Studies on the Formulation and Admixture of Parenteral Preparations. II. Degradation of Penicillins and Cephalospolin C's by Sodium Bisulfite

TERAO MOTOME, MARUI ETSUKO, YONEZAWA SEIICHI, KAWASHIMA NORIKO

doi:10.1248/yakushi1947.102.10_978

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Other Title

注射剤の処方化と混合に関する研究(第2報)亜硫酸水素ナトリウムによるペニシリン類およびセファロスポリンC類の分解
注射剤の処方化と混合に関する研究-2-亜硫酸水素ナトリウムによるペニシリン類およびセファロスポリンC類の分解
チュウシャザイノショホウカトコンゴウニカンスルケンキュウ 2 アリュ

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The degradation rates of penicillins and cephalospolin C's in aqueous solution were found to be accelerated by the coexistence of sodium bisulfite (SBS). The action of SBS was recognized to be catalytic. The destructive actions of SBS on penicillin G, carbenicillin, methicillin and sulbenicillin were shown by comparatively small catalytic rate constants. The actions of SBS on ampicillin and cloxacillin were shown by one figure larger catalytic rate constants, i.e., catalytic rate constants for penicillin G and ampicillin were 4.47 M^-1h^-1 and 30.53 M^-1h^-1, respectively, at 60°C, pH 6.5 and μ=0.1. The degradations of cephaloridine and cephalothin were also remarkably accelerated by SBS. As the results of stability studies on ampicillin in solution, the action of SBS was shown to be largest at pH value of approximately 6.5 and pH-rate profile was known to be inverse to that of the straight solution of ampicillin, and the effects of temperature and the concentration of SBS on the actions were determined. By utilizing these data, a new practical approach by use of a nomograph was proposed to predict the stability of ampicillin in the admixture of the antibiotics with parenterals containing SBS as an additive.

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YAKUGAKU ZASSHI

YAKUGAKU ZASSHI 102 (10), 978-983, 1982

The Pharmaceutical Society of Japan

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