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新抗疟药磷酸咯啶和伯喹合用对大白鼠血浆伯喹浓度的影响
THE EFFECT OF PYRACRINI PHOSPHAS ON PLASMA PRIMAQUINE-LEVEL FOLLOWING COMBINED ADMINISTRATION TO RATS
【摘要】 <正> 磷酸咯啶(研制号6701)是上海第十四制药厂研制的新抗疟药,化学名为3-氯-7-甲氧基-9-{3′,5′-双-[(N-吡咯烷基)甲基]-4′-羟苯胺基}吖啶的三磷酸盐。临床用于疟疾抑制性治疗,具有控制症状快,副作用较小等优点,但仍需与伯喹(伯氨喹啉)合用,以杀灭恶性疟原虫配子体和间日疟抗复发治疗。已知阿的平(Quinacrine)与扑疟喹啉(Pamaquine)合用
【Abstract】 Pyracrini phosphas(6701)is a new antimalarial drug developed in China. It possesses the same acridine nucleus as that in quinacrine (A). It had been shown that the toxicity of pamaquine was enhanced by concurrent quinacrine administration, and the maximal plasma pamaquine concentrations were many times higher following quinacrine therapy than the control values. Since both pamaquine and primaquine (PQ) belong to 8-aminoquinoline series, so it is of practical importance to clarify whether there is any effect of pyracrini phosphas on plasma primaquine level following their combined administration.Using a spectrofluorometric method to estimate the plasma primaquine level, the following results were obtained:1. The biological half life of primaquine following concurrent quinacrine administration (A+PQ group) was about twice longer than that following concurrent pyracrini phosphas administration (6701+PQ group), or that after primaquine medication alone.2. The mean plasma primaquine level of A+PQ group is about 10 times higher than that of 6701+PQ group or PQ group at 12 hours after medication.3. No significant difference was found between the plasma primaquine level of 6701+PQ group and that of PQ group.Therefore, it is considered that there is little effect of pyracrini phosphas on plasma primaquine level following combined administration of these drugs to rats.
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1980年10期
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