Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-03-25
1995-12-26
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544363, A61K 31495, A61K 3147, C07D40104
Patent
active
054788293
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR92/00841, filed Sep. 25, 1992.
FIELD OF THE INVENTION
The present invention relates to a novel pharmaceutical composition suitable for the parenteral administration of sparfloxacin.
BACKGROUND OF THE INVENTION
Sparfloxacin of formula: ##STR2## as well as its addition salts with acids or bases, useful as antimicrobial agents, have been described in Patent Application EP 221,463.
Patent Application EP 284935 also describes quinolones and their salts and, amongst these products, sparfloxacin.
Unfortunately, the salts of sparfloxacin are generally insoluble or unstable in solution. It has thus not been possible until now to prepare suitable compositions for parenteral administration.
European Patent EP 322,892 mentions these difficulties and describes lyophilised compositions containing a salt of sparfloxacin with an acid. However, these compositions do not allow stable solutions to be obtained for a prolonged period and for this reason only the preparation of a solution to be used at once is possible. In addition, such solutions risk being unsuitable for use in slow perfusions.
DESCRIPTION OF THE INVENTION
The present invention relates to stable injectable solutions. These compositions can be kept for a prolonged period and are in general stable to heat.
The solutions according to the invention are aqueous solutions containing: at least in a stoichiometric quantity with respect to sparfloxacin, pharmaceutically acceptable acid intended to ensure a pH of complete solubilization of the salt thus formed, of less than or equal to 5, acceptable adjuvants.
The solutions according to the invention contain at least 1% of sparfloxacin. However, they can contain concentrations which can increase to 40% of sparfloxacin. It is well known that solutions of concentration less than 1% are likewise practicable and clinically utilisable; these solutions likewise come within the scope of the present invention.
The polyhydroxymonocarboxylic acid is chosen in such a way that its pK.sub.a is greater than 3 at 25.degree. C. By way of example, it can be chosen from amongst lactobionic, glucoheptonic, gluconic or ascorbic acid.
The quantity of the polyhydroxymonocarboxylic acid is a function of the quantity of sparfloxacin. It is determined so as to have at least stoichiometric proportions and in such a way as preferably to obtain solutions in which the pH is not less than 3.5.
The acid capable of ensuring complete solubilization can be chosen from amongst the pharmaceutically acceptable acids which do not risk, by reason of their nature and/or their concentration, displacing, in a significant fashion, the salt of sparfloxacin with the polyhydroxymonocarboxylic acid. By way of example, organic acids can be chosen such as acetic acid, propionic acid, tartaric acid, succinic acid or hydroxy- or polyhydroxymonocarboxylic acids. Stronger acids can likewise be utilized, particularly such as sulphonic acids (methanesulphonic acid for example), carboxylic acids (maleic acid, oxalic acid, malonic acid for example), or mineral acids (for example hydrochloric acid, phosphoric acid, sulphuric acid) in the cases where their concentration can be fixed in such a way that they do not risk displacing, in a significant fashion, the salt of sparfloxacin with the polyhydroxymonocarboxylic acid. However, it is understood that for reasons of convenience, it is quite advantageous to adjust the solubility and the pH of the solutions by means of the polyhydroxymonocarboxylic acid employed.
The pH of the solutions is less than or equal to 5. In a general manner, the pH of the solutions may be compatible with direct administration. It is preferably between 3.5 and 5.
Preferably, the solutions according to the invention are isotonic. However, non-isotonic solutions intended for injection in a glucose perfusion bag likewise come within the scope of the present invention.
The solutions according to the invention can be rendered isotonic by addition of a tonicity regulator such as, for example, glucose, glycerol, sorbi
REFERENCES:
patent: 4795751 (1989-01-01), Matsumoto et al.
Henley III Raymond
Rhone-DPC Europe
Spivack Phyllis G.
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