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Pharmaceutical composition of lenvatinib, and applications thereof

A technology of lenvatinib and a composition, applied in the field of pharmaceutical preparations, can solve the problems of insufficient calcium hydrogen phosphate to improve product stability, easy gelation of raw materials, growth of degraded impurities, etc., to ensure bioavailability and rapid dissolution , the effect of stable quality

Inactive Publication Date: 2020-04-24
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have shown that calcium hydrogen phosphate is not enough to improve product stability. By comparing the prescription containing only anhydrous calcium hydrogen phosphate (without adding alkaline preparations) and adding alkaline preparations, the result is that the amount of degraded impurities in the former is significantly greater than that in the latter, and in Significant growth of degraded impurities during storage
[0007] The prior art also discloses a cyclodextrin inclusion compound of lenvatinib. Although the hydrophilicity of cyclodextrin can be used to improve the dissolution rate of the product to a certain extent, the principle is only to increase the solubility of raw materials. And it still fails to solve the problem that the raw material is easy to gel when it meets water and hinders the low dissolution rate

Method used

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  • Pharmaceutical composition of lenvatinib, and applications thereof
  • Pharmaceutical composition of lenvatinib, and applications thereof
  • Pharmaceutical composition of lenvatinib, and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 15

[0096] Preparation prescription (1000 capsules):

[0097]

[0098] The preparation method is as follows:

[0099] Take the prescribed amount of lenvatinib mesylate (D90: 40 μm), sodium bicarbonate (D90: 200 μm), sodium carbonate (D90: 200 μm), lactose, hydroxypropyl cellulose, microcrystalline cellulose KG802, cross-linked polymer Mix evenly in a vinylpyrrolidone mixer, add appropriate amount of ethanol to granulate, dry the granules in an oven below 60°C, control the water content to <3%, add microcrystalline cellulose PH302 and talc powder, mix evenly, and pack into capsules (capsule No. 4).

Embodiment 16

[0101] Preparation prescription (1000 capsules):

[0102]

[0103] The preparation method is as follows:

[0104]Take the prescribed amount of lenvatinib mesylate (D90: 40 μm), sodium bicarbonate (D90: 200 μm), sodium carbonate (D90: 200 μm), starch, povidone k30, and sodium starch glycolate and mix them evenly in a mixer, Add appropriate amount of ethanol to granulate, dry the granules in an oven below 60°C, control the water content to <3%, add microcrystalline cellulose PH302 and magnesium stearate, mix evenly, and pack into capsules (capsule No. 4).

Embodiment 17

[0106] Preparation prescription (1000 capsules):

[0107]

[0108]

[0109] The preparation method is as follows:

[0110] Take the prescribed amount of lenvatinib mesylate (D90: 40 μm), sodium bicarbonate (D90: 200 μm), sodium carbonate (D90: 200 μm), starch, povidone k30, and sodium starch glycolate and mix them evenly in a mixer, Add appropriate amount of ethanol to granulate, dry the granules in an oven below 60°C, control the water content to <3%, add microcrystalline cellulose PH302 and magnesium stearate, mix evenly, and pack into capsules (capsule No. 4).

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Abstract

The invention provides a pharmaceutical composition, which contains lenvatinib or a pharmaceutically acceptable salt thereof, sodium carbonate and sodium bicarbonate. According to the invention, the pharmaceutical composition solves the problem of difficulty in dissolution of lenvatinib, has excellent dissolution behavior, improves the bioavailability of the drug, has excellent stability, and canensure clinical medication safety.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing lenvatinib, pharmaceutical preparations and uses thereof. More specifically, it relates to a pharmaceutical composition that improves the dissolution rate and stability of lenvatinib or a pharmaceutically acceptable salt thereof. Background technique [0002] Lenvatinib is a multi-receptor tyrosine kinase (RTK) inhibitor developed by Japan's Eisai Company. It was approved for marketing in the United States, Japan, and Europe in 2015 for thyroid tumor indications; in the first half of 2017 In Japan, the United States, and Europe, registration declarations have been made for liver cancer indications. Its chemical name is 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide, and its structural formula is as follows: [0003] The lenvatinib compound has poor solubility and is slightly soluble in wat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61K47/04A61P35/00
CPCA61K31/47A61K47/02A61P35/00
Inventor 徐飞刘文友景文娜蒙霏霏王小雪王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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