Acemetacin sustained-release preparation and preparation method

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...

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