# US 10,307,396 B2 · Pharmaceutical composition containing silybin, VE and L-carnitine > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,307,396 B2 - Document ID: US10307396B2 - Status: Granted - Kind: B2 - Application number: 15/560,568 - Filed: 2016-03-22 - Published: 2018-03-01 - Granted: 2019-06-04 - Earliest claimed: 2015-03-23 - Assignees: Tasly Pharmaceutical Group Co., Ltd. - Applicants: Tasly Pharmaceutical Group Co., Ltd. - Inventors: He Sun; Xijun Yan; Naifeng Wu; Kaijing Yan; Yonghong Zhu; Shunnan Zhang; Xiaolin Bai; Xiaohui Ma; Yi He; Ting Li; Lei Li - Web page: https://patentgrep.com/patent/US10307396B2 ## CPC - A61K 31/357: having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel - A61K 9/08: Solutions {(composition of solutions A61K47/00)} - A61K 9/1617: {Organic compounds, e.g. phospholipids, fats} - A61K 9/1682: {Processes} - A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} - A61K 31/205: Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine - A61K 31/355: Tocopherols, e.g. vitamin E - A61K 31/683: Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols - A61K 36/488: Pueraria (kudzu) - A61K 36/82: Theaceae (Tea family), e.g. camellia - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics - A61K 2236/19: involving fermentation using yeast, bacteria or both; enzymatic treatment - Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE ## Abstract A pharmaceutical composition. The pharmaceutical composition is prepared from the following raw materials in parts by weight: 8.75-60 parts of silybin, 15-65 parts of phospholipid, 25-200 parts of a Pu'er tea extract, 6.25-40 parts of vitamin E, and 8.3-60 parts of L-carnitine. The composition can be used for treating non-alcoholic fatty liver diseases. ## Claims ### Claim 1 A pharmaceutical composition comprising 8.75-60 parts by weight of silybin; 15-65 parts by weight of phospholipid; 25-200 parts by weight of Pu'er tea extract; 6.25-40 parts by weight of vitamin E; and 8.3-60 parts by weight of L-carnitine. ### Claim 2 (depends on 1) The pharmaceutical composition of claim 1 comprising 25-40 parts by weight of silybin; 30-50 parts by weight of phospholipid; 80-120 parts by weight of Pu'er tea extract; 10-30 parts by weight of vitamin E; and 25-40 parts by weight of L-carnitine. ### Claim 3 (depends on 2) The pharmaceutical composition of claim 2 comprising 35 parts by weight of silybin; 42 parts by weight of phospholipid; 100 parts by weight of Pu'er tea extract; 16.7 parts by weight of vitamin E; and 33.3 parts by weight of L-carnitine. ### Claim 4 (depends on 1) The pharmaceutical composition according to claim 1, wherein the vitamin E is vitamin E acetate or vitamin E succinate. ### Claim 5 (depends on 1) The pharmaceutical composition according to claim 1, wherein the L-carnitine is L-carnitine tartrate. ### Claim 6 (depends on 1) A pharmaceutical preparation comprising the pharmaceutical composition of claim 1, further comprising pharmaceutically acceptable carriers; wherein the pharmaceutically acceptable carriers are 0.1-99.9% of the total preparation by weight. ### Claim 7 (depends on 6) The pharmaceutical preparation of claim 6, wherein the pharmaceutically acceptable carriers are selected from the group consisting of mannitol, sorbitol, sorbic acid or sylvite, sodium metabisulfite, sodium bisulfite, sodium thiosulfate, cysteine hydrochloride, mercaptoacetic acid, methionine, vitamin A, vitamin C, vitamin E, vitamin D, azone, disodium EDTA, calcium disodium EDTA, hydrochloric acid, acetic acid, sulfuric acid, phosphoric acid, amino acid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivate thereof, alginate, gelatin, polyvinyl pyrrolidone, glycerine, propylene glycol, ethanol, polysorbate 60-80, sorbitan monooleate, beeswax, lanolin, liquid paraffin, cetyl alcohol, gallic acid esters, agar, triethanolamine, basic amino acid, urea, allantoin, calcium carbonate, calcium bicarbonate, surfactant, polyethylene glycol, cyclodextrin, beta-cyclodextrin, phospholipid material, kaolin, talc, calcium stearate, magnesium stearate, and microcrystalline cellulose, and a carbonate, acetate, or phosphate salt of a monovalent alkali metal or aqueous solution thereof. ### Claim 8 (depends on 7) The pharmaceutical preparation of claim 7, wherein the pharmaceutical preparation is are selected from the group consisting of a tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, oral agent, granule, pill, powder, paste, sublimed preparation, supensoid agent, solution, injection, suppository, ointment, emplastrum, creme, spray, and patch. ### Claim 9 (depends on 6) A method of preparing the pharmaceutical preparation according to claim 6, comprising: (1) taking a prescription amount of raw materials for later use; (2) preparing a silybin complex liquid by weighing a prescription amount of silybin and phospholipin, and dissolving them in anhydrous ethanol, heating and refluxing to clarify the solution and continuing to heat for a time, then concentrating the clear solution under reduced pressure to a concentrated volume, to obtain the silybin complex liquid for later use; (3) granulating by weighing a prescription amount of Pu'er tea extract as a base material, taking the silybin complex liquid prepared in step (2) as a feed liquid, and preparing granules by a fluidization spray method with a fluidized bed, and drying after the liquid complex is all sprayed in for later use; (4) achieving total blending by mixing the vitamin E, the L-carnitine and the granules prepared in step (3) uniformly to get the pharmaceutical composition; and (5) combining the pharmaceutical composition and the pharmaceutically acceptable carriers to make a conventional preparation. ### Claim 10 (depends on 9) The method according to claim 9, wherein the heating time in step (2) is 0.5-1.5 hours; the concentrated volume is 5%-20% of the original volume and the temperature of concentration under reduced pressure is 60-80° C.; the parameters of the fluidized bed in step (3) are that the temperature of the materials is 40-65° C., and parameters such as fan frequency, the inlet air temperature and the infusion frequency are adjusted to keep the materials in a good fluidizing state during the granulation process; and wherein after granulation is completed, the granules are dried for 10-60 minutes and the drying temperature is 55-65° C. ### Claim 11 (depends on 1) A method of using the pharmaceutical composition of claim 1 for treating non-alcoholic fatty liver diseases and/or reducing fat, losing weight, and beautifying skin, comprising administering a therapeutically effective amount to a human in need thereof. ### Claim 12 (depends on 2) A pharmaceutical preparation comprising the pharmaceutical composition of claim 2, further comprising pharmaceutically acceptable carriers; wherein the pharmaceutically acceptable carriers are 0.1-99.9% of the total preparation by weight. ### Claim 13 (depends on 12) The pharmaceutical preparation of claim 12, wherein the pharmaceutically acceptable carriers are selected from the group consisting of mannitol, sorbitol, sorbic acid or sylvite, sodium metabisulfite, sodium bisulfite, sodium thiosulfate, cysteine hydrochloride, mercaptoacetic acid, methionine, vitamin A, vitamin C, vitamin E, vitamin D, azone, disodium EDTA, calcium disodium EDTA, hydrochloric acid, acetic acid, sulfuric acid, phosphoric acid, amino acid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivate thereof, alginate, gelatin, polyvinyl pyrrolidone, glycerine, propylene glycol, ethanol, polysorbate 60-80, sorbitan monooleate, beeswax, lanolin, liquid paraffin, cetyl alcohol, gallic acid esters, agar, triethanolamine, basic amino acid, urea, allantoin, calcium carbonate, calcium bicarbonate, surfactant, polyethylene glycol, cyclodextrin, beta-cyclodextrin, phospholipid material, kaolin, talc, calcium stearate, magnesium stearate, and microcrystalline cellulose, and a carbonate, acetate, or phosphate salt of a monovalent alkali metal or aqueous solution thereof. ### Claim 14 (depends on 12) The pharmaceutical preparation of claim 12, wherein the pharmaceutical preparation is selected from the group consisting of a tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, oral agent, granule, pill, powder, paste, sublimed preparation, supensoid agent, solution, injection, suppository, ointment, emplastrum, creme, spray, and patch. ### Claim 15 (depends on 3) A pharmaceutical preparation comprising the pharmaceutical composition of claim 3, further comprising pharmaceutically acceptable carriers; wherein the pharmaceutically acceptable carriers are 0.1-99.9% of the total preparation by weight. ### Claim 16 (depends on 15) The pharmaceutical preparation of claim 15, wherein the pharmaceutically acceptable carriers are selected from the group consisting of mannitol, sorbitol, sorbic acid or sylvite, sodium metabisulfite, sodium bisulfite, sodium thiosulfate, cysteine hydrochloride, mercaptoacetic acid, methionine, vitamin A, vitamin C, vitamin E, vitamin D, azone, disodium EDTA, calcium disodium EDTA hydrochloric acid, acetic acid, sulfuric acid, phosphoric acid, amino acid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivate thereof, alginate, gelatin, polyvinyl pyrrolidone, glycerine, propylene glycol, ethanol, polysorbate 60-80, sorbitan monooleate, beeswax, lanolin, liquid paraffin, cetyl alcohol, gallic acid esters, agar, triethanolamine, basic amino acid, urea, allantoin, calcium carbonate, calcium bicarbonate, surfactant, polyethylene glycol, cyclodextrin, beta-cyclodextrin, phospholipid material, kaolin, talc, calcium stearate, magnesium stearate, and microcrystalline cellulose, and a carbonate, acetate, or phosphate salt of a monovalent alkali metal or aqueous solution thereof. ### Claim 17 (depends on 15) The pharmaceutical preparation of claim 15, wherein the pharmaceutical preparation is selected from the group consisting of a tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, oral agent, granule, pill, powder, paste, sublimed preparation, supensoid agent, solution, injection, suppository, ointment, emplastrum, creme, spray, or patch; preferably, wherein the pharmaceutical preparation is a capsule, granule, and tablet. ### Claim 18 (depends on 12) A method of preparing the pharmaceutical preparation according to claim 12, comprising: (1) taking a prescription amount of raw materials for later use; (2) preparing a silybin complex liquid by weighing a prescription amount of silybin and phospholipin, and dissolving them in anhydrous ethanol, heating and refluxing to clarify the solution and continuing to heat for a time, then concentrating the clear solution under reduced pressure to a concentrated volume, to obtain the silybin complex liquid for later use; (3) granulating by weighing a prescription amount of Pu'er tea extract as a base material, taking the silybin complex liquid prepared in step (2) as a feed liquid, and preparing granules by a fluidization spray method with a fluidized bed, and drying after the liquid complex is all sprayed in for later use; (4) achieving total blending by mixing the vitamin E, the L-carnitine and the granules prepared in step (3) uniformly to get the pharmaceutical composition; and (5) combining the pharmaceutical composition and the pharmaceutically acceptable carriers to make a conventional preparation. ### Claim 19 (depends on 18) The method according to claim 18, wherein the heating time in step (2) is 0.5-1.5 hours; the concentrated volume is 5%-20% of the original volume and the temperature of concentration under reduced pressure is 60-80° C.; the parameters of the fluidized bed in step (3) are that the temperature of the materials is 40-65° C., and parameters such as fan frequency, the inlet air temperature and the infusion frequency are adjusted to keep the materials in a good fluidizing state during the granulation process; and wherein after granulation is completed, the granules are dried for 10-60 minutes and the drying temperature is 55-65° C. ### Claim 20 (depends on 6) A method of using the pharmaceutical preparation of claim 6 for treating non-alcoholic fatty liver diseases and/or reducing fat, losing weight, and beautifying skin, comprising administering a therapeutically effective amount to a human in need thereof.