替硝唑在唾液和血浆中浓度的相关性探讨

Relation of tinidazole concentration in plasma and saliva

目的：探讨替硝唑在唾液浓度和血浆浓度的相关性。方法：８ 名健康男性志愿者交叉口服２ ｇ 的替硝唑胶囊和片剂，用 Ｈ Ｐ Ｌ Ｃ 法测定其在血浆中浓度经时过程及相应时间点的唾液中浓度。结果：替硝唑胶囊的血浆及唾液中的ｔ１／２ｋａ 分别为（０４７ ±０２４） 、（０６３ ±０３８）ｈ ，ｔ１／２ｋｅ 分别为（１３７１ ±１５２） 、（１３７８ ±３３７）ｈ ， ρｍａｘ 分别为（５２０７ ±９１１） 、（４８１０ ±８０１） μｇ／ｍ Ｌ， Ａ Ｕ Ｃ 分别为（１ ０９２９８ ±１１１８３） 、（１ ０１１２８ ±１１５２０）μｇ·ｈ／ｍ Ｌ；替硝唑片剂的血浆及唾液中的ｔ１／２ｋａ 分别为（０８６±０６７） 、（０７８ ±０５２）ｈ ，ｔ１／２ｋｅ 分别为（１４１９ ±１９５） 、（１３００ ±２０７）ｈ ，ρｍａｘ 分别为（５１０７ ±１０３２） 、（４９０９ ±９２７）μｇ／ｍ Ｌ， Ａ Ｕ Ｃ 分别为（１ １２３００ ±１２８２５） 、（１ ０４４１５ ±１７９５４）μｇ·ｈ／ｍ Ｌ。结论：替硝唑在唾液和血浆中的药代动力学参数相似，均无显著性差异。

Aim:To study the relation of tinidazole concentration in plasma and saliva. Methods: The relation of tinidazole in plasma and saliva was investigated in a crossover trial in eight healthy volunteers after oral administration of 2 g tinidazole capsule and tinidazole tablets. The concentration of tinidazole in plasma and saliva were measured by HPLC method. Results: Experimental results indicated: for tinidazole capsule, the plasma and saliva t 1/2ka were (0.47±0.24)\,(0.63±0.38)h; t 1/2ke were (13.71±1 52)\,(13.78±3.37)h;the peak concentration were (52.07±9.11)\,(48.10±8.01)μg/mL;AUC were (1 092.98±111.83)\,(1 011.28±115.20) (μg·h/mL) respectively; for tinidazole tablets, the plasma and saliva t 1/2ka were (0.86±0.67)\,(0.78±0.52)h; t 1/2ke were (14.19±1.95\,13.00± 2.07 )h; the peak concentration were (51.07±10.32)\,(49.09±9.27)μg/mL;AUC were (1 123.00±128.25)\,( 1 044.15 ±179.54(μg·h/mL) respectively. Conclusion: There were no significant difference between pharmacokinetic parameters of tinidazole in plasma and saliva. The saliva concentration were closely related with plasma concentration.