GB805523A - Local anesthetic composition and preparation thereof - Google Patents

Abstract

An aqueous composition, suitable for parenterol injection to produce local an sthesia and controlled xerostromia in the oral cavity, comprises an aqueous solution of a local an sthetic containing also an alkantheline in the amount of 1-50 mg. per ml. of said solution. Alkanthelines are defined as being quaternary ammonium salts of alkamine esters of 9-xanthene-carboxylic acid having the structural formula: <FORM:0805523/VI/1> where the lower alkyl groups have from 1 to 4 carbon atoms and may be the same or different, and An is a non-toxic anion, e.g. chloride, bromide or sulphate. Preferred compounds are methantheline bromide (2-diethylaminoethyl-9-xanthene carboxylate methobromide) or propanthaline bromide (2-diisopropylaminoethyl-9-xanthene carboxylate methobromide). Suitable local an sthetics are procaine, tetracaine, butathamine, propoxycaine, lidocaine, hexylcaine, and 2-diethylaminoethyl-3-amino-2-(n-butoxy) benzoate. The concentration of an sthetic in the solution is from 0.5 to 4 per cent by weight, and the solutions may also contain vasoconstrictors, e.g. hydrochloride or tartrate of epinaphrine, lero-arterenal and "Nordefrin" (Registered Trade Mark), and preserving agents. The compositions may be prepared by simply dissolving the appropriate amounts of active ingredients in water.