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A kind of voriconazole preparation and preparation method thereof

A technology of voriconazole and voriconazole granules is applied in the directions of pharmaceutical formulations, antifungal agents, medical preparations of inactive ingredients, etc., and can solve the problems of poor stability of voriconazole, restricting the development of voriconazole granules, low solubility of voriconazole, etc., which is not easy to achieve. The effect of deterioration, small differences in dissolution profiles, and stable drug quality

Active Publication Date: 2021-08-31
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, due to the extremely low solubility of voriconazole in water (almost insoluble at pH = 7, 0.2 mg / ml at pH = 3), it is easy to settle after flushing after making granules, and because voriconazole is in a solution state after flushing However, the stability of voriconazole in the solution state is not good, which limits the development of voriconazole granules

Method used

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  • A kind of voriconazole preparation and preparation method thereof
  • A kind of voriconazole preparation and preparation method thereof
  • A kind of voriconazole preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Prescription (consumption: mass percentage)

[0047]

[0048] Preparation:

[0049] 1) Voriconazole is micronized to control the particle size D 90 In the range of 80μm ~ 150μm;

[0050] 2) Mix micronized voriconazole, lactose, pregelatinized starch, citric acid and croscarmellose sodium according to the prescription quantity, add povidone K 30 Prepare soft materials from aqueous solution, sieve and granulate to obtain wet granules;

[0051] 3) drying the above granules to obtain dry granules;

[0052] 4) Sieve the dry granules for granulation, add magnesium stearate, mix evenly, after passing the quality inspection, pack into bags to obtain the voriconazole granules.

Embodiment 2

[0054] Prescription (Amount: Percentage)

[0055]

[0056] Preparation:

[0057] 1) Voriconazole is micronized to control the particle size D 90 In the range of 100μm ~ 120μm;

[0058] 2) Mix the micronized voriconazole, lactose, starch, citric acid and low-substituted hydroxypropyl cellulose evenly according to the prescription amount, add ethyl cellulose and appropriate amount of water to make a soft material, sieve and granulate to obtain wet granules;

[0059] 3) drying the above granules to obtain dry granules;

[0060] 4) Sieve the dry granules for granulation, add magnesium stearate, mix evenly, after passing the quality inspection, pack into bags to obtain the voriconazole granules.

Embodiment 3

[0062] Prescription (Amount: Percentage)

[0063]

[0064] Preparation:

[0065] 1) Voriconazole is micronized to control the particle size D 90 In the range of 100μm ~ 120μm, the particle size D 90 Particles between 110 μm and 120 μm account for 30% of the total voriconazole, particle size D 90 Particles between 100 μm and 110 μm account for 70% of the total voriconazole;

[0066] 2) Mix micronized voriconazole, dextrin, microcrystalline cellulose, citric acid and carboxymethyl starch sodium evenly according to the prescription amount, add hypromellose and appropriate amount of water to make soft material, sieve and granulate to obtain wet granules ;

[0067] 3) drying the above granules to obtain dry granules;

[0068] 4) Sieve the dry granules for granulation, add magnesium stearate, mix evenly, after passing the quality inspection, pack into bags to obtain the voriconazole granules.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and in particular relates to a voriconazole preparation and a preparation method thereof. The voriconazole preparation is a granule prepared from voriconazole and pharmaceutically acceptable adjuvants, wherein the particle size of voriconazole is D 90 In the range of 80 μm to 150 μm, preferably in the range of 100 μm to 120 μm, more preferably 110 μm < particle size D 90 Particles ≤ 120 μm account for 5-30% of the total voriconazole, 100 μm ≤ particle size D 90 Particles ≤110 μm accounted for 70-95% of the total voriconazole. The present invention solves the problem that voriconazole is easy to settle after being made into granules by controlling the particle size distribution of the active ingredient voriconazole; by adding the corrective agent citric acid, it not only solves the problem of poor stability of voriconazole in neutral and alkaline solution states The problem, and increased solubility, further improved the problem that it is easy to settle when washed into water after being made into granules.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a voriconazole preparation and a preparation method thereof. Background technique [0002] Voriconazole (Voriconazole CAS No.: 137234-62-9) chemical structure has been disclosed in European Patent EP0440372, and its structural formula is as follows: [0003] [0004] The product was approved by the US FDA in May 2002, and the trade name is "Vfend" and "Weifan". Voriconazole is a second-generation synthetic triazole antifungal drug. Its mechanism of action is to inhibit the demethylation of 14α-sterol mediated by cytochrome P450 in fungi, thereby inhibiting the biosynthesis of ergosterol. In vitro tests have shown that voriconazole has a spectrum of antifungal effects. The product has antibacterial effect on Candida (including fluconazole-resistant Candida krusei, Candida glabrata and Candida albicans drug-resistant strains), and has bactericidal effect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/12A61K31/506A61P31/10
CPCA61K9/1617A61K31/506
Inventor 刘丽媛刘冬马鹰军王印
Owner HAINAN JINRUI PHARMA CO LTD