| Synonym |
| Thai / English name |
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Single-blind trialN(Total) : 13N(Treatment) : 13Sex : MaleAge : 35 +/- 8 yrs.Route : Oral administrationDose/Conc.(herb) : 8 ozDuration :Type of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : 6 mg (p.o.)Result : PositiveRemark : Subjects: healthy male volunteers participated in a randomized, single-dose, 5-way crossover study, with 1 week elapsing between trials. The 5 treatment groups were: 1. Intravenous (IV) midazolam (2 mg) preceded by water 2. Oral midazolam (6 mg) preceded by water 3. IV midazolam (2 mg) preceded by pomegranate juice 4. Oral midazolam (6 mg) preceded by pomegranate juice 5. Oral midazolam (6 mg) preceded by grapefruit juice Results: Pretreatment of volunteer subjects with pomegranate juice did not alter the elimination half-life, volume of distribution, or clearance of intravenous midazolam (2 mg). Administration of pomegranate juice also did not affect Cmax, total area under the curve (AUC), or clearance of oral midazolam (6 mg).
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Cross overN(Total) : 13N(Treatment) : 13Sex : MaleAge : 35 +/- 8 yrs.Route : Oral administrationDose/Conc.(herb) : 8 ozDuration :Type of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : 6 mg (p.o.)Result : PositiveRemark : Subjects: healthy male volunteers participated in a randomized, single-dose, 5-way crossover study, with 1 week elapsing between trials. The 5 treatment groups were: 1. Intravenous (IV) midazolam (2 mg) preceded by water 2. Oral midazolam (6 mg) preceded by water 3. IV midazolam (2 mg) preceded by pomegranate juice 4. Oral midazolam (6 mg) preceded by pomegranate juice 5. Oral midazolam (6 mg) preceded by grapefruit juice Results: Pretreatment of volunteer subjects with pomegranate juice did not alter the elimination half-life, volume of distribution, or clearance of intravenous midazolam (2 mg). Administration of pomegranate juice also did not affect Cmax, total area under the curve (AUC), or clearance of oral midazolam (6 mg).
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: (AUC0-8) of midazolam was higher on days 1 and 3 than on the control day (mean ratio, 2.12 and 1.47, respectively). The AUC0-8 returned to the control level on day 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : OATP (ORGANIC ANION TRANSPORTER PROTEIN) INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: (AUC0-8) of midazolam was higher on days 1 and 3 than on the control day (mean ratio, 2.12 and 1.47, respectively). The AUC0-8 returned to the control level on day 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: (AUC0-8) of midazolam was higher on days 1 and 3 than on the control day (mean ratio, 2.12 and 1.47, respectively). The AUC0-8 returned to the control level on day 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 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) : Caco-2 cell cultures were first preincubated with micromol/L of 6',7'-dihydroxybergamottin for 30 minutes and then incubated simultaneously with 6',7'-dihydroxybergamottin and midazolam (3 micromol/L) for 4 hours.Duration : 30 min. and 4 hr.Type of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : midazolam (CYP3A probe) 3 micromol/LResult : PositiveRemark : Result: 6',7'-Dihydroxybergamottin (10 micromol/L) inhibited midazolam 1'-hydroxylation by 93% compared with control. Comparatively, the CYP3A4 inhibitors troleandomycin (30 micromol/L) and ketoconazole (1 and 10 micromol/L) inhibited midazolam 1'-hydroxylation by 60% and at least 75%, respectively. Mean control activities for mechanismbased inhibitor- and ketoconazole-treated cultures were 95 and 107 pmol per hour per culture, respectively.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : BergaptenType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : Caco-2 cell cultures were first preincubated with 10 micromol/L of betgapten for 30 minutes and then incubated simultaneously with bergapten and midazolam (3 micromol/L) for 4 hours.Duration : 30 min. and 4 hr.Type of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : midazolam (CYP3A probe) 3 micromol/LResult : EquivocalRemark : Result: Bergapten (10 micromol/L) inhibited midazolam 1'-hydroxylation only 34% compared with control. Comparatively, the CYP3A4 inhibitors troleandomycin (30 micromol/L) and ketoconazole (1 and 10 micromol/L) inhibited midazolam 1'-hydroxylation by 60% and at least 75%, respectively. Mean control activities for mechanismbased inhibitor- and ketoconazole-treated cultures were 95 and 107 pmol per hour culture, respectively.
