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Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 21*N(Treatment) : 21Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : 200 ml GFJDuration : For development of the pharmacokinetic model of felodipine-GFJ interaction in this study, they utilized pharmacokinetic data obtained from two clinical trials. In the first, nine healthy male volunteers were given 10 mg felodipine ER orally together with either 200 ml tap water or GFJ at 0, 1, 4, 10 or 24 h before administration of felodipine. In the second, 12 healthy male volunteers received 10 mg felodipine ER after daily intake of either 200 ml of tap water of GFJ for 1 day or 14 days.Type of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : 10 mg felodipine ER (extended release formulation)Result : PositiveRemark : Result: The model gave a turnover rate of CYP3A4 of 0.0849 h-1, corresponding to a half-life of 8.16 h. Conclusions: GFJ-felodipine interaction increases with increasing frequency and amount of GFJ ingestion, and that an interval of 2-3 days between GFJ intake and felodipine administration is necessary if GFJ-felodipine interaction is to be avoided.
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 21*N(Treatment) : 21Sex : MaleAge : -Route : Oral administrationDose/Conc.(herb) : 200 ml GFJDuration : For development of the pharmacokinetic model of felodipine-GFJ interaction in this study, they utilized pharmacokinetic data obtained from two clinical trials. In the first, nine healthy male volunteers were given 10 mg felodipine ER orally together with either 200 ml tap water or GFJ at 0, 1, 4, 10 or 24 h before administration of felodipine. In the second, 12 healthy male volunteers received 10 mg felodipine ER after daily intake of either 200 ml of tap water of GFJ for 1 day or 14 days.Type of interaction : PharmacokineticsInteraction with drug : FelodipineDose/Conc.(drug) : 10 mg felodipine ER (extended release formulation)Result : PositiveRemark : Result: The model gave a turnover rate of CYP3A4 of 0.0849 h-1, corresponding to a half-life of 8.16 h. Conclusions: GFJ-felodipine interaction increases with increasing frequency and amount of GFJ ingestion, and that an interval of 2-3 days between GFJ intake and felodipine administration is necessary if GFJ-felodipine interaction is to be avoided.
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 : CYP3A4 INHIBITIONSolvent/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 : CYP3A4 INHIBITIONSolvent/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 : CYP1A INHIBITIONSolvent/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 : EFFECTS ON PHARMACOKINETICSolvent/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 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.
