Blood Levels, Urinary Excretion and Serum Protein-Binding of 2- (2′-Methyl-3′-Chloro) Anilino Nicotinic Acid (SCH 10304) in Man

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Blood levels were determined after oral administration of SCH 10304 in man. Five healthy male volunteers received a single dose of 300 mg, two divided doses of 150 mg each, or a single dose of 150 mg. Male and female patients with rheumatoid arthritis received two divided doses of 150 mg each. The blood level reached a peak one or two hours after administration in subjects who received a single dose of 300 mg. The level was considerably lowered, but still detectable, six hours after administration. Time of drug administration in relation to food intake (administration before, immediately after, and two hours after food intake) had no significant influence on blood level of SCH 10304 at the peak period and at four hours after administration. No difference in blood levels of SCH 10304 were noted between the patients and the volunteers receiving similar doses of the drug. A single dose of 300 mg and two divided doses of 150 mg each showed no significant difference in the blood level of SCH 10304. The recovery of the drug in the urine, over a period of 24 hours after administration, averaged 72.8% in four volunteers, two each from the 300 and 150 mg single dose groups. The binding rate of the drug with plasma protein was very high and showed up to 97%, 4 hours after administration.
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