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Method for preparing azilsartan solid dispersion by supercritical anti-solvent method

A supercritical anti-solvent, solid dispersion technology, applied in the field of medicine, can solve the problems of inappropriate preparation of azilsartan solid dispersion, and achieve the effects of outstanding substantive characteristics, improved dissolution performance, and significant progress

Active Publication Date: 2018-06-01
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the parameters provided by this method are not suitable for the preparation of solid dispersions of azilsartan

Method used

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  • Method for preparing azilsartan solid dispersion by supercritical anti-solvent method
  • Method for preparing azilsartan solid dispersion by supercritical anti-solvent method
  • Method for preparing azilsartan solid dispersion by supercritical anti-solvent method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: Single factor method investigates the impact of each parameter value range on cumulative dissolution rate and recovery rate

[0034] Experimental Instruments and Materials

[0035] The main instruments used in the experiment are shown in Table 1, and the main raw materials and reagents are shown in Table 2.

[0036] Table 1 Main Instruments

[0037] device name

model

Manufacturer

Supercritical Particle Preparation System

Helix

AppliedSeparations, USA

Series1500 high pressure infusion pump

Helix

AppliedSeparations, USA

air compressor pump

TYW-2

Suzhou Tongtong Electromechanical Co., Ltd.

Low temperature constant temperature bath

SDC-6

Nanjing Xinchen Biotechnology Co., Ltd.

UV-visible spectrophotometer

UV-1800

Shimadzu Corporation

Intelligent Dissolution Tester

ZRS-8L

Tianjin Tianda Tianfa Technology Co., Ltd.

Analytical Balances

BS124S

...

Embodiment 2

[0061] Embodiment 2: Application of supercritical antisolvent method to prepare preferred parameters of azilsartan solid dispersion

[0062] The method for preparing azilsartan solid dispersion by supercritical antisolvent method comprises the steps:

[0063] Step S1, dissolving azilsartan and a water-soluble carrier in an organic solvent to obtain azilsartan-carrier mixed solution;

[0064] Step S2, the CO 2 Pass into the crystallization kettle, adjust the temperature and pressure in the crystallization kettle;

[0065] Step S3, continue to feed CO 2 , maintaining the temperature and pressure in the crystallization tank constant, while passing the azilsartan-carrier mixed solution prepared in step S1 into the crystallization tank;

[0066] Step S4, after the azilsartan-carrier solution is passed through, continue to pass through CO 2 , keep the temperature and pressure in the crystallization kettle constant, and release the pressure after a period of time; when the pressu...

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Abstract

The invention discloses a method for preparing an azilsartan solid dispersion by a supercritical anti-solvent method. The method comprises the following steps: S1, dissolving azilsartan and a water-soluble carrier in an organic solvent to obtain a mixed azilsartan-carrier solution; S2, inflating CO2 into a crystallization kettle, and adjusting the temperature and the pressure in the crystallization kettle; S3, continuing inflating CO2, maintaining the temperature and the pressure in the crystallization kettle unchanged, and inletting the mixed azilsartan-carrier solution prepared in the S1 into the crystallization kettle; S4, after inletting of the mixed azilsartan-carrier solution, continuing inflating CO2, maintaining the temperature and the pressure in the crystallization kettle unchanged, relieving the pressure after a period of time, and when the pressure in the crystallization kettle is reduced to the atmospheric pressure, opening the crystallization kettle for collecting the azilsartan solid dispersion, wherein the water-soluble carrier is PVP-K3. By the method, the azilsartan is dispersed in the PVP-K30 in an amorphous form, so that the dissolution rate of the azilsartan can be increased, and the stability thereof can be improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a method for preparing azilsartan solid dispersion by a supercritical antisolvent method. Background technique [0002] Azilsartan (Azilsartan), the molecular formula is C 25 h 20 N 4 o 5 , the product name is AZILVA, developed by Takeda Pharmaceutical Company (Takeda) of Japan, it was launched in Japan in January 2012, and the US FDA approved its listing on February 25, 2011. As a new generation of angiotensin II receptor blocker for the treatment of hypertension, azilsartan can competitively and reversibly cut off the combination of angiotensin II and AT1 receptor, thereby lowering blood pressure. Azilsartan is a poorly soluble drug, the solubility in water is less than 9 μg / ml, and the solubility in organic solvents is also very low. After the drug is absorbed, its effect mainly depends on the water solubility of its active ingredients and the permeability to...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/32A61K31/4245A61P9/12
CPCA61K9/1635A61K9/1682A61K31/4245
Inventor 王志祥宋雅琴徐文博陈震缪虹刚王为彦
Owner CHINA PHARM UNIV
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