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Celecoxib solid composition with high dissolution, preparation method and application

A solid composition, a technology of celecoxib, which is applied in the directions of non-active components of polymer compounds, pharmaceutical combinations, medical preparations of non-active components, etc. The problems such as low dissolution rate of lecoxib can achieve the effect of good preparation performance, simple preparation method and fast dissolution rate

Inactive Publication Date: 2012-11-07
HANGZHOU HEZE PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The first technical problem that the present invention needs to solve improves the solubility of celecoxib, develops a kind of preparation method of the celecoxib solid composition of preparation tool high dissolution rate, improves the dissolution rate of celecoxib preparation greatly, overcomes Celecoxib's low dissolution rate and low bioavailability solve the problem that raw materials are not easy to prepare solid oral preparations
[0010] The second technical problem to be solved in the present invention is to improve the solubility of celecoxib, develop a solid composition of celecoxib with a high dissolution rate, greatly improve the dissolution rate of celecoxib preparations, and overcome the celecoxib Coxib has low dissolution rate and low bioavailability, and solves the problem that raw materials are not easy to prepare solid oral preparations
[0011] The third technical problem to be solved in the present invention is to solve the application of this celecoxib solid composition with high dissolution rate in the preparation of oral solid preparations, greatly improve the dissolution rate of celecoxib preparations, and overcome the celecoxib solid composition. The problem of low dissolution and low bioavailability solves the problem that raw materials are not easy to prepare solid oral preparations

Method used

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  • Celecoxib solid composition with high dissolution, preparation method and application
  • Celecoxib solid composition with high dissolution, preparation method and application
  • Celecoxib solid composition with high dissolution, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Preparation of celecoxib solid composition with high dissolution rate

[0036] Table 1: Preparation of solid composition A1

[0037]

[0038] Add absolute ethanol into a container containing celecoxib, heat to 70~80°C to obtain a clear solution, absorb the solution with micropowder silica gel, dry at 60~70°C, and remove ethanol to obtain a solid composition of celecoxib A1.

[0039] Table 2: Preparation of solid composition A2

[0040]

[0041] Add sodium lauryl sulfate to absolute ethanol, heat to 70~80°C to obtain a clear solution, add celecoxib, dissolve to obtain a clear solution, absorb with micropowder silica gel, dry and evaporate at 60~70°C Celecoxib solid composition A2 obtained from ethanol.

[0042] Table 3: Preparation of solid composition A3

[0043]

[0044] Add sodium lauryl sulfate to absolute ethanol, heat to 70~80°C to obtain a clear solution, add celecoxib, dissolve to obtain a clear solution, absorb with micropowder silica g...

Embodiment 2

[0061] Embodiment 2: Preparation of oral solid preparation

[0062] Preparation of capsules

[0063] Take 28.00 g of the solid composition A1, pulverize it, pass through an 80-mesh sieve, and pack it into 100 capsules to obtain capsules containing 200 mg of celecoxib.

[0064] Take 28.80 grams of the solid composition A2, pulverize it, pass through an 80-mesh sieve, and pack it into 100 capsules to obtain capsules containing 200 mg of celecoxib.

[0065] Take 25.60 grams of the solid composition A3, pulverize it, pass through an 80-mesh sieve, and pack it into 100 capsules to obtain capsules containing 200 mg of celecoxib.

[0066] Take 30.02 grams of the solid composition A4, pulverize it, pass through an 80-mesh sieve, and pack it into 100 capsules to obtain capsules containing 200 mg of celecoxib.

[0067] Take 29.20 grams of the solid composition A5, pulverize it, pass through an 80-mesh sieve, and pack it into 100 capsules to obtain capsules containing 200 mg of cel...

Embodiment 3

[0076] Embodiment 3: the preparation of tablet

[0077] Table 10: A1 tablet

[0078] Material name Sample weight (g) mass percentage A1 28.00 87.50% Crospovidone 1.25 3.91% Polyvinylpyrrolidone 1.00 3.13% Sodium dodecyl sulfate 1.25 3.91% Micropowder silica gel 0.15 0.47% Magnesium stearate 0.35 1.09% water Appropriate amount —— total 32.00 100.00%

[0079] Weigh raw and auxiliary materials according to Table 10, dissolve sodium lauryl sulfate and polyvinylpyrrolidone in water and configure an aqueous solution as an adhesive for standby use, take material A1 and use adhesive to make soft material, granulate, and pass through a 40-mesh sieve , dried, granulated, added cross-linked povidone, micro-powder silica gel, magnesium stearate, mixed evenly, and pressed into 320mg / tablet.

[0080] Table 11: A2 Tablets

[0081] Material name Sample weight (g) mass percentage A2 28.80 90.00% ...

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Abstract

The invention provides a celecoxib solid composition with high dissolution, a preparation method and an application. The amorphous composition of celecoxib is obtained by dissolving the celecoxib into one or more pharmaceutically acceptable solvents and adsorbing and drying with pharmaceutically acceptable auxiliary materials. The composition can be further prepared into various solid preparation forms such as tablets, capsules and granules according to the actual requirement. Through the prepared celecoxib composition and preparations thereof, the dissolution of the celecoxib can be greatly improved, and the defects of low dissolution and low bioavailability of the celecoxib are overcome.

Description

technical field [0001] The invention relates to the preparation of a therapeutic drug for rheumatic and rheumatoid arthritis, in particular to a solid composition of celecoxib with high dissolution rate, a preparation method and application. Background technique [0002] Celecoxib (Celecoxib) is a drug for the treatment of rheumatoid arthritis, rheumatoid arthritis and osteoarthritis listed by Pfizer in 1999. The imported drug name is Celebrex. Has the following structure (see attached figure 1 ). [0003] Due to the crystal structure, the physical and chemical properties of celecoxib show poor preparation performance. This feature is manifested as: first, it is almost insoluble in water, and if the uncrushed drug is directly filled into capsules, the oral absorption of the drug will be slow, which will affect the bioavailability; second, the texture is light, the bulk density is low, and it is easy to agglomerate into agglomerates , making it very difficult to improve s...

Claims

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Application Information

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IPC IPC(8): A61K31/635A61K47/40A61K47/38A61K47/04A61P29/00A61P19/02
Inventor 倪晟赵航胡秀波谢齐昂
Owner HANGZHOU HEZE PHARMA TECH
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