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Riociguat oral solid preparation and preparing method thereof

A technology of solid preparation, riociguat, which is applied in the field of pharmaceutical preparations, can solve the problems of slow dissolution rate, low dissolution rate in vitro, poor solubility of riociguat, etc., and achieve the effect of simple composition and simple preparation process

Inactive Publication Date: 2016-05-25
郑州大明药物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Riociguat has extremely poor solubility, slow dissolution rate, and low in vitro dissolution rate, which is unfavorable for drug absorption

Method used

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  • Riociguat oral solid preparation and preparing method thereof
  • Riociguat oral solid preparation and preparing method thereof
  • Riociguat oral solid preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 prescription and preparation technology

[0031]

[0032] Preparation.

[0033] 1) Weigh the main drug and various auxiliary materials required for the prescription amount.

[0034] 2) Weigh 50% of the prescribed amount of disintegrant, grind it together with the main ingredient and filler for 30 minutes, and pass through a 100-mesh sieve.

[0035] 3) Prepare the binder into a 3~5% solution, add it to the mixture obtained in step 2), stir well and granulate with a 24-mesh sieve. The particles are dried at 60~70℃ for 1~3h.

[0036] 4) Mix the granules prepared in step 3) with 50% of the prescription amount of disintegrant and lubricant to obtain the total mixture.

[0037] 5) Tablet compression: according to conventional methods, the obtained total mixture is compressed into tablets to obtain tablet cores.

[0038] 6) Coating the tablet core obtained in step 5) to obtain a film-coated tablet.

Embodiment 2

[0039] Embodiment 2 prescription and preparation technology

[0040] .

Embodiment 3

[0041] Embodiment 3 prescription and preparation technology

[0042]

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Abstract

The invention provides a solid pharmaceutical preparation containing Riociguat, and in parts by weight, 1mg of Riociguat oral solid preparation is prepared from 1mg of Riociguat, 60-80mg of filler, 2-8mg of binder, 2-8mg of disintegrating agent and 0.5-1.5mg of lubricating agent. The solid pharmaceutical preparation adopts a solid dispersion technology, by mixing and grinding main medicine and the filler, solubleness of the main medicine is improved, a dissolving effect is improved, the dissolving speed of the preparation is ensured, the content uniformity is high, and the bioavailability is high. The preparing process is simple in production process, low in cost and suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a solid pharmaceutical preparation containing riociguat and a preparation method thereof. Background technique [0002] Riociguat, its chemical name is: N-[4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl] -5-pyrimidinyl]-N-methylcarbamate methyl ester, the specific structure is as formula (I): [0003] . [0004] Riociguat can stimulate guanylate cyclase (sGC), and sGC regulates the vasodilation of multiple blood vessels by acting on cGMP, and can be used for the treatment of chronic thromboembolic pulmonary hypertension and pulmonary hypertension. Riociguat oral tablets were approved by the FDA in October 2013. The trade name is ADEMPAS, and the product specifications are 0.5mg, 1mg, 1.5mg, 2mg, and 2.5mg. [0005] Riociguat has extremely poor solubility, slow dissolution rate, and low dissolution rate in vitro, which is unfavorable for drug absor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/506A61K47/38A61P7/02A61P9/12A61P11/00
CPCA61K9/2054A61K9/2059A61K9/2813A61K9/2866A61K31/506
Inventor 毛影刘志庆李沁沁朱赞梅王翠侠苏国娜张佳美
Owner 郑州大明药物科技有限公司
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