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Method for preparing celecoxib nano-crystal preparation

A technology of celecoxib and nanocrystals, which is used in anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of long preparation time, easy pollution, etc., and meets the requirements of equipment and personnel quality. The effect of low burden and low energy consumption

Inactive Publication Date: 2018-09-18
LIAOCHENG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the media grinding method is considered to have shortcomings such as long preparation time and easy pollution, the method is simple to operate, high in production efficiency, strong in controllability, and good in reproducibility, and is suitable for large-scale industrial production. An important method that must be investigated for the preparation of pharmaceutical nano-preparations

Method used

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  • Method for preparing celecoxib nano-crystal preparation
  • Method for preparing celecoxib nano-crystal preparation
  • Method for preparing celecoxib nano-crystal preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 4g of hydroxypropyl cellulose (HPC) and 0.5g of sodium dodecyl sulfate (SDS), add 500mL of pure water, and stir slowly for 30min until the solution is clear. Weigh 20 g of the celecoxib bulk drug, add the above aqueous solution under slow stirring, and disperse the bulk drug particles in the solution to obtain a coarse suspension. Add 250mL of grinding media (specification d=0.3mm) into the grinding chamber (500mL) of the sand mill, and feed the coarse suspension into the grinding chamber through a feed pump, and grind for 100min at a speed of 10m / s to obtain a nanosuspension. The obtained nanosuspension was freeze-dried at -55° C. for 10 h to obtain a celecoxib nanocrystal preparation.

Embodiment 2

[0030] Weigh 4g of hypromellose acetate succinate (HPMC-AS) and 0.5g of sodium dodecyl sulfate (SDS), add 500mL of pure water, and stir slowly for 30min until the solution is clear. Weigh 20 g of the celecoxib bulk drug, add the above aqueous solution under slow stirring, and disperse the bulk drug particles in the solution to obtain a coarse suspension. Add 250mL of grinding media (specification d=0.3mm) into the grinding chamber (500mL) of the sand mill, and feed the coarse suspension into the grinding chamber through a feed pump, and grind for 100min at a speed of 10m / s to obtain a nanosuspension. The obtained nanosuspension was freeze-dried at -55° C. for 10 h to obtain a celecoxib nanocrystal preparation.

Embodiment 3

[0032] Weigh 4g of polyvinylpyrrolidone (PVP K30) and 0.5g of sodium dodecyl sulfate (SDS), add 500mL of pure water, and stir slowly for 30min until the solution is clear. Weigh 20 g of the celecoxib bulk drug, add the above aqueous solution under slow stirring, and disperse the bulk drug particles in the solution to obtain a coarse suspension. Add 250mL of grinding media (specification d=0.3mm) into the grinding chamber (500mL) of the sand mill, and feed the coarse suspension into the grinding chamber through a feed pump, and grind for 100min at a speed of 10m / s to obtain a nanosuspension. The obtained nanosuspension was freeze-dried at -55° C. for 10 h to obtain a celecoxib nanocrystal preparation.

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Abstract

The invention provides a method for preparing a celecoxib nano-crystal preparation, and belongs to the field of medicinal preparations. The preparation is prepared from the following components in percentage by weight: 60-85 percent of celecoxib, 10-30 percent of a spatial stabilizer and 1-10 percent of an ionic stabilizer. According to the prescription, a celecoxib nano-crystal suspension is prepared by adopting a wet medium grinding method, is subjected to freeze-drying or spray-drying technique to prepare solid powder. The celecoxib nano-crystal preparation prepared by the prescribed process has the characteristics of simple preparation process, high safety, high drug loading capacity and good stability. Dissolution in-vitro and rat in-vivo pharmacokinetic experiments evaluation provesthat the dissolution and bioavailability of celecoxib in the nano-crystal preparation can be remarkably improved.

Description

technical field [0001] The invention relates to a preparation method of a nano-crystal powder preparation of celecoxib, which belongs to the technical field of medicines. Background technique [0002] Celecoxib (CXB) is a specific and selective non-steroidal anti-inflammatory analgesic drug commonly used in clinical practice. It was successfully developed by GD Searle & Pfizer in the United States and was launched in the United States in 1999. In 2000, my country approved the import of Pfizer's celecoxib preparation product, whose trade name is Celebrex (CELEBREX). Compared with traditional non-steroidal anti-inflammatory analgesics, CXB exerts anti-inflammatory and analgesic effects by specifically inhibiting cyclooxygenase-2 (COX-2) and blocking the synthesis of prostaglandins from arachidonic acid. The curative effect is definite, and the gastrointestinal side effects are effectively reduced. It is clinically applicable to the treatment of acute pain in adults, as well ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/635A61K47/38A61K47/20A61K47/32A61K47/34A61P29/00A61P19/02
CPCA61K9/145A61K9/146A61K31/635A61P19/02A61P29/00
Inventor 丁壮邢杨杨赵燕娜高岩韩军
Owner LIAOCHENG UNIV
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