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Seven hopane Tongqiao piece Sanchi extract Epimedium extract composition of the compound traditional Chinese medicine preparation. In recent years, Epimedium or thirty-seven to improve the clinical symptoms of Alzheimer's patients and animal AD (Alzheimer's), VD (vascular dementia) model behavior has been reported, which mainly Epimedium Ng Sanchi extract on cerebral ischemia-reperfusion a significant improvement in role modeling spatial learning and memory impairment. Panax notoginseng saponins (Panaxnotoginseng saponins, PNS) has a distinct role in improving cholinergic function, anti-apoptosis, and regulate the levels of sex hormones. There are also studies have shown that icariin has significant plant estrogen-like effects, has a protective effect on hydrogen peroxide-induced injury in human umbilical vein endothelial cells. These pharmacological effects on the prevention and treatment of Alzheimer's drug development has a positive meaning. Under this guidance, the pharmacology and toxicology of our hospital and Institute of Biochemical Pharmacy, according to the results of pharmacological experiments, Panax notoginseng extracts objects and Epimedium extract feeding into a tablet by a certain percentage, prevention and treatment of vascular dementia new Chinese medicine, named seven-hopane Tongqiao piece. In order to cope with the drug research and development, in accordance with the reporting requirements of the new Chinese medicine, on March 7, Epimedium extract and tablets on the basis of the initial quality study, this study further improve the seven hopane Tongqiao piece quality inspection, and its quality The formulation of standards to provide experimental basis. Thirty-seven and Epimedium as commonly used in traditional Chinese medicine, the pharmacokinetic and pharmacodynamic studies have been reported in the literature, but the simultaneous determination of the two drugs administered in admixture the biological samples notoginsenoside R 1 , ginsenosides RG 1 , ginsenoside Re, the ginseng saponins Rb 1 and icariin and other active ingredients have not been reported. In this paper, UPLC / MS were studied in rats in vivo pharmacokinetics of these several active ingredients; while the difference between the two herbs compatibility and alone when the pharmacokinetics of the active ingredient for the drug's clinical application and development of new drugs to provide theoretical and experimental basis. 1. VII-hopane Tongqiao piece of quality analysis purposes establish the in seven hopane Tongqiao of tablets five active ingredients notoginsenoside R 1 , the ginsenoside Rg 1 ginseng saponins Re, ginseng the saponin Rb 1 and icariin measurement methods; improve the identification of tablets, check the contents; examine the stability of the tablets formulated seven-hopane Tongqiao sheet quality standards to provide experimental basis. Method was determined by RP-HPLC, Agilent SB-C18 column (250 × 4.6 mm, 5μm), acetonitrile - water as the mobile phase gradient elution, detection wavelength of 203nm and 270nm, the injection volume was 50 ul of flow rate: 1.0 mL · min -1 , column temperature ≤ 24 ° C. Methodological studies and real kind of determination of the method for the determination, according to the \And in accordance with the Chinese Pharmacopoeia 2005 edition two Appendix XIX C drug stability test guidelines for the test tablet stability test. Results in the investigated concentration range of each component showed a good linear relationship (notoginsenoside R 1 r = 0.9993, the ginsenoside Rg 1 r = 0.9998, ginsenoside Re r = 0.9991, the ginseng saponins Rb 1 r = 0.9992 and icariin r, = 0.9994), with different concentrations of the various components of the recovery in the range of 96.0% to 117.2%, RSD <5.0 %, intra-day RSD <5.3%. Among them, the notoginsenoside R 1 content and 0.007282 ~ 0.007883g / piece content in the ginsenoside Rg 1 and 0.03288 ~ 0.03373g / piece measured four batches of tablets content ginsenoside Re content of 0.003632 ~ 0.003999g / tablet the ginseng saponin Rb 1 content of 0.02826 ~ 0.03013g /, the icariin content and 0.007010 ~ 0.007466g / piece. The test tablet in 15 minutes or so completely dissolution, disintegration time and tablet weight differences are in compliance with the requirements of the pharmacopoeia. Stability test results obtained with zero results compare the influencing factors of heat, light, wet dissolution and content of the goods were not affected, but the humidity Appearance of the goods. Accelerated test results were not significantly affect the content of the product, dissolution, Appearance. Long-term stay about 24 months, the dissolution Appearance had no significant effect, but after 12 months of icariin decreased slightly. Conclusion The analysis method is sensitive, accurate, specific, and available seven hwo Tongqiao piece of identification, inspection and the determination of. Dissolution, disintegration, and the the tablet weight difference results are in line with the requirements of the pharmacopoeia. The stability test results show that this product should be home and dry place, the retention samples at room temperature for quality in 2002 is basically stable. 2 Seven-hopane Tongqiao piece of pharmacokinetic studies the purpose of (1) the establishment of UPLC / MS method for simultaneous determination the seven hopane Tongqiao of sheet 5 rat plasma active ingredient Sanchi extract Epimedium extract compatibility and the active ingredient alone pharmacokinetic behavior in rats and explored two herbs compatibility whether pharmacokinetic differences investigated tablet excipients on the active ingredient. (2) research the seven hopane Tongqiao piece in rat urine metabolites, combined with the main active ingredient ginsenoside Rg 1 Rb 1 and icariin in rats hepatic microsomal metabolism study to compare the results. Method (1) to take five male SD rats were gavage respectively after seven hopane Tongqiao tablets min Last 4,9,25,45,60,90,120,180,240,360,480,720,1440,2880,4320, venous blood, plasma samples were treated plasma concentration was measured using UPLC-MS method, seven-hopane Tongqiao film of each component drug curves and pharmacokinetic parameters. (2) to take 20 male Sprague-Dawley rats were divided into four groups (n = 5), respectively, were given Sanchi extract materials, Epimedium Extract accessories, Sanchi extract Epimedium Extract, seven hopane Tongqiao piece blood was collected from the tail vein at the same point in time, plasma samples were treated with UPLC-MS method, determination of plasma concentration of each of the four groups of rats active ingredient concentration-time curve and pharmacokinetic parameters. (3) collect the urine of rats the 12h UPLC / MS analysis; HPLC method was used to study the ginsenoside Rg 1 Rb 1 and icariin in rat liver particles metabolism in the body. UPLC / MS methodology results: the concentration range of the inspection of each component showed a good linear relationship (notoginsenoside R 1 r = 0.9991, ginsenoside Rg 1 r = 0.9998, the ginseng saponin Re r = 0.9994, ginsenoside Rb 1 r = 0.9990 and Epimedium glycosides r = 0.9992), different components of different extraction recoveries of 78.6% to 98.3 %, RSD <13.7%, accuracy 87.2% -109.3%, intra-day RSD <16.7%. Seven-hopane Tongqiao film five active ingredient in SD rats in vivo pharmacokinetic behavior of icariin rapidly eliminated in the body, can not be detected after 6 h, notoginsenoside R 1 and ginsenoside Re could be detected after 12h. And ginsenoside Rg 1 in rats duration is longer, to 24 could be detected. The ginseng saponins Rb 1 are different pharmacokinetic behavior in rats with several other components detected 72h still in the body. Compare parameters obtained on the main pharmacokinetic parameters of each component in the case of a single flavor administration and tablets under the administration of one-way ANOVA and two-sample T-test (95% confidence for each parameter interval). It was found that accessories to add saponin T max , influential, P <0.05, significant difference, not add accessories, saponins faster peak; icariin no this phenomenon. Compare the results of the remaining parameters P values ??were greater than 0.05, there was no significant difference statistically significant. Detected several metabolites in rat urine, and speculated that the metabolic pathways, consistent with the literature reported. The main active ingredient in rat liver microsomes, icariin one phase metabolism, the remaining components were not observed metabolic. Conclusion The UPLC / MS method is rapid, accurate, sensitive, 9 minutes several components are completely separated. Seven-hopane Tongqiao Tablets of each active ingredient in the biological sample analysis can be effectively used. Seven-hopane Tongqiao film of the various herbs single to and tablets administered results, the main pharmacokinetic parameters were no significant differences. 5 main active ingredient in rat metabolism deglycosylated.
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