CN104546848A - Medicine for treating colitis - Google Patents
Medicine for treating colitis Download PDFInfo
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- CN104546848A CN104546848A CN201410719512.3A CN201410719512A CN104546848A CN 104546848 A CN104546848 A CN 104546848A CN 201410719512 A CN201410719512 A CN 201410719512A CN 104546848 A CN104546848 A CN 104546848A
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- hydrochloric acid
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- colitis
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- acid raceanisodamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to the technical field of medicines, and provides application of hydrochloric acid racanisodamine in preparing medicines for treating colitis, particularly ulcerative colitis. The animal experiment shows that hydrochloric acid racanisodamine can remarkably reduce disease activity indexes of mouse colitis induced by DSS, weight loss is alleviated, the degree of colon shortening is reduced, and the pathological change of colon tissue is improved. A new method for clinical treatment on colitis is provided.
Description
Technical field
The present invention relates to medical art, be specifically related to a kind of medicine for the treatment of colitis, this medicine is Hydrochloric acid raceanisodamine.
Background technology
Hydrochloric acid raceanisodamine, chemical name: (±)-6 β-Qiang Ji – 1 α H, 5 α H – Tuo Wan – 3 α – alcohol tropates, medicine is called: 654,654-1,654-2, English name: Anisodamine, molecular formula C
17h
23nO
4, molecular weight 305.38, anticholinergic agent, can make smooth muscle loosening, and remove vasospasm and therefore have analgesic effect, patent medicine has tablet and injection.Multiplex injection clinically, because oral absorption is poor.Bibliographical information Hydrochloric acid raceanisodamine also can be used for treating following disease:
1. vertebral disc infection: as (need share with antibacterials) such as fulminant type epidemic cerebrospinal meningitis, toxic dysenterys;
2. vascular illness: cerebral thrombosis, cerebral embolism, paralysis, cerebral vasospasm, angioneurotic headache, thromboangiitis obliterans etc.;
3. various neuralgia: as trigeminal neuralgia, sciatica etc.;
4. smooth muscle spasm: taste-blindness rate, biliary spasm etc.;
5. dizziness;
6. optical fundus illness: central serous chorioretinopathy, retinitis pigmentosa, arteria retina thrombosis etc.;
7. sudden deafness: coordinate new acupuncture can treat other deafnesses (low dose of acupoint injection therapy).
The cause of disease of ulcerative colitis is still failed to understand so far, thinks that allogenic material causes the result of host response, gene and Immunological Effect triple interaction at present.
Bloody diarrhea is the modal early symptom of ulcerative colitis, other symptoms have stomachache successively, have blood in stool, lose weight, tenesmus, vomiting etc.Main manifestations is arthritis, iridocyclitis, hepatic insufficiency and dermatosis once in a while.In most patient, primary disease shows as chronic, low pernicious, in the process that acute, calamity are broken out in a few patients (accounting for 15%).
Treatment of ulcerative colitis means comprise medical treatment and surgical operation, and medical treatment is mainly
(1) lie up and whole body Supporting Therapy comprise balance of fluid and electrolyte, to note simultaneously protein supplement, improve nutrition of whole body situation, have anemia person to give blood transfusion.
(2) Drug therapy 1. sulfasalazine Salicylic Acid Formulations be primary treatment medicine, as Etiasa, mesalazine etc.2. corticosteroid common medicine is prednisone or dexamethasone, but does not think that the maintenance of long-term hormone can prevent recurrence at present.3. the value of immunosuppressant in ulcerative colitis still belongs to suspicious.4. treatment by Chinese herbs diarrhea-type ulcerative colitis can use traditional Chinese medical herbal treatment, and effectiveness comparison is desirable.Should be careful in one's diet and living habit simultaneously.
For fulminant type and the patient that is in a bad way, as the case of medical treatment poor effect, operative treatment can be considered.
The mouse colitis of DSS induction, it is the Animal Model of Ulcerative Colitis of this area accreditation, list of references: Stefan Wirtz.et al.Chemically induced mouse models of intestinalinflammation.Nature Protolols 2,541-546.NO.3 (2007).
Hydrochloric acid raceanisodamine is used for the treatment of taste-blindness rate, and pharmacological action is relaxing smooth muscle.Because taste-blindness rate mainly hydrochloric acid secretion too much and helicobacter pylori infections, cause harmonization of the stomach duodenal mucosa even muscle layer also invaded, patient's main manifestations is rest pain under xiphoid-process, and time hungry, gastrointestinal peristalsis increases, and patient pain is obvious.In and gastric acid or feed can alleviating pain.And ulcerative colitis is mainly due to the inflammatory reaction that immunity causes, patient's main manifestations for suffering from abdominal pain, have blood in stool, lose weight, tenesmus, vomiting etc.Treatment is main based on Salicylates, hormones and immunosuppressant.No matter clinical manifestation, pathogenesis, therapeutic scheme etc. are all different for taste-blindness rate and ulcerative colitis.
Chinese patent CN99123843.5, application publication number: CN1295858A, disclose a kind of preparation method for the treatment of ulcerative colitis medicine, the ulcerative colitis medicine wherein related to is a large compound recipe combined by Chinese crude drug, Chinese patent medicine and Western medicine, Chinese medicine: lucky 15 grams of sky, Bai Haiweng 15 grams, Conch Meretricis seu Cyclinae 15 grams, Radix Scutellariae 15 grams, Rhizoma Coptidis 15 grams, Cortex Phellodendri 15 grams, Indigo Naturalis 15 grams; Chinese patent medicine: XILEI SAN 1.5 grams, YUNNAN BAIYAO 2.0 grams, Fu Xinna 10 grams, dioctahedral smectite 6 grams; Western medicine: 2% lignocaine 0.4 gram, 'Compound berberine pin 10ml, 10 milligrams, dexamethasone pin, 20 milligrams, chlorphenamine pin, cimetidine 0.6 gram, gentamycin pin 240,000 unit, Anisodamine 15 milligrams.This patent documentation Radix Anisodi Tangutici alkali number used is considerably less, and what effect Anisodamine plays actually and all do not relate in so large compound recipe.
There is no at present about the Hydrochloric acid raceanisodamine bibliographical information relevant to colitis, particularly ulcerative colitis.
Summary of the invention
The object of the invention is to the new medical usage studying Hydrochloric acid raceanisodamine.
The invention provides the application of Hydrochloric acid raceanisodamine in preparation treatment colitis medicine, described medicine is that Hydrochloric acid raceanisodamine is as sole active composition.
The application of Hydrochloric acid raceanisodamine of the present invention in preparation treatment colitis medicine, described colitis is ulcerative colitis.
The application of Hydrochloric acid raceanisodamine of the present invention in preparation treatment colitis medicine, in described medicine, the content of Hydrochloric acid raceanisodamine is 0.1-99.9wt%.Be preferably 0.5-90wt%.
The application of Hydrochloric acid raceanisodamine of the present invention in preparation treatment colitis medicine, described medicine is decoction, powder, pill, medicated wine, lozenge, colloid, plaster, medicinal tea, herbal leaven, cake agent, distillate medicinal water, stick, line agent, medicated roll, nail agent, agent is pressed in moxibustion, unguentum, sublimed preparation, microencapsulation, vein emulsion, Liposomal formulation, aerosol, precursor medicine preparation, injection, mixture, peroral ampule agent, tablet, capsule, drop pill, Emulsion, ointment, rubber plaster, membrane, sponginum, ionophore, or cutaneous permeable agent.It is preferably injection.
The present invention confirms by experiment, and Hydrochloric acid raceanisodamine obviously can alleviate the disease activity index of the mouse colitis of DSS induction, reduces the degree losing weight and shorten with colon.Wherein the prevention of 50mg/kg Hydrochloric acid raceanisodamine or therapeutic administratp significantly can alleviate the disease activity index of mouse colitis, improve Mouse Weight alleviate with colon shorten effect also clearly, and 25mg/kg Hydrochloric acid raceanisodamine has some improvement in body weight change and colon lengths, 12.5mg/kg Hydrochloric acid raceanisodamine also can alleviate the degree that colon shortens.
Beneficial effect of the present invention is as follows: Hydrochloric acid raceanisodamine is as conventional medicament, and toxic and side effects is little; Simple synthetic method is easy to get.The present invention is that the clinical treatment of colitis provides new means.
Accompanying drawing explanation
Fig. 1 is the impact of Hydrochloric acid raceanisodamine on ulcerative colitis mouse disease activity index, wherein A is the disease activity index of mice every day, B is the area under curve of disease activity index, * P<0.05 vs DSS group, * * P<0.01 vs DSS group.
Fig. 2 is the impact of Hydrochloric acid raceanisodamine on ulcerative colitis Mouse Weight, * P<0.05 vs DSS group, * * P<0.01 vs DSS group.
Fig. 3 is the impact of Hydrochloric acid raceanisodamine on ulcerative colitis mouse Colon length, wherein A is the change of colon lengths numerical value, wherein 12.5,25, the prevention administration of 50mg/kg Hydrochloric acid raceanisodamine and 50mg/kg Hydrochloric acid raceanisodamine therapeutic administratp all can suppress the colon of ulcerative colitis mice to shorten degree, * P<0.05 vs DSS group, * * P<0.01 vs DSS group; B is the representational colon picture of model group and treatment group.
Fig. 4 is the impact of Hydrochloric acid raceanisodamine on the pathological change of ulcerative colitis mouse Colon, and wherein A is each group of representational pathological tissue picture, and B is the histological scores of colon's damage, * * P<0.01 vsDSS group.
Detailed description of the invention
Now in conjunction with the accompanying drawings and embodiments, the present invention is described in detail, but enforcement of the present invention is not limited only to this.
The experimental technique of unreceipted actual conditions in the following example, usually conveniently condition, or according to the condition that manufacturer advises.Unless otherwise indicated, otherwise percentage ratio and number calculate by weight.
The Hydrochloric acid raceanisodamine crude drug that the present embodiment is used, purchased from Hangzhou Fu Ma Chemical Co., Ltd., is dissolved in normal saline by Hydrochloric acid raceanisodamine crude drug, be made into 12.5 respectively, 25,50mg/ml, respectively to mouse peritoneal injection 0.1ml/10g body weight.
Embodiment 1: Hydrochloric acid raceanisodamine is on the impact of ulcerative colitis mouse disease activity index
Test medicine Hydrochloric acid raceanisodamine is divided into five groups (n=10): 12.5mg/kg, 25mg/kg, 50mg/kg prevent administration and 50mg/kg therapeutic.Prevention administration is for feeding just to Hydrochloric acid raceanisodamine water first day from DSS, one day twice gavage, therapeutic then starts to Hydrochloric acid raceanisodamine for feeding water from DSS the 3rd day, one day twice gavage.Negative control group is with isopyknic normal saline gavage.
The mode inducing mouse adopting 3%DSS to feed water produces the model of ulcerative colitis, then gives Hydrochloric acid raceanisodamine according to above dosage and mode respectively and treats, then observe the state of mice every day.
Disease activity index (DAI) is assessed in such a way: DAI is stool hardness and intestinal bleeding scoring sum.Specific as follows: for feces, be normally 0 point, soft but keep shape be 1 point, very soft is 2 points, and diarrhoea is 3 points; For hemorrhage, negative 0 point of occult blood experiment, the occult blood experiment positive is 1 point, and feces is 2 points with blood stain, and hemorrhage of rectum is 3 points.
Result is as shown in Figure 1A, B, after DSS modeling there is hemafecia in mice, diarrhoea, Hydrochloric acid raceanisodamine is preventative gives various dose (12.5,25,50mg/kg) all can alleviate mouse disease activity index, wherein 25 and 50mg/kg Be very effective, therapeutic gives 50mg/kg Hydrochloric acid raceanisodamine also can reduce its disease activity index.
Embodiment 2: Hydrochloric acid raceanisodamine is on the impact of ulcerative colitis Mouse Weight
Test medicine, mouse model structure, administering mode are with embodiment 1.
Body weight with first day for 100%, the change of body weight calculates with hundred-mark system on this basis.
Result as shown in Figure 2, Mouse Weight continuous decrease after DSS modeling, various dose Hydrochloric acid raceanisodamine prevention or therapeutic after can lose weight decline degree, wherein 25,50mg/kg effects are better.
Embodiment 3: Hydrochloric acid raceanisodamine is on the impact of ulcerative colitis mouse Colon length
Test medicine, mouse model structure, administering mode are with embodiment 1.
Put to death mice after 6 days, take out colon, measure length.
Result is as shown in Fig. 3 A, B, and can cause colitis after DSS modeling, intestinal wall is thinning, finally causes colon lengths to shorten, can the shortening of suppression colon in various degree after Hydrochloric acid raceanisodamine treatment, wherein 25,50mg/kg Be very effective.
Embodiment 4: Hydrochloric acid raceanisodamine is on the impact of ulcerative colitis mouse Colon pathological change
Test medicine, mouse model structure, administering mode are with embodiment 1.
Put to death mice after 6 days, take out colon, from the intestinal segment cutting 0.5cm length near rectum end, 4% paraformaldehyde is fixed, paraffin embedding afterwards, the change of gut wall structure is observed in HE dyeing, and marks: what NIP showed is 0 point, the comparatively subinflammation of fragmentary monocyte infiltration is 1 point, the moderate inflammation of the monocyte infiltration of multiple point is 2 minutes, blood vessel hyperplasia, and the thinning hyperphlogosis of intestinal wall is 3 points, the leukocyte infiltration of saturating wall, it is 4 points that goblet cell disappears.
Result, as shown in Fig. 4 A, B, can cause mucous membrane of colon body of gland arrangement disorder after DSS modeling, basement membrane fracture or disappearance, and various inflammatory cells infiltrates, and crypt abscess is formed, submucosal edema and fibrosis.After Anisodamine In The Treatment, above-mentioned change alleviates.
Below the preferred embodiment of the invention is illustrated, but the invention is not limited to described embodiment, those of ordinary skill in the art also can make all equivalent modification or replacement under the prerequisite without prejudice to the invention spirit, and these equivalent modification or replacement are all included in the application's claim limited range.
Claims (4)
1. the application of Hydrochloric acid raceanisodamine in preparation treatment colitis medicine, it is characterized in that, described medicine is that Hydrochloric acid raceanisodamine is as sole active composition.
2. the application of Hydrochloric acid raceanisodamine according to claim 1 in preparation treatment colitis medicine, it is characterized in that, described colitis is ulcerative colitis.
3. the application of Hydrochloric acid raceanisodamine according to claim 1 and 2 in preparation treatment colitis medicine, it is characterized in that, in described medicine, the content of Hydrochloric acid raceanisodamine is 0.1-99.9wt%.
4. the application of Hydrochloric acid raceanisodamine according to claim 1 and 2 in preparation treatment colitis medicine, it is characterized in that, described medicine is decoction, powder, pill, medicated wine, lozenge, colloid, plaster, medicinal tea, herbal leaven, cake agent, distillate medicinal water, stick, line agent, medicated roll, nail agent, agent is pressed in moxibustion, unguentum, sublimed preparation, microencapsulation, vein emulsion, Liposomal formulation, aerosol, precursor medicine preparation, injection, mixture, peroral ampule agent, tablet, capsule, drop pill, Emulsion, ointment, rubber plaster, membrane, sponginum, ionophore, or cutaneous permeable agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410719512.3A CN104546848A (en) | 2014-12-01 | 2014-12-01 | Medicine for treating colitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410719512.3A CN104546848A (en) | 2014-12-01 | 2014-12-01 | Medicine for treating colitis |
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|---|---|
| CN104546848A true CN104546848A (en) | 2015-04-29 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410719512.3A Pending CN104546848A (en) | 2014-12-01 | 2014-12-01 | Medicine for treating colitis |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107998463A (en) * | 2017-12-21 | 2018-05-08 | 张楷乐 | A kind of relieving spasm and pain lubricating gel |
| CN110742889A (en) * | 2019-11-25 | 2020-02-04 | 镇江星盘商务咨询有限公司 | Medicine for treating colitis |
-
2014
- 2014-12-01 CN CN201410719512.3A patent/CN104546848A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| 叶仁高等: "《叶仁高内科手册》", 31 January 2004 * |
| 孙清杰: "甲硝唑及山莨菪碱治疗溃疡性结肠炎38例", 《新消化病学杂志》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107998463A (en) * | 2017-12-21 | 2018-05-08 | 张楷乐 | A kind of relieving spasm and pain lubricating gel |
| CN110742889A (en) * | 2019-11-25 | 2020-02-04 | 镇江星盘商务咨询有限公司 | Medicine for treating colitis |
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Application publication date: 20150429 |
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