阅读说明：本技术 一种治疗结肠炎的药物 (Medicine for treating colitis ) 是由 刘冲 张静静 于 2019-11-25 设计创作，主要内容包括：本发明公开了一种治疗结肠炎的药物,属于医药技术领域。本发明公开了一种治疗结肠炎的药物,该药物中消旋山莨菪碱和新斯的明的质量比为500：1；消旋山莨菪碱作为传统药物,合成方法简便易得,与新斯的明联合应用,治疗作用增强,毒副作用减小,克服了药物单独应用副作用大的缺点,本发明为结肠炎的临床治疗提供了新的手段。(The invention discloses a medicine for treating colitis, and belongs to the technical field of medicines. The invention discloses a medicament for treating colitis, wherein the mass ratio of racanisodamine to neostigmine in the medicament is 500: 1; the racanisodamine is used as a traditional medicine, the synthesis method is simple and easy to obtain, the racanisodamine is combined with neostigmine for application, the treatment effect is enhanced, the toxic and side effect is reduced, the defect of large side effect caused by the independent application of the medicine is overcome, and the invention provides a new means for the clinical treatment of the colitis.)

1. The medicine for treating colitis is characterized in that the mass ratio of racanisodamine to neostigmine in the medicine is 500: 1.

2. a medicament as claimed in claim 1, wherein the colitis is ulcerative colitis.

3. The pharmaceutical composition of claim 1 or 2, wherein the pharmaceutical composition is in the form of decoction, powder, pill, medicated wine, lozenge, gum, plaster, medicated tea, yeast, cake, lotion, stick, thread, strip, nail, moxibustion, ointment, pellet, microcapsule, intravenous emulsion, liposome preparation, aerosol, prodrug preparation, injection, mixture, oral ampoule, tablet, capsule, drop pill, emulsion, ointment, rubber plaster, membrane, sponge, iontophoresis agent, or transdermal absorbent.

Technical Field

The invention relates to the technical field of medicines, in particular to a medicine for treating colitis.

Background

Racanisodamine, chemical name (+ -) -6 β -hydroxy-1 α H, 5 α H-tropane-3 α -alcohol tropine ester, alias of drug is 654, 654-1, 654-2, English name is Anisodamine, molecular formula C₁₇H₂₃NO₄The molecular weight is 305.38, the anisodamine belongs to a choline receptor blocker, but compared with the atropine, the anisodamine has weak pharmacological action and lower toxicity and adverse reaction, so the anisodamine is more commonly used than the atropine clinically, can relax smooth muscle and relieve vasospasm, and can be used for treating ① infection toxic shock:such as epidemic cerebrospinal meningitis and toxic dysentery (combined with antibacterial agent), ② vascular diseases such as cerebral thrombosis, cerebral embolism, paralysis, cerebral vasospasm, angioneurotic headache, thromboangiitis obliterans, ③ neuralgia such as trigeminal neuralgia and sciatica, ④ smooth muscle spasm, gastric ulcer, duodenal ulcer, biliary tract spasm, ⑤ vertigo, ⑥ fundus diseases such as central retinitis, retinitis pigmentosa and retinal artery thrombosis, ⑦ sudden deafness, and can be used for treating other deafness (small-dose acupoint injection) by matching with new needle therapy.

Neostigmine is an artificially synthesized substitute for physostigmine, under the chemical name: n, N, N-trimethyl-3- [ (dimethylamino) formyloxy group]Anilinium, english name: neostigmine, molecular formula C₁₂H₁₉N₂O₂The molecular weight of the compound is 223.30, the compound has cholinesterase resisting effect, can be used for ① treatment of myasthenia gravis and can be used as a diagnosis medicine of the myasthenia gravis and can reverse the neuromuscular blockade effect of a non-depolarizing neuromuscular blocking medicine, ② treatment of glaucoma, intraocular pressure reduction, optic atrophy, juvenile pseudomyopia and the like, ③ treatment of paralytic intestinal obstruction and postoperative urine retention, ④ is used as a detoxifying medicine for snake venom (nerve toxicity) poisoning and tetrodotoxin poisoning, and ⑤ is used as an antagonist of a non-depolarizing muscle relaxant such as tubocurarine and the like.

The etiology of ulcerative colitis has not yet been clarified, and it is now thought that exogenous substances cause interactions among host responses, genes, and immune influences. Bloody diarrhea is the most common early symptom of ulcerative colitis, and other symptoms are abdominal pain, hematochezia, weight loss, tenesmus, vomiting and the like in sequence. Occasionally, arthritis, iridocyclitis, liver dysfunction and skin lesions are mainly manifested. The disease manifests itself in chronic, low malignancy in most patients and in acute, catastrophic outbreaks in a few patients (about 15%).

The therapeutic means of ulcerative colitis include medical treatment and surgical operation, the medical treatment mainly comprises (1) bed rest and whole body support treatment including liquid and electrolyte balance, attention is paid to protein supplement, whole body nutrition status is improved, anemia patients can be transfused with blood, (2) drug treatment, ① salicylic acid sulfasalazine salicylic acid preparation is main therapeutic drug, such as adisa, mesalazine and the like, ② corticosteroid is usually strong pine or dexamethasone, but long-term hormone maintenance is not considered to prevent recurrence at present, ③ immunosuppressant has doubtful value in ulcerative colitis, ④ traditional Chinese medicine preparation, such as white atractylodes rhizome powder, dark plum pills and traditional Chinese medicine enema has certain curative effect on ulcerative colitis, ⑤ flora transplantation can obviously improve the clinical remission rate of partial patients, attention is paid to diet and habit life, and colon resection operation can be adopted for patients who have uncontrolled bleeding, perforation or are about to have perforation and patients who have ulcerative colitis and are treated with colonic resection.

At present, the medicines for treating colitis, in particular ulcerative colitis, have the problems of large dosage, obvious side effect and the like. Therefore, providing a medicament for treating colitis is a problem that those skilled in the art need to solve urgently.

Disclosure of Invention

In view of the above, the invention provides a medicine for treating colitis, which not only avoids the problems of large dosage and the like caused by the single use of racanisodamine, but also avoids the side effects of the single use of neostigmine on the cardiovascular system and the digestive system.

In order to achieve the purpose, the invention adopts the following technical scheme:

a medicine for treating colitis is provided, wherein the mass ratio of racanisodamine to neostigmine in the medicine is 500: 1.

further, the colitis is ulcerative colitis.

Further, the dosage form of the medicine is decoction, powder, pill, medicated wine, lozenge, gum, plaster, medicated tea, starter, cake preparation, lotion, stick, thread, stick, nail, moxibustion, paste, pellet, microcapsule, intravenous emulsion, liposome preparation, aerosol, prodrug preparation, injection, mixture, oral ampoule, tablet, capsule, drop pill, emulsion, ointment, rubber plaster, membrane, sponge, iontophoresis agent, or transdermal absorbent. Preferably an injection.

The racanisodamine is used for treating gastric ulcer and duodenal ulcer, has the main functions of relaxing smooth muscle and relieving gastrointestinal colic caused by enteritis, and is symptomatic treatment. Gastrointestinal colic is a clinical symptom of ulcerative colitis, is an expression of ulcerative colitis, and is not a cause of ulcerative colitis, the cause of ulcerative colitis includes related factors such as immunity, inflammation, environment, heredity and the like, and patients mainly show abdominal pain, hematochezia, weight loss, tenesmus, vomiting and the like. The treatment mainly comprises salicylic acid medicines, hormones and immunosuppressants. Gastric and duodenal ulcers are different from ulcerative colitis in clinical manifestations, pathogenesis and treatment scheme.

According to the technical scheme, compared with the prior art, the invention discloses a medicine for treating colitis, wherein the mass ratio of racanisodamine to neostigmine in the medicine is 500: 1; the racanisodamine is used as a traditional medicine, the synthesis method is simple and easy to obtain, the racanisodamine is combined with neostigmine for application, the treatment effect is enhanced, the toxic and side effect is reduced, the defect of large side effect caused by the independent application of the medicine is overcome, and the invention provides a new means for the clinical treatment of the colitis.

Drawings

In order to more clearly illustrate the embodiments of the present invention or the technical solutions in the prior art, the drawings used in the description of the embodiments or the prior art will be briefly described below, it is obvious that the drawings in the following description are only embodiments of the present invention, and for those skilled in the art, other drawings can be obtained according to the provided drawings without creative efforts.

FIG. 1 is a graph showing the effect of the combined use of racanisodamine and neostigmine of the present invention on the disease activity index of mice with ulcerative colitis,. P <0.05,. P < 0.01;

FIG. 2 is a graph showing the effect of the combined use of racanisodamine and neostigmine of the present invention on the body weight of mice with ulcerative colitis,. P <0.05,. P < 0.01;

FIG. 3 is a graph showing the effect of the combined use of racanisodamine and neostigmine on the length of the colon in mice with ulcerative colitis, specifically the change in the value of the length of the colon, P <0.01vs normal group; # P <0.05vs model group, # P <0.01vs model group;

FIG. 4 is a diagram showing the effect of the combined use of racanisodamine and neostigmine on the length of the colon in mice with ulcerative colitis, specifically, representative colon pictures in the normal, model and treatment groups;

wherein, 1. normal group; 2. a model group; 3. anisodamine 5mg/kg + neostigmine 10 μ g/kg; 4. anisodamine 10mg/kg + neostigmine 20 μ g/kg; 5. anisodamine 20mg/kg + neostigmine 40 μ g/kg;

FIG. 5 is a drawing showing the effect of the combined application of racanisodamine and neostigmine on the pathological changes of the colon of mice with ulcerative colitis, specifically, representative pathological tissue pictures of each group;

FIG. 6 is a graph showing the effect of the combined use of racanisodamine and neostigmine on pathological changes in the colon of mice with ulcerative colitis, specifically, the pathological score of the lesions in the colon tissue, P <0.01vs normal group; # P <0.05vs model group.

Detailed Description

The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the drawings in the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.

The experimental procedures, in which specific conditions are not noted in the following examples, are generally carried out under conventional conditions or conditions recommended by the manufacturers. Unless otherwise indicated, percentages and parts are by weight.

The racanisodamine bulk drug used in this example was purchased from Hangzhou fumaric chemical Co., Ltd, and was dissolved in physiological saline to prepare 0.5, 1, 2mg/ml, respectively. The neostigmine raw material drug is purchased from sigma company, and is dissolved in physiological saline to be respectively prepared into 1, 2 and 4 mu g/ml. Racanisodamine and neostigmine were separately gavaged into mice at 0.1ml/10g body weight.

DSS (dextran sulfate μ Ι fate sodi μm), is an art-recognized animal model of ulcerative colitis, reference: stefan Wirtz.et al.chemical ly ind μ ced mo μ se models of organic information. nat μ re Protolls 2,541-546.No.3(2007).