PROSTACYCLIN ANALOGUE PREPARATIONS Russian patent published in 2021 - IPC A61K31/192 A61K31/5578 A61K31/5585 A61K47/10 A61K47/14 A61K47/18 A61K47/20 A61K47/24 A61K9/00 A61P9/12 A61P9/10 

FIELD: pharmacology; medicine.

SUBSTANCE: group of inventions relates to the field of pharmacology and medicine, namely to an injectable precursor drug for the treatment of a condition selected from pulmonary arterial hypertension (hereinafter – PAH), severe PAH, PAH-associated chronic obstructive pulmonary disease (COPD), Raynaud’s disease and ischemia. The precursor drug contains: a) from 38 to 52% by weight of diacillipid, which is glycerin dioleate; b) from 38 to 52% by weight of phospholipid selected from phosphatidylcholine and dioleoyl phosphatidylcholine; c) from 5 to 15% by weight of a biocompatible organic solvent selected from ethanol, propylene glycol, N-methylpyrrolidone, dimethyl sulfoxide and their mixtures; and d) from 0.1 to 10% by weight of a prostacycline analogue, which is treprostinyl or its salt; while the specified precursor drug forms or is capable of forming at least one structure in a liquid crystal phase when in contact with an excess of water-based liquid. In addition, the following is described: the use of the above-mentioned precursor drug for prolonged injection of treprostinil, a method for the treatment of pulmonary arterial hypertension (PAH), severe PAH, Raynaud's disease and ischemia in a subject, including the injection of a therapeutic dose of the precursor drug to the subject, the use of a pharmaceutical precursor drug in the production of a drug, and a pre-filled device for the injection of treprostinil.

EFFECT: presented precursor drug undergoes a phase transition when exposed to water-based fluids, such as body fluids, resulting in a composition with controlled release of treprostinil for the treatment of pulmonary arterial hypertension (PAH), severe PAH, Raynaud’s disease, ischemia and related conditions.

22 cl, 10 dwg, 15 tbl, 7 ex