Patent RU-2718900-C2 (RU)
Title: Pharmaceutical compositions for prolonged release of sebacoyl-dinalbuphine ester
Inventor: LI Chan-Tszyun
IPC: A61K9/08
Filed: 2016-05-27
Granted: 2020-04-15
Abstract: FIELD: medicine; pharmaceuticals. 
     SUBSTANCE: declared group of inventions refers to pharmaceutics and represents a pharmaceutical composition for pain treatment containing sebacoyl-dinalbuphine ester (SDE) dissolved in a pharmaceutically acceptable oil and an oil-miscible solvent, where the concentration of the SDE in composition is 75 mg/ml, where the oil-miscible solvent is benzyl benzoate, where the weight ratio of the solvent to be mixed with the oil to the pharmaceutically acceptable oil is 1.12:1, and where the pharmaceutical composition is a clear solution and is to be injected, method of preparing a pharmaceutical composition comprising steps of: dissolving SDE in benzyl benzoate and mixing the solution obtained at the previous step with a pharmaceutically acceptable oil until a homogeneous solution is obtained, wherein the composition is a clear solution and is intended for administration by injection, a method of treating pain, comprising using a therapeutically effective amount of a pharmaceutical composition, where the pharmaceutical composition is administered by intramuscular injection 6–36 hours before the development of pain symptoms, a pharmaceutical composition for pain management containing sebacoyl-dinalbuphine ester (SDE), a pharmaceutically acceptable oil and an oil-miscible solvent, where the composition is a transparent solution to be injected, and releases the SDE in a prolonged manner, where the pharmaceutically acceptable oil is soya oil, peanut butter, sesame oil or a mixture thereof, wherein the oil-miscible solvent is benzyl benzoate, benzyl alcohol or a mixture thereof, and wherein weight ratio of oil-retaining solvent to pharmaceutically acceptable oil is greater than 1, and the duration of the pharmaceutical composition is equal to or greater than 5 days, and/or the release period of the pharmaceutical composition is equal to or greater than 14 days, a pharmaceutical composition for treating pain, comprising sebacoyl-dinalbuphine ester (SDE), a pharmaceutically acceptable oil and an oil-miscible solvent, where the composition is a transparent solution to be injected, and releases the SDE in a prolonged manner, where the pharmaceutically acceptable oil is soya oil, peanut butter, sesame oil or a mixture thereof, wherein the oil-miscible solvent is benzyl benzoate, benzyl alcohol or a mixture thereof, wherein weight ratio of oil-retaining solvent to pharmaceutically acceptable oil is less than 1, and duration of action of pharmaceutical composition is less than 6 days, and/or the release period of the pharmaceutical composition is less than 14 days, a method of preparing a prolonged release composition for injections containing sebacoyl-dinalbuphine ester (SDE), with a predetermined release period of more than 14 days, comprising the steps of: preparing an oil-mixed solvent and a pharmaceutically acceptable oil, wherein weight ratio of oil mixed solvent to pharmaceutically acceptable oil is greater than 1; and mixing SDE with oil-miscible solvent and pharmaceutically acceptable oil until obtaining a homogeneous solution, wherein the composition is administered by injection, and a method of preparing a prolonged release composition for injections containing sebacoyl-dinalbuphine ester (SDE), with a predetermined release period of less than 14 days, comprising the steps of: preparing an oil-mixed solvent and a pharmaceutically acceptable oil, wherein the weight ratio of the solvent to be mixed with the oil to the pharmaceutically acceptable oil is less than 1; and mixing SDE with an oil-miscible solvent and a pharmaceutically acceptable oil until a homogeneous solution is obtained, wherein the composition is administered by injection. 
     EFFECT: use of the disclosed composition enables to obtain a homogeneous stable composition having a long shelf life, while maintaining homogeneity and free from formation of solid particles and precipitation, in form of a transparent solution suitable for administration by controlled release injection for treating pain. 
     17 cl, 15 dwg, 21 tbl, 10 ex