Sulfamethoxazole と Trimethoprimの研究 ¹⁴C-Trimethoprimの生体内分布に関する全身オートラジオグラフィ的研究

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The distribution and antibacterial effect of trimethoprim orally administered to rats or mice were studied by means of whole body autoradiography and autobacteriography.
When administered alone in a dose of 20 mg/kg, ¹⁴C-trimethoprim was rapidly and easily absorbed from the digestive tract and distributed to almost all tissues or organs except the central nervous system. The radioactivity in the various tissues or organs reached at their maximum levels within 30 minutes, and then decreased gradually, and was almost diminished at 24 hours after the administration.
The highest radioactivity was found in the kidney, liver, salivary gland, adrenal medulla, pituitary gland, pineal body and the next higher radioactivity was observed in the spleen, pancreas, adrenal cortex, thyroid, bone marrow, lymph nodes and prostate.
¹⁴C-trimethoprim and/or its metabolites were excreted into the urine, bile and saliva.
When ¹⁴C-trimethoprim (20 mg/kg) was administered in the combination with sulfamethoxazole (100 mg/kg), the distribution pattern was not essentially different from that of ¹⁴C-trimethoprim alone.
When trimethoprim, in the dose from 3.14 to 200 mg/kg, or its combination with sulfamethoxazole, in the dose from 1.87 to 120 mg/kg, was administered to mice infected intraperitoneally with Staphylococcus aureus, the numbers of viable organisms in various tissues of mice were apparently less in the latter than in the former.