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Lenvatinib mesylate solid dispersion and preparation method and application thereof

A technology of solid dispersion and lenvatinib, applied in the field of medicine, can solve the problem of low solubility of lenvatinib mesylate, and achieve the effect of good therapeutic effect and improved solubility

Active Publication Date: 2020-01-17
LEPU PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although the crystal forms are different, the solubility of lenvatinib mesylate is not high. According to the patent US20180155291A, the solubility of crystal form C and crystal form M in simulated feeding state intestinal fluid are 0.0003mg / mL and 0.0004mg / L respectively

Method used

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  • Lenvatinib mesylate solid dispersion and preparation method and application thereof
  • Lenvatinib mesylate solid dispersion and preparation method and application thereof
  • Lenvatinib mesylate solid dispersion and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Embodiment 1: Preparation of lenvatinib mesylate solid dispersion (I)

[0023] Add 24.5g of lenvatinib mesylate into 150ml of acetone / water mixed solvent (mass ratio, 10:1), heat up to about 55°C, stir to dissolve, add 15g of hydroxypropyl cellulose evenly, stir to dissolve ,spare. Add 245g of calcium carbonate into the fluidized bed, set the inlet air temperature at 60°C, and when the material temperature reaches 25°C, spray the lenvatinib mesylate solution into the fluidized bed. After spraying, add 10mL of acetone / water mixed solvent (mass ratio, 10:1) to spray into the fluidized bed, and dry until the water content is below 1.0%. After grinding, 268.23 g of solid dispersion was obtained, yield 94.28%.

Embodiment 2

[0024] Embodiment 2: Preparation of lenvatinib mesylate solid dispersion (II)

[0025] Add 49g of lenvatinib mesylate into 200ml of acetone / water mixed solvent (mass ratio, 10:1), heat up to about 55°C, stir to dissolve, add 30g of hypromellose evenly, stir to dissolve, spare. Add 490g of calcium carbonate into the high-shear wet granulator, open the cutting knife and the granulating knife, and atomize and spray the lenvatinib mesylate solution. After that, put the material into a blast drying oven at 60°C to dry to a moisture content below 1%. After grinding, the collected material was 529.21g, and the yield was 93.01%.

Embodiment 3

[0026] Embodiment 3: Preparation of lenvatinib mesylate solid dispersion (III)

[0027] Add 25g of lenvatinib mesylate into 150ml of acetone / water mixed solvent (mass ratio, 10:1), heat up to about 55°C, stir to dissolve, add 15g of hydroxypropyl cellulose evenly, stir to dissolve, spare. Add 200g of mannitol into the fluidized bed, set the inlet air temperature to 60°C, and when the material temperature reaches 25°C, spray the lenvatinib mesylate solution into the fluidized bed. After spraying, add 10mL of acetone / water mixed solvent (mass ratio, 10:1) to spray into the fluidized bed, and dry until the water content is below 1.0%. After grinding, 213.34 g of solid dispersion was obtained, yield 88.89%.

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Abstract

The invention discloses a lenvatinib mesylate solid dispersion and a preparation method and application thereof, and belongs to the field of chemical pharmacy. The solid dispersion is obtained by thefollowing steps: dissolving lenvatinib mesylate into a solvent, then adding a cellulose derivative, performing stirring for dissolving, spraying the obtained solution onto a carrier, and removing a solvent by drying to obtain the lenvatinib mesylate solid dispersion. The carrier is one or a mixture of more than two of inorganic calcium salt, mannitol, sorbitol, microcrystalline cellulose and low-substituted hydroxypropyl cellulose in any proportion. The lenvatinib mesylate capsule prepared by the method disclosed by the invention improves the problems of the solubility, dissolution rate and stability of lenvatinib mesylate, and can better play a role in treatment.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a solid dispersion of lenvatinib mesylate and a preparation method and application thereof. Background technique [0002] Lenvatinib mesylate is a kinase inhibitor, which mainly inhibits angiogenesis by inhibiting vascular endothelial growth factor receptor VEGFR and fibroblast growth factor receptor FGFR, thereby exerting an anti-tumor effect. Developed by Japan's Eisai Pharmaceutical Company, it was approved by the US FDA on February 13, 2015 for the treatment of thyroid cancer. Approved in China on September 4, 2018, the indication is unresectable hepatocellular carcinoma that has not received systemic therapy before. [0003] Yuanyan Eisai Pharmaceutical Co., Ltd. applied for a patent CN101337933B disclosing crystal forms A, B and C of lenvatinib mesylate for use in preparations. Suzhou Jingyun Pharmaceutical Technology Co., Ltd. applied for a patent US2018015...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/48A61K47/38A61K47/02A61K31/47A61P35/00
CPCA61K9/146A61K9/143A61K9/1652A61K31/47A61P35/00
Inventor 杜阳森骆献丽付晓宁李海峰
Owner LEPU PHARMACEUTICAL CO LTD
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