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 L 1，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 ac cumulative 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＜ . According to the order of Ka and Peff of each intestinal ： segment in different fatty oil dosage groups ，the absorption 0531-89628590。E-mail：1310394709@qq.com 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 w as 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 micelle s composed of Euphorbiae Semen fatty oil and deoxycholate can increase the absorption of euphorbia L 1，L2，L3，L8 in each intestinal segment to different extent，and the jejunum is the main absorption segment.
ABSTRACT
Objective: The solubilization of 4 compounds(Euphorbia factor L1,L2,L3 and L8),caused by mixed micelles self-assembled from fatty oil of Euphorbiae Semen and bile salt of intestinal juice,was researched in the simulated human intestinal environment. Method: The mixed micelles were prepared with different amounts of fatty oil of Euphorbiae Semen.The transmission electron microscope(TEM) was used to observe the morphology of the micelles.Particle size detector was used to determine the particle size and Zeta potential.HPLC was used to assay the solubility of these 4 compounds.The variation tendency of the total dissolution of these 4 compounds with the change of standing time was observed. Result: Particle size of the mixed micelles was uniform and its morphology was spherical.The absolute values of Zeta potential were less than 20 mV.When the amount of sodium deoxycholate was fixed 4.96 g·L-1,the solubility of these 4 compounds with the concentration of fatty oil at 0.1-4 g·L-1 were significantly greater than that at the dosage of 0 g·L-1.The solubility of these 4 compounds in the micelles formed by fatty oil was 1.3 to 4 times as much as the micelles without fatty oil.The micelles was stable for 36 h. Conclusion: The micelles self-assembled from fatty oil of Euphorbiae Semen and bile salt of intestinal juice,have significant solubilization effect on Euphorbia factor L1,L2,L3 and L8.This research can lay the foundation for clarifying the detoxification mechanism of removing fatty oil and making frostlike powder from the perspective of pharmaceutics.
ABSTRACT
Objective To determine the contents of four effective constituents in Euphorbiae Semen decoction;To provide evidence for Euphorbiae Semen decoction into clinical application. Methods Established quantitative analysis multi-components by single marker method was used to determine the contents of diterpenoids constituents, such as euphorbia storoid, euphorbia factor L2, and euphorbia factor L3. HPLC method was used to determine the contents of aesculetin. Results Contents of euphorbia storoid, euphorbia factor L2, and euphorbia factor L3 in smashed Euphorbiae Semen decoction were 0.015 9%, 0.005 9% and 0.024 1%, respectively. However, the contents of the above three constituents could not be detected in whole Euphorbiae Semen decoction. The content of aesculetin (0.693 6%) in smashed Euphorbiae Semen decoction was more than that in whole Euphorbiae Semen decoction (0.288 2%). Conclusion Decoction digestion effect of diterpenoids constituents in Euphorbiae Semen decoction is not good. Decocting with water is not suitable for the clinical application of Euphorbiae Semen for purgation and diuresis. Aesculetin in smashed Euphorbiae Semen decoction has good decoction digestion effect, in which clinical use for antisepsis and anti-inflammation is effective.