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Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/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 : EFFECTS ON PHARMACOKINETICSolvent/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 : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/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 : 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 : 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.
Part Used : น้ำจากผลActivity : EFFECTS ON PHARMACOKINETICSolvent/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.
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : Furanocoumarins, Fruit juices of 'changshanhuyou' (Citrus changshanhuyou Y.B. Chang)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 Changshanhuyou 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.
Part Used : น้ำจากผลActivity : EFFECTS ON PHARMACOKINETICSolvent/Active Compound : Furanocoumarins, Fruit juices of 'changshanhuyou' (Citrus changshanhuyou Y.B. Chang)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 Changshanhuyou 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.
Part Used : น้ำจากผลActivity : EFFECTS ON PHARMACOKINETICSolvent/Active Compound : Furanocoumarins, Fruit juices of pummel grapefruit (Citrus paradisi Mscf)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 : 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 had 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 : DRUG INTERACTIONSolvent/Active Compound : Furanocoumarins, Fruit juices of pummel grapefruit (Citrus paradisi Mscf)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 : 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 had 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.