Compound sustained-release preparation of guaiacol olycerin ether, pseudoephedrine and dextromethorphan

A technology of guaiacol glyceryl ether and pseudoephedrine, which is applied in the field of medicine, can solve the problems of short half-life of dextromethorphan, large fluctuation of blood drug concentration, easy to cause side effects, etc., and achieves less medication frequency, reduced medication frequency and safety. high effect

Inactive Publication Date: 2010-06-30
COSCI MED TECH 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, the general dose is 15-30 mg, which needs to be administered 3-4 times a day, and the blood concentration fluctuates greatly, which is likely to cause side effects

Method used

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  • Compound sustained-release preparation of guaiacol olycerin ether, pseudoephedrine and dextromethorphan
  • Compound sustained-release preparation of guaiacol olycerin ether, pseudoephedrine and dextromethorphan
  • Compound sustained-release preparation of guaiacol olycerin ether, pseudoephedrine and dextromethorphan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] prescription:

[0030] Guaifenesin 400g

[0031] Pseudoephedrine Hydrochloride 90g

[0032] Dextromethorphan Hydrobromide 30g

[0033] Carnauba Wax 45g

[0034] Microcrystalline Cellulose 50g

[0035] 5% povidone K30 aqueous solution appropriate amount

[0036] Magnesium Stearate Appropriate amount

[0037] Opadry 10g

[0038] Add pure water to 1000ml

[0039]

[0040] Made into 1000 grains (tablets)

[0041] Preparation:

[0042] (1) Preparation of granules Carnauba wax and microcrystalline cellulose were sieved separately and mixed evenly. Then add pseudoephedrine hydrochloride, guaiacol glyceryl ether, and dextromethorphan hydrobromide in sequence, mix well, use 5% povidone K30 aqueous solution as a binder to make a soft material, make wet granules with a 20-mesh sieve, and dry at 45°C , 20-mesh sieve and granulated, set aside.

[0043] (2) Preparation of coating solution Add Opadry to pure water, and add pur...

Embodiment 2

[0052] prescription:

[0053] Guaifenesin 800g

[0054] Pseudoephedrine Hydrochloride 60g

[0055] Dextromethorphan Hydrobromide 60g

[0056] Hypromellose K100M 80g

[0057] Hypromellose E5 55g

[0058] Lactose 65g

[0059] 5% povidone K30 aqueous solution appropriate amount

[0060] Appropriate amount of talcum powder

[0061] Opadry 10g

[0062] Pure water 1000ml

[0063]

[0064] Made into 1000 grains (tablets)

[0065] Preparation:

[0066] (1) Preparation of granules: Hypromellose K100M, hydroxypropylmethylcellulose E5, and lactose were sieved separately, mixed thoroughly, and then added with prescribed amounts of guaiacol glyceryl ether, pseudoephedrine hydrochloride 40g, and hydrobromide Dextromethorphan acid is mixed evenly, and a soft material is made with 5% povidone K30 aqueous solution as a binder, wet granules are prepared through a 20-mesh sieve, dried at 55°C, granulated through a 20-...

Embodiment 3

[0078] prescription:

[0079] Guaifenesin 400g

[0080] Pseudoephedrine Sulfate 90g

[0081] Dextromethorphan Hydrobromide 30g

[0082] Blank ball core 105g

[0083] Hypromellose E5 6g

[0084] Surelease Solids 30g

[0085] Water-soluble coating powder 5g

[0086] Titanium dioxide 1g

[0087] Stearic acid 5g

[0088] Proper amount of povidone K30

[0089] Appropriate amount of pure water

[0090] Anhydrous ethanol amount

[0091] Opadry 30g

[0092]

[0093] Made into 1000 grains (tablets)

[0094] Preparation:

[0095] (1) Pseudoephedrine Sulfate Sustained Release Pellets

[0096] 1, prepare 10% HPMC E5 aqueous solution, standby;

[0097] II. Take Surelease solids, add water, shake well and set aside;

[0098] III. Prepare a water-soluble coating solution containing 10% of water-soluble coating powder and 1% of titanium dioxide;

[0099] IV, prepare 40% pseudoephedrine sulfate aqueous soluti...

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PUM

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Abstract

The invention relates to a sustained-release preparation which takes guaiacol olycerin ether, pseudoephedrine or salt which is physiologically accepted by pseudoephedrine, and dextromethorphan or salt which is physiologically accepted by dextromethorphan as active ingredients. The sustained-release preparation of the invention not only can fully overcome relative symptoms such as cold and express the effect of synergy of compound medicines, but also the release and absorption of three active ingredients of the sustained-release preparation can reach synchronization, and the expected medicine release behavior can be gained inside and outside a human body. The medicine release behavior can reduce the times of taking medicine (from 4 times each day to 2 times each day, i.e. respectively taking medicine once in the morning and in the evening). The preparation is characterized in that times of taking medicine are reduced, the medicine can be slowly released in the human body, the blood concentration is stable, the fluctuation is small, the bioavailability is high, and the safety is high.

Description

technical field [0001] The invention relates to a sustained-release preparation with guaiacol glyceryl ether, pseudoephedrine or a physiologically acceptable salt thereof and dextromethorphan or a physiologically acceptable salt thereof as active components, and belongs to the field of medicine. Background technique [0002] A cold is an infection of the upper respiratory tract mucosa caused by many different types of viruses. The main symptoms are nasal congestion, sneezing, mild sore throat, and fever. Systemic symptoms include general discomfort, headache, and myalgia. Because there is no specific treatment at all, it is not necessary to make the virus firm, and only symptomatic treatment can be used to promote the relief of many symptoms of the cold. Since there is still no one drug to alleviate the coexisting symptoms, various compound preparations have been listed one after another. These compound preparations are composed of drugs with different curative effects to r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K31/09A61K31/137A61K9/30A61P11/00A61P31/12
Inventor 林鹏李育巧郑顺利
Owner COSCI MED TECH CO LTD
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