2006•Traditional Chinese Drug Research and Clinical PharmacologyRequires access

Pharmacokinetics Study of Schisandrin in Shengmai Granule

JI Liyue

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Abstract

objective To study the pharmacokinetics of lignans components in Shengmai granule in volunteers and in mice. Methods After oral administration of Shengmai granule (3.6 g/person) for the volunteers and ig administration of the drug (4.7 g/kg) for the mice, the plasma was collected at different time points. The lignans components in Shengmai granule and in the plasma were analyzed by HPLC to monitor the changes of plasma concentration of schisandrind. Pharmacokinetic parameters were calculated from the plasma concentration- time data with the 3P97 software package. Results After oral administration of Shengmai granule by volunteers and mice, schisandrin and some new components in plasma were detected. The new components may be the metabolites of schisandrin. The main pharmacokinetic parameters of schisandrin in mice and in volunteers were as follows: T1/2ka was 0.03 and 0.04 hour, T1/2ke 0.88 and 0.86 hour, Vd 19.12 and 1.73 L· kg- 1, CL 15.06 and 1.46 L· h- 1· kg- 1, Cmax 1.196 and 0.098 mg· L- 1, Tpeak0.21 and 0.50 h, AUC0- ∞ 1.096 and 0.137 mg· h· L- 1, respectively. Conclusion Schisandrin in Shengmai granule can be absorbed in the volunteers and mice after oral administration. It can be absorbed and eliminated rapidly, and can be transformed into the metabolite. The pharmacokinetics of plasma Schizandrin complies with linear kinetic course.

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What this paper is about

objective To study the pharmacokinetics of lignans components in Shengmai granule in volunteers and in mice. Methods After oral administration of Shengmai granule (3.6 g/person) for the volunteers and ig administration of the drug (4.7 g/kg) for the mice, the plasma was collected at different time points. The lignans components in Shengmai granule and in the plasma were analyzed by HPLC to monitor the changes of plasma concentration of schisandrind. Pharmacokinetic parameters were calculated from the plasma concentration- time data with the 3P97 software package. Results After oral administration of Shengmai granule by volunteers and mice, schisandrin and some new components in plasma were detected. The new components may be the metabolites of schisandrin. The main pharmacokinetic parameters of schisandrin in mice and in volunteers were as follows: T1/2ka was 0.03 and 0.04 hour, T1/2ke 0.88 and 0.86 hour, Vd 19.12 and 1.73 L· kg- 1, CL 15.06 and 1.46 L· h- 1· kg- 1, Cmax 1.196 and 0.098 mg· L- 1, Tpeak0.21 and 0.50 h, AUC0- ∞ 1.096 and 0.137 mg· h· L- 1, respectively. Conclusion Schisandrin in Shengmai granule can be absorbed in the volunteers and mice after oral administration. It can be absorbed and eliminated rapidly, and can be transformed into the metabolite. The pharmacokinetics of plasma Schizandrin complies with linear kinetic course.

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Available abstract

objective To study the pharmacokinetics of lignans components in Shengmai granule in volunteers and in mice. Methods After oral administration of Shengmai granule (3.6 g/person) for the volunteers and ig administration of the drug (4.7 g/kg) for the mice, the plasma was collected at different time points. The lignans components in Shengmai granule and in the plasma were analyzed by HPLC to monitor the changes of plasma concentration of schisandrind. Pharmacokinetic parameters were calculated from the plasma concentration- time data with the 3P97 software package. Results After oral administration of Shengmai granule by volunteers and mice, schisandrin and some new components in plasma were detected. The new components may be the metabolites of schisandrin. The main pharmacokinetic parameters of schisandrin in mice and in volunteers were as follows: T1/2ka was 0.03 and 0.04 hour, T1/2ke 0.88 and 0.86 hour, Vd 19.12 and 1.73 L· kg- 1, CL 15.06 and 1.46 L· h- 1· kg- 1, Cmax 1.196 and 0.098 mg· L- 1, Tpeak0.21 and 0.50 h, AUC0- ∞ 1.096 and 0.137 mg· h· L- 1, respectively. Conclusion Schisandrin in Shengmai granule can be absorbed in the volunteers and mice after oral administration. It can be absorbed and eliminated rapidly, and can be transformed into the metabolite. The pharmacokinetics of plasma Schizandrin complies with linear kinetic course.

Key concepts: Pharmacokinetics, Granule (geology), Cmax, Pharmacology, Plasma concentration, Oral administration, Chemistry, Active metabolite

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