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Medicinal composition containing roxadustat solid dispersion and preparation method of medicinal composition

A technology of solid dispersion and roxadustat, which can be applied to medical preparations containing active ingredients, medical preparations without active ingredients, and drug combinations, etc. The problems of poor stability and undisclosed preparation process can achieve the effects of good photostability, increased solubility, and improved in vitro dissolution rate and bioavailability.

Pending Publication Date: 2021-12-10
南京科默生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent CN 105377242A discloses that the excipients of roxadustat capsules include: lactose monohydrate, microcrystalline cellulose, povidone, croscarmellose sodium and magnesium stearate, but the preparation process is not disclosed
Generally, the method of micronization of the raw material drug is adopted, but the fluidity of the micronized roxadustat is poor, the electrostatic effect is strong, the drug powder aggregates into agglomerates, and the mixing is uneven, resulting in uneven content uniformity of the preparation and affecting the efficacy of the drug

Method used

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  • Medicinal composition containing roxadustat solid dispersion and preparation method of medicinal composition
  • Medicinal composition containing roxadustat solid dispersion and preparation method of medicinal composition
  • Medicinal composition containing roxadustat solid dispersion and preparation method of medicinal composition

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Experimental program
Comparison scheme
Effect test

Embodiment 1-2

[0033] Table 1 Example 1-2 prescription list

[0034]

[0035] Embodiment 1-2 preparation method

[0036] ① According to the above prescription, ultrasonically dissolve the prescribed amount of roxadustat and povidone in 100g of 50% ethanol solution at the same time as the drug-containing carrier solution. The drug-containing carrier solution is a light yellow transparent liquid without lumps and bubble;

[0037] ② Take the prescription amount of croscarmellose sodium and microcrystalline cellulose and mix them in a fluidized bed for 5 minutes;

[0038] ③Continue to spray the drug-containing carrier solution in step 1, and obtain a solid dispersion containing roxadustat through one-step granulation, and dry (moisture content 1-3%);

[0039] ④Sizing and blending: 30-mesh sizing, then put the dry granules in a three-dimensional mixer, add magnesium stearate for total blending, set the parameters at 12rpm, and mix for 5 minutes;

[0040] ⑤Filling: Fill the total mixed granu...

Embodiment 3-4

[0042] Table 2 Example 3-4 prescription list

[0043]

[0044] Embodiment 3-4 preparation method

[0045] ① According to the above prescription, ultrasonically dissolve the prescribed amount of roxadustat and povidone in 100g of 50% ethanol solution at the same time as the drug-containing carrier solution. The drug-containing carrier solution is a light yellow transparent liquid without lumps and bubble;

[0046] ② Take the prescribed amount of croscarmellose sodium, microcrystalline cellulose and lactose and mix them in a fluidized bed for 5 minutes;

[0047] ③Continue to spray the drug-containing carrier solution in step 1, and obtain a solid dispersion containing roxadustat through one-step granulation, and dry (moisture content 1-3%);

[0048] ④Sizing and blending: 30-mesh sizing, then put the dry granules in a three-dimensional mixer, add magnesium stearate for total blending, set the parameters at 12rpm, and mix for 5 minutes;

[0049] ⑤Filling: Fill the total mixe...

Embodiment 5-6

[0051] Table 3 Example 5-6 prescription list

[0052]

[0053] Embodiment 5-6 preparation method

[0054] ① According to the above prescription, ultrasonically dissolve the prescribed amount of roxadustat and hypromellose in 100 g of 50% ethanol solution at the same time as the drug-containing carrier solution. The drug-containing carrier solution is a light yellow transparent liquid without lumps blocks and bubbles;

[0055] ②Take the prescribed amount of croscarmellose sodium and lactose in a fluidized bed and mix for 5 minutes;

[0056] ③Continue to spray the drug-containing carrier solution in step 1, and obtain a solid dispersion containing roxadustat through one-step granulation, and dry (moisture content 1-3%);

[0057] ④Sizing and blending: 30-mesh sizing, then put the dry granules in a three-dimensional mixer, add magnesium stearate for total blending, set the parameters at 12rpm, and mix for 5 minutes;

[0058] ⑤Filling: Fill the total mixed granules to obtain ro...

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Abstract

The invention relates to the field of medicinal preparations, and particularly discloses a medicinal composition containing a roxadustat solid dispersion and a preparation method of the medicinal composition. The preparation method comprises the steps of firstly, preparing a roxadustat carrier solution containing roxadustat from a medicinal carrier material with a solubilizing effect and the roxadustat through an ethanol solution with a certain concentration; and preparing the medicinal preparation containing the roxadustat solid dispersion from the roxadustat solid dispersion and other pharmaceutically acceptable auxiliary materials through the steps of one-step granulation, size stabilization and the like. The medicinal composition containing the roxadustat solid dispersion has good dissolution performance, the preparation process is simple and easy to operate, energy is saved, the input cost is reduced, raw materials do not need to be micronized, the solubility of the roxadustat medicine is improved, the content uniformity is improved, the in-vitro dissolution rate and the bioavailability are further improved, besides, the one-step granulation process avoids material exposure, and the preparation has good light stability and is convenient for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid dispersion of roxadustat, a pharmaceutical composition containing the dispersion and a preparation method thereof. Background technique [0002] Roxadustat belongs to 4-hydroxyisoquinoline derivatives, small molecule HIF-PH enzyme inhibitors; the chemical name is [[(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3 -)carbonyl]-amino]-acetic acid; the structural formula is C 19 H1 6 N 2 o 5 ; Relative molecular mass 352.3407; The structure of roxadustat is as follows: [0003] [0004] Roxadustat is the world's first small molecule hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI) drug developed for the treatment of renal anemia. The physiological role of hypoxia-inducible factor (HIF) not only increases the expression of erythropoietin, but also increases the expression of erythropoietin receptor and proteins that promote iron absorpt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/32A61K47/38A61K47/26A61K9/48A61K31/472A61P7/06
CPCA61K9/1682A61K9/1635A61K9/1652A61K9/1623A61K31/472A61P7/06
Inventor 苏梅汪丹钱义云张慧婷代孔恩张孝清
Owner 南京科默生物医药有限公司
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