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Voriconazole composition and preparation method thereof

A technology of voriconazole and voriconazole tablets, which is applied in the direction of pill delivery, antifungal agents, etc., and can solve the problems of shortening the time to maintain the drug effect, problems with the speed or degree of drug absorption, and small safety index

Inactive Publication Date: 2012-10-31
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The absorption rate of drugs in the body is often determined by the speed of dissolution. Before being absorbed, the drugs in oral solid preparations 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 If the dissolution rate is extremely slow, there may be problems with the absorption rate or degree of the drug in the preparation. On the other hand, some drugs with severe pharmacological effects, low 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 composition and preparation method thereof
  • Voriconazole composition and preparation method thereof
  • Voriconazole composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045]

[0046] Preparation Process:

[0047] (i) Weigh the internal phase material and add it to the high-speed stirring granulator, start stirring to make the mixture uniform;

[0048] (ii) PVP-K90 is formulated into a 5g / 100g aqueous solution, added to the inner phase material, and stirred in a granulator at high speed to prepare a soft material;

[0049] (iii) swinging granulator to prepare 24 mesh granules;

[0050] (iv) drying the obtained particles using a fluidized bed, and the drying temperature is controlled at 30-40°C;

[0051] (v) The dried particles are granulated through a 20-mesh sieve;

[0052] (vi) The particles are evenly mixed with the external phase material;

[0053] (vii) Compression into tablets.

[0054] (viii) Coating with a high-efficiency coating machine, and the weight gain of the coating is 3.5%.

Embodiment 2

[0056]

[0057]

[0058] Preparation Process:

[0059] (i) Weigh the internal phase material and add it to the high-speed stirring granulator, start stirring to make the mixture uniform;

[0060] (ii) PVP-K90 is formulated into a 5g / 100g aqueous solution, added to the inner phase material, and stirred in a granulator at high speed to prepare a soft material;

[0061] (iii) swinging granulator to prepare 24 mesh granules;

[0062] (iv) drying the obtained granules using a fluidized bed, and the drying temperature is controlled at 30-40°C;

[0063] (v) The dried particles are granulated through a 20-mesh sieve;

[0064] (vi) The particles are evenly mixed with the external phase material;

[0065] (vii) Compression into tablets.

[0066] (viii) Coating with a high-efficiency coating machine, and the weight gain of the coating is 5.0%.

Embodiment 3

[0068]

[0069] Preparation Process:

[0070] (i) Weigh the internal phase material and add it to the high-speed stirring granulator, start stirring to make the mixture uniform;

[0071] (ii) PVP-K90 is formulated into a 5g / 100g aqueous solution, added to the inner phase material, and stirred in a granulator at high speed to prepare a soft material;

[0072] (iii) swinging granulator to prepare 24 mesh granules;

[0073] (iv) drying the obtained granules using a fluidized bed, and the drying temperature is controlled at 30-40°C;

[0074] (v) The dried particles are granulated through a 20-mesh sieve;

[0075] (vi) The particles are evenly mixed with the external phase material;

[0076] (vii) Compression into tablets.

[0077] (viii) Coating with a high-efficiency coating machine, and the weight gain of the coating is 3.5%.

[0078] The following comparative examples are voriconazole tablets prepared by adopting several concentrations of PVP-K30 and several concentrati...

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Abstract

The invention relates to a voriconazole tablet, wherein the tablet core of the tablet comprises lactose hydrous, pregelatinized starch, croscarmellose sodium, povidone K90 and magnesium stearate. The prepared tablet core can reach higher hardness, is low in friability, facilitates coating, and can maintain the physical form during packaging and transport process; and although the hardness of the tablet core is higher, the dissolution rate of the tablet is not influenced, and the tablet can be disintegrated within about 20 minutes or a shorter time.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composition of voriconazole and a preparation method thereof. Background technique [0002] Voriconazole, the English name is voriconazole, the chemical name is (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidine)-1-(1H-1,2, 4-triazol-1-yl)-2-butanol. [0003] Voriconazole belongs to triazole antifungal drugs, mainly used for invasive aspergillin, candida infection resistant to fluconazole, severe infection caused by fungi of the genus Fusarium and Scedospora, and also commonly used for neuter Empiric treatment of febrile neutropenic patients. [0004] At present, the imported product of voriconazole oral preparations in my country is a tablet named VFEND, produced by the original manufacturer Pfizer, with a specification of 50mg or 200mg, and the excipients are lactose monohydrate, pregelatinized starch, and croscarmellose sodium (cross-linked CMC-Na), povidone...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/506A61K47/38A61P31/10
Inventor 辛伟张志宏张素娟杨丽霞梁敏王世霞
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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