Boehringer Mannheim Gmbh

Werner Rothe

Helmut Heinemann

Heinrich Woog

Felix Helmut Schmidt

Werner Gruber

Peter Rieckmann

Gunter Betzien

Gregor Groppenbacher

An instillation composition, comprising an effective amount of at least one sparingly soluble active material suspended or partly dissolved in an aqueous emulsion containing a swelling agent. Advantageously the active substance is nitrofurantoin or a quinolone or pyridazine derivative, the active material has a particle size less than about 10 .mu.m and the swelling agent is a polysaccharide derivative present in about 0.3 to 3% by weight of the composition, the composition further containing at least one local anesthetic, antiphlogistic substance, emulsifier, buffer or stabilizer. With the invention, unit doses of only 50 ml. will contain sufficient active material.

Instillation composition

Stable, physiologically compatible, injectable solutions comprising, as an active ingredient, an alkali metal salt of canrenoic acid or a mixture of an alkali metal canrenoate and a diuretic, and an aqueous, physiologically compatible alkaline buffer having a low buffer capacity and yielding a pH range of 10.2 to 11.2, e.g., tripotassium phosphate, potassium carbonate or potassium glycinate.

Injectable pharmaceutical solutions

A blood sugar lowering composition comprising as the active material particulate glibenclamide having a surface area of about 3 to 10 m.sup.2 /g in admixture with a pharmacologically acceptable non-ionic wetting agent present in about 2 to 20 times the weight of the glibenclamide. The preferred wetting agent is polyoxyethylene stearate present in about 5 to 10 times the weight of the glibenclamide.

Rapidly resorbable glibenclamide

Coated tablets are prepared by applying to a core of active material, at least one layer of a coating composition made up of a film forming aqueous synthetic resin dispersion and from 2-50% by weight of a water or alkaline soluble material and thereafter permitting the coating composition layer to dry. The resulting coated tablet has a core surrounded by a continuous porous matrix of synthetic resin formed from the aqueous dispersion which is insoluble in water and insoluble in the gastrointestinal tract. The pores of the continuous resin matrix are filled with a discontinuous particulate material which is water or alkaline soluble. The coated tablet initially is air and moisture tight.

Tablets coated with aqueous resin dispersions

The method of preparing adjuvant-free tablets from a tableting mass having a tendency to stick, comprising alternately in the same mold forming tablets from said tableting mass and from an adjuvant mass containing an easily tableted substance, a lubricant and a mold parting agent. The lubricant may be talc or sodium benzoate present in about 5 to 20% by weight, and the mold release agent may be stearic acid, a stearate, paraffin or a silicone oil in about 0.5 to 10% by weight. By this method tablets of pure fructose can be formed.

Preparation of adjuvant-free fructose tablets

Rapidly resorbable particulate glibenclamide having a particle surface area of active material of at least 3 m.sup.2 /g is produced by precipitating the active material from its solution in an organic solvent or in water or aqueous alcohol, preferably rendered alkaline, using water which is preferably acidified.

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Hockenheim, Germany

Werner Rothe