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Method for preparing aceclofenac enteric microcapsules

An aceclofenac, enteric-coated technology, applied in the field of preparation of pharmaceutical preparations, can solve the problems of difficulty in optimal process investigation, difficulty in achieving the effect of capsule shells, poor reproducibility and the like

Inactive Publication Date: 2012-09-26
SHAANXI UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the tablet is affected by many factors such as pressure and powder fluidity, which brings many difficulties to the investigation of the best process in the later stage.
Coated tablets have poor slow / controlled release stability because it is difficult to accurately control the coating thickness
Capsules are loaded directly. Due to the influence of materials, it is often difficult to achieve a uniform effect with capsule shells from different manufacturers, and the reproducibility is poor.

Method used

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  • Method for preparing aceclofenac enteric microcapsules
  • Method for preparing aceclofenac enteric microcapsules
  • Method for preparing aceclofenac enteric microcapsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1) Take 3.8g of acrylic resin II and dissolve it in acetone to obtain solution A;

[0027] 2) Then add 2.6g of aceclofenac powder to solution A to fully dissolve to obtain solution B, put solution B in a flask and stir at 200r / min at 8-10°C to obtain colostrum;

[0028] 3) Take 5ml of Span 80 and add it to 100ml of liquid paraffin and stir fully at the bottom of the temperature at 15°C;

[0029] 4) Add the colostrum prepared in step 2) into the stirred liquid paraffin in step 3), gradually heat up to 40°C while stirring at 200r / min, keep stirring for 3 hours, then gradually heat up to 75°C, keep stirring for 1h, Prepare microcapsules;

[0030] 5) After filtration, wash with n-hexane for 3 times and dry to obtain the finished microcapsules.

Embodiment 2

[0032] 1) Take 4.5g of hydroxypropyl methylcellulose phthalate and disperse it in acetone to obtain solution A;

[0033] 2) Then add 2.8g of aceclofenac powder to solution A to fully dissolve to obtain solution B, put solution B in a flask and stir at 200r / min at 8-10°C to obtain colostrum;

[0034] 3) Take 8ml of Span 80 and add it to 70ml of liquid paraffin and stir fully at the bottom of the temperature at 15°C;

[0035] 4) Add the colostrum prepared in step 2) into the stirred liquid paraffin in step 3), gradually heat up to 40°C while stirring at 200r / min, keep stirring for 3 hours, then gradually heat up to 75°C, keep stirring for 1h, Prepare microcapsules;

[0036] 5) After filtration, wash with n-hexane for 3 times and dry to obtain the finished microcapsules.

Embodiment 3

[0038] 1) Take 5.1g of cellulose acetate phthalate and disperse it in acetone to obtain solution A;

[0039] 2) Then add 2.5g of aceclofenac powder to solution A to fully dissolve to obtain solution B, put solution B in a flask and stir at 200r / min at 8-10°C to obtain colostrum;

[0040] 3) Take 10ml of Span 80 and add it to 200ml of liquid paraffin and stir fully at the bottom of the temperature at 15°C;

[0041] 4) Add the colostrum prepared in step 2) into the stirred liquid paraffin in step 3), gradually heat up to 40°C while stirring at 200r / min, keep stirring for 3 hours, then gradually heat up to 75°C, keep stirring for 1h, Prepare microcapsules;

[0042] 5) After filtration, wash with n-hexane for 3 times and dry to obtain the finished microcapsules.

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Abstract

Disclosed is a method for preparing aceclofenac enteric microcapsules, comprising dissolving eudragit II, hydroxypropylmethylcellulose phthalate (HPMCP) or cellulose acetate phthalate in acetone to acquire a solution A; then adding aceclofenac powder into the solution A and fully dissolving the aceclofenac powder to obtain a solution B, and acquiring a primary emulsion by placing the solution B in a flask and stirring; adding span 80 into liquid paraffin and fully stirring; adding the primary emulsion into the well-stirred liquid paraffin, heating up to 75 DEG C gradually while stirring, and acquiring microcapsules by stirring continuously while preserving the temperature; and washing the microcapsules by using n-hexane three times after filtering and drying to acquire the finished microcapsules. According to the invention, the aceclofenac slow-release enteric microcapsules are prepared by using a property that decomposition of a capsule wall material is influenced by pH values. Through controlling the capsule wall material, the following effects can be achieved: drugs are sent directionally to the small intestine and released slowly to gentle the plasma concentration, prolong the action time, and improve the curative effect; the dosing frequency can be reduced and the plasma concentration is maintained in the body; and an adverse reaction in the gastrointestinal tract is reduced effectively and patient compliance is also improved effectively.

Description

Technical field: [0001] The invention relates to a preparation method of a pharmaceutical preparation, in particular to a preparation method of aceclofenac enteric-coated microcapsules. Background technique [0002] Aceclofenac is mainly used to treat various rheumatoid arthritis, rheumatoid arthritis, osteoarthritis and spondylitis, and can also be used for pain and fever caused by various diseases. The drug is safer and more effective than diclofenac, ketoprofen, indomethacin, etc. But its half-life is short, in order to maintain the effective concentration of treatment, it needs to be taken several times a day, which is inconvenient to use, and the blood drug concentration fluctuates greatly, and the curative effect is unstable. Rarely, it can cause peptic ulceration and bleeding. Especially for patients with allergies and elderly patients, it is more likely to cause some adverse reactions (Wang Guanglong, Liu Aiyan, Tang Li. Two cases of adverse reactions caused by ace...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/50A61K31/216A61K47/38A61K47/32A61P29/00A61P19/02
Inventor 王兰王谦赵彦钊周军
Owner SHAANXI UNIV OF SCI & TECH
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