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AIM: To investigate the absorption of helicid in different segments of intestine based on rat everted intestine sac model. METHODS: To establish a high-performance liquid chromatography method for simultaneous determination of helicid and its metabolite. Krebs-ringer solution containing helicid was added to everted intestine sacs of different segments (duodenum, Jejunum, ileum and colon). Drug concentration in sacs was determined at different time points (5, 10, 15, 30, 45, 60, 75, 90 min). Adsorptions of helicid in four intestinal segments were compared. RESULTS: This high-performance liquid chromatography was successfully applied to the simultaneous determination of helicid and its metabolite. Absorption of helicid was rapid and time-dependent. The absorption and metabolism of helicid in duodenum segment were higher than these in other segments. CONCLUSION: The duodenum segment is the main site of segmental absorption and metabolism of helicid. This is the first report on intestinal segment metabolism of helicid.
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AIM: To study chronopharmacokinetics of helicid and its metabolites. METHODS: An HPLC-MS method for simultaneous determination of helicid and its three phase I metabolites were established and validated. At 8:00, 14:00 and 0:00, the rats were given helicid 50 mg/kg by gavage, respectively. Blood samples were collected from ophthalmic venous plexus. Then plasma concentration was measured. Pharmacokinetic behaviors of the original drug and its metabolites after administration at different time points were calculated and compared. RESULTS: This established HPLC-MS/MS method was successfully applied to simultaneous determination of helicid and its three metabolites in rat plasma after intragastric administration. Using AUC
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OBJECTIVE: To explore the effects of helicid on the hippocampal neurogenesis in chronically stressed mice and its possible action mechanism of antidepressants. METHODS: Mice were exposed to chronic stress and isolated breed for 28 consecutive days with coadministration of helicid (10, 20, 40 mg · kg-1, ig) or fluoxetine(2.6 mg · kg-1, ig). The proliferation of hippocampal progenitor cells and level of brain derived neurotrophic factor (BDNF) were measured by immunohistochemistry and Western blot analysis. RESULTS: Immunohistochemistry showed decreased expression of BrdU and BDNF in hippocampal dentate gyrus in chronic stress mice. Compared with chromic stress group, helicid and fluoxetine significantly increased expression of BrdU and BDNF. CONCLUSION: The antidepressant mechanisms of Helicid in chronically stressed mice is probalblely related to promote neurogenesis in dentate gyrus and induce up-regulation of BDNF. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVE: To establish a method for the determination of the content of helicidum in helicid tablet intermediats.METHODS: The content of helicidum in intermediate was determined by the UV-visible spectrophotometry with the detective wavelength set at 270 nm.RESULTS: The linear range of helicidum was 4.05～12.15 ?g?mL-1(r=0.999 9) and its average recovery was 99.81%(RSD=0.35%).CONCLUSION: This method is simple,rapid and accurate,and suitable for the quality control of helicid tablet intermediats.
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0.05).Conclusion The administration of helicid to pregnant rats did not affect the early development of nervous system, neurobehavioral function and brain histology of offspring.
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AIM: To investigate the influence of three dimentional printing processes(3DP) on the release of controlled-release helicid tablet. METHODS: Parameters of 3DP,such as skeleton polymer,binder,thickness of powder layering,number of spray painting,subregion ser up and diameter of aperture,were selected in the preparation of donut-shape multilayer controlled-release helicid tablet.Dissolution tests in vitro were carried out to analyse the effect of technological parameters on the release of helicid. RESULTS: Under the condition of fixed subregion and diameter of aperture,the selections of binders and thickness of spray painting were key factors concerning the release period of helicid. CONCLUSION: 3DP processes shows high flexibility and efficacy in the preparation of controlled-release tablets.
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0.05).Conclusion:Helicid had no effects on the early development of central nervous system in rat offspring.