Urinary Elimination of Ephedrines Following Administration of the Traditional Chinese Medicine Preparation Kakkon-to

Abstract

Kakkon-to is one of the most common Traditional Chinese Medicine preparations for the attenuation of colds. Ephedrae Herba is one of the prescriptions of Kakkon-to. The major ingredients of Ephedrae Herba, ephedrines, are banned substances on the World Anti-Doping Agency (WADA) list. The purpose of this study was to investigate the elimination of urinary ephedrines after administering Kakkon-to and to determine the possibility of urinary positive ephedrine test results. Six healthy volunteers took one single dose of 2.5 g Kakkon-to extract granules. The concentrations of urinary ephedrines were analyzed by high-performance liquid chromatography. The result showed that ephedrine and norpseudoephedrine were excreted in the urine after taking one single dose of Kakkon-to. However, the highest amount of ephedrines in urine was ephedrine and the peak concentration was 4.35 +/- 1.82 microg/mL (mean +/- standard deviation), which was lower than the WADA permitted value (10 microg/mL). The estimated elimination half-lives of ephedrine, norephedrine, pseudoephedrine, and norpseudoephedrine following administration of this preparation were: 5.2 +/- 1.2, 4.2 +/- 1.3, 4.2 +/- 0.9, and 6.5 +/- 2.8 h, respectively. This study concluded that the urine would not violate the rule of doping after administering a single dose of Kakkon-to. Nevertheless, a further study on administering the preparation for 3 times per day for 3 days showed a positive ephedrine result. Athletes should be careful when taking more than a single dose of Kakkon-to.

The traditional herbal medicine, Ge-Gen-Tang, inhibits pacemaker potentials by nitric oxide/cGMP dependent ATP-sensitive K+ channels in cultured interstitial cells of Cajal from mouse small intestine

“…They have become more popular worldwide (Goldbeck-Wood, 1996;Eisenberg et al, 1998). GGT is one of the most important preparations of TCM which has been used as anti-cold, antipyretic, analgesic, and for nasal decongestion (Chan et al, 2008). In GI tract, GGT had immunosuppressive effects and interfered with the infiltration of mucosal mast cells in the colons of mice with induced food allergy, leading to improvement of allergic symptoms (Yamamoto et al, 2009).…”

Traditional Chinese medicine and sports drug testing: identification of natural steroid administration in doping control urine samples resulting from musk (pod) extracts

“…The potential risk of adverse analytical findings in the course of doping controls has also been discussed particularly for TCM preparations used for the attenuation of the common cold, containing, for example, Ephedrae Herba as a major component of Sho-seiryu-to,3 Kakkon-to4 and Ma Huang 5. These herbal products were shown to contain ephedrine and its structural analogues such as norephedrine, pseudoephedrine and cathine that would lead to a positive test result if urinary threshold levels are exceeded.…”

Ephedra alkaloid contents of Chinese herbal formulae sold in Taiwan

“…Chan et al . administered single doses of 2.5 g GGT (containing 3.44 mg E, 0.42 mg ME, 0.25 mg NPE, 1.55 mg PE, and 0.15 mg NE) or 2.5 g XQLT (containing 2.98 mg E, 0.36 mg ME, 0.23 mg NPE, 1.35 mg PE, and 0.14 mg NE) and demonstrated urine concentrations of 5.33 and 4.67 μg/mL for E, negligible concentrations for ME, 0.53 and 0.46 μg/mL for NPE, 2.66 and 2.40 μg/mL for PE, and 0.57 and 0.58 μg/mL for NE in participants who took GGT and XQLT.…”

“…Minor metabolic products – 1.6% NE after E consumption, 1.6% E after ME consumption, and 0.7% NPE after PE consumption, respectively – were also noted. These findings explained the low excretion of ME noted in previous studies …”