http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-824311-A

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D459-00
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D459-00
filingDate 1956-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1959-11-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-824311-A
titleOfInvention New alkaloid and process for manufacturing same
abstract The invention comprises the alkaloid reserpoxidine and its salts, together with its preparation from reserpine mother liquors (containing the weakly basic alkaloids less the greater part of the reserpine, deserpidine and rescinnamine present) by treatment with nitric acid, separating the nitrate salt formed, and, if desired, converting this to the free base (e.g. with ammonia) and thence into another salt. Reserpoxidine can be reduced to reserpine catalytically or with zinc and acetic acid. Examples are given of the isolation of reserpoxidine (as nitrate and free base), and conversion into oxalate, perchlorate, sulphate and hydrochloride. Salts can also be made with phosphoric, acetic, propionic, lactic, succinic, malic, tartaric, citric, p ascorbic, methanesulphonic, ethanesulphonic, isethionic, benzoic, salicylic, p-aminosalicylic, toluenesulphonic and picric acids. The starting material can be obtained from Rauwolfia serpentina, R. canesceus or R. vomitoria by the method of Specification 734,108, and the reserpine mother liquor (e.g. as ethanol extract) freed from deserpidine and rescinnamine by the method of Specification 809,912.ALSO:Pharmaceutical preparation comprise the hypotensive alkaloid reserpoxidine (or a salt thereof) with a carrier, e.g. in the form of tablets, powder, capsules, pills, solutions, emulsions or suspensions. There may be present (1) auxiliary substances such as preservatives, stabilizers, wetting or emulsifying agents, buffers or salts for the control of osmotic pressure; and (2) other active substances such as ganglionic blockers, adrenergic blockers, sedatives, central nervous stimultants, cholinergic blockers or antihistaminics. Specified substances of type (2) are N : N : N1 : N1 : 3-pentamethyl - N : N1 - diethyl - 3 - azopentylene-1 : 5-diammonium dibromide, hexamethylene-bis - trimethylammonium bromide, pentamethylene - bis - methylpyrrolidinium tartrate, 2 - (21 - dimethylaminoethyl) - 4 : 5 : 6 : 7-tetrachloro - isoindoline dimethochloride, 2-(N1 - p - tolyl - N1 - m - hydroxyphenylaminomethyl) - imidazoline, ergot alkaloid derivatives, 1 - hydrazino - phthalazine, 1 : 4 - dihydrazinophthalazine, reserpine, deserpidine, 3 : 4 : 5 - trimethoxycinnamoyl methyl reserpate or deserpidate, acetyl methyl reserpate, 3 - ethyl - 3 - phenyl - 2 : 6 - dioxo - piperidine, barbiturates, N - (31 - dimethylaminopropyl) - 3-chlorophenthiazine, methyl a - piperidylphenyl - acetate, a - methylphenylethylamine, diethylaminoethyl a - cyclohexyl - a - phenyl glycollate methobromide, atropine, diethylaminoethyl 9 - xanthenecarboxylate methobromide, and 2 - [benzyl - (21 - dimethylaminoethyl) - amino] - pyridine. Examples show compositions of reserpoxidine in the form of tablets or as injections containing citric acid, benzyl alcohol, polyethyleneglycol and water. Other specified ingredients are vegetable oils, ascorbic acid, propylene glycol, petroleum jelly and cholesterol. The amount of reserpoxidine in each dose may be 0.1 to 100 mg., preferably 0.2 to 20 mg.
priorityDate 1955-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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