LIPOSOMAL COMPOSITIONS CONTAINING SLIGHTLY ACIDIC DRUGS, AND THEIR USE Russian patent published in 2022 - IPC A61K9/127 A61K31/5575 A61K31/5578 A61K31/5585 A61K31/56 A61P11/00 

FIELD: medicine.

SUBSTANCE: group of inventions relates to the field of medicine, namely to a pharmaceutical composition for the treatment and/or preventive treatment of pulmonary hypertension, chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis, lower respiratory tract infection, bronchiectasis, bronchitis, bronchiolitis, or croup, containing one or several liposomes. In this case, the specified liposome contains: (a) a lipid bilayer containing at least one vesicle-forming lipid; and (b) an internal aqueous medium inside the lipid bilayer, containing bicarbonate salt at a concentration from 50 mM±10% to 800 mM±10% and a slightly acidic drug with pK_a from 1±10% to 6±10%. At the same time, liposomes are suspended in an external aqueous medium. pH of the external aqueous medium is higher than pK_a value of the slightly acidic drug, which is up to 7±10%, and pH of the internal aqueous medium is at least one unit higher than pH of the external aqueous medium. The invention also relates to a method for the treatment of a respiratory disease, including stages of administration of a pharmaceutical composition containing one or more liposomes. In this case, the specified liposome contains: (a) a lipid bilayer containing at least one vesicle-forming lipid; and (b) an internal aqueous medium inside the lipid bilayer, containing bicarbonate salt at a concentration from 50 mM±10% to 800 mM±10% and a slightly acidic drug, where the slightly acidic drug is prostaglandin, steroid, antibiotic, warfarin, nonsteroidal anti-inflammatory drug (NSAID), or any combination thereof. At the same time, liposomes are suspended in the external aqueous medium, while pH of the external aqueous medium is higher than pK_a value of the slightly acidic drug, which is up to 7±10%, while pH of the internal aqueous medium is at least one unit higher than pH of the external aqueous medium. The respiratory disease is pulmonary hypertension, chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis, lower respiratory tract infection, bronchiectasis, bronchitis, bronchiolitis, or croup. The invention also relates to a pharmaceutical composition for the treatment and/or preventive treatment of pulmonary hypertension, containing one or more liposomes. In this case, the specified liposome contains: (a) a lipid bilayer containing at least one vesicle-forming lipid; and (b) an internal aqueous medium inside a lipid bilayer, containing bicarbonate salt at a concentration from 50 mM±10% to 800 mM±10% and prostacyclin. At the same time, liposomes are suspended in the external aqueous medium, while pH of the external aqueous medium is higher than pK_a value of prostacyclin, which is up to 7±10%, and pH of the external aqueous medium is at least one unit higher than pH of the external medium.

EFFECT: group of inventions provides the creation of liposomal compositions with high efficiency of drug loading to increase therapeutic efficiency.

22 cl, 6 tbl, 6 ex