COMPOSITAE (ASTERACEAE) Carthamus tinctorius  L.

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[1] EFFECTS OF HYDROXYSAFFLOR YELLOW A ON THE ACTIVITY AND MRNA EXPRESSION OF FOUR CYP ISOZYMES IN RATS.
REN-AI XU,ZHI-SHENG XU , REN-SHAN GE
J ETHNOPHARMACOL 2014 Vol.151(),1141-46  $50677 [Full]

Part Used : ดอก
Activity : DRUG INTERACTION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : EFFECTS ON PHARMACOKINETIC
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : DRUG INTERACTION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : EFFECTS ON PHARMACOKINETIC
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 3 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Equivocal
Remark : Drug; On the fourth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration. Results; The pharmacokinetic parameters of phenacetin in rats showed no significant difference among LSG, HSG and BCG.
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : DRUG INTERACTION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; After pretreatment with HSYA, the t1/2, Tmax, Cmax, AUC (0- infinity) and MRT (0-infinity) of phenacetin in LLG were increased significantly by 36.2%, 33.3%, 32.9%, 94.6% and 74.9% (P<0.05) compared to those of BCG, CL of phenacetin in LLG was decreased significantly by 46.3% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : EFFECTS ON PHARMACOKINETIC
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; After pretreatment with HSYA, the t1/2, Tmax, C max, AUC (0- infinity) and MRT (0-infinity) of phenacetin in LLG were increased significantly by 36.2%, 33.3%, 32.9%, 94.6% and 74.9% (P<0.05) compared to those of BCG, CL of phenacetin in LLG was decreased significantly by 46.3% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : CYP1A2 INHIBITION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 3.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; After pretreatment with HSYA, the t1/2, Tmax, C max, AUC (0- infinity) and MRT (0-infinity) of phenacetin in LLG were increased significantly by 36.2%, 33.3%, 32.9%, 94.6% and 74.9% (P<0.05) compared to those of BCG, CL of phenacetin in LLG was decreased significantly by 46.3% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.

Part Used : ดอก
Activity : DRUG INTERACTION
Solvent/Active Compound : Hydroxysafflor yellow A (HSYA)
Type of experiment : in vivo
Type of animal : rat
Type of study : -
N(Total) : -
N(Treatment) : -
Sex : -
Age : -
Route : Intravenous
Dose/Conc.(herb) : 12.0 mg/kg
Duration : 14 days
Type of interaction : Pharmacokinetics
Interaction with drug : Phenacetin*/Acetophenetidin
Dose/Conc.(drug) : -
Result : Positive
Remark : Drug; On the eleventh or fifteenth day, a cocktail solution at a dose of 5 mL/kg, which contained phenacetin (20 mg/kg), tolbutamide (5 mg/kg), dextromethorphan (20 mg/kg) and midazolam (10 mg/kg) in CMC-Na solution, was administered orally to all rats in each group. Blood samples of each rat were collected pre-dose (0 h) and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 h after probe drugs administration through the tail vein. Results; The t1/2, Tmax, Cmax, AUC (0- infinity) and MRT (0-infinity) of phenacetin in HLG were increased significantly by 63.8%, 52.6%, 82.6%, 193.5% and 78.7% (P<0.05) compared to those of BCG, CL of phenacetin in HLG was decreased significantly by 46.5% (P<0.05).
Note : T1/2: half-life; Tmax: the time of peak concentration; Cmax: the peak or maximum concentration; AUC(0-infinity): area under a curve extrapolated to infinity; MRT: mean residence time; CL: the total body clearance; BCG: blank control group; LSG: low dosage (3.0 mg/kg/day) and short period (3 days) group; LLG: low dosage and long period (14 days) group; HSG: high dosage (12.0 mg/kg/day) and short period group; HLG: high dosage and long period group.


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