Preparation method of valsartan particles

A technology of valsartan granules and valsartan, applied in the field of medicine and chemical industry, can solve the problems of poor fluidity, poor uniformity, uneven mixing, etc., and achieve the effects of avoiding the introduction of risks, improving uniformity and improving fluidity.

Pending Publication Date: 2021-04-06
ZHEJIANG HUAHAI PHARMA CO LTD
View PDF0 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] After recrystallization and drying of valsartan raw material drug, when crushing with ordinary mechanical pulverizer, the particle size of the obtained valsartan is too small (particle size distribution is D10: 0-2μm, D50: 10-30μm), resulting in flow Poor sex
When the preparation is produced in this particle size distribution range, it is very easy to cause bridging and other poor transportation problems at the hopper, which will lead to uneven mixing and poor uniformity, seriously affecting the quality and performance of the drug

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
  • Preparation method of valsartan particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Put 400 kg of crude valsartan and 3200 liters of ethyl acetate into the reaction kettle, heat up to 50°C, and stir until it dissolves. Slowly lower the temperature in the reactor to 39°C, keep it warm for 2 hours, then slowly drop the temperature to 0°C, keep it warm for 2 hours to crystallize. After the crystallization operation is completed, the feed liquid is put into a centrifuge for rejection filtration, and the amount of the filtered mother liquor is controlled to 3000 liters to obtain a wet product of valsartan, and the mass content of ethyl acetate in the wet product is detected to be 30%.

[0027] Install the FZB pulverizer with a sieve with an aperture of 1.0cm, adjust the speed of the pulverizer to 1950rpm, tie a polyethylene bag on the discharge port, start the pulverizer, and slowly add the above-mentioned wet product of valsartan into the working chamber until the processing is completed ; Place the pulverized product in a double-cone vacuum dryer and dry ...

Embodiment 2

[0030] The steps of valsartan recrystallization are the same as in Example 1. After the crystallization operation is completed, the feed liquid is put into a centrifuge for rejection filtration, and the amount of the filtered mother liquor is controlled to 3000 liters to obtain a wet product of valsartan, and the mass content of ethyl acetate in the wet product is detected to be 30%.

[0031] Install the FZB pulverizer with a sieve with an aperture of 2.0cm, adjust the speed of the pulverizer to 3600rpm, tie a polyethylene bag on the discharge port, start the pulverizer, and slowly add the above-mentioned wet product of valsartan into the working chamber until the processing is completed ; Place the pulverized product in a double-cone vacuum dryer and dry it at 55-60°C for 12 hours;

[0032] Install the CFS pulverizer with a sieve with an aperture of 1.6mm, adjust the speed of the pulverizer to 5000rpm, pulverize the dried product, and detect the particle size. The D10 is 4.48...

Embodiment 3

[0034] The steps of valsartan recrystallization are the same as in Example 1. After the crystallization operation is finished, the feed liquid is put into a centrifuge for rejection filtration, and the amount of the filtered mother liquor is controlled to 2900 liters to obtain a wet product of valsartan, and the mass content of ethyl acetate in the wet product is detected to be 45%.

[0035] Install the FZB type pulverizer with a screen with an aperture of 1.0cm, adjust the speed of the pulverizer to 2200rpm, tie a polyethylene bag on the discharge port, start the pulverizer, and slowly add the above-mentioned wet product of valsartan into the working chamber until the processing is completed ; Place the pulverized product in a double-cone vacuum dryer, and dry it at 55-60°C for 13 hours;

[0036] Install the CFS type pulverizer with a sieve with an aperture of 1.2 mm, adjust the speed of the pulverizer to 2000 rpm, and pulverize the dried product. The particle size is detect...

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

PropertyMeasurementUnit
pore sizeaaaaaaaaaa
pore sizeaaaaaaaaaa
Login to view more

Abstract

The invention discloses a preparation method of valsartan particles, which comprises the following steps of pulverizing and screening recrystallized and filtered valsartan wet product, drying, pulverizing and screening again to obtain the valsartan particles. The invention provides valsartan active pharmaceutical ingredient particles with different particle sizes, and valsartan preparations with different requirements can be met.

Description

technical field [0001] The invention relates to a preparation method of valsartan granules, which belongs to the field of medicine and chemical industry. Background technique [0002] Valsartan, chemical name N-(1-pentanoyl)-N[4-[2-(1H-tetrazol-5-yl)phenyl]benzyl]-L-valine, developed by Novartis, First approved for marketing in Germany on July 1, 1996, it is the second non-peptide angiotensin II (AT1) type I receptor antagonist approved for clinical treatment of hypertension. [0003] In the pharmaceutical industry, the particle characteristics of APIs have become one of the crucial factors in product development and quality control of oral solid dosage forms. The particle size distribution of the API will have a significant impact on the performance of the preparation product, such as solubility, bioavailability, content uniformity, stability, etc. In addition, the particle size distribution of the API will also affect the manufacturability of the drug, such as fluidity, ...

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 Applications(China)
IPC IPC(8): A61K9/16A61K31/41A61P9/12
CPCA61K9/1682A61K31/41A61P9/12
Inventor 李伟黄志勇刘永江梁尊俊
Owner ZHEJIANG HUAHAI PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap