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Capsules containing naphthyridine compound and preparation method thereof

A ketone compound and compound technology are applied in the field of capsules containing naphthyridine compounds and the field of preparation thereof, achieving the effects of large drug loading, good fluidity and improving taking compliance

Pending Publication Date: 2021-11-12
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no reports about the preparation products of this class of compounds at present

Method used

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  • Capsules containing naphthyridine compound and preparation method thereof
  • Capsules containing naphthyridine compound and preparation method thereof
  • Capsules containing naphthyridine compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A capsule containing naphthyridine compounds, the contents of which include in parts by weight: 5-((3-fluoro-4-((7-(2-hydroxyl-2-methylpropyl) quinoline -4-yl)oxo)phenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-one 82 parts, first diluent (calcium sulfate) 54 parts , 43 parts of the second diluent (lactose and mannitol mass ratio is the mixture of 1.2:1), 4 parts of binder, 6 parts of polyvinyl alcohol hydrogenated castor oil and 2.5 parts of lubricant, wherein the binder is a weight ratio of 1:6 polyvinylpyrrolidone K30 and polyethylene glycol 6000, the lubricant is magnesium stearate, calcium stearate and micropowder silica gel in a weight ratio of 4:0.8:2.

[0030] Its preparation method comprises the following steps:

[0031] Step a, weigh 5-((3-fluoro-4-((7-(2-hydroxyl-2-methylpropyl)quinolin-4-yl)oxo) through a 60 mesh sieve in parts by weight Phenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-one, adding corresponding parts of the first diluent and...

Embodiment 2

[0037] A capsule containing naphthyridine compounds, the contents of which include in parts by weight: 5-((3-fluoro-4-((7-(2-hydroxyl-2-methylpropyl) quinoline -4-yl)oxo)phenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-one 88 parts, the first diluent (calcium sulfate and hydrogen phosphate Calcium mass ratio is 1:1.5 mixture) 56 parts, the second diluent (lactose) 43 parts, binder 5 parts, sodium lauryl sulfate 4.5 parts and lubricant 2 parts, wherein the binder is the weight ratio The ratio of polyvinylpyrrolidone K30 and polyethylene glycol 6000 is 1:7.5, and the lubricant is magnesium stearate, calcium stearate and micronized silica gel at a weight ratio of 6:0.6:1.5.

[0038] Its preparation method comprises the following steps:

[0039] Step a, weigh 5-((3-fluoro-4-((7-(2-hydroxyl-2-methylpropyl)quinolin-4-yl)oxo) through a 60 mesh sieve in parts by weight Phenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-one, adding corresponding parts of the first diluent...

Embodiment 3

[0045] A capsule containing naphthyridine compounds, the contents of which include in parts by weight: 5-((3-fluoro-4-((7-(2-hydroxyl-2-methylpropyl) quinoline -4-yl)oxo)phenyl)amino)-3-(4-fluorophenyl)-1,6-naphthyridin-4(1H)-one 86 parts, first diluent (calcium carbonate) 54 parts , 44 parts of the second diluent (a mixture of mannitol and sorbitol at a mass ratio of 1:1.5), 4.8 parts of an adhesive, 5 parts of a mixture of polyvinyl alcohol hydrogenated castor oil and Tween 80 at a mass ratio of 2:1.5 and lubricating 2.2 parts of agent, wherein the binder is polyvinylpyrrolidone K30 and polyethylene glycol 6000 with a weight ratio of 1:7, and the lubricant is magnesium stearate, calcium stearate and micropowdered silica gel with a weight ratio of 5:0.8:1.5 .

[0046] Its preparation method comprises the following steps:

[0047]Step a, weigh 5-((3-fluoro-4-((7-(2-hydroxyl-2-methylpropyl)quinolin-4-yl)oxo) through a 60 mesh sieve in parts by weight Phenyl)amino)-3-(4-fluor...

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PUM

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses capsules containing a naphthyridine compound and a preparation method thereof. The content of the capsules comprises components in parts by weight: 80-90 parts of 1, 6-naphthyridine-1 (2H)-ketone compound, 50-60 parts of first diluent, 40-50 parts of second diluent, 4-6 parts of adhesive and 4-6 parts of solubilizer; the first diluent comprises at least one of calcium sulfate, calcium hydrophosphate or calcium carbonate; and the second diluent comprises at least one of lactose, mannitol or sorbitol. The sustained-release capsules are reasonable in formula, the prepared capsules are good in dissolution rate and high in bioavailability, meanwhile, the preparation process is simple, the production efficiency is high, few manual operations are adopted, and the sustained-release capsules are suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a capsule containing naphthyridine compounds and a preparation method thereof. Background technique [0002] Naphthyridine compounds are an important class of natural products and drug building blocks, which have a wide range of biomedical applications and can be used to treat a variety of diseases associated with abnormal kinase activity, such as tumors, psoriasis, liver cirrhosis, diabetes, ophthalmic diseases, rheumatoid Arthritis and many other diseases. In view of the good development and application prospects of naphthyridine compounds, the synthesis and research of new derivatives are constantly emerging. Patent CN201610880102.6 develops new naphthyridine compounds, including 1,6-naphthyridine-1(2H)-one compounds shown in structural formula I or pharmaceutically acceptable salts thereof, because the structure has excellent Kinase inhibitory activity a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/02A61K47/26A61K47/20A61K47/44A61K47/22A61K47/12A61K47/04A61K31/4709A61P35/00A61P19/00A61P9/10A61P11/00
CPCA61K9/485A61K9/4858A61K9/4866A61K31/4709A61P35/00A61P19/00A61P9/10A61P11/00
Inventor 孙立杰于洲李彪刘新戎艳艳李莎
Owner SHIJIAZHUANG NO 4 PHARMA