Levoamlodipine besylate tablet and preparation method thereof

A technology of levamlodipine besylate and levorotatory besylate, which is applied in the field of levamlodipine besylate tablets and its preparation, to achieve the effects of being easy to take, high yield, and inhibiting the production of impurity D

Active Publication Date: 2022-07-08
HAINAN JINRUI PHARMA CO LTD
View PDF20 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Magnesium stearate is a relatively common pharmaceutical excipient, which is usually used as a glidant, lubricant and anti-adhesive agent. A small amount of intake will not cause great harm to the human body, but long-term use will cause respiratory system, diseases of the skin

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
  • Levoamlodipine besylate tablet and preparation method thereof
  • Levoamlodipine besylate tablet and preparation method thereof
  • Levoamlodipine besylate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 A kind of preparation method of levamlodipine besylate

[0028] The present embodiment is a preparation method of levamlodipine besylate, and the specific preparation process comprises the following steps:

[0029] 1) Preparation of S-(-)-amlodipine-R-(-)-mandelate

[0030] Take 950 mL of N,N-dimethylformamide and 150 mL of water (the volume ratio of N,N-dimethylformamide to water is BL1=6.33:1), stir and mix evenly, and filter to obtain a resolution aid solution for backup;

[0031] Take 20.7g of R-(-)-mandelic acid and add it to 200mL of resolution aid solution, stir to dissolve, filter to remove insoluble impurities, and obtain a resolution agent solution for subsequent use;

[0032] Take 100g of racemic amlodipine and add it to 700mL of resolution aid solution, stir to dissolve, filter to remove insoluble impurities, add resolution solution dropwise to the filtrate, stir and react at room temperature for 1h, add a trace amount of S-(-)-ammonia Seed c...

Embodiment 2～6

[0037] The preparation method of embodiment 2~6 levamlodipine besylate

[0038] Embodiments 2~6 are respectively a kind of preparation method of levamlodipine besylate, and their steps are basically identical with embodiment 1, and the difference is only in the difference of raw material consumption and process parameter, see Table 1 for details:

[0039] List of various process parameters in Table 1 Examples 2 to 6

[0040]

[0041] The contents of other parts of Examples 2 to 6 are the same as those of Example 1.

[0042] The levamlodipine besylate prepared in Examples 1-6 has high yield and good purity.

Embodiment 7

[0043] Embodiment 7 A kind of preparation method of levamlodipine besylate tablet

[0044] In the present embodiment, the prescription of levamlodipine besylate tablet is as follows:

[0045] Table 2 prescription (specification: 5mg in terms of levamlodipine)

[0046] Levoamlodipine besylate (from Example 1) 6.94g microcrystalline cellulose 100g Sodium starch glycolate 85g calcium phosphate 0.8g Xylitol 8g production 1000 pieces

[0047] In the present embodiment, the preparation method of levamlodipine besylate tablet comprises the following steps:

[0048] S1) drying microcrystalline cellulose, sodium starch glycolate, calcium phosphate and xylitol at 60°C for 2h respectively, passing through a 60-mesh sieve, for subsequent use;

[0049] S2) respectively take the microcrystalline cellulose, sodium starch glycolate, calcium phosphate and xylitol of the recipe quantity, adopt the equal amount incremental addition method, stir and mi...

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
angle of reposeaaaaaaaaaa
hardnessaaaaaaaaaa
hardnessaaaaaaaaaa
Login to view more

Abstract

The invention provides levamlodipine besylate tablets and a preparation method thereof, belonging to the technical field of drug preparation. Weight parts, 30-90 weight parts of sodium starch glycolate, 0.5-1 weight part of calcium phosphate and 5-10 weight parts of xylitol are mixed and pressed into tablets to obtain the levamlodipine besylate tablet. In the present invention, calcium phosphate and xylitol in appropriate proportions are used as glidants, and the prepared levamlodipine besylate tablets are complete, good in gloss, stable in tablet weight, less than 39° in angle of repose, and more than 55N in hardness.

Description

technical field [0001] The invention relates to the preparation of tablets, in particular to a levamlodipine besylate tablet and a preparation method thereof. Background technique [0002] Levoamlodipine besylate is a powerful dihydropyridine calcium channel blocker, which has the effect of vasodilating and can be used to treat hypertension, angina pectoris and other diseases. Amlodipine besylate has two isomers, levorotatory and dextrorotatory. The calcium ion activity of the levorotatory isomer is 1000 times that of the dextrorotatory isomer and twice that of the racemate. Since the drug activity of the levorotatory form is significantly higher than that of the racemate, the resolution of amlodipine besylate is still a research focus in the preparation process of levamlodipine besylate. [0003] Currently, methods for the preparation of enantiomerically pure amlodipine mainly focus on the resolution of racemates, i.e. the separation of the enantiomers of racemic mixtures ...

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): A61K9/20A61K31/4422A61K47/38A61K47/36A61K47/02A61K47/26A61P9/10A61P9/12
CPCA61K31/4422A61K9/2054A61K9/2059A61K9/2009A61K9/2018A61P9/12A61P9/10
Inventor 王寿春黄月娜王小芳
Owner HAINAN JINRUI 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