Slow release composition containing levomilnacipran and preparation method of composition

Abstract

The invention relates to a slow release composition containing levomilnacipran and a preparation method of the composition. The composition contains the following component in parts by weight: 10-70 parts of levomilnacipran or pharmaceutically acceptable salts thereof as an active ingredient and is characterized in that the composition also comprises the following components in parts by weight: 5-30 parts of high-viscosity hydroxypropyl methylcellulose as a hydrophilic gel slow release framework material and 3.5-7.5 parts of acrylic resin as a pH regulator. During preparation, the levomilnacipran, hydroxypropyl methylcellulose and acrylic resin are mixed fully and uniformly. The composition can achieve consistency of release behaviors in artificial gastric fluid and artificial intestinal fluid and sustained release effect can be kept for 12 hours; and the composition is low in preparation losses, high in efficiency and good in stability, simple to operate and easy to popularize.

Description

technical field

[0001] 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

[0002] 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.

[0003] 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 necessary to provide a sustained-release levomilnacipran sustained-release composition administered once or twice a day, so as to reduce the number of medications taken by patients and increase the adaptability of medication.

[0004] At present, milnacipran hyd...

Examples

Embodiment 1

[0059]

[0060] 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.

[0061] 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.

[0062] Take this product, according to the release test method (Chinese Pharmacopoeia 2010 edition two appendix X D first method), using t...

Embodiment 2

[0067] This embodiment is only used for comparison and description, and is not the content of the present invention.

[0068]

[0069] 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.

[0070] In this case, only acrylic resin is used as the skeleton material, and calcium hydr...

Embodiment 3

[0077]

[0078] 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.

[0079] 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...

technical field

[0001] 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

[0002] 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.

[0003] 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 necessary to provide a sustained-release levomilnacipran sustained-release composition administered once or twice a day, so as to reduce the number of medications taken by patients and increase the adaptability of medication.

[0004] At present, milnacipran hyd...

Examples

Embodiment 1

[0059]

[0060] 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.

[0061] 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.

[0062] Take this product, according to the release test method (Chinese Pharmacopoeia 2010 edition two appendix X D first method), using t...

Embodiment 2

[0067] This embodiment is only used for comparison and description, and is not the content of the present invention.

[0068]

[0069] 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.

[0070] In this case, only acrylic resin is used as the skeleton material, and calcium hydr...

Embodiment 3

[0077]

[0078] 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.

[0079] 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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