CN116077540A - Application of Rhus chinensis extract in preparing medicine for treating stomach-related diseases - Google Patents
Application of Rhus chinensis extract in preparing medicine for treating stomach-related diseases Download PDFInfo
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- CN116077540A CN116077540A CN202111315084.4A CN202111315084A CN116077540A CN 116077540 A CN116077540 A CN 116077540A CN 202111315084 A CN202111315084 A CN 202111315084A CN 116077540 A CN116077540 A CN 116077540A
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- Prior art keywords
- extract
- gastric
- rhus chinensis
- ethanol
- related diseases
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- 235000014220 Rhus chinensis Nutrition 0.000 title claims abstract description 43
- 240000003152 Rhus chinensis Species 0.000 title claims abstract description 39
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 12
- 239000003814 drug Substances 0.000 title claims abstract description 12
- 201000010099 disease Diseases 0.000 title claims abstract description 10
- 210000002784 stomach Anatomy 0.000 title description 13
- 230000002496 gastric effect Effects 0.000 claims abstract description 21
- 238000002360 preparation method Methods 0.000 claims abstract description 13
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 29
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- 208000007107 Stomach Ulcer Diseases 0.000 claims description 5
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- 229940079593 drug Drugs 0.000 abstract description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 12
- 230000000694 effects Effects 0.000 description 10
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
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- YREYEVIYCVEVJK-UHFFFAOYSA-N rabeprazole Chemical compound COCCCOC1=CC=NC(CS(=O)C=2NC3=CC=CC=C3N=2)=C1C YREYEVIYCVEVJK-UHFFFAOYSA-N 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
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- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 239000004375 Dextrin Substances 0.000 description 2
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- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 2
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- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
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- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 239000000661 sodium alginate Substances 0.000 description 2
- 235000010413 sodium alginate Nutrition 0.000 description 2
- 229940005550 sodium alginate Drugs 0.000 description 2
- 229940032147 starch Drugs 0.000 description 2
- ZGDLVKWIZHHWIR-UHFFFAOYSA-N 4-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl]morpholine Chemical compound O1C(C)(C)C(C)(C)OB1C1=CC=C(N2CCOCC2)N=C1 ZGDLVKWIZHHWIR-UHFFFAOYSA-N 0.000 description 1
- 241000208223 Anacardiaceae Species 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical compound O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 description 1
- 208000005156 Dehydration Diseases 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 238000002965 ELISA Methods 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000002421 anti-septic effect Effects 0.000 description 1
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- 239000000605 aspartame Substances 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
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- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
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- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
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- 235000003599 food sweetener Nutrition 0.000 description 1
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- 239000011521 glass Substances 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 230000002262 irrigation Effects 0.000 description 1
- 238000003973 irrigation Methods 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
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- 210000004877 mucosa Anatomy 0.000 description 1
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- 230000036407 pain Effects 0.000 description 1
- 229960001412 pentobarbital Drugs 0.000 description 1
- WEXRUCMBJFQVBZ-UHFFFAOYSA-N pentobarbital Chemical compound CCCC(C)C1(CC)C(=O)NC(=O)NC1=O WEXRUCMBJFQVBZ-UHFFFAOYSA-N 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
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- 210000001187 pylorus Anatomy 0.000 description 1
- 229960001778 rabeprazole sodium Drugs 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000010008 shearing Methods 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 229940001584 sodium metabisulfite Drugs 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 229940001474 sodium thiosulfate Drugs 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 239000007779 soft material Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 208000018556 stomach disease Diseases 0.000 description 1
- 230000035882 stress Effects 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 210000002417 xiphoid bone Anatomy 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/22—Anacardiaceae (Sumac family), e.g. smoketree, sumac or poison oak
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/55—Liquid-liquid separation; Phase separation
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medical Informatics (AREA)
- Biotechnology (AREA)
- Alternative & Traditional Medicine (AREA)
- Botany (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention belongs to the technical field of medicines, and discloses application of a Rhus chinensis extract in preparing a medicine for treating gastric related diseases, namely application of the Rhus chinensis extract in preparing a medicine for preventing or treating gastric related diseases and preparation of H + ‑K + -use of an atpase inhibitor.
Description
Technical Field
The invention belongs to the technical field of medicines, and in particular relates to a novel application of a Rhus chinensis extract, namely an application of the Rhus chinensis extract in preparing a medicine for preventing or treating gastric related diseases and H + -K + -use of an atpase inhibitor.
Background
The Rhus chinensis (Rhus chinensis Mill.) is a plant of Rhus genus of Rhus of family Anacardiaceae, and all other provinces except northeast, inner Mongolia and Xinjiang are grown in the forest or bush of sunny hillside, valley, and stream side with altitude of 170-2700 m. Distributed in india, peninsula in the middle south, malaysia, indonesia, japan and korea.
We found in a large number of screening worksThe extract of Rhus chinensis has high gastric H + -K + The extract has obvious protective effect on inflammatory pain and gastric mucosal hemorrhage caused by cold stress, and the extract has effect of promoting ulcer healing on a chronic acetic acid ulcer model, so far no report on the research on curing stomach diseases by Rhus chinensis is seen.
Disclosure of Invention
The technical problem solved by the invention is to provide the application of the Rhus chinensis extract in preparing a medicament for preventing or treating gastric related diseases; in preparation of H + -K + -use of an atpase inhibitor.
In order to solve the technical problems of the invention, the invention provides the following technical scheme:
according to a first aspect of the technical scheme, the invention provides a preparation method of the extract of the Rhus chinensis + -K + -use of an atpase inhibitor.
Further, the stomach-related diseases include gastric mucosal hemorrhage and gastric ulcer.
Further, the gastric mucosal hemorrhage comprises gastric mucosal hemorrhage caused by inflammation and pain and gastric mucosal hemorrhage caused by cold stress.
Further, the preparation method of the Rhus chinensis extract is characterized by comprising the following steps of: extracting with 95% ethanol under reflux for 3 times, mixing filtrates, filtering to remove residues, mixing filtrates, and concentrating under reduced pressure to obtain paste. Then volatilizing the extract, suspending in water, passing through HP-20 macroporous resin, eluting with water, 30%,70% and 95% ethanol respectively, wherein the 95% ethanol eluate is concentrated under reduced pressure to obtain extract.
In a second aspect, the present invention provides a pharmaceutical composition for preparing H + -K + -use of an atpase inhibitor, characterized in that said pharmaceutical composition comprises an extract of sumac according to the first aspect of the invention and a pharmaceutically acceptable carrier or excipient.
The invention also provides application of the pharmaceutical composition in preparing medicines for preventing or treating stomach-related diseases, which is characterized in that the pharmaceutical composition comprises the Rhus chinensis extract of any one of claims 1-7 and a pharmaceutically acceptable carrier or excipient.
The beneficial technical effects are as follows: the application of the Rhus chinensis extract in preparing the medicines for treating gastric ulcer is found for the first time, and is not reported in China.
Detailed Description
The raw medicinal materials are identified as the Chinese sumac by the specimen room of the medical institute of Chinese medical science
EXAMPLE 1 preparation of Rhus chinensis extract
20 kg of Rhus chinensis root is extracted with 95% ethanol under reflux for three times, each time for one hour, and the extractive solution is concentrated under reduced pressure to obtain 2.1kg of extract. Then, the mixture is suspended in water, and is eluted by 5 column volumes of water, 30 percent, 70 percent and 95 percent ethanol respectively through HP-20 macroporous resin, wherein the 95 percent ethanol eluted part is decompressed and concentrated to obtain extractum.
Pharmacological experiments:
experimental example 1 Rhus chinensis extract pair H + -K + Influence of ATPase Activity
The method comprises the following steps: 96-well plates were used, and the blank and control were each 20ul, with 1.0mg/ml of the extract of Rhus chinensis, 10-3mol/L and 10-4mol/L of sodium rabeprazole. Adding pig H diluted 20 times with the reaction solution + -K + 160ul of ATPase, incubated for 20 minutes at 37℃with 20mg/ml ATP and no ATP in the blank. The reaction was carried out at 37℃for 30 minutes. The reaction was stopped by adding 50ul of 10% TCA. 20mg/ml ATP was added to the blank at 20ul. 50 μl of the mixture is placed in a 96-well ELISA plate, 200ul of phosphorus determination solution is added for color reaction, and color comparison is carried out at 660 nm. Inhibition was calculated as = (control-sample)/(control-blank) ×100%.
Results: rhus chinensis extract for treating pig stomach H + -K + The ATPase activities have stronger inhibition effect, and the inhibition rates of 100ug/ml are 58% respectively. Rabeprazole sodium 10 -4 mol/L and 10 -5 The mol/L inhibition was 72% and 57%, respectively.
Experimental example 2 influence of Rhus chinensis extract on rat anti-inflammatory pain type gastric ulcer model
The method is to take male wistar rats and fasted for 48 hours. The animals were randomly divided into control groups, pantoprazole sodium group and Rhus chinensis extract group, 5 animals each. The administration by gastric lavage is 10ml/kg. The control group was given vehicle, pantoprazole sodium was given by gavage at 5mg/kg and the extract of Rhus chinensis was given by gavage at 50mg/kg. The anti-inflammatory pain is injected into the abdominal cavity for 40mg/kg after 0.5 hour, the cervical vertebra is removed after 6.0 hours, the rat is sacrificed, the stomach is taken out and injected with 10ml of water, the water is fixed in 3% formaldehyde solution, and the number of bleeding points of the mucous membrane part is counted. Significance testing was performed using the t-program.
As a result, after the extract of the Rhus chinensis is administrated in advance, the bleeding point of the gastric mucosa caused by the indomethacin can be obviously reduced, the extract of the Rhus chinensis has obvious protection effect on the bleeding of the gastric mucosa caused by the indomethacin, and the inhibition rate is 70%. The inhibition rate of pantoprazole sodium at the dose used was 95%.
Experimental example 3 Effect of Rhus chinensis extract on rat Water stress restraint ulcer model
The method comprises the following steps: male wistar rats were fasted for 48 hours. The animals were randomly divided into control groups, pantoprazole sodium group and Rhus chinensis extract group, 5 animals each. The administration by gastric lavage is 10ml/kg. The control group was given a vehicle for gavage, pantoprazole sodium was given 5mg/kg for gavage, and 50 or 100mg/kg of the extract of Rhus chinensis was given for gavage. After 0.5 hours, the rats were placed in custom stress cages and placed in a 16 ℃ water bath with water up to the xiphoid process of the rats. Animals were sacrificed after 6 hours. Taking out stomach, injecting 10ml water, fixing in 3% formaldehyde solution, shearing to promote appetite, and counting ulcer number of mucosa.
Results 1: after the extract of the Chinese sumac is administrated by stomach irrigation in advance, the gastric mucosa bleeding point caused by cold stress can be reduced, and 50mg/kg of the extract of the Chinese sumac has better protection effect on the gastric mucosa bleeding caused by cold stress, and the inhibition rate is 51%. The inhibition rate of pantoprazole sodium at the dose used was 100%.
Results 2: after the extract of the Chinese sumac is administrated by stomach infusion in advance, the gastric mucosa bleeding point caused by cold stress can be obviously reduced, the 100mg/kg extract of the Chinese sumac has a good protection effect on the gastric mucosa bleeding caused by cold stress, the inhibition rate is 77%, and the P is less than 0.01. The inhibition rate of pantoprazole sodium at the dose used was 68%.
Experimental example 4 influence on the model of chronic acetic acid type ulcer in rats
The method comprises the following steps: rats were fasted for 24 hours, anesthetized with sodium pentobarbital, the abdominal cavity was opened, the stomach was gently flattened, the adenostomach was injected with 20 μl of 30% acetic acid on the pylorus side, and the abdominal cavity was closed. Animals were randomly grouped. The administration was started the next day after the operation, the dose of the Rhus chinensis extract was 500mg/kg, the sodium rabeprazole was 100mg/kg and the vehicle was administered as a control. Once daily for 10 consecutive days. Rats were fasted for 24 hours after the last dose, animals were sacrificed the next day, and the stomach was removed, infused with 10ml of water, and fixed in 3% formaldehyde solution. After 30 minutes, the stomach was cut and apped along the greater curvature, the stomach was flattened on a glass plate, photographed with a digital camera, the image was processed with spot advanced software, and the ulcer area was determined.
Results: the ulcerated area of the rats given 500mg/kg of the Rhus chinensis extract was reduced by 29.7%. The ulcer area of the sodium rabeprazole with the concentration of 100mg/kg is reduced by 33.0 percent. Showing that the Rhus chinensis extract has the effect of promoting ulcer healing on chronic acetic acid ulcer model.
Preparation of the formulation
The extract or extract powder prepared in the examples 1 and 2 is added with relevant auxiliary materials to prepare medicinal granules, powder, capsules, tablets, oral liquid and other dosage forms.
1. Granule preparation
Comprises soluble granule and block agent, mixing the dry powder obtained by the first and second methods with proper amount of excipient (such as dextrin, starch, microcrystalline cellulose, alginic acid, sodium alginate, carboxymethyl starch, low substituted hydroxypropyl cellulose, etc.), drying to obtain granule, and packaging with moisture-proof packaging material (such as thick plastic, aluminum foil, etc.). Or wet granulating the extract with excipient, drying, and tabletting.
2. Capsule preparation
Adding appropriate amount of adjuvants (selected from calcium carbonate, mannitol, magnesium carbonate, magnesium oxide, micropowder silica gel, etc.), appropriate amount of lubricant (selected from pulvis Talci, magnesium stearate, glycol ester, polysilicone, etc.), appropriate amount of binder (selected from mineral oil, edible oil, etc.), mixing to obtain dry powder or granule, and making into capsule. Or making soft material with excipient (polyethylene glycol, oil, etc.), filling into bags by pump pressure method, and packaging in sealed aluminum plastic package.
3. Tablet formulation
Including plain tablets, film coated tablets, and the like. The dry powder or extract obtained by the first and second methods is added with a proper amount of diluent (selected from dextrin, starch, microcrystalline cellulose, mannitol and the like), a proper amount of binder (selected from water, ethanol, starch slurry, cellulose and the like), a proper amount of disintegrating agent (selected from starch, alginic acid, sodium alginate, carboxymethyl starch, low-substituted hydroxypropyl cellulose and the like), a proper amount of lubricant (selected from talcum powder, magnesium stearate, polyethylene glycol and the like), and the dry powder or the dry powder is granulated and tabletted. If the film-coated tablet is coated, the film-forming material (cellulose, polyethylenglycol, etc.) can be used for conventional coating, and the coated tablet is packaged into a closed bottle or an aluminum-plastic plate.
4. Oral liquid
The preparation method comprises preparing soluble oral liquid by conventional method, dissolving the dry powder or extract obtained by the first and second methods in water or ethanol, adding stabilizer (selected from disodium edetate, sodium metabisulfite, sodium thiosulfate, VC derivative, etc.) or antiseptic (selected from benzoic acid, parabens, sorbic acid, etc.), and packaging in sealed bottles.
5. Powder preparation
The above dosage forms can be added with appropriate amount of sweetener such as D-xylose, xylitol, maltitol, steviosin, aspartame, etc.
Claims (10)
1. Preparation of Rhus chinensis extract in H + -K + -use of an atpase inhibitor.
2. Application of Rhus chinensis extract in preparing medicine for preventing or treating gastric related diseases is provided.
3. The use according to claim 2, wherein said gastric related disorder comprises gastric mucosal hemorrhage, gastric ulcer, reflux esophagitis.
4. The use according to claim 3, wherein said gastric mucosal hemorrhage comprises a gastric mucosal hemorrhage due to indomethacin, a gastric mucosal hemorrhage due to cold stress.
5. The use according to any one of claims 1 to 4, characterized in that the preparation method of the extract of sumac comprises: extracting Rhus chinensis with solvent under reflux for 3 times, mixing filtrates, filtering to remove residues, and concentrating the filtrate under reduced pressure to obtain paste. Then suspending in water, passing through HP-20 macroporous resin, eluting with water, 30% ethanol, 70% ethanol, and 95% ethanol respectively, wherein the 95% ethanol eluate is concentrated under reduced pressure to obtain extract.
6. The method according to claim 5, wherein the solvent is selected from the group consisting of mixed solutions of water and alcohol in different proportions.
7. The method according to claim 6, wherein the alcohol is methanol, ethanol, isopropanol, butanol or a mixture thereof.
8. A pharmaceutical composition for preparing H + -K + -use of an atpase inhibitor, characterized in that said pharmaceutical composition comprises an extract of sumac according to any of claims 1-7 and a pharmaceutically acceptable carrier or excipient.
9. Use of a pharmaceutical composition comprising the extract of sumac according to any of claims 1-7 and a pharmaceutically acceptable carrier or excipient for the preparation of a medicament for the prevention or treatment of gastric related diseases.
10. The use according to claim 9, wherein said gastric related disorder comprises gastric mucosal hemorrhage, gastric ulcer, reflux esophagitis.
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| CN101152445A (en) * | 2006-09-26 | 2008-04-02 | 韦英杰 | Medicament composition for treating peptic ulcer |
| CN109045087A (en) * | 2018-09-25 | 2018-12-21 | 福建中医药大学 | A kind of enriching and purifying technique of Chinese sumac active component |
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| CN112494526A (en) * | 2020-12-25 | 2021-03-16 | 大理大学 | Rhus chinensis extract, and preparation method and application of pharmaceutical composition thereof |
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2021
- 2021-11-08 CN CN202111315084.4A patent/CN116077540B/en active Active
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| CN101152445A (en) * | 2006-09-26 | 2008-04-02 | 韦英杰 | Medicament composition for treating peptic ulcer |
| CN109045087A (en) * | 2018-09-25 | 2018-12-21 | 福建中医药大学 | A kind of enriching and purifying technique of Chinese sumac active component |
| CN112194698A (en) * | 2019-07-08 | 2021-01-08 | 福建中医药大学 | Triterpenoid compound and preparation method and application thereof |
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