Posaconazole liquid suspension and preparation method thereof

A technology of posaconazole and suspension, which is applied in the field of medicine, can solve the problems of large particle size variation of posaconazole, large fluctuation of batch particle size, complicated preparation process, etc., and achieve good bioavailability, particle size The effect of small change and simple preparation process

Active Publication Date: 2017-01-18
WUHAN QR PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the easy sedimentation of the existing posaconazole liquid suspension, and the particle size of posaconazole varies greatly before and after ultrasonic dispersion; the particle size fluctuation between batches is also relatively large; And the preparation process is complicated, the defect that is difficult to industrialize, and a kind of posaconazole liquid suspension and preparation method thereof are provided

Method used

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  • Posaconazole liquid suspension and preparation method thereof
  • Posaconazole liquid suspension and preparation method thereof
  • Posaconazole liquid suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 (using microcrystalline cellulose-carboxymethylcellulose sodium complex CL-611 type as suspending agent to prepare posaconazole liquid suspension)

[0038] Taking the total amount of raw materials of the posaconazole liquid suspension as 100mL, the raw material formula of the posaconazole liquid suspension of the present embodiment is as shown in Table 1:

[0039] The raw material formula of the posaconazole liquid suspension of table 1 embodiment 1

[0040]

[0041]

[0042] The preparation method of posaconazole liquid suspension in the present embodiment comprises the steps:

[0043](1) Add simethicone, polysorbate 80, a part of glycerin, sodium benzoate and posaconazole to a part of purified water, stir (stirring speed 300rpm) and mix evenly, and use a high-pressure homogenizer to homogenize (homogeneous pressure 1000bar) to The particle diameter of posaconazole is 2000nm, gets posaconazole concentrated solution; In step (1), the amount of descri...

Embodiment 2

[0046] Embodiment 2 (using microcrystalline cellulose-carboxymethylcellulose sodium complex RC-581 type as suspending agent to prepare posaconazole liquid suspension)

[0047] Taking the total amount of raw materials of the posaconazole liquid suspension as 100mL, the raw material formula of the posaconazole liquid suspension of the present embodiment is as shown in Table 2:

[0048] The raw material formula of the posaconazole liquid suspension of table 2 embodiment 2

[0049]

[0050]

[0051] The preparation method of posaconazole liquid suspension in the present embodiment comprises the steps:

[0052] (1) Add simethicone, polysorbate 80, a part of glycerin, sodium benzoate and posaconazole to a part of purified water, stir (stirring speed 50rpm) and mix well, use a high-pressure homogenizer to homogenize (homogeneous pressure 800bar) to The particle diameter of posaconazole is 1000nm, gets posaconazole concentrated solution; In step (1), the amount of described a p...

Embodiment 3

[0055] Embodiment 3 (using microcrystalline cellulose-carboxymethylcellulose sodium complex RC-591 type as suspending agent to prepare posaconazole liquid suspension)

[0056] Taking the total amount of raw materials of the posaconazole liquid suspension as 100mL, the raw material formula of the posaconazole liquid suspension of the present embodiment is as shown in table 3:

[0057] The raw material formula of the posaconazole liquid suspension of table 3 embodiment 3

[0058]

[0059]

[0060] The preparation method of posaconazole liquid suspension in the present embodiment comprises the steps:

[0061] (1) Add simethicone, nonionic surfactant, part of glycerin, sodium benzoate and posaconazole to a part of purified water, stir (stirring speed 500rpm) and mix evenly, and homogenize with a high-pressure homogenizer (homogeneous pressure 2500bar) The particle diameter until posaconazole is 2000nm, gets posaconazole concentrated solution; In step (1), the amount of desc...

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Abstract

The invention discloses a posaconazole liquid suspension and a preparation method thereof. The raw materials are posaconazole, a microcrystalline cellulose-carboxymethylcellulose sodium compound, a nonionic surfactant, a buffer solution, dimeticone, sodium benzoate, titanium dioxide, high fructose syrup and a pharmaceutically acceptable liquid carrier; and wherein the pharmaceutically acceptable liquid carrier is purified water and glycerin. The posaconazole liquid suspension has the advantages of high stability, good reappearance between batches, and difficult settlement, and the preparation method has the advantages of simple process and easy industrialization.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a posaconazole liquid suspension and a preparation method thereof. Background technique [0002] Posaconazole, chemical name 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazole -1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3- Base]-1,2,4-triazol-3-one, whose structural formula is shown in formula I, is a drug for the prevention or treatment of fungal infections, a broad-spectrum antifungal drug developed by Schering-Plough, and its trade name is Noxafi. It was launched in Germany for the first time in December 2005, and was launched in the United States and the United Kingdom in 2006. So far, it has been listed in more than 60 countries or regions around the world. [0003] [0004] Posaconazole is indicated for the treatment of a variety of invasive fungal infections in adults who are intolerant or refractory to amphoter...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/496A61P31/10
Inventor 陈昂谈邹念靳华林王培全刘勇王朝东
Owner WUHAN QR PHARMA CO LTD
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