GB655519A - Improvements in or relating to penicillin compositions - Google Patents

Abstract

Solid readily dispersable preparations containing procaine penicillin are manufactured by intimately mixing (e.g. by trituration) procaine penicillin with a small amount (e.g. 0.1-1.0 per cent), of a water-soluble non-ionic surface-active agent in the presence of an organic solvent selected from lower aliphatic alcohols, ketones and chlorinated hydrocarbons, aliphatic carboxylic acid esters and aromatic hydrocarbons, and having a boiling point not substantially above 130 DEG C., at normal pressure, the organic solvent being thereafter removed, e.g. by the action of heat. Suitable solvents include methyl and n-butyl alcohol, ethyl, n- and isopropyl and n-butyl acetate, chloroform, carbon tetrachloride, dichlorethylene and especially acetone, whilst preferred surface-active agents are the polyoxyalkylene derivatives of partial esters of polyhydric alcohols having at most 10 hydroxy groups with fatty acids having at least 4 carbon atoms in the molecule, especially a polyoxyalkylene derivative of a hexitol inner anhydride partial long-chain fatty acid ester. In examples, the surface-active agent is polyoxyethylene sorbitan mono-oleate, alternatives to which are listed. Specifications 661,272 and 3806/46 (as open to inspection under Sect. 91) are referred to.ALSO:Solid readily dispersable preparations containing procaine penicillin are manufactured by intimately mixing (e.g. by trituration), procaine penicillin with a small amount (e.g. 0.1-1.0 per cent), of a water-soluble non-ionic surface active agent in the presence of an organic solvent selected from lower aliphatic alcohols, ketones and chlorinated hydrocarbons, aliphatic carboxylic acid esters and aromatic hydrocarbons, and having a boiling point not substantially above 130 DEG C at normal pressure, the organic solvent being thereafter removed, e.g. by the action of heat. The products, which may be distributed in vials, yield injectible suspensions by dispersing them in an injectible menstruum, especially water. Suitable organic solvents include methyl and n-butyl alcohol, ethyl, n-and iso-propyl and n-butyl acetate, chloroform, carbon tetrachloride, dichlorethylene and especially acetone, whilst preferred surface active agents are the polyoxyalkylene derivatives of partial esters of polyhydric alcohols having at most 10 hydroxy groups with fatty acids having at least 4 carbon atoms in the molecule, especially a polyoxyalkylene derivative of a hexitol inner anhydride partial long chain fatty acid ester. In examples, the surface active agent is polyoxyethylene sorbitan monooleate, alternatives to which are listed. Specifications 661,272 and 3806/46 (as open to inspection under Sect. 91), are referred to.