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Part Used : น้ำจากผลActivity : P-GLYCOPROTEIN 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 : P-GLYCOPROTEIN 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 : P-GLYCOPROTEIN INHIBITIONSolvent/Active Compound : 6',7'-DihydroxybergamottinType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 6',7'-Dihydroxybergamottin 0 to 50 micromol/L.Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Grapefruit juice reduced enterocyte concentrations of CYP3A4, inhibition of P-glycoprotein ativity by other compounds, 6',7'-Dihydroxybergamottin not.Note : Conclusions: 6'7'-Dihydroxybergamottin is not responsible for the effects of grapefruit juice on cyclosporine. Because the interaction did not occur with Seville orange juice despite reduced enterocyte concentrations of CYP3A4, inhibition of P-glycoprotein activity by other compounds in grapefruit juice may be responsible. Reduced enterocyte CYP3A4 by 6',7'-dihydroxybergamottin could be important for other drugs whose bioavailability is less dependent on P-glycoprotein. Data incomplete.
Part Used : น้ำจากผลActivity : P-GLYCOPROTEIN INHIBITIONSolvent/Active Compound : 3,5,6,7,8,3',4'-heptamethoxyflavone, 3,5,6,7,3',4'-hexamethoxyflavone (quercetagetin hexamethyl ether), 5,6,7,3',4'-pentamethoxyflavone (sinensetin) และ 5,6,7,8,3',4'-hexamethoxyflavone (nobiletin)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 : Result: สารที่แยกได้จากน้ำส้มเช้ง ได้แก่ 3,5,6,7,8,3',4'-heptamethoxyflavone, 3,5,6,7,3',4'-hexamethoxyflavone (quercetagetin hexamethyl ether), 5,6,7,3',4'-pentamethoxyflavone (sinensetin) และ 5,6,7,8,3',4'-hexamethoxyflavone (nobiletin) มีฤทธิ์ยังยั้งการทำงานของ Pgp โดยไม่มีผลต่อการทำงานของ CYP3A4Note : Data incomplete
