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METHOD FOR PRODUCING STABLE AMORPHOUS HYBRID NANOPARTICLES CONTAINING AT LEAST ONE KIND OF PROTEIN KINASE INHIBITOR AND AT LEAST ONE KIND OF POLYMERIC STABILIZED MATRIX-FORMING COMPONENT
METHOD FOR PRODUCING STABLE AMORPHOUS HYBRID NANOPARTICLES CONTAINING AT LEAST ONE KIND OF PROTEIN KINASE INHIBITOR AND AT LEAST ONE KIND OF POLYMERIC STABILIZED MATRIX-FORMING COMPONENT
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机译:包含至少一类蛋白激酶抑制剂和至少一类聚合物稳定基质形成成分的稳定非晶态混合纳米颗粒的制备方法
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摘要
PROBLEM TO BE SOLVED: To provide a method for increasing dissolution rate and bioavailability of a protein kinase inhibitor (PKI) which is useful in a pharmaceutical composition.SOLUTION: Stable amorphous hybrid nanoparticles are produced by a specific production method from nilotinib being hardly water-soluble drug PKI, or salt or hydrate or solvate, or combinations thereof, and at least one kind of polymeric stabilized matrix-forming component. A pressurized flow of nilotinib dissolved in solvent and a second pressurized flow of anti-solvent are mixed, a mixed flow is sprayed from a nozzle outlet to form hybrid nanoparticles, and generated hybrid nanoparticles are recovered. In the production method, at least one of the first flow or the second flow contains a polymeric stabilized matrix-forming component, furthermore at least one of the first flow and the second flow is supercritical or subcritical COfluid, and is supplied to the nozzle outlet at approximately 10 to approximately 25°C at the pressure of approximately 100 to approximately 150 bar.SELECTED DRAWING: Figure 1
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