CN102018707A - Medicinal composition for treating diarrhea and preparation thereof - Google Patents
Medicinal composition for treating diarrhea and preparation thereof Download PDFInfo
- Publication number
- CN102018707A CN102018707A CN2010105637963A CN201010563796A CN102018707A CN 102018707 A CN102018707 A CN 102018707A CN 2010105637963 A CN2010105637963 A CN 2010105637963A CN 201010563796 A CN201010563796 A CN 201010563796A CN 102018707 A CN102018707 A CN 102018707A
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- adjuvant
- racecadotril
- drug combination
- berberine hydrochloride
- combination preparation
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- 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
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Abstract
The invention discloses a composition for treating diarrhea and a preparation thereof, relating to a medicinal composition for stopping the diarrhea. The invention also relates to a preparation of the medicinal composition for stopping the diarrhea. The medicinal composition is mainly prepared from the main raw materials of 1 part of Racecadotril and 0.25-25 parts of berberine hydrochloride as well as 0.01-250 parts of auxiliary materials in proportion. The medicinal composition has scientific and reasonable prescription, and can be used for inhibiting the rise of calcium ion concentration in colon smooth muscle cells and improving the motion functional coordination of the intestinal tract to realize the effect on stopping the diarrhea mainly by inhibiting the activity of enkephalinase and further inhibiting the excessive secretion of water and electrolyte via the Racecadotril, and simultaneously by the stronger bactericidal effect of the berberine hydrochloride on escherichia coli, Streptococcus hemolyticus, Diplococcus pneumoniae and the like.
Description
Technical field
The present invention relates to a kind of antidiarrheal product, particularly a kind of diarrheal preparation for the treatment of.
Background technology
Racecadotril is a kind of inhibitor of enkephalinase, has higher specificity secretion inhibitor effect.It is by suppressing the enkephalinase activity, and then suppress power and water and separate the matter excessive secretion and bring into play its diarrhea effect, enkephalin is the neurotransmitter in the gastrointestinal tract, thereby it activates δ-opiate receptors and causes the decline of cAMP level to reduce moisture and electrolytical secretion in the intestinal, and intestinal power is unaffected.The characteristics of racecadotril are: efficient, effect rapidly, therapeutic index is high, central nervous system, respiratory system, cardiovascular system, hormonal system there is not obvious effect, do not cause constipation, the diarrhea effect is only just arranged when excessive secretion occurring, and do not have this effect in the ordinary course of things.
Berberine hydrochloride claims berberine again, is to extract from plants such as Rhizoma Coptidis, Cortex Phellodendri or the alkaloid of synthetic, and bitter in the mouth has functions such as heat clearing away, detoxifcation, pathogenic fire purging.The Chinese medicine of hydrochloric berberine is used for the treatment of the existing nearly 3,000 years history of diarrhoea at home, and the good reputation of " dysentery man panacea " is arranged.Modern pharmacological research shows that berberine has broad-spectrum antibacterial action, can treat infectious diarrhea, and the secretory diarrhea due to cholera toxin, the stable type colicine etc. is had excellent curative, and is to exudative, inflammatory diarrhea, also effective as gastroenteritis etc.; Clinical trial proves that berberine treatment bacterial enteritis is difficult for drug resistance, totally is better than chloromycetin, gentamycin, Ekvacilline and Co-trimoxazole Tablet etc.; Modern clinical research proves that berberine hydrochloride all has strong bacteriostasis to escherichia coli, Hemolytic streptococcus, the Diplococcus pneumoniae that causes infantile diarrhea, also can kill fungus, and the traditional Chinese medical science is thought heat clearing and damp drying, the thick the intestines and stomach effect of antidiarrheal, energy removing summer-heat the intestines and stomach pyretic toxicity; Berberine hydrochloride can also obviously suppress the rising of colonic smooth muscle intracellular calcium concentration, improves the intestinal movement orthofunction.
More with treatment diarrheal product in the market, great majority are antibiotic, very easily cause bacterium to be lacked of proper care and produce new Resistant strain and do not reach the basic goal of treatment.What deserves to be mentioned is, much treat diarrheal product baby and ban use of.
Summary of the invention
Purpose of the present invention is intended to overcome the defective of prior art, provide a kind of and can realize diarrhea-relieving function, can suppress power and water separates the matter excessive secretion, and can improve the intestinal movement function, suppress to cause the excessive multiplication of diarrheal escherichia coli, Hemolytic streptococcus, Diplococcus pneumoniae and to reach the antidiarrheal purpose simultaneously, and adult, baby treatment diarrheal all applicatory pharmaceutical composition, another object of the present invention provides the preparation of this pharmaceutical composition.
Treatment diarrheal pharmaceutical composition of the present invention mainly is to be that primary raw material preparation gets by racecadotril, berberine hydrochloride, and its main components in percentage by weight is: 1 part of racecadotril, berberine hydrochloride 0.25-25 part, adjuvant 0.01-250 part.
Described racecadotril should meet the requirement of national drug quality standard.
Described berberine hydrochloride should meet the requirement of national drug quality standard.
Described preparation is a kind of in tablet, film coated tablet, capsule, soft capsule, granule, suspensoid, dry suspension, the suppository.
The adjuvant of described tablet, film coated tablet is two or more in microcrystalline Cellulose, starch, magnesium stearate, hypromellose, the carboxymethylstach sodium.
The adjuvant of described capsule is two or more in starch, microcrystalline Cellulose, carboxymethylstach sodium, magnesium stearate, the Capsules
Described soft capsule adjuvant is gelatin, glycerol.
The adjuvant of described granule is one or more in sucrose, mannitol, lactose, glucose, the aspartame.
The adjuvant of described suspensoid, dry suspension is two or more in water, hypromellose, carmethose, arabic gum, tragakanta, gelatin, Polyethylene Glycol, anhydride silica, citric acid, sodium citrate, the tween 80
The adjuvant of described suppository is two or more in semi-synthetic fatty acid glyceride, cocoa butter, Cera Flava, Oleum Linderae, hydrogenation cotton seed, hydrogenated groundnut, hydrogenated coconut oil, glycerol, gelatin, Polyethylene Glycol, tween-61, polyoxyethylene stearate (40) ester, water-soluble chitosan, poloxamer, the tween 80
The preparation of treatment diarrheal pharmaceutical composition of the present invention, its preparation method is:
A. under the normal temperature and pressure with racecadotril and berberine hydrochloride mix homogeneously;
B. add adjuvant;
C. be prepared as required dosage form;
D. sterilization, packing.
Antidiarrheal preparation of the present invention is to be the preparation that primary raw material is made by racecadotril and berberine hydrochloride.Racecadotril is a kind of inhibitor of enkephalinase, and it is by suppressing the enkephalinase activity, and then suppresses power and water and separate the matter excessive secretion and bring into play its diarrhea effect.Berberine hydrochloride, promptly berberine all has strong bacteriostasis to causing diarrheal escherichia coli, Hemolytic streptococcus, Diplococcus pneumoniae, can also obviously suppress the rising of colonic smooth muscle intracellular calcium concentration simultaneously, improves the intestinal movement orthofunction.Scientific formulation of the present invention, rationally, adopt preparation for treating provided by the invention diarrhoea, can separate the matter excessive secretion, and can improve the intestinal movement function, suppress to cause that the excessive multiplication of diarrheal escherichia coli, Hemolytic streptococcus, Diplococcus pneumoniae reaches the antidiarrheal effect simultaneously by suppressing power and water.Racecadotril and berberine compatibility be used for the treatment of that diarrhoea has quick-acting, side effect and untoward reaction is few, do not cause dysbacteriosis in constipation and the body, be difficult for producing characteristics such as drug resistance, and all can be used for infant and adult's dissimilar diarrhea treatment.
Racecadotril of the present invention and berberine hydrochloride, behind 10mg:10mg, 30mg:300mg, three groups of ratio mixings of 60mg:600mg, add an amount of distilled water and give mouse stomach by the 0.4ml/10g body weight, every group 40, male and female half and half, the normal raising, observed 7 days, three groups all do not occur dead, its stool, urine, mental status, activity, hair color are all normal, the growth of body weight is also normal, and the oral toxic reaction that do not occur after racecadotril and berberine hydrochloride are by said ratio is described, clinical practice is safer.
Racecadotril and berberine hydrochloride in 10mg:10mg, 30mg:300mg, three groups of ratio mixings of 60mg:600mg after, add an amount of distilled water and give rat continuous use 3 months by the 2ml/100g body weight, every group 20, male and female half and half, the normal raising, 2 weeks of drug withdrawal get blood and carry out the related item inspection, the result shows: during the medication and after the drug withdrawal, three groups death all occurs, and its action, hair, body weight, appetite, routine blood test, blood fat, blood glucose, liver function and organ coefficient etc. do not have significant difference with matched group.The histological examination result shows: observe in the internal organs such as the heart of rat, liver, spleen, lung, kidney and examine no significant change, histological examination does not also have obvious change, illustrate that racecadotril and berberine hydrochloride are lower to rat prolonged application toxicity by said ratio, use safer.
Racecadotril and berberine hydrochloride are used for the rat model of Oleum Ricini diarrhea inducing by the 2ml/100g body weight after in 10mg:10mg, 30mg:300mg, three groups of ratio mixings of 60mg:600mg, the result shows: the total amount of defecating the every day of test group animal is 44.03%, 71.12%, 68.34% of a blank model group, its anti-diarrhea effect appears at after the medication about 40 minutes, anti-diarrhea effect and dosage are not dose-effect relationship, and the normal group of Oleum Ricini diarrhea inducing useless is not but had anti-diarrhea effect.Extracorporeal bacteria inhibitor test shows: three groups all have obvious bacteriostasis to escherichia coli, Hemolytic streptococcus, and are dose-effect relationship.
The specific embodiment
Below in conjunction with embodiment the present invention is done progressive explanation, but be not limited to embodiment.
Embodiment 1
Racecadotril 100g
Berberine hydrochloride 150g
Microcrystalline Cellulose 42.5g
Carboxymethylstach sodium 5g
Magnesium stearate 2.5g
Make 1000
Preparation method: with racecadotril, berberine hydrochloride, microcrystalline Cellulose mix homogeneously, granulate, granulate adds magnesium stearate, carboxymethylstach sodium mixing, and tabletting or coating operation bag film-coat routinely promptly get tablet or film coated tablet.Be used for the treatment of infantile diarrhea, a twice-daily, is fully recovered after 3 days treatment by each 1.
Embodiment 2
Racecadotril 30g
Berberine hydrochloride 150g
Starch 17.5g
Magnesium stearate 2.5g
Make 1000
Preparation method: with racecadotril, berberine hydrochloride, starch, magnesium stearate mix homogeneously, detection level is used the Capsules filling, promptly gets capsule.Be used for the treatment of adult diarrhea, three times on the one, each 2, after 2 days treatment, fully recover.
Embodiment 3
Racecadotril 30g
Berberine hydrochloride 25g
Sucrose 975g
Lactose 970
Make 1000 bags
Preparation method: with racecadotril, berberine hydrochloride, cane sugar powder, lactose mix homogeneously, make wetting agent with 40% ethanol, the system soft material is granulated, 70 ± 10 ℃ of dryings, and granulate, packing promptly gets granule.Be used for the treatment of gastroenteritis diarrhoea, three times on the one, each 1 bag, after 2 days treatment, fully recover.
Embodiment 4
Racecadotril 30g
Berberine hydrochloride 50g
Arabic gum 20g
Anhydride silica 20g
Citric acid 60g
Sodium citrate 80g
Sucrose 2730g
Tween 80 10g
Make 1000 bags
Preparation method: with racecadotril, berberine hydrochloride, cane sugar powder, arabic gum, citric acid, sodium citrate, anhydride silica, tween 80 mix homogeneously, make wetting agent, the system soft material with 40% ethanol, granulate 70 ± 10 ℃ of dryings, granulate, packing promptly gets dry suspension.Be used for the treatment of infantile diarrhea, three times on the one, each 1 bag, after 2 days treatment, fully recover.
Embodiment 5
Racecadotril 30g
Berberine hydrochloride 100g
Polyethylene Glycol 1790g
Tween 80 80g
Make 1000
Preparation method: racecadotril, berberine hydrochloride are added in the fused Polyethylene Glycol of 500g, and mix homogeneously adds tween 80 again, behind the mix homogeneously again with the fused Polyethylene Glycol mixing of remainder, pour in the preprepared bolt mould, treat condensation after, take out and promptly to get suppository.Be used for the treatment of the secretory diarrhea diarrhoea due to cholera toxin, the stable type colicine etc., three times on the one, each 2, after 2 days treatment, fully recover.
Claims (9)
1. treatment diarrheal pharmaceutical composition mainly is to be that the primary raw material preparation gets by racecadotril, berberine hydrochloride, it is characterized in that its proportioning raw materials is: 1 part of racecadotril, berberine hydrochloride 0.25-25 part, adjuvant 0.01-250 part.
2. treat the diarrheal drug combination preparation for one kind, it is characterized in that, with 1 part of racecadotril, berberine hydrochloride 0.25-25 part, adjuvant 0.01-250 part are prepared as a kind of in tablet, film coated tablet, capsule, soft capsule, granule, suspensoid, dry suspension, the suppository.
3. treatment diarrheal drug combination preparation according to claim 2 is characterized in that the adjuvant of described tablet, film coated tablet is two or more in microcrystalline Cellulose, starch, magnesium stearate, hypromellose, the carboxymethylstach sodium.
4. treatment diarrheal drug combination preparation according to claim 2 is characterized in that the adjuvant of described capsule is two or more in starch, microcrystalline Cellulose, carboxymethylstach sodium, magnesium stearate, the Capsules.
5. treatment diarrheal drug combination preparation according to claim 3 is characterized in that described soft capsule adjuvant is gelatin, glycerol.
6. treatment diarrheal drug combination preparation according to claim 3 is characterized in that the adjuvant of described granule is one or more in sucrose, mannitol, lactose, glucose, the aspartame.
7. treatment diarrheal drug combination preparation according to claim 3, it is characterized in that the adjuvant of described suspensoid, dry suspension is two or more in water, hypromellose, carmethose, arabic gum, tragakanta, gelatin, Polyethylene Glycol, anhydride silica, citric acid, sodium citrate, the tween 80.
8. treatment diarrheal drug combination preparation according to claim 3, it is characterized in that the adjuvant of described suppository is two or more in semi-synthetic fatty acid glyceride, cocoa butter, Cera Flava, Oleum Linderae, hydrogenation cotton seed, hydrogenated groundnut, hydrogenated coconut oil, glycerol, gelatin, Polyethylene Glycol, tween-61, polyoxyethylene stearate (40) ester, water-soluble chitosan, poloxamer, the tween 80.
9. treatment diarrheal drug combination preparation according to claim 2 is characterized in that its preparation method is:
A. under the normal temperature and pressure with racecadotril and berberine hydrochloride mix homogeneously;
B. add adjuvant;
C. be prepared as a kind of dosage form in tablet, film coated tablet, capsule, soft capsule, granule, suspensoid, dry suspension, the suppository;
D. sterilization, packing.。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010105637963A CN102018707A (en) | 2010-11-29 | 2010-11-29 | Medicinal composition for treating diarrhea and preparation thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010105637963A CN102018707A (en) | 2010-11-29 | 2010-11-29 | Medicinal composition for treating diarrhea and preparation thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102018707A true CN102018707A (en) | 2011-04-20 |
Family
ID=43860759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010105637963A Pending CN102018707A (en) | 2010-11-29 | 2010-11-29 | Medicinal composition for treating diarrhea and preparation thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102018707A (en) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140275246A1 (en) * | 2012-06-28 | 2014-09-18 | Mcneil-Ppc, Inc. | Racecadotril lipid compositions |
| CN104188919A (en) * | 2014-09-25 | 2014-12-10 | 河南亚卫动物药业有限公司 | Thiamphenicol powder dry suspension for livestock and preparation method of thiamphenicol powder dry suspension |
| CN104224724A (en) * | 2013-06-08 | 2014-12-24 | 北京韩美药品有限公司 | Racecadotril granules and preparation technology thereof |
| EP2918268A1 (en) * | 2014-03-10 | 2015-09-16 | Galenicum Health S.L. | Pharmaceutical compositions comprising an active agent |
| WO2017123485A1 (en) * | 2016-01-13 | 2017-07-20 | Johnson & Johnson Consumer Inc. | New improved composition comprising at least one cadotril |
| US10039712B2 (en) | 2012-06-28 | 2018-08-07 | Johnson & Johnson Consumer Inc. | Racecadotril lipid compositions |
| CN108853475A (en) * | 2018-09-29 | 2018-11-23 | 沈阳师范大学 | Antibacterial suppository of a kind of acidification enteron aisle and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1279946A (en) * | 2000-06-12 | 2001-01-17 | 昆明市延安医院 | Berberine hydrochloride suppository and its producing method |
| CN101103960A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Dry mixed suspension containing racecadotril and preparation method thereof |
| CN101442990A (en) * | 2006-05-15 | 2009-05-27 | 生物计划公司 | New form of administration of racecadotril |
-
2010
- 2010-11-29 CN CN2010105637963A patent/CN102018707A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1279946A (en) * | 2000-06-12 | 2001-01-17 | 昆明市延安医院 | Berberine hydrochloride suppository and its producing method |
| CN101442990A (en) * | 2006-05-15 | 2009-05-27 | 生物计划公司 | New form of administration of racecadotril |
| CN101103960A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Dry mixed suspension containing racecadotril and preparation method thereof |
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140275246A1 (en) * | 2012-06-28 | 2014-09-18 | Mcneil-Ppc, Inc. | Racecadotril lipid compositions |
| US9801819B2 (en) * | 2012-06-28 | 2017-10-31 | Johnson & Johnson Consumer Inc. | Racecadotril compositions |
| US10039712B2 (en) | 2012-06-28 | 2018-08-07 | Johnson & Johnson Consumer Inc. | Racecadotril lipid compositions |
| US20140271832A1 (en) * | 2013-03-15 | 2014-09-18 | Mcneil-Ppc, Inc. | Racecadotril lipid compositions |
| US9636300B2 (en) * | 2013-03-15 | 2017-05-02 | Johnson & Johnson Consumer Inc. | Racecadotril lipid compositions |
| CN104224724A (en) * | 2013-06-08 | 2014-12-24 | 北京韩美药品有限公司 | Racecadotril granules and preparation technology thereof |
| EP2918268A1 (en) * | 2014-03-10 | 2015-09-16 | Galenicum Health S.L. | Pharmaceutical compositions comprising an active agent |
| CN104188919A (en) * | 2014-09-25 | 2014-12-10 | 河南亚卫动物药业有限公司 | Thiamphenicol powder dry suspension for livestock and preparation method of thiamphenicol powder dry suspension |
| CN104188919B (en) * | 2014-09-25 | 2018-01-26 | 河南亚卫动物药业有限公司 | A kind of livestock and poultry Thiamphenicol dried bean noodles supensoid agent and preparation method thereof |
| WO2017123485A1 (en) * | 2016-01-13 | 2017-07-20 | Johnson & Johnson Consumer Inc. | New improved composition comprising at least one cadotril |
| CN108853475A (en) * | 2018-09-29 | 2018-11-23 | 沈阳师范大学 | Antibacterial suppository of a kind of acidification enteron aisle and preparation method thereof |
| CN108853475B (en) * | 2018-09-29 | 2021-06-18 | 沈阳师范大学 | Acidified intestinal bacteriostatic suppository and preparation method thereof |
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Application publication date: 20110420 |