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A kind of pharmaceutical composition of varenicline tartrate and preparation method thereof

A technology of varenicline tartrate and its mixture, which is applied in the direction of drug combinations, pharmaceutical formulas, and active ingredients of heterocyclic compounds. It can solve the problems of reduced dissolution rate of tablets, unsuitability for long-term use, and cumbersome process, and achieve high dissolution rate. , small brittleness, good fluidity

Active Publication Date: 2022-06-24
SHANGHAI HANSOH BIOMEDICAL +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] CN107753449A discloses a varenicline tablet composition, but the application needs to control the particle size of varenicline tartrate to a certain size, the process is complicated and the cost is high, and sodium lauryl sulfate needs to be added simultaneously, but dodecyl Sodium sulphate is toxic to the human body and has many side effects, so it is not suitable for long-term use
[0013] Therefore, in order to solve the varenicline tartrate tablet in the process of depositing, the dissolution rate of the tablet tends to decrease with the prolongation of time, and the problem of impurities is easy to be produced, it is necessary to develop a kind with high dissolution rate and good stability, Varenicline tartrate preparation with small impurity content, simple process and convenient operation

Method used

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  • A kind of pharmaceutical composition of varenicline tartrate and preparation method thereof
  • A kind of pharmaceutical composition of varenicline tartrate and preparation method thereof
  • A kind of pharmaceutical composition of varenicline tartrate and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0045]

[0046] 1) when one third of the weight of magnesium stearate, microcrystalline cellulose and varenicline tartrate are mixed after 20 minutes at a rotating speed of 15rpm, sieve and granulate, wherein the screen aperture is 0.8-2.0mm during granulation, to prepare a mixture;

[0047] 2) mixing the mixture obtained in step 1) with mannitol, polyvinylpyrrolidone, and low-substituted hydroxypropyl cellulose for 10-30 minutes at a rotating speed of 15 rpm;

[0048] 3) adding residual magnesium stearate to the mixture obtained in step 2), and mixing for 10-20 minutes at a rotating speed of 15 rpm;

[0049] 4) Tablet the blended granules obtained in step 3).

Embodiment 2

[0051]

[0052] 1) when one third of the weight of magnesium stearate, microcrystalline cellulose and varenicline tartrate are mixed after 20 minutes at a rotating speed of 15rpm, sieve and granulate, wherein the screen aperture is 0.8-2.0mm during granulation, to prepare a mixture;

[0053]2) mixing the obtained mixture of step 1) with calcium hydrogen phosphate, polyvinylpyrrolidone, and low-substituted hydroxypropyl cellulose for 10-30 minutes at a rotating speed of 15 rpm;

[0054] 3) adding residual magnesium stearate to the mixture obtained in step 2), and mixing for 10-20 minutes at a rotating speed of 15 rpm;

[0055] 4) Tablet the blended granules obtained in step 3).

Embodiment 3

[0057]

[0058] 1) when one third of the weight of magnesium stearate, microcrystalline cellulose and varenicline tartrate are mixed after 20 minutes at a rotating speed of 15rpm, sieve and granulate, wherein the screen aperture is 0.8-2.0mm during granulation, to prepare a mixture;

[0059] 2) mixing the mixture obtained in step 1) with sorbitol, polyvinylpyrrolidone, and low-substituted hydroxypropyl cellulose for 10-30 minutes at a rotating speed of 15 rpm;

[0060] 3) adding residual magnesium stearate to the mixture obtained in step 2), and mixing for 10-20 minutes at a rotating speed of 15 rpm;

[0061] 4) Tablet the blended granules obtained in step 3).

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Abstract

The invention provides a varenicline tartrate composition and a preparation method thereof. In the composition, the weight percentage of sorbitol and microcrystalline cellulose is 5:1 to 10:1, and includes a disintegrant, a binder agents and lubricants. This product adopts the powder direct pressing process, the preparation process is simple, easy to operate, good reproducibility, and suitable for large-scale industrial production. Moreover, the varenicline tartrate composition prepared by the present invention not only does not need to control the particle size, but also has small friability, good fluidity, high dissolution rate, good stability and low probability of adverse reactions.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition of varenicline tartrate and a preparation method thereof. Background technique [0002] Varenicline can specifically bind to acetylcholine receptors and is used to modulate cholinergic function. Accordingly, the compounds can be used to treat various diseases or conditions including, but not limited to, inflammatory bowel disease, irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, vasoconstriction, anxiety, panic disorder, depression , bipolar disorder, autism, sleep disorders, jet lag syndrome, amyotrophic lateral sclerosis (ALS), cognitive impairment, hypertension, bulimia, anorexia, obesity, cardiac arrhythmias, hypersecretion of gastric acid , ulcers, pheochromocytoma, chemical dependence and addiction (eg, dependence or addiction to nicotine (and / or tobacco products), alcohol, benzodiazepines, barbiturates, opioids, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/26A61K47/32A61K31/55A61P25/34
CPCA61K9/2054A61K9/2018A61K9/2027A61K31/55A61P25/34
Inventor 张春林李巍袁恒立宗书敏赵娜
Owner SHANGHAI HANSOH BIOMEDICAL
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