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Part Used : น้ำจากผลActivity : CYP3A INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0.05-2.5% (v/v)Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Type of experiment: human liver microsomes Results: For grapefruit juice, the IC50 without preincubation was 0.55 (+/-0.03)%; after preincubation, this was significantly reduced to 0.41 (+/-0.03)%, indicating increased inhibitory potency.
Part Used : น้ำจากผลActivity : CYP3A INHIBITIONSolvent/Active Compound : grapefruit juiceType of experiment : humanType of animal : -Type of study : Open trialN(Total) : 11* (M/F = 6/5)N(Treatment) : 11 (M/F = 6/5)Sex : Both sexAge : 14 -43 yrs. (median 32)Route : Oral administrationDose/Conc.(herb) : There were 5 study days, each separated by 3 days of washout. A dose of 30 mg of dextromethorphan (DM) hydrobromide was taken on each study day before bedtime. Volunteers took the DM followed by 200 ml of water (Study Day 1), by 200 ml of grapefruit juice (Study Day 2), by 200 ml of water (Study Day 3), by 200 ml seville orange juice (Study Day 4) and by 200 ml of water (Study Day 5).Duration : On each of the 5 days, a spot urine sample was obtained before administration of DM and the 8-h complete urine output was colloected in the morning.Type of interaction : PharmacokineticsInteraction with drug : Dextromethorphan*/Dextromethorfan/DextromorphanDose/Conc.(drug) : A dose of 30 mg of dextromethorphan hydrobromide (contained in 10 ml of the over-the-counter cough medicine Balmini DM(R))Result : PositiveRemark :Note : *Subject total: Subjects were healthy volunteers. Result: Bioavailability of DM increased significantly with grapefruit and seville orange juice, but only returned to half the baseline value after three days of washout. This confirms that grapefruit and seville orange juice are long lasting and perhaps irreversible inhibitors of gut CYP3A/P-glycoprotein. Grapefruit and seville orange juice appeared to have the same overall effect on DM pharmacokinetics.
Part Used : น้ำจากผลActivity : CYP3A INHIBITIONSolvent/Active Compound : seville orange juiceType of experiment : humanType of animal : -Type of study : Open trialN(Total) : 11* (M/F = 6/5)N(Treatment) : 11 (M/F = 6/5)Sex : Both sexAge : 14 -43 yrs. (median 32)Route : Oral administrationDose/Conc.(herb) : There were 5 study days, each separated by 3 days of washout. A dose of 30 mg of dextromethorphan (DM) hydrobromide was taken on each study day before bedtime. Volunteers took the DM followed by 200 ml of water (Study Day 1), by 200 ml of grapefruit juice (Study Day 2), by 200 ml of water (Study Day 3), by 200 ml seville orange juice (Study Day 4) and by 200 ml of water (Study Day 5).Duration : On each of the 5 days, a spot urine sample was obtained before administration of DM and the 8-h complete urine output was colloected in the morning.Type of interaction : PharmacokineticsInteraction with drug : Dextromethorphan*/Dextromethorfan/DextromorphanDose/Conc.(drug) : A dose of 30 mg of dextromethorphan hydrobromide (contained in 10 ml of the over-the-counter cough medicine Balmini DM(R))Result : PositiveRemark :Note : *Subject total: Subjects were healthy volunteers. Result: Bioavailability of DM increased significantly with grapefruit and seville orange juice, but only returned to half the baseline value after three days of washout. This confirms that grapefruit and seville orange juice are long lasting and perhaps irreversible inhibitors of gut CYP3A/P-glycoprotein. Grapefruit and seville orange juice appeared to have the same overall effect on DM pharmacokinetics.
Part Used : น้ำจากผลActivity : CYP3A INHIBITIONSolvent/Active Compound : Furanocoumarins, Fruit juices of Changshanhuyou (Citrus changshanhuyou Y.B. Chang)Type of experiment : in vitroType of animal : -Type of study : -N(Total) :N(Treatment) :Sex : -Age : -Route : Oral administrationDose/Conc.(herb) :Duration :Type of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) :Result : PositiveRemark : Results: Citrus paradisi had more furanocoumarins and at higher levels than C. grandis Osbeck vs. Guanxi while C. changshanhuyou Y.B. Chang hand none, and their potencies for in vitro CYP3A inhibition were in the order as C. paradisi > C. grandis Osbeck vs. Guanxi > C. changshanhuyou Y.B. Chang.Note : Data incomplete.
Part Used : น้ำจากผลActivity : CYP3A INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Type of experiment: human liver microsomes The inhibitory potential of human CYP3A was in the order: grapefruit > black mulberry > wild grape > pomegranate > black raspberry.Note : Data incomplete
Part Used : น้ำจากผลActivity : CYP3A INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0.2-6.0% (v/v)Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Type of experiment: human liver microsomes Among the tropical fruit juices tested (common papaw, dragon fruit, kiwi fruit, mango, passion fruit, pomegranate, rambutan, and star fruit), star fruit juice showed the most potent inhibition of CYP3A.Note : Data incomplete
