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Parecoxib sodium pharmaceutical composition for injection and preparation method thereof

A technology of parecoxib sodium and parecoxib meter, which is applied in the field of parecoxib sodium pharmaceutical composition for injection and its preparation, and can solve the problems of small dosage of the main drug, high water content, and high requirements for production equipment , to achieve the effect of reducing dosage, meeting safety requirements and avoiding adverse events

Active Publication Date: 2016-06-01
CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the operation is cumbersome and requires high production equipment, which increases the cost input
[0006] In addition, the appearance formability, resolubility and high water content of parecoxib sodium are the difficulties in the production of preparations
The Chinese patent (application number CN02810765.9) adopts the method of cooling from room temperature to -50°C within 1.75 hours in the freezing stage, and keeping it for 7.0 hours. The freezing and cooling time is long, and the solute cannot be frozen into shape quickly, which is not conducive to the full sublimation of water.
In addition, due to the small dose and low concentration of the main drug, the rigidity of the freeze-dried product in the sublimation stage is low. If the drying temperature is too high, the rigidity of the solid matrix is ​​not enough to maintain the honeycomb structure, and the solid matrix wall of the cavity will collapse; and The temperature is too low and the water content is high, which will affect the stability and resolubility of the product

Method used

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  • Parecoxib sodium pharmaceutical composition for injection and preparation method thereof
  • Parecoxib sodium pharmaceutical composition for injection and preparation method thereof
  • Parecoxib sodium pharmaceutical composition for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment 1: Parecoxib Sodium Preparation Method 1

[0062] Add 100g of the crude product of parecoxib sodium into 100ml of acetone, stir mechanically, heat up to reflux, add 1000ml of acetonitrile dropwise, keep stirring for 1 hour, then cool down to room temperature, filter, rinse the filter cake with acetonitrile, and dry under reduced pressure to obtain 94.4 g Parecoxib sodium was crystallized, and the yield was 94.4%. Related substances adopt HPLC method, and the total impurity is 0.02%; use Cu-ka ray to carry out X-ray powder measurement, with the following description: figure 1 X-ray powder diffraction pattern shown.

Embodiment 2

[0063] Embodiment 2: Parecoxib sodium preparation method 2

[0064] Add 100g of crude parecoxib sodium to 100ml of ethanol, stir mechanically, heat up to reflux, add 1000ml of methyl tert-butyl ether dropwise, keep stirring for 1 hour, cool down to room temperature, filter, filter cake with methyl tert-butyl Rinse with ether and dry under reduced pressure to obtain 94.8 g of parecoxib sodium crystals with a yield of 94.8%. Related substances adopt HPLC method, and the total impurity is 0.02%; use Cu-ka ray to carry out X-ray powder measurement, its X-ray powder diffraction pattern and attached figure 1 unanimous.

Embodiment 3

[0066] Embodiment 3: Parecoxib sodium for injection (in 1000 bottles, unit: g)

[0067] Parecoxib Sodium

[0068] Preparation process: pour 50% of the prepared water for injection into the liquid preparation tank, cool down to make the temperature lower than 40°C, add the prescribed amount of parecoxib sodium and anhydrous disodium hydrogen phosphate, and stir until dissolved; Adjust the pH to 8.0 with sodium hydroxide or phosphoric acid solution, add 0.05% (W / V) medicinal charcoal, stir and adsorb for 20 minutes, filter with a 0.22 μm PES filter, and then add water for injection to the full amount; fill in 1ml per bottle Place in a vial; freeze-dry in a freeze-drying box, drop the plate layer from room temperature to -40°C for 30 minutes, and maintain it for 4 hours to completely freeze the sample. Turn on the condenser, and when the temperature of the condenser drops below -45°C , turn on the vacuum pump to evacuate, the pre-vacuum is lower than 0.2mbar, and start ...

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Abstract

The invention provides a parecoxib sodium pharmaceutical composition for injection and a preparation method thereof. The parecoxib sodium pharmaceutical composition for injection has the advantages that prescription of the parecoxib sodium pharmaceutical composition for injection is simple, dosage of disodium hydrogen phosphate is decreased greatly as compared with that of the prior art, and requirement for injection medicine safety is met well; since parecoxib sodium is in the shape of crystal, time for dissolution is shortened and time for dosing is then shortened, quality stability is guaranteed, and production efficiency is improved; by a rapid freezing process during preparation, free-dried products maintain good pore structure with quite uniform granularity which is favorable for complete sublimation of moisture; since a nitrogen charge operation is omitted, production procedure is simplified, cost is reduced, and socialized mass production is facilitated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition of parecoxib sodium for injection and a preparation method thereof. Background technique [0002] Parecoxib sodium, chemical name: N-[[4-(5-methyl-3-phenyl-4-isoxazolyl)phenyl]sulfonyl]propionamide sodium salt, chemical structural formula: [0003] [0004] Parecoxib sodium is a highly selective COX-2 inhibitor, which belongs to the coxib analgesics in anti-arthritis drugs, and can be used for short-term treatment of pain after surgery. Parecoxib sodium is easily hydrolyzed into valdecoxib, and valdecoxib has poor solubility in water, which makes it difficult to make injections. As the prodrug of valdecoxib, parecoxib sodium has high solubility. In order to avoid its rapid transformation into valdecoxib in aqueous solution, parecoxib sodium is mainly made into lyophilized preparations. [0005] Although parecoxib is rapidly converted in...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/42A61K47/04A61P29/00A61P19/02C07D261/08
CPCA61K9/0019A61K9/19A61K31/42A61K47/02C07B2200/13C07D261/08
Inventor 王颖张亚兰
Owner CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
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