CN1589793A - Application of tannic acid berberine in preparation of medicine for treating ulcero colonitis - Google Patents
Application of tannic acid berberine in preparation of medicine for treating ulcero colonitis Download PDFInfo
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- CN1589793A CN1589793A CN 200410054779 CN200410054779A CN1589793A CN 1589793 A CN1589793 A CN 1589793A CN 200410054779 CN200410054779 CN 200410054779 CN 200410054779 A CN200410054779 A CN 200410054779A CN 1589793 A CN1589793 A CN 1589793A
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- berberine tannate
- berberine
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Abstract
The invention relates to the application of tannic acid berberine in preparation of medicine for treating ulcero colonitis. The application dosage range is 0.1 to 3 g, preferably 0.3 to 1.5 g. The invention provides medicine combination for treating ulcero colonitis using tannic acid berberine as active ingredient, wherein the combination can be tablet, capsule, granule, colon release capsule or oral liquid, preferably colon release capsules.
Description
Technical field
The present invention relates to the application of berberine tannate in the medicine of preparation treatment ulcerative colitis.
Background technology
Ulcerative colitis (UC) is the very not clear and definite rectum of a kind of reason and the chronic inflammation disease of colon.Clinical in stomachache, diarrhoea, mucus or the bloody purulent stool of outbreak, protracted course of disease are feature repeatedly.Fibercolonscopy shows proctitis, proctosigmoiditis, a left side or right hemicolon inflammation, regional colitis, pancolitis and false polyp etc.
The inventor finds that by great deal of experimental berberine tannate has good therapeutical effect to ulcerative colitis.
Summary of the invention
The invention provides the application of berberine tannate in the medicine of preparation treatment ulcerative colitis, its application dose scope is 0.1-3g; The preferred dose scope is 0.3-1.5g.
The invention provides with the berberine tannate is the pharmaceutical composition of active component, its dosage unit is 0.05-1.0g, be preferably 0.15-0.3g, it can exist with the form of tablet, capsule, granule, oral liquid or colon release capsule, is preferably the colon release capsule.
Berberine tannate pharmaceutical composition provided by the invention can adopt pharmaceutically conventional preparation method to be prepared from.
The present invention understands that by the test illustration berberine tannate is in the purposes for preparing the medicine for the treatment of the soup colitis of bursting and the effect power of different dosage form.
The specific embodiment
Embodiment 1: berberine tannate colon release capsule (specification: 0.15g)
Prescription: berberine tannate 150.0g
Starch 32.0g
Carboxymethyl starch sodium 18.0g
3%PVP
K30Aqueous solution is an amount of
Make 1000 capsules altogether
Operation: cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, starch and carboxymethyl starch sodium of recipe quantity, add 3% PVP
K30Aqueous solution is made soft material in right amount, and 28 mesh sieves are granulated, about 3 hours of 60 ℃ of dryings, and 26 mesh sieve granulate are adorned colon colloidal sol capsule No. 1, regulate the about 200mg of loading amount, promptly.
Embodiment 2: berberine tannate colon release capsule (specification: 0.3g)
Prescription: berberine tannate 300.0g
Starch 32.0g
Carboxymethyl starch sodium 18.0g
3%PVP
K30Aqueous solution is an amount of
Make 1000 capsules altogether
Operation: cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, starch and carboxymethyl starch sodium of recipe quantity, add 3% PVP
K30Aqueous solution is made soft material in right amount, and 28 mesh sieves are granulated, about 3 hours of 60 ℃ of dryings, and 26 mesh sieve granulate are adorned colon colloidal sol capsule No. 00, regulate the about 350mg of loading amount, promptly.
Embodiment 3: berberine tannate colon release capsule (specification: 0.05g)
Prescription: berberine tannate 50.0g
Starch 32.0g
Carboxymethyl starch sodium 18.0g
3%PVP
K30Aqueous solution is an amount of
Make 1000 capsules altogether
Operation: cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, starch and carboxymethyl starch sodium of recipe quantity, add 3% PVP
K30Aqueous solution is made soft material in right amount, and 28 mesh sieves are granulated, about 3 hours of 60 ℃ of dryings, and 26 mesh sieve granulate are adorned colon colloidal sol capsule No. 4, regulate the about 100mg of loading amount, promptly.
Embodiment 4: berberine tannate tablet (specification 0.15g)
Prescription: berberine tannate 150.0g
Icing Sugar 35.0g
Carboxymethyl starch sodium 13.0g
3%PVP
K30Aqueous solution is an amount of
Magnesium stearate 2.0g
Make 1000 altogether
Cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, Icing Sugar, carboxymethyl starch sodium of recipe quantity, add 3%PVP
K30Aqueous solution is made soft material in right amount, and 20 mesh sieves are granulated, 60 ℃ of dryings 3 hours, and 18 mesh sieve granulate add the magnesium stearate of recipe quantity, φ 10mm scrobicula stamping behind the mix homogeneously, the heavily about 200mg of adjustment sheet, promptly.
Embodiment 5: berberine tannate tablet (specification 1.0g)
Prescription: berberine tannate 1000.0g
Icing Sugar 105.0g
Carboxymethyl starch sodium 39.0g
3%PVP
K30Aqueous solution is an amount of
Magnesium stearate 6.0g
Make 1000 altogether
Operation: cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, Icing Sugar, carboxymethyl starch sodium of recipe quantity, add the 3%PVPK30 aqueous solution and make soft material in right amount, 20 mesh sieves are granulated, 60 ℃ of dryings 3 hours, 18 mesh sieve granulate, the magnesium stearate of adding recipe quantity, φ 10mm scrobicula stamping behind the mix homogeneously, the heavily about 1200mg of adjustment sheet, promptly.
Embodiment 6: berberine tannate tablet (specification 0.5g)
Prescription: berberine tannate 500.0g
Icing Sugar 70.0g
Carboxymethyl starch sodium 26.0g
3%PVP
K30Aqueous solution is an amount of
Magnesium stearate 4.0g
Make 1000 altogether
Operation: cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, Icing Sugar, carboxymethyl starch sodium of recipe quantity, add the 3%PVPK30 aqueous solution and make soft material in right amount, 20 mesh sieves are granulated, 60 ℃ of dryings 3 hours, 18 mesh sieve granulate, the magnesium stearate of adding recipe quantity, φ 10mm scrobicula stamping behind the mix homogeneously, the heavily about 600mg of adjustment sheet, promptly.
Embodiment 7: berberine tannate tablet (specification 0.05g)
Prescription: berberine tannate 50.0g
Icing Sugar 135.0g
Carboxymethyl starch sodium 15.0g
3%PVP
K30Aqueous solution is an amount of
Magnesium stearate 2.0g
Make 1000 altogether
Operation: cross 100 mesh sieves after taking by weighing the abundant mix homogeneously of berberine tannate, Icing Sugar, carboxymethyl starch sodium of recipe quantity, add the 3%PVPK30 aqueous solution and make soft material in right amount, 20 mesh sieves are granulated, 60 ℃ of dryings 3 hours, 18 mesh sieve granulate, the magnesium stearate of adding recipe quantity, φ 10mm scrobicula stamping behind the mix homogeneously, the heavily about 200mg of adjustment sheet, promptly.
Test example 1, berberine tannate are to the effect of experimental rat ulcerative colitis
(1), the making of UC model and pathologic finding
Get 72 rats, body weight 220-250g, female, fasting 16 hours, 10% chloral hydrate anesthesia, abdomen is opened in the abdominal part sterilization, clamps with the bulldog clamp of sterilizing apart from returning the about 4 centimeters colons of cecum, colonic injects 7% acetic acid 1.0ml, uses the 5ml normal saline flushing after 15 seconds, sews up abdominal part.In second day random packet, 12 every group, be respectively berberine tannate colon administration group, berberine tannate is irritated the high, medium and low dosage group of stomach, sulfasalazine (SASP) group and model group (giving normal saline).Administering mode except that tannic acid berberine colon administration group from anum administration, other respectively organize gastric infusion.Administration volume: 1.0ml/200g.Below respectively organize and be administered once every day, successive administration 7 days, rat is put to death in the experiment back that finishes, and observes the degree of injury apart from anus 6～8cm place colon, and gets wherein 0.5cm pathological changes intestinal tissue with 4% formaldehyde fixed, the routine paraffin wax section, HE dyes and light microscopy checking.
(2), colonic mucosal injury index (CMDI) and histopathology scoring (HS) standard
Colonic mucosal injury index (CMDI): 0 minute: not damaged; 1 minute: mild hyperaemia, edema, surface light, no erosion or ulcer; 2 minutes: congestion and edema, the coarse granular sensation that is of mucosa has erosion or intestinal adhesion; 3 minutes: the height congestion and edema, there are necrosis and ulcer in the surface, the maximum vertical footpath＜1cm of ulcer, intestinal wall thickens or there are necrosis and inflammation in the surface; 4 minutes: the height congestion and edema, mucosal necrosis and ulcer, the maximum vertical footpath＞1cm of ulcer, or wall bowel necrosis, toxic megacolon cause death entirely.
Histopathology scoring (HS) standard: HS standard reference document also improves slightly: 1. acute inflammation cellular infiltration, 0 minute: do not have 1 fen: slightly increase by 2 fens: significantly increase; 2. chronic inflammation cellular infiltration, 0 minute: do not have 1 fen: slightly increase by 2 fens: significantly increase; 3. fibrin deposition, 0 minute: do not have 1 minute: have; 4. edema under the mucosa, 0 minute: do not have 1 minute: lamellar, 2 minutes: plocoid; 5. epithelium necrosis, 0 minute: do not have 1 fen: limitation, 2 minutes: extensively; 6. epithelium ulcer, 0 minute: do not have 1 minute: have.
(3), statistical procedures: all measurement datas are all represented with X ± S, relatively adopt the t check between group.
(4), result of the test
The result shows (table 1): rat the feces character promptly occurs and changes after acetic acid treatment, the seriality pathological changes of human ulcerative colitis appears being similar in colon, show as mucosa height congestion and edema, there are necrosis and ulcer in the surface, and part animal even generation toxic megacolon cause death.The mucosa pathological change shows as mucosa and the obvious edema of tela submucosa, fibrin precipitation, neutrophil infiltration, occurs epithelium necrosis and ulcer when serious.But berberine tannate is irritated stomach dose dependent ground and is alleviated the CMDI degree of acetic acid colitis rat, and the rat colon of improvement mucosa pathology damaging action is arranged, and shows that the rat colon mucosa injury that acetic acid is caused has significant protective effect.Berberine tannate colon administration group dosage and berberine tannate gastric infusion low dose group dosage identical (being 75mg/kg), and pharmacodynamics effect and berberine tannate gastric infusion high dose group (300mg/kg) are suitable.
Table 1 berberine tannate is to the influence of experimental rat ulcerative colitis
Group dosage (mg/kg) CMDI HS
Model group 2.91 ± 0.67 4.25 ± 0.78
5-ASA 100 1.52±0.93 3.20±0.51
Berberine tannate colon administration group 75 1.20 ± 0.35
*3.21 ± 1.06
*
Berberine tannate is irritated stomach high dose group 300 1.11 ± 0.38
*3.12 ± 1.16
*
Berberine tannate is irritated dosage group 150 1.78 ± 0.89 in the stomach
*3.40 ± 1.10
*
Berberine tannate is irritated stomach low dose group 75 2.63 ± 0.84 3.84 ± 1.8
Annotate:
*P＜0.05,
*Compare with model group P＜0.01.
The different preparation administrations of test example 2, berberine tannate are to the effect of ulcerative colitis
Selection is through fibercolonscopy, and clinical diagnosis is ulcerative colitis patient 60 examples (age 35-50 years), is divided into 3 groups at random, every group 20 example, and the administration cycle is 1 month.The 1st group gives berberine tannate common oral preparation (tablet), and dosage is 0.9g, tid; The 2nd group gives berberine tannate colon enteric coated capsule, dosage 0.3g, tid; The 3rd group gives Olsalazine, 0.5g, tid.All capable colonoscopy before and after the administration.
The therapeutic effect evaluation of ulcerative colitis: 1. alleviate fully: line up shape stool≤3 times every day, no hemafecia, body temperature is normal, and the General Symptoms of ulcerative colitis disappears, lab testing is roughly normal, and the microscopically that colonoscope reaches biopsy down shows the evidence that does not all have acute and chronic inflammation; 2. part is alleviated: above each point all has improvement in various degree, does not alleviate but reach fully; 3. state of an illness no change: does not promptly all have obviously change under the clinical and colonoscope before and after the treatment; 4. sb.'s illness took a turn for the worse: performance further increases the weight of under the clinical and colonoscope in treatment back.
During therapeutic evaluation, add up with invalid (comprise and treat back state of an illness no change or deterioration) according to treatment effective (alleviating fully or the part alleviation after comprising treatment).The result shows, effective 8 examples of oral common berberine tannate preparation (tablet) group, invalid 12 examples; Oral berberine tannate colon enteric coated capsule group, effective 18 examples, invalid 2 examples; Oral Olsalazine group, effective 16 examples, invalid 4 examples.Untoward reaction does not all appear in oral berberine tannate ordinary preparation and berberine tannate colon enteric coated capsule group; Oral Olsalazine group, feeling sick appears in 3 examples, and 1 example diarrhoea occurs and increases the weight of.
Above result shows that berberine tannate is an effectively medicine of treatment ulcerative colitis.Its therapeutic effect is relevant with the partial drug level of ulcer.Oral berberine tannate colon enteric coated capsule has better therapeutic effect to ulcerative colitis.The berberine tannate colon administration obviously is better than oral ordinary preparation to the curative effect of ulcerative colitis; And there is not tangible untoward reaction.
Claims (7)
1. the application of berberine tannate in the medicine of preparation treatment ulcerative colitis.
2. application according to claim 1, its using dosage scope is 0.1-3g.
3. application according to claim 2, its preferred using dosage scope is 0.3-1.5g.
4. be the pharmaceutical composition of active component with the berberine tannate, its dosage unit is 0.05-1.0g.
5. pharmaceutical composition according to claim 4, its dosage unit is preferably 0.15-0.3g.
6. according to claim 4 or 5 described pharmaceutical compositions, it can exist with the form of tablet, capsule, granule, oral liquid or colon release capsule.
7. pharmaceutical composition according to claim 6, it is preferably the colon release capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410054779 CN1589793A (en) | 2003-07-24 | 2004-07-21 | Application of tannic acid berberine in preparation of medicine for treating ulcero colonitis |
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|---|---|---|---|
| CN03132959 | 2003-07-24 | ||
| CN03132959.4 | 2003-07-24 | ||
| CN 200410054779 CN1589793A (en) | 2003-07-24 | 2004-07-21 | Application of tannic acid berberine in preparation of medicine for treating ulcero colonitis |
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| CN1589793A true CN1589793A (en) | 2005-03-09 |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014530883A (en) * | 2011-10-24 | 2014-11-20 | インスティチュート オブ マテリア メディカ，チャイニーズ アカデミー オブ メディカル サイエンシズ | Protoberberine biological alkaloid derivatives and their use to inhibit ulcerative colitis |
| CN104211709A (en) * | 2013-05-29 | 2014-12-17 | 中国医学科学院药物研究所 | Coptisine alkaloid derivatives and application thereof on preventing ulcerative colitis |
| CN107125461A (en) * | 2016-02-29 | 2017-09-05 | 湖南晶天科技实业有限公司 | A kind of feed addictive enteric coating tannin acid derivative and a kind of feed |
| CN109464417A (en) * | 2018-12-19 | 2019-03-15 | 中国药科大学 | A kind of demethyleneberberinehydrochloride hydrochloride capsulae enterosolubilis and preparation method thereof |
| US20210032265A1 (en) * | 2012-04-16 | 2021-02-04 | Case Western Reserve University | Compositions and methods of modulating 15-pgdh activity |
| US11690847B2 (en) | 2016-11-30 | 2023-07-04 | Case Western Reserve University | Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof |
| US11718589B2 (en) | 2017-02-06 | 2023-08-08 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase |
-
2004
- 2004-07-21 CN CN 200410054779 patent/CN1589793A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2014530883A (en) * | 2011-10-24 | 2014-11-20 | インスティチュート オブ マテリア メディカ，チャイニーズ アカデミー オブ メディカル サイエンシズ | Protoberberine biological alkaloid derivatives and their use to inhibit ulcerative colitis |
| EP2789612A4 (en) * | 2011-10-24 | 2015-12-16 | Inst Materia Medica Cams | Derivatives of protoberberine biological alkaloids and use of same inhibiting ulcerative colitis |
| US20210032265A1 (en) * | 2012-04-16 | 2021-02-04 | Case Western Reserve University | Compositions and methods of modulating 15-pgdh activity |
| CN104211709A (en) * | 2013-05-29 | 2014-12-17 | 中国医学科学院药物研究所 | Coptisine alkaloid derivatives and application thereof on preventing ulcerative colitis |
| CN104211709B (en) * | 2013-05-29 | 2018-09-25 | 中国医学科学院药物研究所 | The purposes of coptisine Alkaloid derivative and its anti-ulcerative colitis |
| CN107125461A (en) * | 2016-02-29 | 2017-09-05 | 湖南晶天科技实业有限公司 | A kind of feed addictive enteric coating tannin acid derivative and a kind of feed |
| US11690847B2 (en) | 2016-11-30 | 2023-07-04 | Case Western Reserve University | Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof |
| US11718589B2 (en) | 2017-02-06 | 2023-08-08 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase |
| CN109464417A (en) * | 2018-12-19 | 2019-03-15 | 中国药科大学 | A kind of demethyleneberberinehydrochloride hydrochloride capsulae enterosolubilis and preparation method thereof |
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