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Mosapride citrate sustained-release tablet

A technology of mosapride citrate and sustained-release tablets, which is applied in the direction of medical preparations of non-active ingredients, digestive system, organic active ingredients, etc., can solve the problem of increased repetitive research work, poor compliance, and differences in release Larger issues

Active Publication Date: 2012-02-01
重庆健能医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmacokinetic studies have shown that the half-life (t1 / 2) of mosapride citrate in the human body after oral administration is 2 hours, which requires administration 3 times a day to maintain effective blood drug concentration, and the compliance is poor. Release tablets can solve this problem
[0005] The process stability of sustained-release tablets has always been a difficult point in the development process of sustained-release tablets, which is mainly reflected in the process from laboratory preparation to mass production. The same prescription and process have large differences in release, and the prepared samples have undergone In the stability test, the change of the release rate is also relatively large. This difficulty has set up obstacles for the development of sustained-release preparations, and also added a lot of repetitive research work from laboratory scale-up to production, wasting a lot of manpower and material resources

Method used

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  • Mosapride citrate sustained-release tablet
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  • Mosapride citrate sustained-release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] 1. Prescription:

[0026] Mosapride citrate

15g

HPMC K4M

30g

HPMC K15M

15g

lactose

40g

80% ethanol solution

Appropriate amount

Magnesium stearate

2g

Opadry

2g

A total of 1000 pieces were made

[0027] 2. Process steps:

[0028] Take mosapride citrate, pulverize it and pass through a 100-mesh sieve, mix it with HPMCK4M, HPMCK15M and lactose, etc., moisten it with 80% ethanol, granulate it, dry it at 50°C, granulate it, add magnesium stearate, Mix evenly, press tablets, and coat with Opadry.

[0029] Release measurement method:

[0030] Get this product, according to dissolution assay (Chinese Pharmacopoeia version in 2005 two appendices XC second method), with 0.1mol / L hydrochloric acid solution 900ml as dissolution medium, rotating speed is 75 revolutions per minute, operate according to law, through 1, 6, After 12 hours, 10ml of the solution was taken, filtere...

Embodiment 2

[0039] 1. Prescription:

[0040] Mosapride citrate

15g

HPMC K4M

25g

HPMC K15M

10g

microcrystalline cellulose

40g

70% ethanol solution

Appropriate amount

Magnesium stearate

1g

Micropowder silica gel

1g

Opadry

1g

A total of 1000 pieces were made

[0041] 2. Process steps:

[0042] Take mosapride citrate, crush it and pass through a 100-mesh sieve, mix it evenly with HPMCK4M, HPMCK15M and microcrystalline cellulose, moisten it with 70% ethanol, granulate it, dry it at 50°C, granulate it, and add stearin Magnesium acid, micropowder silica gel, mixed evenly, pressed into tablets, coated with Opadry. The release measurement results are as follows:

[0043] time (h)

cumulative release %

1

32

6

65

12

94

[0044] In production, according to the prescription and process, the release of 10,000 and 100,...

Embodiment 3

[0050] 1. Prescription:

[0051] Mosapride citrate

15g

HPMC K4M

30g

HPMC K15M

10g

microcrystalline cellulose

20g

lactose

20g

70% ethanol solution

Appropriate amount

Magnesium stearate

2g

Opadry

3g

A total of 1000 pieces were made

[0052] 2. Process steps:

[0053] Take mosapride citrate, crush it and pass through a 100-mesh sieve, mix it with HPMCK4M, HPMCK15M, microcrystalline cellulose and lactose, etc., wet it with 70% ethanol and granulate it, dry it at 50°C and granulate it, add Magnesium stearate, mixed evenly, pressed into tablets, coated with Opadry. The release measurement results are as follows:

[0054] time (h)

cumulative release %

1

35

6

60

12

95

[0055] In production, according to the prescription and process, the release of 10,000 and 100,000 samples of samples is as follows...

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PUM

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Abstract

The invention discloses a mosapride citrate sustained-release tablet. The mosapride citrate sustained-release tablet comprises mosapride citrate, slow-release materials, a diluent, an adhesive, a lubricant and a coating material. A release degree of the mosapride citrate sustained-release tablet has good repeatability, regardless of being detected in an experiment or in mass production. After being subjected to stability monitoring for 6 months, the mosapride citrate sustained-release tablet still has an almost changeless release degree.

Description

technical field [0001] The invention relates to the technical field of drug sustained-release preparations, in particular to a mosapride citrate sustained-release tablet. Background technique [0002] Mosapride citrate, namely (±) 4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobenzyl)-2-morpholinyl]methyl}benzene Formamide citrate dihydrate, developed by Nippon Pharmaceutical Co., Ltd. See eg Japanese Patent JP3090274, US Patent US4807704, European Patent EP2043959. Mosapride citrate is the first potent and selective 5-HT4 receptor agonist, which increases the release of acetylcholine from nerve endings, thereby inducing or strengthening physiological movements and promoting the emptying of the digestive system. It is mainly used clinically for functional dyspepsia with heartburn, belching, nausea, vomiting, early satiety, upper abdominal distension and other gastrointestinal symptoms; it can also be used for gastroesophageal reflux disease, diabetic gastroparesis and partial ga...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/5375A61K47/38A61P1/14
Inventor 王国华胡延贵刘萍杨勇黄红菱罗成文
Owner 重庆健能医药开发有限公司
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