Duloxetine delayed release pharmaceutical composition and preparation method thereof

Abstract

The invention discloses a duloxetine delayed release pharmaceutical composition and a preparation method thereof, the pharmaceutical composition comprises a pill core containing duloxetine or a salt thereof and an enteric-coated layer coating the pill core, the enteric-coated layer comprises cellulose acetate trimellitate and a plasticizer, the plasticizer is glycerin or a glycerin mixture, and based on accidental discovery, the enteric-coated layer can be used for preparing the duloxetine delayed release pharmaceutical composition. The drug prepared by coating the inert pellet core of duloxetine or the salt thereof with an intestinal solution prepared from cellulose acetate trimellitate and a glycerol plasticizer is basically the same as an original grinding agent in dissolution performance, is excellent in performance and stable in dissolution, does not need to be neutralized by ammonia water in the preparation process of the intestinal solution, simplifies the drug forming process again, improves the stability, and is suitable for industrial production. And the yield is improved, the cost is relatively reduced, and the competitiveness of the product is improved.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a duloxetine delayed-release pharmaceutical composition and a preparation method. Background technique [0002] Duloxetine is chemically (+)-(S)-N-methyl-γ-(1-naphthyloxy)-2-thienylamine, commonly used as its hydrochloride salt, and is a selective serum Sine and norepinephrine reuptake inhibitors (SSNRIs), which are effective in major depressive disorder, are equally effective in generalized anxiety disorder. [0003] Duloxetine is commercially available in the United States under the tradename CYMBALTA™ as capsules containing delayed-release pellets. It has been approved by the FDA to treat major depressive disorder, generalized anxiety disorder, treat neuropathic pain associated with diabetic peripheral neuropathy, and treat fibromyalgia. Duloxetine is also available in Europe under the trade name CYMBALTA TM and YENTREVE TM is commercially available in the form of Stomac...

AI Technical Summary

Problems solved by technology

[0007] The application of cellulose acetate trimesate (CAT) in duloxetine enteric-coated layer has not been found in the retrieved prior art. In addition, CAT, HPMCAS, etc. need ammonia neutralization in the prior art, but ammonia The degree of neutralization needs to be accurately controlled, which can easily have a great impact on dissolution, resulting in a decrease in yield and difficulty in molding

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