Felodipine ramipril compound sustained-release preparation and preparation method thereof

Abstract

The invention discloses a compound sustained-release preparation containing felodipine and ramipril and a preparation method of the compound sustained-release preparation, wherein the compound sustained-release preparation is prepared by mixing felodipine sustained-release pellets and ramipril immediate-release pellets according to a specific dose proportion. The felodipine sustained-release pellets can sustainably release for 12 hours, and can be taken once a day, so as to keep the antihypertensive effect for a long time, the ramipril immediate-release pellets can be quickly absorbed so as to achieve the antihypertensive effect and treat the plasma concentration, due to the combination of the two kinds of pellets, the antihypertensive effect can be greatly enhanced, the toxic and side effect of the medicine can be reduced, the administration frequency can be reduced, sustainably stable antihypertensive effect can be achieved in a human body, the patient compliance can be enhanced, the compound sustained-release preparation consists of hundreds and thousands of pellets in uniform particle sizes, so that the damage of individual pellets will not cause burst release of the whole preparation, and compared with the sustained release tablets, the compound sustained-release preparation disclosed by the invention has the advantages of higher safety, lower irritation to gastrointestinal tract, more stable plasma concentration and capability of effectively improving the clinical effect.

Description

technical field

[0001] The invention relates to the technical field of a compound sustained-release preparation, in particular to a felodipine-ramipril compound sustained-release preparation and a preparation method thereof. It belongs to a compound sustained-release preparation of antihypertensive drugs. Background technique

[0002] Hypertension is one of the most common cardiovascular diseases, and it is also a major risk factor leading to increased morbidity and mortality of congestive heart failure, stroke, coronary heart disease, renal failure, and aortic aneurysm. In recent years, with the continuous improvement of the living standards of the Chinese people and the growth of the elderly population, hypertension is becoming a common disease with a very high prevalence rate and has entered our lives. At present, there is no effective way to cure hypertension in the world. Once the disease is diagnosed, it will be accompanied by lifelong and cause many other related dis...

Examples

Embodiment 1

[0042] 1. Preparation of fenodipine sustained-release pellets:

[0043] Prescription: Fenordipine 15g, microcrystalline cellulose 180g, lactose 150g, sodium lauryl sulfate 6g, ethyl cellulose aqueous dispersion (Surelease) 140.4g, titanium dioxide 2g.

[0044] Preparation process: Mix fenodipine, microcrystalline cellulose and lactose uniformly in an equal increasing method, and mix the powder for later use. Dissolve sodium lauryl sulfate in 35% ethanol solution, add to the above mixed powder to make soft material, use extrusion spheronization method to make pill core, dry, sieve and select 20-30 mesh pill core for coating . The prescribed amount of Surelease and titanium dioxide was prepared with purified water to form a slow-release coating solution with a solid content of 15%, dissolved and stirred for 45 minutes to make it fully dispersed. The 300g drug-containing pill core is placed in a fluidized bed, the process parameters are adjusted to ensure a fluidized state, the...

Embodiment 2

[0055] 1. Preparation of fenodipine sustained-release pellets:

[0056] Prescription: Fenordipine 15g, microcrystalline cellulose 180g, lactose 150g, sodium lauryl sulfate 6g, ethylcellulose aqueous dispersion (Aquacoat) 182.5g, dibutyl phthalate 4.5g, titanium dioxide 2g.

[0057] Preparation process: Mix fenodipine, microcrystalline cellulose and lactose uniformly in an equal increasing method, and mix the powder for later use. Dissolve sodium lauryl sulfate in 35% ethanol solution, add to the above mixed powder to make soft material, use extrusion spheronization method to make pill core, dry, sieve and select 20-30 mesh pill core for coating . Prepare the prescribed amount of Aquacoat, dibutyl phthalate and titanium dioxide with purified water to prepare a slow-release coating solution with a solid content of 15%, dissolve and stir for 45 minutes to fully disperse. 300g of drug-containing pill cores are placed in a fluidized bed, and the process parameters are adjusted to...

Embodiment 3

[0068] 1. Preparation of fenodipine sustained-release pellets:

[0069] Prescription: Fenordipine 15g, microcrystalline cellulose blank core 300g, PVP-K30 10g, Tween 5g, Eudragit NE30D 65.2g, talcum powder 15.6g, titanium dioxide 2g.

[0070] Preparation process: Dissolve fenodipine, PVP-K30 and Tween in 50% ethanol solution, stir and use to dissolve completely, and prepare the drug-containing solution. Put the microcrystalline cellulose blank pellet core in a fluidized bed, spray the above-mentioned drug-containing solution on the surface of the blank pellet core, and prepare the drug-containing pellet core by using the method of adding medicine, dry, sieve and select 20-30 mesh drug-containing pellet cores, and coat use. Dissolve and dilute the prescribed amount of Eudragit NE30D, talcum powder and titanium dioxide with purified water to prepare a slow-release coating solution with a solid content of 20%, and stir for 45 minutes to make it fully dispersed. 300g of drug-con...

technical field

[0001] The invention relates to the technical field of a compound sustained-release preparation, in particular to a felodipine-ramipril compound sustained-release preparation and a preparation method thereof. It belongs to a compound sustained-release preparation of antihypertensive drugs. Background technique

[0002] Hypertension is one of the most common cardiovascular diseases, and it is also a major risk factor leading to increased morbidity and mortality of congestive heart failure, stroke, coronary heart disease, renal failure, and aortic aneurysm. In recent years, with the continuous improvement of the living standards of the Chinese people and the growth of the elderly population, hypertension is becoming a common disease with a very high prevalence rate and has entered our lives. At present, there is no effective way to cure hypertension in the world. Once the disease is diagnosed, it will be accompanied by lifelong and cause many other related dis...

Examples

Embodiment 1

[0042] 1. Preparation of fenodipine sustained-release pellets:

[0043] Prescription: Fenordipine 15g, microcrystalline cellulose 180g, lactose 150g, sodium lauryl sulfate 6g, ethyl cellulose aqueous dispersion (Surelease) 140.4g, titanium dioxide 2g.

[0044] Preparation process: Mix fenodipine, microcrystalline cellulose and lactose uniformly in an equal increasing method, and mix the powder for later use. Dissolve sodium lauryl sulfate in 35% ethanol solution, add to the above mixed powder to make soft material, use extrusion spheronization method to make pill core, dry, sieve and select 20-30 mesh pill core for coating . The prescribed amount of Surelease and titanium dioxide was prepared with purified water to form a slow-release coating solution with a solid content of 15%, dissolved and stirred for 45 minutes to make it fully dispersed. The 300g drug-containing pill core is placed in a fluidized bed, the process parameters are adjusted to ensure a fluidized state, the...

Embodiment 2

[0055] 1. Preparation of fenodipine sustained-release pellets:

[0056] Prescription: Fenordipine 15g, microcrystalline cellulose 180g, lactose 150g, sodium lauryl sulfate 6g, ethylcellulose aqueous dispersion (Aquacoat) 182.5g, dibutyl phthalate 4.5g, titanium dioxide 2g.

[0057] Preparation process: Mix fenodipine, microcrystalline cellulose and lactose uniformly in an equal increasing method, and mix the powder for later use. Dissolve sodium lauryl sulfate in 35% ethanol solution, add to the above mixed powder to make soft material, use extrusion spheronization method to make pill core, dry, sieve and select 20-30 mesh pill core for coating . Prepare the prescribed amount of Aquacoat, dibutyl phthalate and titanium dioxide with purified water to prepare a slow-release coating solution with a solid content of 15%, dissolve and stir for 45 minutes to fully disperse. 300g of drug-containing pill cores are placed in a fluidized bed, and the process parameters are adjusted to...

Embodiment 3

[0068] 1. Preparation of fenodipine sustained-release pellets:

[0069] Prescription: Fenordipine 15g, microcrystalline cellulose blank core 300g, PVP-K30 10g, Tween 5g, Eudragit NE30D 65.2g, talcum powder 15.6g, titanium dioxide 2g.

[0070] Preparation process: Dissolve fenodipine, PVP-K30 and Tween in 50% ethanol solution, stir and use to dissolve completely, and prepare the drug-containing solution. Put the microcrystalline cellulose blank pellet core in a fluidized bed, spray the above-mentioned drug-containing solution on the surface of the blank pellet core, and prepare the drug-containing pellet core by using the method of adding medicine, dry, sieve and select 20-30 mesh drug-containing pellet cores, and coat use. Dissolve and dilute the prescribed amount of Eudragit NE30D, talcum powder and titanium dioxide with purified water to prepare a slow-release coating solution with a solid content of 20%, and stir for 45 minutes to make it fully dispersed. 300g of drug-con...

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