GB812138A — Improvements relating to antibiotic composition

USPTO Abstract

An intramuscularly acceptable antibiotic composition comprises tetracycline or oxytetracycline or their acid or basic salts, a soluble source of magnesium ions, a soluble source of absorption-enhancing non-toxic acid ions which source is solid in the dry state, and a non-toxic local an sthetic. The source of absorption-enhancing ions may be a water-soluble non-toxic carboxylic or thiocarboxylic acid or a lactone of such acids including citric, ascorbic, gluconic and thioglycollic acids or may be a soluble mineral acid salt of an amino acid. The antibiotic may be used in salt form as the hydrochloride, hydrobromide, sulphate, nitrate, citrate, ascorbate or gluconate, or as the sodium, potassium, ammonium, calcium, or magnesium salts as well as in the neutral form. The magnesium source may be a soluble ionizable salt such as the halides and their hydrates, e.g. magnesium chloride hexahydrate, or magnesium sulphate, nitrate, bromide, acetate, glycinate or as the magnesium salt of one of the absorption enhancing acids such as magnesium citrate or ascorbate. Specified local an sthetics include procaine, xylocaine, hydroxy-procaine, 2-chloroprocaine, piperocaine, hexylcaine, diethoxin, tetracaine and larocaine. They may be used as the free base or more conveniently as the hydrochlorides. The compositions may be prepared as a sterile, dry powder to which water may be added immediately prior to use, or alternatively one or more of the storage stable constituents may be present in the aqueous diluent. The components may be mixed and sterilized by ethylene oxide or if desired by high frequency radiation or by neutrons. The final composition should preferably contain 10 to 100 milligrams/millilitre of antibiotic calculated as antibiotic hydrochloride, an amount of an sthetic equivalent in effect to that obtained from 0.5 to 40 milligrams/millilitre, from 1 to 15 milligrams/millilitre of magnesium ions and the absorption-enhancing ions in an amount equal to up to three times that of the antibiotic. In an example, tetracycline hydrochloride, anhydrous citric acid and procaine hydrochloride are ground together and sterilized by exposure to ethylene oxide. Heated ground magnesium chloride hexahydrate is added and the mixture filled into glass vials. Reference has been directed by the Comptroller to Specification 739,736.