Benidipine hydrochloride nanoparticle and preparation method thereof

A technology of benidipine hydrochloride and benidipine hydrochloride, applied in the field of medicine, can solve the problems of large energy and time, wide crystal particle size distribution, etc.

Active Publication Date: 2012-10-24
合肥贝霓医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method not only consumes huge energy and time, but also has a wide crystal particle size distribution.

Method used

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  • Benidipine hydrochloride nanoparticle and preparation method thereof
  • Benidipine hydrochloride nanoparticle and preparation method thereof
  • Benidipine hydrochloride nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Add 10 mL of benidipine hydrochloride primary crystals to 10 mL of absolute ethanol, heat to reflux to dissolve, cool down in an ice bath, crystallize with 150W ultrasound for 10 min, and filter with suction to obtain pale yellow crystals. The crystal size is shown in Figure 1.

Embodiment 2

[0033] Add 10 mL of methanol to 10.1 g of primary crystals of benidipine hydrochloride, heat to reflux to dissolve, cool down in an ice bath, crystallize with 150 W ultrasound for 10 min, and suction filter to obtain light yellow crystals.

Embodiment 3

[0035] Add 10.2g of benidipine hydrochloride primary crystals, add 12mL of absolute ethanol, heat to reflux to dissolve, add 12mL of water, cool down in an ice bath, 150W ultrasonic, continue ultrasonication for 2min after crystallization.

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Abstract

The present invention relates to nanoparticles of benidipine hydrochloride (+ / -)-(R*)-1, 4-dihydro-2, 6-dimethyl-4-(m-nitrophenyl)-3, 5-picolinic acid methyl ester [(R*)-1-benzyl-3-piperidine alcohol ester] hydrochloride and an ultrasonic preparation method thereof.

Description

technical field [0001] The invention relates to the technical field of medicine, and is a benidipine hydrochloride (±)-(R*)-1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3 , Nanoparticles of methyl 5-pyridinecarboxylate [(R*)-1-benzyl-3-piperidinol ester] hydrochloride and a preparation method thereof. Background technique [0002] Dihydropyridine calcium channel blockers are currently widely used clinically because of their safety and effectiveness. Especially benidipine hydrochloride is an ideal, safe and effective antihypertensive and therapeutic renal agent with its unique three-channel blocking effect, high affinity effect on cell membrane, vascular selective effect and renal protection effect. Drugs for essential hypertension, angina pectoris and other diseases. [0003] Because the solubility of benidipine hydrochloride in water is very low, in order to make benidipine hydrochloride dissolve rapidly from the preparation, it is often necessary to pulverize the drug into...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90
CPCC07D401/12A61P9/10A61P9/12A61P13/12A61P43/00
Inventor 张震姚建忠陈建明张兆勇岳立群陈琼
Owner 合肥贝霓医药科技有限公司
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