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A kind of varenicline tartrate tablet and preparation method thereof

A technology for varenicline tartrate and tablets, which is applied in the directions of pill delivery, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the problems of reduced dissolution rate of tablets, unsuitable for long-term use, cumbersome process, etc. High dissolution, low friability and good fluidity

Active Publication Date: 2022-07-15
JIANGSU HANSOH PHARMA CO LTD +1
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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 varenicline tartrate tablet and preparation method thereof
  • A kind of varenicline tartrate tablet and preparation method thereof
  • A kind of varenicline tartrate tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[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 mixture obtained in step 1) with mannitol, 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) compressing the obtained mixed granules in step 3), and controlling the hardness of the tablet to be 3~10Kp;

[0056] 5) Transfer the plain tablet compressed in step 4) to a coating machine for coating operation.

Embodiment 2

[0058]

[0059] 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;

[0060] 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;

[0061] 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;

[0062] 4) compressing the obtained mixed granules in step 3), and controlling the hardness of the tablet to be 3~10Kp;

[0063] 5) Transfer the plain tablet compressed in step 4) to a coating machine for coating operation.

Embodiment 3

[0065]

[0066] 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;

[0067] 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;

[0068] 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;

[0069] 4) compressing the obtained mixed granules in step 3), and controlling the hardness of the tablet to be 3~10Kp;

[0070] 5) Transfer the plain tablet compressed in step 4) to a coating machine for coating operation.

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Abstract

The invention provides a varenicline tartrate tablet and a preparation method thereof. The weight percentage of sorbitol and microcrystalline cellulose in the composition is 5:1 to 10:1, and includes a disintegrating agent, a binder agents and lubricants. The preparation process of the product is simple, easy to operate, good in 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 varenicline tartrate tablet and a preparation method thereof. Background technique [0002] Varenicline can specifically bind to acetylcholine receptors to regulate cholinergic function. Accordingly, the compounds are useful in the treatment of 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 Disorder, Jet Lag, Amyotrophic Lateral Sclerosis (ALS), Cognitive Impairment, Hypertension, Hyperphagia, Anorexia, Obesity, Cardiac Arrhythmia, Hyperacidity , ulcers, pheochromocytoma, chemical dependence and addiction (eg, dependence on or addiction to nicotine (and / or tobacco products), alcohol, benzodiazepines, barbiturates, opioids, or cocaine), Headache, migraine, stroke, traum...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K47/38A61K47/26A61K31/55A61P25/34
CPCA61K9/2866A61K9/2054A61K9/2018A61K31/55A61P25/34
Inventor 张春林张晓瑜宗书敏
Owner JIANGSU HANSOH PHARMA CO LTD
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