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Technical study for preparing Nim-PLLA (nimesulide-poly-l-lactic acid) composite microsphere with supercritical anti-solvent method

A technology of L-polylactic acid and composite microspheres is applied in the directions of anti-inflammatory agents, drug combinations, non-central analgesics, etc., and can solve the problems of difficulty in product separation and purification, low product bioavailability, and large product particle size, etc. Achieve uniform morphology, high product yield and uniform particle size distribution.

Inactive Publication Date: 2016-06-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These traditional methods have many problems that are difficult to solve, such as low encapsulation efficiency, large product particle size and wide distribution, etc.
These problems lead to difficulties in the separation and purification of the product, as well as the disadvantages of low bioavailability of the product.

Method used

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  • Technical study for preparing Nim-PLLA (nimesulide-poly-l-lactic acid) composite microsphere with supercritical anti-solvent method
  • Technical study for preparing Nim-PLLA (nimesulide-poly-l-lactic acid) composite microsphere with supercritical anti-solvent method
  • Technical study for preparing Nim-PLLA (nimesulide-poly-l-lactic acid) composite microsphere with supercritical anti-solvent method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0035] Weigh 100 mg of nimesulide raw material, 500 mg of L-polylactic acid, dissolve in 20 mL of dichloromethane to form a solution. Set the pressure in the crystallization tank to 10MPa, the temperature to 40°C, and remove the air in the tank. After the pressure and temperature are constant, adjust the flow control valve to keep the CO 2 The exhaust speed is 8L / min, start the high-efficiency liquid phase pump, and the solution is input into the crystallization kettle at a speed of 0.8mL / min. After the solution completely enters the crystallization kettle, keep the gas in and out for more than 30 minutes. Subsequent shutdown of the CO 2 Inlet valve, depressurize and remove sample.

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Abstract

The invention relates to a method for preparing a Nim-PLLA (nimesulide-poly-l-lactic acid) composite microsphere with a supercritical anti-solvent crystallization technology. The nimesulide sustained-release microsphere with a sustained-release effect is prepared. The grain size of the drug composite microsphere can be effectively controlled through change of the drug solvent variety, the solution concentration, the crystallization pressure, the crystallization temperature, the flow velocity of the introduction of a solution sample and the like, and the grain size of the prepared microsphere is in a range from 1 mu m to 10 mu m. According to the drug sustained-release microsphere prepared with the method, the drug solubility and the drug sustained-release property are effectively improved.

Description

technical field [0001] The invention relates to a method for preparing nimesulide-L-polylactic acid sustained-release microspheres, in particular to a method for preparing nimesulide-L-polylactic acid sustained-release microspheres using supercritical fluid technology. Background technique [0002] Nimesulide is a non-steroidal anti-inflammatory drug. Nimesulide is mainly used for antipyretic, analgesic, anti-inflammation, treatment of rheumatic pain, headache, trauma pain, cancer pain, etc., and it is widely accepted clinically because of its small digestive tract side effects. Nimesulide has the effect of anti-proliferation and induction of apoptosis on various tumor cells such as esophageal cancer, colon cancer and liver cancer. It is considered to be a non-steroidal anti-inflammatory drug with fast onset, good curative effect, high safety and good development prospects. Compared with ibuprofen and acetaminophen, nimesulide has faster antipyretic and analgesic effects. ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/18A61K47/34A61P29/00
CPCA61K9/1641A61K31/18
Inventor 王志祥印东航黄德春缪虹刚刘尚德王为彦程月
Owner CHINA PHARM UNIV
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