff ）of 4 kinds of euphorbia in different intestinal segments were calculated. The ileum segment
with better absorption was selected as the object to investigate and calculate the accumulative absorption of 4 kinds of euphorbia.
RESULTS：The self-assembled micelles formed by different concentrations of fatty oil of Euphorbiae Semen could significantly
increase the absorption of 4 kinds of euphorbia in different intestinal segments to different extents. When the dosage of Euphorbiae
Semen fatty oil was 0.4 g/L，the intestinal absorption effect of 4 kinds of euphorbia were all the best；the Peff was significantly
increased，compared with no fat oil group （P＜0.05 or P＜
Δ 基金项目：国家自然科学基金资助项目（No.81673597）；山东省
0.01）. According to the order of Ka and Peff of each intestinal
优秀中青年科学家科研奖励基金项目（No.BS2014YY053）
segment in different fatty oil dosage groups，the absorption
＊硕士研究生。研究方向：中药新药研发、中药炮制原理。电话：
0531-89628590。E-mail：1310394709@qq.com effect of 4 kinds of euphorbia in each intestinal segment was
# 通信作者：副教授，硕士生导师，博士。研究方向：中药新药研 the best in jejunum and the worst in colon. Compared with no
发、中药炮制原理。电话：0531-89628590。E-mail：tougaotcm@163.com fatty oil group，when the amount of Euphorbiae Semen fatty

中国药房 2020年第31卷第4期 China Pharmacy 2020 Vol. 31 No. 4 ·435 ·