Composition, useful for treating infections in animals e.g. otitis and ophthalmic infections, comprises a pyrido(3,2,1-ij)benzoxadiazine derivative and a solubilizer in a carrier

摘要

#CMT# #/CMT# Antiinfectious composition comprises a pyrido[3,2,1-ij]benzoxadiazine derivative (I) or its salt and a solubilizer in a carrier. #CMT# : #/CMT# 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. #CMT#[Image]#/CMT# #CMT#ACTIVITY : #/CMT# 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). #CMT#MECHANISM OF ACTION : #/CMT# None given. #CMT#USE : #/CMT# The composition is useful for treating infections in animals, e.g. sheep, cattle, pigs, goats, horses, poultry, dogs or cats, including infections of the respiratory, reproductive, urinary, digestive, locomotor or cardiovascular system, skin infections, otitis and ophthalmic infections. #CMT#ADVANTAGE : #/CMT# The composition is well tolerated on injection and has good cold stability. #CMT#PHARMACEUTICALS : #/CMT# Preferred Composition: (I) Is present in an amount of 15-20 w/v%. The solubilizer is gluconic acid or gluconolactone and is present in an amount of 7-20 w/v%. The molar ratio of solubilizer to (I) is 1.1-2.4:1. The composition has a pH of 2.8-5. The composition also contains a stabilizer, especially benzyl alcohol, in an amount of 1-3 w/v%. The molar ratio of stabilizer to (I) is 0.2-1:1. #CMT#ADMINISTRATION : #/CMT# The composition is preferably administered as an injectable solution (no dosage given). #CMT#SPECIFIC COMPOUNDS : #/CMT# Use of one compound (I) is specifically claimed i.e. marbofloxacin (9-fluoro-2,3-dihydro-3-methyl-10(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[3,2,1-ij]benzoxadiazine-6-carboxylic acid) (Ia). #CMT#EXAMPLE : #/CMT# No relevant example given.