Title:Effect of Carbonized Herba schizonepetae on the Bioavailability of Eight Active
Components from Pulsatillae Decoction in its Particular Adsorption and Release
Performance
Volume: 22
Issue: 12
Author(s): Cuiyan Liu, Yun Zhu, Yanfei He, Guangtai Fan, Jingang Gu* Chunyang Han*
Affiliation:
- Institute of Agricultural Resources and Regional Planning
(IARRP), Chinese Academy of Agricultural Sciences, Beijing 100081, China
- College of Animal Science and Technology, Anhui Agricultural University, Hefei, 230036, China
Keywords:
Carbonized Herba schizonepetae, Pulsatillae decoction, adsorption, release, pharmacokinetics, bioavailability.
Abstract:
Background: Carbonized herbal medicine has been used clinically for centuries in China; however, its
influence on the bioavailability of compatible medicinal herbs is still unknown.
Objectives: To explore the effect of a carbonized herbal medicine on the in vivo adsorption and release and absorption
of other active pharmaceutical ingredients in a compound prescription.
Methods: The bioavailability of carbonized Herba schizonepetae (CHS) to eight active components (epiberberine,
coptisine, palmatine, berberine, phellodendrine, aesculin, aesculetin, and anemoside B4) in the aqueous extract of
Pulsatillae Decoction (PDAE) was evaluated by the in vitro adsorption and release and in vivo pharmacokinetics
tests. Activated carbon (AC) was used as the control.
Results: In vitro experiment showed that the cumulative adsorption rates of CHS to the eight active components were
33.17%, 54.32%, 21.48%, 42.01%, 39.1%, 25.11%, 32.11%, and 23.08% which was characterized by copsitine >
berberine > phellodendrine > epiperberine > aesculetin > anemoside B4 > palmatine., and they were significantly
lower than those of AC. The stable release concentration in sequence was 3.23, 3.04, 3.32, 7.29, 3.17, 2.80, 1.45, and
3.81 μg/mL, which was characterized by berberine > anemoside B4 > palmatine > epiberberine > phellodendrine >
coptisine > aesculin > aesculetin, and they were significantly higher than those of AC. The animal experiment indicated
that the areas under the concentration-time curve (AUC0-∞) of epiberberine, berberine, aesculetin, and anemoside
B4 in PDAE+CHS group were significantly higher than those in the PDAE and PDAE+AC groups, and the
other four components in the PDAE+CHS group were lower than those in PDAE group but higher than those in
PDAE+AC group.
Conclusion: CHS could significantly improve the bioavailability of epiberberine, berberine, aesculetin, and anemoside
B4 in Pulsatillae Decoction and has a sustained-release effect on berberine, aesculin, aesculetin, and anemoside
B4.