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Voriconazole tablet and preparation method thereof

A technology for voriconazole tablets and tablet cores, which is used in pill delivery, antifungal agents, pharmaceutical formulations, etc., can solve problems such as inability to deduce the dosage of excipients and process parameters, slow dissolution rate, adverse reactions, etc.

Active Publication Date: 2021-09-03
ZHEJIANG ANGLIKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Although the types of excipients and a small amount of process information of the original research can be found through various channels, it is still impossible to deduce the specific amount of excipients and process parameters from the existing information
Voriconazole tablets contain multiple components and there are complex interrelationships. Changes in one component, content, or even addition method may affect other components, thereby affecting the disintegration and dissolution of the tablet. Waiting for behavior
[0009] The speed of drug absorption in the body is usually determined by the speed of dissolution. Before being absorbed, the drug in the tablet must go through the process of disintegration and / or dissolution and then turn into a solution. If the drug is not easily released from the preparation or the drug is dissolved If the speed is extremely slow, there may be problems with the absorption speed or degree of the drug in the preparation. On the other hand, some drugs with severe pharmacological effects, small safety index, and rapid absorption may cause obvious adverse effects if the dissolution rate is too fast. reaction, the time to maintain the drug effect will also be shortened, therefore, the dissolution rate of the drug in the preparation should be controlled

Method used

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  • Voriconazole tablet and preparation method thereof
  • Voriconazole tablet and preparation method thereof
  • Voriconazole tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034]

[0035] Preparation Process:

[0036] 1. Weigh the internally added material and add it to the high-speed stirring granulator, start stirring to make the mixture even;

[0037] 2. Prepare povidone K30 into a 5g / 100g aqueous solution. In 90-180s, add to the added material, high-speed stirring granulator to prepare soft material;

[0038] 3. The swing type granulator prepares 24 mesh granules;

[0039] 4. Use a fluidized bed to dry the obtained granules, control the air inlet temperature at 60-70°C, and keep the granule moisture at 3-5%;

[0040] 5. The dried granules are passed through a 20-mesh sieve for granulation;

[0041] 6. Granules are mixed evenly with external materials;

[0042] 7. Compressed into tablets;

[0043] 8. High-efficiency coating machine coating, coating weight gain 2.0-4.0%.

Embodiment 2

[0045]

[0046] Preparation Process:

[0047] 1. Weigh the internally added material and add it to the high-speed stirring granulator, start stirring to make the mixture even;

[0048] 2. Prepare povidone K30 into a 5g / 100g aqueous solution. In 90-180s, add to the added material, high-speed stirring granulator to prepare soft material;

[0049] 3. The swing type granulator prepares 24 mesh granules;

[0050] 4. Use a fluidized bed to dry the obtained granules, control the air inlet temperature at 60-70°C, and keep the granule moisture at 3-5%;

[0051] 5. The dried granules are passed through a 20-mesh sieve for granulation;

[0052] 6. Granules are mixed evenly with external materials;

[0053] 7. Compressed into tablets;

[0054] 8. High-efficiency coating machine coating, coating weight gain 2.0-4.0%.

Embodiment 3

[0056]

[0057]

[0058] Preparation Process:

[0059] 1. Weigh the internally added material and add it to the high-speed stirring granulator, start stirring to make the mixture even;

[0060] 2. Prepare povidone K30 into a 5g / 100g aqueous solution. In 90-180s, add to the added material, high-speed stirring granulator to prepare soft material;

[0061] 3. The swing type granulator prepares 24 mesh granules;

[0062] 4. Use a fluidized bed to dry the obtained granules, control the air inlet temperature at 60-70°C, and keep the granule moisture at 3-5%;

[0063] 5. The dried granules are passed through a 20-mesh sieve for granulation;

[0064] 6. Granules are mixed evenly with external materials;

[0065] 7. Compressed into tablets;

[0066] 8. High-efficiency coating machine coating, coating weight gain 2.0-4.0%.

[0067] Dissolution results

[0068] According to the dissolution test method (Chinese Pharmacopoeia 2020 edition general rule 0931 second method), the ...

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Abstract

The invention provides a voriconazole tablet and a preparation method thereof, and belongs to the technical field of medicine preparations characterized by tablets. Voriconazole is used as a raw material, and lactose monohydrate, spray-dried lactose, pregelatinized starch, croscarmellose sodium, povidone K30 and sodium stearyl fumarate are used as auxiliary materials to prepare the quick-release voriconazole tablet. The voriconazole tablet disclosed by the invention can release more than 80% of drugs within 30 minutes, the voriconazole tablet is similar to an original developed agent in in-vitro dissolution, and the obtained voriconazole tablet is less affected by environmental change, can be stably stored for a long time, and has the advantages of good stability, simple preparation process, easiness in industrial mass production and the like.

Description

technical field [0001] The application relates to a voriconazole tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations characterized by tablets. Background technique [0002] Voriconazole is a second-generation synthetic triazole antifungal drug. Its mechanism of action is to inhibit the demethylation of 14-α sterol mediated by cytochrome P450 in fungi, thereby inhibiting the biosynthesis of ergosterol. Voriconazole, manufactured by Pfizer, USA, is indicated for the treatment of invasive aspergillosis; severe invasive infections caused by fluconazole-resistant Candida species (including C. . It is mainly used to treat progressive, potentially life-threatening infections in immunocompromised patients. [0003] Voriconazole Molecular Formula C 16 h 14 f 3 N 5 O: molecular weight 349.31, logP2.18, its chemical name is as follows: [0004] (αR,βS)-α-(2,4-difluorophenyl)-5-fluoro-β-methyl-α-(1H-1,2,4-triazol-1-ylmethyl)-4...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/506A61K47/26A61K47/38A61K47/36A61K47/14A61P31/10
CPCA61K9/28A61K9/2018A61K9/2013A61K9/2059A61K9/2054A61K31/506A61P31/10
Inventor 董王明宋迎权徐成苗周波金豪胡亚妮刘美玲
Owner ZHEJIANG ANGLIKANG PHARMA
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