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Duloxetine hydrochloride enteric mini-pill preparation

A technology of loxetine intestinal and hydrochloric acid degree, which is applied in the directions of medical preparations containing active ingredients, microcapsules, organic active ingredients, etc., can solve the problems that HPMCAS is not easy to buy, unfavorable in process, and high in production cost, and achieves improved acid resistance. properties, promoting solubility, and being easily degradable

Inactive Publication Date: 2016-05-04
北京修正创新药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The duloxetine hydrochloride enteric-coated preparation disclosed in the patent US5508276 has problems such as high production cost and unfavorable process for industrial production, and HPMCAS is not easy to purchase

Method used

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  • Duloxetine hydrochloride enteric mini-pill preparation
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  • Duloxetine hydrochloride enteric mini-pill preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Table-1 Example 1 prescription (1000 capsules)

[0042]

[0043]

[0044] Preparation Process

[0045] 1. Preparation of drug-loaded pellet cores: suspend duloxetine hydrochloride in 5% HPMC aqueous solution, and prepare drug-loaded pellets by spraying the suspension on blank sugar pill cores. Set the inlet air temperature of the bottom spray fluidized bed at 40-45°C, the atomization pressure at 1.0-1.5bar, and the air volume at 40-50m 3 / h, control the temperature of the material at 37-40°C.

[0046] 2. Preparation of isolation coat layer: After dissolving sorbitol and HPMC, add Talc to fully disperse until uniform. The suspension is sprayed onto the drug-loaded pellet core prepared in step 1 through a bottom-spray fluidized bed to obtain isolated drug-loaded pellets. Set the inlet air temperature of the bottom spray fluidized bed at 40-45°C, the atomization pressure at 1.0-1.5bar, and the air volume at 40-50m 3 / h, control the temperature of the material at ...

Embodiment 2

[0052] Table-2 embodiment 2 prescription (1000 grains)

[0053]

[0054]

[0055] Preparation process: with embodiment 1.

[0056] Dissolution profile see figure 2 , it can be seen that the dissolution behavior of the enteric-coated pellet preparation of Example 2 is similar to that of the positive control drug (Cymbalta), and better dissolution can be achieved.

Embodiment 3

[0058] Table-3 embodiment 3 prescription (1000 grains)

[0059]

[0060] Preparation process: with embodiment 1.

[0061] Dissolution profile see image 3 ,Depend on image 3 It can be seen that the dissolution behavior of the enteric-coated pellet preparation of Example 3 is similar to that of the positive control drug (Cymbalta), and better dissolution can be achieved.

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Abstract

The invention relates to a duloxetine hydrochloride enteric mini-pill preparation. Mini-pills include medicine-carrying pill cores, isolation coating layers, enteric coating layers and dispensable modification layers. When a relatively common methyl acrylic copolymer is adopted as an enteric material in a prescription, the purpose that an in-vitro dissolution curve of active ingredients is consistent to positive control medicine Cymbalta is achieved by adding sorbitol into the isolation layers. The duloxetine hydrochloride enteric mini-pill preparation adopts medicinal acrylic resin which is marked with medicinal registration batch number and easy to obtain as an enteric material. An adopted conventional preparation method and a process are simple, the duloxetine hydrochloride enteric mini-pill preparation is suitable for industrial production, and a medicine reasonable in price and reliable in treating effect is provided for patients suffering from depression.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an enteric-coated pellet preparation of duloxetine hydrochloride. Background technique [0002] Duloxetine Hydrochloride (DuloxetineHydrochloride, API) is an effective 5-hydroxytryptamine and norepinephrine dual absorption inhibitor for the treatment of depression, and its chemical name is: s-(+)-N-methyl-3- (1-naphthyloxy)-3-(2-thienyl)-propylamine hydrochloride, its structural formula is: [0003] [0004] Duloxetine hydrochloride is white or off-white crystalline powder or powder, slightly soluble in water, unstable under acidic conditions, and easy to degrade, so it is suitable to be made into enteric-coated preparations to resist the damage of gastric juice to the drug. [0005] Eli Lilly's patent US5508276 discloses a kind of enteric-coated pellets of duloxetine, which includes a) a drug core composed of duloxetine and pharmaceutically acceptable excipients; b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/381A61P25/24
CPCA61K9/5078A61K9/5015A61K9/5026A61K9/5042A61K9/5089A61K31/381
Inventor 刘海波苏宇魏墨玺
Owner 北京修正创新药物研究院有限公司
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