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Solid medicine composition containing voriconazole

A voriconazole and composition technology, applied in the field of new antifungal pharmaceutical compositions, can solve the problems of poor patient compliance, large difference in dissolution rate between batches, poor water solubility of voriconazole, etc., and achieve high bioavailability and fast absorption in vivo

Inactive Publication Date: 2009-03-25
AVENTIS PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] CN200510095595.4 discloses a voriconazole injection and a preparation method thereof, but it is inconvenient to use and patient compliance is poor; CN200510068033.0 discloses a voriconazole preparation and a preparation method thereof, wherein suspending agents such as beeswax are used to prepare soft capsules, Although liquid hard capsules and drop pills have overcome the limitations of storage, transportation, and inconvenient use of liquid preparations such as injections in the past, the prescriptions contain a certain amount of preservatives, and the production process is cumbersome
[0004] Oral solid preparations currently on the market in China are ordinary tablets, but due to the poor water solubility of voriconazole, the dissolution rate of the tablet is low, and the difference in dissolution rate between batches is large, and the treatment response is not good. At the same time, due to the strong hydrophobicity of voriconazole properties, making it difficult to granulate and compress tablets

Method used

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  • Solid medicine composition containing voriconazole
  • Solid medicine composition containing voriconazole
  • Solid medicine composition containing voriconazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: It is in the form of a chewable tablet

[0018]

[0019] Preparation process: Weigh voriconazole and poloxamer according to the prescription amount to prepare solid dispersion, weigh the rest of the excipients, pass through 100 mesh, mix well, add 10% povidone aqueous solution as adhesive, make soft material, pass through 20 mesh Sieve and granulate, dry, granulate with a 24-mesh sieve; add magnesium stearate and orange flavor according to the prescription ratio, mix well, and compress into tablets.

Embodiment 2

[0020] Embodiment 2: It exists in the form of dispersible tablets

[0021]

[0022] Preparation process: Weigh voriconazole and poloxamer according to the prescription amount to prepare solid dispersion, weigh the rest of the excipients, pass through 100 mesh, mix well, add sucralose aqueous solution as adhesive, make soft material, pass through 20 mesh sieve granules, dried, sieved with 24 meshes; add magnesium stearate and orange flavor according to the prescription ratio, mix well, and compress into tablets.

[0023] Embodiment 2 is compared with the dissolution rate of commercially available common tablet (n=6, X ± SD)

[0024]

[0025] The results show that: the dissolution of the sample prepared in Example 2 at each time point is faster than that of the common tablet.

Embodiment 3

[0026] Embodiment 3: It exists in the form of an orally disintegrating tablet

[0027]

[0028] Preparation process: Weigh voriconazole and poloxamer according to the prescription amount to prepare solid dispersion, weigh the rest of the excipients, pass through 100 mesh, mix well, use water as binder, make soft material, pass through 20 mesh sieve to granulate, dry, Sieve through a 24-mesh sieve; add magnesium stearate and orange flavor according to the prescription ratio, mix well, and compress into tablets.

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PUM

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Abstract

The invention discloses voriconazole solid combination. The solid dispersion technology is adopted in the preparation process of the combination. The preparation forms include dispersible tablets, orally disintegrating tablets and chewable tablets. The voriconazole solid combination is used for the treatment of the diseases caused by fungal infection.

Description

technical field [0001] The invention relates to a novel antifungal pharmaceutical composition containing voriconazole, in particular to a solid pharmaceutical composition containing voriconazole solid dispersion. Background technique [0002] In recent years, the incidence of deep fungal infection has continued to increase, and drug-resistant strains have also shown an upward trend, making it gradually become the main cause of death caused by infectious diseases in courtyards. Fungal infections in immunocompromised patients are associated with high morbidity and mortality, and those at greatest risk are those with severely compromised immune systems from cancer chemotherapy, bone marrow or organ transplantation, high-dose corticosteroid use, and AIDS. In order to solve the problems faced by the clinical treatment of deep fungal infections, Pfizer developed a new type of broad-spectrum triazole antifungal drug - voriconazole (voriconazole) based on the original antifungal dru...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K47/34A61K47/38A61K9/20A61P31/10A61K47/10
Inventor 孟凡静
Owner AVENTIS PHARMA HAINAN
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