The metabolism of cilostamide in the rat in vitro and in vivo

T. Shimizu Laboratories of Drug Metabolism and Analytical Research, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd, 463-10 Kagasuno, Kawauchi-cho, Tokushima, 771-01, Japan

H. Mori Laboratories of Drug Metabolism and Analytical Research, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd, 463-10 Kagasuno, Kawauchi-cho, Tokushima, 771-01, Japan

Y. Yasuda Laboratories of Drug Metabolism and Analytical Research, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd, 463-10 Kagasuno, Kawauchi-cho, Tokushima, 771-01, Japan

S. Morita Laboratories of Drug Metabolism and Analytical Research, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd, 463-10 Kagasuno, Kawauchi-cho, Tokushima, 771-01, Japan

K. Nakagawa Laboratories of Drug Metabolism and Analytical Research, Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd, 463-10 Kagasuno, Kawauchi-cho, Tokushima, 771-01, Japan

Abstract

1. The metabolism of N-cyclohexyl-N-methyl-4-(1,2-dihydro-2-oxo-6-quinolyl-oxy)butyramide (cilostamide) was studied in vitro and in vivo after oral administration to rats.

2. Recovery of orally administered ¹⁴C-cilostamide (3 mg/kg) and its metabolites in 48 h was 50.5% dose in urine and 47.6% dose in faeces. The drug was extensively metabolized.

3. The metabolites of cilostamide in rats were identified by t.l.c., g.l.c.-mass spectrometry and n.m.r. The major route of metabolism is hydroxylation at the cyclohexyl ring.

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The metabolism of cilostamide in the rat in vitro and in vivo

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