WO2020221184A1 - Composition pharmaceutique ayant pour effet de réduire l'acide urique - Google Patents
Composition pharmaceutique ayant pour effet de réduire l'acide urique Download PDFInfo
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- WO2020221184A1 WO2020221184A1 PCT/CN2020/087128 CN2020087128W WO2020221184A1 WO 2020221184 A1 WO2020221184 A1 WO 2020221184A1 CN 2020087128 W CN2020087128 W CN 2020087128W WO 2020221184 A1 WO2020221184 A1 WO 2020221184A1
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- WIPO (PCT)
- Prior art keywords
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- weight
- pharmaceutical composition
- inulin
- citric acid
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 36
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 title claims abstract description 27
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 title claims abstract description 24
- 229940116269 uric acid Drugs 0.000 title claims abstract description 24
- 230000000694 effects Effects 0.000 title claims abstract description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims abstract description 105
- 229920001202 Inulin Polymers 0.000 claims abstract description 51
- JYJIGFIDKWBXDU-MNNPPOADSA-N inulin Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)OC[C@]1(OC[C@]2(OC[C@]3(OC[C@]4(OC[C@]5(OC[C@]6(OC[C@]7(OC[C@]8(OC[C@]9(OC[C@]%10(OC[C@]%11(OC[C@]%12(OC[C@]%13(OC[C@]%14(OC[C@]%15(OC[C@]%16(OC[C@]%17(OC[C@]%18(OC[C@]%19(OC[C@]%20(OC[C@]%21(OC[C@]%22(OC[C@]%23(OC[C@]%24(OC[C@]%25(OC[C@]%26(OC[C@]%27(OC[C@]%28(OC[C@]%29(OC[C@]%30(OC[C@]%31(OC[C@]%32(OC[C@]%33(OC[C@]%34(OC[C@]%35(OC[C@]%36(O[C@@H]%37[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O%37)O)[C@H]([C@H](O)[C@@H](CO)O%36)O)[C@H]([C@H](O)[C@@H](CO)O%35)O)[C@H]([C@H](O)[C@@H](CO)O%34)O)[C@H]([C@H](O)[C@@H](CO)O%33)O)[C@H]([C@H](O)[C@@H](CO)O%32)O)[C@H]([C@H](O)[C@@H](CO)O%31)O)[C@H]([C@H](O)[C@@H](CO)O%30)O)[C@H]([C@H](O)[C@@H](CO)O%29)O)[C@H]([C@H](O)[C@@H](CO)O%28)O)[C@H]([C@H](O)[C@@H](CO)O%27)O)[C@H]([C@H](O)[C@@H](CO)O%26)O)[C@H]([C@H](O)[C@@H](CO)O%25)O)[C@H]([C@H](O)[C@@H](CO)O%24)O)[C@H]([C@H](O)[C@@H](CO)O%23)O)[C@H]([C@H](O)[C@@H](CO)O%22)O)[C@H]([C@H](O)[C@@H](CO)O%21)O)[C@H]([C@H](O)[C@@H](CO)O%20)O)[C@H]([C@H](O)[C@@H](CO)O%19)O)[C@H]([C@H](O)[C@@H](CO)O%18)O)[C@H]([C@H](O)[C@@H](CO)O%17)O)[C@H]([C@H](O)[C@@H](CO)O%16)O)[C@H]([C@H](O)[C@@H](CO)O%15)O)[C@H]([C@H](O)[C@@H](CO)O%14)O)[C@H]([C@H](O)[C@@H](CO)O%13)O)[C@H]([C@H](O)[C@@H](CO)O%12)O)[C@H]([C@H](O)[C@@H](CO)O%11)O)[C@H]([C@H](O)[C@@H](CO)O%10)O)[C@H]([C@H](O)[C@@H](CO)O9)O)[C@H]([C@H](O)[C@@H](CO)O8)O)[C@H]([C@H](O)[C@@H](CO)O7)O)[C@H]([C@H](O)[C@@H](CO)O6)O)[C@H]([C@H](O)[C@@H](CO)O5)O)[C@H]([C@H](O)[C@@H](CO)O4)O)[C@H]([C@H](O)[C@@H](CO)O3)O)[C@H]([C@H](O)[C@@H](CO)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 JYJIGFIDKWBXDU-MNNPPOADSA-N 0.000 claims abstract description 51
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Classifications
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- A—HUMAN NECESSITIES
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-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Definitions
- the invention belongs to the technical field of biomedicine, and specifically contains a pharmaceutical composition with uric acid lowering and anti-fatigue effects.
- the essential cause of gout is the increase in the level of uric acid in the body, which causes the deposition of urate in the joints and kidneys.
- the main causes of gout include but are not limited to: (1) dietary reasons. After eating too much meat and seafood, and drinking too much beer, the body's uric acid level increases, which may cause urate deposition; (2) Obesity. The consequence of obesity is the increase of uric acid in the body, and the kidneys cannot completely remove the excess uric acid; (3) Taking certain drugs. These drugs can increase the level of uric acid in the body; (4) Family history. If your family member suffers from gout, the probability of your illness will also increase greatly.
- Gout is a common and complex type of arthritis, which can be affected by all ages.
- the incidence rate of men is higher than that of women.
- Gout patients often experience sudden joint pain at night, the onset is acute, severe pain, edema, redness, and inflammation appear in the joints. The pain is slowly reduced until it disappears, lasting several days or weeks. When the pain occurs, the patient wakes up in the middle of the night while sleeping.
- Some patients describe the pain as similar to the burning of the big toe.
- the most common joint is the big toe (medical term: first metatarsal), but the joints that are affected are not limited to this, and are also common in hand joints, knees, elbows, etc.
- the affected joints will eventually become red, swollen and inflamed. After the edema, the tissues will become soft and movement will be restricted, which will eventually affect daily life. Therefore, research on new products that can reduce uric acid has important clinical significance.
- the applicant obtained a new pharmaceutical composition after many creative researches, which is prepared from inulin, sodium citrate, potassium citrate and citric acid.
- the research shows that the present invention
- the composition has the pharmacological effect of lowering uric acid, which further illustrates that the composition of the present invention can be used for gout patients.
- the special medical food mentioned in the present invention means that it must be consumed alone or in combination with other foods under the guidance of a doctor or clinical nutritionist. It refers to a formula food specially processed and formulated to meet the special needs of people with eating restrictions, digestion and absorption disorders, metabolic disorders or specific disease states for nutrients or diet. Special medical foods are not medicines, but they are not ordinary foods eaten by normal people. They are formula foods specially developed and produced after extensive medical research by clinicians and nutritionists and based on scientific objective facts. When the target population cannot eat ordinary meals or cannot meet their nutritional needs with daily meals, formula foods for special medical purposes can be used as a way of nutritional supplementation to play a nutritional support role. The food cannot replace the therapeutic effect of drugs, and the product cannot claim the preventive and therapeutic functions of diseases.
- the inulin in the present invention refers to inulin or natural fructan, which uses Jerusalem artichoke (Jerusalem artichoke) rhizome or chicory as raw material to remove protein, gum, crude fiber and minerals, and is extracted with water and ion exchanged. , Membrane filtration, spray drying and other production processes to obtain inulin.
- the present invention is achieved through the following technical solutions.
- Said pharmaceutical composition comprises 15-20 parts by weight of inulin, 10-15 parts by weight of sodium citrate, 10-15 parts by weight of potassium citrate and 1-5 parts by weight of citric acid.
- Said pharmaceutical composition comprises 18 parts by weight of inulin, 14 parts by weight of potassium citrate, 12 parts by weight of sodium citrate and 4 parts by weight of citric acid.
- the pharmaceutical composition is applied in the preparation of special medical food for lowering uric acid.
- a pharmaceutical composition for treating gout which is prepared from the following raw materials: 15-20 parts by weight of inulin, 10-15 parts by weight of sodium citrate, 10-15 parts by weight of potassium citrate, and citric acid 1-5 parts by weight; the preferred pharmaceutical composition is prepared from the following raw materials: 18 parts by weight of inulin, 14 parts by weight of potassium citrate, 12 parts by weight of sodium citrate and 4 parts by weight of citric acid.
- a pharmaceutical composition with the effect of lowering uric acid which is prepared from the following raw materials: 15-20 parts by weight of inulin, 10-15 parts by weight of sodium citrate, 10-15 parts by weight of potassium citrate and lemon The acid is 1-5 parts by weight; the preferred pharmaceutical composition is prepared from the following raw materials: 18 parts by weight of inulin, 14 parts by weight of potassium citrate, 12 parts by weight of sodium citrate and 4 parts by weight of citric acid.
- the inulin in the present invention refers to inulin or natural fructan, which uses Jerusalem artichoke (Jerusalem artichoke) rhizome or chicory as raw material to remove protein, gum, crude fiber and minerals, and is extracted with water and ion exchanged. , Membrane filtration, spray drying and other production processes to obtain inulin.
- the inulin of the present invention has the following pharmacological effects: 1. Control blood lipids; 2. Lower blood sugar; 3. Promote the absorption of minerals; 4. Adjust the intestinal microflora, improve intestinal health, and prevent constipation; 5. . Inhibit the production of toxic fermentation products, protect the liver, and prevent colon cancer; 6. Prevent constipation and treat obesity. Dietary fiber reduces the residence time of food in the gastrointestinal tract and increases the amount of feces to effectively treat constipation. Its weight loss effect is to increase the viscosity of the contents and reduce the speed of food from the stomach to the small intestine, thereby reducing hunger and reducing food intake. 7. Inulin contains a small amount of 2-9 oligofructose.
- inulin can increase the expression of neurotrophic factors in brain nerve cells, and has a good protective effect on corticosterone-induced neuronal damage. Antidepressant effect. After the composition of inulin and citric acid, sodium citrate and potassium citrate three substances, by regulating intestinal function, etc., thereby promoting the excretion of intestinal uric acid, it has a good effect of lowering uric acid.
- the pharmaceutical composition of the present invention can be prepared into oral solid preparations, or can be prepared into granules by adding other raw and auxiliary materials.
- the pharmaceutical composition of the present invention can also be prepared by adding one or more of sorbitol, isomaltulose (palatinose, sucrose), nutritional fortifier premix, and sucralose Into composite powder.
- the nutritional supplement premix includes the following components by weight: 130-140 parts of taurine, 220-230 parts of vitamin C, 10-20 parts of vitamin E, 0.5-1 parts of ⁇ -carotene, vitamin B 2 2- 3 parts vitamin B 6 1-2 parts, 5-10 parts of pantothenic acid, folic acid, 0.05 to 2 parts.
- Preferred dietary supplement premix parts by weight of component comprising: 140 parts of taurine, 225 parts of vitamin C, vitamin E 18 parts, 0.6 parts of [beta] -carotene, vitamin B 2 2.2 parts of Vitamin B 6 1.81 parts , 8 parts of pantothenic acid, 0.06 parts of folic acid.
- the sources of the raw and auxiliary materials of the present invention are shown in Table 1.
- the present invention is based on inulin, supplemented by sodium citrate, potassium citrate and citric acid. It is used for gout patients and it is used under the guidance of clinicians or nutritionists, rather than ordinary food; On the basis of inulin, sodium citrate, potassium citrate and citric acid, you can also add sorbitol, isomaltulose (palatinose, sucrose), nutritional fortifier premix, three One or more of sucralose.
- the following experiments of the present invention are conclusive experiments by research and development personnel based on the technical solutions to be protected by the present invention on the basis of multiple creative experiments.
- the quantitative experiments in the following examples are all set to three repeated experiments, and the data is the average value of the three repeated experiments or the average ⁇ standard deviation.
- test group
- Test group 1 inulin
- Test group 2 Inulin 1.8g, sodium citrate 2.6g;
- Test group 3 Inulin 1.8g, potassium citrate 2.6g;
- Test group 4 Inulin 1.8g, sodium malate 1.73g;
- Test group 5 inulin 1.8g, sodium bicarbonate 0.74g;
- Test 7 inulin 1.8g, potassium citrate 1.5g, and citric acid 1.5g.
- Test 8 group inulin 1.8g, potassium citrate 1.4g, sodium citrate 1.2g and citric acid 0.4g.
- Test method Kunming mice, male, weighing 18-22g, randomly grouped, blank control group, model group, test group, 10 mice in each group, except for mice in the blank group, the other groups are given potassium oxazinate every morning (100mg/kg) model, the present group was given 4g/kg of raw material every afternoon, and the model group was given the same volume of distilled water in the afternoon. Each group was administered once a day for a total of 30 days, and relevant indicators were tested on 30 days during the administration period. Index detection: Fasting for 12 hours (cannot help water) before the start of the formal experiment, and taking 1 mL of blood from the orbit before administration.
- centrifuge 4000r/min, 15min to separate the serum and store it at -20°C for standby. Used to detect the serum UA level before the experiment. On the 30th day after the administration, the blood was collected by the same method, except for the UA level after 30 days.
- Test group 1 Inulin 1.8g, potassium citrate 1.4g, sodium citrate 1.2g and citric acid 0.4g.
- Test group 2 Inulin 1.8g, potassium citrate 1.4g, sodium citrate 1.2g and citric acid 0.6g.
- Test group 4 Inulin 1.8g, potassium citrate 1.4g, sodium citrate 1.2g and citric acid 1.0g.
- Test method same as test 1.
- Sorbitol 3000g inulin 1500g, isomaltulose 1000g, potassium citrate 1000g, sodium citrate 1000g, citric acid 100g, nutrition enhancer premix 50g, sucralose 10g.
- the above-mentioned raw materials are mixed completely.
- the above-mentioned raw materials are mixed completely.
- the above raw materials are mixed together.
- the ratio between fortifier premix as a raw material 140 parts of taurine, 225 parts of vitamin C, vitamin E 18 parts, 0.6 parts of [beta] -carotene, vitamin B 2 2.2 parts of Vitamin B 6 1.81 Parts, 8 parts of pantothenic acid, 0.06 parts of folic acid.
- the inulin in the present invention refers to inulin or natural fructan, which uses Jerusalem artichoke (Jerusalem artichoke) rhizome or chicory as raw material to remove protein, gum, crude fiber and minerals, and is extracted with water and ion exchanged. , Membrane filtration, spray drying and other production processes to obtain inulin.
- the pharmaceutical composition of the present invention can be prepared into oral solid preparations, or can be prepared into granules by adding other raw and auxiliary materials.
- composition of the present invention can be used alone to treat or prevent the onset of gout, or it can be combined with drugs for the treatment of gout, such as febuxostat, colchicine, and allopurin. Alcohol, benzbromarone and other drugs.
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Abstract
L'invention concerne une composition pharmaceutique ayant pour effet de réduire l'acide urique. La composition pharmaceutique est constituée d'inuline, de citrate de sodium, de citrate de potassium et d'acide citrique et peut être utilisée pour des patients atteints de goutte.
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CN110651862A (zh) * | 2019-11-21 | 2020-01-07 | 李海齐 | 一种能够促进喝茶后降低尿酸的口服固体饮料及其制备方法 |
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