Ivabradine hydrochloride osmotic pump controlled-release tablet and preparation method thereof

Abstract

The invention provides an ivabradine hydrochloride osmotic pump controlled-release tablet and a preparation method thereof. The osmotic pump controlled-release tablet is characterized by containing active ingredients of ivabradine hydrochloride and comprising a double-layer tablet core and a semipermeable coating membrane, wherein the double-layer tablet core is formed by pressing a high polymer material, osmotic pressure active substances and the like. The ivabradine hydrochloride osmotic pump controlled-release tablet enables the ivabradine hydrochloride to be slowly released at a constant speed in 0-24 hours, the release rate is more than 90%, and the osmotic pump controlled-release tablet has a long-acting zero-level drug-releasing characteristic. The osmotic pump controlled-release tablet can be used for treating patients suffering from chronic angina pectoris, stabilize the blood concentration, reduce adverse reactions caused by large fluctuation of the blood concentration and improve drug safety, and meanwhile reduces drug taking times of the patients and improves adaptability of the patients.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations. Specifically relates to an ivabradine hydrochloride osmotic pump controlled-release tablet and a preparation method thereof. Background technique

[0002] The speed of the heart rate reflects the excitability of the human sympathetic nerve to a certain extent. Studies have confirmed that heart rate is an independent risk predictor for various cardiovascular diseases such as coronary heart disease, hypertension, and heart failure. Tachycardia exerts a toxic effect on the myocardium by increasing myocardial oxygen consumption, reducing diastolic myocardial blood perfusion, increasing arterial blood pressure and catecholamine levels, and increasing the hospitalization rate and mortality of patients. Therefore, effectively controlling the heart rate is an important clinical decision in the treatment of cardiovascular diseases, and a variety of heart rate-lowering drugs, mainly β-blockers,...

Examples

Embodiment 1

[0031] Tablet prescription:

[0032]

[0033] Coating prescription

[0034] composition

Dosage / g

Cellulose acetate

100

polyethylene glycol 4000

10

acetone

Appropriate amount

water

Appropriate amount

[0035] Preparation Process:

[0036] Pass the drug and polyoxyethylene in the prescription amount of the drug-containing layer through a 80-mesh sieve, add a lubricant and mix evenly; pass the prescription amount of polyoxyethylene, sodium chloride and magnesium stearate in the booster layer through a 80-mesh sieve, and add a lubricant Mix evenly, use the No. 8 punch twice to pressurize to get the tablet core. Cellulose acetate and polyethylene glycol were dissolved in acetone and distilled water respectively and mixed evenly, and the tablet core was coated with a coating pan with a weight gain of 6%. After coating, it was cured in an oven at 40°C for 12 hours. Then prepare and punch a 0.6mm diameter release h...

Embodiment 2

[0038] Tablet prescription:

[0039]

[0040] Coating film prescription:

[0041] composition

Dosage / g

Ethyl cellulose

100

polyethylene glycol 4000

12.5

acetone

Appropriate amount

distilled water

Appropriate amount

[0042] Preparation Process:

[0043] Pass the drug, polyoxyethylene, and lactose in the prescription amount of the drug-containing layer through a 80-mesh sieve, add lubricant, and mix evenly; pass the prescription amount of polyoxyethylene and sodium chloride in the booster layer through an 80-mesh sieve, add lubricant and mix evenly , Use the No. 8 punch to pressurize twice to get the tablet core. Dissolve ethyl cellulose and polyethylene glycol in acetone and distilled water respectively and mix evenly, coat the tablet core with a coating pan, with a weight gain of 6%, and cure in an oven at 40°C for 12 hours after coating . Then prepare a 0.6mm diameter drug release hole on the drug-contai...

Embodiment 3

[0045]Tablet prescription:

[0046]

[0047] Coating film prescription:

[0048] composition

Dosage / g

Cellulose acetate

100

polyethylene glycol 4000

12.5

acetone

Appropriate amount

water

Appropriate amount

[0049] Preparation Process:

[0050] Pass the drug, polyoxyethylene, and mannitol in the prescription amount of the drug-containing layer through a 80-mesh sieve, add lubricant and mix evenly, pass the prescription amount of polyoxyethylene and sodium chloride in the booster layer through an 80-mesh sieve, add lubricant and mix evenly , Use the No. 8 punch to pressurize twice to get the tablet core. Cellulose acetate and polyethylene glycol were dissolved in acetone and distilled water respectively and mixed evenly, and the tablet core was coated with a coating pan, with a weight gain of 8%. After coating, it was cured in an oven at 40°C for 12 hours. Then prepare a 0.6mm diameter release hole on the si...

technical field

[0001] The invention belongs to the field of pharmaceutical preparations. Specifically relates to an ivabradine hydrochloride osmotic pump controlled-release tablet and a preparation method thereof. Background technique

[0002] The speed of the heart rate reflects the excitability of the human sympathetic nerve to a certain extent. Studies have confirmed that heart rate is an independent risk predictor for various cardiovascular diseases such as coronary heart disease, hypertension, and heart failure. Tachycardia exerts a toxic effect on the myocardium by increasing myocardial oxygen consumption, reducing diastolic myocardial blood perfusion, increasing arterial blood pressure and catecholamine levels, and increasing the hospitalization rate and mortality of patients. Therefore, effectively controlling the heart rate is an important clinical decision in the treatment of cardiovascular diseases, and a variety of heart rate-lowering drugs, mainly β-blockers,...

Examples

Embodiment 1

[0031] Tablet prescription:

[0032]

[0033] Coating prescription

[0034] composition

Dosage / g

Cellulose acetate

100

polyethylene glycol 4000

10

acetone

Appropriate amount

water

Appropriate amount

[0035] Preparation Process:

[0036] Pass the drug and polyoxyethylene in the prescription amount of the drug-containing layer through a 80-mesh sieve, add a lubricant and mix evenly; pass the prescription amount of polyoxyethylene, sodium chloride and magnesium stearate in the booster layer through a 80-mesh sieve, and add a lubricant Mix evenly, use the No. 8 punch twice to pressurize to get the tablet core. Cellulose acetate and polyethylene glycol were dissolved in acetone and distilled water respectively and mixed evenly, and the tablet core was coated with a coating pan with a weight gain of 6%. After coating, it was cured in an oven at 40°C for 12 hours. Then prepare and punch a 0.6mm diameter release h...

Embodiment 2

[0038] Tablet prescription:

[0039]

[0040] Coating film prescription:

[0041] composition

Dosage / g

Ethyl cellulose

100

polyethylene glycol 4000

12.5

acetone

Appropriate amount

distilled water

Appropriate amount

[0042] Preparation Process:

[0043] Pass the drug, polyoxyethylene, and lactose in the prescription amount of the drug-containing layer through a 80-mesh sieve, add lubricant, and mix evenly; pass the prescription amount of polyoxyethylene and sodium chloride in the booster layer through an 80-mesh sieve, add lubricant and mix evenly , Use the No. 8 punch to pressurize twice to get the tablet core. Dissolve ethyl cellulose and polyethylene glycol in acetone and distilled water respectively and mix evenly, coat the tablet core with a coating pan, with a weight gain of 6%, and cure in an oven at 40°C for 12 hours after coating . Then prepare a 0.6mm diameter drug release hole on the drug-contai...

Embodiment 3

[0045]Tablet prescription:

[0046]

[0047] Coating film prescription:

[0048] composition

Dosage / g

Cellulose acetate

100

polyethylene glycol 4000

12.5

acetone

Appropriate amount

water

Appropriate amount

[0049] Preparation Process:

[0050] Pass the drug, polyoxyethylene, and mannitol in the prescription amount of the drug-containing layer through a 80-mesh sieve, add lubricant and mix evenly, pass the prescription amount of polyoxyethylene and sodium chloride in the booster layer through an 80-mesh sieve, add lubricant and mix evenly , Use the No. 8 punch to pressurize twice to get the tablet core. Cellulose acetate and polyethylene glycol were dissolved in acetone and distilled water respectively and mixed evenly, and the tablet core was coated with a coating pan, with a weight gain of 8%. After coating, it was cured in an oven at 40°C for 12 hours. Then prepare a 0.6mm diameter release hole on the si...

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