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Preparation method of Levamlodipine besylate tablet

Inactive Publication Date: 2013-01-02
YANGZIJIANG PHARMA GROUP SHANGHAI HAINI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] But, because levamlodipine besylate is slightly soluble in water, the dissolution rate of levamlodipine besylate prepared by general method is relatively low, which is not suitable for rapid onset of action of medicine, and has certain influence on clinical application
Thereby, adopt improved method to prepare levamlodipine besylate, for example, can improve its stripping by micronization, but this method has defect, in actual preparation, after hydrophobic material pulverizes, with the reduction of particle size If the particle size is small, the surface free energy increases, and the particles are prone to re-agglomeration, so the crushing efficiency is not high; Enhanced, not conducive to the dissolution of the tablet

Method used

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  • Preparation method of Levamlodipine besylate tablet
  • Preparation method of Levamlodipine besylate tablet
  • Preparation method of Levamlodipine besylate tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] (1) Formula: (calculated on the basis of 1,000,000 plain tablets)

[0022]

[0023] The filler is: microcrystalline cellulose, calcium hydrogen phosphate

[0024] The disintegrant is sodium carboxymethyl starch, the lubricant is magnesium stearate

[0025] The above raw and auxiliary materials are all sold in the market.

[0026] (2) method:

[0027] Firstly, levamlodipine besylate and calcium hydrogen phosphate are pulverized through a 100-mesh sieve, microcrystalline cellulose and carboxymethyl starch sodium are pulverized through a 80-mesh sieve, and then mixed together. Then, mix evenly through a fluidized bed one-step granulator, and the air volume during granulation is 854-964m3 / h; the spray speed is 75rpm; the spray pressure is 1.7bar. Dry, the air volume is 854~964m when dry 3 / h; material temperature 20℃~60℃; set inlet air temperature 40℃~80℃, control moisture 1.5~2.5%. After passing through the 24-mesh sieve, add lubricant and mix evenly in the mixer. ...

Embodiment 2

[0029] The stability of the levamlodipine besylate that embodiment 1 method makes, dissolution rate investigation test:

[0030] 1. Prescription ingredients:

[0031] According to the compatibility test method of excipients, calcium hydrogen phosphate (CaHPO4), lactose and levamlodipine besylate (main drug) were mixed in a ratio of 5:1 respectively, and the prepared samples were respectively placed in an oven at 60° C. 0 day, 5 days, and 10 days to investigate the changes of related substances. To investigate the compatibility of excipients and main ingredients.

[0032] Table 1 Prescription screening test results

[0033]

[0034] The above results show that the application of calcium hydrogen phosphate is more conducive to controlling the amount of related substances in levamlodipine besylate tablets than lactose.

[0035] 2 Stability test results

[0036] (1). Illumination test Take levamlodipine besylate tablets (prepared in Example 1), put them in an open petri dis...

Embodiment 3

[0046] Example 3 The key indicators of the levamlodipine besylate tablets prepared by the method in Example 1 were compared with those of the "Shihuida" product purchased in the market.

[0047] According to the following method, compare the key indicators of commercially available products and self-developed products, that is, related substances, dissolution rate, and content.

[0048] (1) the levamlodipine besylate sheet that embodiment 1 method makes

[0049] 【Related Substances】Keep away from light. Take an appropriate amount of this product’s fine powder (approximately equivalent to levamlodipine 15 mg), accurately weigh it, put it in a 25ml measuring bottle, add an appropriate amount of mobile phase, sonicate to dissolve levamlodipine, let it cool, and dilute to the mark with mobile phase , Shake up, filter, get the continued filtrate as the test solution; precision measure 1ml, put in a 100ml measuring bottle, dilute to the mark with mobile phase, shake up, as the cont...

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Abstract

A preparation method of a Levamlodipine besylate tablet includes pulverizing Levamlodipine besylate, a filler and a disintegrant, sieving, mixing, adding a lubricant, granulating, and tableting. The invention reduces the amount of related substance of the Levamlodipine besylate tablet, and improves stability. The method uses a fluidized bed granulation step to prepare the Levamlodipine besylate tablet, so as to simplify preparation step, shorten time, optimize process parameter, significantly increase the dissolution of the product and improve quality. The inventive method is suitable for industrial production.

Description

technical field [0001] The invention relates to medicine preparation, in particular to a preparation method for long-term stability of levamlodipine besylate tablets and improving its dissolution rate. Background technique [0002] Levoamlodipine besylate is a calcium ion antagonist, which has antihypertensive effects and relieves angina pectoris, and has been used clinically. [0003] But, because levamlodipine besylate is slightly soluble in water, the dissolution rate of levamlodipine besylate prepared by the general method is relatively low, which is not suitable for rapid drug onset, and has certain influence on clinical application. Thereby, adopt improved method to prepare levamlodipine besylate, for example, can improve its stripping by micronization, but this method has defect, in actual preparation, after hydrophobic material pulverizes, with the reduction of particle size If the particle size is small, the surface free energy increases, and the particles are pron...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4422A61P9/12A61P9/10
Inventor 郭晓静戴学忠徐赟姚书扬
Owner YANGZIJIANG PHARMA GROUP SHANGHAI HAINI PHARMA
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