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Method for micronization of raw materials of dihydropyridine antihypertensive drugs

A technology of drug addition, applied in the field of micronization of dihydropyridine antihypertensive drug raw materials, which can solve the problems of difficult particle size, low yield, and high energy consumption in the process

Active Publication Date: 2021-02-26
HEFEI LIFEON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, the most common method is to use jet milling method to micronize pharmaceutical raw materials, but the particle size after pulverization by jet milling method is too large, and it often needs to be pulverized twice or even multiple times to meet the required particle size requirements, but it is difficult to achieve a particle size below 10um
And the yield is low, and the process energy consumption is also large

Method used

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  • Method for micronization of raw materials of dihydropyridine antihypertensive drugs
  • Method for micronization of raw materials of dihydropyridine antihypertensive drugs
  • Method for micronization of raw materials of dihydropyridine antihypertensive drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Get and meet " Chinese Pharmacopoeia " 2015 edition quality standards Felodipine crude drug powder (D90 is 76 μ m) 10.0g, be placed in the 50ml round bottom flask that is equipped with condenser, add concentration and be 95% ethanol (the first solvent) 30.0g mL, and then under electromagnetic stirring, dissociate in a 60°C water bath until completely dissolved, then continue to heat and stir for 5 minutes, then remove the hot water bath, and let the solution naturally cool to room temperature for later use.

[0070] Pour the prepared ethanol (first solvent) solution in which the felodipine crude drug powder is dissolved into a preheated dropping funnel for subsequent use.

[0071] A 1500ml reaction flask equipped with an electric stirrer and a thermometer was placed in an ice-salt water pot, and then 900mL of purified water (second solvent) was added to the round bottom flask. After the addition was complete, the electric stirring was started to cool down.

[0072]When ...

Embodiment 2～ Embodiment 22

[0076] The main process parameters of Examples 2-22 are recorded in Table 1, and for other parameters not recorded in Table 1, please refer to the content of Example 1. Wherein, the second solvent of embodiment 2~20 is water, and the second solvent of embodiment 21 is the sodium chloride aqueous solution that concentration is 1.0%, and the second solvent of embodiment 22 is the lauryl sulfuric acid of concentration 0.4% sodium solution.

Embodiment 23

[0078] Get the felodipine crude drug powder (D 90 76μm) 10g, put in a round bottom flask, then add 30mL of prepared ethanol (the first solvent), and heat it on a 60°C water bath until it is completely dissolved, then continue to keep stirring for 5min, then remove the hot water bath, and dissolve the solution Allow to cool naturally to room temperature for later use.

[0079] Pour the prepared ethanol solution dissolving the felodipine crude drug powder into the preheated spray gun for standby.

[0080] A 1500mL round-bottomed flask equipped with an electric stirrer and a thermometer was placed in an ice-salt bath, and then 900mL of purified water (second solvent) was added to the round-bottomed flask. After the addition was complete, the electric stirring was started to cool down.

[0081] When the water temperature in the round bottom flask drops to about 1°C, adjust the stirring speed to 650r / min, then adjust the spray gun pressure to 35KPa, and spray the above concentrati...

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PUM

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Abstract

The application provides a new method for micronizing dihydropyridine antihypertensive drug raw materials, which relates to the technical field of biopharmaceutical preparations. A new method for micronizing dihydropyridine antihypertensive drug raw materials, comprising: dissolving the dihydropyridine antihypertensive drug raw materials in a first solvent, dissolving the first dihydropyridine antihypertensive drug raw materials The solvent is added to the second solvent to realize anti-solvent recrystallization of dihydropyridine antihypertensive drugs; the first solvent includes lower aliphatic alcohols or aliphatic ketones; the second solvent includes water, an aqueous solution containing electrolytes, or surfactants aqueous solution. The method can further improve the in vivo bioavailability of the oral preparations of felodipine and other dihydropyridine antihypertensive drugs.

Description

technical field [0001] The present application relates to the technical field of biopharmaceutical preparations, in particular to a new method for micronizing dihydropyridine antihypertensive drug raw materials. Background technique [0002] Felodipine (felodipine) is currently one of the most widely used dihydropyridine antihypertensive drugs, and the most commonly used in clinical practice is its oral sustained and controlled release preparations. The biopharmaceutical classification of felodipine is BCSII, which belongs to low solubility and high permeability drugs, and improving the solubility of the poorly soluble drug in the preparation to ensure drug absorption in the body is a problem that must be solved for felodipine slow and controlled release preparations. Among the solubilization solutions for insoluble drugs, drug micronization is the most commonly used, convenient and effective method. [0003] In the prior art, the most common method is to use jet milling me...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/90
CPCC07D211/90
Inventor 李孝常李冰李春正陈军季永明季俊虬苗青
Owner HEFEI LIFEON PHARMA
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