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Quinoline derivative-containing pharmaceutical composition

a technology of pharmaceutical compositions and derivatives, which is applied in the direction of drug compositions, inorganic non-active ingredients, biocides, etc., can solve the problems of delayed dissolution of quinoline derivatives (i) and (i) of pharmaceutical compositions that are active ingredients, and achieve excellent absorption into the living body

Inactive Publication Date: 2012-03-29
EISIA R&D MANAGEMENT CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012]The pharmaceutical composition of the present invention is excellent in dissolution of the quinoline derivative (I), which is a principal agent, and is also excellent in absorption into a living body. The pharmaceutical composition is also a pharmaceutical composition that is maintained even after long term storage.

Problems solved by technology

However, the quinoline derivative (I) has been found to degrade under humidifying and warming storage conditions when formulated into a pharmaceutical composition.
In addition, when the pharmaceutical composition absorbs moisture, dissolution of the quinoline derivative (I) from the pharmaceutical composition that is an active ingredient may delay because of gelation on the surface of the composition.

Method used

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  • Quinoline derivative-containing pharmaceutical composition
  • Quinoline derivative-containing pharmaceutical composition
  • Quinoline derivative-containing pharmaceutical composition

Examples

Experimental program
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examples

[0044]The present invention will be described in more detail below with reference to Examples, but is not limited to the Examples.

examples 1 to 3

[0045]Wet granulation was performed with purified water as a solvent using a high-shear granulator (apparatus name: FM-VG-10, manufactured by Powrex Corporation) with the C form crystal of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate (hereinafter referred to as compound A), D-mannitol (trade name: Mannitol, Merck), precipitated calcium carbonate (trade name: Whiton F, Shiraishi Calcium), hydroxypropylcellulose (HPC-L, Nippon Soda), low-substituted hydroxypropylcellulose (trade name: L-HPC (LH-21), Shin-Etsu Chemical) and microcrystalline cellulose (trade name: Ceolus PH-101, Asahi Kasei Chemicals) according to the formulation proportions in Table 1. The granules of which a moisture content was reduced to be less than 2% by further drying were sized using a screen mill (apparatus name: Power Mill P-04S, manufactured by Showa Giken KK) so that their granule diameters were less than 1 mm. Then, microcrystalline cellulose (trade...

examples 4 to 9

, Comparative Examples 1 to 2

[0046]The compound A, precipitated calcium carbonate, low-substituted hydroxypropylcellulose, D-mannitol and talc were thoroughly mixed using a mortar and a pestle according to the formulation proportions in Table 2 and Table 3. Hard capsules size #3 were filled with 100 mg of the resultant mixtures to prepare capsules in Examples 4 to 9. Capsules in Comparative Examples 1 to 2, which contained no precipitated calcium carbonate, were also prepared by the same method.

TABLE 2Com.Ex. 1Ex. 4Ex. 5Ex. 6Compound A5555Precipitated calcium carbonate051020Low-substituted30252010hydroxypropylcelluloseD-Mannitol62626262Talc3333Total100100100100Unit: weight %

TABLE 3Com.Ex. 2Ex. 7Ex. 8Ex. 9Compound A20202020Precipitated calcium carbonate051020Low-substituted30252010hydroxypropylcelluloseD-Mannitol47474747Talc3333Total100100100100Unit: weight %

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Abstract

A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof; and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor:wherein, R1 is a hydrogen atom, a C1-6 alkyl group or a C3-8 cycloalkyl group; and R2 is a hydrogen atom or a methoxy group.

Description

TECHNICAL FIELD[0001]The present invention relates to a pharmaceutical composition comprising a quinoline derivative, useful as a medicament. More specifically, the present invention relates to a pharmaceutical composition improved in dissolution of a quinoline derivative or a pharmaceutically acceptable salt thereof or a solvate thereof.BACKGROUND ART[0002]A quinoline derivative represented by the formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof (hereinafter referred to as quinoline derivative (I)) has been known to have a potent angiogenesis inhibitory effect (Patent Literature 1) and a c-Kit kinase inhibitory effect (Patent Literature 2) and to be useful as a preventive or therapeutic agent against various tumors such as thyroid cancer, lung cancer, melanoma and pancreatic cancer, and as an metastatic inhibitor against these tumors:wherein, R1 is a hydrogen atom, a C1-6 alkyl group or a C3-8 cycloalkyl group; and R2 is a hydrogen atom or a methoxy gr...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61P35/00
CPCA61K9/1611A61K9/1652A61K9/485A61K47/02A61K31/47C07D215/48A61K9/4866A61P35/00A61P35/04A61P43/00A61K47/36
Inventor BANDO, MASASHI
Owner EISIA R&D MANAGEMENT CO LTD
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