Abstract
Chaihu-Shu-Gan-San (CSGS), a traditional Chinese medicine (TCM) formula containing seven herbal medicines, has been used in the clinical treatment of gastritis, peptic ulcer, irritable bowel syndrome and depression in China. In order to explore the interaction between naringin and other constituents in CSGS, the pharmacokinetic difference of naringin in rats after oral administration of CSGS aqueous extract and naringin alone was investigated. The pharmacokinetic parameters of naringin in rats were achieved by quantification of its aglycone, naringenin by LC-MS/MS method. The double peaks phenomenon was observed in both serum profiles of rats after orally administered CSGS aqueous extract and naringin alone. However, the T1/2β was significantly decreased in rats given CSGS aqueous extract compared with naringin alone, and the mean residence time (MRT) and the area under the serum concentration–time curve (AUC0-τ) were higher than those of naringin, which indicated that naringin in CSGS had higher bioavailability, longer term efficacy and somewhat faster metabolism and excretion than those of naringin. The results suggested that certain ingredients co-exist in CSGS could influence pharmacokinetic behavior of naringin. This also provides a reference for human studies.
Highlights
Traditional Chinese Medicines (TCMs) have been proved to have a significant effect in the treatment of chronic and systematic diseases with fewer side effects than other treatments
After the rats were orally administrated of CSGS aqueous extract or naringin monomer, the main present form in serum was naringenin glucuronide conjugation
The concentration of naringin in rat serum can be expressed by the concentration of naringenin glucuronide conjugation, which was determined by a liquid chromatography system coupled to a mass spectrometry detector (MS/MS)
Summary
Traditional Chinese Medicines (TCMs) have been proved to have a significant effect in the treatment of chronic and systematic diseases with fewer side effects than other treatments. In Chinese herbal therapy, the most widely used medicines are combined by many herbs and prepared according to TCM formulation concepts. It is acknowledged that complex interactions could produce synergistic effects and reduce possible side effects from some of the herbs. Little evidence is available to interpret the mechanisms of those magic actions. Pharmacokinetics is useful to explain the metabolism status of drugs in vivo and to predict situations related to pharmacodynamics. Pharmacokinetic characteristics of herbal medicines maybe benefit the interpretation of the rationality for the advantage of multi-constituents
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