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Aprepitant solid dispersion composition

A technology of solid dispersion and aprepitant, applied in drug combination, drug delivery, organic active ingredients, etc., can solve the problems of slow drug release, affecting drug release, slow dissolution rate, etc.

Active Publication Date: 2012-07-04
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the one hand, if the carrier material swells too quickly, it may encapsulate the drug, which will affect the release of the drug
On the other hand, too slow dissolution rate of the carrier material will result in too slow drug release

Method used

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  • Aprepitant solid dispersion composition
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  • Aprepitant solid dispersion composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1: the preparation of aprepitant raw material

[0053] With reference to the method of Example 75 of Chinese invention patent application CN1142819A, crystalline aprepitant is prepared, and it has the following properties as determined by X-ray diffraction: figure 1 For the XRD pattern shown, the measurement conditions are: Cu (40kV, 40mA), 3.0°~45.0°(2θ) scanning, and the prominent X-ray diffraction peaks are as follows:

[0054]

[0055] It also has figure 2 DSC spectrum shown.

Embodiment 2

[0057]Take 48 grams of aprepitant prepared in Example 1 and pass through a 100-mesh sieve for later use, and copovidone (Copovidone, N-vinylpyrrolidone / vinyl acetate copolymer) VA64 pass through a 60-mesh sieve for later use. Divide aprepitant equally into 3 parts, 12 grams each, and mix them with copovidone VA64 at a mass ratio of 1:5, 1:1 and 1:0.5, and then divide the powder mixture into equal parts each containing There are 12 parts of a mixture of 4 grams of aprepitant, and the mixtures containing different mass ratios are heated at 100°C, 150°C, 200°C, and 250°C to prepare solid dispersion compositions. The specific operation is to feed the powder mixture into a twin-screw extruder, pulverize, mix, and melt in the extruder, extrude a strip-shaped translucent melt, and place the extrudate in a tray to cool and solidify at room temperature. Grinding and passing through a 60-mesh sieve to obtain a solid dispersion composition powder, and measuring its stability and dissolut...

Embodiment 3

[0067] The aprepitant of 4 grams of embodiment 1 is mixed with 4 grams of copovidone (Copovidone, N-vinylpyrrolidone / vinyl acetate copolymer) VA64 respectively after passing through 100 mesh and 60 mesh sieves, then this powder mixture is fed into In the twin-screw extruder, pulverize, mix and melt in the extruder, extrude a strip-shaped translucent melt, put the extrudate in a pan, cool and solidify at room temperature, pulverize and grind through a 60-mesh sieve to obtain a solid dispersion composition powder, its XRD pattern is as attached image 3 As shown, the measurement conditions are: Cu (40kV, 40mA), 3.0°~45.0°(2θ) scanning, the prominent X-ray diffraction peaks are as follows:

[0068]

[0069]

[0070] It also has Figure 4 DSC spectrum shown.

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Abstract

The invention belongs to the field of medicinal preparation, and particularly provides an aprepitant solid dispersion composition and a preparation method thereof as well as a medicinal composition prepared from the solid dispersion composition. The composition contains aprepitant and at least one water-soluble polymer, and the aprepitant is uniformly dispersed in the water-soluble polymer. The mass ratio of the aprepitant to the water-soluble polymer is 1:(0.5-10). The aprepitant solid dispersion composition provided by the invention is dissolved in a water-based medium at an unexpected high level in a relatively short time, and has the advantages of improved dissolution characteristic and obvious physical stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations. Specifically, the invention provides an aprepitant solid dispersion composition and a preparation method thereof, which also includes further preparing the solid dispersion composition into a pharmaceutical composition. Background technique [0002] Aprepitant (Aprepitant) is an NK1 receptor antagonist developed and marketed by Merck. It was approved by the FDA in 2003 as an oral capsule and was listed in the United States for the prevention of postoperative nausea and vomiting, or with other antiemetics. Combined to prevent nausea and vomiting caused by chemotherapy drugs. Compound aprepitant was disclosed for the first time in WO9516679, and its chemical name is 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3 -(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazole)methyl)-morpholine, the structure is shown in formula I . Aprepitant is almost insoluble in water. At pH 2-10, th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/5377A61K47/38A61P1/08
Inventor 周文亮张来芳方晓志
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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