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Acemetacin sustained-release preparation and preparation method

A technology of acemetacin and sustained-release preparations, applied in the field of sustained-release pharmaceutical preparations and its preparation, can solve the problems of patient inconvenience, ulcers (sometimes accompanied by bleeding and perforation, short half-life, etc.), to reduce adverse reactions, long-term Drug stable release, the effect of controlled drug stable release

Active Publication Date: 2009-12-02
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the short plasma half-life of acemetacin, the active compound is excreted or metabolized after a few hours, and the blood drug concentration also drops to a level that is not enough to play a therapeutic role. Therefore, it is necessary to increase the dosage of the drug, that is, increase the daily dose The number of times, but then increased in patients with nausea, vomiting, abdominal pain, diarrhea, loss of appetite, feces occult blood (individual cases may lead to anemia), peptic ulcer (sometimes accompanied by bleeding and perforation), headache, dizziness, lethargy / fatigue, The probability of adverse symptoms such as tinnitus, which brings inconvenience to the patient

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0029] Embodiment 1-6 prepares 1000 grains / tablet acemetacin sustained-release dosage form

[0030] Drug core composition:

Embodiment 1

[0031] Example 1 2 3 4 5 6

[0032] Acemetacin 70g 80g 90g 100g 110g 120g

[0033] Microcrystalline Cellulose 105g 120g 135g 150g 165 180g

[0034] Hydroxypropyl methylcellulose 7g 8g 9g 10g 11g 12g

[0035] Controlled release layer composition:

[0036] Composition 1 30% xanthan gum, 70% chitosan;

[0037] Composition 2 40% xanthan gum, 60% chitosan;

[0038] Composition 3 50% xanthan gum, 50% chitosan;

[0039] Composition 4 60% xanthan gum, 40% chitosan;

[0040] Composition 5 70% xanthan gum, 30% chitosan;

[0041] Composition 6 80% xanthan gum, 20% chitosan.

[0042] The above-mentioned controlled-release layer is formulated into a solution with 95% ethanol during spray coating.

[0043] Preparation:

[0044]Any drug core composition in the embodiment of the present invention can choose the above-mentioned multi-layer controlled-release layer with different proportions, as long as the adjacent two layers contain xanthan gum-chitosan in different amounts from each...

Embodiment 7

[0075] Example 7: Preparation of acemetacin sustained-release dosage form containing a dual-release system of acemetacin sustained-release preparation of the present invention and acemetacin immediate-release preparation

[0076] Acemetacin immediate-release drug formulation prescription

[0077] Acemetacin 30g Sucrose powder 40g Micropowder silica gel 0.75g 50% ethanol amount

[0078] Preparation method of acemetacin immediate release drug preparation

[0079] Weigh acemetacin, sucrose powder, and micropowdered silica gel, mix evenly, add 50% ethanol to make granules, dry at 60±5°C, and take granules between 20-40 mesh for later use;

[0080] Preparation of Acemetacin Dual Delivery System Preparation

[0081] Weigh the acemetacin quick-release preparation and the sustained-release preparation of the present invention, add magnesium stearate, mix uniformly, pack into capsules or compress tablets.

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PUM

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Abstract

The invention discloses an acemetacin slow-release preparation and a preparation method thereof, which belong to the technical field of medicine and are used to solve the problems of acemetacin's short plasma half-life and short duration of therapeutic action. It consists of an acemetacin drug core and a controlled-release layer wrapping the drug core. The controlled-release layer is composed of a xanthan gum-chitosan mixture, wherein the content of xanthan gum accounts for the total weight of xanthan gum-chitosan The percentage is 20% to 80%. In the present invention, the acemetacin drug core is coated with multiple layers of controlled-release layers, and the release speed of the drug is slowed down by increasing the number of layers of the controlled-release layer or the wrapping rate. Tests have shown that compared with conventional dosage forms, the preparation can well control the release of the drug, and can maintain the blood drug concentration of the therapeutic amount within 24 hours in a once-a-day administration mode. It overcomes the deficiencies of the prior art and provides an oral dosage form that can control the stable release of drugs for a long time, prolong the curative effect of drugs, reduce adverse reactions, and basically avoid incomplete drug release.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical preparation and a preparation method thereof, in particular to an acemetacin sustained-release preparation, which belongs to the technical field of medicine. Background technique [0002] Acemetacin (Acemetacin), the chemical name is 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-ethanecarboxylic acid methyl ester, is a non-steroidal It is an anti-inflammatory drug, which can produce anti-inflammatory, analgesic and antipyretic effects by inhibiting the synthesis of prostaglandins. Acemetacin is mainly used for the treatment of: 1. Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis; 2. Frozen shoulder, bursitis, tendon and tenosynovitis; 3. Low back pain, sprains, strains and Other soft tissue injuries; 4. Acute gout; 5. Dysmenorrhea, toothache and postoperative pain. After oral administration of acemetacin, indomethacin and a small amount of acemetacin mainly exist in the bloo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/14A61K31/405A61P29/00
Inventor 郭卫芹张育李国聪
Owner CSPC OUYI PHARM CO LTD
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