Method for preparing acipimox-ethylcellulose sustained release micro-capsule

Abstract

The invention discloses a method for preparing an acipimox-ethylcellulose sustained release micro-capsule. The method comprises the following steps: (1) dissolving ethyl cellulose powder into a volatile organic solvent to obtain a solution a; (2) adding the acipimox powder to the solution a to obtain a solution b under an agitation state, wherein the mass ratio of the acipimox powder to the ethyl cellulose powder is (1:1) to (3:1); (3) dissolving an emulsifier sodium dodecyl benzene sulfonate into nonvolatile high boiling liquid at 30-35 DEG C to obtain a solution c, wherein the volume ratio of the nonvolatile high boiling liquid to the volatile organic solvent is (3:1) to (5:1), and the mass percent concentration of the sodium dodecyl benzene sulfonate in the solution c is 1-2%; and (4) adding the solution b to the solution c at 30-35 DEG C, agitating for 3-6 hours, then carrying out suction filtration, washing the solid by water, and naturally drying at room temperature. By adopting the method disclosed by the invention, the half-life period of the acipimox medicine can be prolonged, the bioavailability of the medicine is improved, and the medicine action time is prolonged.

Description

technical field

[0001] The invention relates to a preparation method of a new drug dosage form, that is, a sustained-release microcapsule, in particular to a preparation method of an acipimox-ethylcellulose sustained-release microcapsule. Background technique

[0002] With the continuous development of society and the continuous growth of economy, people pay more and more attention to the improvement of the quality of life, and at the same time, they also pay more and more attention to health issues, and realize the importance of medical care. Hyperlipidemia has endangered the health of more and more people. Among them, primary hyperlipidemia refers to hyperlipidemia that occurred without any other diseases, usually because of genetic factors; secondary hyperlipidemia Lipidemia refers to hyperlipidemia caused by various reasons, such as: diabetes, hypothyroidism, nephrotic syndrome, kidney transplantation, biliary obstruction, etc. Hyperlipidemia caused by bad eating habits,...

Examples

Embodiment 1

[0027] Use a drug pulverizer to pulverize amoxicillin to 80 mesh, and after ethylcellulose with a viscosity specification of 10CP is pulverized to 40 mesh, take amoxicillin drug powder and ethylcellulose powder, and its mass ratio is 3: 1. Slowly add ethyl cellulose to dichloromethane under stirring at a rotating speed of 400rmp to obtain solution a; add pulverized amoxicil drug powder to solution a under stirring at a rotating speed of 400rmp to obtain solution b ; The solution b was left to stand under stirring at a rotating speed of 400rmp, and the water with a volume ratio of 5:1 to dichloromethane was placed in a 30°C constant temperature water bath, and 1% emulsifier SDS was added while stirring to fully disperse the emulsifier. Obtain solution c; add solution b to solution c, continue to stir in a 30°C constant temperature water bath for 4 hours, then suction filter, wash and dry, and finally obtain microcapsules with good roundness and adhesion. Such as figure 1 As sh...

Embodiment 2

[0034] Use a drug pulverizer to pulverize amoxicillin to 80 mesh, and after ethylcellulose with a viscosity specification of 10CP is pulverized to 40 mesh, weigh amoxicillin drug powder and ethylcellulose powder, and its mass ratio is 2: 1. Slowly add ethyl cellulose to dichloromethane under stirring at a rotational speed of 250rmp to obtain solution a; add pulverized amoximus drug powder to solution a under stirring at a rotational speed of 250rmp to obtain solution b ; The solution b was left to stand under stirring at a rotating speed of 400rmp, and the water with a volume ratio of 4:1 to dichloromethane was placed in a 32°C constant temperature water bath, and 1% emulsifier SDS was added while stirring to fully disperse the emulsifier. Obtain solution c; add solution b to solution c, continue to stir in a 32°C constant temperature water bath for 3 hours, then suction filter, wash and dry, and finally obtain microcapsules with good roundness and adhesion.

[0035] The relea...

Embodiment 3

[0037]Use a drug pulverizer to pulverize amoxix to 80 mesh, and after ethylcellulose with a viscosity specification of 10CP is pulverized to 40 mesh, weigh the amoxix drug powder and ethylcellulose powder, and the mass ratio is 1: 1. Slowly add ethyl cellulose to dichloromethane under stirring at a rotating speed of 300rmp to obtain solution a; add pulverized amoximus drug powder to solution a under stirring at rotating speed of 300rmp to obtain solution b The solution b was left to stand under stirring at a rotating speed of 300rmp, and the water with a volume ratio of 3:1 to dichloromethane was placed in a 35°C constant temperature water bath, and 1.5% emulsifier SDS was added while stirring to fully disperse the emulsifier. Obtain solution c; add solution b to solution c, continue to stir in a 35°C constant temperature water bath for 4 hours, then suction filter, wash and dry, and finally obtain microcapsules with good roundness and adhesion.

[0038] The release rate of th...

technical field

[0001] The invention relates to a preparation method of a new drug dosage form, that is, a sustained-release microcapsule, in particular to a preparation method of an acipimox-ethylcellulose sustained-release microcapsule. Background technique

[0002] With the continuous development of society and the continuous growth of economy, people pay more and more attention to the improvement of the quality of life, and at the same time, they also pay more and more attention to health issues, and realize the importance of medical care. Hyperlipidemia has endangered the health of more and more people. Among them, primary hyperlipidemia refers to hyperlipidemia that occurred without any other diseases, usually because of genetic factors; secondary hyperlipidemia Lipidemia refers to hyperlipidemia caused by various reasons, such as: diabetes, hypothyroidism, nephrotic syndrome, kidney transplantation, biliary obstruction, etc. Hyperlipidemia caused by bad eating habits,...

Examples

Embodiment 1

[0027] Use a drug pulverizer to pulverize amoxicillin to 80 mesh, and after ethylcellulose with a viscosity specification of 10CP is pulverized to 40 mesh, take amoxicillin drug powder and ethylcellulose powder, and its mass ratio is 3: 1. Slowly add ethyl cellulose to dichloromethane under stirring at a rotating speed of 400rmp to obtain solution a; add pulverized amoxicil drug powder to solution a under stirring at a rotating speed of 400rmp to obtain solution b ; The solution b was left to stand under stirring at a rotating speed of 400rmp, and the water with a volume ratio of 5:1 to dichloromethane was placed in a 30°C constant temperature water bath, and 1% emulsifier SDS was added while stirring to fully disperse the emulsifier. Obtain solution c; add solution b to solution c, continue to stir in a 30°C constant temperature water bath for 4 hours, then suction filter, wash and dry, and finally obtain microcapsules with good roundness and adhesion. Such as figure 1 As sh...

Embodiment 2

[0034] Use a drug pulverizer to pulverize amoxicillin to 80 mesh, and after ethylcellulose with a viscosity specification of 10CP is pulverized to 40 mesh, weigh amoxicillin drug powder and ethylcellulose powder, and its mass ratio is 2: 1. Slowly add ethyl cellulose to dichloromethane under stirring at a rotational speed of 250rmp to obtain solution a; add pulverized amoximus drug powder to solution a under stirring at a rotational speed of 250rmp to obtain solution b ; The solution b was left to stand under stirring at a rotating speed of 400rmp, and the water with a volume ratio of 4:1 to dichloromethane was placed in a 32°C constant temperature water bath, and 1% emulsifier SDS was added while stirring to fully disperse the emulsifier. Obtain solution c; add solution b to solution c, continue to stir in a 32°C constant temperature water bath for 3 hours, then suction filter, wash and dry, and finally obtain microcapsules with good roundness and adhesion.

[0035] The relea...

Embodiment 3

[0037]Use a drug pulverizer to pulverize amoxix to 80 mesh, and after ethylcellulose with a viscosity specification of 10CP is pulverized to 40 mesh, weigh the amoxix drug powder and ethylcellulose powder, and the mass ratio is 1: 1. Slowly add ethyl cellulose to dichloromethane under stirring at a rotating speed of 300rmp to obtain solution a; add pulverized amoximus drug powder to solution a under stirring at rotating speed of 300rmp to obtain solution b The solution b was left to stand under stirring at a rotating speed of 300rmp, and the water with a volume ratio of 3:1 to dichloromethane was placed in a 35°C constant temperature water bath, and 1.5% emulsifier SDS was added while stirring to fully disperse the emulsifier. Obtain solution c; add solution b to solution c, continue to stir in a 35°C constant temperature water bath for 4 hours, then suction filter, wash and dry, and finally obtain microcapsules with good roundness and adhesion.

[0038] The release rate of th...

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