氨苯砜和单乙酰氨苯砜在犬体内的处置（38516）

The disposition of dapsone and monoacetyldapsone in the dog (38516).

作者信息

Peters J H, Gordon R, Biggs J T, Levy L

出版信息

Proc Soc Exp Biol Med. 1975 Jan;148(1):251-5. doi: 10.3181/00379727-148-38516.

Abstract

Four female dogs receiving 1.0 mg dapsone (DDS)/kg iv exhibited logarithmic decline of plasma levels of DDS with a mean half-time of disappearance (T-1/2 of 11.7 hr. No evidence of acetylation of DDS to monoacetyl DDS (MADDS) was found. An equimolar dose of MADDS was deacetylated slowly to DDS by the same dogs. The mean T 1/2 of MADDS was 6.5 hr, significantly less than that of DDS. In 2-hr plasma samples after these doses of drugs, protein-binding of DDS and MADDS averaged 71 and 84%, respectively. Tests of protein-binding of the two drugs in vitro confirmed the observations in vivo.

摘要

四只接受1.0毫克/千克氨苯砜（DDS）静脉注射的雌性犬，其血浆中DDS水平呈对数下降，平均消失半衰期（T-1/2）为11.7小时。未发现DDS乙酰化为单乙酰氨苯砜（MADDS）的证据。相同的犬将等摩尔剂量的MADDS缓慢脱乙酰化为DDS。MADDS的平均T 1/2为6.5小时，显著短于DDS的T 1/2。在这些药物剂量后的2小时血浆样本中，DDS和MADDS的蛋白结合率分别平均为71%和84%。两种药物的体外蛋白结合试验证实了体内观察结果。