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Bosentan tablet composition and preparation method thereof

A technology of composition and tan tablet, applied in the field of bosentan tablet composition and its preparation, to achieve the effects of uniform granule size, improvement of bioavailability, and reduction of adverse reactions

Inactive Publication Date: 2019-08-23
JIANGSU YABANG QIANGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the low dissolution rate of bosentan tablets is not fundamentally solved in this patent

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A bosentan tablet composition, its composition by mass is as follows: 65 parts of bosentan principal agent, 65 parts of sodium bicarbonate, 55 parts of skeleton material, 12 parts of disintegrant, 2 parts of glidant, 2 parts of lubricant 0.1 part of enteric coating material.

[0021] Wherein, the principal ingredient of bosentan is bosentan hydrate.

[0022] Among them, the skeleton material is a mixture of carboxymethyl cellulose, sodium carboxymethyl starch and sodium alginate, the mass ratio of which is 1:1.2:1.

[0023] Wherein, the disintegrant adopts cornstarch.

[0024] Wherein, colloidal silicon dioxide is selected as the glidant.

[0025] Among them, the lubricant magnesium stearate.

[0026] Among them, hydroxypropyl methylcellulose phthalate is selected as the enteric coating material.

[0027] The above-mentioned bosentan tablet composition adopts wet granulation and compression, mixes the main ingredient of bosentan with each raw material evenly, extrud...

Embodiment 2

[0029] A bosentan tablet composition, its composition by mass is as follows: 70 parts of bosentan principal agent, 70 parts of sodium bicarbonate, 60 parts of skeleton material, 15 parts of disintegrant, 3 parts of glidant, 3 parts of lubricant part, 0.3 part of enteric coating material.

[0030] Wherein, the principal ingredient of bosentan is bosentan hydrate.

[0031] Among them, the skeleton material is a mixture of carboxymethyl cellulose, sodium carboxymethyl starch and sodium alginate, the mass ratio of which is 1:1.5:1.

[0032] Wherein, the disintegrating agent adopts sodium carboxymethyl starch.

[0033] Wherein, colloidal silicon dioxide is selected as the glidant.

[0034] Among them, the lubricant magnesium stearate.

[0035] Among them, hydroxypropyl methylcellulose phthalate is selected as the enteric coating material.

[0036] The above-mentioned bosentan tablet composition adopts wet granulation and compression, mixes the main ingredient of bosentan with e...

Embodiment 3

[0038] A bosentan tablet composition, its composition by mass is as follows: 100 parts of bosentan principal agent, 100 parts of sodium bicarbonate, 80 parts of skeleton material, 16 parts of disintegrant, 3 parts of glidant, 3 parts of lubricant part, 0.6 part of enteric coating material.

[0039] Wherein, the principal agent of bosentan is bosentan hydrochloride.

[0040] Among them, the skeleton material is a mixture of carboxymethyl cellulose, sodium carboxymethyl starch and sodium alginate, the mass ratio of which is 1:1.8:1.

[0041] Among them, the disintegrant is a mixture of cross-linked polyvinylpyrrolidone and effervescent disintegrant, the mass ratio of which is 1:1.

[0042] Wherein, colloidal silicon dioxide is selected as the glidant.

[0043] Among them, the lubricant magnesium stearate.

[0044] Among them, hydroxypropyl methylcellulose phthalate and hydroxypropyl methylcellulose phthalate are selected as the enteric coating material.

[0045] The above-me...

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Abstract

The invention relates to the technical field of pharmacy, in particular to a bosentan tablet composition and a preparation method thereof. The bosentan tablet composition is prepared from the following components in parts by mass: 65 to 130 parts of bosentan main medicine, 65 to 130 parts of sodium bicarbonate, 55 to 100 parts of skeleton material, 12 to 24 parts of disintegrating agent, 2 to 5 parts of flow aid, 2 to 5 parts of lubricant and 0.1 to 1.2 parts of enteric coating material. The lubricant, the enteric coating material, the disintegrating agent and the sodium bicarbonate are addedin the bosentan tablet composition, so that the water dissolution rate is effectively increased, the bioavailability of the medicine is improved and the untoward effect on the stomach after use is reduced. Granules prepared by the preparation method are uniform in granularity and high in flowability, loose tablets, sticking and astringent flushing phenomena of the tablets are avoided, the hardnessof the tablet can reach to above 5 kg and the preparation is suitable for coating operation; and the sodium bicarbonate is added, so that the pH value is increased, dissolution of the bosentan main medicine is benefited and the bioavailability is improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a bosentan tablet composition and a preparation method thereof. Background technique [0002] Bosentan is a non-peptide non-selective endothelin receptor blocker highly substituted pyrimidine derivatives or a competitive blocker of endothelin-1 (ET-1) receptors, and endothelin receptor A in blood vessels (ETA) and endothelin receptor B (ETB) in brain, epithelial and smooth muscle cells. ET-1 is a potent endogenous vasoconstrictor with proliferative, fibrotic and inflammatory effects, and its concentration is high in plasma and lung tissue of patients with pulmonary arterial hypertension (PAH). The blocking effect of ET-1 in pulmonary circulation can reduce the resistance of pulmonary vessels and weaken the remodeling effect of chronic hypertension on blood vessels. It is used to treat PAH patients with dyspnea symptoms at rest or light exercise (functional status score is grad...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/32A61K31/506A61K47/38A61K47/36A61K47/32A61K47/02A61P9/12A61P11/00
CPCA61K9/2009A61K9/2027A61K9/205A61K9/2054A61K9/2059A61K9/284A61K9/2866A61K31/506A61P9/12A61P11/00
Inventor 王思清毛白杨王彬薛良军荆戟
Owner JIANGSU YABANG QIANGSHENG PHARMA
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