PHASE I STUDY OF CEFACLOR
スポンサーリンク
概要
- 論文の詳細を見る
Cefaclor (CCL), a new cephalosporin antibiotic, was administered orally to twenty one healthy adult male volunteers to study the degree of safety and pharmacological properties. In single dose studies, 14 volunteers were randomly assigned to the doses of 250 mg and 500 mg of CCL or 250 mg of cephalexin (CEX) with or without food, then they received different dose every weekend for 4 weeks. In multiple dose studies, 7 volunteers received 500 mg of CCL in capsules every 6 hours for a week.<BR>Tolerance of administered CCL was, in general, good and no side effect or adverse reaction was found except 3 cases with transient mild gastrointestinal disturbance in multiple dose studies.<BR>CCL plasma concentrations usually peaked at 45 minutes after the dosing without food and steadily declined with no CCL detectable in plasma at 6 hours. The mean peak plasma levels of CCL were 7.42μg/ml for a 250 mg and 13.04μg/ml for a 500 mg and the plasma halflife calculated was about 30 minutes. During the 0- to 8- hour interval, about 70% of the total dose was excreted in urine.<BR>From the comparative pharmacokinetic studies of CCL and CEX, the peak plasma concentration and the plasma halflife of CCL were a bit lower and shorter than those of CEX without food.<BR>In the case of dosing 30 minutes after breakfast, CCL plasma concentrations peaked at 2 hours after the administration and the mean peak plasma levels were 3.22μg/ml for a 250 mg and 5.33μg/ml for a 500mg. Plasma levels of CCL were clearly influenced by dosing with food, however, equivalent value of AUC (area under the curve) suggests the quite similar bioavailability of CCL by dosing without food. Urinary excretion of CCL was also delayed at first by dosing with food, but about 70% of the total dose was excreted in urine during 8 hours.<BR>In the case of multiple dose studies, the similar patterns of plasma concentrations and urinary excretion derived from the 500 mg single dose study were seen everytime examined and no plasma accumulation of CCL was demonstrated.
- 公益社団法人 日本化学療法学会の論文
公益社団法人 日本化学療法学会 | 論文
- DISPOSITION OF 7432-8 IN RATS (I)
- CLINICAL STUDIES ON T-1220 IN SURGICAL CASES
- CLINICAL STUDIES OF PIVALOYLOXYMETHYL D-α-AMINOBENZYL-PENICILLINATE HYDROCHLORIDE IN SURGICAL INFECTIONS
- STUDIES ON AC-1370
- Primary treatment with a combination of cyclophosphamide, vincristine, and dacarbazine for recurrent malignant pheochromocytoma: A case report.