NEW METHOD FOR PRODUCTION OF LIPOPLEX FOR LOCAL INTRODUCTION AND ANTI-TUMOR MEDICATION THAT USES SUCH LIPOPLEX Russian patent published in 2018 - IPC A61K31/7088 A61K31/7105 A61K9/127 A61K9/19 A61K45/00 A61K47/24 A61P35/00 

Abstract RU 2671857 C1

FIELD: pharmaceuticals.

SUBSTANCE: group of inventions relates to the chemical and pharmaceutical industry and is a process for producing a lipoplex comprising a mixture of lipids consisting of dioleoylphosphatidylethanolamine (DOPE), phosphatidylcholine and cationic lipid, and RNAi molecules, comprising the steps of dissolving dioleoylphosphatidylethanolamine (DOPE), phosphatidylcholine and cationic lipid in ethanol, where phosphatidylcholine is 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), palmitoyloleoylphosphatidylcholine (POPC) or 1,2-dicycosenoyl-sn-glycero-3-phosphocholine (DEPC), and wherein the cationic lipid is O,O'-ditetradecanoyl-N-(α-trimethylammonioacetyl)diethanolamine chloride (DC-6-14); adding the ethanol solution obtained in the previous step, dropwise to a solution of RNAi molecules in water with stirring; and lyophilization of the solution. Also, the invention includes a pharmaceutical composition that comprises lipoplex and a short, hairpin-forming RNA (short hairpin RNA) capable of inhibiting the expression of thymidylate synthase by RNA-i (TS-short hairpin RNA). Also, the group of inventions includes a combined product for the treatment of peritoneal metastases in stomach cancer, ovarian cancer and pancreatic cancer, comprising a pharmaceutical composition and an anticancer chemotherapeutic agent that has an inhibitory depolymerization of the microtubules of the mechanism of action.

EFFECT: group of inventions makes it possible to create a combined preparation exhibiting an additive or synergistic effect by combining lipoplex and an anticancer chemotherapeutic agent.

11 cl, 12 dwg, 7 ex

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RU 2 671 857 C1

Authors

Fukushima, Masakazu

Eshima, Kiyoshi

Ishida, Tatsuhiro

Dates

2018-11-07Published

2015-10-28Filed