Ivashchenko Aleksandr Vasilevich (US),Иващенко Александр Васильевич (US),Ivashchenko Andrej Aleksandrovich (RU),Иващенко Андрей Александрович (RU),Savchuk Nikolaj Filippovich (US),Савчук Николай Филип
申请号：
RU2019113338
公开号：
RU0002716257C1
申请日:
2019.04.30
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
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 Ibhave the following crystal characteristics:crystalline formmonoclinicZ1hspatial groupP21/ca15.0367(4)Åb25.2592(6)Åc6.89727(19)Åα-β91.216(2)°γV, Ά2623.79(12)Å3and indicators powder X having interplanar spacings (D) and relative intensities (Irel = I/Io × 100) diffraction peaks of the monoclinic phase of the sample in angle region 2θ° 6°–30°:(D)I/Io×1007.6297.21006.5374.7674.1703.985MMSC 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 exИзобретение относится к микронизированным кристаллам моноклинной симметрии (МКМС) со средним диаметром частиц ≤130 мкм натрий {[4-({[4-бром-3-(3-хлор-5-цианофенокси)-2-фторфенил]ацетил}амино)-3-хлорфенил]-сульфонил}(пропаноил)азанида - формулы Ib, натрий {[4-({[4-бром-3-(3-хлор-5-цианофенокси)-2-фторфенил]ацетил}амино)-3-хлорфенил]-сульфонил}(пропаноил)азаниду форм
