No abstract

On high performance liquid chromatography, the caffeoylquinic acid (CQ) occupying the highest proportion of the water-ethanol (7:3) extract of Aster glehni (Compositae) leaves was 3-Op-coumaroylquinic acid (46.10 ± 4.22 mg/g of dried weight) among CQs tested. The IC₅₀ of the water-ethanol (7:3) extract was 4.23 ± 0.24 μg/mL in the peroxynitrite (ONOO(-))-scavenging assay. Phytochemical isolation from A. glehni extract yielded three kaempferol glycosides. The water-ethanol (7:3) extract and both p-coumaric acid and caffeic acid, phenylpropanoid moieties of CQs, had sedative effects in pentobarbital-induced sleeping time in mice and anticonvulsant effects in pentylenetetrazole-induced mice. Furthermore, the phenolic substance-rich W-E (7:3) extract of A. glehni could be used to treat anxiety or convulsion partly due to its peroxynitrite-scavenging mechanism.

After the administration of CR and IR formulations of the same daily dose of sarpogrelate hydrochloride, the overall systemic exposure was slightly higher for the CR than for the IR formulation, whereas peak concentration was comparable between the two formulations. Food reduced the bioavailability of sarpogrelate CR.

No abstract

The interaction between statins and omega-3 fatty acids remains controversial. The aim of this phase 1 trial was to evaluate the pharmacokinetics of drug-drug interaction between atorvastatin and omega-3 fatty acids. Treatments were once-daily oral administrations of omega-3 (4 g), atorvastatin (40 mg), and both for 14 days, 7 days, and 14 days, respectively, with washout periods. The concentrations of atorvastatin, 2-OH-atorvastatin, docosahexaenoic acid (DHA), and eicosapentaenoic acid (EPA) were determined with LC-MS/MS. Parameters of DHA and EPA were analyzed after baseline correction. A total of 37 subjects completed the study without any major violations. The geometric mean ratios (GMRs) and 90% confidence intervals (CIs) of the co-administration of a single drug for the area under the concentration–time curve during the dosing interval at steady state of atorvastatin, 2-OH-atorvastatin, DHA, and EPA were 1.042 (0.971–1.118), 1.185 (1.113–1.262), 0.157 (0.091–0.271), and 0.557 (0.396–0.784), respectively. The GMRs (90% Cis) for the co-administration at steady state of atorvastatin, 2-OH-atorvastatin, DHA, and EPA were 1.150 (0.990–1.335), 1.301 (1.2707–1.1401), 0.320 (0.243–0.422), and 0.589 (0.487–0.712), respectively. The 90% CIs for most primary endpoints were outside the range of typical bioequivalence, indicating a pharmacokinetic interaction between atorvastatin and omega-3.