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Voriconazole dried suspension and preparation method thereof

A voriconazole dry, voriconazole technology, applied in the field of voriconazole dry suspension and its preparation, can solve the problems of low bioavailability, low drug dissolution, etc., and achieve high bioavailability, fast absorption, and large distribution area

Inactive Publication Date: 2011-11-09
HANGZHOU SHARPLY PHARM R&D INSTIT +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve the problems of low dissolution and low bioavailability of existing oral dosage forms, and provide a dry suspension of itraconazole that is fast absorbed, high in bioavailability and suitable for the elderly and children.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] prescription

[0026] Composition Weight (g) Ratio (%)

[0027] Voriconazole 200 6

[0028] Xanthan gum 216.7 6.5

[0029] Sucrose 2516.7 75.5

[0030] Citric acid 33.3 1

[0031] Sodium citrate 253.3 7.6

[0032] Sodium Benzoate 3.3 0.1

[0033] Micronized silica gel 33.3 1

[0034] Orange flavor 10 0.3

[0035] Titanium dioxide 66.7 2

[0036] Make 1000 bags.

[0037] Preparation:

[0038] (1), after drying and mixing the pulverized voriconazole, xanthan gum, sucrose, sodium citrate, and citric acid of the prescribed amount, pass through a 100-mesh sieve.

[0039] (2) Add appropriate amount of water to the mixed material in step (1) to make a soft material, then granulate with a 30-mesh sieve, and dry to become dry granules.

[0040] (3), after mixing the dry granules of step (2) with the prescribed amount of titanium dioxide, micropowder silica gel, orange flavor essence and sodium benzoate, then sub-package.

Embodiment 2

[0042] prescription

[0043] Composition Weight (g) Ratio (%)

[0044] Voriconazole 200 10

[0045] Carboxymethylcellulose 300 15

[0046] Sucrose 1250 62.5

[0047] Citric acid 42 2.1

[0048] Sodium citrate 160 8

[0049] Sodium benzoate 2 0.1

[0050] Micronized silica gel 20 1

[0051] Cream essence 6 0.3

[0052] Titanium dioxide 40 2

[0053] Make 1000 bags.

[0054] Preparation:

[0055] (1), after drying and mixing the pulverized voriconazole, carboxymethylcellulose, sucrose, sodium citrate and citric acid of the prescribed amount, pass through a 100-mesh sieve.

[0056] (2) Add appropriate amount of water to the mixed material in step (1) to make a soft material, then granulate with an 18-mesh sieve, and dry to become dry granules.

[0057] (3) Mix the dried granules in step (2) with the prescribed amount of titanium dioxide, micropowder silica gel, butter essence and sodium benzoate, and then pack them separately.

Embodiment 3

[0059] prescription

[0060] Composition Weight (g) Ratio (%)

[0061] Voriconazole 200 8

[0062] Xanthan gum 250 10

[0063] Microcrystalline cellulose 870 34.8

[0064] Sucrose 1100 44

[0065] Tartaric acid 25 1

[0066] Potassium tartrate 245 9.8

[0067] Sodium Benzoate 2.5 0.1

[0068] Micronized silica gel 25 1

[0069] Apple flavor 7.5 0.3

[0070] Titanium dioxide 5 2

[0071] Make 1000 bags.

[0072] Preparation:

[0073] (1), after drying and mixing the pulverized voriconazole, xanthan gum, microcrystalline cellulose, sucrose, potassium tartrate and tartaric acid of the prescribed amount, pass through a 100-mesh sieve.

[0074] (2) Add appropriate amount of water to the mixed material in step (1) to make a soft material, then granulate with a 30-mesh sieve, and dry to become dry granules.

[0075] (3), after mixing the dried granules in step (2) with the prescribed amount of titanium dioxide, micropowder silica gel, apple essence and sodium benzoate, then...

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PUM

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Abstract

The invention relates to a Voriconazole dried suspension, comprising 5-15wt% of Voriconazole, 3-20wt% of suspending agent, 30-60wt% of filling agent, 20-50wt% of sweetening agent, 0.1-10wt% of PH regulator, 0.2-2wt% of lubricant, 0.1-2wt% of flavoring agent and 1-5wt% of opacifier. The Voriconazole dried suspension is a fine particle dosage form with more advantages than tablet and other solid dosage forms, has the advantages of large distribution area in gastrointestinal tract, fast absorption and high bioavailability, and can avoid the disadvantage of difficult swallowing of the tablet. Dried suspension is stored as solid, and is given through the mouth in suspension state, so as to be suitable for drugs with low water stability, and for children, the old and the patients who has difficult in swallowing.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for treating fungi, in particular to a voriconazole dry suspension and a preparation method thereof. Background technique [0002] Voriconazole has been disclosed in European Patent EP0440372 and is effective in the treatment of fungal infections. [0003] Voriconazole (Voriconazole) is a newly synthesized triazole drug, which is the second-generation synthetic fluconazole derivative. As a new type of antifungal drug, it has the characteristics of broad antibacterial spectrum and strong antibacterial efficacy. According to the report of "Foreign Medicine", the drug has been widely used clinically abroad and has achieved satisfactory curative effect. [0004] A large number of experimental studies and in vitro tests have shown that voriconazole, as a newly synthesized compound, has a wider antifungal spectrum and stronger efficacy than the current antifungal drugs. When used for Candida, whether i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/506A61P31/10
Inventor 范敏华姜新东刘华
Owner HANGZHOU SHARPLY PHARM R&D INSTIT
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