Literature DB >> 14725362

Radical mechanisms in the radiosterilization of metoprolol tartrate solutions.

Catherine Slegers1, Gérard Baldacchino, Dominique Le Parc, Bernard Hickel, Bernard Tilquin.   

Abstract

PURPOSE: Study of the radical mechanisms in the radiosterilization of metoprolol tartrate aqueous solutions in order to determine the parameters governing its radiostability.
METHODS: Pulse radiolysis with pseudo-first-order kinetics to measure Ihe reaction rate constants of hydrated electrons and hydroxyl radicals with metoprolol tartrate. Chemsimul was used to solve the decay kinetics of transients and to simulate the radiolysis of metoprolol tartrate solutions.
RESULTS: Hydrated electrons react with metoprolol and the tartrate ion with rate constants of 6.8 x 10(7) M(-1) s(-1) and 1.7 x 10(7) M(-1) s(-1), respectively. Hydroxyl radicals react with metoprolol and the tartrate ion with rate constants of 5.2 x 10(9) M(-1) s(-1) and 5.5 x 10(8) M(-1) s(-1), respectively. The hydroxyl-metoprolol transients are found to scavenge the superoxide anion (5.5 x 10(10) M(-1) s(-1)), react with oxygen (1.0 x 10(8) M(-1) s(-1)), and follow a biradical decay (2.0 x 10(8) M(-1) s(-1). A simplified radical mechanism is used to simulate the loss of potency of metoprolol tartrate aqueous solutions during radiosterilization.
CONCLUSIONS: To decrease the loss of potency of metoprolol tartrate. the sterilization dose must be lowered and very high dose rates used.

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Year:  2003        PMID: 14725362     DOI: 10.1023/b:pham.0000008045.31305.b6

Source DB:  PubMed          Journal:  Pharm Res        ISSN: 0724-8741            Impact factor:   4.200


  7 in total

1.  Radiosterilization of cefotaxime: investigation of potential degradation compounds by liquid chromatography-electrospray mass spectrometry.

Authors:  N Barbarina; B Tilquin; E de Hoffmann
Journal:  J Chromatogr A       Date:  2001-09-21       Impact factor: 4.759

2.  Determination of radical yields in solid-state drugs as one technique to identify drugs that will withstand radiosterilization: radioresistance of beta blockers.

Authors:  Alix Engalytcheff; Véronique Deridder; René Debuyst; Bernard Tilquin
Journal:  Radiat Res       Date:  2003-07       Impact factor: 2.841

3.  [Radiation sterilization of drugs].

Authors:  B Tilquin
Journal:  J Pharm Belg       Date:  1991 Nov-Dec

4.  Attack of cefotaxime by different radicals: comparison of the effects.

Authors:  A S Crucq; B L Tilquin
Journal:  Free Radic Biol Med       Date:  1996       Impact factor: 7.376

Review 5.  Gamma processing technology: an alternative technology for terminal sterilization of parenterals.

Authors:  B D Reid
Journal:  PDA J Pharm Sci Technol       Date:  1995 Mar-Apr

6.  Spin trapping of polyunsaturated fatty acid-derived peroxyl radicals: reassignment to alkoxyl radical adducts.

Authors:  S I Dikalov; R P Mason
Journal:  Free Radic Biol Med       Date:  2001-01-15       Impact factor: 7.376

7.  Radical mechanisms of cephalosporins: a pulse radiolysis study.

Authors:  A S Crucq; B L Tilquin; B Hickel
Journal:  Free Radic Biol Med       Date:  1995-05       Impact factor: 7.376

  7 in total

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