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Duloxetine hydrochloride enteric micropill preparation

A technology for duloxetine hydrochloride and loxetine enteric, which is applied in the field of pharmaceutical preparations, can solve the problems of low dissolution rate, unfavorable process and high production cost of duloxetine hydrochloride enteric-coated preparations, and achieves reliable curative effect, simple process, low cost effect

Active Publication Date: 2014-01-15
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The duloxetine hydrochloride enteric-coated preparations disclosed in patent US5508276 and CN101756960A have problems such as high production cost and unfavorable technology for industrial production. The enteric-coated preparation of loxetine adopts methacrylic acid copolymer as the enteric-coated material. Compared with HPMCAS, the enteric-coated material is easy to buy, the cost is also low, and the process is simple and suitable for industrial production. However, there is duloxetine hydrochloride prepared Disadvantages of low dissolution rate of enteric-coated preparations

Method used

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  • Duloxetine hydrochloride enteric micropill preparation
  • Duloxetine hydrochloride enteric micropill preparation
  • Duloxetine hydrochloride enteric micropill preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Prescription: (20,000 capsules)

[0036] .

[0037] Preparation Process:

[0038] 1. Drug-loaded pellet core: suspend duloxetine hydrochloride in 5% HPMC aqueous solution, and prepare drug-loaded pellets by spraying the suspension on the blank sugar pill core. Set the inlet air temperature of the bottom spray fluidized bed at 40-45°C, the atomization pressure at 1.0-1.5 bar, the air volume at 40-50 m3 / h, and control the material temperature at 37-40°C.

[0039] 2. Isolation coat layer: After dissolving mannitol 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, the air volume at 40~50 m3 / h, and control the material temperature at 37~40°C.

[0040] 3. Enteric coating layer: Dissolve the plas...

Embodiment 2

[0045] Prescription: (20,000 capsules)

[0046] .

[0047] Preparation process: with embodiment 1.

[0048] Dissolution profile see figure 2 , it can be seen that the dissolution behavior of the enteric-coated pellet preparation in Example 2 is similar to that of the positive control drug (Cymbalta), and better dissolution can be achieved.

Embodiment 3

[0050] Prescription: (20,000 capsules)

[0051] .

[0052] Preparation process: with embodiment 1.

[0053] Dissolution profile see image 3 ,Depend on image 3 It can be seen that the dissolution behavior of the enteric-coated pellet preparation in 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 micropill preparation which is composed of a drug-carrying pill core, an isolating coating layer and an enteric coating layer. When the enteric materials in the prescription adopt common methacrylic acid copolymers, sugar alcohol can be added into the isolating layer to achieve the goal that the active component in-vitro dissolution curve is consistent with a positive control drug (Cymbalta of Eli Lilly and Company). The product has the advantages of high acid resistance, high dissolution speed, high rate and the like; the methacrylic acid copolymers used as the enteric material are easy to purchase and low in cost; and the adopted conventional preparation method is simple in technique and suitable for industrial production, thereby providing a drug with reasonable price and reliable curative effect for patients with melancholia.

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 (API) is an effective dual absorption inhibitor of serotonin and norepinephrine for the treatment of depression. 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) an optional isolation layer; ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/381A61P13/10A61P25/24A61P29/00
Inventor 赫玉霞刘英帝吴欢欢杨敏邹亮
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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