Stabilized divalproex sodium coated granules, preparation method and solid preparation thereof

A technology of divalproex sodium and coated granules, which is applied in the direction of medical preparations of non-active ingredients, pill delivery, and pharmaceutical formulations, which can solve the problem of increasing operating costs, which is not conducive to the work of preparation production personnel, divalproex sodium Instability in the storage process and other problems, to achieve the effect of good fluidity

Active Publication Date: 2011-09-21
ZHEJIANG HUAHAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The relative humidity of the normal solid preparation production environment is between 45% and 65%. The relative humidity of the environment below 20% disclosed in this patent requires a dehumidification and air conditioning system, which increases equipment investment and operating costs during the production process. At the same time, 20% The working environment of relative humidity is also not conducive to the work of preparation production personnel
[0005] In order to solve the problem of instability and easy caking of divalproex sodium during storage, as well as the problem of sticking and punching of the product during tablet compression, the inventors have successfully prepared divalproex sodium through extensive laboratory and industrial-scale research. Sodium valproate coated granules, invented a method for preparing divalproex sodium coated granules

Method used

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  • Stabilized divalproex sodium coated granules, preparation method and solid preparation thereof
  • Stabilized divalproex sodium coated granules, preparation method and solid preparation thereof
  • Stabilized divalproex sodium coated granules, preparation method and solid preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Divalproex sodium is pulverized to obtain 1 kg of powder whose particle size D (90) is 327 μm; 100 g of hypromellose (E5) is dissolved in 1900 g of purified water to prepare a solution of 5% concentration; 1 kg of pulverized divalproex Sodium valerate and 20g of micropowder silica gel are placed in the ENGER fluidized bed of the model WBF-III, and the mode of bottom spray coating is adopted, and the air inlet flow rate is set to 80m 3 / h, the inlet air temperature is 50°C, after the fluidized state is formed in the fluidized bed, the hypromellose solution is sprayed into the material surface of the fluidized bed through the peristaltic pump, the atomization pressure is 150kPa, and the peristaltic pump speed is 25rpm, after the hypromellose solution is sprayed, the air inlet temperature is raised to 65°C for drying, and when the drying weight loss of the material measured by the infrared moisture analyzer is ≤3.0%, the drying is stopped to obtain the hydroxypropyl methylc...

Embodiment 2

[0047] Divalproex sodium is pulverized to obtain 1kg particle diameter D (90) is the powder of 634 μm; 18g glyceryl monostearate, 60g triethyl citrate and 7.2g polysorbate 80 are dissolved in 655g purified water, then add to 2000g In L 30D-55, stir evenly to obtain a coating solution with a solid content of 25%; place 1 kg of pulverized divalproex sodium in an ENGER fluidized bed model WBF-III, and use top spray coating mode, Set the air intake flow rate to 80m 3 / h, the air inlet temperature is 50°C, after forming a fluidized state in the fluidized bed, the coating solution is sprayed into the material surface of the fluidized bed through a peristaltic pump, the atomization pressure is 200-250kPa, and the peristaltic pump speed is 20-50rpm , after the coating solution is sprayed, the air inlet temperature is increased to 65°C, and dried, and the drying is stopped when the drying weight loss of the material measured by the infrared moisture analyzer is ≤3.0%, and the coated ...

Embodiment 3

[0049] Divalproex sodium is pulverized to obtain 200g of a powder whose particle size D (90) is 32 μm; 200 g of hydroxypropyl cellulose (EF) is dissolved in 3800 g of purified water to prepare a solution of 5% concentration; 200 g of pulverized divalproex Sodium bicarbonate is dispersed in the solution of hydroxypropyl cellulose, spray-dried in BUCHI-290 spray dryer, the air flow rate is 100m 3 / h, the air inlet temperature is 125°C, the air outlet temperature is 50°C, the spray rate is 25%, the suction power is 100%, and the air pressure is 85psi to obtain the hyprolose-coated granules of divalproex sodium. The bulk density of the sodium-coated particles is 0.273 g / ml, the particle size D(90)=82 μm, and has good fluidity.

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Abstract

The invention discloses stabilized divalproex sodium coated granules containing cores of divalproex sodium crystal granules and coatings made of coating material. The invention also discloses a preparation method of the coated granules and a solid preparation containing the divalproex sodium coated granules. The divalproex sodium coated granules are characterized in that: no caking occurs after long-term storage, and preparations are easily prepared by using the granules.

Description

technical field [0001] The invention relates to coated granules of divalproex sodium used for treating epilepsy, bipolar affective disorder and migraine, a preparation method thereof, and a solid preparation containing the divalproex sodium coated granules. Background technique [0002] Divalproex sodium is an important drug for the treatment of epilepsy, bipolar disorder, migraine and other nervous system diseases with the following structure. [0003] [0004] Divalproex sodium is a new compound prepared from valproic acid and sodium valproate as intermediates. As a derivative of valproic acid, divalproex sodium solves the problem of strong hygroscopicity of sodium valproate , has stable physical properties, and has little hygroscopicity. However, the intermolecular forces of divalproex sodium are very strong. During the storage process, the API will gather into agglomerates in a short period of time to form a solid block, and the divalproex sodium stored in the whole ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/20A61K47/12A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P25/08A61P25/06A61P25/00
Inventor 李巧霞杜江永邱宗杰彭俊清胡功允
Owner ZHEJIANG HUAHAI PHARMA CO LTD
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