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Medicament for treating ulcerative colitis and preparation method thereof

A technology for ulcerative colitis and drugs, applied in the field of medicine, can solve the problems of large individual differences in drug release, slow onset of effect, and incomplete understanding of pathogenesis

Inactive Publication Date: 2010-01-27
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the etiology and pathogenesis are not fully understood. Modern medicine often uses sulfasalazine (SASP) combined with corticosteroids for treatment of this disease, mainly to control acute attacks, alleviate the condition, reduce recurrence, and prevent and treat complications. Afterwards, it is cleaved by bacterial azoreductase in the colon, enters the liver, is acetylated, and is excreted in the urine. The bioavailability is low, and it cannot form an effective drug concentration at the inflammation of the colon; other corticosteroids such as prednisolone Pine, hydrocortisone succinate, etc. can rapidly induce remission of ulcerative colitis in the acute stage, but long-term application can lead to eight major side effects of hormone drugs such as full moon face, electrolyte imbalance, and osteoporosis. There is also corticosteroid resistance; immunosuppressants such as 6-mercaptopurine and azathioprine, etc., are often used in patients who are ineffective in SASP and corticosteroid therapy and in patients with corticosteroid toxicity or long-term continuous dependence on corticosteroids, which can block Proliferation and activation of lymphocytes, inhibition of chemotaxis of neutrophils, but slow onset, toxic and side effects such as bone marrow suppression, acute pancreatitis, nausea, fever, hepatitis and allergies are quite serious; anti-cytokine regulators such as Inflix Cycloximab, Daclizumab, etc., which are used for patients with moderate to severe ulcerative colitis who have not responded well to corticosteroids and / or immunosuppressants, and nausea is a frequent side effect
[0004] 2. Traditional Chinese medicine has rich experience in treating this disease, but only decoction is the main form, and the dosage form is single
Most of the early studies were based on the theory of pH dependence and time lag, but due to the influence of individual differences, gastrointestinal contents, and pathophysiological conditions of the patient's digestive tract, the drug was often released early or not released in the small intestine.
The drug release of the pressure-controlled system depends on the pressure in the human colon, but even under normal circadian rhythm, the pressure in the colon is greatly affected by various physiological factors, so that the individual differences in drug release are also large, and the expected release of the drug cannot be guaranteed.

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  • Medicament for treating ulcerative colitis and preparation method thereof
  • Medicament for treating ulcerative colitis and preparation method thereof
  • Medicament for treating ulcerative colitis and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The tablet preparation of embodiment 1 medicine of the present invention

[0036] Mix the full prescription amount of Pulsatilla chinensis, the full prescription amount of Jiaobaizhu, and the half prescription amount of other medicinal flavors in the prescription medicinal materials, and ultrafinely pulverize it until the particle size reaches below 100nm to obtain the nano powder original drug.

[0037]Decoct the half-prescription amount of other medicinal herbs except Pulsatilla Pulsatillae and Jiaobaizhu in water for 1 hour, filter out the medicinal residues and add water to decoct for another 1 hour, combine the decoctions, and concentrate to a specific gravity of 1.2 to 1.8 for use as a binder.

[0038] Spray the extract concentrate on the nanopowder original drug to make soft materials, pass through a 14-mesh sieve to make wet granules, dry at 50°C-60°C for 1.5h, pass through a 14-mesh sieve for granulation, and press into plain tablets.

[0039] Add low-methyl es...

Embodiment 2

[0041] The in vitro dissolution test of Chinese medicine colon tablet of embodiment 2 of the present invention

[0042] 1 Determination method of index component astragaloside IV

[0043] 1.1 Determination of maximum absorption wavelength of astragaloside IV

[0044] Accurately weigh 4.895 mg of the astragaloside reference substance, and dilute it to a 10 ml measuring bottle with a phosphate buffer solution of pH=8 to obtain an astragaloside reference substance solution with a concentration of 0.4895 mg / ml, and carry out ultraviolet-visible full-wavelength ( 190~900nm) scan. The maximum absorption wavelength was determined to be 538nm. There is no interference from other drugs in the prescription and calcium pectate at 538nm.

[0045] 1.2 Establishment of Astragaloside IV Standard Curve

[0046] Precisely draw 0.1, 0.2, 0.3, 0.5, 0.7 and 0.9ml of 0.4895mg / ml astragaloside reference substance solution into a 50ml measuring bottle, accurately add phosphate buffer to constant...

Embodiment 3

[0050] Dissolution test in vivo of Chinese medicine colon granule of embodiment 3 of the present invention

[0051] Make granules of the self-made traditional Chinese medicine tablets for treating ulcerative colitis, and wrap the above-mentioned self-made pectin calcium coating film; take 6 rabbits with a body weight of about 2 kg, and pour 0.2 g of the above-mentioned pectin calcium granules every 6 hours, canning 6 times . Rabbits were killed and dissected 3 hours after the last administration. An average of about 0.2 g of intact calcium pectin particles was found in the rabbit stomach, an average of 0.05 g of intact calcium pectin particles was found in the small intestine, and the rest were estimated to have been degraded in the cecum. The individual conditions of the 6 rabbits were basically similar.

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Abstract

The invention belongs to the medicine technical field, in particular a medicament for treating ulcerative colitis and a preparation method thereof. The medicament for treating the ulcerative colitis is prepared from the following raw materials by weight: 5-30 portions of Chinese bulbul, 4-24 portions of golden cypress, 2-12 portions of coptis chinensis, 4-24 portions of ash bark, 3-18 portions of raw astragalus root, 3-18 portions of deep-fried atractylodes, 3-18 portions of flos sophorae, 3-18 portions of sanguisorba officinalis and 2-10 portions of aconite albertdeng. In the invention, calcium pectate is also used as a coating material and an effective medicament prime tablet to prepare a colitis tablet so as to realize colonic targeting drug administration, therefore, the curative effect of the medicament for treating ulcerative colitis is obviously superior to the prior medicament.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a medicine for treating ulcerative colitis and a preparation method thereof. Background technique [0002] 1. Ulcerative colitis is one of the intractable diseases of the digestive system. The curative effect of modern medical treatment is not satisfactory, and the side effects are large [0003] Ulcerative colitis (UC) is an inflammatory bowel disease and one of the refractory diseases of the digestive system. Clinically, it is characterized by abdominal pain, diarrhea, pus, blood and mucus in the stool, and endoscopically, colonic mucosal ulcers and erosions are the main manifestations. Its incidence rate is higher in western countries, and it also has an increasing trend in our country. However, the etiology and pathogenesis are not fully understood. Modern medicine often uses sulfasalazine (SASP) combined with corticosteroids for treatment of this disease, mainl...

Claims

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Application Information

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IPC IPC(8): A61K36/756A61K9/36A61K47/36A61P1/04
Inventor 卜平胡荣徐海荣
Owner YANGZHOU UNIV