Colon-released preparation of Melocicon and beta-cyclodextrin or its derivative composition

A technology for meloxicam and colon localization, which is applied to the colon localized release preparations of meloxicam and β-cyclodextrin or its derivatives, and the field of meloxicam colon localized release formulations, which can solve the problem of weakening individual differences. , drug efficacy uncertainty, difficulties and other issues, to achieve the effect of increasing solubility

Inactive Publication Date: 2006-11-22
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(2) In order to solve the problem of poor water solubility of meloxicam, the process adopts a complex and difficult-to-handle powder application method, because this method first needs to micronize the drug to about 3-5 μm, which is relatively difficult
(3) The preparation adopts a single pH-dependent colon-localized delivery technology, and there is always a burst release phenomenon of 3.94%-9.75%, which cannot eliminate or weaken individual differences, resulting in a certain degree of uncertainty in drug efficacy

Method used

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  • Colon-released preparation of Melocicon and beta-cyclodextrin or its derivative composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Meloxicam Colon-targeted Release Capsules of 7.5mg Specification

[0041] Take 75g of β-cyclodextrin, add 780mL of water, heat to dissolve at 80°C, add 25g of meloxicam passed through a 100-mesh sieve, add about 2mL of ammonia water, make the pH value 7.5, stir for 4 hours, and dissolve. Freeze-dry to obtain a solidified product of the meloxicam / β-cyclodextrin complex. Get 100g pectin, 170g lactose as diluent, 30g microcrystalline cellulose as disintegrant, use 5% HPMC (6cps) as binding agent to granulate, cross 16 mesh sieves, dry at 60°C for 2 hours, pass 20 mesh Sieve the granules, add 1% magnesium stearate and mix. Select No. 3 B-type enteric-coated capsules (colon-positioned release capsules) for filling. A new formulation of meloxicam colon-targeted release capsules with a specification of 7.5 mg was obtained.

Embodiment 2

[0042] Example 2 7.5 mg of meloxicam colon-targeted release matrix tablet

[0043] Take 75g of β-cyclodextrin, add 780mL of water, heat to dissolve at 80°C, add 25g of meloxicam passed through a 100-mesh sieve, add about 2mL of ammonia water, make the pH value 7.5, stir for 4 hours, and dissolve. Freeze-dry to obtain a solidified product of the meloxicam / β-cyclodextrin complex. Get 100g pectin, 170g lactose as diluent, 30g microcrystalline cellulose as disintegrant, use 5% HPMC (6cps) as binding agent to granulate, cross 16 mesh sieves, dry at 60°C for 2 hours, pass 20 mesh Sieve the granules, add 1% magnesium stearate and mix. Select a concave die with a diameter of 7mm, adjust the pressure to 5-7kg, and press the tablet. A new formulation of meloxicam colon-targeted release matrix tablet with a specification of 7.5 mg was obtained.

Embodiment 3

[0044] Example 3 Preparation of 10 mg meloxicam colon-targeted pellets

[0045] Take 75g of β-cyclodextrin, add 780mL of water, heat to dissolve at 80°C, add 25g of meloxicam passed through a 100-mesh sieve, add 2mL of ammonia water, make the pH value 7.5, stir for 4 hours, and dissolve. Add 5g of hydroxypropylmethylcellulose (12cps) as a binder, stir and dissolve at 40°C, add 5g of talcum powder as an anti-sticking agent, stir to form a uniform suspension, and set aside. Take 500 g of blank sugar pills with a diameter of 810 μm, place them in a fluidized bed (Glatt GPCG1) bottom spray container, select a nozzle with a diameter of 1.0 mm, turn on the fluidization switch, adjust the fluidization state, and preheat the material to about 30 ° C; heat Apply the drug coating solution to 30°C. Set the parameters of the fluidized bed as air inlet temperature 45°C, air inlet valve 50%, atomization pressure 1.5bar, spray rate 5ml / min, the inlet air temperature after the state is stabl...

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Abstract

The invention relates to capsules, matrix tablets and micropill preparations for colon-localized release of meloxicam / β-cyclodextrin or derivatives thereof. The preparation utilizes the principle that the colonic flora can degrade the polysaccharide cyclodextrin, combined with the pH-sensitive coating material or carrier, enables the drug preparation to achieve the precise positioning effect of specific release in the colon, and solves the problem of the drug before reaching the colon. The problem of burst release and the problem of rapid release in the mucous environment of the colon. The preparation of the invention is beneficial to the treatment of meloxicam on local diseases of the colon, such as ulcerative colitis, colon cancer, colon polyps and the like.

Description

technical field [0001] The invention relates to a colonic localized release preparation of a compound of meloxicam and β-cyclodextrin or a derivative thereof and a method for preparing the meloxicam colonic localized release preparation. Background technique [0002] It is well known that many drugs do not release well through the gastrointestinal tract, especially the colon, for various reasons. The colon is one of the most frequently-occurring diseases in the human body, and the symptoms are usually colitis, ulcerative colitis, colon polyps, or colon cancer. Since the above-mentioned diseases or symptoms are located in the deep part of the gastrointestinal tract, the drug is usually in the upper part of the small intestine when it is administered orally. Absorption, the concentration of the drug in the colon is very low or even non-existent, enema or suppository administration can only act on the rectum or sigmoid colon, and cannot reach the ascending colon and transverse ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5415A61K9/20A61K9/48A61K9/50A61P29/00
Inventor 梅兴国高春生单利
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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