Patent GB-638606-A (GB)
Title: Improvements in or relating to processes of preparing new antihistaminic compositions, and the new compositions resulting from said processes
IPC: A61K31/54
Filed: 1948-01-22
Abstract: A pharmaceutical preparation comprises an antihistaminic drug and a xanthine.  Specified anti-histamine drugs are tertiary-aliphatic-amino-alkyl (esp. b  dialkyl amino alkyl) benzohydryl ethers, e.g., b -dimethyl (or b -diethyl)-aminoethyl benzohydryl ether; N-tertiary-aliphatic-amino-alkyl (esp. N-beta dialkylamino-alkyl)-N-aryl methyl a -aminopyridine, e.g., N-beta-dimethyl-amino-ethyl N-benzyl a -amino-pyridine; N-p-methoxy-benzyl-N-p-dimethyl aminoethyl-a -amidopyridine; N-beta-dimethylaminoethyl-N-benzyl (or ethyl)-aniline; 10-beta-dimethylaminoethylphenothiazine; 10-beta-dimethylaminoethylacridan; beta-dimethylaminoethyl fluorene-9-carboxylate; beta-dimethylamino-ethyl diphenylcarbinol; beta-dimethylaminoethyl phenyl-a -pyridylmethyl ether; 10-beta-diethyl-aminoethyl thioxanthene; beta-dimethylaminoethyl 9,10-dihydro-9-anthryl ketone; N-beta-dimethylaminoethyl-N-benzyl-2-amino-pyrimidine; 10-beta-dimethyl-aminoethyl thioxanthene; 9-beta-dimethyl-aminoethyl-9, 10-dihydroanthracene; 10-beta-dimethylaminoethylxanthene; beta-diethyl (or dimethyl) aminoethyl 9,10-dihydroanthracene - 9 - carboxylate; beta-dimethylamino - ethyl - 9,10 - dihydro - 9 - anthryl-carbinol; benzohydryl beta-diethylaminopropionate and ethyl 4-phenyl-1-methylpiperidine-4-carboxylate.  The dimethyl (or diethyl) aminoethyl groups in the above compounds may be replaced by similar dialkylaminoalkyl groups such as diethylaminopropyl, dipropylaminoisopropyl, methylethylaminoethyl, 1-methyl-propylamino-2-butyl, or by the groupings morpholinoethyl, piperidonopropyl, pyrrolidinoethyl, methylpiperidinoisopropyl and 1-dimethyl piperidino-2-propyl.  The drug may be used in the form of the free base or of a non-toxic inorganic or organic salt, e.g., of hydrochloric, hydrobromic, sulphuric, phosphoric, sulphamic, tartaric, citric, lactic or acetic acids.  Specified xanthines are theophylline, aminophylline, caffeine, theobromine, paraxanthine and the methylxanthines.  The compositions with or without suitable diluents such as starch, gelatin, milk sugar, cane sugar, dextrin, acacia, tragacanth, sodium phosphate, kaolin and calcium carbonate, may be filled into capsules or compressed into tablets with the aid of lubricants such as petrolatum, boric acid, talc, lycopodium, cocoa butter and stearic acid.  Elixirs and emulsions may also be prepared. According to one example, tablets of aminophylline are enteric coated by alternatively spraying with an alcoholic solution of gum mastic and drying by the application of powdered magnesium stearate.  The tablets so treated are moistened with an aqueous solution of gelatin, acacia and sugar, and dried by applying benzohydryl beta-dimethylaminoethyl ether hydrochloride in a diluent (e.g., chalk, acacia and sugar), the operation being repeated until the desired quantity of antihistamine drug has been incorporated.  The tablets are finished off with a coating of sugar syrup.  An elixir is given containing aminophylline, beta-dimethylaminoethyl benzohydryl ether, sugar, glycyrrhiza syrup, alcohol and glycerin.