Oxcarbazepine sustained release tablet and preparation method thereof

A gentle, tablet-core technology, applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, pill delivery, etc., can solve problems such as increased potassium gas conductivity

Inactive Publication Date: 2017-05-31
浙江四维医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the antiepileptic effect of oxcarbazepine may also be attributed to the increase

Method used

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  • Oxcarbazepine sustained release tablet and preparation method thereof
  • Oxcarbazepine sustained release tablet and preparation method thereof
  • Oxcarbazepine sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] According to the amount of 100 tablets, weigh 60g of oxcarbazepine, add 1.3g of colloidal silicon dioxide, mix evenly, and then perform jet milling, then add 9g of microcrystalline cellulose, mix and then perform jet milling, and the particle size of the mixture is controlled at D90 of 25 μm ., D50 is 15 μm, D5 is 5 μm, then add microcrystalline cellulose 10g, hypromellose K4M12g, L100-55 4.5g, PVP3g, mix well, add an appropriate amount of purified water to 24 mesh wet granulation, and dry at 50-55°C When the water content reaches 3%, the granules are sized at 24 meshes, and then 1.2g of KG-802, 0.5g of magnesium stearate, and 1.5g of colloidal silicon dioxide are added, mixed evenly, and then compressed into tablets. The theoretical tablet weight is 1.03g, and the tablet hardness is It is controlled at 10-19kg, and then coated with a gastric-soluble coating powder containing an opacifying agent to form a mixed solution, and the theoretical weight gain is 2-4%.

Embodiment 2

[0053] According to the amount of 100 tablets, weigh 60g of oxcarbazepine, add 1.0g of colloidal silicon dioxide, mix evenly, and then perform jet milling, then add 10g of microcrystalline cellulose, mix and then perform jet milling, and the particle size of the mixture is controlled at D90 of 25 μm ., D50 is 15 μm, D5 is 5 μm, then add microcrystalline cellulose 10g, hypromellose K15M7g, L100-55 7.5g, PVP3g, mix well, add an appropriate amount of purified water to 24 mesh wet granulation, and dry at 50-55°C When the water content is 3%, the granules are granulated at 24 mesh, and then 1.2g of KG-802, 3g of magnesium stearate, and 1.5g of colloidal silicon dioxide are added, mixed evenly, and then pressed into tablets. The theoretical tablet weight is 1.042g, and the tablet hardness is controlled. At 10-19 kg, the stomach-soluble coating powder containing an opacifying agent is formulated into a mixed solution for coating, and the theoretical weight gain is 2-4%.

Embodiment 3

[0055] According to the amount of 100 tablets, weigh 60g of oxcarbazepine, add 0.8g of colloidal silicon dioxide, mix evenly, and then perform jet milling, then add 6g of microcrystalline cellulose, mix and then perform jet milling, and the particle size of the mixture is controlled at D90 of 25 μm ., D50 is 15 μm, D5 is 5 μm, then add microcrystalline cellulose 8g, hypromellose K15M7g, L100-55 7.5g, PVP 2g, mix well, add an appropriate amount of purified water to 24 mesh wet granulation, and dry at 50-55°C When the water content is 3%, the granules are granulated at 24 mesh, and then 1.3g of KG-802, 0.5g of magnesium stearate, and 1.5g of colloidal silicon dioxide are added, mixed evenly, and then compressed into tablets. The theoretical tablet weight is 0.946g, and the tablet hardness is It is controlled at 10-19kg, and then coated with a gastric-soluble coating powder containing an opacifying agent to form a mixed solution, and the theoretical weight gain is 2-4%.

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Abstract

The invention relates to an oxcarbazepine sustained release tablet and a preparation method thereof. According to the method adopted by the invention, raw materials are specially treated together with an auxiliary material first to prepare oxcarbazepine composition, and the particle size of the oxcarbazepine composition is strictly controlled. KG-802 is added into an extra auxiliary material. According to the oxcarbazepine sustained release tablet prepared with the method provided by the invention, the use of a large amount of a cosolvent namely sodium lauryl sulfate in an original developed preparation is avoided, the toxicity of a preparation finished product to a human body after taking is reduced, and the pollution to the environment in a preparation process is reduced; and compared with a reference product on sale, release curves in release media with different pH values can keep similar, the bioequivalence of an in-vitro test is ensured, and the release curves of the release media with different pH values are more similar to one another in comparison with the preparation on sale. The oxcarbazepine sustained release tablet provided by the invention is prepared by adopting a conventional granulation and tabletting process, the process is simple, and the oxcarbazepine sustained release tablet is suitable for large-scale production.

Description

technical field [0001] The invention relates to a sustained-release preparation containing oxcarbazepine and a preparation method thereof, more specifically to a sustained-release tablet containing oxcarbazepine and a preparation method thereof. Background technique [0002] Drug name: Oxcarbazepine [0003] Chemical name: 10,11-dihydro-10-oxo-5H-diphenyl[b,f]azepine-5-carboxamine [0004] Structural formula: [0005] [0006] Molecular formula: C 15 h 12 N 2 o 2 Molecular weight: 252.27 Solubility of oxcarbazepine: almost insoluble in water or ethanol, slightly soluble in methanol, acetone or dichloromethane; slightly soluble in chloroform, soluble in 0.1mol / L hydrochloric acid or 0.1mol / L hydrogen Almost insoluble in sodium oxide solution. [0007] The pharmacological activity of oxcarbazepine is mainly realized through its 10-monohydroxy metabolite (MHD). The precise mechanism by which oxcarbazepine and its metabolite MHD produce antiepileptic effects is curren...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/55A61K47/04A61K47/38A61P25/08
CPCA61K9/0002A61K9/2009A61K9/2054A61K31/55
Inventor 阮建山丁仲杰韩松陈祥伟俞秋燕马悦甜
Owner 浙江四维医药科技有限公司
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