Pharmacokinetic characteristics of N7‐substituted theophylline derivatives and their interaction with quinolone in rats

Takaaki Hasegawa, Masayuki Nadai, Ruttikorn Apichartpichean, Isao Muraoka, Toshitaka Nabeshima, Kenzo Takagi

研究成果: Article査読

6 被引用数 (Scopus)

抄録

Disposition of diprophylline (DPP) and proxyphylline (PXP) and the effect of enoxacin on their disposition were investigated in rats. Concentrations of the two drugs in plasma and urine were measured by HPLC. The pharmacokinetic parameters of the two drugs were estimated by model‐independent methods. Although the chemical structures of the two drugs are very similar, remarkable differences in the disposition of the two drugs were observed. Total body clearance (CLT) of DPP was 1.77 L/h/kg, which was sevenfold greater than that of PXP (0.26 L/h/kg). Diprophylline was excreted in an almost completely unchanged form in the urine, but only 50% of PXP was excreted. However, no binding of either drug to proteins in rat plasma was observed. The DPP renal clearance (CLR) was 1.75 L/h/kg, ∼ 13‐fold the CLR for PXP (0.13 L/h/kg) and sevenfold the rat glomerular filtration rate. This study indicates that in rats, DPP is mainly excreted by active tubular secretion and that renal tubular reabsorption contributes to renal excretion of PXP with glomerular filtration. No significant changes in any pharmacokinetic parameters of the two drugs were observed when they were coadministered with enoxacin, compared with the drug administered alone, suggesting that enoxacin had no effect on the pharmacokinetics of either drug.

本文言語English
ページ(範囲)962-965
ページ数4
ジャーナルJournal of Pharmaceutical Sciences
80
10
DOI
出版ステータスPublished - 10-1991
外部発表はい

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

フィンガープリント 「Pharmacokinetic characteristics of N<sup>7</sup>‐substituted theophylline derivatives and their interaction with quinolone in rats」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

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