FIELD: pharmaceutics.
SUBSTANCE: group of inventions relates to a method for obtaining an anesthetic composition with delayed release and to a composition for local administration of an anesthetic to a subject in need obtained by this method. A method for obtaining a delayed-release anesthetic composition involves: dissolving a lipid mixture and at least one amide-type anesthetic in a solvent system to obtain a liquid structure; removal of a solvent system from a liquid structure where the solvent system contains tert-butanol or tert-butanol/water as a co-solvent, to obtain a lipid structure with a high degree of capture (HELS); hydration of HELS using an aqueous buffer solution at a pH of 5.5 to 8.0. Moreover, as a result of hydration of HELS, multilayer vesicles (MLV) with a captured amide-type anesthetic are formed; moreover, the median diameter of MLV vesicles with a captured amide-type anesthetic is at least 1 mcm; and the molar ratio of an amide-type anesthetic and phospholipid in MLV vesicles with a captured amide-type anesthetic is at least 0.5:1. The anesthetic composition obtained by the above method contains multilayer vesicles with a captured amide-type anesthetic, the median diameter of which is at least 1 mcm, and the molar ratio of an amide-type anesthetic and phospholipid in the specified vesicles is at least 0.5:1.
EFFECT: use of the composition obtained by the above method provides a rapid onset of anesthesia and a prolonged duration of local anesthesia with minimal toxicity.
12 cl, 5 dwg, 2 tbl, 5 ex
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Authors
Dates
2023-03-09—Published
2018-08-28—Filed