Good S S, de Miranda P
Am J Med. 1982 Jul 20;73(1A):91-5. doi: 10.1016/0002-9343(82)90071-7.
Two guinea pigs and two rabbits were each inoculated subcutaneously with 14C-labeled acyclovir (25 mg/kg). Both species excreted the entire amount within 72 hours. The rabbits excreted all of the radioactivity in the urine while the guinea pigs excreted an average of 14.2 percent in the feces. The rabbits excreted an average of 71.0 percent of the dose as unchanged drug; 25.1 percent was excreted as 9-carboxymethoxymethylguanine (CMMG) and 3.5 percent as 8-hydroxy-9-(2-hydroxyethoxymethyl)guanine (8-hydroxyacyclovir). An average of 60.7 percent of the dose was recovered from the guinea pigs as acyclovir; 32.3 percent was excreted as CMMG and 3.1 percent as 8-hydroxyacyclovir. The two rabbits showed elimination-phase half-lives (t 1/2 beta) for plasma acyclovir of 0.8 and 2.2 hours. Mean t 1/2 beta for acyclovir in two rhesus, four patas, and four african green monkeys, each receiving acyclovir (10 mg/kg) as a bolus intravenous injection, were 1.2, 1.7, and 1.8 hours respectively. The average 48 hour urinary excretion of acyclovir, 8-hydroxyacyclovir, and CMMG in the rhesus monkey was estimated to be 21.3 percent, 15.3 percent, and 7.1 percent, respectively, of the total administered amount. The patas and african green species excreted the dose mostly as acyclovir and CMMG.
给两只豚鼠和两只兔子分别皮下注射14C标记的阿昔洛韦（25毫克/千克）。两种动物均在72小时内排出全部剂量。兔子将所有放射性物质经尿液排出，而豚鼠平均有14.2%经粪便排出。兔子平均以原形药物排出剂量的71.0%；25.1%以9-羧甲氧基甲基鸟嘌呤（CMMG）形式排出，3.5%以8-羟基-9-（2-羟基乙氧基甲基）鸟嘌呤（8-羟基阿昔洛韦）形式排出。豚鼠平均有60.7%的剂量以阿昔洛韦形式回收；32.3%以CMMG形式排出，3.1%以8-羟基阿昔洛韦形式排出。两只兔子血浆中阿昔洛韦的消除相半衰期（t 1/2β）分别为0.8小时和2.2小时。两只恒河猴、四只粗尾猴和四只非洲绿猴，每只均接受阿昔洛韦（10毫克/千克）静脉推注，阿昔洛韦的平均t 1/2β分别为1.2小时、1.7小时和1.8小时。恒河猴48小时内阿昔洛韦、8-羟基阿昔洛韦和CMMG的平均尿排泄量估计分别为总给药量的21.3%、15.3%和7.1%。粗尾猴和非洲绿猴这两个物种排出的剂量大多为阿昔洛韦和CMMG。
