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Pharmaceutical composition containing isavuconazole

A technology of isavuconazole and its composition, applied in the field of pharmaceutical preparations, can solve the problems of poor solubility, difficult to maintain therapeutic effective concentration, low bioavailability, etc., achieve reduction of related substances, increase bioavailability, and simple preparation process Effect

Inactive Publication Date: 2017-05-03
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Isavuconazole however is very lipophilic and therefore has very poor solubility in aqueous media
Due to the limited solubility of the drugs in aqueous media, their bioavailability after oral administration is usually rather low, making it difficult to maintain therapeutically effective concentrations

Method used

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  • Pharmaceutical composition containing isavuconazole
  • Pharmaceutical composition containing isavuconazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: Isavuconazole pharmaceutical composition prescription:

[0023] Raw material name dosage

[0024] Isavuconazole 100g,

[0025] β-cyclodextrin 20g,

[0026] Microcrystalline Cellulose 96g,

[0027] Crospovidone 12g,

[0028] Povidone 7.2g, is made into 10wt% povidone aqueous solution and adds,

[0029] Magnesium Stearate 4.8g,

[0030] A total of 1000 units were made.

[0031] Preparation Process:

[0032] 1) Take 20g of β-cyclodextrin to make a saturated aqueous solution at 50°C, then put it in a high-speed mixer, start stirring at a speed of 1000 rpm; dissolve 100g of isavuconazole in 3000ml of ethanol, and then add it dropwise to In the stirred saturated aqueous solution of β-cyclodextrin, the dropping rate is 2ml / min, and stirred at constant temperature for 1 hour; stop heating and continue stirring to room temperature, stop stirring after 3 hours, and spray dry to obtain β-cyclodextrin inclusion compound ;

[0033] 2) The prepared β-cyclodextr...

Embodiment 2

[0035] Embodiment 2: Isavuconazole pharmaceutical composition prescription:

[0036] Raw material name dosage

[0037] Isavuconazole 100g,

[0038] β-cyclodextrin 60g,

[0039] Lactose 180g,

[0040] Croscarmellose Sodium 16g,

[0041] Hydroxypropyl methylcellulose 9.6g, is made into 2wt% hydroxypropyl methylcellulose aqueous solution and adds,

[0042] Talc powder 6.4g,

[0043] A total of 1000 units were made.

[0044] Preparation process 1) Weigh β-cyclodextrin according to the prescription amount to make a saturated aqueous solution at 50°C, then put it in a high-speed mixer, start stirring at a speed of 1500 rpm; dissolve 100g of isavuconazole in 3000ml of ethanol, and then Add dropwise into the stirred saturated aqueous solution of β-cyclodextrin at a speed of 2 ml / min, and stir at constant temperature for 30 minutes. Stop heating and continue stirring to room temperature, stop stirring after 2.5 hours, and spray dry to obtain β-cyclodextrin inclusion compound;

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PUM

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Abstract

The invention relates to a pharmaceutical composition containing isavuconazole. Cyclodextrin inclusion technology is adopted, and uniform mixing with pharmaceutically acceptable auxiliary materials is carried out so as to obtain oral tablets. The pharmaceutical composition containing isavuconazole is capable of improving water solubility of drugs, covering the bitter taste of isavuconazole, improving drug compliance of patients, and increasing drug bioavailability to a great degree.

Description

[0001] Technical Field The present invention relates to a pharmaceutical composition containing isavuconazole, which belongs to the technical field of pharmaceutical preparations. Background technique [0002] Isavuconazole (chemical name: 4-[2-[(1R,2R)-2-(2,5-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2 ,4-triazol-1-yl)propyl]-4-thiazolyl]benzonitrile, English name: Isavuconazole, CAS number: 241479-67-4), the drug is mainly used for the treatment of invasive aspergillosis and Mycosis is a broad-spectrum antifungal drug developed by Astellas Japan. [0003] However, isavuconazole is very lipophilic and therefore has very poor solubility in aqueous media. Due to the limited solubility of the drugs in aqueous media, their bioavailability after oral administration is also usually rather low, making it difficult to maintain therapeutically effective concentrations. Other well known methods of increasing the bioavailability of poorly water soluble compounds are the formation of ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/4439A61P31/10
Inventor 严洁
Owner TIANJIN HANKANG PHARMA BIOTECH