Anti-infective solution comprising a compound of pyrido(3,2,1-ij)-benzoxadiazine type

A compound and anti-infection technology, applied in the direction of anti-infective drugs, medical preparations containing active ingredients, medical preparations with non-active ingredients, etc., can solve problems such as exerting sufficient effects, inapplicable and incapable of all molecular types, etc.

Active Publication Date: 2013-01-16
VETOQUINOL SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, this type of formulation, previously designed for use with tetracyclines, may prove to be unsuitable or insufficiently effective for all molecule types, especially when certain quinolones are involved

Method used

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  • Anti-infective solution comprising a compound of pyrido(3,2,1-ij)-benzoxadiazine type
  • Anti-infective solution comprising a compound of pyrido(3,2,1-ij)-benzoxadiazine type
  • Anti-infective solution comprising a compound of pyrido(3,2,1-ij)-benzoxadiazine type

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] The solutions described in Table 1 below were prepared:

[0077]

1st copy comparative example Marbofloxacin (unit g) 15.00 10.00 Gluconolactone (unit g) 8.11 8.00 demineralized water qsp 100ml 100ml

[0078] Pigs with a weight of 70-80kg received intramuscular injection, and the injection solution was a single comparative solution in the right column or the first solution in the left column, and the dose was 8ml / kg. One week after dosing, local tolerance (damage) was checked.

[0079] Injection of the first solution presents a lesion volume of approximately 9 cm 3 , while the injection solution of the comparative example exhibits up to 32cm 3 damage volume.

[0080] The results indicated that the concentrated solution of marbofloxacin exhibited better local tolerance compared to the control solution.

Embodiment 2

[0082] The following solutions were prepared:

[0083]

1st copy 2nd copy 3rd copy 4th copy Marbofloxacin 20.00g 20.00g 20.00g 20.00g Gluconolactone 19.00g 19.00g 17.00g 17.00g Benzyl alcohol - 2.00g - 2.00g demineralized water qsp100ml qsp100ml qsp100ml qsp100ml stability at low temperature 24 hours >7 days* 24 hours >7 days*

[0084] * After 7 days, no precipitation was found.

[0085] "Stability at low temperature" refers to the time for each solution to stand at +4 to +8°C until a precipitate forms.

[0086] The above data clearly show the improved stability of the solutions of the invention.

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Abstract

Antiinfectious composition comprises a pyrido[3,2,1-ij]benzoxadiazine derivative (I) or its salt and a solubilizer in a carrier. Antiinfectious composition comprises a pyrido[3,2,1-ij]benzoxadiazine derivative of formula (I), or its salt, and a solubilizer in a carrier. X : H, halo or OH; R 1>1-piperazinyl (optionally 4-substituted with Me), acetyl of 4-aminobenzyl; morpholino; 1-pyrrolidinyl (optionally 3-substituted with Cl, NH 2, aminomethyl, methylaminomethyl, ethylaminomethyl or OMe); 1-imidazolyl (optionally 4-substituted with Me); or 1-piperidinyl (optionally 4-substituted with OH or OMe); R 2>1-10C alkyl. [Image] - ACTIVITY : Antibacterial; Virucide; Respiratory-Gen.; Endocrine-Gen.; Uropathic; Gastrointestinal-Gen.; Cardiovascular-Gen.; Dermatological; Muscular-Gen.; Auditory; Ophthalmological. An aqueous solution of marbofloxacin (15 g / 100 ml) and gluconolactone (8.11 g / 100 ml) was administered to pigs by intramulsular injection at a dose of 8 mg / kg. The lesion volume after 1 week was 9 cm 3>, compared with 32 cm 3> using an aqueous solution of marbofloxacin (10 g / 100 ml) and gluconolactone (8 g / 100 ml). - MECHANISM OF ACTION : None given.

Description

technical field [0001] The technical field of the invention relates to an anti-infective solution for the treatment of animals. [0002] The invention more particularly relates to an anti-infective solution, in particular a concentrated solution, containing at least one pyrido(3,2,1-ij)benzoxadiazine compound. Background technique [0003] It is very common to administer anti-infective products for therapeutic, prophylactic or quasi-prophylactic purposes to livestock such as cattle, pigs, goats, sheep, poultry and / or horses, as well as pets, especially by injection. [0004] The amount of product to be administered parenterally and the number of injection sites are important considerations when selecting a product formulation. The purpose of making concentrated formulations is to reduce the amount and / or frequency of administration, especially in livestock, to reduce the muscle areas that cannot be processed at slaughter. Another factor to consider when preparing concentra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/26A61K47/12A61K47/02A61P31/00
CPCA61K31/5395A61K9/0019A61P31/00
Inventor M·莫罗
Owner VETOQUINOL SA
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