SUSTAINED RELEASE ANESTHETIC COMPOSITIONS AND METHODS FOR PREPARATION THEREOF Russian patent published in 2024 - IPC A61K9/127 A61K31/167 A61K47/24 A61K47/28 A61P23/02 

FIELD: chemistry.

SUBSTANCE: group of inventions relates to an anaesthetic composition for local administration of a local anaesthetic to a subject in need thereof, comprising a lipid-based complex, containing ropivacaine base and a mixture of lipids containing at least one neutral saturated phospholipid in an aqueous buffer with pH 5.5 to 8.0, wherein at least one neutral saturated phospholipid is obtained from saturated fatty acids, wherein each fatty acid independently contains a carbon chain with not more than 18 carbon atoms; wherein the lipid-based complex is characterized by a median diameter of not less than 1 mcm; wherein the molar ratio of ropivacaine base to phospholipid in the lipid-based complex is at least 0.5:1, also relates to an anaesthetic composition for treating pain in a subject in need of anaesthesia by nerve block, by infiltration anaesthesia or by field block, containing a lipid-based complex containing ropivacaine base and a mixture of lipids, including at least one neutral saturated phospholipid in an aqueous buffer with pH 5.5 to 8.0, wherein at least one neutral saturated phospholipid is obtained from saturated fatty acids, wherein each fatty acid independently contains a carbon chain with not more than 18 carbon atoms; wherein the lipid-based complex is characterized by a median diameter ranging from 1 to 30 mcm, and the molar ratio of the ropivacaine base to the phospholipid in the lipid-based complex is at least 0.5:1, also relates to a method of providing anaesthesia or pain relief in a subject in need thereof, which provides for administering an anaesthetic composition to a subject, and also relates to a method of controlling pain or prophylactic treatment of pain in a subject, involving administering an anaesthetic composition to the subject.

EFFECT: group of inventions provides a sustained-release local anaesthetic composition characterized by improved anaesthetic efficacy, which provides the subject with a sufficient amount of ropivacaine base to prolong the action of anaesthesia after local administration.

18 cl, 4 dwg, 2 tbl, 5 ex