COMPOSITION FOR INHIBITING ANOMALOUS DEPOSITION AND MOBILIZATION OF CALCIUM PHOSPHATE IN HUMAN TISSUE

摘要

Pharmaceutical compositions for inhibiting anomalous deposition and mobilization of calcium and phosphate in human tissue comprise one or more polyphosphonates of the formulae: in which R 1 and R 2 are each H or -CH 2 OH n is an integer from 3 to 10 R 3 is H, alkyl, cycloalkyl, alkenyl, aryl, phenethenyl, benzyl, halogen, amino, substituted a m i n o , -CH 2 COOH, -CH 2 PO 3 H 2 , -CH(PO 3 H 2 ) (OH) or -CH 2 CH (PO 3 H 2 ) 2 and R 4 is H, alkyl, amino, benzyl, halogen, -OH, -CH 2 COOH, -CH 2 PO 3 H 2 or -CH 2 CH 2 PO 3 H 2 or a pharmaceutically acceptable salt thereof in admixture with a solid or liquid pharmaceutically acceptable carrier, which carrier is not water alone and does not include a phenolic or quaternary ammonium bactericide or more than 10% by weight of the active compound, of a wetting agent. Suitable salts include alkali metal (e.g. Na, K), alkaline earth metal (e.g. Ca, Mg), non-toxic heavy metal (e.g. Sn, In), ammonium and substituted ammonium (e.g. mono-, di- and triethanolammonium) salts. Ethane-1-hydroxy-1, 1-diphosphonic acid (also known as 1-hydroxyethylidene diphosphonic acid) is the preferred active compound. The compositions may be administered orally, parenterally or rectally in unit dosage forms comprising tablets, suppositories, pills, dragees, wrapped powders, cachets, sachets, capsules, ampoules or granules. A medicament in dosage unit form may comprise the polyphosphonate(s) alone or in admixture with a carrier.