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Macitentan microsphere and preparation method thereof

A technology of macitentan and microspheres, applied in the field of macitentan microsphere preparation and its preparation

Inactive Publication Date: 2017-07-07
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As an endothelin receptor antagonist, macitentan still has risks such as hepatotoxicity and embryo-fetal toxicity after oral administration

Method used

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  • Macitentan microsphere and preparation method thereof
  • Macitentan microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The drug-loaded microspheres were prepared by emulsification-solvent evaporation method. Weigh 600mg PLGA and 30mg macitentan and dissolve it in 2.82g dichloromethane, as the oil phase, take 0.5% PVA aqueous solution as the water phase, add the oil phase to the water phase at a ratio of 1:15 at room temperature, High shear at 7000rpm for 120s to form an O / W emulsion. The obtained O / W emulsion was added to the 0.1% PVP aqueous solution in a stirring state at a volume ratio of 1:3, and the stirring was continued for 3 h to fully volatilize the dichloromethane to obtain the macitentan microspheres of the present invention. Subsequently, the macitentan microspheres were centrifuged, washed three times with distilled water, and dried.

[0045] The encapsulation efficiency, drug loading and particle size of the obtained microspheres were determined by the following methods.

[0046] Weigh 5 mg of microspheres into a 15 mL centrifuge tube, add 0.5 mL of dichloromethane, soni...

Embodiment 2

[0052] Drug-loaded microspheres were prepared in the same manner as in Example 1, except that the shear rate was 8500 rpm. It was determined that the encapsulation efficiency of the obtained microspheres was 93.76%, the drug loading was 4.37%, the average particle size was 16.8 μm, and 91.6% of the microspheres had a particle size distribution of 7-30 μm. figure 2 .

Embodiment 3

[0054]Drug-loaded microspheres were prepared in the same manner as in Example 1, except that the shear rate was 10,000 rpm. It was determined that the encapsulation efficiency of the obtained microspheres was 85.76%, the drug loading was 4.15%, the average particle size was 11.6 μm, and 86.3% of the microspheres had a particle size distribution of 7-30 μm. image 3 .

[0055] It can be seen from the results of Examples 1-3 that the size of the shear rate affects the particle size of the microspheres: in the range of 7000rpm-10000rpm, the larger the shear rate, the smaller the particle size of the microspheres. Most preferably, the shear rate is 8500 rpm.

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Abstract

The invention provides a macitentan microsphere preparation and a preparation method thereof. The macitentan microsphere provided by the invention consists of macitentan, a polymer carrier material, an emulsifier and a stabilizer. The preparation method of the macitentan microsphere preparation provided by the invention comprises the following steps: (1) dissolving the polymer carrier material and the macitentan in an oil-phase solvent so as to obtain an oil phase, and taking a water solution of the emulsifier as an aqueous phase; (2) adding the oil phase to the aqueous phase and conducting homogenizing so as to obtain an O / W emulsion; (3) adding the emulsion to a water solution of the stabilizer, so that the solvent of the oil phase completely volatilizes; and (4) separating, washing and drying the microsphere so as to obtain the microsphere preparation provided by the invention.

Description

technical field [0001] This application relates to the field of pharmaceutical preparations. Specifically, the present invention relates to a macitentan microsphere preparation and a preparation method thereof. Background technique [0002] Pulmonary arterial hypertension refers to the persistent increase of pulmonary arterial pressure caused by various reasons. The complex etiology, difficult diagnosis and treatment are the main reasons for the slow development of this therapeutic field for a long time. There are an estimated 130,000 people with pulmonary hypertension in the United States and Europe alone. In China, due to the large population base and many pathogenic factors, the incidence of pulmonary hypertension is greatly underestimated. If patients do not receive effective treatment within 2 years after the onset of pulmonary hypertension, their survival rate is only 40%-55%. [0003] Macitentan is an endothelin (ET) receptor antagonist developed by Actelion Pharm...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/506A61K47/34A61P11/00A61P9/12
CPCA61K9/1641A61K31/506
Inventor 龙伟颜携国陶安进袁建成
Owner HYBIO PHARMA
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