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Objective This paper was to study the absorption and metabolism differences of intestine and liver for multicomponent licorice.Methods The components were identified with the UPLC-MS/MS. In situ closed-loop method was used to carry out the comparative experiments of absorption and metabolism differences between intestine and liver.Results 13 components were identified by UPLC-MS/MS. The absorption and metabolism results indicated some components in licorice water extract could be absorbed into blood and metabolism happened during this process. 14 metabolites were detected in the plasma sample. The hepatic metabolism results indicated many components could experience complex metabolism and more metabolites could be generated.Conclusions Liver was the major metabolism organ for licorice water extract and some components could be metabolized along with the absorption process in intestine. The absorption and metabolism differences between intestine and liver were significant.
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Objective To study the multicomponent in vivo dynamic process in Chuanxiong Rhizoma;To elaborate in vivo metabolic profiling. Methods HPLC was used to establish the fingerprint of aqueous extract of Chuanxiong Rhizoma, and multicomponent changes were detected at the same time. Closed-loop intestine method was used to study the multicomponent changes of oral administration of Chuanxiong Rhizoma after stomach-intestine-liver process. Results Totally 17 components were detected in the fingerprint of aqueous extract of Chuanxiong Rhizoma and they were basically stable in the digestive juice. For in vivo metabolism, 4 components were metabolized by intestinal flora;3 components were metabolized by liver;2 new components were the metabolites of intestinal flora;1 component was the metabolite of liver. Conclusion Multicomponent sequential metabolism and closed-loop intestine method were used to clarify that multicomponent metabolic profiling was feasible, and it could provide experimental basis for the metabolism of traditional Chinese medicine.
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Objective To investigate dynamic metabolism in vivo of Ginkgo Folium Tablet under the guidance of sequential metabolism thoughts. Methods In situ closed-loop in rats was carried out to study sequential metabolism of Ginkgo Folium Tablet through oral digestive system, namely to investigate and compare the intestinal flora metabolism, the gut wall metabolism and hepatic metabolism, combined with chromatographic fingerprint of blood samples. Results The analysis showed that 12 peaks in Ginkgo Folium Tablet were metabolized by intestinal flora, and 7 peaks generated through the gut wall. Most components of Ginkgo Folium Tablet were metabolized in liver, and 3 original medicine components were directly into the blood. Conclusion This study conducts a qualitative description of metabolism of Ginkgo Folium Tablet in different parts of the oral route, and provides references for the quality control, mechanism explanation and secondary development for Ginkgo Folium Tablet.
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Druggability is crucial in pharmaceutical drug development as the source of drug research. Druggability research will face greater challenges because Chinese materia medica (CMM) is the multicomponent drug. In this paper, ideas and methods of study on CMM druggability were mainly proposed in combination with the chemical material basis of muticomponents of CMM.
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Objective To compare the dissolution of Chuangxiong powder in different medium and discuss the dissolution characteristics in vitro of Changxiong powder. Methods The paddle method was adopted, the UV spectrophotometric method was developed to determine the in vitro dissolution quantity of Changxiong powder in five medium (water, 0.1 mol/L hydrochloric acid, acetate buffer of pH 4.5, phosphate buffer of pH 6.8, phosphate buffer of pH 7.4) with ferulic acid as index, and evaluated by drawing the dissolution curve and using the similar factor method and Weibull model. Results The dissolution quantity of Changxiong oral powder in five medium was different. The dissolution quantity in water, 0.1 mol/L hydrochloric acid, acetate buffer of pH 4.5 and phosphate buffer of pH 6.8 was similar and fit Weibull model, but it mutated in phosphate buffer of pH 7.4 and reached the maximum amount at 30 min. Conclusion The dissolution quantity of Changxiong powder is gradually increasing and the time is shorted in the medium from acidic to neutral then to alkaline. Dissolution curve is similar in the acidic and neutral medium. Changxiong powder dissolves out fast and completely in the alkaline medium.
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This study was aimed to determine the solubility an d oil-water partition coefficient of main active com-ponents in Ge-Gen Qin-Lian (GGQL) Tablets (puerarin, baicalin and berberine hydrochloride) in phosphate buffer solution of different pH values and under the background of many components. Solubility of puerarin, baicalin and berberine hydrochloride in different medium pH, and oil-water partition coefficient of the octanol-water and oc-tanol-buffer system were determined by HPLC method. The results showed that the solubility and oil-water partition coefficient of puerarin, baicalin and berberine hydrochloride were varied with the change of pH, and varied under the background of components. At pH 7.4, the solubility was the biggest;puerarin was 7.56 mg·mL-1;baicalin was 17.07 mg·mL-1; berberine hydrochloride was 3.57 mg·mL-1. Oil-water partition coefficient P of these components at pH 1.0 was bigger;puerarin was 0.420 (lgP=-0.38);baicalin was 10.783 (lgP=1.03);berberine hydrochloride was 0.267 (lgP=-0.57). It was concluded that lipid solubility of puerarin, baicalin and berberine hydrochloride at pH 1.0 was better. It was speculated that better absorption in the stomach, and low lipid solubility under other pH. It was speculated that lipid solubility may be one of the reasons affecting the intestinal absorption.
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Objective To select the components for quality control of Fructus Lycii based on the absorption of its extract. Methods To investigate metabolism of components of Fructus Lycii, everted rat gut sacs was carried out as well as the blood was taken from abdominal aorta,.and all samples were analysised by HPLC. Results There are twelve constituents absorbed between ileum and jejunum of rat , and four constituents were detected in the blood. Compound 2, 3, 4, 5, 6, 9, 10, 11 were absorbed in prototype forms in the intestine directly,and compound 1, 7, 8, 12 were new ones. On the other hand, four compositions(3, 7, 10, 13)could be absorbed into blood through analysis serum samples obtaining from aorta abdominalis of rats. Two of them (3, 10)could be absorbed directly by intestine, while(7)was absorbed into blood in new form . Conclusion Based on the intestinal absorption experiment and analysion of compsition in blood, components (3, 10, 13) can be the quality control ingredients of Fructus Lycii.