Bruun J N, Ostby N, Bredesen J E, Kierulf P, Lunde P K
Antimicrob Agents Chemother. 1981 Jan;19(1):82-5. doi: 10.1128/AAC.19.1.82.
Various sulfonamides and trimethoprim were given orally twice a day to healthy volunteers. The drug concentrations in serum and tissue fluid from skin blisters were determined concomitantly. Maximal serum concentrations were obtained after 1 to 3 h. Absorption of sulfacarbamide and sulfadimidine was more rapid than for sulfadiazine, sulfamethoxazole, and trimethoprim. The penetration to blister fluid was delayed and maximal concentrations were usually reached after 4 to 8 h. The highest penetration to blister fluid was found for sulfacarbamide, sulfadiazine, and trimethoprim. During maintenance therapy sulfadiazine and trimethoprim gave blister fluid concentrations usually above 50% of the serum level. However, on the basis of dosage the highest sulfonamide concentration both in serum and blister fluid was obtained with sulfamethoxazole.
给健康志愿者每天口服两次各种磺胺类药物和甲氧苄啶。同时测定血清和皮肤水疱组织液中的药物浓度。服药后1至3小时达到血清最大浓度。磺胺脲和磺胺二甲嘧啶的吸收比磺胺嘧啶、磺胺甲恶唑和甲氧苄啶更快。药物渗透到水疱液中的过程延迟,通常在4至8小时后达到最大浓度。磺胺脲、磺胺嘧啶和甲氧苄啶在水疱液中的渗透最高。在维持治疗期间,磺胺嘧啶和甲氧苄啶在水疱液中的浓度通常高于血清水平的50%。然而,基于给药剂量,血清和水疱液中磺胺类药物浓度最高的是磺胺甲恶唑。