A kind of posaconazole fat emulsion injection and preparation method thereof

A technology for posaconazole fat and posaconazole, which is applied in the directions of emulsion delivery, oil/fat/wax inactive ingredients, pharmaceutical formulations, etc., can solve problems such as low solubility, achieve simple preparation process and improve stability , good reproducibility

Inactive Publication Date: 2017-03-08
JINAN KANGHE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the prior art, the present invention provides a posaconazole fat emulsion injection that does not contain β-cyclodextrin series derivatives. The posaconazole is encapsulated in the fat emulsion particles, which solves the problem of its The problem of low solubility in water improves its solubility in the drug delivery system, solves a series of application limitations such as serious adverse reactions caused by β-cyclodextrin series derivatives in clinical applications, and enhances patient compliance

Method used

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  • A kind of posaconazole fat emulsion injection and preparation method thereof
  • A kind of posaconazole fat emulsion injection and preparation method thereof
  • A kind of posaconazole fat emulsion injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Embodiment 1: 1000ml posaconazole fat emulsion injection preparation method

[0032] Under the protection of nitrogen, mix 100 g of soybean oil and 10 g of soybean lecithin evenly, heat to 80 ° C, add 18 g of the main drug posaconazole while stirring, and mix well to obtain an oil phase;

[0033] Add 50g of mannitol to 750ml of water for injection, dissolve evenly, and heat to 80°C at the same time to obtain the water phase;

[0034] Under the protection of nitrogen, the obtained oil phase was added dropwise to the water phase under high-speed stirring (2500rpm), kept stirring for 5 minutes, adjusted the pH to 2.0 with a pH regulator, added water for injection to the full amount, and mixed well to obtain the initial Emulsion;

[0035] Under the protection of nitrogen, at room temperature, the obtained primary emulsion was circulated in a high-pressure homogenizer for 4 times under high pressure (the set homogeneous pressure was 600bar) to obtain an emulsion;

...

Embodiment 2

[0037] Embodiment 2: Preparation method of 1000ml posaconazole fat emulsion injection

[0038] Under nitrogen protection, mix 100 g of soybean oil and 20 g of soybean lecithin evenly, heat to 75°C, add 20 g of the main drug posaconazole while stirring, and mix well to obtain an oil phase;

[0039] Add 50g of mannitol to 700ml of water for injection, dissolve evenly, and heat to 75°C at the same time to obtain the water phase;

[0040] Under the protection of nitrogen, the obtained oil phase was added dropwise to the water phase under high-speed stirring (1800rpm), kept stirring for 5 minutes, adjusted the pH to 2.6 with a pH regulator, added water for injection to the full amount, and mixed well to obtain the initial Emulsion;

[0041] Under the protection of nitrogen, at room temperature, the obtained primary emulsion was circulated in a high-pressure homogenizer for 4 times under high pressure (the set homogeneous pressure was 400bar) to obtain an emulsion;

[0042...

Embodiment 3

[0043] Embodiment 3: 1000ml posaconazole fat emulsion injection preparation method

[0044] Under nitrogen protection, mix 75g of soybean oil, 5g of soybean lecithin and 5g of poloxamer evenly, heat to 75°C, add 18g of the main drug posaconazole while stirring, and mix well to obtain an oil phase;

[0045] Add 55g of glucose to 650ml of water for injection, dissolve evenly, and heat to 75°C at the same time to obtain the aqueous phase;

[0046] Under the protection of nitrogen, the obtained oil phase was added dropwise to the water phase under high-speed stirring (2500rpm), kept stirring for 5 minutes, adjusted the pH to 3.0 with a pH regulator, added water for injection to the full amount, and mixed well to obtain the initial Emulsion;

[0047] Under the protection of nitrogen, at room temperature, the obtained primary emulsion was circulated in a high-pressure homogenizer for 4 times under high pressure (the set homogenization pressure was 500 bar) to obtain an emuls...

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Abstract

The invention provides a posaconazole fat emulsion injection and a preparation method thereof. It uses posaconazole as a medicinal active ingredient, and uses oily solvent, water, an osmotic pressure regulator and a pH regulator to make fat The emulsion solves the problem of low solubility of posaconazole in water, has high drug loading, no drug leakage, and improves the stability of posaconazole in the preparation. The invention also provides a preparation process of the preparation, which has simple process and good reproducibility, and can realize industrial production. The formulation was developed for intravenous administration for the prophylaxis of invasive Aspergillus infections in patients with severely compromised immune systems.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a posaconazole fat emulsion injection and a preparation method thereof. Background technique [0002] Posaconazole is a derivative of itraconazole, posaconazole (posaconazole, trade name Noxafil, CAS registration number 171228-49-2, chemical name: 4-[4-[4-[4-[[ (3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy] Phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypent-3-yl]-1,2,4-triazol-3-one) is Schering-Plough The third-generation antifungal drug developed by Pharmaceutical Co., Ltd. was first launched in Germany in December 2005, and launched in the UK in March 2006. On September 18, 2006, it was approved by the FDA. In 2014, the FDA has approved posaconazole injection (18mg / mL), which is a new intravenous (IV) dosage form of posaconazole, suitable for patients aged 18 and above. Merck's antifungal drug is also marketed as posaconazole (...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/496A61K47/44A61P31/10A61K47/24A61K47/10
Inventor 张颖刘元鑫杨春芬赫红曲延伟杨江勇何花
Owner JINAN KANGHE MEDICAL TECH
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