IE36204L - Penicilloic acid derivatives. - Google Patents

Abstract

1322149 Penicillin compositions F HOFFMANN-LA ROCHE & CO AG 10 March 1972 [11 March 1971] 11351/72 Heading A5B [Also in Division C2] Pharmaceutical compositions for penicillin treatment where a penicillin allergy exists or is suspected and for the prophylactic treatment of penicillin allergies contain a therapeutically active penicillin and a penicilloyl acid derivative of the formula: wherein X represents a hydrogen atom or a group of the formula R'-NH- in which R' represents a hydrogen atom or a C 1-7 acyl group, n represents a whole number from 1-4 and R represents 2-pentenyl, n-pentyl, nheptyl, allylthiomethyl, 5-amino-5-carboxypentyl, benzyl, carboxybenzyl, α-aminobenzyl, phenoxybenzyl, phenoxymethyl, α-phenoxyethyl, α-phenoxypropyl, 2, 6-dimethoxyphenyl, 2-ethoxy-1-naphthyl, 3-carboxy-2-quinoxalinyl, 5-methyl-3-phenyl - 4 - isoxazolyl, 3 - (2-chlorophenyl)-5-methyl-4-isoxazolyl, 3-(2, 6-dichlorophenyl)-5-methyl-4-isoxazolyl or 2-furoyloxyisobutyl or a pharmaceutically acceptable salt thereof. Preferably the therapeutically active penicillin is benzyl penicillin, α-phenoxyethylpenicillin, sodium 2, 6-dimethoxyphenylpenicillin monohydrate, sodium 3-(2-chlorophenyl)-5- methyl-4-isoxozolylpenicillin monohydrate or α-aminobenzylpenicillin or salts or hydrates thereof. Salts referred to include organic ammonium salts such as the procaine, bis benzylammonium or bisdicyclohexylammonium salts and mineral salts such as the sodium, potassium or calcium salts. R in the penicilloyl acid derivative is preferably the same as in the therapeutically active penicillin and a preferred composition comprises benzyl penicillin and N<SP>6</SP>-(benzyl-α-penicilloyl)aminocaproic acid. The compositions may be administered enterally or parenterally in the form of tablets, dragÚes, suppositories, capsules, salves, solutions, suspensions or emulsions. [GB1322149A]