Pseudopolymorphic forms of carvedilol
OwnerAndre Gerard Bubendorf, Rolf-Dieter Gabel +5inventors
InventorsAndre Gerard Bubendorf, Rolf-Dieter Gabel, Michael Hennig, Siegfried Krimmer, Guenter Neugebauer, Walter Preis, Alexander Wirl
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Abstract
The present invention is concerned with pseudopolymorphic forms of 1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole (carvedilol) or of optically active forms or pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them.
Claims18
A pseudopolymorphic form of (±)1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole or of an optically active form or pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising (a) the compound (±)1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole hemihydrate having the following X-ray diffraction pattern obtained with a CuKα1-radiation at 2θ=7.0, 8.3, 11.5, 15.7, and 17.2, an infrared spectrum having sharp peaks at 3526 cm−1, 3492 cm−1 and 3400 cm−1, and a melting point of approximately T Onset=94-96° C. and (b) a pharmaceutically acceptable carrier and/or adjuvant.
The composition according to claim6, wherein polyethylene glycol is present as the adjuvant which is not surface-active.
The composition according to claim8, wherein a sugar substitute is present as the adjuvant which is not surface-active.
The composition according to claim13, wherein the ratio of adjuvants which are not surface active to non-ionic tensides lies between 1000:1 and 1:1, preferably between 100:1 and 10:1.
The composition according to claim14, wherein the compound is present in a concentration between 5% (wt./wt.) and 60% (wt./wt.).
The composition according toclaim16, wherein highly dispersed silicon dioxide is present.
A composition according toclaim17, which contains 10-20% (wt./wt.) of the compound, 65-85% (wt./wt.) polyethylene glycol, 1-10% (wt./wt.) polyoxyethylene-polyoxypropylene copolymer and 0.1-10% (wt./wt.) highly dispersed silicon dioxide.
Dependencies are inferred from the claim text.