阿昔洛韋的水溶性不佳,口服形式的生物利用度不高(15-30%),因此如果需要高濃度的效果,則需透過靜脈注射的形式。口服給藥後1-2小時後出現最大血藥濃度。根據美國生物製藥分類系統(英語:Biopharmaceutical Classification System)(BCS),阿昔洛韋屬於BCS III 類藥物,即具可溶性但腸道滲透性低。[51]阿昔洛韋分佈率高,報導的蛋白質結合率為9%至33%。[52]阿昔洛韋的生物半衰期(t½)取決於年齡:新生兒為4小時、1-12歲兒童為2-3小時,而成人為3小時。[2]
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