Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-07-07
1999-12-07
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31495
Patent
active
05998418&
DESCRIPTION:
BRIEF SUMMARY
Solutions of quinolonecarboxylic acids for parenteral administration are already known from EP-OS (European Published Specification) 67 666. They are based on salts of the corresponding quinolonecarboxylic acids with various hydroxycarboxylic acids.
Injection or infusion solutions of quinolonecarboxylic acids, inter alia of ciprofloxacin, based on the lactic acid salts with an excess of acid, are known from EP-OS (European Published Specification) 138 018.
Aqueous infusion solutions of ca 0.01 to 0.5% of ciprofloxacin, to which acids are added for stabilization, are known from EP-OS (European Published Specification) 214 784. Lactic acid, in particular, is mentioned as the preferred acid in said document.
Injection solutions based on fine suspensions of quinolonecarboxylic acids are known from DE-OS (German Published Specification) 39 02 079.
The present invention relates to novel injection and infusion solutions of the following composition: solution, in the form of its salts with polyhydroxycarboxylic acids or amino acids or mixtures thereof; molar excess, based on enrofloxacin; weight of the solution;
Compared with the injection solutions of enrofloxacin known hitherto, the solutions according to the invention have the advantage of a potent effect which sets in rapidly. This is shown by the fact that high blood levels of the active substance are reached only a short time after administration. However, the active substance is also eliminated rapidly, which is a great advantage, especially in the treatment of animals used for food production (short waiting times).
The injection and infusion solutions according to the invention contain the active substance enrofloxacin in concentrations preferably of 1 to 10%, particularly preferably of 2.5 to 10% (percent by weight based on the total weight of the solution).
Polyhydroxycarboxylic acids which may be mentioned are gluconic acid, galacturonic acid, glucuronic acid and lactobionic acid. The acids can be in the open-chain form or in the form of their lactones. If the acids are used as lactones, the lactone ring is at least partially hydrolyzed before salt formation and complex formation with enrofloxacin take place. Amino acids which may be mentioned are glutamic acid and aspartic acid. The polyhydroxycarboxylic acids or amino acids are present in 0.1 to 5 molar excess, based on the amount of enrofloxacin in the solution. The excess of acid is preferably 0.2 to 2 molar, particularly preferably 0.5 to 1 molar.
Part of the acid present in excess can also be displaced by other acids, e.g. hydrochloric acid, methanesulphonic acid, ethanesulphonic acid, propionic acid, succinic acid, glutaric acid, citric acid, ascorbic acid, phosphoric acid or lactic acid.
In addition to water for injections, the aqueous injection solutions can also contain ethanol, glycerol, propylene glycol, polyethylene glycol and triethylene glycol, for example, as liquid vehicles. The pH can be adjusted to the range 3 to 6.5, as far as possible, by using a variety of substances such as phosphoric acid, citric acid, Tris, ascorbic acid, acetic acid, succinic acid, tartaric acid, gluconic acid and lactic acid, and salts thereof. The pH of the aqueous formulations according to the invention is 3 to 5.5, preferably 3.5 to 5. The osmolality of the aqueous suspensions is 200 to 900 mOsmol/kg, preferably 260 to 390 mOsmol/kg, and can be adapted to isotonic conditions by the addition of NaCl, glucose, fructose, glycerol, sorbitol, mannitol, sucrose or xylitol, or mixtures of these substances.
It is further possible to use formulation aids such as thickeners (e.g. inter alia methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone and gelatin), absorbents, light stabilizers, crystallization retarders, complexing agents (e.g. inter alia NaEDTA, phosphates, nitrates, acetates and citrates), antioxidants (inter alia ascorbic acid, sulphite compounds, L-cysteine, thiodipropionic acid, thiolactic acid, monothioglycerol and propyl gallate) and p
REFERENCES:
patent: 4670444 (1987-06-01), Grohe et al.
Bonse Gerhard
Hamm Martin
Muller Hanns-Peter
Naik, deceased Arundev Haribhai
Scheer Martin
Akorli Godfried R.
Bayer Aktiengesellschaft
Gil Joseph C.
Henley III Raymond
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