Patent GB-959282-A (GB)
Title: Improvements relating to organic aluminium compounds
Inventor: DAVISON BRIAN KAY
IPC: C07F5/06
Filed: 1959-08-19
Abstract: Pharmaceutically active compounds with a predetermined rate of hydrolysis are prepared by reacting a polyoxo aluminium alkoxide (-O-Al-O-R) with water or with a pharmacologically reactive compound containing at least one OH, carboxylic acid, sulphonic acid, imido or keto-enolic group and with a hydrolysis-limiting compound, which may be oleic, stearic or benzoic acid, oleyl, stearyl, or ceto-stearyl alcohol, or castor oil.  Suitable aluminium starting compounds are polyoxo-aluminium isopropoxide, and polyoxoaluminium s-butoxide. They may be prepared by the method of Specification 869,171.  A list of suitable pharmacologically active substances is given in the Specification.  The polymeric aluminium compound may first be reacted with the hydrolysis-limiting substance and then with water or the pharmacologically active substance, or all three substances may be reacted simultaneously.  An alternative method where the substances contain acidic groups is to react an aluminium mono-soap of the pharmacologically-active substance with an aluminium mono-soap of the hydrolysis-limiting substance and by condensation with elimination of water to build up the aluminium containing polymer.  In examples the following products are prepared (1) polyoxo-aluminium oleate-p-amino-salicylate (2) polyoxo-aluminium benzoate-p-aminosalicylate (3) polyoxo-aluminium oleylate ascorbate (4) polyoxo-aluminium hydroxide oleate (5) a polyoxo-aluminium benzoate-chloral hydrate compound (6) polyoxo-aluminium stearate acetylsalicylate (7) polyoxo-aluminium prednisolone-stearate (8) polyoxo-aluminium stearate-ascorbate (9) polyoxo-aluminium oleate acetylsalicylate (10) an aluminium phenobarbitone derivative containing stearic acid residues.ALSO:Pharmaceutically active compounds with a predetermined rate of hydrolysis are prepared by reacting a polyoxo aluminium alkoxide (-O-A,L-O-R) with water or with a pharmacologically reactive compound containing at least one OH, carboxylic acid, sulphonic acid, imido or ketoenolic group and with a hydrolysis limiting compound, which may be oleic, stearic or benzoic acid, oleyl, stearyl, or ceto-stearyl alcohol, or castor oil. Suitable aluminium starting compounds are polyoxo-aluminium isopropoxide, and polyoxo-aluminium s-butoxide. They may be prepared by the method of Specification 869,171.  A list of suitable pharmacologically active substances is given in the Specification. The polymeric aluminium compound may first be reacted with the hydrolysis-limiting substance and then with water or the pharmacologically active substance, or all three substances may be reacted simultaneously.  An alternative method when the substances contain acidic groups is to react an aluminium mono-soap of the pharmacologically active substance with an aluminium mono-soap of the hydrolysis-limiting substance and by condensation with elimination of water to build up the aluminium containing polymer. In examples the following products are preferred:  (1) polyoxo-aluminium oleate-p-aminosalicylate, (2) polyoxo-aluminium benzoate -p-aminosalicylate, (3) polyoxo-aluminium oleylate ascorbate, (4) polyoxo-aluminium hydroxide oleate, (5) a polyoxo-aluminium benzoate, chloral hydrate compound, (6) polyoxo-aluminium stearate acetylisalicylate, (7) polyoxo-aluminium prednisolone-stearate, (8) polyoxo-aluminium stearate-ascorbate, (9) polyoxo-aluminium oleate acetylsalicylate, (10) an aluminium phenobarbitone derivative containing stearic acid residues.