Introduction: Asari Radix et Rhizoma (ARR) and dried ginger (Zingiber officinalis)
(DG) are often used together in drug preparations in traditional Chinese medicine (TCM) to treat
respiratory diseases, including cold, bronchitis and pneumonia. Previous studies suggested that
ARR and/or DG may influence the pharmacokinetics of other herbal components. In the current
study, we examined pharmacokinetic interactions between ARR and DG in rats after oral administration.
Methods: We developed a method based on ultra-high-performance liquid chromatographytandem
mass spectrometry to simultaneously measure serum concentrations of two active components
each in ARR (L-asarinin and sesamin) and DG (6-gingerol and 6-shogaol). Adult Sprague-
Dawley rats were starved overnight, then given ARR extract, DO extract, or a co-decoction
of ARR and DG by gastric gavage (6 g raw material per kg body weight; n = 6 per group). Blood
samples were collected prior to drug administration and at the following times (h) afterward: 0.5,
1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 12.0 and 24.0. Pharmacokinetic parameters were compared using
Student’s t test for independent samples.
Results: A simple, rapid, sensitive analytical method has been developed to detect four bioactive
components simultaneously in the ARR-DG herbal pair. Pharmacokinetic parameters including
Cmax, Tmax, T1/2 and AUC(0~t) were calculated using the non-compartmental model with the DAS
2.0 pharmacokinetic software. For L-asarinin, Tmax was 2.00 ± 0.00 h in ARR animals and
1.67±0.26 h in ARR-DG animals (P<0.05), T1/2 was 8.58 ± 1.75 h in ARR and 11.93 ± 2.13 h in
ARR-DG (P<0.05). For 6-gingerol, Cmax was 350.48 ± 23.85 ng/mL in DG animals and 300.21 ±
20.02 ng/mL in ARR-DG (P<0.01), Tmax was 2.83 ± 0.41 h in DG and 2.17 ± 0.41 h in ARR-DG
(P<0.05) and AUC(0~t) was 1.93 ± 0.15 mg/mL.h in ARR and 1.70 ± 0.15 mg/mL.h in ARR-DG
(P<0.05). For 6-shogaol, Cmax was 390.28 ± 26.02 ng/mL in DG animals and 455.63 ± 31.01
ng/mL in ARR-DG (P<0.01), Tmax was 2.93 ± 0.10 h in DG and 1.92 ± 0.10 h in ARR-DG
(P<0.01), T1/2 was 3.74 ± 0.29 h in DG and 3.28 ± 0.22 h in ARR-DG (P<0.01), and AUC(0~t)
was 2.15 ± 0.18 mg/mL.h in DG and 2.73 ± 0.15 mg/mL.h in ARR-DG (P<0.01).
Conclusion: Pharmacokinetic interactions between ARR and DG decreased Tmax, increased T1/2
but did not affect the overall bioavailability of L-asarinin in ARR. The interactions in ARR-DG
decreased Cmax and Tmax but increased T1/2 and AUC(0~t) of 6-gingerol in DG. The interactions increased
Cmax and AUC(0~t) but decreased Tmax and T1/2 of 6-shogaol in DG. Interactions in ARRDG
did not affect the pharmacokinetics of sesamin.