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Riociguat orally disintegrating tablet and preparation method thereof

A technology of orally disintegrating tablets and disintegrants, applied in the field of orally disintegrating tablets containing riociguat and its preparation, can solve the problems of complex preparation process and low solubility of riociguat, and achieve short disintegration time and simple preparation process Easy to implement and good promotion prospects

Inactive Publication Date: 2016-08-24
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Riociguat has a low solubility in water. In order to solve this problem, CN201410635422.6 discloses a solid pharmaceutical preparation comprising Riociguat, which uses a water-soluble polymer material as a drug carrier. After heating, high-speed stirring, low-temperature cooling, Grinding and preparing into solid dispersion, the preparation process is complicated

Method used

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  • Riociguat orally disintegrating tablet and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

1%

[0031] Preparation:

[0032] (1) Co-micronize Riociguat and mannitol at a ratio of 1:10, and grind the rest of the excipients separately through a 100-mesh sieve;

[0033] (2) Dissolve the prescribed amount of povidone in 20% ethanol aqueous solution to make a 3% povidone solution;

[0034] (3) After sieving and mixing the co-powder, the remaining amount of mannitol in the prescription, microcrystalline cellulose, 10% sodium carboxymethyl starch in the prescription amount, and aspartame, add the povidone solution in the prescription amount, preparation of soft materials;

[0035] (4) Granulate through a 24-mesh sieve, dry in an oven at 50°C until the moisture content of the granules is between 1.0 and 3.0%, and pass through a 24-mesh sieve for granulation;

[0036] (5) Add micropowder silica gel, magnesium stearate, and sodium carboxymethyl starch remaining in the prescription to the dry granules obtained in (4), and mix well;

[0037] (6) Determining the content...

Embodiment 2

1%

[0040] Preparation:

[0041] (1) Riociguat and mannitol were co-micronized at a ratio of 1:8, and the rest of the excipients were finely ground and passed through a 100-mesh sieve;

[0042] (2) Dissolve the prescribed amount of hydroxypropyl cellulose in 20% ethanol aqueous solution to make a 5% hydroxypropyl cellulose solution;

[0043] (3) After sieving and mixing the co-powder, the remaining amount of mannitol in the prescription, microcrystalline cellulose, 10% croscarmellose sodium in the prescription amount, and aspartame, add the prescribed amount of hydroxypropyl Base cellulose solution to prepare soft materials;

[0044] (4) Granulate through a 24-mesh sieve, dry in an oven at 50°C until the moisture content of the granules is between 1.0 and 3.0%, and pass through a 24-mesh sieve for granulation;

[0045] (5) Add magnesium stearate and the remaining amount of croscarmellose sodium in the prescription to the dry granules obtained in (4), and mix well;

...

Embodiment 3

1%

[0049] Preparation:

[0050] (1) Co-micronize Riociguat and mannitol at a ratio of 1:10, and grind the rest of the excipients separately through a 100-mesh sieve;

[0051] (2) Dissolve the prescribed amount of hydroxypropyl cellulose in 20% ethanol aqueous solution to make a 5% hydroxypropyl cellulose solution;

[0052] (3) After sieving and mixing the co-powder, the remaining amount of mannitol in the prescription, pregelatinized starch, 10% crospovidone in the prescription amount, aspartame, and lemon flavor, add the prescribed amount of hydroxypropyl Base cellulose solution to prepare soft materials;

[0053] (4) Granulate through a 24-mesh sieve, dry in an oven at 50°C until the moisture content of the granules is between 1.0 and 3.0%, and pass through a 24-mesh sieve for granulation;

[0054] (5) Add micropowder silica gel, magnesium stearate, and crospovidone remaining in the prescription to the dry granules obtained in (4), and mix well;

[0055] (6) Deter...

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Abstract

The invention discloses a riociguat orally disintegrating tablet and a preparation method of the riociguat orally disintegrating tablet. The disintegrating tablet is a medicinal composition containing riociguat, a filling agent, a disintegrating agent, a wetting agent, a binding agent, a corrigent and a lubricating agent. The preparation method adopts the wet granulation tabletting method. The invention aims at providing the riociguat orally disintegrating tablet which is simple in preparation process, low in cost, convenient to take, rapid in taking effect, and high in bioavailability; the dosage form can improve the medicine taking compliance of patients, and thus the treatment for diseases is benefited.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an orally disintegrating tablet containing riociguat and a preparation method thereof. technical background [0002] Riociguat was approved by the FDA on October 8, 2013 for the treatment of pulmonary arterial hypertension. It is the first new class of soluble guanylate cyclase (sGC) agonists. sGC is an important signal transduction enzyme, which can be activated by NO to catalyze the synthesis of cGMP, which is the classic NO-sGC-cGMP signaling pathway. NO synthesis is insufficient in patients with pulmonary arterial hypertension, and NO donor drugs are effective but have a short half-life. Riociguat can act synergistically with NO or independently of NO to directly activate sGC, thereby up-regulating the second messenger cGMP. Clinical studies have shown that riociguat is not only effective in treating pulmonary hypertension, but also easy to tolerate, with mild adver...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/506A61P7/02A61P9/12A61P11/00
CPCA61K9/0056A61K9/2054A61K9/2059A61K31/506
Inventor 石娟张庭
Owner BEIJING VENTUREPHARM BIOTECH
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