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Pharmaceutical composition containing nitroxyquinoline prodrug and its preparation method and application

A nitroxoline and prodrug technology is applied to pharmaceutical compositions containing nitroxoline prodrugs and the fields of preparation and application thereof, and achieves the effects of excellent pharmacokinetic properties, excellent dissolution properties and good stability

Active Publication Date: 2021-04-06
JIANGSU YAHONG MEDITECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, in the prior art, there is no preparation for the above-mentioned nitraxine prodrugs

Method used

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  • Pharmaceutical composition containing nitroxyquinoline prodrug and its preparation method and application
  • Pharmaceutical composition containing nitroxyquinoline prodrug and its preparation method and application
  • Pharmaceutical composition containing nitroxyquinoline prodrug and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Made into 500 tablets, each about 160mg.

[0086] Immediate-release tablet preparation method:

[0087] (1) Weigh the API, filler, disintegrant and lubricant of each prescription according to the above table;

[0088] (2) Pass API and other components through a 60-mesh sieve for subsequent use;

[0089] (3) Mix other components in step (2) except the lubricant, add 20-30mL of purified water for wet granulation to prepare soft materials, pass through a 18-mesh sieve for wet granulation, and dry at 60°C until the water content is 1.5-3.5 wt%, use 18-mesh sieve to dry the whole grain, then add lubricant and mix for 10 minutes;

[0090] (4) Use TDP-6 to compress tablets and compress plain tablets;

[0091] (5) BY-300 was used for film coating, the weight gain of the coating was 3%, and the concentration of the coating solution was 15 wt%, to obtain the immediate-release tablet of this embodiment.

Embodiment 2

[0093] Made into 500 tablets, each about 450mg.

[0094] Immediate-release tablet preparation method:

[0095] (1) Weigh the API, filler, binder, disintegrant and lubricant of each prescription according to the above table;

[0096] (2) Preparation of binder (10wt% hydroxypropyl methylcellulose solution): Weigh about 90mL of purified water, slowly add hydroxypropyl methylcellulose, stir while adding, let stand, until completely dissolved ,spare;

[0097] (3) API and other components are passed through a 60-mesh sieve for subsequent use;

[0098] (4) Mix other components in step (3) except the lubricant, add the binder prepared in step (2) and wet granulate to prepare a soft material, pass through a 18-mesh sieve for wet granulation, and dry at 60°C until Moisture content 1.5-3.5wt%, granulate with 18 mesh sieve, then add lubricant and mix for 10 minutes;

[0099] (5) Use ZPS008 to compress the tablet and compress the plain tablet;

[0100] (6) BGB-5F was used for film coa...

Embodiment 3

[0102] Made into 120 tablets, each about 800mg.

[0103] Immediate-release tablet preparation method:

[0104] (1) Weigh the API, filler, disintegrant and lubricant of each prescription according to the above table;

[0105] (2) Pass API and other components through a 60-mesh sieve for subsequent use;

[0106] (3) Mix other components in step (2) except the lubricant, add 25-30mL of purified water for wet granulation to prepare soft materials, pass through a 18-mesh sieve for wet granulation, and dry at 60°C until the water content is 1.5-3.5 wt%, use 18-mesh sieve to dry the whole grain, then add lubricant and mix for 10 minutes;

[0107] (4) Use TDP-6 to compress tablets and compress plain tablets;

[0108] (5) BY-300 was used for film coating, the weight gain of the coating was 3%, and the concentration of the coating solution was 15 wt%, to obtain the immediate-release tablet of this embodiment.

[0109] In addition, according to the same composition, dosage and prepar...

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Abstract

The invention discloses a pharmaceutical composition containing nitroxyquinoline prodrug, a preparation method and application thereof. The pharmaceutical composition comprises the following components in parts by weight: 100 parts of active pharmaceutical ingredients, 22.5-320 parts of fillers, 0-40 parts of disintegrants, 0-95 parts of binders and 2-30 parts of lubricants; Relative to every 100 parts by weight of the active pharmaceutical ingredient, the total amount of the filler, the disintegrant and the binder is 54-345 parts by weight; the active pharmaceutical ingredient is (S)-(5- Nitroquinoline-8-yloxy)methyl 1-isopropionylpyrrolidine-2-carboxylate. The pharmaceutical composition has good stability and dissolution properties, and has good pharmacokinetic characteristics, and can be advantageously used in the preparation and clinical application of medicines.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing nitroxyquinoline prodrug, a preparation method and application thereof. Background technique [0002] Nitroxoline, the English full name is Nitroxoline, and its chemical name is 5-nitro-8-hydroxyquinoline. It was developed as an oral antibiotic drug in the 1960s, mainly for urinary system infections, and has a relatively safe history of use. It was later replaced by the discovery and use of new antibiotics. In recent years, new studies have found that nitroquinoline can simultaneously inhibit methionine aminopeptidase MetAP2 and silent information regulator 2-related enzymes SIRT1 in vascular endothelial cells, exerting a synergistic inhibitory effect on tumor angiogenesis, and at the same time Inhibits the proliferation of tumor cells. Therefore, nitroquinoline has been redeveloped for the treatment of tumors including bladder cancer. [0003] A prodrug is a chemically modified compou...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4709A61K9/28A61K9/16A61P31/00A61P13/02A61P35/00
CPCA61K31/4709A61K9/28A61K9/2059A61K9/1682A61P31/00A61P13/02A61P35/00A61K9/2054A61K9/2018A61K9/2866A61K9/2027A61K9/2013A61K9/2009A61K31/47A61K9/16A61K47/02A61K47/26A61K47/36
Inventor 陈杰申帅吴友斌刘江华郭玉申
Owner JIANGSU YAHONG MEDITECH CO LTD
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