Zhao K C, Song Z Y
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing.
Yao Xue Xue Bao. 1990;25(2):147-9.
Qinghaosu (QHS), also known as artemisinine and arteannuin, is isolated from the Chinese herb Artemisia annua L. It is highly active against both chloroquine-sensitive and chloroquine-resistant strains of P. berghei and has been approved by the Ministry of Health for the treatment of malaria. When QHS is treated with sodium borohydride, dihydroqinghaosu (DH QHS) is resulted with the antimalarial activity enhanced several fold. This paper reports the pharmacokinetics of DHQHS studied with the radioimmunoassay method. When the drug was given orally in tablet form to rabbits at doses of 10, 20 and 30 mg/kg, peak serum levels of 0.03, 0.05 and 0.13 micrograms/ml, respectively, were obtained in 1 to 2 h. The corresponding T1/2 of the drug were found to be 1.19, 1.00 and 1.10 h and the MRTs were 1.73, 1.36 and 1.53 h. No significant difference between dosages used was observed. When dogs were given DHQHS tablets at the dose of 20 mg/kg, a peak serum concentration of 0.13 micrograms/ml wes reached in about 2 h with a T1/2 of 2.10 h and an MRT of 3.04 h. However, when dogs were given QHS tablets at the dose of 70 mg/kg, no drug was detected in the serum. It would appear that the bioavailability of DHQHS tablets is much higher than that of QHS when given orally to the dog.
青蒿素（QHS），又称黄花蒿素和青蒿苷，是从中药黄花蒿中提取的。它对伯氏疟原虫的氯喹敏感株和氯喹耐药株均具有高效活性，已被卫生部批准用于治疗疟疾。当青蒿素用硼氢化钠处理时，会产生双氢青蒿素（DH QHS），其抗疟活性提高了几倍。本文报道了用放射免疫分析法研究双氢青蒿素的药代动力学。当以片剂形式给家兔口服该药物，剂量分别为10、20和30mg/kg时，在1至2小时内血清峰值水平分别为0.03、0.05和0.13微克/毫升。发现该药物相应的半衰期分别为1.19、1.00和1.10小时，平均驻留时间分别为1.73、1.36和1.53小时。未观察到所用剂量之间的显著差异。当以20mg/kg的剂量给犬服用双氢青蒿素片时，约2小时后血清峰值浓度达到0.13微克/毫升，半衰期为2.10小时，平均驻留时间为3.04小时。然而，当以70mg/kg的剂量给犬服用青蒿素片时，血清中未检测到药物。口服给药时，双氢青蒿素片的生物利用度似乎远高于青蒿素。
