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Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : Seville orange juiceType of experiment : humanType of animal : -Type of study : Cross overN(Total) : 10* (M/F = 5/5)N(Treatment) : 10 (M/F = 5/5)Sex : Both sexAge : 21 - 32 yrs.Route : Oral administrationDose/Conc.(herb) : a single oral dose of a felodipine 10-mg extended-release tablet with 240 mL of Seville orange juiceDuration : Peripheral venous blood (7 mL) was collected just before felodipine and juice administration and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 12, and 24 hours thereafterType of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : a single oral dose of felodipine 10-mg extended-release tabletResult : PositiveRemark : Result: The felodipine area under the plasma concentration-time curve was increased by 76% and 93% after Seville orange juice and grapefruit juice ingestion, respectively, compared with common orange juice. The effects of Seville orange juice and grapefruit juice were similar in that the felodipine maximum concentration was augmented while the terminal elimination half-life was unchanged and the dehydrofelodipine area under the plasma concentration time-curve was increased, but the dehydrofelodipine-felodipine area under the plasma concentration-time curve ratio was reduced. *Subject toal: Subjects were healthy nonsmoking volunteers.
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : Dilute grapefruit juiceType of experiment : humanType of animal : -Type of study : Cross overN(Total) : 10* (M/F = 5/5)N(Treatment) : 10 (M/F = 5/5)Sex : Both sexAge : 21 - 32 yrs.Route : Oral administrationDose/Conc.(herb) : a single oral of a felodipine 10-mg extended-release tablet with 240 mL of dilute grapefruit juice (that contained equivalent total molar concentrations of bergamottin plus 6',7'-dihydroxybergamottin)Duration : Peripheral venous blood (7 mL) was collected just before felodipine and juice administration and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 12, and 24 hours thereafterType of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : a single oral dose of felodipine 10-mg extended-release tabletResult : PositiveRemark : Result: The felodipine area under the plasma concentration-time curve was increased by 76% and 93% after Seville orange juice and grapefruit juice ingestion, respectively, compared with common orange juice. The effects of Seville orange juice and grapefruit juice were similar in that the felodipine maximum concentration was augmented while the terminal elimination half-life was unchanged and the dehydrofelodipine area under the plasma concentration time-curve was increased, but the dehydrofelodipine-felodipine area under the plasma concentration-time curve ratio was reduced. *Subject toal: Subjects were healthy nonsmoking volunteers.
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : Dilute grapefruit juiceType of experiment : humanType of animal : -Type of study : Cross overN(Total) : 10* (M/F = 5/5)N(Treatment) : 10 (M/F = 5/5)Sex : Both sexAge : 21 - 32 yrs.Route : Oral administrationDose/Conc.(herb) : a single oral of a felodipine 10-mg extended-release tablet with 240 mL of common orange juice (negative control)Duration : Peripheral venous blood (7 mL) was collected just before felodipine and juice administration and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 12, and 24 hours thereafterType of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : a single oral dose of felodipine 10-mg extended-release tabletResult : EquivocalRemark : Result: The common orange juice was used as negative control. *Subject toal: Subjects were healthy nonsmoking volunteers.
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/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 : DRUG INTERACTIONSolvent/Active Compound : grapefruit juiceType of experiment : humanType of animal : -Type of study : Cross overN(Total) : 5* (M/F = 2/3)N(Treatment) : 5 (M/F = 2/3)Sex : Both sexAge : 20 - 37 yrs.Route : Oral administrationDose/Conc.(herb) : After an overnight fast, each subject was given a 10-mg extended-release tablet of felodipine with 240 mL of grapefruit juice. To control for the ethanol content (5%) in the orange juice-containing serum, ethanol was added to the orange juice and grapefruit juice to yield a final concentration of 5%.Duration : Blood (5 mL) was collected immediately before administration of felodipine with the juice and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours thereafterType of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : A single tablet of 10-mg extended-release tablet of felodipineResult : PositiveRemark : Result: For every subject except subject B (who appeared to have minimal response to either grapefruit juice or grapefruit juice serum), both the AUC(0-Clast) and Cmax of felodipine with grapefruit juice were increased by at least 2.2-fold relative to plain orange juice. *Subject total: Subjects were healthy volunteers.
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : grapefruit juice serum (aqueous extract)Type of experiment : humanType of animal : -Type of study : Cross overN(Total) : 5* (M/F = 2/3)N(Treatment) : 5 (M/F = 2/3)Sex : Both sexAge : 20 - 37 yrs.Route : Oral administrationDose/Conc.(herb) : After an overnight fast, each subject was given a 10-mg extended-release tablet of felodipine with 240 mL of grapefruit juice. To control for the ethanol content (5%) in the orange juice-containing serum, ethanol was added to the orange juice and grapefruit juice to yield a final concentration of 5%.Duration : Blood (5 mL) was collected immediately before administration of felodipine with the juice and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, and 24 hours thereafterType of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : A single tablet of 10-mg extended-release tablet of felodipineResult : PositiveRemark : Result: For every subject except subject B (who appeared to have minimal response to either grapefruit juice or grapefruit juice serum), both the AUC(0-Clast) and Cmax of felodipine with grapefruit juice were increased by at least 2.2-fold relative to plain orange juice. *Subject total: Subjects were healthy volunteers.
Part Used : ผลActivity : DRUG INTERACTIONSolvent/Active Compound : limoninType 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 : Doxorubicin*/Adrimycin/ADR/AdriaDose/Conc.(drug) : -Result : PositiveRemark : Limonin effectively enhanced the anticancer activity of doxorubicin in drug resistant Caco-2 colon and CEM/ADR5000 leukemia cells at a concentration of 20 micromolar.Note : Data from review
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : 6',7'-DihydroxybergamottinType of experiment : humanType of animal : -Type of study : Open trialN(Total) : -N(Treatment) : -Sex : -Age : -Route : Oral administrationDose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : Ciclosporin*/Cyclosporin/Cyclosporin A/Cyclosporine/CsA/CyADose/Conc.(drug) : -Result : PositiveRemark : Subjects were healthy subjects. Result: Area under the whole blood concentration-time curve and peak concentration of cyclosporine were increased by 55% and 35%, respectively, with grapefruit juice (P < .05).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 : DRUG INTERACTIONSolvent/Active Compound : Furanocoumarins, Fruit juices of pummel grapefruit (Citrus paradisi Macf.)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 12*N(Treatment) : 12Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : 250 mL of fruit juices of pummel grapefruit with 26-mmol (10-mg) plain tablet felodipine.Duration : Observed for 12 h after administration of drugType of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : 26-mmol (10-mg) plain tablet felodipineResult : PositiveRemark : Results: The geometric mean and 90% confidence intervals of pharmacokinetic parameters for human oral felodipine with C. paradisi, C. grandis Osbeck vs. Guanxi, C. changshanhuyou Y.B. Chang and water were respectively as follows: peak plasma concentration (nmol.bul.L-1), 37 (32-44), 25 (21-29), 19 (16-22) and 18 (15-21); area under the plasma concentration-time curve (nmol.bul.h.bul.L-1), 118 (103-136), 84 (73-97), 64 (56-74) and 59 (51-68). Subjects showed higher heart rates with C. paradisi Macf than with C. changshanhuyou Y.B. Chang or water. *Subject total: Subjects were healthy volunteers.Note : Data incomplete.
