Pharmaceutical composition for edoxaban tablets

Abstract

The invention provides pharmaceutical composition for edoxaban tablets. The composition is prepared from 10-50 parts of p-toluenesulfonic acid edoxaban monohydrate, 15-35 parts of a disintegrant, 2-10parts of a 5% polyvinylpyrrolidone 95% ethanol solution, 20-45 parts of filler and 0.5-2 parts of a lubricant, and has the advantages of high disintegration speed, high bioavailability, good stability and the like.

Description

technical field

[0001] The invention relates to an edoxaban p-toluenesulfonate tablet pharmaceutical composition, which belongs to the technical field of medicine. Background technique

[0002] With the acceleration of the pace of life and the increase of people's life pressure, thrombosis is gradually becoming an important disease that threatens human health, and it has become one of the common causes of blood circulation disorders in patients, especially in patients with cardiovascular and cerebrovascular thrombosis Among them, the morbidity, disability and mortality rates are high.

[0003] Thrombosis can cause stenosis and occlusion of the vascular lumen, leading to ischemia and infarction of major organs, thereby causing various diseases, such as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. Venous thromboembolism (VTE), including deep vein thrombosis (deep vein thrombosis, DVT) and pulmonary embolism (pulmonary embolism, PE), has bec...

Examples

Embodiment 1

[0034] Embodiment 1: Edoxaban p-toluenesulfonate sheet (1000)

[0035]

[0036] A total of 1000 tablets were produced, each tablet weighed 0.1g, and the specification was 30mg based on edoxaban.

[0037] Preparation process: The raw material drug is pulverized to make its particle size distribution reach D 50 ≤30μm and D 90 ≤60μm; crush the rest of the excipients through an 80-mesh sieve; accurately weigh the raw and excipients in the prescribed amount, mix them evenly, granulate with 5% PVP K30 95% ethanol solution, granulate with a 18-mesh sieve, and dry at 40°C. Add the prescribed amount of magnesium stearate, mix evenly, pass through a 18-mesh sieve, measure the content of the main drug in the granules, determine the weight of the tablet, and compress the tablet to obtain final product. The dispersion time of the resulting tablet was 126s.

Embodiment 2

[0038] Embodiment 2: Edoxaban p-toluenesulfonate sheet (1000)

[0039]

[0040]

[0041] A total of 1000 tablets were produced, each tablet weighed 0.1g, and the specification was 15mg based on edoxaban.

[0042] Preparation process: The raw material drug is pulverized to make its particle size distribution reach D 50 ≤30μm and D 90 ≤60μm; crush the rest of the excipients through an 80-mesh sieve; accurately weigh the raw and excipients in the prescribed amount, mix them evenly, granulate with 5% PVP K30 95% ethanol solution, granulate with a 18-mesh sieve, and dry at 40°C. Add the prescribed amount of talcum powder, mix evenly, pass through a 18-mesh sieve, measure the content of the main drug in the granules, determine the weight of the tablet, and compress the tablet to obtain the product. The dispersion time of the resulting tablet was 84s.

Embodiment 3

[0043] Embodiment 3: Edoxaban p-toluenesulfonate sheet (1000)

[0044]

[0045] A total of 1000 tablets were produced, each tablet weighed 0.1g, and the specification was 15mg based on edoxaban.

[0046] Preparation process: The raw material drug is pulverized to make its particle size distribution reach D 50 ≤30μm and D 90 ≤60μm; crush the rest of the excipients through an 80-mesh sieve; accurately weigh the raw and excipients in the prescribed amount, mix them evenly, granulate with 5% PVP K30 95% ethanol solution, granulate with a 18-mesh sieve, and dry at 40°C. Add the prescribed amount of magnesium stearate, mix evenly, pass through a 18-mesh sieve, measure the content of the main drug in the granules, determine the weight of the tablet, and compress the tablet to obtain final product. The dispersion time limit of the obtained tablet was 60s.

technical field

[0001] The invention relates to an edoxaban p-toluenesulfonate tablet pharmaceutical composition, which belongs to the technical field of medicine. Background technique

[0002] With the acceleration of the pace of life and the increase of people's life pressure, thrombosis is gradually becoming an important disease that threatens human health, and it has become one of the common causes of blood circulation disorders in patients, especially in patients with cardiovascular and cerebrovascular thrombosis Among them, the morbidity, disability and mortality rates are high.

[0003] Thrombosis can cause stenosis and occlusion of the vascular lumen, leading to ischemia and infarction of major organs, thereby causing various diseases, such as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. Venous thromboembolism (VTE), including deep vein thrombosis (deep vein thrombosis, DVT) and pulmonary embolism (pulmonary embolism, PE), has bec...

Examples

Embodiment 1

[0034] Embodiment 1: Edoxaban p-toluenesulfonate sheet (1000)

[0035]

[0036] A total of 1000 tablets were produced, each tablet weighed 0.1g, and the specification was 30mg based on edoxaban.

[0037] Preparation process: The raw material drug is pulverized to make its particle size distribution reach D 50 ≤30μm and D 90 ≤60μm; crush the rest of the excipients through an 80-mesh sieve; accurately weigh the raw and excipients in the prescribed amount, mix them evenly, granulate with 5% PVP K30 95% ethanol solution, granulate with a 18-mesh sieve, and dry at 40°C. Add the prescribed amount of magnesium stearate, mix evenly, pass through a 18-mesh sieve, measure the content of the main drug in the granules, determine the weight of the tablet, and compress the tablet to obtain final product. The dispersion time of the resulting tablet was 126s.

Embodiment 2

[0038] Embodiment 2: Edoxaban p-toluenesulfonate sheet (1000)

[0039]

[0040]

[0041] A total of 1000 tablets were produced, each tablet weighed 0.1g, and the specification was 15mg based on edoxaban.

[0042] Preparation process: The raw material drug is pulverized to make its particle size distribution reach D 50 ≤30μm and D 90 ≤60μm; crush the rest of the excipients through an 80-mesh sieve; accurately weigh the raw and excipients in the prescribed amount, mix them evenly, granulate with 5% PVP K30 95% ethanol solution, granulate with a 18-mesh sieve, and dry at 40°C. Add the prescribed amount of talcum powder, mix evenly, pass through a 18-mesh sieve, measure the content of the main drug in the granules, determine the weight of the tablet, and compress the tablet to obtain the product. The dispersion time of the resulting tablet was 84s.

Embodiment 3

[0043] Embodiment 3: Edoxaban p-toluenesulfonate sheet (1000)

[0044]

[0045] A total of 1000 tablets were produced, each tablet weighed 0.1g, and the specification was 15mg based on edoxaban.

[0046] Preparation process: The raw material drug is pulverized to make its particle size distribution reach D 50 ≤30μm and D 90 ≤60μm; crush the rest of the excipients through an 80-mesh sieve; accurately weigh the raw and excipients in the prescribed amount, mix them evenly, granulate with 5% PVP K30 95% ethanol solution, granulate with a 18-mesh sieve, and dry at 40°C. Add the prescribed amount of magnesium stearate, mix evenly, pass through a 18-mesh sieve, measure the content of the main drug in the granules, determine the weight of the tablet, and compress the tablet to obtain final product. The dispersion time limit of the obtained tablet was 60s.

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