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Solid preparation containing [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid

A solid preparation, phenoxy technology, applied in the field of solid preparations containing [-amino]-acetic acid, can solve problems such as stability, inability to guarantee preparations, and inability to guarantee in vivo bioavailability

Inactive Publication Date: 2021-04-06
JIANGSU WANBANG BIOPHARMLS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] After research, the inventors of the present invention found that in the preparation process of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, directly use physical Form A, which is considered to be the most stable in stability tests, cannot be guaranteed to obtain a formulation that stabilizes drug dissolution in vitro, which may mean that stable bioavailability in vivo cannot be guaranteed

Method used

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  • Solid preparation containing [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid
  • Solid preparation containing [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid
  • Solid preparation containing [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～ Embodiment 4

[0072] In the wet granulator, put into the A crystal of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid (roxadustat), excipient The agent was mixed at a stirring speed of 400rpm and a shearing speed of 500rpm. Then, at a stirring speed of 300 rpm, a soft material made of 20% (W / W) binder povidone aqueous solution was slowly added at a uniform speed under a shear of 700 rpm, and dried at 60° C. to obtain a soft material containing about 13% by weight of the main ingredient particles. Pass the prepared granules through a vibrating sieve machine to remove particles above 710 μm to obtain sieved granules. The disintegrant and lubricant were blended into 143 g of sieved granules to obtain the total blended granules. The powder for filling capsules is filled into capsules with a capsule filling machine, and the specific raw material ratio is shown in Table 1.

[0073] Table 1 Embodiment 1~Example 4 prescription ratio

[0074]

[0075] The particle s...

Embodiment 5

[0097] For the preparations prepared in Examples 1 to 4, they were stored for 6 months at 40°C / RH75%, using a paddle method 75rpm dissolution device, and 0.05M phosphate pH6.0 buffer as the dissolution medium for in vitro dissolution studies , the dissolution results are shown in Table 8, and it was confirmed that there was no significant change in the dissolution rate of the preparation 60 minutes after manufacture and after storage.

[0098] Table 8 Dissolution research results before and after storage of Examples 1 to 4

[0099]

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Abstract

The invention discloses a solid preparation containing [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, and the [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]- acetic acid in the solid preparation is a single crystal form with a particle size range of 3-65 [mu] m. The solid preparation also comprises one or more hydrophilic polymer materials as adhesives. The solid preparation disclosed by the invention is high in dissolution rate and bioavailability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a solid preparation containing [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid for the purpose of oral administration . Background technique [0002] As described in the specification CN201310302481.7, roxadustat is a hypoxia-inducible factor prolyl hydroxylase (HIF-pH) inhibitor, which has the effect of increasing erythropoietin that stimulates erythropoiesis (erythropoiesis) The role of endogenous production. The compounds are useful in the treatment and prevention of disorders associated with HIF, including anemia, ischemia and hypoxia, among others. It is highly anticipated as a drug for the treatment of anemia. [0003] In addition, CN201310302481.7 describes [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid roxadustat free acid (type A-D ) crystal form and preparation method and characterization of the amorph...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/28A61K31/472A61P7/06A61P9/10
CPCA61K9/2018A61K9/2027A61K9/2054A61K9/28A61K9/4858A61K9/4866A61K31/472A61P7/06A61P9/10
Inventor 王飞曲静怡王程程王克艳
Owner JIANGSU WANBANG BIOPHARMLS
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