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Lyophilized parecoxib sodium powder and preparation method thereof

A technology of parecoxib sodium and freeze-dried powder, applied in the field of parecoxib sodium freeze-dried powder and preparation thereof, can solve the problems such as insufficient analgesic effect, difficulty in oral administration, etc. The effect of shortening freeze-drying time and improving stability

Active Publication Date: 2015-12-23
上海华源药业(宁夏)沙赛制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Parecoxib sodium is the first specific cyclooxygenase-2 (COX-2) inhibitor that can be administered intravenously and intramuscularly, which can solve the difficulty of oral administration or insufficient analgesic effect in postoperative patients with oral dosage forms swift downside

Method used

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  • Lyophilized parecoxib sodium powder and preparation method thereof
  • Lyophilized parecoxib sodium powder and preparation method thereof
  • Lyophilized parecoxib sodium powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1, the preparation of parecoxib sodium freeze-dried powder and its effect detection:

[0048] 1. Preparation: The prescription is 40g of parecoxib sodium, 2g of glycine, 30g of mannitol and an appropriate amount of pH regulator, and add water for injection to 500ml. The specific preparation method is as follows:

[0049] Dissolve 30g of mannitol in 200ml of water for injection at 20°C, add 0.5g of medicinal charcoal to it, stir at room temperature 25°C for 15min, and filter through a 0.45μm filter to obtain solution I.

[0050] Then add 2 g of glycine into 600 ml of water for injection, after dissolving, add 40 g of parecoxib sodium, stir until dissolved, and obtain solution II.

[0051] Mix solution I and solution II evenly, adjust the pH to 8.6 with 0.1M phosphoric acid solution, add water for injection to 1000ml; then filter the whole system through a 0.22μm microporous membrane in turn, with an ultrafiltration membrane with a molecular weight cut-off of 1...

Embodiment 2

[0077] Embodiment 2, the preparation of parecoxib sodium freeze-dried powder and its effect detection:

[0078] 1. Preparation: The prescription is 40g of parecoxib sodium, 2.5g of glycine, 20g of mannitol and an appropriate amount of pH regulator, and add water for injection to 500ml. The specific preparation method is as follows:

[0079]Dissolve 20g of mannitol in 100ml of water for injection at 25°C, add 0.05g of medicinal charcoal to it, stir for 15min at room temperature at 25°C, and filter through a 0.45μm filter to obtain solution I.

[0080] Then add 2.5g of glycine into 300ml of water for injection, after dissolving, add 40g of parecoxib sodium, stir until dissolved, and obtain solution II.

[0081] Mix solution I and solution II evenly, adjust the pH to 9.0 with 0.1M phosphoric acid solution, add water for injection to 500ml; then filter the whole system through a 0.22μm microporous membrane in turn, with an ultrafiltration membrane with a molecular weight cut-off o...

Embodiment 3

[0099] Embodiment 3, the preparation of parecoxib sodium freeze-dried powder and its effect detection:

[0100] 1. Preparation: The prescription is 40g of parecoxib sodium, 3g of glycine, 10g of mannitol and an appropriate amount of pH regulator, and add water for injection to 500ml. The specific preparation method is as follows:

[0101] Dissolve 10g of mannitol in 100ml of water for injection at 30°C, add 0.05g of medicinal charcoal to the solution, stir at room temperature 25°C for 15min, and filter through a 0.45μm filter to obtain solution I.

[0102] Then add 3 g of glycine into 300 ml of water for injection, and after dissolving, add 40 g of parecoxib sodium and stir until dissolved to obtain solution II.

[0103] Mix solution I and solution II evenly, adjust the pH to 9.0 with 0.1M phosphoric acid solution, add water for injection to 500ml; then filter the whole system through a 0.22μm microporous membrane in turn, with an ultrafiltration membrane with a molecular weig...

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Abstract

The invention discloses lyophilized parecoxib sodium powder and a preparation method thereof. The lyophilized parecoxib sodium powder comprises, by mass, 40 parts of parecoxib sodium, 1-3 parts of stabilizers, 5-30 parts of lyophilization excipients and 0.1-0.5 part of pH (potential of hydrogen) regulators. The preparation method includes the steps of 1) mixing the lyophilization excipients, water and medicinal carbon with stirring, and filtering to obtain a solution I; 2) mixing the stabilizers, the water and the parecoxib sodium with stirring so as to obtain a solution II; 3) mixing the solution I with the solution II and filtering to obtain a solution III; 4) lyophilizing the solution III to obtain the lyophilized parecoxib sodium powder. A lyophilized parecoxib sodium composition prepared by the preparation method has the advantages that since the parecoxib sodium is degraded difficultly, 'degradation product' content is extremely low and stability during long-term storage is high; treatment effect and safety of the lyophilized parecoxib sodium composition during clinical application are greatly improved.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to a freeze-dried powder of parecoxib sodium and a preparation method thereof. Background technique [0002] Parecoxib is a non-steroidal anti-inflammatory drug and a water-soluble inactive prodrug of valdecoxib. After intravenous injection, it can be rapidly hydrolyzed into valdecoxib by liver carboxylesterase. Its metabolism mainly It is mediated by cytochrome P450 (CYP) 3A4 and 2C9 isozymes, and exerts anti-inflammatory, analgesic and antipyretic effects by specifically inhibiting COX-2 and blocking the synthesis of prostaglandins from arachidonic acid. Parecoxib sodium is the first specific cyclooxygenase-2 (COX-2) inhibitor that can be administered intravenously and intramuscularly, which can solve the difficulty of oral administration or insufficient analgesic effect in postoperative patients with oral dosage forms Quick downsides. Parecoxib sodium has been sh...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/42A61K47/16A61P29/00
Inventor 芦莉娜惠彩霞陈通
Owner 上海华源药业(宁夏)沙赛制药有限公司
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