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目的：观察正常人口服泛昔洛韦片剂的剂量耐受性、药动学和生物利用度，提出安全的临床治疗剂量。方法：４ 组（ 每组６ 人）健康人分别口服０－１２５ｇ 、０－２５ｇ 、０－５ｇ 、０－７５ｇ 泛昔洛韦片剂，进行剂量耐受性试验。用ＨＰＬＣ 法测定９ 人分别口服国产和进口的泛昔洛韦（ｆａ ｍｃｉｃｌｏｖｉｒ） 片各０－２５ｇ 后血和尿的喷昔洛韦（ｐｅｎｃｉｃｌｏｖｉｒ） 浓度。结果：口服０－１２５ｇ ～０－７５ ｇ 泛昔洛韦片剂呈现良好的耐受性。口服０－２５ｇ 泛昔洛韦国产片除了与进口片有生物等效性外，药－ 时曲线呈二房室开放模型，约１ｈ 前达峰，Ｃｍ ａｘ ２－２０ ｍ ｇ／ Ｌ，Ｔ１／２α（１－０１ ±１－５１）ｈ ，Ｔ１／２β（２－９３ ±０－８３）ｈ ，Ｖ／Ｆ（５５－１ ±２７－８） Ｌ，２４ｈ 尿喷昔洛韦累积率为（６６－３ ±１５－３） ％ 。结论：国产泛昔洛韦片口服后具有吸收较快、喷昔洛韦在体内分布迅速而广泛、大部分经肾排泄的特点。单剂量口服泛昔洛韦良好的耐受性和药动学特点的事实，推荐口服泛昔洛韦０－１２５ｇ ～０－７５ｇ 、１ 日３ 次的给药方案用于临床可能是安全的。
OBJECTIVE: To observe the dose tolerance, pharmacokinetics and bioavailability of famciclovir tablet in normal population and to propose a safe clinical dose. Methods: Four groups (6 in each group) of healthy individuals were orally given 0-125g, 0-25g, 0-5g and 0-75g of famciclovir tablets for dose tolerance test. The concentrations of penciclovir in blood and urine of 0-25 g each of domestic and imported fa mciclovir tablets were determined by HPLC. Results: Oral 0-125g ~ 0-75 g of famciclovir tablets showed good tolerance. In addition to oral administration of 0-25g famciclovir domestic tablets in addition to imported tablets with bioequivalence, the drug-time curve was two-bedroom open model, peaked about 1h, Cm ax 2-20 m g / L, T1 / 2α (1- 01 ± 1-51) h, T1 / 2β (2-93 ± 0-83) h, V / F (55-1 ± 27-8) L, and the cumulative urine penciclovir cumulative rate was (66-3 ± 15-3)%. Conclusion: Domestic famciclovir tablets have the characteristics of rapid absorption after oral administration, rapid and extensive distribution of penciclovir in the body and most of excretion by the kidneys. For single-dose oral famciclovir good tolerability and pharmacokinetic characteristics of the fact that recommended oral famciclovir 0-125g ~ 0-75g, 3 times a day for the clinical administration of the program may be safe.