Celecoxib solid composition with increased dissolution rate, and preparation method and application thereof

A technology of solid composition and celecoxib, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of affecting the therapeutic effect of drugs, affecting solubility, and dissolution effects. To achieve satisfactory results and other issues, to achieve the same chemical properties and celecoxib monomer, to improve the effect of slow dissolution and good dissolution effect

Active Publication Date: 2014-02-19
HAINAN HERUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it turns out that celecoxib has a very strong electrostatic effect, is light in weight, and is easy to aggregate. During the powder mixing process, the celecoxib is unevenly separated, and the content uniformity of the preparation cannot meet the requirements, thus affecting the drug’s efficacy. treatment effect
[0008] Patents CN102838542A, CN102838543A, CN102838544A, and CN102838545A mention that celecoxib has crystal forms I, II, III, and IV respectively. Regardless of whether single crystal or mixed crystal is used, according

Method used

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  • Celecoxib solid composition with increased dissolution rate, and preparation method and application thereof
  • Celecoxib solid composition with increased dissolution rate, and preparation method and application thereof
  • Celecoxib solid composition with increased dissolution rate, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1, solid composition

[0042] Take celecoxib 100g, polyvinylpyrrolidone K 30 45g, 40g of hydroxypropyl methylcellulose, 1.0g of disodium hydrogen phosphate and 0.5g of sodium hydroxide (of which polyvinylpyrrolidone K 30 and hydroxypropyl methylcellulose as a dispersing co-solvent, disodium hydrogen phosphate and sodium hydroxide as an alkaline compound), mix evenly and place in the grinding chamber for grinding, nitrogen protection is circulated throughout the grinding process, and the grinding chamber is controlled The temperature in the body is controlled at 15-30°C, and the grinding time is between about 5-8 μm according to the particle size distribution D90 of the powder. A co-ground solid composition is obtained.

Embodiment 2

[0043] Embodiment 2, solid composition

[0044] Take celecoxib 100g, polyvinylpyrrolidone K 30 45g, poloxamer 40g, disodium hydrogen phosphate 1.0g and sodium hydroxide 0.5g (where polyvinylpyrrolidone K 30 and poloxamer as a dispersing co-solvent, disodium hydrogen phosphate and sodium hydroxide are basic compounds), mixed evenly and then placed in a ball mill for co-grinding, nitrogen protection is circulated throughout the grinding process, and the temperature in the chamber of the ball mill is controlled not to exceed At 30°C, the grinding time is between about 5 and 20 μm according to the particle size distribution D90 of the powder. A co-ground solid composition is obtained.

Embodiment 3

[0045] Embodiment 3, solid composition

[0046] Take celecoxib 100g, β-cyclodextrin 45g, hydroxypropyl cellulose 30g, disodium hydrogen phosphate 0.5g (wherein β-cyclodextrin and hydroxypropyl cellulose are dispersing cosolvents, disodium hydrogen phosphate is Alkaline compounds), mixed evenly and placed in a ball mill to grind together for 80 minutes. During the grinding process, nitrogen protection was circulated throughout the process, and the temperature in the chamber of the ball mill was controlled at 15-30°C. The grinding time was based on the particle size distribution of the powder D90 at about 5-20 μm between. A co-ground solid composition is obtained.

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Abstract

The invention relates to a psychotherapeutic drug for OA (Oarthritis) and RA (Rheumatoid Arthritis), in particular to a celecoxib solid composition with an increased dissolution rate, and the preparation method and application thereof. The celecoxib solid composition comprises celecoxib, a dispersion promoter and an alkali compound, wherein the mass ratio of the celecoxib, the dispersion promoter and the alkali compound is 100 : (5- 95) : (0.1- 1.5); the D90 of the celecoxib solid composition ranges from 5 to 20 micron. The celecoxib solid composition provided by the invention solves the technological difficulties of strong material static and low probability of powder mixing no matter under a condition that the celecoxib bulk drug is monocrystal or mixed polycrystal, so that the problem that the celecoxib is hydrophilic is solved, the physical property that the drug is difficult to dissolve is improved, and the dissolution rate of the drug is increased, thereby being beneficial to drug absorbing.

Description

technical field [0001] The present invention relates to a therapeutic drug for osteoarthritis (OA) and adult human rheumatoid arthritis (RA), in particular to a celecoxib solid composition with increased dissolution rate and its preparation method and application. Background technique [0002] Celecoxib, the chemical name is 4-[5-(4-methylphenyl)-3-trifluoromethyl-1H-pyrazol-1-yl]benzenesulfonamide. Its molecular formula is C 17 h 14 f 3 N 3 o 2 S, the molecular weight is 381.38. It is the first selective COX-2 inhibitor non-steroidal anti-inflammatory drug developed by Searle Company of the United States. It was first approved for marketing in the United States in December 1998. The indication is to relieve the symptoms and signs of osteoarthritis and rheumatoid arthritis . In September 2000, celecoxib of Pfizer Pharmaceutical Co., Ltd. was listed in my country. At present, the State Food and Drug Administration has not approved the production of this dosage form by ...

Claims

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Application Information

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IPC IPC(8): A61K31/635A61K47/38A61P29/00A61P19/02
CPCY02A50/30
Inventor 钟正明
Owner HAINAN HERUI PHARMA
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