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Orally disintegrating tablet containing varenicline solid dispersion, and preparation method of orally disintegrating tablet

A solid dispersion and orally disintegrating tablet technology, which is applied to medical preparations containing active ingredients, medical preparations without active ingredients, and pharmaceutical formulas, can solve the problem that the success rate is less than 3%, and it is difficult to achieve the taste masking effect And other issues

Pending Publication Date: 2021-09-24
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A survey shows that more than 70% of smokers have thought of quitting smoking, but the proportion of real success is less than 3%
The bitterness of varenicline is extremely strong, and it is difficult to achieve the ideal taste-masking effect by conventional flavoring methods

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Varenicline orally disintegrating tablets are prepared from the following components, in quantities of 1000 tablets

[0021] Varenicline 4.0g Eudragit E100 4.0g lactose 40.0g microcrystalline cellulose 20.0g Croscarmellose sodium (additional) 4.5 Croscarmellose sodium (extra) 4.5 Magnesium stearate 2.4 Acesulfame K 0.6

[0022] Its preparation method comprises the following steps:

[0023] (1) Take varenicline, dissolve it in 10 times the weight of ethanol solution, add the prescribed amount of Eudragit E100, stir to dissolve it into a clear and transparent solution, spray dry to remove the solvent, and obtain a solid dispersion.

[0024] (2) Mix the varenicline solid dispersion with the prescribed amount of lactose, microcrystalline cellulose, and internal croscarmellose sodium, then dry granulate, add external croscarmellose sodium, hard Magnesium fatty acid and acesulfame potassium are uniformly mixed and compr...

Embodiment 2

[0026] Varenicline orally disintegrating tablets are prepared from the following components, in quantities of 1000 tablets

[0027] Varenicline 4.0g Eudragit E100 12.0g Mannitol 30.32g microcrystalline cellulose 30.0g Low-substituted hydroxypropyl cellulose (internal addition) 1.6 Low-substituted hydroxypropyl cellulose (additional) 1.6 Magnesium stearate 0.4 aspartame 0.08

[0028] Its preparation method comprises the following steps:

[0029] (1) Take varenicline, dissolve it in 50 times the weight of ethanol solution, add the prescribed amount of Eudragit E100, stir to dissolve it into a clear and transparent solution, spray dry to remove the solvent, and obtain a solid dispersion.

[0030] (2) Mix varenicline solid dispersion with prescribed amount of mannitol, microcrystalline cellulose, internally added low-substituted hydroxypropyl cellulose, dry granulate, add externally added low-substituted hydroxypropyl cellulo...

Embodiment 3

[0032] Varenicline orally disintegrating tablets are prepared from the following components, in quantities of 1000 tablets

[0033] Varenicline 4.0g Eudragit E100 12.0g Mannitol 23.2.0g pregelatinized starch 23.2g Crospovidone (internal addition) 8.0 Low-substituted hydroxypropyl cellulose (additional) 8.0 Sodium stearyl fumarate 0.8 Sucralose 0.8

[0034] Its preparation method comprises the following steps:

[0035] (1) Take varenicline, dissolve it in 25 times the weight of ethanol solution, add the prescribed amount of Eudragit E100, stir to dissolve it into a clear and transparent solution, spray dry to remove the solvent, and obtain a solid dispersion.

[0036] (2) Uniformly mix varenicline solid dispersion with prescribed amount of mannitol, pregelatinized starch, and internally added crospovidone, then dry granulate, add externally added low-substituted hydroxypropyl cellulose, stearyl fumarate Sodium bicarbonate...

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PUM

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Abstract

The invention belongs to the field of medicine preparations, and particularly relates to a varenicline orally disintegrating tablet and a preparation method thereof. By aiming at the problems that varenicline has a bitter taste and has poor oral administration compliance, varenicline, a carrier and a solvent are prepared into a solid dispersion so as to cover the poor taste of a medicine; and the solid dispersion is adopted for preparing the orally disintegrating tablet, and the orally disintegrating tablet can be quickly disintegrated within 30 seconds, has a good taste, and remarkably improves the oral administration compliance.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an orally disintegrating tablet containing varenicline solid dispersion, and also relates to a preparation method of the orally disintegrating tablet and a method for improving dissolution rate. . Background technique [0002] Smoking will cause great damage to various organs of the human body: smoking will increase the viscosity of platelets, make blood more likely to coagulate, and cause harm to the heart and blood vessels; the impact of smoking on the lungs is beyond doubt, and the damage to the lungs is often Irreversible: Smoking can cause lung cancer and emphysema, and the probability of getting sick is 10 times that of a person who smokes 10 cigarettes a day compared to a non-smoker. Therefore, there are many benefits of quitting smoking: reducing the risk of disease, improving blood circulation, delaying aging, prolonging life and so on. A survey sho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4995A61K47/32A61P25/34
CPCA61K9/2027A61K9/0056A61K31/4995A61P25/34
Inventor 吴霞王宇杰
Owner BEIJING VENTUREPHARM BIOTECH
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