GB808269A — Barbiturate pharmaceutical preparations

USPTO Abstract

b : b - Methyl - ethyl - glutaramic acid is prepared by treating b : b -methyl-ethyl-glutaric anhydride in water with ammonia followed by acidification with hydrochloric acid. b : b -Methyl-ethyl-dithioglutarimide is prepared by boiling methyl-ethyl-glutarimide in xylene with phosphorus pentasulphide. b : b - Methyl - isobutyl-glutarimide is prepared by heating b : b -methyl-isobutyl-glutaric acid with urea. a : b -Dimethyl - b - ethyl - glutarimide is prepared by treating a : a 1 - dicyano - b : b - methyl - ethyl-glutarimide with dimethyl sulphate in presence of sodium and absolute alcohol to give N - methyl - a : a 1 - dicyano - a - methyl - b : b - methyl-ethyl-glutarimide, converting this by treatment with sulphuric acid to N-methyl-a : b - dimethyl - b - ethyl - dicarbamoyl - glutarimide, hydrolysing this with sulphuric acid to a : b - dimethyl - b - ethyl - glutaric acid, distilling this to give a : b -dimethyl-b -ethyl-glutaric acid anhydride and heating this with urea.ALSO:A pharmaceutical preparation comprising a medicinal barbiturate and a substituted glutaric acid derivative selected from b ,b -methyl ethyl glutaramic acid, b ,b -methyl ethyl dithioglutarimide, b -spirocyclopentane glutarimide, b -spirocyclohexane glutarimide, b -spirocycloheptane glutarimide, b ,b - dimethyl glutarimide, b ,b - diethyl glutarimide, b ,b - methyl isobutyl glutarimide, b ,b -methyl-n-propyl glutarimide, a ,b ,b - trimethyl glutarimide, a ,b - dimethyl - b - ethyl glutarimide, a - ethyl - b ,b - dimethyl glutarimide and camphoric acid imide, or mixtures thereof in an amount insufficient to interfere with a therapeutic dose of barbiturate but sufficient to overcome the toxic effects of overdose. Specified barbiturates are phenobarbitone, amylobarbitone, butobarbitone, pentobarbitone sodium, quinolbarbitone sodium, hexobarbitone sodium. The proportion of substituted glutaric acid derivative should be 5-200 per cent, preferably 25-150 per cent, by weight of the barbiturate. In addition the preparation may include b ,b -methyl ethyl glutarimide; mild stimulants such as caffeine and amphetamine; mild sedatives such as sodium bromide; hypnotics such as chloral and paraldehyde; analgesics such as aspirin, phenacetin and codeine; antiasthmatics such as ephidrine; anticholinergics such as atropine; anticonvulsants such as hydantoin. The preparation may be in the form of an injection, suppository, tablet, elixir or capsule and may embody an agent when in capsule or tablet form, delaying the release of the substituted glutaric acid derivative. In tablet form the barbiturate may form a layer compressed over a core containing substituted glutaric acid derivative.