Composition containing ezetimibe and atorvastatin calcium and preparation method of composition

Abstract

The invention relates to a tablet composition containing ezetimibe and atorvastatin calcium and a preparation method of the composition. According to the method, the stability of atorvastatin calcium in a pharmaceutical composition can be effectively improved, and the in-vivo bioavailability of the medicine is improved. Moreover, the method has the advantages that the process is simple and feasible to operate, the requirement on preparation equipment is low, and the production cost is reduced. The solid oral preparation is used for treating or preventing cardiovascular and cerebrovascular diseases.

Description

technical field

[0001] The invention relates to a tablet for treating dyslipidemia, in particular to its prescription composition and preparation process, and belongs to the technical field of medicine. Background technique

[0002] Coronary heart disease (CHD) is an important cause of disability and death in developed and developing countries, and it is also the main cause of late heart failure. Dyslipidemia has been recognized as a risk factor for cardiovascular disease and is one of the main risk factors for coronary heart disease. Low density lipoprotein cholesterol (LDL-C) is the most important pathogenic factor of CHD, and its plasma concentration Elevation was positively correlated with the risk of coronary heart disease. For high-risk groups with CHD and its equivalent risk diseases (diabetes), the optimal lipid-lowering target should be LDL-C ≤ 2.6mmol L-1, and for extremely high-risk groups (such as CHD complicated with diabetes, acute coronary syndrome) should be...

Examples

Embodiment 1

[0029] Tablet prescription:

[0030] Ezetimibe 10 g Atorvastatin Calcium Meglumine Mixed Powder 10 g anhydrous lactose 120 g sodium lauryl sulfate 2 g lactose monohydrate 55 g microcrystalline cellulose 30 g Croscarmellose Sodium 12 g povidone 4 g sodium bicarbonate 6 g hypromellose 5 g Magnesium stearate 2 g

[0031] Preparation Process:

[0032] (1) Micronize atorvastatin calcium and meglumine at a ratio of 5:1, and control the particle size at 60-100 μm; pass ezetimibe through a 80-100 mesh sieve, and set aside; lactose monohydrate, micro Crystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, anhydrous lactose, hypromellose, and sodium bicarbonate were passed through a 60-mesh sieve, and set aside;

[0033] (2) Add water to the prescription amount of povidone to make a 10% mass ratio adhesive, then add 10g ezetimibe, 55g lactose monohydrate, 2g sodium lauryl sulfate, 5g croscarmellose ...

Embodiment 2

[0037] Tablet prescription:

[0038] Ezetimibe 10 g Atorvastatin Calcium Meglumine Mixed Powder 20 g anhydrous lactose 130 g sodium lauryl sulfate 1 g lactose monohydrate 45 g microcrystalline cellulose 20 g Croscarmellose Sodium 12 g povidone 5 g sodium bicarbonate 9 g hypromellose 2 g Magnesium stearate 1 g

[0039] Preparation Process:

[0040] (1) Micronize atorvastatin calcium and meglumine at a ratio of 6:1, and control the particle size at 50-80 μm; pass ezetimibe through a 80-100 mesh sieve for use; Crystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, anhydrous lactose, hypromellose, and sodium bicarbonate were sieved separately, and set aside;

[0041] (2) Add water to the prescribed amount of povidone to make an 8% mass ratio adhesive, then add 10g ezetimibe, 45g lactose monohydrate, 1g sodium lauryl sulfate, 5g croscarmellose sodium Mix at a speed of 300 rpm, first stir for ...

Embodiment 3

[0045] Tablet prescription:

[0046] Ezetimibe 10 g Atorvastatin Calcium Meglumine Mixed Powder 40 g anhydrous lactose 150 g sodium lauryl sulfate 3 g lactose monohydrate 60 g microcrystalline cellulose 20 g Croscarmellose Sodium 12 g povidone 6 g sodium bicarbonate 12 g hypromellose 6 g Magnesium stearate 1 g

[0047] Preparation Process:

[0048] (1) Micronize atorvastatin calcium and meglumine at a ratio of 4:1, and control the particle size at 10-50 μm; pass ezetimibe through a 80-100 mesh sieve, and set aside; lactose monohydrate, micro Crystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, anhydrous lactose, hypromellose, and sodium bicarbonate were sieved separately, and set aside;

[0049] (2) Add water to the prescribed amount of povidone to make a 15% mass ratio adhesive, then add 10g ezetimibe, 60g lactose monohydrate, 3g sodium lauryl sulfate, 5g croscarmellose sodium Mixing ...

technical field

[0001] The invention relates to a tablet for treating dyslipidemia, in particular to its prescription composition and preparation process, and belongs to the technical field of medicine. Background technique

[0002] Coronary heart disease (CHD) is an important cause of disability and death in developed and developing countries, and it is also the main cause of late heart failure. Dyslipidemia has been recognized as a risk factor for cardiovascular disease and is one of the main risk factors for coronary heart disease. Low density lipoprotein cholesterol (LDL-C) is the most important pathogenic factor of CHD, and its plasma concentration Elevation was positively correlated with the risk of coronary heart disease. For high-risk groups with CHD and its equivalent risk diseases (diabetes), the optimal lipid-lowering target should be LDL-C ≤ 2.6mmol L-1, and for extremely high-risk groups (such as CHD complicated with diabetes, acute coronary syndrome) should be...

Examples

Embodiment 1

[0029] Tablet prescription:

[0030] Ezetimibe 10 g Atorvastatin Calcium Meglumine Mixed Powder 10 g anhydrous lactose 120 g sodium lauryl sulfate 2 g lactose monohydrate 55 g microcrystalline cellulose 30 g Croscarmellose Sodium 12 g povidone 4 g sodium bicarbonate 6 g hypromellose 5 g Magnesium stearate 2 g

[0031] Preparation Process:

[0032] (1) Micronize atorvastatin calcium and meglumine at a ratio of 5:1, and control the particle size at 60-100 μm; pass ezetimibe through a 80-100 mesh sieve, and set aside; lactose monohydrate, micro Crystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, anhydrous lactose, hypromellose, and sodium bicarbonate were passed through a 60-mesh sieve, and set aside;

[0033] (2) Add water to the prescription amount of povidone to make a 10% mass ratio adhesive, then add 10g ezetimibe, 55g lactose monohydrate, 2g sodium lauryl sulfate, 5g croscarmellose ...

Embodiment 2

[0037] Tablet prescription:

[0038] Ezetimibe 10 g Atorvastatin Calcium Meglumine Mixed Powder 20 g anhydrous lactose 130 g sodium lauryl sulfate 1 g lactose monohydrate 45 g microcrystalline cellulose 20 g Croscarmellose Sodium 12 g povidone 5 g sodium bicarbonate 9 g hypromellose 2 g Magnesium stearate 1 g

[0039] Preparation Process:

[0040] (1) Micronize atorvastatin calcium and meglumine at a ratio of 6:1, and control the particle size at 50-80 μm; pass ezetimibe through a 80-100 mesh sieve for use; Crystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, anhydrous lactose, hypromellose, and sodium bicarbonate were sieved separately, and set aside;

[0041] (2) Add water to the prescribed amount of povidone to make an 8% mass ratio adhesive, then add 10g ezetimibe, 45g lactose monohydrate, 1g sodium lauryl sulfate, 5g croscarmellose sodium Mix at a speed of 300 rpm, first stir for ...

Embodiment 3

[0045] Tablet prescription:

[0046] Ezetimibe 10 g Atorvastatin Calcium Meglumine Mixed Powder 40 g anhydrous lactose 150 g sodium lauryl sulfate 3 g lactose monohydrate 60 g microcrystalline cellulose 20 g Croscarmellose Sodium 12 g povidone 6 g sodium bicarbonate 12 g hypromellose 6 g Magnesium stearate 1 g

[0047] Preparation Process:

[0048] (1) Micronize atorvastatin calcium and meglumine at a ratio of 4:1, and control the particle size at 10-50 μm; pass ezetimibe through a 80-100 mesh sieve, and set aside; lactose monohydrate, micro Crystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, anhydrous lactose, hypromellose, and sodium bicarbonate were sieved separately, and set aside;

[0049] (2) Add water to the prescribed amount of povidone to make a 15% mass ratio adhesive, then add 10g ezetimibe, 60g lactose monohydrate, 3g sodium lauryl sulfate, 5g croscarmellose sodium Mixing ...