Lenvatinibsolid dispersion and preparation method thereof and preparation

A technology of solid dispersion and lenvatinib, which is applied in the direction of active ingredients of heterocyclic compounds, drug combination, powder delivery, etc., can solve the problem of low bioavailability of lenvatinib, and improve bioavailability and production cost Low, increase the effect of dissolution rate and dissolution rate

Inactive Publication Date: 2018-12-21
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of this, the present invention aims to propose a solid dispersion of lenvatinib to solve the problem of low bioavailability of existing lenvatinib

Method used

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  • Lenvatinibsolid dispersion and preparation method thereof and preparation
  • Lenvatinibsolid dispersion and preparation method thereof and preparation
  • Lenvatinibsolid dispersion and preparation method thereof and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A solid dispersion of lenvatinib, which comprises lenvatinib and a water-soluble carrier material; the mass ratio of lenvatinib and the water-soluble carrier material is 10:1-1:10.

[0036] The lenvatinib solid dispersion of this embodiment uses water-soluble carrier materials as the carrier of lenvatinib, which can convert needle-like crystal lenvatinib into amorphous lenvatinib, and is highly dispersed in water-soluble The carrier material greatly improves the dissolution rate and dissolution rate of lenvatinib, thereby improving the bioavailability of lenvatinib.

[0037] In this embodiment, the water-soluble carrier material is preferably polyethylene glycol 3000, polyethylene glycol 4000, polyethylene glycol 6000, polyethylene glycol 8000, povidone K15, povidone K25, povidone K30 , povidone K60, povidone K90, copovidone, stearic acid, sodium dodecylbenzene sulfonate, quaternary ammonium compound, lecithin, amino acid type, betaine type, fatty acid glyceride, fatty ...

Embodiment 2

[0047] A solid dispersion of lenvatinib, which is specifically prepared through the following steps:

[0048] 1) Add 60mg of lenvatinib and 40mg of copovidone into 20ml of methanol, heat up to 55°C and stir for 30min to obtain reaction solution A;

[0049] 2) distilling off the methanol in the reaction solution A to obtain the initial lenvatinib solid dispersion;

[0050] 3) The initial lenvatinib solid dispersion is vacuum-dried, wherein the drying temperature is 30°C, the drying time is 12h, and ground and passed through an 80-mesh sieve to obtain a white powdery lenvatinib solid that meets the particle size requirements Dispersions.

Embodiment 3

[0052] A solid dispersion of lenvatinib, which is specifically prepared through the following steps:

[0053] 1) Add 50mg of lenvatinib and 50mg of copovidone into 20ml of methanol, heat up to 55°C and stir for 30min to obtain reaction solution A;

[0054] 2) distilling off the methanol in the reaction solution A to obtain the initial lenvatinib solid dispersion;

[0055] 3) The initial lenvatinib solid dispersion is vacuum-dried, wherein the drying temperature is 30°C, the drying time is 12h, and ground and passed through an 80-mesh sieve to obtain a white powdery lenvatinib solid that meets the particle size requirements Dispersions.

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Abstract

The invention provides a lenvatinibsolid dispersion and a preparation method thereof and a preparation. The lenvatinibsolid dispersion comprises lenvatinib and a water soluble carrier material based on the mass ratio of (10: 1)-(1: 10). According to the lenvatinibsolid dispersion, the water soluble carrier material is used as a carrier of lenvatinib and is capable of converting needle bar shaped crystalized lenvatinib into amorphous state lenvatinib, and the lenvatinib is highly dispersed into the water soluble carrier material. Therefore, the lenvatinib dissolving out speed and the dissolution rate can be greatly increased, and as a result, the bioavailability of the lenvatinib is improved.

Description

technical field [0001] The invention relates to the technical field of solid dispersions, in particular to a solid dispersion of lenvatinib and a preparation method and preparation thereof. Background technique [0002] An oral multi-receptor tyrosine kinase (RTK) inhibitor Lenvatinib (Lenvatinib) is a white to light brown powder with a molecular formula of C 21 h 19 ClN 4 o 4 , with a relative molecular mass of 426.85, a melting point of 217-219°C, and a chemical name of 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxyquinoline-6-methyl Amide, its chemical structure is: [0003] [0004] As an oral tyrosine kinase inhibitor, lenvatinib was developed by Eisai Corporation of Japan. It was approved for marketing by the FDA in February 2015 through various fast-track pathways such as priority review, accelerated approval, and orphan drug qualification. It is suitable for the treatment of patients with locally recurrent or metastatic, progressive, radioact...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/47A61P35/00
CPCA61K9/146A61K31/47A61P35/00
Inventor 胡学雷武磊冯菊红
Owner WUHAN INSTITUTE OF TECHNOLOGY
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