Physicochemical properties of amphoteric β‐lactam antibiotics I: Stability, solubility, and dissolution behavior of amino penicillins as a function of pH

Akira Tsuji, Emi Nakashima, Shoichiro Hamano, Tsukinaka Yamana

研究成果: Article査読

126 被引用数 (Scopus)

抄録

The degradation rate, solubility, and dissolution rate of amino penicillins, amoxicillin, ampicillin, epicillin, and cyclacillin, were determined quantitatively as a function of pH. In the pH range studied, 0.30‐10.50, the degradation of amoxicillin and epicillin followed pseudo‐first‐order kinetics to give the same type of pH‐rate profiles as those of ampicillin and cyclacillin. Cyclacillin anhydrate was the most soluble, followed in order by ampicillin anhydrate, ampicillin trihydrate, amoxicillin trihydrate, and epicillin anhydrate. These pH‐solubility profiles showed U‐shaped curves. The dissolution rate constants from the rotating disk were analyzed by the simultaneous chemical reaction and diffusion models. Their relative bioavailability after a single oral administration was assessed from their physicochemical properties determined in vitro.

本文言語English
ページ(範囲)1059-1066
ページ数8
ジャーナルJournal of Pharmaceutical Sciences
67
8
DOI
出版ステータスPublished - 1978 8

ASJC Scopus subject areas

  • Pharmaceutical Science

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