Ciba-Geigy Corporation

Henkel Kommanditgesellschaft Auf Aktien

Carlo Voellmy

Pier G Ferrini

Jonathan Green

Peter H Stahl

Hans Hess

The invention relates to topically administrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.3 alkyl.

Topical formulations

The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.1 -alkyl, or that is disubstituted by optionally Ar-containing alkylene, wherein two alkylene carbon atoms mar additionally be linked to one another via alkylene and Ar and Het.sub.1 are each as defined above, with the proviso that when R.sub.2 is --A--R.sub. 3, A is ethylene and R.sub.3 is unsubstituted or C.sub.1 -C.sub.3 alkyl-substituted amino, R.sub.1 is other than hydroxy.

Topically administrable pharmaceutical preparations

Divisible tablet having controlled and delayed release of the active substance and consisting of a compact that is optionally provided with a coating and is formed by at least one active substance in an adjunct composition that effects a delayed and controlled release of the active substance and optionally one or more additional adjunct compositions that optionally contain active substances and are arranged in longitudinal layers, the compact being of an oblong shape in which the ratio of length to width to depth is approximately 2.5 to 5: approximately 0.9 to 2:1 and the width constitutes at most 2/3 of the length, and in which one or more relatively deep dividing grooves are present which run perpendicularly to the length and the depth and have a total depth constituting from approximately 1/3 to approximately 1/2 of the depth of the tablet, but are at least so deep that one fracture surface area multiplied by the number of possible fragments constitutes a maximum of 15% of the surface area of the undivided tablet, the base and top faces independently of one another are planar or are convexly curved about the longitudinal axis or about parallels to this axis, the side faces are planar, the end faces can be of any shape and edges are optionally bevelled or rounded.

Growing community of inventors

Rheinfelden, Switzerland

Carlo Voellmy