Nakae Hajime, Fujita Yuji, Igarashi Toshiko, Tajimi Kimitaka, Endo Shigeatsu
Department of Integrated Medicine, Division of Emergency and Critical Care Medicine, Akita University School of Medicine, Akita, Japan.
Biomed Res. 2008 Oct;29(5):225-31. doi: 10.2220/biomedres.29.225.
Processed Bushi powder for ethical dispensing, called TJ-3022, is a herbal drug of processed Aconiti tuber (Aconitum carmichaeli Debeaux) and TJ-3023 is newly developed to contain a higher proportion of diester alkaloid of aconitine (Aconitum carmichaeli Debeaux and Aconitum japonicum Thunberg). Safety of TJ-3022 and TJ-3023 was evaluated by measuring the level of aconitum alkaloids in healthy adult volunteers. Forty subjects were assigned to one of two groups (each 20 subjects): TJ-3022 group or TJ-3023 group. The subjects received the powdered processed Aconiti tuber 3 g/day and the blood concentrations of aconitum alkaloids were measured at 90 min and 72 h after taking the study drug. The serum concentrations of aconitum alkaloids after 90 min and 72 h in the TJ-3023 group were higher than those in the TJ-3022 group. As for the chronological changes in the serum concentration, a significant decrease was observed in the TJ-3022 group, while no significant decrease was seen in the TJ-3023 group, which suggests that an analgesic effect in TJ-3023 was stronger than in TJ-3022. Aconitum alkaloids, which always have been believed to have the blood concentration below the measurement limit in human, were detected for the first time, although the detected amounts were minute. The results suggest that TJ-3023 shows sufficient analgesic effect with smaller dose than TJ-3022.
用于规范调配的炮制附子散剂,称为TJ - 3022,是一种以制川乌(乌头)为原料的草药制剂,而TJ - 3023是新开发的,含有更高比例的乌头碱双酯生物碱(乌头和日本乌头)。通过测量健康成年志愿者体内乌头生物碱水平来评估TJ - 3022和TJ - 3023的安全性。40名受试者被分为两组(每组20名受试者):TJ - 3022组或TJ - 3023组。受试者每天服用3克炮制附子散剂,并在服用研究药物后90分钟和72小时测量乌头生物碱的血药浓度。TJ - 3023组在90分钟和72小时后的乌头生物碱血清浓度高于TJ - 3022组。关于血清浓度的时间变化,TJ - 3022组观察到显著下降,而TJ - 3023组未观察到显著下降,这表明TJ - 3023的镇痛效果比TJ - 3022更强。尽管检测到的量很少,但首次检测到一直被认为在人体血药浓度低于测量限的乌头生物碱。结果表明,TJ - 3023比TJ - 3022以更小的剂量显示出足够的镇痛效果。