Lovastatin enteric coated sustained-release pellet capsule and preparation method thereof

Abstract

The invention discloses a lovastatin-containing enteric coated sustained-release pellet capsule and a preparation method thereof. The lovastatin-containing enteric coated sustained-release pellet capsule comprises two parts, namely, an enteric coated sustained-release pellet and a hollow capsule, wherein the enteric coated sustained-release pellet comprises 55-86% of medicine-containing pellet core, 2-5% of isolation coating layer, 2-15% of a sustained-release coating layer and 10-25% of enteric-coated coating layer by weight. The prepared lovastatin enteric coated sustained-release pellet capsule is uniform in granule size and stable in medicine release; the medicine is not released in gastric acid but is slowly and constantly released in intestinal tracts and livers, has the characteristic of targeted medicine release, is small in irritation to gastrointestinal tracts, and can reduce the toxic and side effects of the medicine and reduce the number of the medicine administrations, so that the compliance of patients is improved; and meanwhile as the enteric coated sustained-release pellet preparation is composed of hundreds of pellets of uniform granule sizes, the sudden release of the whole preparation is not caused by the breakage of individual pellets, so that the medicine is safer than a sustained-release tablet, smaller in irritation to gastrointestinal tracts and more stable in blood concentration, and the clinical effectiveness and security are effectively improved.

Description

Technical field

[0001] The invention relates to the technical field of enteric-coated sustained-release preparations, in particular to a lovastatin enteric-coated sustained-release pellet capsule and a preparation method thereof. It belongs to an enteric-coated sustained-release preparation of hypolipidemic drugs. Background technique

[0002] Cardiovascular disease is one of the most common and serious diseases that endanger human health (especially middle-aged and elderly people). Dyslipidemia is an important risk factor for atherosclerosis, coronary heart disease and other cardiovascular and cerebrovascular diseases. Lipid-lowering drugs can reduce these The incidence and mortality of diseases have a positive and profound impact on the prevention and treatment of cardiovascular diseases. With the advent of the aging society, the proportion of cardiovascular diseases in the elderly, such as hypertension and other diseases caused by hyperlipidemia, is increasing year by year, s...

Examples

Embodiment 1

[0039] 1. Prescription:

[0040]

[0041] 2. Preparation process:

[0042] (1) Preparation of pill-containing core: the micronized lovastatin, lactose, and microcrystalline cellulose are mixed uniformly in equal increments, sodium lauryl sulfate is dissolved in water to make a diluted solution, and then added to the mixed powder. The soft material is obtained, pellets are extruded and spheronized, dried in an oven at 60°C, and sieved to select 20-40 mesh-containing pellet cores.

[0043] (2) Coating isolation layer: Dissolve Opadry in water to prepare a 15% solid content coating solution, place the pill-containing core in a fluidized bed for coating, and then coat the pill with isolation layer at 50°C Oven drying.

[0044] (3) Coating slow-release coating layer: Dissolve Eudragit S100, triethyl citrate and talc in absolute ethanol to prepare a coating solution with a solid content of 12%, and place the plain pills in a fluidized bed for coating. The coated and sustained-release pell...

Embodiment 2

[0048] 1. Prescription:

[0049]

[0050] 2. Preparation process:

[0051] (1) Preparation of pill-containing core: the micronized lovastatin, lactose, and microcrystalline cellulose are mixed uniformly in equal increments, sodium lauryl sulfate is dissolved in water to make a diluted solution, and then added to the mixed powder. The soft material is obtained, pellets are extruded and spheronized, dried in an oven at 60°C, and sieved to select 20-40 mesh-containing pellet cores.

[0052] (2) Coating isolation layer: Dissolve Opadry in water to prepare a 15% solid content coating solution, place the pill-containing core in a fluidized bed for coating, and then coat the pill with isolation layer at 50°C Oven drying.

[0053] (3) Coating slow-release coating layer: Dissolve Eudragit S100, triethyl citrate and talc in absolute ethanol to prepare a coating solution with a solid content of 12%, and place the plain pills in a fluidized bed for coating. The coated and sustained-release pell...

Embodiment 3

[0057] 1. Prescription:

[0058]

[0059] 2. Preparation process:

[0060] (1) Preparation of pill-containing core: Dissolve and disperse micronized lovastatin and sodium lauryl sulfate in water to make a drug-containing solution, and place the blank pill core in a fluidized bed to adjust the process parameters to ensure fluidization State, spray the above-mentioned drug-containing solution on the surface of the pellet core, dry, and select 20-40 mesh pellet cores.

[0061] (2) Coating isolation layer: Dissolve Opadry in water to prepare a 15% solid content coating solution, place the pill-containing core in a fluidized bed for coating, and then coat the pill with isolation layer at 50°C Oven drying.

[0062] (3) Coating the sustained-release coating layer: Dissolve Eudragit NE30D and talc in water to prepare a 15% solid content coating solution. Place the pellet core in a fluidized bed for coating. Dry and mature in an oven at ℃ for 24 hours.

[0063] (4) Enteric coating layer: Diss...

Technical field

[0001] The invention relates to the technical field of enteric-coated sustained-release preparations, in particular to a lovastatin enteric-coated sustained-release pellet capsule and a preparation method thereof. It belongs to an enteric-coated sustained-release preparation of hypolipidemic drugs. Background technique

[0002] Cardiovascular disease is one of the most common and serious diseases that endanger human health (especially middle-aged and elderly people). Dyslipidemia is an important risk factor for atherosclerosis, coronary heart disease and other cardiovascular and cerebrovascular diseases. Lipid-lowering drugs can reduce these The incidence and mortality of diseases have a positive and profound impact on the prevention and treatment of cardiovascular diseases. With the advent of the aging society, the proportion of cardiovascular diseases in the elderly, such as hypertension and other diseases caused by hyperlipidemia, is increasing year by year, s...

Examples

Embodiment 1

[0039] 1. Prescription:

[0040]

[0041] 2. Preparation process:

[0042] (1) Preparation of pill-containing core: the micronized lovastatin, lactose, and microcrystalline cellulose are mixed uniformly in equal increments, sodium lauryl sulfate is dissolved in water to make a diluted solution, and then added to the mixed powder. The soft material is obtained, pellets are extruded and spheronized, dried in an oven at 60°C, and sieved to select 20-40 mesh-containing pellet cores.

[0043] (2) Coating isolation layer: Dissolve Opadry in water to prepare a 15% solid content coating solution, place the pill-containing core in a fluidized bed for coating, and then coat the pill with isolation layer at 50°C Oven drying.

[0044] (3) Coating slow-release coating layer: Dissolve Eudragit S100, triethyl citrate and talc in absolute ethanol to prepare a coating solution with a solid content of 12%, and place the plain pills in a fluidized bed for coating. The coated and sustained-release pell...

Embodiment 2

[0048] 1. Prescription:

[0049]

[0050] 2. Preparation process:

[0051] (1) Preparation of pill-containing core: the micronized lovastatin, lactose, and microcrystalline cellulose are mixed uniformly in equal increments, sodium lauryl sulfate is dissolved in water to make a diluted solution, and then added to the mixed powder. The soft material is obtained, pellets are extruded and spheronized, dried in an oven at 60°C, and sieved to select 20-40 mesh-containing pellet cores.

[0052] (2) Coating isolation layer: Dissolve Opadry in water to prepare a 15% solid content coating solution, place the pill-containing core in a fluidized bed for coating, and then coat the pill with isolation layer at 50°C Oven drying.

[0053] (3) Coating slow-release coating layer: Dissolve Eudragit S100, triethyl citrate and talc in absolute ethanol to prepare a coating solution with a solid content of 12%, and place the plain pills in a fluidized bed for coating. The coated and sustained-release pell...

Embodiment 3

[0057] 1. Prescription:

[0058]

[0059] 2. Preparation process:

[0060] (1) Preparation of pill-containing core: Dissolve and disperse micronized lovastatin and sodium lauryl sulfate in water to make a drug-containing solution, and place the blank pill core in a fluidized bed to adjust the process parameters to ensure fluidization State, spray the above-mentioned drug-containing solution on the surface of the pellet core, dry, and select 20-40 mesh pellet cores.

[0061] (2) Coating isolation layer: Dissolve Opadry in water to prepare a 15% solid content coating solution, place the pill-containing core in a fluidized bed for coating, and then coat the pill with isolation layer at 50°C Oven drying.

[0062] (3) Coating the sustained-release coating layer: Dissolve Eudragit NE30D and talc in water to prepare a 15% solid content coating solution. Place the pellet core in a fluidized bed for coating. Dry and mature in an oven at ℃ for 24 hours.

[0063] (4) Enteric coating layer: Diss...

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