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Part Used : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 12 (M/F=6/6)N(Treatment) : 12 (M/F=6/6)Sex : Both sexAge : 67+/-5.2 yrs.Route : Oral administrationDose/Conc.(herb) : 60 mg four times daily (standardized to 24% flavones glycoside and 6% terpene lactones)Duration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : 8 mgResult : NegativeRemark :Note : Twelve healthy volunteers were randomly assigned to receive each botanical supplement for 28 days followed by a 30-day washout period. Probe drug cocktails of midazolam, caffeine, chlorzoxazone and debrisoquine were administered before (days -1, 0) and at the end of supplementation (days 27, 28). Pre- and post-supplementation phenotypic ratios were determined for CYP3A4, CYP1A2, CYP2E1 and CYP2D6 using 1-hydroxymidazolam/midazolam serum ratios (1-hour), paraxanthine/caffeine serum ratios (6-hour), 6-hydroxychlorzoxazone/chlorzoxazone serum ratios (2-hour) and debrisoquine urinary recovery ratios (8-hour), respectively.
Part Used : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 25 microgram/mlDuration : 5 minutesType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Ginkgo extracts: 4.78% Quercetin, 3.73% Kaempferol, 2.13% Isorhamnetin, 12.0% Quercetin glycoside, 9.65% Kaempferol glycoside, 5.19% Isorhamnetin glycoside, 1.61% Bilobalide, 1.41% Ginkgolide A, 0.31% Ginkgolide J, 5.57% Ginkgolide B, 0.38% Ginkgolide C. - Results: The degree of CYP3A4 inhibition of Ginkgo biloba was 45.9% and IC50 values of that inhibit CYP3A4-mediated metabolism of midazolam = 75.1 microgram/ml, 95% Cl: 53.0-106.Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
Part Used : ใบActivity : CYP3A4 INHIBITIONSolvent/Active Compound : Ginkgo biloba extraction (GBE)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 10N(Treatment) : 10Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : GBE intake 360 mg/dDuration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : - Midazolam 8 mg were orally administered to 10 male healthy volunteers before and after GBE intake. - AUC0-alpha for midazolam was singnificantly (25%) increased by GBE intake and oral clearance was significantly (26%) decreased.Note : - Data incomplete