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provides coniferyl ferulate(CAS#:129-06-6) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
This study deals with the competitive interactions of sulindac (CAS 38194-50-2) with specific markers for the major binding areas on human serum albumin (HSA): phenylbutazone (CAS 50-33-9) and warfarin (CAS 129-06-6) for Site I, and diazepam (CAS 439-14-5) for Site II. The method used is high-performance liquid affinity chromatography with HSA-immobilized stationary phase. The affinity constants during the cobinding are determined, and the major thermodynamic parameters are calculated. Based on that the nature of the intermolecular interactions involved in the binding process is hypothesized. The cobinding of sulindac and phenylbutazone is simple competitive and is dominated by hydrogen bonds. The binding affinity of sulindac is significantly decreased by R-warfarin (anticooperative binding), and conformational changes resulting in alteration of the binding mechanisms (electrostatic as well as hydrophobic interactions) are supposed. S-Warfarin hardly affects the binding affinity of sulindac. Sulindac competes with diazepam for two types of binding site: high affinity Site II where the cobinding seems to be dominated by hydrophobic bonding, and low affinity Site I, the latter affinity being significantly decreased (anticooperative binding). These results contribute to a better understanding of the molecular mechanisms of the binding of the investigated drugs with HSA.
Molecular basis of sulindac competition with specific markers for the major binding sites on human serum albumin
Veska N Russeva 1, Zvetanka D Zhivkova
This was a double-blind, randomised, placebo-controlled, cross-over study to determine the possible pharmacodynamic and pharmacokinetic interaction of miglitol (CAS 72432-03-2, Bay m 1099) and warfarin sodium (CAS 129-06-6) in healthy volunteers. The study comprised 2 treatment periods of 8 days each, with a medication-free period of 14 days between the 2 treatment periods. The volunteers received medication for 7 days and were assessed over 8 days in both treatment periods. According to the randomisation, the volunteers received either 100 mg of miglitol or matching placebo, 3 times daily during the treatment periods. On Day 4 of each treatment period the volunteers received a single oral dose of 25 mg warfarin sodium together with miglitol or placebo. The effect of miglitol on both the pharmacokinetics and pharmacodynamics (prothrombin time and clotting factor VII activity) of warfarin sodium was investigated. The study results indicate that the concomitant administration of miglitol and warfarin does not affect the pharmacokinetics of R- and S-warfarin, or the pharmacodynamics of warfarin.
Study of the effect of miglitol on the pharmacokinetics and pharmacodynamics of warfarin in healthy males
R Schall 1, F O Muller, H K Hundt, L Duursema, G Groenewoud, M V Middle
The aim of this study was to elucidate the effects of warfarin on senkyunolide I in a rat model of biliary drainage after oral administration Chuanxiong extract based on pharmacokinetics. Thirty-two rats were randomly divided into four groups: CN, healthy rats after a single administration of Chuanxiong; CO, rats with biliary drainage after a single administration of Chuanxiong; WCN, healthy rats after the administration of Chuanxiong and warfarin; WCO, rats with biliary drainage after the administration of Chuanxiong and warfarin. A series of blood samples were collected at different time points before and after oral administration. An ultra-performance liquid chromatography coupled to tandem mass spectrometry (UPLC-MS/MS) method for quantification of the main components of Chuanxiong and methyclothiazide (internal standard) have been established. The validated method was successfully applied to a comparative pharmacokinetics study. After calculated by the DAS 2.1.1 software, the pharmacokinetics parameters of senkyunolide I showed a significant difference between the CN and CO groups, the AUC0?t, and Cmax of CO group increased by 5.45, 4.02 folds, respectively. There was a significant difference between the WCO and WCN groups, the Tmax of WCO group prolonged 67%; compared to the CN group, the AUC0?t, and Cmax of WCN group raised 4.84, 3.49 folds, respectively; the Tmax and Cmax between the CO and WCO groups also showed a significant difference. The drug warfarin significantly affected the senkyunolide I disposition, which partly due to its enterohepatic circulation process in rat plasma after oral administration of Chuanxiong. The present study highlights an urgent evidence for drug-herb interactions.
senkyunolide I, Chuanxiong, warfarin, pharmacokinetics, UPLC-MS/MS, biliary drainage
The Effects of Warfarin on the Pharmacokinetics of Senkyunolide I in a Rat Model of Biliary Drainage After Administration of Chuanxiong
Haigang Li,1,2 Yu Jiang,3 Yang Wang,2,* Huiying Lv,4 Haitang Xie,5 Guoping Yang,6 Chengxian Guo,6 Jing Tang,1 and Tao Tang2,*