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Medicinal composition containing lenvatinib, and preparation method thereof

A technology of lenvatinib and composition, which is applied in the field of pharmaceutical composition containing lenvatinib and its preparation, and can solve the problems of slow release and low dissolution

Active Publication Date: 2017-04-05
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN200580026468.7 discloses a lenvatinib tablet, comprising a stabilizer, such as magnesium oxide, calcium oxide, sodium carbonate, or sodium bicarbonate, etc.; and a gelation preventing agent, such as light silicon dioxide, silicic acid Calcium, magnesium silicate, or magnesium aluminosilicate, etc., solve the problem of low dissolution caused by the dissolution and gelation of raw materials, but there are certain problems in the stability of the composition
[0007] CN201080030508.6 discloses a lenvatinib capsule, containing magnesium carbonate or calcium carbonate, using wet granulation to prepare granules, controlling the water content below 2%, using hypromellose to prepare capsules, and the stability of the obtained composition The performance was improved, but the release test found that the capsules released slowly in the first 15 minutes

Method used

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  • Medicinal composition containing lenvatinib, and preparation method thereof
  • Medicinal composition containing lenvatinib, and preparation method thereof
  • Medicinal composition containing lenvatinib, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The influence of embodiment 1 anhydrous calcium hydrogen phosphate on the dissolution rate of lenvatinib mesylate capsule

[0028] This embodiment investigates and illustrates the influence of anhydrous calcium hydrogen phosphate on the dissolution rate of lenvatinib mesylate capsules.

[0029] Lenvatinib mesylate capsules were prepared according to the prescription shown in Table 1 below, and the dissolution rate was measured, and the results are shown in Table 2.

[0030] Preparation method: Put the prescribed amount of lenvatinib mesylate, anhydrous calcium hydrogen phosphate, filler, and disintegrating agent into a fluidized bed and mix evenly, use 95% ethanol for granulation, and dry until the water content is less than 2%. Discharge, granulate the dried granules, add lubricant and mix evenly, and then fill into capsules.

[0031] Table 1 Components and dosages of prescriptions 1 to 6

[0032]

[0033] Table 2 Dissolution test results of prescriptions 1 to 6 ...

Embodiment 2

[0036] Embodiment 2 Anhydrous calcium hydrogen phosphate particle size is on the influence of capsule dissolution rate and uniformity

[0037] This example examines and illustrates the influence of anhydrous calcium hydrogen phosphate particle size on capsule dissolution rate and particle uniformity.

[0038] Lenvatinib mesylate capsules were prepared according to the prescription shown in Table 3 below. Wherein the particle diameter of anhydrous calcium hydrogen phosphate in prescription 7,10 is about 80 orders (equivalent to D 90 ≤180μm), the particle size of anhydrous calcium hydrogen phosphate in prescriptions 8, 9, 11, and 12 is about 200 mesh (equivalent to D 90 ≤75μm).

[0039] Preparation method one (prescriptions 7, 8, 10, 11): put lenvatinib mesylate, anhydrous calcium hydrogen phosphate, filler, and disintegrant into the fluidized bed and mix evenly with 5% poly The vitamin K30 ethanol solution is granulated, dried until the water content is less than 2%, and t...

Embodiment 3

[0049] The preparation of embodiment 3 lenvatinib mesylate capsules

[0050] Prescription 13:

[0051]

[0052] Preparation method: similar to Example 1. Anhydrous calcium hydrogen phosphate is micronized, and the particle size is about 400 mesh.

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Abstract

The invention provides a medicinal composition containing lenvatinib. The medicinal composition comprises, by weight, 1-20% of lenvatinib mesylate, 20-60% of anhydrous calcium hydrogen phosphate, 10-55% of a filler, 5-35% of a disintegrating agent, 0-10% of an adhesive and 0.5-5% of a lubricant. Preferably, the particle size of the anhydrous calcium hydrogen phosphate is 200-600 meshes, or the D90 is about 20-75 [mu]m. The medicinal composition has good stability, has a dissolubility reaching 90% or above in 15 min, has effectively improved bioavailability, is easy to prepare, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing lenvatinib and a preparation method thereof. Background technique [0002] Lenvatinib, Chinese name: lenvatinib, lanvatinib, chemical name 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinoline Formamide, structure as shown in formula I, [0003] [0004] Lenvatinib is a multi-receptor tyrosine kinase (RTK) inhibitor developed by Japan's Eisai Co. Kinase activity of endothelial growth factor receptors VEGFR1 (FLT1), VEGFR2 (KDR) and VEGFR3 (FLT4); also inhibits fibroblast growth factor receptors FGFR1, 2, 3, and 4, platelet-derived growth factor receptor α ( PDGFRα), KIT and RET. Lenvatinib was approved by the US FAD in February 2015 for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer. [0005] The preparations of l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61K47/02A61P35/00
Inventor 赵俊陈祥峰杜有国陈健
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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