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Triamcinolone acetonide acetate particle, and preparation method and medicinal composition thereof

A technology of triamcinolone acetonide acetate and its composition, which is applied in the field of triamcinolone acetonide acetate particles and its preparation, can solve the problems of changes in the physical and chemical properties of the particles, swelling of suspension injections, etc., and achieve the effect of reducing the changes in the physical and chemical properties of the particles

Active Publication Date: 2010-01-06
上海正大通用药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(3) Jet milling may lead to changes in the physical and chemical properties of some particles
(4) Crystal swelling occurs in the prepared suspension injection during storage

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] 1. Heat and dissolve 0.1 g of triamcinolone acetonide acetate with 20 ml of 75% ethanol, and cool naturally to obtain needle-like crystals. Wash off the ethanol on the crystals with water for injection at normal temperature, and dry at 100°C.

[0048] 2. Add the above ethanol-treated triamcinolone acetonide acetate crystals into 3500 ml of water for injection cooled to 10°C.

[0049] 3. Heat 500ml of dimethylformamide to 60°C, add 100g of triamcinolone acetonide acetate, stir to dissolve it completely, and filter. Add the filtrate linearly (100ml / min) dropwise to the above-mentioned water for injection cooled to 10°C, and stir while adding at a speed of 120 rpm.

[0050] 4. After the addition, keep the temperature of the mixture at 15°C, continue to stir for 15 minutes, and then stop stirring. The mixture of water and crystals was filtered. The crystals were washed repeatedly with filtered water for injection at room temperature.

[0051] 5. Particle crystallization...

Embodiment 2

[0056] 1. Heat and dissolve 0.5 g of triamcinolone acetonide acetate with 50 ml of 85% ethanol, and cool naturally to obtain needle-like crystals. Wash off the ethanol on the crystals with water for injection at normal temperature, and dry at 100°C.

[0057] 2. Add the above ethanol-treated triamcinolone acetate crystals to 6000 ml of water for injection cooled to 5°C.

[0058] 3. Heat 500ml of dimethylformamide to above 60°C, add 100g of triamcinolone acetonide, stir to make it completely dissolved, and filter. Add the filtrate linearly (100ml / min) dropwise to the above-mentioned water for injection cooled to 5°C, and stir while adding at a speed of 120 rpm.

[0059] 4. After the addition, keep the temperature of the mixture below 10°C, continue to stir for 5 minutes, and then stop stirring. The mixture of water and crystals was filtered. The crystals were washed repeatedly with filtered water for injection at room temperature. .

[0060] 5. Particle crystallization Unde...

Embodiment 3

[0065] 1. Heat and dissolve 1 g of triamcinolone acetonide acetate with 100 ml of 95% ethanol, and cool naturally to obtain needle-like crystals. Wash off the ethanol on the crystals with water for injection at normal temperature, and dry at 100°C.

[0066] 2. Add the above ethanol-treated triamcinolone acetate crystals to 8000 ml of water for injection cooled to 0°C.

[0067] 3. Heat 500ml of dimethylformamide to above 60°C, add 100g of triamcinolone acetonide, stir to make it completely dissolved, and filter. Add the filtrate linearly (100ml / min) dropwise to the above-mentioned water for injection cooled to 0°C, stir while adding, and the rotation speed is 120 rpm.

[0068] 4. After the addition, keep the temperature of the mixture below 10°C, continue to stir for 1 minute, and then stop stirring. The mixture of water and crystals was filtered. The crystals were washed repeatedly with filtered water for injection at room temperature.

[0069] 5. Particle crystallization ...

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PUM

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Abstract

The invention discloses a triamcinolone acetonide acetate particle, and a preparation method and a medicinal composition thereof. The preparation method comprises the following steps: 1) heating and dissolving triamcinolone acetonide acetate with aqueous solution of ethanol, naturally cooling the obtained solution to obtain acicular crystals, washing away the ethanol from the crystals with water for injection, drying the washed crystals, and then adding the crystals into water for injection at a temperature of 0 to 10 DEG C; 2) linearly adding dropwise triamcinolone acetonide acetate solution dissolved with dimethyl formamide solution into the mixed solution of the water for injection at the temperature of 0 to 10 DEG C obtained in the step 1), simultaneously stirring the mixed solution, keeping the temperature of the mixed solution at 0 to 15 DEG C, and continuing stirring the mixed solution for 1 to 30 minutes to obtain a mixture of water and crystals; and 3) as usual, filtering the mixture of the water and the crystals obtained in the step 2) and vacuum-drying the obtained crystals. The invention adopts a crystal inoculation process, thus crystals of the prepared triamcinolone acetonide acetate particles have regular shapes and uniform particle sizes; crystallization is free from jet milling and the physicochemical property of the particle is stable; and no crystal expansion phenomenon generates in the prepared triamcinolone acetonide acetate suspension injection during storage.

Description

technical field [0001] The invention particularly relates to a triamcinolone acetonide acetate microparticle, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Triamcinolone acetonide injection is a commonly used glucocorticoid drug in clinical practice. It is suitable for various skin diseases, allergic rhinitis, arthralgia, bronchial asthma, frozen shoulder, tenosynovitis, synovitis, acute sprain, rheumatoid arthritis, etc. [0003] Triamcinolone Acetate Injection is a suspension injection. At present, triamcinolone acetonide acetate microparticles are prepared by dimethylformamide solvent crystallization method in preparation pretreatment of triamcinolone acetonide acetate. Its process includes the following steps. [0004] 1. Cool the water for injection to below 5°C. [0005] 2. Heat dimethylformamide to above 60°C, add triamcinolone acetonide, stir to make it completely dissolved, and filter. [0006] 3. Filter the filtra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/10A61K31/58A61P17/00A61P37/08A61P29/00
Inventor 陈伟贺明源
Owner 上海正大通用药业股份有限公司
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