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Composition for veterinary and medical use

A composition and compound technology, applied in application, drug combination, active ingredient of heterocyclic compounds, etc., can solve problems such as weak antibacterial activity

Active Publication Date: 2006-10-11
IRP健康私人有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the antibacterial activity of these compounds is quite weak, very high doses, such as 500-2500 mg / kg body weight / day, are required for treatment[18]

Method used

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  • Composition for veterinary and medical use
  • Composition for veterinary and medical use
  • Composition for veterinary and medical use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Example 1 Preparation of compound of general formula (1), berberine chloride

[0079] The roots and bark (1.5kg, ground) of Berberines vulgaris were refluxed with ethanol (10L×2). The ethanol extract was filtered and evaporated under reduced pressure to obtain a brown oil. The residue was dissolved in a warm 0.1M HCl solution (10L×2), filtered, and the filtrate was evaporated to about 1L in vacuo, and then stirred at room temperature overnight. The yellow precipitate was collected and washed with cold water, then re-dissolved in boiling water (10L×2), cooled to room temperature, filtered, washed with water and air dried to obtain yellow crystalline powder of berberine chloride (44.5g). The crystals were analyzed by NMR and the following results were obtained:

[0080] 1 H-nmr(CD 3 OD)×(ppm)

[0081] 3.16(t, 2H), 4.02(s, 3H), 4.15(s, 3H), 4.88(t, 2H), 6.12(s, 2H), 7.03(s, 1H), 7.74(s, 1H), 7.95 (d, AB, 1H), 8.15 (d, AB, 1H), 8.89 (s, 1H), 9.83 (s, 1H).

Embodiment 2

[0082] Example 2 Preparation of compound of general formula (2), 40% oxidized cellulose

[0083] Under the condition of less than 30℃, add a part of microcrystalline cellulose (particle size diameter is about 20) to a stirred aqueous solution (1.08L) of periodic acid (140.7g, 0.6175mol) with pH<0.5 over 2 hours ( 250g, 1.54 moles). The entire mixture was stirred at 30-32°C for 4 hours and then at room temperature for 16 hours. A 5% sodium hydroxide solution (approximately 480 ml) was added to the resulting reaction mixture to adjust the pH to 5-6. The suspension was filtered; the solid (2L×4) was washed with water until the filtrate did not show the presence of an oxidizing agent on the KI-starch test paper. Then the solid was washed with acetone (0.5 L) and air dried to obtain 40% oxidized cellulose (215 g, 87%) as a white powder.

Embodiment 3

[0084] Example 3 Preparation of the compound of general formula (2), 40% oxidized water-soluble cellulose

[0085] Over two hours, sodium periodate (532.5 mg, 2.48 mmol) was added dropwise to a stirred aqueous solution (25 ml) of carboxymethyl cellulose (molecular weight 250,000, DS = 0.7) (1 g, 6.17 mmol) in an ice bath ) Of aqueous solution. The reaction mixture was stirred at 5-10°C for 16 hours, and then dialyzed against water in a dialysis tube (permeation molecular weight limit of about 10,000) for 48 hours. The solution was then freeze-dried to obtain 40% oxidized water-soluble cellulose (813 mg, 81.4%) as a white powder.

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Abstract

The present invention relates to compositions for treating gastrointestinal disorders and related conditions, including irritable bowel syndrome; inflammatory bowel disease, colitis, Crohn's disease and / or promoting weight gain in animals including humans, said compositions Comprising berberine of general formula (1) or derivatives thereof (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and X are as defined in claim 1) and / or Polydialdehydes are selected from polydialdehydes such as dialdehyde polysaccharides, eg oxycellulose or oxystarch or poly(acrolein / acrylic acid).

Description

Background of the invention [0001] Gastrointestinal ("GI") dysfunction is caused by pathogen invasion, treatment with broad-spectrum antibiotics, improper diet, stressful lifestyle, and other pathogenic factors. This is a common disease with symptoms such as Intestinal Stress Syndrome (IBS), which is present in 20% of American adults. In Canada, IBS is the leading cause of absenteeism in schools and factories, second only to colds. So far, there is no good medicine for IBS and inflammatory bowel disease (IBD). A satisfactory therapeutic composition should meet the following conditions: [0002] ●Non-toxic and safe to use. [0003] ● Will not inhibit the probiotics in the internal organs or produce side effects on them. [0004] ●Preferably has low oral bioavailability (no systemic effect). [0005] ●No bacterial resistance. [0006] ●Anti-inflammatory. [0007] ●Stop diarrhea and inhibit secretion. [0008] ●Anti-motility. [0009] ●Enhance immunity. [0010] ●Neutralize toxins. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A23K20/195A61K31/717A61K31/718A61K31/78A61P1/00A61P31/00
Inventor 金国蓓吴文扬
Owner IRP健康私人有限公司
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