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青蒿素是从我国中草药黄花蒿(Artemisia Annua)中提取出的一种新型倍半萜内酯类的抗疟新药。青蒿琥酯(Aftesunate)是青蒿素的有效衍生物,经药理研究和临床验证均证明该药对一般恶性疟、脑型疟和间日疟都有较好的疗效。因其结构特殊,且具有抗疟效价高,原虫转阴快,毒性小等特点,而受到国内外重视。为了进一步了解该药在体内的代谢规律及开发这个新型的抗疟药物,为临床合理用药提供科学依据。本文采用放射免疫分析法,研究了狗口服青蒿琥酯片剂后的血药时程。 材料和方法 一、动物:家狗,体重9.5～13.0kg,雄性,由本校动物房提供。 二、实验试剂:青蒿琥酯片剂(20mg/片),由广西桂林第二制药厂生产。3~H-双氢青蒿素,比放射性为55.5×10~10Bq/mM,由美国NEN公司提供。抗血清由医学科学院药物研究所提供。
Artemisinin is a new anti-malarial drug which is a new sesquiterpenoid extracted from Chinese herbal medicine Artemisia Annua. Artesunate (Aftesunate) is an effective derivative of artemisinin, pharmacological studies and clinical trials have proved that the drug on the general falciparum, cerebral malaria and Plasmodium vivax have a good effect. Because of its special structure, and has high anti-malarial potency, protozoa Yin Yin fast, small toxicity and other characteristics, which have been valued at home and abroad. In order to further understand the drug’s metabolism in the body and the development of this new type of anti-malarial drugs, provide a scientific basis for clinical rational use of drugs. In this paper, radioimmunoassay was used to study the time course of blood drug administration after oral administration of artesunate tablets in dogs. Materials and methods First, animals: domestic dogs, weighing 9.5 ~ 13.0kg, male, provided by the animal husbandry room. Second, experimental reagents: Artesunate tablets (20mg / tablet), the second pharmaceutical factory in Guilin, Guangxi production. 3 ~ H-dihydroartemisinin, radioactivity 55.5 × 10 ~ 10Bq / mM, provided by the United States NEN company. Antisera are provided by Institute of Materia Medica, Academy of Medical Sciences.