Rapidly-dissolving mosapride citrate composition

A technology of mosapride citrate and its composition, which is applied in the field of mosapride citrate composition, can solve problems such as prone to instability, increased production cost, and unfavorable quality control, so as to avoid instability , easy operation and low production cost

Active Publication Date: 2016-07-20
CHENGDU KANGHONG PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method needs to use organic reagents and carry out under heating conditions, which not only increases the production cost, but also brings certain safety hazards, and mosapride citrate itself is a heat-sensitive compound, which is prone to instability under hot and humid conditions; Moreover, the process steps of this method are complicated, and there are many parameter conditions to be controlled, which is not conducive to quality control in industrial mass production.

Method used

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  • Rapidly-dissolving mosapride citrate composition
  • Rapidly-dissolving mosapride citrate composition
  • Rapidly-dissolving mosapride citrate composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083]

[0084]According to the above prescription, take the API with a particle size D50 of 1.05um and fumed silica and add it to a pulverizer with a rotation speed of 4500 rpm, mix and pulverize it for 25 seconds to make a composition, and mix the prepared composition with mannitol, micro Crystalline cellulose is mixed, then sodium carboxymethyl starch is added, mixed evenly, passed through a 40-mesh sieve to disperse once, magnesium stearate is added for total mixing, mixed evenly, compressed into tablets, and obtained. Test the dissolution rate of the preparation according to the methods described in "1.1" and "1.2", and the results are as follows:

[0085] Table 7 embodiment 1 preparation dissolution investigation result

[0086]

Embodiment 2

[0088]

[0089] According to the above prescription, take the API with a particle size D50 of 1.7um and fumed silica and add it to a pulverizer with a rotating speed of 2000 rpm, mix and pulverize it for 40 seconds to make a composition, and mix the prepared composition with carboxymethyl starch Mix sodium and crospovidone, then add microcrystalline cellulose and sucrose, mix evenly, pass through a 40-mesh sieve to disperse once, add magnesium lauryl sulfate for total mixing, mix evenly, and press into tablets to obtain. Test the dissolution rate of the preparation according to the methods described in "1.1" and "1.2", and the results are as follows:

[0090] Table 8 embodiment 2 preparation dissolution investigation result

[0091]

Embodiment 3

[0093]

[0094] According to the above prescription, API with a particle size D50 of 1.7um and fumed silica were added to a pulverizer with a rotating speed of 1500 rpm, mixed and pulverized for 30 seconds to make a composition, and the prepared composition was mixed with aspartame Mix, then add low-substituted hydroxypropyl cellulose, microcrystalline cellulose, talcum powder, mix evenly, disperse once through a 40-mesh sieve, mix evenly, and press into tablets to obtain. Test the dissolution rate of the preparation according to the methods described in "1.1" and "1.2", and the results are as follows:

[0095] Table 9 Example 3 Preparation Dissolution Investigation Result

[0096]

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Abstract

The invention provides a rapidly-dissolving mosapride citrate composition, which comprises mosapride citrate and fumed silica. Mosapride citrate and fumed silica are mixed and crushed in a crushing machine, wherein mass ratio of mosapride citrate to fumed silica is 1:0.2-1.2; and particle size D50 of the mosapride citrate is less than or equal to 3.0 microns. The composition also contains one or more ingredients selected from a filler, a disintegrating agent, an adhesive, a lubricant, a flow aid and a flavouring agent. By the use of the mosapride citrate composition, dissolution rate of mosapride citrate in a buffer solution (a simulated intestinal fluid) with pH 6.8 is greatly raised, and medication effectiveness is raised for achlorhydria patients. The preparation technology is simple and is easy to operate. Any organic reagents are not used, and hot and humid process is not required. Instability of mosapride citrate in a hot and humid environment is avoided. The composition of the invention is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a fast-dissolving mosapride citrate composition. Background technique [0002] Mosapride citrate is the third-generation gastric motility drug developed by Nippon Pharmaceutical Co., Ltd. It is mainly used clinically for functional dyspepsia with heartburn, belching, nausea, vomiting, early satiety, upper abdominal distension and other gastrointestinal symptoms . Its chemical name is (±)-4-amino-5-chloro-2-ethoxy-N-{[4-(4-fluorobenzyl)-2-morphinyl]methyl}toluamide citrate Dihydrate, which has the formula C 21 h 25 ClFN 3 o 3 ·C 6 h 8 o 7 2H 2 O, the molecular weight is 650.05, and the structural formula is [0003] [0004] Mosapride citrate tablets were approved for marketing in my country in 1999, with clinical specifications of 2.5 mg and 5 mg. Mosapride citrate is a BCS class II drug, and its solubility in water is extremely low. For solid preparations of such drugs, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5375A61K47/04A61K47/38A61K47/36A61P1/14A61P1/08
Inventor 柯潇郑强叶启丞高波
Owner CHENGDU KANGHONG PHARMA GRP
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