GB769517A — Analgesic compositions

USPTO Abstract

An analgesic composition comprises a potent analgesic and an antagonist as defined below in amount effective to counteract the side effects (narcosis, nausea, respiratory depresion, addiction, &c.) of the analgesic without impairing its analgesic activity. Potent analgesics specified include codeine, morphine, dihydromorphine, dihydrocodeine, dihydromorphinone, dihydrocodeinone, diacetylmorphine, d, l-isomethadone, l-isomethadone, d, l-methadone, l-methadone, 3-hydroxy-N-methyl-morphinan 6 - methyl - D 6 - desoxymorphine, ethylmorphine, N - methyl - 4 - phenyl - 4 - carbethoxypiperidine hydrochloride and hydroxydihydrocodeinone. Specified antagonists are N - n - propyl, - allyl, - isobutyl and - methallyl substituted normorphines, dihydronormorphines, desoxynormorphines, dihydrodesoxynormorphines, dihydronormorphinones and their acylates; the methyl ether derivatives of these compounds (i.e. the corresponding codeine compounds) with the exception of N - n - propylnorcodeine, N - isobutylnorcodeine, and the N - substituted - dihydronorcodeines; and 3 - hydroxy - N - allylnormorphinan. Both components of the composition may be in the free base or acid addition salt form, especially the sulphate, phosphate, citrate, hydrochloride and hydrobromide. The compositions may be used parenterally as aqueous suspensions or solutions with the addition of a buffer such as trisodium citrate, monosodium phosphate or disodium phosphate, and an antioxidant such as sodium bisulphate. In an example a composition comprising morphine sulphate N - allyl - normorphine hydrochloride, sodium bisulphite, monosodium phosphate monohydrate, anhydrous disodium phosphate and pyrogen free water is described. Specifications 722,571, 769,516, 769,518 and 769,519 [all in Group IV(b)] are referred to.