CN104188927A - Mosapride citrate tablet and preparation method thereof - Google Patents
Mosapride citrate tablet and preparation method thereof Download PDFInfo
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- CN104188927A CN104188927A CN201410441759.3A CN201410441759A CN104188927A CN 104188927 A CN104188927 A CN 104188927A CN 201410441759 A CN201410441759 A CN 201410441759A CN 104188927 A CN104188927 A CN 104188927A
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Abstract
The invention discloses a mosapride citrate tablet. The preparation method comprises the following steps: dissolving citric acid in ethanol, adding raw materials of mosapride citrate, stirring until the raw materials are dissolved, and drying the solution to obtain a mixture; mixing the mixture with pharmaceutically acceptable accessories and tabletting. Compared with the prior art, the tablet disclosed by the invention can be rapidly dissolved in water; and the preparation process is simple.
Description
Technical field
The invention belongs to medical technical field, be specifically related to a kind of Mosapride Citrate Tablets agent and preparation method thereof.
Background technology
Mosapride citrate (Mosapride Citrate), chemistry 4-amino-5-chloro-2-ethoxy-N-[[4-(4-luorobenzyl)-2-morpholinyl by name] methyl] Benzoylamide citrate, for white or off-white color crystalline powder, odorless, micro-hardship.143～145 DEG C of fusing points.Be soluble in dimethyl formamide and pyridine, be slightly soluble in methanol, be insoluble in 95% ethanol, water insoluble or ether.
Mosapride citrate is novel third generation medicine for stomach dynamic, be mainly used in functional dyspepsia with heartburn, belch, feel sick, vomiting, the symptom of digestive tract such as full, big belly early.This medicine can strengthen gastrointestinal motility, but does not affect gastric acid secretion, and simultaneously without the side effect such as the extrapyramidal symptoms and diarrhoea, and toleration is good.
Oral solid formulation all needs through process in leaching after entering in body, could see through biomembrane and be absorbed by body.But because mosapride citrate is insoluble drug, water-soluble hardly, in the actual production of Mosapride citrate oral solid preparation, often run into the low even underproof problem of dissolution; And because the content of mosapride citrate in preparation is lower, be difficult in the preparation fully mix, have the problem that between low, sheet, stripping differs greatly carrying out often having height when dissolution detects.Clinical in the urgent need in quick-acting, high-efficiency preparation, solve insoluble drug because dissolubility is little, to cause the problem that bioavailability is low be slowly a great problem of pharmaceuticals industry always in stripping.
CN101816639B discloses a kind of tablet that contains mosapride citrate and preparation method thereof.Mosapride citrate is added in dehydrated alcohol, 60 DEG C～65 DEG C heating in water bath add water-solubility carrier material stirring to make its dissolving after dissolving completely, then solution is gone in Rotary Evaporators, 60 DEG C remove ethanol under reduced pressure, make solid dispersion, then be further processed into tablet, technique is comparatively complicated.
CN101273973B disclose a kind of prepare with direct powder compression contain pharmaceutical composition of mosapride citrate and preparation method thereof.In invention, require the quick disintegrate of tablet, but for insoluble drug, after disintegrate, medicine also differs and is dissolved in surely in dissolution medium fast.
In prior art, for the problem that improves mosapride citrate dissolubility, be not reported, and for insoluble drug mosapride citrate, as long as can improve dissolubility, dissolution should have corresponding raising.
Summary of the invention
For the deficiencies in the prior art, the present invention intends providing a kind of dissolution better Mosapride Citrate Tablets agent.
Inventor has carried out great many of experiments, finds unexpectedly, while mosapride citrate being added in the ethanol solution that contains citric acid, mosapride citrate can dissolve completely, then this solution is dry, obtain mixture, this mixture dissolubility in water significantly improves.May be under the prerequisite that adds citric acid, JUYUANSUNMOSHABILI and ethanol have formed mosapride citrate ethanol compound, thereby have improved dissolubility.
Further mixture and pharmaceutically acceptable adjuvant are mixed, tabletting, obtain stripping Mosapride Citrate Tablets agent rapidly.
Particularly, the present invention realizes by following technology:
A kind of Mosapride Citrate Tablets agent, by the following method preparation: citric acid is dissolved in ethanol, adds mosapride citrate raw material, be stirred to dissolve, and dry this solution, obtains mixture; Then this mixture is mixed to tabletting with pharmaceutically acceptable adjuvant.
In described Mosapride Citrate Tablets agent, the weight ratio of mosapride citrate and citric acid is 1:0.1～0.5.
Preferably, the weight ratio of mosapride citrate and citric acid is 1:0.2～0.3.
Described pharmaceutically acceptable adjuvant is filler, disintegrating agent and lubricant.
Described filler is selected from one or more in lactose, microcrystalline Cellulose and starch.
Described disintegrating agent is selected from one or more in carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone.
Described lubricant is selected from one or more in magnesium stearate, Pulvis Talci and silicon dioxide.
Compared with prior art, preparation technology of the present invention is simple, and drug-eluting is rapid, is applicable to suitability for industrialized production.
Detailed description of the invention
Following examples further describe beneficial effect of the present invention, embodiment is only for the object of illustration, do not limit the scope of the invention, within the apparent change that those of ordinary skill in the art make according to the present invention simultaneously and modification are also contained in the scope of the invention.
Embodiment 1
Preparation technology:
Recipe quantity takes citric acid and is dissolved in ethanol, adds the mosapride citrate raw material of recipe quantity, is stirred to dissolve, and 50 DEG C of these solution of drying under reduced pressure, obtain the mixture that contains citric acid and mosapride citrate; This mixture is crossed to 16 mesh sieves, then mix homogeneously with the mixed powder of microcrystalline Cellulose and carboxymethyl starch sodium, add magnesium stearate to mix, tabletting.
Embodiment 2
Preparation technology:
Recipe quantity takes citric acid and is dissolved in ethanol, adds the mosapride citrate raw material of recipe quantity, is stirred to dissolve, and 55 DEG C of these solution of drying under reduced pressure, obtain the mixture that contains citric acid and mosapride citrate; This mixture is crossed to 20 mesh sieves, then mix homogeneously with the mixed powder of microcrystalline Cellulose, lactose, carboxymethyl starch sodium and polyvinylpolypyrrolidone, add magnesium stearate to mix, tabletting.
Embodiment 3
Preparation technology:
Recipe quantity takes citric acid and is dissolved in ethanol, adds the mosapride citrate raw material of recipe quantity, is stirred to dissolve, and 55 DEG C of these solution of drying under reduced pressure, obtain the mixture that contains citric acid and mosapride citrate; This mixture is crossed to 20 mesh sieves, then mix homogeneously with the mixed powder of microcrystalline Cellulose and polyvinylpolypyrrolidone, add magnesium stearate to mix, tabletting.
Embodiment 4
Preparation technology:
Recipe quantity takes citric acid and is dissolved in ethanol, adds the mosapride citrate raw material of recipe quantity, is stirred to dissolve, and 50 DEG C of these solution of drying under reduced pressure, obtain the mixture that contains citric acid and mosapride citrate; This mixture is crossed to 16 mesh sieves, then mix homogeneously with the mixed powder of microcrystalline Cellulose and carboxymethyl starch sodium, add magnesium stearate to mix, tabletting.
Comparative example 1
Preparation technology:
Recipe quantity takes citric acid and is dissolved in ethanol, adds the mosapride citrate raw material of recipe quantity, is stirred to dissolve, and 55 DEG C of these solution of drying under reduced pressure, obtain the mixture that contains tartaric acid and mosapride citrate; This mixture is crossed to 20 mesh sieves, then mix homogeneously with the mixed powder of microcrystalline Cellulose and polyvinylpolypyrrolidone, add magnesium stearate to mix, tabletting.
Comparative example 2
Preparation technology:
Mosapride citrate is crossed 150 mesh sieves, and recipe quantity takes, and then mixs homogeneously with the mixed powder of microcrystalline Cellulose and polyvinylpolypyrrolidone, adds magnesium stearate to mix, tabletting.
Comparative example 3
Preparation technology:
Recipe quantity takes citric acid and is dissolved in methanol, adds the mosapride citrate raw material of recipe quantity, is stirred to dissolve, and 55 DEG C of these solution of drying under reduced pressure, obtain the mixture that contains tartaric acid and mosapride citrate; This mixture is crossed to 20 mesh sieves, then mix homogeneously with the mixed powder of microcrystalline Cellulose and polyvinylpolypyrrolidone, add magnesium stearate to mix, tabletting.
Checking embodiment
Dissolution determination.Chromatographic condition and system suitability octadecylsilane chemically bonded silica are filler; Taking the citric acid soln of 0.05mol/L (regulating pH value to 4.0 with the sodium hydroxide solution of 2mol/L) ,-acetonitrile (65: 35) is as mobile phase, and detection wavelength is 274nm, and number of theoretical plate is not less than 2000 by the calculating of mosapride peak.
Get this product, according to dissolution method (two annex X C the second methods of Chinese Pharmacopoeia version in 2010), taking phosphate buffer (pH6.8) 900ml as dissolution medium, rotating speed is per minute 50 to turn, and operation in accordance with the law, in the time of 5min, 30min, get respectively solution appropriate, filter, discard just filtrate of 10ml, get subsequent filtrate as need testing solution; Separately get mosapride citrate reference substance appropriate, accurately weighed, add dissolve with methanol and quantitatively dilution make in every 1ml the approximately solution containing 0.28mg, precision measures 1ml, puts in 50ml measuring bottle, is diluted to scale with dissolution medium, shakes up, in contrast product solution.Precision measures need testing solution and the each 100 μ l of reference substance solution, and injection liquid chromatography, records chromatogram respectively.Stripping quantity by external standard method with every bag of calculated by peak area.Limit is 70% of labelled amount, should conform with the regulations.
Table 1. embodiment measurement result
As seen from the table, embodiment of the present invention drug-eluting is rapid, and the basic stripping of 5min is complete; Comparative example 1, replaces citric acid with tartaric acid, may be that solubilizing effect is poor compared with citric acid, therefore dissolution weak effect; Comparative example 2, adopt prior art, and raw material is sieved, and poor because of drug solubility, therefore stripping is the slowest; Comparative example 3, replace ethanol with methanol, may be not form mosapride citrate ethanol compound, and stripping is slow compared with the embodiment of the present invention.
Claims (8)
1. a Mosapride Citrate Tablets agent, is characterized in that, by the following method preparation: citric acid is dissolved in ethanol, adds mosapride citrate raw material, is stirred to dissolve, and dry this solution, obtains mixture; Then this mixture is mixed to tabletting with pharmaceutically acceptable adjuvant.
2. Mosapride Citrate Tablets agent according to claim 1, is characterized in that, the weight ratio of mosapride citrate and citric acid is 1:0.1～0.5.
3. Mosapride Citrate Tablets agent according to claim 1, is characterized in that, the weight ratio of mosapride citrate and citric acid is 1:0.2～0.3.
4. Mosapride Citrate Tablets agent according to claim 1, is characterized in that, pharmaceutically acceptable adjuvant is filler, disintegrating agent and lubricant.
5. Mosapride Citrate Tablets agent according to claim 4, is characterized in that, described filler is selected from one or more in lactose, microcrystalline Cellulose and starch.
6. Mosapride Citrate Tablets agent according to claim 4, is characterized in that, described disintegrating agent is selected from one or more in carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone.
7. Mosapride Citrate Tablets agent according to claim 4, is characterized in that, described lubricant is selected from one or more in magnesium stearate, Pulvis Talci and silicon dioxide.
8. the preparation method of Mosapride Citrate Tablets agent according to claim 1, is characterized in that, it comprises the steps: that citric acid is dissolved in ethanol, adds mosapride citrate raw material, is stirred to dissolve, and dry this solution, obtains mixture; Then this mixture is mixed to tabletting with pharmaceutically acceptable adjuvant.
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| CN201410441759.3A CN104188927B (en) | 2014-09-01 | 2014-09-01 | A kind of Mosapride Citrate Tablets agent and preparation method thereof |
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| CN201410441759.3A CN104188927B (en) | 2014-09-01 | 2014-09-01 | A kind of Mosapride Citrate Tablets agent and preparation method thereof |
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| CN104188927B CN104188927B (en) | 2019-04-05 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104622826A (en) * | 2015-03-02 | 2015-05-20 | 孙巧玲 | Mosapride citrate tablet and preparation method thereof |
| CN106214657A (en) * | 2016-09-06 | 2016-12-14 | 江苏豪森药业集团有限公司 | Thin membrane coated tablet of mosapride citrate and preparation method thereof |
| CN107684548A (en) * | 2017-09-19 | 2018-02-13 | 鲁南制药集团股份有限公司 | A kind of mosapride citrate preparation and preparation method thereof |
| CN114560822A (en) * | 2020-11-27 | 2022-05-31 | 鲁南制药集团股份有限公司 | Mosapride dicarboxylic acid crystal |
| CN114560822B (en) * | 2020-11-27 | 2024-05-28 | 鲁南制药集团股份有限公司 | Mosapride dicarboxylic acid crystal |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101816639A (en) * | 2010-01-15 | 2010-09-01 | 鲁南制药集团股份有限公司 | Tablets of mosapride citrate and preparation method thereof |
-
2014
- 2014-09-01 CN CN201410441759.3A patent/CN104188927B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101816639A (en) * | 2010-01-15 | 2010-09-01 | 鲁南制药集团股份有限公司 | Tablets of mosapride citrate and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 张之荣: "《药剂学》", 31 December 2007, 高等教育出版社 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104622826A (en) * | 2015-03-02 | 2015-05-20 | 孙巧玲 | Mosapride citrate tablet and preparation method thereof |
| CN106214657A (en) * | 2016-09-06 | 2016-12-14 | 江苏豪森药业集团有限公司 | Thin membrane coated tablet of mosapride citrate and preparation method thereof |
| CN106214657B (en) * | 2016-09-06 | 2018-04-06 | 江苏豪森药业集团有限公司 | Thin membrane coated tablet of mosapride citrate and preparation method thereof |
| CN107684548A (en) * | 2017-09-19 | 2018-02-13 | 鲁南制药集团股份有限公司 | A kind of mosapride citrate preparation and preparation method thereof |
| CN114560822A (en) * | 2020-11-27 | 2022-05-31 | 鲁南制药集团股份有限公司 | Mosapride dicarboxylic acid crystal |
| CN114560822B (en) * | 2020-11-27 | 2024-05-28 | 鲁南制药集团股份有限公司 | Mosapride dicarboxylic acid crystal |
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| CN104188927B (en) | 2019-04-05 |
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