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Method for preparing aprepitant solid dispersing composition

A technology of solid dispersion and aprepitant, which is applied in the direction of drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problems of solubility and dissolution rate reduction, and achieve the effect of improving dissolution characteristics and significant physical stability

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

During storage, phase separation, crystal growth, or transformation of the amorphous (metastable) to crystalline state inevitably lead to a decrease in solubility and dissolution rate

Method used

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  • Method for preparing aprepitant solid dispersing composition
  • Method for preparing aprepitant solid dispersing composition
  • Method for preparing aprepitant solid dispersing composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Preparation of aprepitant raw materials

[0049] With reference to the method of Chinese invention patent application CN1142819A Example 75 to prepare crystalline aprepitant, it has such figure 1 The XRD pattern shown, the measurement conditions are: Cu (40kV, 40mA), 3.0°~45.0° (2θ) scanning, typical X-ray diffraction peaks are as follows:

[0050]

[0051] It also has figure 2 DSC spectrum shown.

Embodiment 2

[0053] 48 grams of aprepitant prepared in Example 1 was passed through a 100-mesh sieve for later use, and copovidone (Copovidone, N-vinylpyrrolidone / vinyl acetate copolymer) VA64 was passed through a 60-mesh sieve for later use. Divide aprepitant into 3 equal parts, each part is 12 grams, and mix with copovidone VA64 according to the mass ratio of 1:5, 1:1 and 1:0.5, and then divide the powder mixture into equal parts containing A total of 12 parts of a mixture of 4 grams of aprepitant were prepared by heating the mixtures with different mass ratios at 100°C, 150°C, 200°C, and 250°C to prepare a solid dispersion composition. The specific operation is to feed the powder mixture into a twin-screw extruder, pulverize, mix and melt in the extruder to extrude a strip-shaped translucent melt, and the extrudate is placed in a tray and cooled and solidified at room temperature. The powder of the solid dispersion composition was obtained by grinding and passing through a 60-mesh sieve...

Embodiment 3

[0063] 4 grams of aprepitant of Example 1 and 4 grams of copovidone (Copovidone, N-vinylpyrrolidone / vinyl acetate copolymer) VA64 were mixed after passing through 100 mesh and 60 mesh sieves, respectively, and then the powder mixture was fed into In a twin-screw extruder, pulverize, mix, and melt in the extruder, extrude a strip-shaped translucent melt, place the extrudate in a tray, cool and solidify at room temperature, pulverize and grind it 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, typical X-ray diffraction peaks are as follows:

[0064]

[0065] It also has Figure 4 DSC spectrum shown.

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Abstract

The invention belongs to the field of medicament preparations, and in particular provides a method for preparing an aprepitant solid dispersing composition. The composition contains aprepitant and at least one water-soluble polymer. The method comprises the following steps of: crushing, mixing, melting and extruding the aprepitant and the water-soluble polymer in an extruder, wherein the heating temperature of the extruder is not below the Tg value of the water-soluble polymer or between 30 DEG C below the melting point and the melting point of the aprepitant; and cooling and curing the extruded product, and thus obtaining the solid dispersing composition. The aprepitant solid dispersing composition prepared by the method is dissolved in a water-based medium on an unexpected high level in relatively short time, and has improved dissolving characteristic and remarkable physical stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically the invention provides a method for preparing aprepitant solid dispersion composition. Background technique [0002] Aprepitant is a NK1 receptor antagonist developed and marketed by Merck. It was approved by the FDA in 2003 as an oral capsule in the United States for the prevention of postoperative nausea and vomiting, or combined with other antiemetic drugs. Used in combination to prevent nausea and vomiting caused by chemotherapy drugs. The compound aprepitant was first disclosed 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, the solubility of aprepitant in water is very low at pH 2-10, 3-7 μg / ml, and the Log P at pH 7.0 is 4.8. [0003] [0004] Formula I [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/5377A61K47/32A61K47/34A61P1/08
Inventor 周文亮张来芳方晓志
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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