CN1799616A - Gastric ulcer treatment medicine, its preparation process and application - Google Patents

Gastric ulcer treatment medicine, its preparation process and application Download PDF

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Publication number
CN1799616A
CN1799616A CN 200510037406 CN200510037406A CN1799616A CN 1799616 A CN1799616 A CN 1799616A CN 200510037406 CN200510037406 CN 200510037406 CN 200510037406 A CN200510037406 A CN 200510037406A CN 1799616 A CN1799616 A CN 1799616A
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rhizoma alpiniae
alpiniae officinarum
extract
ethanol
centrifugal
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CN100358572C (en
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冯毅凡
蔡健聪
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SHENZHEN DONGFANG TAIGE BIOPHARMACEUTICAL CO Ltd
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SHENZHEN DONGFANG TAIGE BIOPHARMACEUTICAL CO Ltd
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Abstract

The invention relates to a composition for treating gastric ulcer and process for preparation, wherein the composition is prepared from turmerone extract through removing lipophilic constituents through hypercritical extraction methods, extracting hydrophilic significant positions, and refining the significant positions through alcohol dissolving and water settling method.

Description

A kind of medicine for the treatment of gastric ulcer and preparation method thereof and application
Technical field
The present invention relates to tcm field, be specifically related to a kind of Chinese patent medicine that is used for the treatment of gastric ulcer, the invention still further relates to the preparation method and the application of this medicine.
Background technology
Along with the arriving of modern society, rhythm of life is nervous all the more, be that the gastrointestinal disease of main disease is also just seen showed increased more with gastric ulcer, and analgesic effect is definite, taking convenience, and medicine that have no side effect or few side effects is people's demand especially.The western medical treatment of gastric ulcer, it is main being mainly symptomatic treatment, adopts the gastrointestinal antispasmodic medicine more, though its effect is also often brought more untoward reaction and side effect to the patient rapidly with certain, also can only be to take stopgap measures and can not effect a permanent cure simultaneously.Chinese medicine then can remedy the deficiency of this respect, and not only toxic and side effects is little, and can treating both the principal and secondary aspects of a disease.
Summary of the invention
The objective of the invention is to overcome existing gastric ulcer treatment and go up the problem that exists, the pure Chinese medicine medicine of a kind of side effect treatment gastric ulcer little, evident in efficacy is provided.
Another object of the present invention provides manufacturing method for above mentioned medicine.
Further purpose of the present invention provides said medicine is used for the medicine of anti-peptic ulcer, antiinflammatory, analgesia, promotion gastrointestinal function in preparation application.
It is the understanding and the Therapeutic Principle of master's cold syndrome of the stomach pain to gastric ulcer that solution of the present invention is based on motherland's medical science, achieve with reference to modern pharmacological research, on the basis of having consulted a large amount of ancient literatures and modern Chinese medicine research data, from motherland's medicine treasure-house, selected to have warming stomach for dispelling cold, analgesic Chinese medicine Rhizoma Alpiniae Officinarum helps digestion, the extraction and separation technology of employing science, extract the effective site in the Chinese crude drug (Rhizoma Alpiniae Officinarum) to greatest extent, make pure Chinese medicinal preparation, the treatment gastric ulcer has good effect.
A kind of medicine for the treatment of gastric ulcer, be Rhizoma Alpiniae Officinarum extract, mainly be the Rhizoma Alpiniae Officinarum flavone extract, the Rhizoma Alpiniae Officinarum flavone extract also contains compositions such as galangin-3-methyl ether, kaempferol, nimbecetin, Quercetin, Quercetin-3-methyl ether, isorhamnetin in addition based on galangin.Content of total flavone is between 10~100% in the Rhizoma Alpiniae Officinarum flavone extract.
Described Rhizoma Alpiniae Officinarum extract is to be prepared from by following steps:
(1) Rhizoma Alpiniae Officinarum is cleaned up;
(2) Rhizoma Alpiniae Officinarum is dried down at 40~60 ℃;
(3) Rhizoma Alpiniae Officinarum powder after will drying is broken to 10~60 orders;
(4) Rhizoma Alpiniae Officinarum after will pulverizing in 60~90 ℃ of reflux, extract,, extracts each 1~2.5 hour with 60%~90% ethanol 2~3 times; Merge alcohol extract, decompression recycling ethanol is 25%~50% to containing the alcohol amount, places centrifugal, collecting precipitation; It is 1~1.3 (70 ℃) that solution further is concentrated into the solution relative density; The precipitation of collecting before being incorporated in; Place, centrifugal, collecting precipitation, drying gets dry extract.
(5) get dried cream, add the ethanol of 4~8 times of volumes 60%~95%, in 50~60 ℃ of water-bath dissolvings, filtered while hot; Filtrate adds water, makes ethanol content reduce to 20%~40%; Leave standstill, centrifugal, get precipitation and be high good extract.
Wherein, in the Rhizoma Alpiniae Officinarum flavone extract content of galangin between 5~90%.
The preparation method of the medicinal tablet of above-mentioned treatment gastric ulcer may further comprise the steps:
(1) Rhizoma Alpiniae Officinarum is cleaned up;
(2) Rhizoma Alpiniae Officinarum is dried down at 40~60 ℃;
(3) Rhizoma Alpiniae Officinarum powder after will drying is broken to 60 order fine powders;
(4) Rhizoma Alpiniae Officinarum after will pulverizing adopts the supercritical carbon dioxide extraction device to extract and removes low-polarity component, and the medicinal residues after supercritical extraction, the ethanol with 70%~90% extract each 1.5~2.5 hours 2~3 times in 60~90 ℃ of reflux, extract; Merge alcohol extract, decompression recycling ethanol is 25%~50% to containing the alcohol amount, places centrifugal, collecting precipitation; It is 1.1~1.3 (70 ℃) that solution further is concentrated into solution density, the precipitation of collecting before being incorporated in; Place, centrifugal, collecting precipitation, drying gets dry extract;
(5) get dried cream, add the ethanol of 4~8 times of volumes 70%~95%, in 50~60 ℃ of water-bath dissolvings, filtered while hot; Filtrate adds water, makes ethanol content reduce to 30%~40%; Leave standstill, centrifugal, get precipitate Rhizoma Alpiniae Officinarum extract;
(6) get Rhizoma Alpiniae Officinarum extract, add adjuvant, tabletting, the bag film-coat, promptly.
The described adjuvant of above-mentioned steps (6) is that starch, carboxymethyl starch are received, magnesium stearate.
The ethanol of above-mentioned percentage ratio is percent by volume ethanol.
The medicine of above-mentioned treatment gastric ulcer is evident in efficacy in the medicine of anti-peptic ulcer, antiinflammatory, analgesia, promotion gastrointestinal function; The medicine that is used for anti-peptic ulcer, antiinflammatory, analgesia, promotion gastrointestinal function in preparation has important use.Can be prepared into said dosage form on any pharmaceutics.
The present invention compared with prior art has the following advantages: 1, adopt scientific and reasonable method to extract the effective site of medical material, at first remove with function and cure mainly irrelevant low-polarity component with supercritical extraction, extract the hydrophilic effective site in the medicinal residues then, and further adopt pure molten water precipitating method refining according to the character of effective site.Finally obtain highly refined effective site.2, component of the present invention is few, and preparation technology is very simple; 3, experimental result shows that anti-peptic ulcer, antiinflammatory, analgesia, promotion gastrointestinal function effect are remarkable.
The specific embodiment
The present invention is described further below in conjunction with specific embodiment.
Embodiment 1: the preparation of medicinal tablet
With clear water the 12.5kg Rhizoma Alpiniae Officinarum is cleaned up, the Rhizoma Alpiniae Officinarum after cleaning in 50 ℃ of oven dry down of low temperature state, is broken to 60 order fine powders with the Rhizoma Alpiniae Officinarum powder after the oven dry.Rhizoma Alpiniae Officinarum after the pulverizing in 70 ℃ of reflux, extract,, extracts each 2 hours with 85% ethanol 2 times.Merge alcohol extract, decompression recycling ethanol is 38% to containing the alcohol amount, places centrifugal, collecting precipitation.It is 1.1 (70 ℃) that solution further is concentrated into the solution relative density.The precipitation of collecting before being incorporated in.Place, centrifugal, collecting precipitation, drying gets dry extract.Get the dried cream of Rhizoma Alpiniae Officinarum total flavones, add 90% ethanol 2500mL, in 55 ℃ of water-bath dissolvings, filtered while hot.Filtrate adds water, makes ethanol content reduce to 30%.Leave standstill, centrifugal, get precipitate Rhizoma Alpiniae Officinarum yellow powder extract.Get Rhizoma Alpiniae Officinarum flavone extract 375g, add starch 100g, carboxymethyl starch and receive 25g, magnesium stearate 5g, tabletting, the bag film-coat, promptly.
Embodiment 2: the preparation of medicinal tablet
With clear water the 12.5kg Rhizoma Alpiniae Officinarum is cleaned up, the Rhizoma Alpiniae Officinarum after cleaning in 45 ℃ of oven dry down of low temperature state, is broken to 60 order fine powders with the Rhizoma Alpiniae Officinarum powder after the oven dry.Rhizoma Alpiniae Officinarum after the pulverizing in 80 ℃ of reflux, extract,, extracts each 2.5 hours with 80% ethanol 2 times.Merge alcohol extract, decompression recycling ethanol is 50% to containing the alcohol amount, places centrifugal, collecting precipitation.It is 1.3 (70 ℃) that solution further is concentrated into solution density.The precipitation of collecting before being incorporated in.Place, centrifugal, collecting precipitation, drying gets dry extract.Get the dried cream of Rhizoma Alpiniae Officinarum total flavones, add 90% ethanol 2750mL, in 60 ℃ of water-bath dissolvings, filtered while hot.Filtrate adds water, makes ethanol content reduce to 35%.Leave standstill, centrifugal, get precipitate Rhizoma Alpiniae Officinarum yellow powder extract.Get Rhizoma Alpiniae Officinarum flavone extract 375g, add starch 100g, carboxymethyl starch and receive 25g, magnesium stearate 5g, tabletting, the bag film-coat, promptly.
Embodiment 3: the preparation of medicinal tablet
With clear water the 12.5kg Rhizoma Alpiniae Officinarum is cleaned up, the Rhizoma Alpiniae Officinarum after cleaning in 50 ℃ of oven dry down of low temperature state, is broken to 60 order fine powders with the Rhizoma Alpiniae Officinarum powder after the oven dry.Rhizoma Alpiniae Officinarum after the pulverizing adopts the supercritical carbon dioxide extraction device to extract and removes low-polarity component.Medicinal residues after supercritical extraction, the ethanol with 78% extract each 1.5 hours 3 times in 75 ℃ of reflux, extract.Merge alcohol extract, decompression recycling ethanol is 45% to containing the alcohol amount, places centrifugal, collecting precipitation.It is 1.2 (70 ℃) that solution further is concentrated into solution density.The precipitation of collecting before being incorporated in.Place, centrifugal, collecting precipitation, drying gets dry extract.Get the dried cream of Rhizoma Alpiniae Officinarum total flavones, add 90% ethanol 3000mL, in 55 ℃ of water-bath dissolvings, filtered while hot.Filtrate adds water, makes ethanol content reduce to 35%.Leave standstill, centrifugal, get precipitate Rhizoma Alpiniae Officinarum yellow powder extract.Get Rhizoma Alpiniae Officinarum flavone extract 375g, add starch 100g, carboxymethyl starch and receive 25g, magnesium stearate 5g, tabletting, the bag film-coat, promptly.
Embodiment 4: the preparation of medicinal tablet
With clear water the 12.5kg Rhizoma Alpiniae Officinarum is cleaned up, the Rhizoma Alpiniae Officinarum after cleaning in 60 ℃ of oven dry down of low temperature state, is broken to 60 order fine powders with the Rhizoma Alpiniae Officinarum powder after the oven dry.Rhizoma Alpiniae Officinarum after the pulverizing adopts the supercritical carbon dioxide extraction device to extract and removes low-polarity component.Medicinal residues after supercritical extraction, the ethanol with 85% extract each 2 hours 3 times in 85 ℃ of reflux, extract.Merge alcohol extract, decompression recycling ethanol is 35% to containing the alcohol amount, places centrifugal, collecting precipitation.It is 1.1 (70 ℃) that solution further is concentrated into solution density.The precipitation of collecting before being incorporated in.Place, centrifugal, collecting precipitation, drying gets dry extract.Get the dried cream of Rhizoma Alpiniae Officinarum total flavones, add 85% ethanol 3000mL, in 60 ℃ of water-bath dissolvings, filtered while hot.Filtrate adds water, makes ethanol content reduce to 40%.Leave standstill, centrifugal, get precipitate the Rhizoma Alpiniae Officinarum yellow powder.Get Rhizoma Alpiniae Officinarum flavone extract 375g, add starch 100g, carboxymethyl starch and receive 25g, magnesium stearate 5g, tabletting, the bag film-coat, promptly.
Embodiment 5: the preparation of medicinal tablet
With clear water the 12.5kg Rhizoma Alpiniae Officinarum is cleaned up, the Rhizoma Alpiniae Officinarum after cleaning in 55 ℃ of oven dry down of low temperature state, is broken to 60 order fine powders with the Rhizoma Alpiniae Officinarum powder after the oven dry.Rhizoma Alpiniae Officinarum after the pulverizing adopts the supercritical carbon dioxide extraction device to extract and removes low-polarity component.Medicinal residues after supercritical extraction, the ethanol with 80% extract each 1.5 hours 2 times in 80 ℃ of reflux, extract.Merge alcohol extract, decompression recycling ethanol is 40% to containing the alcohol amount, places centrifugal, collecting precipitation.It is 1.2 (70 ℃) that solution further is concentrated into solution density.The precipitation of collecting before being incorporated in.Place, centrifugal, collecting precipitation, drying gets dry extract.Get the dried cream of Rhizoma Alpiniae Officinarum total flavones, add 80% ethanol 2500mL, in 55 ℃ of water-bath dissolvings, filtered while hot.Filtrate adds water, makes ethanol content reduce to 30%.Leave standstill, centrifugal, get precipitate Rhizoma Alpiniae Officinarum yellow powder extract.Get Rhizoma Alpiniae Officinarum flavone extract 375g, add starch 100g, carboxymethyl starch and receive 25g, magnesium stearate 5g, tabletting, the bag film-coat, promptly.
Embodiment 6: the test of Rhizoma Alpiniae Officinarum flavone extract anti-peptic ulcer
A the results are shown in Table 1 to the influence of water logging stress gastric ulcer animal model.
Table 1 Rhizoma Alpiniae Officinarum flavone extract is to the influence of water logging stress ulcer model (x ± s)
Group Number of animals (only) Dosage (g/kg) Ulcer index (mm) Suppression ratio (%)
Blank group WEINAIAN group Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 10 10 10 10 10 Deng capacity 1.5 0.125 0.25 0.5 29.55±7.15 10.00±3.83 *** 17.85±6.20 ** 14.55±5.32 *** 10.90±4.53 *** 66.16 39.59 50.76 63.11
Annotate: with blank group ratio *P<0.05, *P<0.01, * *P<0.001
As seen from Table 1: Rhizoma Alpiniae Officinarum flavone extract group ulcer index is starkly lower than the blank group, significant difference is all arranged by comparison, and the various dose group is dose-effect relationship.
B the results are shown in Table 2 to the influence of pylorus ligature law ulcer model.
Table 2 Rhizoma Alpiniae Officinarum flavone extract is to the influence of pylorus ligature law ulcer model (x ± s)
Group Number of animals (only) Dosage (g/kg) Ulcer index (mm) Suppression ratio (%)
Blank group ranitidine group Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 10 10 10 10 10 Deng capacity 0.05 0.125 0.25 0.5 4.10±1.72 1.70±0.64 *** 2.60±0.80 * 2.20±0.40 ** 1.80±0.59 *** 58.53 36.59 46.34 56.10
Annotate: with blank group ratio *P<0.05, *P<0.01, * *P<0.001
Table 2 is the result show: Rhizoma Alpiniae Officinarum flavone extract ulcer index is starkly lower than the blank group, and significant difference is arranged, and there is tangible dose-effect relationship in the various dose group.High dose group P<0.001, middle dosage group P<0.01, low dose group P<0.05.
C the results are shown in Table 3 to the influence of acetic acid inustion ulcer model.
The influence of table 3 Rhizoma Alpiniae Officinarum flavone extract Dichlorodiphenyl Acetate inustion ulcer model (x ± s)
Group Number of animals (only) Dosage (g/kg) Ulcer index (mm) Suppression ratio (%)
Blank group ranitidine group Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 10 10 10 10 10 Deng capacity 0.05 0.125 0.25 0.5 6.48±0.81 2.08±1.32 *** 4.68±1.01 4.20±1.25 ** 2.25±1.81 ** 67.90 27.78 35.19 65.28
Annotate: with the blank group than * P<0.05, * * P<0.01, * * * P<0.001
As seen from Table 3: the ulcer index of Rhizoma Alpiniae Officinarum flavone extract high dose group and middle dosage group has been compared significant difference with the blank group, high dose group P<0.001, and middle dosage group P<0.01, low dose group is there was no significant difference (P>0.05) then.
D causes the influence of rat acute gastric mucosa injury to ethanol, the results are shown in Table 4.
Table 4 Rhizoma Alpiniae Officinarum flavone extract causes the influence (x ± s) of rat acute gastric mucosa injury to ethanol
Group Number of animals (only) Dosage (g/kg) Ulcer index Suppression ratio (%)
Blank group ranitidine group Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 10 10 10 10 10 Deng capacity 0.05 0.125 0.25 0.5 95.15±29.54 33.43±26.71 *** 66.20±16.92 * 48.30±17.58 *** 40.85±14.57 *** 64.87 30.43 49.24 57.07
Annotate: with blank group ratio *P<0.05, * * P<0.01, * * * P<0.001
Table 4 is the result show, the high, medium and low dosage of Rhizoma Alpiniae Officinarum flavone extract can obviously alleviate rat acute gastric mucosa injury (P<0.01~0.05) due to the ethanol, and ranitidine also makes that the rat acute gastric mucosa injury significantly alleviates (P<0.001) due to the ethanol.Water logging stress gastric ulcer animal model experiment, pyloric ligation ulcers gastric ulcer animal model experiment, acetic acid burn type gastric ulcer animal model experiment, oral ethanol gastric mucosa injury animal model experiment; animal to the modeling success; use Rhizoma Alpiniae Officinarum extract, the result shows four kinds of experimental gastric ulcer models are all had good protective action.Show the anti-peptic ulcer effect.
Embodiment 7: the experiment of Rhizoma Alpiniae Officinarum flavone extract antiinflammatory
The influence of rat hindleg sole of the foot swelling the results are shown in Table 5 due to a on Carrageenan.
The influence of pedal swelling behind the rat due to the table 5 Rhizoma Alpiniae Officinarum flavone extract on Carrageenan (x ± s)
Group Number of animals (only) Dosage (g/k g) Normally (ml) Cause the pedal swelling degree (ml) of scorching back different time (h)
1h 2h 3h 4h 5h
Blank aspirin galangal galangal galangal 10 10 10 10 10 0.1 0.12 5 0.25 0.5 1.25±0.09 1.19±0.06 1.17±0.11 1.19±0.14 1.15±0.07 0.33±0.06 0.15±0.07 ** 0.34±0.11 0.31±0.07 0.32±0.09 0.71±0.11 0.39±0.23 ** 0.64±0.13 0.58±0.16 * 0.56±0.09 * 0.76±0.11 0.45±0.16 ** 0.77±0.08 0.69±0.15 0.66±0.11 * 0.73±0.17 0.57±0.19 0.72±0.08 0.66±0.20 0.62±0.12 0.65±0.19 0.56±0.19 0.60±0.13 0.59±0.19 0.55±0.11
Annotate: with the blank group than * P<0.05, * * P<0.01
The result shows: the rat paw edema that middle and high dosage group of Rhizoma Alpiniae Officinarum flavone extract and aspirin group all have obvious inhibition to be caused by carrageenin.
B the results are shown in Table 6 to the influence of the saturating property of mouse peritoneal blood capillary pain.
Table 6 Rhizoma Alpiniae Officinarum flavone extract is to the influence of the saturating property of intraperitoneal mouse blood capillary pain (x ± s)
Group Number of animals (only) Dosage (g/kg) The OD value
Blank group aspirin group Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 12 12 12 12 12 - 0.2 0.25 0.5 1.0 0.357±0.067 0.069±0.037 *** 0.333±0.096 0.302±0.064 * 0.284±0.072 *
Annotate: the blank group is than * P<0.05, * * P<0.01, * * * P<0.001
The result shows: the saturating property of mouse peritoneal blood capillary pain that the middle and high dosage group of Rhizoma Alpiniae Officinarum flavone extract can significantly suppress due to the glacial acetic acid increases, and is dose-effect relationship.The saturating property of mouse peritoneal blood capillary pain that aspirin also can significantly suppress due to the glacial acetic acid increases (P<0.001).
The influence of c xylol induced mice auricle edema the results are shown in Table 7.
The influence of table 7 Rhizoma Alpiniae Officinarum flavone extract xylol induced mice auricle edema (x ± s)
Group Number of animals only Dosage g/kg Ear swelling degree mg
Blank aspirin Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 10 10 10 10 10 - 0.2 0.25 0.5 1.0 6.34±2.51 2.64±0.60 ** 5.43±1.18 4.91±0.75 * 4.54±1.24 *
Annotate: the blank group is than * P<0.05, * * P<0.01
Table 7 is the result show, the middle and high dosage of Rhizoma Alpiniae Officinarum flavone extract can significantly alleviate the ear swelling degree (P<0.05) of the scorching mice of caused by dimethylbenzene xylene, and low dosage then acts on not significantly (P>0.05).Aspirin also can significantly alleviate the ear swelling degree (P<0.01) of mice.Mice caused by dimethylbenzene xylene auricle edema experiment, rat paw carrageenin cause swollen experiment, the mouse peritoneal capillary permeability increases experiment, and the result shows that Rhizoma Alpiniae Officinarum extract increases glacial acetic acid induced mice abdominal cavity capillary permeability and acute inflammation models such as the swelling of rat carrageenan toes, dimethylbenzene induced mice auricle edema all have obvious inhibitory action.Show antiinflammatory action.
Embodiment 8: Rhizoma Alpiniae Officinarum flavone extract analgesic test
A causes the influence that pain acts on to the mice hot plate method, the results are shown in Table 8.
Table 8 Rhizoma Alpiniae Officinarum flavone extract to the influence of mice hot plate method analgesic experiment (x ± s, n=12)
Group Dosage (the g crude drug/g) The pain sensation response time (second) Percentage rate (%) is improved in the threshold of pain
Before the administration After the administration
Blank group aspirin Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum - 0.1g 0.25 0.5 1.0 18.4±4.6 18.4±4.6 18.3±3.5 18.0±4.6 18.4±5.3 18.9±3.4 44.0±16.1 19.0±4.8 22.3±5.8 23.1±7.8 5.8±3.2 150.5±109.5 ** 9.7±7.5 32.6±30.8 * 37.4±34.3 **
Annotate: compare with matched group: * P<0.05; * P<0.01; The t check.
By table 8 as seen, the middle and high dosage group of Rhizoma Alpiniae Officinarum flavone extract obviously improves mice threshold of pain percentage rate, and relatively there were significant differences with matched group.
B the results are shown in Table 9 to the influence of glacial acetic acid induced mice writhing response.
The effect of table 9 Rhizoma Alpiniae Officinarum flavone extract Dichlorodiphenyl Acetate induced mice pain influence (X ± SD)
Group Dosage (g/kg) Number of animals (only) Turn round body number of times (15min)
Blank group aspirin Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum - 0.1g 0.25 0.5 1.0 12 12 12 12 12 31.3±7.9 7.8±6.1 ** 25.6±5.5 23.9±7.3 * 21.1±6.9 **
Annotate: compare with matched group: * P<0.05; * P<0.01 t check.
By table 9 as seen, the mouse writhing number of times that Rhizoma Alpiniae Officinarum flavone extract height, the obvious inhibition of middle dosage group are caused by glacial acetic acid, relatively there were significant differences with matched group.Mouse writhing experiment and hot plate method experiment, the result shows that Rhizoma Alpiniae Officinarum extract can obviously improve mice threshold of pain percentage rate, suppresses the mouse writhing number of times that is caused by glacial acetic acid.Show analgesic activity.
Embodiment 9: the test of Rhizoma Alpiniae Officinarum flavone extract gastrointestinal function
A the results are shown in Table 10 to the influence of normal mouse gastric emptying.
Table 10 Rhizoma Alpiniae Officinarum flavone extract is to the influence of normal mouse gastric emptying (X ± SD)
Group Dosage (ml/kg) Number of animals (only) Gastric residual rate (%)
Blank motilium Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum - 10mg 0.25 0.5 1.0 12 12 12 12 12 43.4±11.1 35.6±10.2 ** 48.8±5.8 47.3±8.1 45.1±10.0
Annotate: compare with matched group: *P<0.05; *P<0.01
As seen from Table 10: motilium can promote the normal mouse gastric emptying, and Rhizoma Alpiniae Officinarum flavone extract and blank group compare there was no significant difference, show that the Rhizoma Alpiniae Officinarum flavone extract does not have obvious influence to the normal mouse gastric emptying.
B the results are shown in Table 11 to the hyperfunction influence of pyridostigmine bromide induced mice gastric emptying.
The influence hyperfunction to pyridostigmine bromide induced mice gastric emptying of table 11 Rhizoma Alpiniae Officinarum flavone extract (X ± SD)
Group Dosage (g/kg) Number of animals (only) Gastric residual rate (%)
Blank pyridostigmine bromide atropine Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum - 3mg 0.3mg 0.25 0.5 1.0 12 12 12 12 12 12 44.8±11.5 28.3±8.5 47.6±9.3 ** 34.8±9.1 * 37.7±10.9 * 39.7±9.0 **
Annotate: compare △ △ P<0.01 with the blank group; Compare with the neostigmine group: *P<0.05; *P<0.01
As seen from Table 11: pyridostigmine bromide can obviously promote the mice gastric emptying, and atropine, the high, medium and low dosage group of Rhizoma Alpiniae Officinarum flavone extract have tangible antagonism to pyridostigmine bromide induced mice gastric emptying is hyperfunction, and be dose-effect relationship.
C the results are shown in Table 12 to the influence of gastric juice, gastric acid, pepsin activity.
Table 12 Rhizoma Alpiniae Officinarum flavone extract is to the excretory influence of rat gastric juice (X ± SD)
Group Number of animals (only) Dosage (g/kg) Gastric juice amount (ml) Total acidity (mmol/L) Total acid output (mmol/L.h) Pepsin activity (active unit/ml)
Blank ranitidine Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum 10 10 10 10 10 - 0.05 0.5 0.25 0.125 5.48±1.52 4.12±1.58 * 3.32±1.15 ** 3.70±0.68 ** 4.76±1.72 0.095±0.014 0.064±0.015 *** 0.104±0.020 0.092±0.018 9.094±0.009 0.132±0.048 0.066±0.26 *** 0.089±0.040 * 0.086±0.026 * 0.112±0.044 239.0±99.0 311.3±111.9 289.4±161.9 261.4±139.0 318.5±125.6
Annotate: with blank group ratio *P<0.05, * * P<0.01, * * * P<0.001
As seen from Table 12, Rhizoma Alpiniae Officinarum flavone extract high dose and middle dosage all can effectively reduce rat stomach liquid measure and total acid output, have compared significant difference with the blank group, and low dosage does not then have obvious influence; In addition, each group of Rhizoma Alpiniae Officinarum flavone extract does not all have tangible influence to pepsin activity.Ranitidine can significantly suppress the gastric juice amount, reduces gastric acidity, total acid output.
D the results are shown in Table 13 to the influence of ACH effect isolated rat stomach bar.
Table 13 Rhizoma Alpiniae Officinarum flavone extract to rat stomach at the bottom of the influence (X ± SD) of longitudinal muscle bar shrink tension
Group Number of samples (only) Final concentration (mg/ml) Spasmolytic percentage rate (%)
Dosage group low dose group atropine group in the blank group high dose group 10 10 10 10 10 - 0.6 0.15 0.0375 0.067 0.39±0.97 95.51±7.66 *** 75.78±9.92 *** 70.00±10.26 *** 80.38±13.79 ***
Annotate: with blank group ratio *P<0.05, * * P<0.01, * * * P<0.001
The result shows: the spasmolytic percentage rate of various dose Rhizoma Alpiniae Officinarum flavone extract all has significant difference with the blank group, and is dose-effect relationship.As seen the rat stomach smooth muscle is under the state of tetanic contraction adding Ach, the Rhizoma Alpiniae Officinarum flavone extract can obviously reduce pipe smooth muscle tension force, and showing that rat stomach smooth muscle convulsion that the Rhizoma Alpiniae Officinarum flavone extract causes Ach is twin has an obvious suppression effect.
E the results are shown in Table 14 to the influence (charcoal end method) of small intestine movement of mice ahead running.
Table 14. Rhizoma Alpiniae Officinarum flavone extract is to the influence of small intestine movement of mice ahead running (X ± SD)
Group Dosage (m/kg) Number of animals (only) Advance percentage rate (%)
Blank group FUKEAN Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum Rhizoma Alpiniae Officinarum - 1g 0.25 0.5 1.0 12 12 12 12 12 71.3±7.60 61.3±8.30 * 68.2±10.1 66.1±7.1 63.7±7.3 *
Compare with matched group: *P<0.05; *P<0.01.Compare △ △ P<0.01 with the FUKEAN group;
The result shows: motion has the obvious suppression effect to Rhizoma Alpiniae Officinarum flavone extract high dose to small intestine movement of mice, and low, the middle dosage of Rhizoma Alpiniae Officinarum flavone extract does not have obvious influence to the small intestine movement of mice ahead running.Emptying test, gastric analysis test (measuring gastric juice amount, gastric acidity, pepsin activity), intestinal propulsion exercise test, the test of gastrointestinal smooth muscle spasmolytic, experimental result shows that the Rhizoma Alpiniae Officinarum flavone extract has certain inhibitory action to gastric acid secretion, but pepsin activity is not had influence, rat stomach smooth muscle under the spasticity is had tangible spasmolysis; The normal mouse gastric emptying is not had obvious influence, but tangible antagonism arranged, the small intestine movement of mice ahead running is had certain influence pyridostigmine bromide induced mice gastric emptying is hyperfunction.Show and have the adjusting action of enterogastric function.

Claims (4)

1, a kind of medicine for the treatment of gastric ulcer is Rhizoma Alpiniae Officinarum extract, and described Rhizoma Alpiniae Officinarum extract is to be prepared from by following steps:
(1) Rhizoma Alpiniae Officinarum is cleaned up;
(2) Rhizoma Alpiniae Officinarum is dried down at 40~60 ℃;
(3) Rhizoma Alpiniae Officinarum powder after will drying is broken to 10~60 orders;
(4) Rhizoma Alpiniae Officinarum after will pulverizing in 60~90 ℃ of reflux, extract,, extracts each 1~2.5 hour with 60%~90% ethanol 2~3 times; Merge alcohol extract, decompression recycling ethanol is 25%~50% to containing the alcohol amount, places centrifugal, collecting precipitation; It is 1~1.3 that solution further is concentrated into the solution relative density; The precipitation of collecting before being incorporated in; Place, centrifugal, collecting precipitation, drying gets dry extract.
(5) get dried cream, add the ethanol of 4~8 times of volumes 60%~95%, in 50~60 ℃ of water-bath dissolvings, filtered while hot; Filtrate adds water, makes ethanol content reduce to 20%~40%; Leave standstill, centrifugal, get precipitation and be high good extract.
2, the preparation method of the medicinal tablet of the described treatment gastric ulcer of a kind of claim 1 is characterized in that may further comprise the steps:
(1) Rhizoma Alpiniae Officinarum is cleaned up;
(2) Rhizoma Alpiniae Officinarum is dried down at 40~60 ℃;
(3) Rhizoma Alpiniae Officinarum powder after will drying is broken to 60 order fine powders;
(4) Rhizoma Alpiniae Officinarum after will pulverizing adopts the supercritical carbon dioxide extraction device to extract and removes low-polarity component, and the medicinal residues after supercritical extraction, the ethanol with 70%~90% extract each 1.5~2.5 hours 2~3 times in 60~90 ℃ of reflux, extract; Merge alcohol extract, decompression recycling ethanol is 25%~50% to containing the alcohol amount, places centrifugal, collecting precipitation; It is 1.1~1.3 that solution further is concentrated into solution density, the precipitation of collecting before being incorporated in; Place, centrifugal, collecting precipitation, drying gets dry extract;
(5) get dried cream, add the ethanol of 4~8 times of volumes 70%~95%, in 50~60 ℃ of water-bath dissolvings, filtered while hot; Filtrate adds water, makes ethanol content reduce to 30%~40%; Leave standstill, centrifugal, get precipitate Rhizoma Alpiniae Officinarum extract;
(6) get Rhizoma Alpiniae Officinarum extract, add adjuvant, tabletting, the bag film-coat, promptly.
3, the described medicine of claim 1 is used for the application of the medicine of anti-peptic ulcer, antiinflammatory, analgesia, promotion gastrointestinal function in preparation.
4, application as claimed in claim 3 is characterized in that described medicine is used for the application of the medicinal tablet of anti-peptic ulcer, antiinflammatory, analgesia, promotion gastrointestinal function in preparation.
CNB2005100374068A 2005-09-22 2005-09-22 Gastric ulcer treatment medicine, its preparation process and application Expired - Fee Related CN100358572C (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108066683A (en) * 2018-01-25 2018-05-25 海南医学院 Application of the galangal in the drug or health products for preparing the gastric ulcer that prevention and treatment non-steroidal anti-inflammatory drugs triggers
US10098924B1 (en) * 2018-01-23 2018-10-16 King Saud University Anticancer extracts of Alpinia officinarum hance

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10098924B1 (en) * 2018-01-23 2018-10-16 King Saud University Anticancer extracts of Alpinia officinarum hance
CN108066683A (en) * 2018-01-25 2018-05-25 海南医学院 Application of the galangal in the drug or health products for preparing the gastric ulcer that prevention and treatment non-steroidal anti-inflammatory drugs triggers

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