Oral colon target preparation for treating colitis ulcerativa and its making method

A technology for ulcerative colitis and colon targeting, which is applied in the directions of pill delivery, medical raw materials derived from arthropods, digestive system, etc. Effects of side effects

Inactive Publication Date: 2006-11-01
杨明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0026] Although there have been reports on the use of Periplaneta americana extracts in the treatment of ulcerative colitis, there is no relevant report on the preparation of oral colon-targeted preparations for the treatment of ulcerative colitis.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0048] Example 1 Screening of coating excipients for pH-dependent formulations

[0049] EUDRAGIT S100: Triethyl citrate (g:g)

[0050] The second method in the Pharmacopoeia Appendix XC Dissolution Test Method was used to evaluate the release of the above samples, that is, the paddle method; dissolution medium: artificial gastric juice (0.1mol / l hydrochloric acid solution) 750ml, artificial intestinal juice (pH 6.8 phosphate buffer) ) 1000ml, 900ml of artificial colon fluid (pH.7.8~8.0 phosphate buffer); rotating speed of stirring paddle: 150rpm; temperature: 37±0.5°C.

[0051] The prepared colon-targeting capsules were put into the cups and put into the artificial gastric juice respectively. After 2 hours, 5ml was sampled (and the same amount of dissolution medium was added at the same time), passed through a 0.46μm microfiltration membrane, and sampled for determination. Add 250ml of 0.2mol / L sodium phosphate solution, adjust the pH=6.8, take a sample of 5ml after 4 ...

example 2

[0056] Example 2 Screening of coating excipients for enzyme-dependent preparations

[0057] Proportion of HPMC in accessories (g / g)

[0058] The second method in the Pharmacopoeia Appendix XC Dissolution Test Method was used to evaluate the release of the above samples, that is, the paddle method; dissolution medium: artificial gastric juice (0.1mol / l hydrochloric acid solution) 750ml, artificial intestinal juice (pH 6.8 phosphate buffer) ) 1000ml, artificial colon fluid (pH 7.8-8.0 phosphate buffer) 900ml, and pectinase solution (pH 4); stirring paddle speed: 150rpm; temperature: 37±0.5°C.

[0059] The prepared colon-targeting capsules were put into the cups and put into the artificial gastric juice respectively. After 2 hours, 5ml was sampled (and the same amount of dissolution medium was added at the same time), passed through a 0.46μm microfiltration membrane, and sampled for determination. Add 250ml of 0.2mol / L sodium phosphate solution, adjust the pH=6.8, take a ...

example 3

[0064] Example 3 Preparation process of oral colon targeting capsules

[0065] Take 1000g of American cockroach, add ethanol to reflux and extract three times, the alcohol concentration is 70% to 90%, combine the extracts, defatted, and dry to obtain 178g of dry powder of medicine. Add starch 178g, talc powder 5g, carboxymethyl cellulose sodium 5g, pan-pill method to prepare pellets, get 330g vegetarian pill; take 100g acrylic resin III or EUDRAGIT S100, 10g triethyl citrate, add 95% ethanol to 1250g , Get the coating liquid. Spray coating at the bottom of the fluidized bed, spray the coating liquid at a speed of 4g / min to coat the pellets, and the spray pressure is 0.8kg / cm 2 , The inlet air temperature is 34°C, which increases the weight of the pellets by 18%, and the pellets are dried in an oven at 40°C for 2 hours, and the pellets are encapsulated to obtain the finished product.

[0066] Specification: 0.42g / capsule, each capsule is equivalent to 1g of original medicinal mater...

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Abstract

An orally taken target medicine for treating the ulcerative colitis with high curative effect and low dosage is prepared from the extract of American periplaneta. Its preparing process is also disclosed.

Description

Technical field [0001] The invention relates to an oral colon targeting preparation for treating ulcerative colitis, specifically, a medicine prepared with Chinese medicinal materials as raw materials and a preparation method and application thereof, belonging to the field of Chinese medicine. Background technique [0002] Ulcerative colitis is a primary, non-specific chronic disease of the colon. Under colonoscopy, it can be seen that only the mucosa and submucosa of the colon are invaded, and there are erosions and superficial ulcers. [0003] At present, Western medicine treatment of ulcerative colitis mainly includes the following types of drugs: sulfonamides, antibiotics, metronidazole, hormone therapy, oral corticosteroids, topical administration, immunosuppressive agents; the above-mentioned western medicines have passed long-term efficacy trials and clinical trials All proved to have reliable therapeutic effects, but most of them are toxic and h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K35/64A61P1/04
Inventor 杨明邱雪兰谢兴亮肖禾
Owner 杨明
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