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(1)
摘 要 目的：研究不同千金子脂肪油用量的自組装胶束对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
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<0.01). According to the order of Ka and Peff of each intestinal segment in different fatty oil dosage groups， the absorption effect of 4 kinds of euphorbia in each intestinal segment was the best in jejunum and the worst in colon. Compared with no fatty oil group， when the amount of Euphorbiae Semen fatty oil was 0.2-4 g/L， accumulative amount of 4 kinds of euphorbia in the ileum of rats increased significantly (P<0.05 or P<0.01)， and the highest in 0.4 g/L Euphorbiae Semen fatty oil group. CONCLUSIONS： The self-assembly micelles composed of Euphorbiae Semen fatty oil and deoxycholate can increase the absorption of euphorbia L1， L2， L3， L8 in each intestinal segment to different extent， and the jejunum is the main absorption segment., 百拇医药(袁曜晖 许晶晶 郭菲 张超 王英姿)
关键词 千金子脂肪油;千金子素;自组装胶束;大鼠;肠吸收
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<0.01). According to the order of Ka and Peff of each intestinal segment in different fatty oil dosage groups， the absorption effect of 4 kinds of euphorbia in each intestinal segment was the best in jejunum and the worst in colon. Compared with no fatty oil group， when the amount of Euphorbiae Semen fatty oil was 0.2-4 g/L， accumulative amount of 4 kinds of euphorbia in the ileum of rats increased significantly (P<0.05 or P<0.01)， and the highest in 0.4 g/L Euphorbiae Semen fatty oil group. CONCLUSIONS： The self-assembly micelles composed of Euphorbiae Semen fatty oil and deoxycholate can increase the absorption of euphorbia L1， L2， L3， L8 in each intestinal segment to different extent， and the jejunum is the main absorption segment., 百拇医药(袁曜晖 许晶晶 郭菲 张超 王英姿)
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