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阿糖腺苷(Ara-A)是一种安全有效的抗DNA病毒药物,主要用于治疗单纯疱疹性角膜炎等。近年来国内外医药界越来越重视其对慢性乙型病毒性肝炎的治疗作用,但Ara-A在水中溶解度小(0.45mg/ml)临床用作静脉滴注时间长,使用不便。国外文献报道在Ara-A众多的衍生物中,Ara-Amp是一种用于肌肉和静脉注射的有前途的新抗病毒药。Ara-Amp是Ara-A的前体药物,溶解度大、进入血液后很快脱磷生成Ara-A,为了研究Ara-Amp在体内分布排泄情况,本文用放射性氚标记单磷酸阿糖腺苷(8-~3H-Ara-Amp)作示踪剂进行实验。
Ara-A is a safe and effective anti-DNA virus drug, which is mainly used for the treatment of herpes simplex keratitis. In recent years, more attention has been paid to the therapeutic effect of Ara-A on chronic hepatitis B in domestic and overseas pharmaceutical circles. However, the solubility of Ara-A in water is low (0.45mg / ml) and it is inconvenient to use intravenously for a long time. Absorbed in many foreign Ara-A derivatives, Ara-Amp is a promising new antiviral for muscle and intravenous injection. Ara-Amp is a prodrug of Ara-A, and its solubility is high. After it enters the blood, Ara-A is rapidly dephosphorized. In order to study the distribution and excretion of Ara-Amp in vivo, Ara-Amp was labeled with radioactive tritium 8- ~ 3H-Ara-Amp) as tracer.