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Duloxetine pharmaceutical composition

A technology of duloxetine and its composition, which is applied in the field of pharmaceutical preparations, can solve problems such as slow dissolution and lower bioavailability of active compounds, and achieve the effects of reducing reactions, improving stability, and shortening the process

Pending Publication Date: 2021-01-05
宁波高新区美诺华医药创新研究院有限公司
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0004] However, duloxetine reacts with many known enteric coatings to form a slowly dissolving or even insoluble coating, which reduces the bioavailability of the active compound

Method used

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  • Duloxetine pharmaceutical composition
  • Duloxetine pharmaceutical composition
  • Duloxetine pharmaceutical composition

Examples

Experimental program
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Effect test

preparation example Construction

[0042] The preparation technology of embodiment 1-8 is as follows:

[0043] Step 1: Drug layer – pellet core part

[0044] Duloxetine and Opadry YS-1-7006 (binder), crospovidone and talc were dissolved in purified water. This solution was coated onto sugar sphere cores in a Wurster fluidized bed.

[0045] Step 2: Isolation Layer

[0046] The above drug-loaded pellets were then first coated with a dispersion of sucrose, hypromellose 2910 and purified talc (glidant) in the purification in a Wurster fluidized bed to form coated pellets.

[0047] Step 3: Enteric Coated Layer

[0048] The talc was then purified using hydroxypropylmethylcellulose phthalate (HPMCP) 50 and hydroxypropylmethylcellulose phthalate (HPMCP) 55 in a Wurster fluidized bed (flow aid agent) and diethyl phthalate (plasticizer) in purified water and acetone to coat the above barrier layer pellets to form enteric layered duloxetine pellets.

[0049] Step 4: Outermost Layer

[0050] The enteric-coated layer ...

example 4

[0058]Example 4 was completely dissolved in the buffer within 1 hour, showing that the in vitro release was similar to that of a well-known brand product (Cymbalta, lot number C926601A).

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Abstract

The invention discloses a duloxetine pharmaceutical composition. The duloxetine pharmaceutical composition comprises (1) a pellet loaded with a certain amount of duloxetine; and (2) an enteric layer consisting of two types of hydroxypropylmethyl cellulose phthalate different in pH solubility, wherein the enteric layer coats the pellet. According to the pharmaceutical composition, the polymer hydroxypropylmethyl cellulose phthalate (HPMCP) with different levels of pH solubility is used, and adding ammonia for neutralization is not needed, so that the process is shortened, the reaction between the enteric layer and active substances of the duloxetine on the pellet is greatly reduced, and stability is increased; in addition, different HPMCP forms the enteric layer, so that the duloxetine is prevented from being damaged by the acidic condition of a stomach, and the duloxetine is released in a gastrointestinal tract (GIT) with relatively high pH, for example, in a small intestine, and thus,accurate release of the drug at a target part is facilitated, and the risk of dose dumping of the drug within an initial time interval is greatly lowered.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a duloxetine pharmaceutical composition. Background technique [0002] Duloxetine (+)-(S)-N-methyl-y-(1-naphthyl)-2-thienylamine hydrochloride is an SSNRI (hereinafter referred to as selective serotonin and norepinephrine reuptake inhibitor agent) class of well-known drugs for the treatment of major depressive disorder (MDD) and diabetic peripheral neuropathic pain. It is usually used in the form of its hydrochloride salt, and the term "duloxetine" is used hereinafter to refer generally to the free base, but also to the salts and other compounds of duloxetine, usually to the hydrochloride salt. [0003] It is recognized that duloxetine is unstable in acidic media. Therefore, there is a need to protect duloxetine from the acidic conditions of the stomach and to release it at the higher pH of the gastrointestinal tract (GIT), such as in the small intestine. C...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61K31/381A61K47/38A61K47/26A61P3/10A61P25/02A61P25/24
CPCA61K9/5042A61K9/5015A61K9/5073A61K9/2081A61K31/381A61P25/24A61P25/02A61P3/10
Inventor 苏尼尔·库马尔·潘达叶连挺晏培福汪宜俊姚振江王春艳戴勋仁曹倩王飞云
Owner 宁波高新区美诺华医药创新研究院有限公司
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