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Granules containing dextromethorphan hydrobromide and guaiacol glycerin and preparation method thereof

A technology of dextromethorphan hydrobromide and guaiacol glycerol ether, which can be applied in the directions of ether/acetal active ingredients, bulk delivery, respiratory system diseases, etc. Drug concentration fluctuations, side effects, large fluctuations in blood drug concentration, and many times of administration, etc., to overcome low stability, avoid peak-to-valley phenomenon, and prolong action time.

Inactive Publication Date: 2011-12-21
NANJING CHENGONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the short half-life of dextromethorphan hydrobromide, the general dose is 15-30 mg, which needs to be administered 3-4 times a day, and the blood drug concentration fluctuates greatly, which can easily cause dizziness, headache, drowsiness, irritability, belching, and loss of appetite , constipation, nausea, skin allergies and other side effects
[0005] Compound Yumei preparations in the prior art are mainly dispersible tablets, granules and syrups. These oral preparations are given many times a day and are difficult to overcome hydrogen Side effects caused by large fluctuations in blood concentration of dextromethorphan bromate

Method used

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  • Granules containing dextromethorphan hydrobromide and guaiacol glycerin and preparation method thereof
  • Granules containing dextromethorphan hydrobromide and guaiacol glycerin and preparation method thereof
  • Granules containing dextromethorphan hydrobromide and guaiacol glycerin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Granule prescription one:

[0031]

[0032] Note: Hydroxypropyl-β-cyclodextrin can also choose CAS128446-35-5 (molecular weight 1541.54); or CAS136019-12-0 (molecular weight 1541.54).

[0033] Preparation Process:

[0034] 1) Dry dextromethorphan hydrobromide, guaiacol glyceryl ether, hydroxypropyl-β-cyclodextrin, diluent and adhesive at 50°C for 3 hours, pass through a 100-mesh sieve for use;

[0035] 2) Make hydroxypropyl-β-cyclodextrin a saturated aqueous solution at 45°C, and then place them in a high-speed mixer, start stirring at a speed of 1000r / min;

[0036] 3) Dissolve dextromethorphan hydrobromide in 30% mass-volume ratio of acetonitrile aqueous solution, and then slowly add them dropwise to the saturated hydroxypropyl-β-cyclodextrin aqueous solution prepared in step 2) at a speed of 1 mL / min, continue to stir for 3 hours after the dropwise addition is completed, stop stirring, and spray dry to obtain cyclodextrin inclusion compound;

[0037] 4) Pass th...

Embodiment 2

[0039] Granule prescription two:

[0040]

[0041] Note: Hydroxypropyl-β-cyclodextrin can also choose CAS128446-35-5 (molecular weight 1541.54); or CAS136019-12-0 (molecular weight 1541.54).

[0042] Preparation Process:

[0043] 1) Dry dextromethorphan hydrobromide, guaiacol glyceryl ether, hydroxypropyl-β-cyclodextrin, diluent and adhesive at 50°C for 3 hours, pass through a 100-mesh sieve for use;

[0044] 2) Prepare hydroxypropyl-β-cyclodextrin into saturated aqueous solutions at 60°C, and then place them in high-speed mixers, start stirring at a speed of 3000r / min;

[0045]3) Dissolve dextromethorphan hydrobromide in 30% mass-volume ratio of acetonitrile aqueous solution, and then slowly add them dropwise to the saturated hydroxypropyl-β-cyclodextrin aqueous solution prepared in step 2) and keep stirring, at a speed of 3 mL / min, continue to stir for 3 hours after the dropwise addition is completed, stop stirring, and spray dry to obtain cyclodextrin inclusion compou...

Embodiment 3

[0048] Granule prescription three:

[0049]

[0050] Note: Hydroxypropyl-β-cyclodextrin can also choose CAS128446-35-5 (molecular weight 1541.54); or CAS136019-12-0 (molecular weight 1541.54).

[0051] Preparation Process:

[0052] 1) Dry dextromethorphan hydrobromide, guaiacol glyceryl ether, hydroxypropyl-β-cyclodextrin, diluent and adhesive at 50°C for 3 hours, pass through a 100-mesh sieve for use;

[0053] 2) Prepare hydroxypropyl-β-cyclodextrin into saturated aqueous solutions at 50°C, and then place them in high-speed mixers, start stirring, and rotate at a speed of 750r / min;

[0054] 3) Dissolve dextromethorphan hydrobromide in 30% mass-volume ratio of acetonitrile aqueous solution, and then slowly add them dropwise to the saturated hydroxypropyl-β-cyclodextrin aqueous solution prepared in step 2) and keep stirring, at a speed of 3 mL / min, continue to stir for 3 hours after the dropwise addition is completed, stop stirring, and spray dry to obtain cyclodextrin in...

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Abstract

The invention relates to a granule containing dextromethorphan hydrobromide and guaiacol glyceryl ether and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The granules are composed of dextromethorphan hydrobromide cyclodextrin inclusion compound, guaiacol glycerin ether, diluent and binder, wherein the dextromethorphan hydrobromide cyclodextrin inclusion compound The molar ratio of the dosage of dextromethorphan hydrobromide to the cyclodextrin is 1:1-1:3, and the cyclodextrin is hydroxypropyl-β-cyclodextrin. The granule containing dextromethorphan hydrobromide and guaiacol glyceryl ether of the present invention has good stability and good taste, and at the same time solves the problem that the blood concentration of dextromethorphan hydrobromide fluctuates greatly in patients after taking the medicine, and is effective Reduced drug side effects.

Description

technical field [0001] The invention relates to a granule containing dextromethorphan hydrobromide and guaiacol glyceryl ether and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Coughing is a reflex defense action, which can remove respiratory secretions and foreign objects in the airway. But coughing also has disadvantages. For example, coughing can spread infection in the respiratory tract, severe coughing can lead to respiratory tract bleeding, and even induce spontaneous pneumothorax. Therefore, if frequent cough affects work and rest, it is a pathological state. Coughing up sputum is a morbid phenomenon. Normal bronchial mucosa glands and goblet cells only secrete a small amount of mucus to keep the respiratory mucosa moist. When inflammation occurs in the respiratory tract, mucosal hyperemia, edema, increased mucus secretion, increased capillary wall permeability, and serous exudation. ...

Claims

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Application Information

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IPC IPC(8): A61K31/485A61K31/09A61K9/16A61P11/14A61P11/10
Inventor 郭昭
Owner NANJING CHENGONG PHARM CO LTD
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