A sustained-release enteric-coated preparation of duloxetine, core material and preparation method thereof

Abstract

The invention discloses a Duloxetine nteric-coated sustained release preparation as well as a core material and a preparation method thereof. The core material consists of Duloxetine as active medicinal ingredient or salts thereof and pharmaceutically acceptable auxiliary, wherein the pharmaceutically acceptable auxiliary contains a hot-melt material which at least contains a water-soluble hot-melt material and a hydrophobic hot-melt material, and the content of the hot-melt material is 20%-35%, the content of Duloxetine or salts thereof is 50%-75%, the rest is other pharmaceutically acceptable auxiliary the percentage of which is the mass percentage thereof based on the total amount of the core material. According to the invention, the core material of the Duloxetine nteric-coated sustained release preparation is prepared by adopting hot-melt technology, which avoids the introduction of water or organic solvents during preparation, lessens the degradation of principal and residual solvent, achieves a proper delay on the release of Duloxetine in intestines, namely 4-hour release amount in phosphate buffer with 6.8 of pH accounting for over 70% of the total amount, and is favorable for reducing adverse reaction of patients.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to a slow-release enteric preparation of duloxetine, a core material and a preparation method thereof. Background technique [0002] Duloxetine is a selective serotonin and norepinephrine reuptake inhibitors (SNRIs). It is a safe and effective antidepressant with the chemical name (S)-(+)-N-methyl 3-(1-naphthyloxy)-3-(2-thienyl)-propylamine is usually used in the form of hydrochloride. The elimination half-life of duloxetine hydrochloride is about 12 hours (variation range is 8-17 hours). Within the treatment range, its pharmacokinetic parameters are proportional to the dose, and the steady-state plasma concentration is generally reached after 3 days of taking the drug. [0003] Because duloxetine is unstable and prone to degradation in an acidic environment, it is appropriate to make duloxetine or its salt into an enteric-coated preparation to resist gastric juice fr...

AI Technical Summary

Problems solved by technology

[0009] Therefore, the technical problem to be solved in the present invention is that the core material of the existing duloxetine enteric-coated preparation is in contact with water or organic solvents during the preparation process, which causes the partial degradation of the active ingredient duloxetine and the shortage of solvent residues. And after the existing duloxetine hydrochloride enteric-coated solid preparation is taken, some patients will have the defect of adverse reactions in terms of gastrointestinal disorders, and provide a new duloxetine core material, enteric-coated preparation and its preparation The method, the duloxetine core material does not contact any water and organic solvents during the preparation process, the active ingredient duloxetine has little degradation and high stability, and the duloxetine enteric-coated preparation passes through the artificial gastric juice, and at pH6 .8 In phosphate buffer solution, the release amount in 1 hour is less than 50% of the labeled amount, and the release amount in 4 hours is greater than 70% of the labeled amount

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