CN1411849A - Preparation for relieving alcoholism - Google Patents

Preparation for relieving alcoholism Download PDF

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Publication number
CN1411849A
CN1411849A CN 01136384 CN01136384A CN1411849A CN 1411849 A CN1411849 A CN 1411849A CN 01136384 CN01136384 CN 01136384 CN 01136384 A CN01136384 A CN 01136384A CN 1411849 A CN1411849 A CN 1411849A
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Prior art keywords
aescin
ethanol
dextrin
magnesium stearate
corn starch
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CN 01136384
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Chinese (zh)
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张伯庆
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Individual
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Individual
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Priority to CN 01136384 priority Critical patent/CN1411849A/en
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Abstract

The medicine for releiving alcoholism, protecting liver and nourishing stomach is made up by using aesculus chinensis saponin which is extract of dried mature fruit horse chestnut of aesculus chinensis or aesculus wilsonii, sodium carboxymethylstarch, dextrin, corn starch, magnesium stearate and talcum powder as raw material through a certain preparation process.

Description

A kind of Medicament for Alcoholism
The present invention relates to the Chinese herbal and crude drugs preparations technical field, especially relate to a kind of Medicament for Alcoholism and preparation method thereof.
The goods kind that present domestic market is used to sober up is more, mostly is Chinese prescription greatly and is distributed into oral liquid or tablet after decoction filtering.In recent years a large amount of vitamin Cs of adding are made the tablet listing after also seeing shellfish product such as Concha Ostreae powder baking powder.The majority goods of sobering up generally reflect DeGrain in the social consumption crowd, such as the Concha Ostreae goods: on the books in " Compendium of Materia Medica) ", the function of Concha Ostreae is: YANG hyperactivity suppressing, astringent or styptic treatment for spontaneous sweating, softening the hard mass, antacid are used for hyperchlorhydria.Also mix in the goods and a large amount of vitamin C preparations.Vitamin can expand blood vessel, microcirculation improvement, and the accelerating oxidation metabolism is used for detoxifcation when heavy dose of.Only use " stomach function regulating " of the traditional Chinese medical science and " the antioxidation detoxifcation " of doctor trained in Western medicine during alcoholism; promoting metabolism is incomplete in the hope of reaching the purpose of sobering up; this class of analysis-by-synthesis product of sobering up, its product was not obvious to the protective effect of harmonization of the stomach liver when its one-sidedness was to sober up.
The present invention is in order to overcome above-mentioned defective, but a kind of medicament and preparation method thereof that relieves the effect of alcohol at antialcoholic while hepatoprotective stomach function regulating to be provided.
The objective of the invention is to realize by the following method: raw material of the present invention and weight proportion thereof are as follows: in 10kg (± 0.1%) total stuff amount (50000 tablet amounts, monolithic weight=200mg),
Aescin 0.25-1.75kg
Carboxymethyl starch sodium 0.9-1.1kg
Dextrin 3.15-3.85kg
Corn starch 4.23-5.17kg
Magnesium stearate 0.135-0.165kg
Pulvis Talci 0.135-0.165kg
10-20% medical ethanol 1-2kg (this adds for outside the raw material total amount)
Being prepared as follows of Aescin wherein: the dry mature fruit Semen Aesculi of natural plants Aesculus chinensis Bunge Aesculus chinensis bge or Aesculus wilonii Aesculus wllsonii Red is pulverized back 80-90% ethanol extraction; extracting solution adsorbs through adsorbent resin; eluent is condensing crystallizing after decolouring; the crude product crystallization is further purified; obtain its function composition chemical compound escin; the structure of this chemical compound is 21 β; 28-O-diacetyl Aescin-3 β-O-[β-D-glycopyranosyl (1-2)] [β-D-glycopyranosyl (1-4)]-beta d glucopyranosiduronic acid (21 β, 28-O-diacetylprotcescigenin-3 β-O-[β-D-glucopyyanosyl (1-2)] [β-D-glucpyranosyl (1-4)]-β-D-glucopyranosiduronic acid).Its molecular formula See Figure:
The application's medicaments preparation method is:
A, take by weighing raw material and adjuvant, put to mix in the powder machine and stir evenly by above proportioning, according to temperature add the 10-20% of batching total amount, the above-mentioned medical ethanol that concentration is 10-20% is made soft material, go into granulation machine and granulate with 14 mesh sieves;
B, the thin stand of collecting granules are gone into oven drying in stainless steel disc;
C, treat to take out behind the particle drying, enter the pelletizing machine granulate, add carboxymethyl starch sodium, dextrin, corn starch and magnesium stearate and mix;
D, ask with 10m/m deep-draw tabletting on tablet machine every heavy 200mg, packing according to sheet is important;
E, above-mentioned whole technical process are produced in requiring between 300,000 grades of dumpers, and temperature is controlled at 18-26 ℃, relative humidity 45-65%; The disintegration time of made tablet was controlled in 5 minutes.
In addition, also can adopt common process that medicament of the present invention is made other conventional peroral dosage form.
The invention will be further described below in conjunction with embodiment.
Embodiment 1
In 10kg (± 0.1%) total stuff amount, raw material is
Aescin 0.25-0.275kg
Carboxymethyl starch sodium 0.9-0.99kg
Dextrin 3.15-3.465kg
Corn starch 4.23-4.653kg
Magnesium stearate 0.135-0.1485kg
Pulvis Talci 0.135-0.485kg
10-20% medical ethanol 1-2kg
Be prepared into medicament as stated above.
Embodiment 2
In 10kg (± 0.1%) total stuff amount, raw material is
Aescin 1-1.1kg
Carboxymethyl starch sodium 0.99-1.089kg
Dextrin 2.735-3.15kg
Corn starch 4.653-5.018kg
Magnesium stearate 0.149-0.164kg
Pulvis Talci 0.149-0.164kg
10-20% medical ethanol 1-2kg
Be prepared into medicament as stated above.
Embodiment 3
10kg (± 0.1%) total stuff amount meter, raw material is
Aescin 1.3-1.43kg
Carboxymethyl starch sodium 0.81-0.9kg
Dextrin 3.465-3.812kg
Corn starch 3.807-4.23kg
Magnesium stearate 0.122-0.135kg
Pulvis Talci 0.122-0.135kg
10-20% medical ethanol 1-2kg
Be prepared into medicament as stated above.
The effect of medicament of the present invention and superiority can illustrate from following obtaining:
For reach make the wine-head take in ethanol after its uptake reduce to greatest extent, ethanol is to human body Liver, stomach, neural damage and the lightest purpose of interference that the human body biochemical metabolism is caused, this A person of good sense from the toxicity of ethanol and metabolic basis, and excessive absorption ethanol after its biochemical reaction human body is caused Harm launched further investigation, find that the principle that Aescin relieves the effect of alcohol is active ingredient seven in the buckeye Leaf saponin Ia, Ib, IIa and IIb, its structure contains 2 '-O-xylopyranosyl and 2 '-O-pyrans Portugal The grape glycosyl. Experimental results show that the former has the effect that suppresses the ethanol activity, latter has and reduces the ethanol activity Effect; And the two all contains deacetylate group, and acyl group is very important to the inhibitory action of ethanol. Experiment Studies have shown that the contained acyl group that goes of Aescin is to suppress the material base that alcohol absorbs, simultaneously research Prove that also this acyl group has significantly but sugar is active.
(1) the digestion and metabolism process of ethanol
Ethanol is through stomach and intestinal absorption, can find the 30-90 branch in drinking in rear 5 minutes in blood Reach maximum concentration behind the clock; Ethanol enters each organ that can arrive body behind the blood flow, also can arrive the brain ridge In liquid, urine and the lung, it is eliminated mainly is that oxidation generates carbon dioxide. Mainly through liver metabolism, by The alcohol dehydrogenase enzymatic generates acetaldehyde, also by catalase and microsomal oxidase oxidation, acetaldehyde Generated acetic acid by the further oxidation of acetaldehyde dehydrogenase, generate at last acetyl coenzyme A and carbon dioxide.
(2), ethanol is excessive in the impact of human body and the impact of other aspect
Ethanol can directly stimulate the stomach hole, discharges gastrin, also can impel stomach inner tissue to discharge tissue Amine increases thereby produce gastric acid secretion, causes acute gastritis. Wine-head's peptic ulcer rate Unusually increase; Long-term wine-head's pathogenesis of fatty liver rate obviously increases. 8% alcoholic can be taken place Cirrhosis; Excessive consumption of alcohol can cause acute pancreatitis; Neural infringement shows as: I ethanol Drunkness, stupor, the reason disappearance of poisoning and causing, the II supervention is in the nervous system nutrition of ethylism Shortage property disease: A, Wernicke-korsokoff syndrome, B, DPN, C, second The alcoholism amblyopia, D, pellagra; The III cerebellar degeneration, cerebral atrophy.
In addition, even if because the chronic or acute outbreak of harm that ethanol causes nervous system, All can impact family and society.
(3), the superiority of goods of the present invention
Aescin Ia, the Ib that the present invention obtains with the high-tech separation method, IIa, IIb can be straight Connect and suppress the ethanol activity, this kind inhibition can think Aescin to the antagonism of ethanol active site or Package action. Goods were the disintegration stripping in oral rear 5 minutes, because effective efficiency group in the goods To the direct repression of ethanol, fast and effective, effect is that amount effect ratio closes with the Aescin consumption System; Take this product before the wine and can obviously increase the intake of alcohol; Taking after drinking this product also can effectively press down Hold back the absorption of alcohol in the stomach processed. Zoopery proof Aescin has anti-inflammatory, imperviously goes out, and is anti-The oedema effect, fairly obvious. It is in the inflammation that suppresses can effectively prevent when ethanol absorbs gastric mucosa Disease, ooze out. Acute or chronic gastritis, the peptic ulcer that causes because being addicted to drink there is distinguished rehabilitation effect Really. Can receive the effect of removing drunk discomfort in oral this product 15-30 minute after the drunk generation.
The sugared effect that presses down of effective efficiency group can among Aescin Ia, Ib, IIa, the IIb in addition Suppress blood sugar and increase, the prevention that postprandial blood sugar is increased is with helpful. Alcohol exists to the impact of human body The biochemical reaction aspect also can cause after drinking that the utilization of periphery blood sugar reduces and the hyperglycaemia of initiation. This Product can effectively prevent wine-head or part of diabetes mellitus people to increase the postprandial hyperglycemia of initiation because of postprandial blood sugar Disease.

Claims (5)

1. medicament that relieves the effect of alcohol is characterized in that it is the medicament of being made according to a conventional method by following materials of weight proportions: in the 10kg total stuff amount,
Aescin 0.25-1.75kg
Carboxymethyl starch sodium 0.9-1.1kg
Dextrin 3.15-3.85kg
Corn starch 4.23-5.17kg
Magnesium stearate 0.135-0.165kg
Pulvis Talci 0.135-0.165kg
10-20% medical ethanol 1-2kg
Wherein the amount of medical ethanol does not account for total stuff amount; being prepared as follows of Aescin: the dry mature fruit Semen Aesculi of natural plants Aesculus chinensis Bunge Aesculus chinensis bge or Aesculus wilonii Aesculus Wllsonii Red is pulverized back 80-90% ethanol extraction; extracting solution adsorbs through adsorbent resin; eluent is condensing crystallizing after decolouring; the crude product crystallization is further purified; obtain its function composition chemical compound escin; the structure of this chemical compound is 21 β; 28-O-diacetyl Aescin-3 β-O-[β-D-glycopyranosyl (1-2)] [β-D-glycopyranosyl (1-4)]-beta d glucopyranosiduronic acid, its molecular formula is
Figure A0113638400021
2. medicament according to claim 1 is characterized in that tablet makes by the following method:
A, take by weighing raw material and adjuvant, put to mix in the powder machine and stir evenly, add the 10-20% of batching total amount, the above-mentioned medical ethanol that concentration is 10-20% is made soft material, go into granulation machine and granulate with 14 mesh sieves by above proportioning;
B, the thin stand of collecting granules are gone into oven drying in stainless steel disc;
C, treat to take out behind the particle drying, enter the pelletizing machine granulate, add carboxymethyl starch sodium, dextrin, corn starch and magnesium stearate and mix;
D, ask with 10m/m deep-draw tabletting on tablet machine according to sheet is important, packing promptly obtains this tablet.
3. medicament according to claim 1, it is characterized in that it is made by following materials of weight proportions: in the 10kg total stuff amount, raw material is
Aescin 0.25-0.275kg
Carboxymethyl starch sodium 0.9-0.99kg
Dextrin 3.15-3.465kg
Corn starch 4.23-4.653kg
Magnesium stearate 0.135-0.1485kg
Pulvis Talci 0.135-0.485kg
10-20% medical ethanol 1-2kg.
4. medicament according to claim 1, it is characterized in that it is made by following materials of weight proportions: in the 10kg total stuff amount, raw material is
Aescin 1-1.1kg
Carboxymethyl starch sodium 0.99-1.089kg
Dextrin 2.735-3.15kg
Corn starch 4.653-5.018kg
Magnesium stearate 0.149-0.164kg
Pulvis Talci 0.149-0.164kg
10-20% medical ethanol 1-2kg.
5. medicament according to claim 1, it is characterized in that it is made by following materials of weight proportions: in the 10kg total stuff amount, raw material is
Aescin 1.3-1.43kg
Carboxymethyl starch sodium 0.81-0.9kg
Dextrin 3.465-3.812kg
Corn starch 3.807-4.23kg
Magnesium stearate 0.122-0.135kg
Pulvis Talci 0.122-0.135kg
10-20% medical ethanol 1-2kg.
CN 01136384 2001-10-12 2001-10-12 Preparation for relieving alcoholism Pending CN1411849A (en)

Priority Applications (1)

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CN 01136384 CN1411849A (en) 2001-10-12 2001-10-12 Preparation for relieving alcoholism

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102532241A (en) * 2010-12-24 2012-07-04 苏州宝泽堂医药科技有限公司 Method for purifying sodium aescinate
CN103655645A (en) * 2012-09-17 2014-03-26 南京星银药业集团有限公司 Chinese buckeye seed extract tablets and preparation method thereof
CN106491627A (en) * 2016-12-05 2017-03-15 深圳前海七叶树生物科技有限公司 Medicament for Alcoholism
CN106540005A (en) * 2016-12-23 2017-03-29 深圳前海七叶树生物科技有限公司 Pharmaceutical preparation for the treatment of peptic ulcer and preparation method thereof

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102532241A (en) * 2010-12-24 2012-07-04 苏州宝泽堂医药科技有限公司 Method for purifying sodium aescinate
CN103655645A (en) * 2012-09-17 2014-03-26 南京星银药业集团有限公司 Chinese buckeye seed extract tablets and preparation method thereof
CN106491627A (en) * 2016-12-05 2017-03-15 深圳前海七叶树生物科技有限公司 Medicament for Alcoholism
CN106540005A (en) * 2016-12-23 2017-03-29 深圳前海七叶树生物科技有限公司 Pharmaceutical preparation for the treatment of peptic ulcer and preparation method thereof

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