ACTIVE COMPONENT, PHARMACEUTICAL COMPOSITION AND DRUG PREPARATION FOR HIV AND AIDS THERAPY Russian patent published in 2020 - IPC C07C311/51 A61K31/18 A61P31/18 

FIELD: chemistry.

SUBSTANCE: invention relates to micronized monoclinic symmetry crystals (MMSC) with average particle diameter of ≤130 mcm sodium {[4-({[4-bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl]acetyl}amino)-3-chlorophenyl]-sulphonyl}(propanoyl)azanide - of formula Ib, sodium {[4-({[4-bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl]acetyl}amino)-3-chlorophenyl]-sulphonyl}(propanoyl)azanide of formula Ib. Crystals are an active component of a pharmaceutical composition and a medicinal agent for use in therapy of human immunodeficiency virus (HIV) and acquired immune deficiency syndrome (AIDS). Micronized crystals of the compound of formula Ib

have the following crystal characteristics:

crystalline form monoclinic Z 1h spatial group P21/c a 15.0367(4)Å b 25.2592(6)Å c 6.89727(19)Å α - β 91.216(2)° γ V, Ά 2623.79(12)
ų

and indicators powder X having interplanar spacings (D) and relative intensities (I_rel = I/I_o × 100) diffraction peaks of the monoclinic phase of the sample in angle region 2θ° 6°–30°:

(D) I/I_o×100 7.6 29 7.2 100 6.5 37 4.7 67 4.1 70 3.9 85

MMSC with said monoclinic crystal structure have DSC values within 244–253.5 °C with peak of 250 °C. Average particle diameter is from 10 to 130 mcm. Pharmaceutical composition has a solid form and additionally contains as excipients at least lactose monohydrate, sodium croscarmellose, povidone and magnesium stearate. Medicinal preparation is used in the form of an oral form.

EFFECT: comparative data on use of micronized and non-micronized particles (Ib and Ia, respectively) show that micronized particles increase exposure time of compound Ib in blood plasma.

17 cl, 4 dwg, 2 tbl, 8 ex