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Lervatinib-gallic acid eutectic crystal form and application thereof

A technology of crystal form and compound, applied in the field of lenvatinib-gallic acid co-crystal form, can solve the problem of less research on lenvatinib co-crystal

Pending Publication Date: 2020-08-25
NOVAGENESIS THERAPEUTIX SUZHOU LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are few studies on lenvatinib co-crystal, so lenvatinib co-crystal still needs to be developed

Method used

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  • Lervatinib-gallic acid eutectic crystal form and application thereof
  • Lervatinib-gallic acid eutectic crystal form and application thereof
  • Lervatinib-gallic acid eutectic crystal form and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] LVB-GA·H 2 O crystal form I preparation method: 500mg lenvatinib, 220mg gallic acid monohydrate (molar ratio 1:1), add 8ml methanol:dichloromethane (1:1), stir for 48 hours, filter, and dry at room temperature.

[0088] LVB-GA·H 2 Preparation method of O crystal form II: take the above-prepared LVB-GA·H 2 O crystal form I was stirred under the condition of appropriate amount of methanol / dichloro / water (5 / 5 / 0.5) for 48 hours to obtain crystal form II.

[0089] Characterization of co-crystals by PXRD

[0090] The prepared co-crystal and bulk drug were analyzed by powder X-ray (PXRD) as follows: Figure 5 As shown, it can be seen from the results that the newly prepared LVB-GA·H 2 O co-crystal form I and form II with raw materials lenvatinib (LVB), gallic acid monohydrate (GA·H 2 O) presents a distinctly different diffraction pattern, indicating that a new co-crystal was successfully prepared.

[0091] Characterization of co-crystals by TGA and DSC

[0092] Thermogr...

Embodiment 2

[0100] LVB-GA·H 2 Preliminary Stability Test of O Eutectic Form I

[0101] The prepared LVB-GA·H 2 O eutectic crystal form I was placed at 40 ° C, 10 days under the conditions of 75% RH accelerated stability determination, from DSC, TGA and PXRD (see Figure 10 ) showed no significant change in the characterization results, indicating that LVB-GA·H 2 O eutectic form I has good initial stability.

[0102] LVB-GA·H 2 O cocrystal form I and form II and the inherent dissolution test results of LVB mesylate salt already on the market

[0103] Experiments were carried out with an inherent dissolution device (Fucus Analytical Instrument Co., Ltd., China). LVB-GA·H 2 O eutectic crystal form I, crystal form II or LVB methanesulfonic acid and water-soluble starch are physically mixed in a weight ratio of 7 / 3, and then compressed at 300kgf for 2 minutes to prepare tablets for dissolution. Intrinsic dissolution conditions: 500ml 0.1M HCl (0.1% Tween 80) dissolution medium, rotating...

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Abstract

The invention discloses a lenvatinib-gallic acid eutectic crystal form and application thereof. The eutectic crystal is composed of a compound as shown in a formula (I) and a compound as shown in a formula (II). The eutectic crystal can be used for inhibiting vascular endothelial growth factor receptors, fibroblast growth factor receptors, platelet-derived growth factor receptors and proto-oncogenes, and can be used for preventing and / or treating thyroid cancer or liver cancer.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular, the invention relates to a lenvatinib-gallic acid co-crystal form and an application thereof. Background technique [0002] Lenvatinib is an anticancer drug developed and marketed by Japan's Eisai Company, which is approved for the treatment of thyroid cancer and liver cancer. Lenvatinib is a multi-enzyme inhibitor that can inhibit three vascular endothelial growth factor receptors (VEGFR1,2,3), fibroblast growth factor receptors (FGFR 1,2,3,4), platelet-derived growth factor receptor (PDGFR) and proto-oncogene. [0003] The co-crystal in pharmacy refers to the crystal formed by the combination of active pharmaceutical ingredient (active pharmaceutical ingredient, API) and cocrystal former (cocrystal former, CCF) under the action of hydrogen bond or other non-covalent bonds, in which API The pure states of CCF and CCF are solid at room temperature, and there is a fixed stoichiometric r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C51/43C07C65/03C07D215/22A61P35/00A61K31/47
CPCC07C65/03C07D215/22A61P35/00C07B2200/13
Inventor 钱锋刘程宇
Owner NOVAGENESIS THERAPEUTIX SUZHOU LTD
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