Clinical Phanmacology of a Newly Synthesized Anti-lipidemic Agent (CGA)

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p-Chlorophenoxy isobutyryl glycine amide (CGA) is a newly synthesized antilipidemic drug, which has been proved to lower serum concentrations of triglyceride and cholesterol in amimal experiments.<BR>The pharmacokinetics of CGA have been studied in six healthy volunteers. Determination of the drug and its metabolites in the blood and urine was carried out using high pressure liquid chromatography and gas chromatography-mass spectrometry.<BR>After oral ingestion of 500mg of CGA, CGA and its active metabolite p-chlorophenoxyisobutyric acid (CPIBA) were detected in blood samples.The peak concentration of CPIBA was observed after that of CGA.These results suggest that CGA is a so-called prodrug or latent form of CPIBA.A multiple dosing study (12-hour intervals for 3 days) reveals that ingestion of CGA at 1000 mg once daily might be sufficient to maintain steady-state plasma concentration of CPIBA.<BR>p-Chloroisobutyryl grycine (CG) was identified as a main metabolite in urine from the mass spectrum.
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