[논문]Pharmacokinetics of Tolbutamide After Oral Administration to Rabbits with Folate-Induced Renal Failure

Choi, Jun-Shik; Shin, Sang-Chul

doi:10.1007/bf02980209

[국내논문] Pharmacokinetics of Tolbutamide After Oral Administration to Rabbits with Folate-Induced Renal Failure 원문보기

Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, v.26 no.11, 2003년, pp.979 - 983

Choi, Jun-Shik (College of Pharmacy, Chosun University) , Shin, Sang-Chul (College of Pharmacy, Chonnan National University)

Abstract ▼ AI-Helper

The pharmacokinetic of tolbutamide was studied after the oral administration to normal rabbits or rabbits with mild to medium folate-induced renal failure. The plasma concentrations of tolbutamide were significantly elevated (p<0.05) during 9 to 24 h in rabbits with mild or medium folate-induced renal failure. Consequently, the area under the plasma concentration-time curves (AUC) was significantly higher in mild (p<0.05) and medium (p<0.01) folate-induced renal failure rabbits (i.e., 2906 $\mu$g/mL$.$h for mild renal failure and 4074 $\mu$g/mL$.$h for moderate renal failure) than that in normal rabbits (i.e., 2295 $\mu$g/mL$.$h). The cumulative urinary excretion of tolbutamide was significantly depressed (p<0.05) in medium folate-induced renal failure rabbits (i.e., 3.3 mg) compared with that in normal rabbits (i.e., 5.9 mg). The elimination rate constant (Kel) of tolbutamide was significantly decreased in medium renal failure rabbits (i.e., 0.027 $h^{-1}$) than that in normal rabbits (i.e., 0.044 $h^{-1}$ ); As a result, the terminal half-life of tolbutamide in medium folate-induced renal failure rabbits (i.e., 25.5 h) was significantly longer (p<0.01) than that in normal rabbits (i.e., 15.7 h). The change in pharmacokinetic parameters is consistent with the hypothesis that the alteration is mediated by the depressed metabolic elimination of the drug by the induction of renal failure. Therefore, these observations indicated that the dosage adjustment may be necessary for tolbutamide in patients with renal insufficiency.

주제어

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문제 정의

However, this aspect of tolbutamide pharmacokinetics has not been studied. The purpose of this study was to characterize and compare the pharmacokinetics of tolbutamide in normal rabbits and rabbits with renal failure.

제안 방법

In this study, the plasma concentration was elevated after the induction of renal faihjre and the elevation was accompanied by the alteration in pharmacokinetic parameters (e.g., AUC and Kel). In general, an elevation of AUG may be manifested by increased input (i.

대상 데이터

White male New Zealand rabbits, weighing 2.0-2.5 kg in body weight, were fasted at least 24 h prior to the experiment; water was given freely to animals. When it was necessary, mild or medium renal faihjre rabbits were induced by the intravenous administration of folate (75 ㎎/㎏ for mile renal failure; 150 ㎎/㎏ for moderated renal failure; vehi이e 0.

데이터처리

When it was necessary to compare mean values, student's f-test was used. In this study, p<0.

이론/모형

open model. Nonlinear least square regression was performed with the MULTI program (Yamaoka et 이., 1981) and the parameter values, i.e., the intercepts and the slopes, obtained using simplex algorithm. The area under the plasma concentration-time curves (AUC) from time zero to the last collection was calculated by trapezoidal「니e and AUC from the last c이lection time to infinity calculated by the standard area extrapolation technique.
, the intercepts and the slopes, obtained using simplex algorithm. The area under the plasma concentration-time curves (AUC) from time zero to the last collection was calculated by trapezoidal「니e and AUC from the last c이lection time to infinity calculated by the standard area extrapolation technique. The maximum plasma concentration (Cmax) and time to reach the maximum plasma concentration (Tmax) were obtained directly from plasma concentration-time curves.

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