Application of pazopanib, pharmaceutical composition, injection, preparation method and application

Abstract

The invention discloses application of pazopanib, a pharmaceutical composition, an injection, a preparation method and application. The pharmaceutical composition comprises the following components: pazopanib, a cyclodextrin solubilizer and a solvent, wherein the mass ratio of pazopanib to the cyclodextrin solubilizer is 1: (13-100); and based on 1mL of the pharmaceutical composition, the concentration of the cyclodextrin solubilizer in the pharmaceutical composition is 6-330mg / mL. The pharmaceutical composition prepared by the invention can be used for treating diseases such as acute lung injury, pulmonary fibrosis and acute respiratory distress syndrome, and the treatment aim can be achieved by using a small amount of pazopanib; and moreover, the pharmaceutical composition is high in bioavailability, high in stability and low in impurity content, and the phenomenon of drug accumulation is avoided.

Description

[0001] This application claims the priority of the Chinese patent application CN202010178371.4 with the filing date of March 13, 2020. This application cites the full text of the above-mentioned Chinese patent application. technical field [0002] The invention relates to the application of pazopanib, a pharmaceutical composition, an injection, a preparation method and application. Background technique [0003] Pazopanib hydrochloride is an oral VEGF-2 inhibitor developed by GlaxoSmithKline. The drug also has inhibitory effects on PDGFR and c-KIT tyrosine kinases at the same time, not only has inhibitory effects on renal cell carcinoma, but also has inhibitory effects on non-small cell carcinoma, breast cancer, sarcoma and other tumors. [0004] Chinese patent document (CN102970871A) discloses a kind of pharmaceutical composition and preparation method thereof, and this pharmaceutical composition comprises the modified cyclodextrin of 10mg / ml pazopanib, 2~13% weight, carrie...

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Problems solved by technology

[0004] Chinese patent document (CN102970871A) discloses a kind of pharmaceutical composition and preparation method thereof, and this pharmaceutical composition comprises the modified cyclodextrin of 10mg / ml pazopanib, 2~13% weight, carries out the modified cyclodextrin The pKa of pazopanib and modified cyclodextrin in water is selected such that the modified cyclodextrin is lower than the pKa of pazopanib alone in water, the pH is 3.5-5.7, and the osmolality is 200-400mOsm Tonicity modifier and water are required, the pharmaceutical composition is only applied in eye drops, there is no presentation on the treatment of acute lung injury

[0007] In summary, although it is disclosed in the prior art that pazopanib can be used to treat pulmonary fibrosis, there is no report that it can be used to treat acute lung injury

And when pazopanib is used for the treatment of pulmonary fibrosis, it can only be taken orally, and a relatively large amount of pazopanib is needed to achieve the defect of treating pulmonary fibrosis.

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