A process for preparing suitable for parenteral administration, stable aqueous solutions containing amino ketone derivatives, and aqueous medium for use thereby.

摘要

1440275 Respiratory stimulating composition RICHTER GEDEON VEGYESZETI GYAR RT 21 Dec 1973 [15 Jan 1973] 59324/ 73 Heading A5B A stable injectable solution comprises (i) an aminoketone derivative of formula: wherein R1 is hydrogen or C1-4 alkyl and R2 is alkylphenyl wherein the alkyl group contains 1 to 10 carbon atoms or R1 and R2 together represent a C3-5 alkylene group and X represents an anion or one equivalent of a polyvalent anion, (ii) a nonionic surface active agent, (iii) a polyhydric alcohol, (iv) an ammonium or amine salt of a strong acid and (v) an organic acid having a pKa value between 2 and 4. In the formula X may be chloride or sulphate. Compounds specified include (i) 1- piperidino - 3 - (4' - n - octylphenyl) - propan- 3-one hydrochloride, 1-piperidino-2-methyl-3- (4-methylphenyl)-propan-3-one hydrochloride and 1-piperidino-methyl-cyclohexane-2-one hydrochloride (ii) an oleic ester-alkylene oxide adduct, a castor oil-ethylene oxide adduct, sorbitan monolaurate-ethylene oxide adduct, (iii) propyleneglycol, glycerol, polyethylene glycol, (iv) ammonium chloride, piperidine hydrochloride, (v) ascorbic acid, maleic acid. The composition may also include a local anaesthetic, e.g. lindocaine hydrochloride.