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Method for preparing metoprolol tartrate particles

A technology of metoprolol tartrate and toprolol granules, which is applied in the field of medicine and can solve the problems of difficult granulation, easy moisture oxidation, and easy sticking.

Active Publication Date: 2012-10-10
GRAND PHARM (CHINA) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The water solubility of metoprolol tartrate is greater than 700mg / ml, but most of the traditional wet granulation uses starch, dextrin or starch dextrin dissolved in purified water and punched as a binder, which is easy to produce when preparing metoprolol tartrate granules. Dissolution, easy sticking and punching, the resulting particles have poor fluidity and are easy to be oxidized by moisture, which brings difficulties to granulation

Method used

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  • Method for preparing metoprolol tartrate particles
  • Method for preparing metoprolol tartrate particles
  • Method for preparing metoprolol tartrate particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Preparation of Metoprolol Tartrate Granules

[0017] Metoprolol tartrate granules prescription:

[0018]

[0019] Preparation process:

[0020] 1. Preparation of adhesive: Preparation of acrylic resin No. II liquid paraffin ethanol solution: the day before production, take the prescribed amount of acrylic resin No. II and dissolve it in ethanol to completely dissolve it, then add liquid paraffin and stir well ,spare.

[0021] 2. Take the prescribed amount of metoprolol tartrate raw materials, auxiliary materials starch, pregelatinized starch, and microcrystalline cellulose and place them in a high-efficiency wet granulator to fully mix the main drug and auxiliary materials. Add an appropriate amount of standby acrylic resin No. II liquid paraffin ethanol solution to make soft materials, wet granules, dry, and dry granules, then add the prescribed amount of magnesium stearate and mix evenly, test, fill capsules (or tablet), process Aluminum and plastic pa...

Embodiment 2

[0022] The influence of embodiment 2 different binders on the preparation of metoprolol tartrate granules

[0023] The acrylic resin No. II liquid paraffin ethanol solution in the process of Example 1 was replaced with starch slurry, dextrin slurry, and starch dextrin slurry respectively, and samples 1, 2, and 3 were obtained respectively through preparation, and compared with the samples of Example 1 , the impact of different binders on the preparation of metoprolol tartrate granules is as follows:

[0024]

[0025] Conclusion: Using acrylic resin No. II liquid paraffin ethanol solution as a binder, its soft material, drying time, granule weight gain by wetting, granule fluidity, granule compressibility, and granule tablet integrity are all better than others. 3 samples.

Embodiment 3

[0026] The influence of embodiment 3 different binders on the stability of metoprolol tartrate granules

[0027] Carry out long-term stability test comparison by embodiment 1 sample and sample 1,2,3:

[0028] Take samples and pack them in aluminum-plastic bags of 2 grams per bag, place them for 6 months at a temperature of 40°C ± 2°C, and a relative humidity of 75% ± 5%. Sampling once at the end of every month and six months, focusing on the change of related substances and content of the particles.

[0029]

[0030]

[0031] Conclusion: Comparing the long-term stability test between the sample of Example 1 and samples 1, 2, and 3, the sample of Example 1 is stable, while the related substances of samples 1, 2, and 3 increase and their content decreases.

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Abstract

The invention relates to a method for preparing metoprolol tartrate particles by a using a high-efficiency wet method mixing granulator. According to the method, a specific variety of auxiliary materials in a certain ratio are involved, and the metoprolol tartrate particles are prepared by using a coating material acrylic resin No.2 white oil ethanol solution as adhesive; the method is obviously superior to the conventional method in which starch and dextrin slurry are used; and the metoprolol tartrate particles prepared by the method are simple in preparation process, high in flowability andcompressibility, and strong in bond resistance, have the effect of insulating air to be prevented from being moisturized and oxidized, and are particularly suitable for being stuffed into capsules and pressed into tablets; and the quality problems that the metoprolol tartrate is easy to dissolve and stick and the like can be effectively solved.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a method for preparing granules, in particular to a method for preparing metoprolol tartrate granules. Background technique [0002] Metoprolol tartrate is widely used clinically to treat hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, cardiac neurosis, etc., and it is still used in the treatment of heart failure in recent years. treat. [0003] Metoprolol tartrate is white or off-white crystalline powder; odorless and bitter. Soluble, almost insoluble in ether; soluble in glacial acetic acid. [0004] The water solubility of metoprolol tartrate is greater than 700mg / ml, but most of the traditional wet granulation uses starch, dextrin or starch dextrin dissolved in purified water and punched as a binder, which is easy to produce when preparing metoprolol tartrate granules. Dissolution, easy sticking and pun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/205A61K31/138A61K47/44A61K47/32A61P9/12A61P9/10A61P9/06A61P5/16A61P9/00A61P25/02A61P9/04
Inventor 杨景华耿海明熊辉陈志平雷娟胡晓岚
Owner GRAND PHARM (CHINA) CO LTD
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