李成韶, 杜以兰. 根据青蒿素药效半衰期制订给药方案的探讨J. 药学学报, 1984, 19(6): 410-414.
引用本文: 李成韶, 杜以兰. 根据青蒿素药效半衰期制订给药方案的探讨J. 药学学报, 1984, 19(6): 410-414.
LI Cheng-shao, DU Yi-lan. RESEARCH ON THE DOSE REGIME OF QINGHAOSU ADMINISTRATION ACCORDING TO ITS BIOLOGICAL HALF-LIFEJ. Acta Pharmaceutica Sinica, 1984, 19(6): 410-414.
Citation: LI Cheng-shao, DU Yi-lan. RESEARCH ON THE DOSE REGIME OF QINGHAOSU ADMINISTRATION ACCORDING TO ITS BIOLOGICAL HALF-LIFEJ. Acta Pharmaceutica Sinica, 1984, 19(6): 410-414.

根据青蒿素药效半衰期制订给药方案的探讨

RESEARCH ON THE DOSE REGIME OF QINGHAOSU ADMINISTRATION ACCORDING TO ITS BIOLOGICAL HALF-LIFE

  • 摘要: 为了降低用青蒿素治疗后疟疾的复燃率,用鼠疟模型测定了青蒿素的药效半衰期,并用两种不同给药方案进行了治疗实验。A方案参照药效半衰期每12 h肌注总量的1/6,首次倍量;B方案仿临床用法每隔24 h肌注总量的1/3。A方案各组与相应的B方案各组3天总量相等。共观察3个月。结果表明青蒿素药效半衰期为10.5±2.3 h,A方案治愈率较B方案提高10~40%,即在总剂量相等时,适当缩短给药间隔时间,可提高疗效。

     

    Abstract: Qinghaosu (Artemisinine) is a new antimalarial drug extracted from the Chinese madicinal herb, Qing Hao (Artemisia annua Linn.). Animal experiments and clinical observations indicate that Oinghaosu is highly effective against erythrocytic parasite with low toxicity and marked effect on falciparum malaria resistant to Chloroquine. But, in the usual clinical dosage (0.3 g im qd for 3 days), its average recrudescence rate is more than 10%. In order to reduce the recrudescence rate, the biological halflife of the drug and therapeutic effect in mice infected with Plasmodiurn berghei ANKA strain were studied.Two different methods were used for the determination of biological half-life of the drug: one was to examine the pharmacodynam.ic attenuation rate at different times after intramuscular injection, the other was to complement the SD50 (half suppresive dose). The results of the two methods were similar, i.e. 10.5±2.3 h and 11 h, respectively.Two dose regimes of drug administration were compared:1. Regime A: based on t1/2, 1/6 of the total test dose of Qinghaosu was administered intramuscularly per 12 hours with the initial dose doubled. The course of the test was 3 days.2. Regime B: referring to the dosage regime used clinically, i.e. 1/3 of the total dose was injected intramuscularly per 24 hours for 3 days. The total dose of the drug in regime B was the same as that in regime A.After treatment the animals were observed for 3 months, the results demonstrate that dosage regime A was better than dosage regime B. The curative rate in regime A was 10~40% higher than that in regime B with the same dosage. The CD50 and CD95 of regime A were 29.4% and 32.8%o lower respectively than those of regime B.

     

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