Unlock instant, AI-driven research and patent intelligence for your innovation.

Method for preparing azilsartan solid dispersion by supercritical antisolvent method

A technology of supercritical anti-solvent and solid dispersion, which is applied in the field of medicine, can solve the problems of unsuitable preparation of azilsartan solid dispersion, etc., and achieve the effect of highlighting substantive characteristics, significant progress, and improved dissolution performance

Active Publication Date: 2020-01-24
CHINA PHARM UNIV
View PDF4 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for preparing azilsartan solid dispersion by supercritical antisolvent method
  • Method for preparing azilsartan solid dispersion by supercritical antisolvent method
  • Method for preparing azilsartan solid dispersion by supercritical antisolvent 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 Beijing Sartorius Instrument System Co., Ltd....

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
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