Objective: To study the pharmacokinetics of 20(R)-Ginsenoside Rg3 in the human body. Methods: High-performance liquid chromatography-ultraviolet detection method was used in this study. Results: The pharmacokinetics o...Objective: To study the pharmacokinetics of 20(R)-Ginsenoside Rg3 in the human body. Methods: High-performance liquid chromatography-ultraviolet detection method was used in this study. Results: The pharmacokinetics of Ginsenoside Rg3 in 14 healthy volunteers were investigated. After a single oral dose of 3.2 mg.g-1 Ginsenoside Rg3 in 8 male volunteers, the plasma concentration-time course fitted in well with a two-compartment open model, with the following pharmacokinetic parameters: Tmax 0.660.10 h, Cmax 166 ngmL-1, T1/2a 0.460.12 h, T1/2b 4.91.1 h, T1/2(Ka) 0.280.04 h, AUC0-∞ 7726 ngmL-1h, respectively. No kinetic analysis was made after an oral dose of 0.8 mg.g-1 Rg3 in other 6 volunteers because of the low concentration, but there was a good correlation between Cmax and dosage of the two groups. Conclusion: The absorption of Rg3 was rapid in the human body, and its elimination was rapid too after oral administration of Ginsenoside Rg3. The pharmacokinetic results shows that it exhibited the first-order kinetic characteristics.展开更多
In the present study, we aimed to investigate the effect of CYP3A4＊ 18 genotype on the pharmacokinetics of zolpidem in healthy Chinese Hui volunteers. Blood samples were collected from volunteers for CYP3A4 genotypin...In the present study, we aimed to investigate the effect of CYP3A4＊ 18 genotype on the pharmacokinetics of zolpidem in healthy Chinese Hui volunteers. Blood samples were collected from volunteers for CYP3A4 genotyping using a polymerase chain reaction-restriction fragment length polymorphism （PCR-RFLP） assay. A pharmacokinetic study was then carried out in three groups with CYP3A4＊1/＊1 （n = 6）, CYP3A4＊1/＊18 （n = 6） and CYP3A4＊18/＊18 （n = 6） genotypes. Plasma levels of zolpidem were determined by HPLC-FLD method before and after a single oral dose of 10 mg zolpidem tartrate tablet. Significant differences were observed in the pharmacokinetic parameters of zolpidem among the three genotype groups （P〈0.05）. Compared with the CYP3A4＊1/＊1 group, the Cm,x of zolpidem in ＊1/＊18 and ＊18/＊18 groups （mean, 95% CI） was 0.89 （0.65-1.12） and 0.57 （0.47-0.66）, respectively, and the AUC0-1 in the ＊1/＊18 and ＊18/＊18 groups （mean, 95% CI） was 0.74 （0.22-1.26） and 0.61 （0.24-0.98）, respectively. There was a significant trend towards lower Cmax and AUC0-1 values of zolpidem in individuals with more CYP3A＊ 18 alleles, suggesting a gene-dosage effect. The study demonstrated that the CYP3A4＊ 18 allele played an important role in the pharmacokinetics of the zolpidem after oral administration.展开更多
文摘Objective: To study the pharmacokinetics of 20(R)-Ginsenoside Rg3 in the human body. Methods: High-performance liquid chromatography-ultraviolet detection method was used in this study. Results: The pharmacokinetics of Ginsenoside Rg3 in 14 healthy volunteers were investigated. After a single oral dose of 3.2 mg.g-1 Ginsenoside Rg3 in 8 male volunteers, the plasma concentration-time course fitted in well with a two-compartment open model, with the following pharmacokinetic parameters: Tmax 0.660.10 h, Cmax 166 ngmL-1, T1/2a 0.460.12 h, T1/2b 4.91.1 h, T1/2(Ka) 0.280.04 h, AUC0-∞ 7726 ngmL-1h, respectively. No kinetic analysis was made after an oral dose of 0.8 mg.g-1 Rg3 in other 6 volunteers because of the low concentration, but there was a good correlation between Cmax and dosage of the two groups. Conclusion: The absorption of Rg3 was rapid in the human body, and its elimination was rapid too after oral administration of Ginsenoside Rg3. The pharmacokinetic results shows that it exhibited the first-order kinetic characteristics.
基金Funds of the Chinese Army Medical Science and Technology Research"Eleventh Five-Year Plan"Project(Grant No.06G023)
文摘In the present study, we aimed to investigate the effect of CYP3A4＊ 18 genotype on the pharmacokinetics of zolpidem in healthy Chinese Hui volunteers. Blood samples were collected from volunteers for CYP3A4 genotyping using a polymerase chain reaction-restriction fragment length polymorphism （PCR-RFLP） assay. A pharmacokinetic study was then carried out in three groups with CYP3A4＊1/＊1 （n = 6）, CYP3A4＊1/＊18 （n = 6） and CYP3A4＊18/＊18 （n = 6） genotypes. Plasma levels of zolpidem were determined by HPLC-FLD method before and after a single oral dose of 10 mg zolpidem tartrate tablet. Significant differences were observed in the pharmacokinetic parameters of zolpidem among the three genotype groups （P〈0.05）. Compared with the CYP3A4＊1/＊1 group, the Cm,x of zolpidem in ＊1/＊18 and ＊18/＊18 groups （mean, 95% CI） was 0.89 （0.65-1.12） and 0.57 （0.47-0.66）, respectively, and the AUC0-1 in the ＊1/＊18 and ＊18/＊18 groups （mean, 95% CI） was 0.74 （0.22-1.26） and 0.61 （0.24-0.98）, respectively. There was a significant trend towards lower Cmax and AUC0-1 values of zolpidem in individuals with more CYP3A＊ 18 alleles, suggesting a gene-dosage effect. The study demonstrated that the CYP3A4＊ 18 allele played an important role in the pharmacokinetics of the zolpidem after oral administration.
