CRYSTALLINE FORMS OF CORTEXOLONE-17α-PROPIONATE AND METHOD FOR PREPARING THEM Russian patent published in 2013 - IPC C12P33/00 C07J5/00 A61K31/573 A61P5/28 

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to biochemistry. What is presented is a crystalline form I and III of cortexolone-17α-propionate. The crystalline form I is characterised by a powder X-ray pattern as presented on Fig. 1, and/or by differential scanning calorimetry as presented on Fig. 2, and/or by an IR spectrum as presented on Fig. 3. The crystalline form III is characterised by a powder X-ray pattern as presented on Fig. 7, 10 or 13, and/or by differential scanning calorimetry as presented on Fig. 8, 11 or 14, and/or by an IR spectrum as presented on Fig. 9, 12 or 15. There are also presented methods for preparing the crystalline form I and III of cortexolone-17α-propionate. The method for preparing the crystalline form I involves crystallisation of cortexolone-17α-propionate for tert-butylmethyl ester. The method for preparing the crystalline form III of cortexolone-17α-propionate involves crystallisation of cortexolone-17α-propionate from a solvent representing a mixture of dichloromethane/n-hexane or a mixture of acetone/n-hexane, or a mixture of ethanol/water.

EFFECT: these crystalline forms in combination with at least one physiologically acceptable excipient are used in pharmaceutical compositions for treating urogenital, endocrine skin and/or and cutaneous appendage pathologies, particularly for treating acne, seborrheic dermatitis, androgenetic alopecia, hirsutism, benign prostatic hyperplasia, prostate cancers, male contraception, polycystic ovarian syndrome, previous puberty syndrome and control of aggressive or aberrant sexual behaviour.

21 cl, 30 dwg, 3 tbl, 9 ex