Slow-release composition containing L-milnacipran and preparation method thereof

Abstract

The invention relates to a sustained-release composition containing Levomilnacipran and a preparation method thereof. The composition of the invention contains Levomilnacipran or a pharmaceutically acceptable salt thereof as an active ingredient, and is characterized in that it also contains High-viscosity hypromellose as a hydrophilic gel-type sustained-release matrix material and an acrylic resin as a pH regulator; the weight ratio of each component is: Levomilnacipran or its pharmaceutically acceptable 10-70 parts of salt, 5-30 parts of hypromellose, 3.5-7.5 parts of acrylic resin; when preparing, be sure to fully mix levomilnacipran, hypromellose and acrylic resin. The composition of the invention can achieve the same release behavior in artificial gastric juice and artificial intestinal juice, maintain the effect of sustained release for up to 12 hours, and has the advantages of small production loss, high efficiency, good stability, simple operation and easy popularization.

Description

[0001] This application is a divisional application with the patent application number "201210323131.4", the filing date is September 4, 2012, and the title of the invention is "a slow-release composition containing levomilnacipran and its preparation method". technical field

[0002] The invention relates to the technical field of pharmaceutical preparations, in particular to a sustained-release composition containing levomilnacipran and a preparation method thereof. Background technique

[0003] L-milnacipran entered clinical phase III in the United States in November 2009. L-milnacipran is the latest generation of antidepressant drugs at home and abroad.

[0004] Pharmacokinetic studies show that Levomilnacipran is rapidly absorbed after oral administration, and the blood concentration reaches its peak in about 1-2 hours, with a short elimination half-life. Ordinary Levomilnacipran tablets usually need to be taken 3 times a day to maintain the treatment. Therefore, it is ...

Examples

Embodiment 1

[0062]

[0063] Mix levomilnacipran with calcium hydrogen phosphate and hypromellose K4M evenly, and set the mixing speed at 20-50 rpm; add 5% hypromellose aqueous solution to prepare wet granules, and granulate Stirring speed is set as: 20-50 rpm, cutting knife speed is 30-80 rpm; the above wet particles are boiled and dried, the drying temperature is set at 50-90 degrees, and the drying time is 10-30 minutes; Arrange the dried granules to obtain uniform dry granules, then add magnesium stearate and mix evenly, the mixing speed is 10-30 rpm, and the mixing time is 5-30 minutes; press the above mixture into tablets, The speed is 10-50 rpm, and the hardness is controlled at 5-13kg.

[0064] In this case, only hypromellose was used as the skeleton material, calcium hydrogen phosphate was used as the filler, and no pH regulator was used.

[0065] Take this product, according to the release test method (Chinese Pharmacopoeia 2010 edition two appendix X D first method), using t...

Embodiment 2

[0070] This embodiment is only used for comparison and description, and is not the content of the present invention.

[0071]

[0072] Mix levomilnacipran with calcium hydrogen phosphate and acrylic resin evenly, and set the mixing speed at 20-50 rpm; add 5% hydroxypropyl cellulose aqueous solution to prepare wet granules, and set the stirring speed for granulation to It is: 20-50 rev / min, cutting knife rotating speed is 30-80 rev / min; the above-mentioned wet granules are boiled and dried, the drying temperature is set at 50-90 degrees, and the drying time is 10-30 minutes; the dried Granules are arranged to obtain uniform dry granules, then magnesium stearate is added and mixed evenly, the mixing speed is 10-30 rpm, and the mixing time is 5-30 minutes; the above mixture is pressed into tablets, and the tableting speed is 10-30 minutes. 50 rpm, the hardness is controlled at 5-13kg.

[0073] In this case, only acrylic resin is used as the skeleton material, and calcium hydr...

Embodiment 3

[0080]

[0081] Mix levomilnacipran with calcium hydrogen phosphate and hypromellose K100M evenly, set the mixing speed at 20-50 rpm; then add acrylic resin (NE30D) and mix evenly, then add 5% hydroxyl The aqueous solution of propyl cellulose prepares wet granules, and the stirring speed of granulation is set as: 20-50 rpm, and the cutting knife rotating speed is 30-80 rpm; the above-mentioned wet granules are boiled and dried, and the drying temperature is set at 50-50 rpm. 90 degrees, the drying time is 10-30 minutes; arrange the dried granules to obtain uniform dry granules, then add magnesium stearate and mix evenly, the mixing speed is 10-30 rpm, and the mixing time is 5-30 minutes ; The above mixture is compressed into tablets, the tableting speed is 10-50 rpm, and the hardness is controlled at 5-13kg.

[0082] In this prescription, hypromellose is used as the skeleton material, calcium hydrogen phosphate is used as the filler, and acrylic resin (NE30D) is used as the...

[0001] This application is a divisional application with the patent application number "201210323131.4", the filing date is September 4, 2012, and the title of the invention is "a slow-release composition containing levomilnacipran and its preparation method". technical field

[0002] The invention relates to the technical field of pharmaceutical preparations, in particular to a sustained-release composition containing levomilnacipran and a preparation method thereof. Background technique

[0003] L-milnacipran entered clinical phase III in the United States in November 2009. L-milnacipran is the latest generation of antidepressant drugs at home and abroad.

[0004] Pharmacokinetic studies show that Levomilnacipran is rapidly absorbed after oral administration, and the blood concentration reaches its peak in about 1-2 hours, with a short elimination half-life. Ordinary Levomilnacipran tablets usually need to be taken 3 times a day to maintain the treatment. Therefore, it is ...

Examples

Embodiment 1

[0062]

[0063] Mix levomilnacipran with calcium hydrogen phosphate and hypromellose K4M evenly, and set the mixing speed at 20-50 rpm; add 5% hypromellose aqueous solution to prepare wet granules, and granulate Stirring speed is set as: 20-50 rpm, cutting knife speed is 30-80 rpm; the above wet particles are boiled and dried, the drying temperature is set at 50-90 degrees, and the drying time is 10-30 minutes; Arrange the dried granules to obtain uniform dry granules, then add magnesium stearate and mix evenly, the mixing speed is 10-30 rpm, and the mixing time is 5-30 minutes; press the above mixture into tablets, The speed is 10-50 rpm, and the hardness is controlled at 5-13kg.

[0064] In this case, only hypromellose was used as the skeleton material, calcium hydrogen phosphate was used as the filler, and no pH regulator was used.

[0065] Take this product, according to the release test method (Chinese Pharmacopoeia 2010 edition two appendix X D first method), using t...

Embodiment 2

[0070] This embodiment is only used for comparison and description, and is not the content of the present invention.

[0071]

[0072] Mix levomilnacipran with calcium hydrogen phosphate and acrylic resin evenly, and set the mixing speed at 20-50 rpm; add 5% hydroxypropyl cellulose aqueous solution to prepare wet granules, and set the stirring speed for granulation to It is: 20-50 rev / min, cutting knife rotating speed is 30-80 rev / min; the above-mentioned wet granules are boiled and dried, the drying temperature is set at 50-90 degrees, and the drying time is 10-30 minutes; the dried Granules are arranged to obtain uniform dry granules, then magnesium stearate is added and mixed evenly, the mixing speed is 10-30 rpm, and the mixing time is 5-30 minutes; the above mixture is pressed into tablets, and the tableting speed is 10-30 minutes. 50 rpm, the hardness is controlled at 5-13kg.

[0073] In this case, only acrylic resin is used as the skeleton material, and calcium hydr...

Embodiment 3

[0080]

[0081] Mix levomilnacipran with calcium hydrogen phosphate and hypromellose K100M evenly, set the mixing speed at 20-50 rpm; then add acrylic resin (NE30D) and mix evenly, then add 5% hydroxyl The aqueous solution of propyl cellulose prepares wet granules, and the stirring speed of granulation is set as: 20-50 rpm, and the cutting knife rotating speed is 30-80 rpm; the above-mentioned wet granules are boiled and dried, and the drying temperature is set at 50-50 rpm. 90 degrees, the drying time is 10-30 minutes; arrange the dried granules to obtain uniform dry granules, then add magnesium stearate and mix evenly, the mixing speed is 10-30 rpm, and the mixing time is 5-30 minutes ; The above mixture is compressed into tablets, the tableting speed is 10-50 rpm, and the hardness is controlled at 5-13kg.

[0082] In this prescription, hypromellose is used as the skeleton material, calcium hydrogen phosphate is used as the filler, and acrylic resin (NE30D) is used as the...

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