Posaconazole solid dispersion composition capable of inhibiting separation by crystallization as well as preparation method thereof

A technology of posaconazole solid and saconazole solid, applied in the field of posaconazole solid dispersion composition and its preparation, can solve problems affecting drug absorption effect, drug precipitation, etc., and achieve strong crystallization inhibition ability, Good absorption in the body

Active Publication Date: 2018-06-08
GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, studies have shown that the finished product of posaconazole will cause drug precipitation in a specific simulated inte

Method used

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  • Posaconazole solid dispersion composition capable of inhibiting separation by crystallization as well as preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The posaconazole solid dispersion composition provided in this embodiment contains: posaconazole 100g, methacrylic acid copolymer type C (trade name: Eudragit L 100-55) 325g, hydroxypropyl cellulose ( Molecular weight 80000) 75g, microcrystalline cellulose 70g, croscarmellose sodium 25g, magnesium stearate 5g and Opadry 24g.

[0048] The preparation method of above-mentioned posaconazole solid dispersion composition is as follows:

[0049] Step 1: The active drug posaconazole, the enteric-coated carrier material methacrylic acid copolymer type C and the plasticizer hydroxypropyl cellulose are pre-mixed respectively to form a mixture, wherein the mixing speed is 10 rpm and the mixing time is 20 minutes;

[0050] Step 2: Set the parameters of the hot-melt extruder, set the working temperature of the hot-melt extrusion to 130°C, the temperature of the extrusion port to 140°C, and the screw speed to 150rpm;

[0051] Step 3: Adjust the material delivery rate to achieve a co...

Embodiment 2

[0058] The posaconazole solid dispersion composition provided in this embodiment contains: posaconazole 100g, methacrylic acid copolymer type A (trade name: Eudragit L 100) 325g, hydroxypropyl cellulose (molecular weight 120000 ) 75g, microcrystalline cellulose 70g, croscarmellose sodium 25g, magnesium stearate 5g and Opadry 24g.

[0059] The preparation method of the posaconazole solid dispersion composition provided in this example is the same as that in Example 1.

Embodiment 3

[0061] The posaconazole solid dispersion composition provided in this embodiment contains: posaconazole 100g, methacrylic acid copolymer type C (trade name: Eudragit L 100-55) 325g, hydroxypropyl cellulose ( Molecular weight 100000) 75g, microcrystalline cellulose 70g, croscarmellose sodium 25g, magnesium stearate 5g and Opadry 24g.

[0062] The preparation method of the posaconazole solid dispersion composition provided in this example is the same as that in Example 1.

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Abstract

The invention discloses a posaconazole solid dispersion composition capable of inhibiting separation by crystallization as well as a preparation method thereof, and relates to the field of posaconazole preparations. The posaconazole solid dispersion composition contains acrylic resin and posaconazole serving as an active component. The research of the invention discovers that compared with hydroxypropyl methylcellulose acetate succinate (HPMCAS) serving as a carrier material, the posaconazole solid dispersion composition taking acrylic resin as a carrier material has the following advantages:after a posaconazole crystal seed is induced in the intestinal environment simulated pH 6.8 dissolution test, the crystallization inhibiting capability is higher and the medicine can be absorbed in vivo better.

Description

technical field [0001] The invention relates to the field of posaconazole preparations, in particular to a posaconazole solid dispersion composition capable of inhibiting crystallization and a preparation method thereof. Background technique [0002] Posaconazole is a derivative of itraconazole, a second-generation triazole drug listed on the FDA in 2006. It has a wider antibacterial spectrum than other triazole drugs, is similar to amphotericin B, and has strong antibacterial activity , It is effective against fungi that cause invasive infections such as Candida, Aspergillus, Zygomycetes and some endemic fungi, and is also effective against other azole drug-resistant strains. [0003] Posaconazole belongs to BCS Class 2 drugs, and its solubility is pH-dependent. Posaconazole has good solubility in acidic environment, and its solubility gradually decreases with the increase of pH. The in vivo research results show that posaconazole is effective. The absorption site is in th...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/496A61K47/32A61P31/04
CPCA61K9/2027A61K9/2806A61K31/496
Inventor 梁兆丰童伟勤
Owner GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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