THERMODYNAMICALLY STABLE MODIFICATION OF (±)-1-(4-CARBAZOLYLOXY)-3-[2-(2- METHOXYPHENOXY)ETHYL-AMINO]-2-PROPANOL, METHOD OF ITS PREPARING AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF Russian patent published in 2003 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel thermodynamically stable modification of (±)-1-(4-carbazolyl-oxy)-3-[2-(2-methoxyphenoxy)ethylamino] -2- propanol (carvedilol) with melting point 123-126 C. X-ray diffraction pattern of this modification obtained by using radioactive source Cu_Kα, angle 2θ exhibits the following values: 9.5; 10.8; 12.0; 14.5; 19.6; 21.5 and 22.3 and its infra- red spectrum shows acute peak at 3451 cm^-1. Method of synthesis of and isolation of carvedilol involves rearrangement of crude carvedilol in methanol at temperature 25-35 C for 3-22 h and obtained modification is isolated from reactive mixture slowly cooled to temperature 0 C. Pharmaceutical composition designated for therapy of cardiovascular diseases involves practically pure form of stable modification of (±)-1-(4- carbazolyloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-2-propanol as acting substance in combination with one or some pharmaceutically acceptable carriers or adjuvants. EFFECT: improved method of synthesis and preparing, valuable medicinal properties. 6 dwg, 2 ex