CN104069082B - A kind of aspartic acid piece and preparation method thereof - Google Patents
A kind of aspartic acid piece and preparation method thereof Download PDFInfo
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- CN104069082B CN104069082B CN201310095733.3A CN201310095733A CN104069082B CN 104069082 B CN104069082 B CN 104069082B CN 201310095733 A CN201310095733 A CN 201310095733A CN 104069082 B CN104069082 B CN 104069082B
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- aspartic acid
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Abstract
The present invention relates to a kind of aspartic acid piece and preparation method thereof.The aspartic acid piece includes label and coating, and the label contains aspartic acid and pharmaceutically acceptable auxiliary material.Wherein auxiliary material includes waxy auxiliary material and other auxiliary materials.Said preparation contains aspartic acid 30~90%, waxy auxiliary material 0.5~20% by weight percentage.Waxy auxiliary material is the one or more in tristerin, glycerin monostearate, stearic acid, insect wax, beeswax, octadecyl alcolol.Compared with the aspartic acid piece for not adding above-mentioned auxiliary material, in its preparation process, the hygroscopicity of material substantially reduces aspartic acid piece of the invention, and compressibility significantly improves, the increase of the stability of finished product, reduces aspartic acid piece and prepares difficulty and production cost.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of aspartic acid piece and preparation method thereof.
Background technology
L-ASPARTIC ACID potassium is a kind of benefit potassium preparation, and its molecular formula is C4H6KNO4·1/2H2O, structural formula are：
Potassium is intracellular dominant cation, required for cells survival, has a variety of physiological actions.98% potassium is present
In intracellular, extracellular fluid only contains 2%.Potassium in extracellular fluid mainly exists with ionic condition, in intracellular fluid potassium divided by from
Outside sub- state is present, a part is combined with protein, and another part is combined with sugar and phosphate.Potassium is in cell metabolism, maintenance
Intracellular fluid osmotic pressure, keep intraor extracellular acid-base balance, the transmission of nerve impulse, contraction of muscle, myocardial excitability, self-disciplining
All played an important role with the maintenance of conductibility and normal organ function etc..
Precursor of the L-aminobutanedioic acid as internal oxaloacetic acid, plays an important role, and participate in ornithine in tricarboxylic acid cycle
Circulation, ammonia and carbon dioxide is combined generation urea, reduce the content of ammonia and carbon dioxide in blood.L-aminobutanedioic acid is affine with cell
Power is strong, potassium ion can be made to return into the cell, promote cell depolarization and cell metabolism, maintaining it just as the carrier of potassium ion
Chang Gongneng.
Clinically many reasons can cause hypopotassaemia, as hypoalimentation, vomiting, severe diarrhea, using row potassium diuresis
The reason such as caused hypopotassaemia after agent, mistake potassium nephrosis and prolonged application glucocorticoid and supplement hypertonic glucose.Low potassium
The resting potential of myocardial cell membrane can be influenceed, inspires aberrant conduction and reentry phenomenon, forms severe arrhythmia, increases digitalis
The incidence of poisoning；The neuro-muscular disorders such as myasthenia, paralysis, respiratory insufficiency can be caused simultaneously, can also result in striated muscle
Dissolving, electrocardiographic abnormality and intestinal obstruction.Long-term Diagnostic value causes renal damage (Diagnostic value nephrosis).
Aspartic acid is the kind that Italian pharmacopeia is recorded, and is also recorded in the 32nd edition big pharmacopeia of Martindale（The
32th Edition Martindial Pharmacopeia）With《Japanese pharmaceutical product collection》.There are more pharmacy corporation productions in Japan
This product, Tian Bian drugmakers produce the tablet, powder and parenteral solution of this product, republicanism medicine company, the tablet of colleague's medicine production this product
Deng.
Aspartic acid piece regular size is 0.3g, and drugloading rate is larger, and aspartic acid raw material have it is very strong draw it is wet
Property, its compressibility is also very poor, easily occurs material moisture absorption sticking in tableting processes, the problem of tablet sliver.
The content of the invention
Based on aspartic acid piece material moisture absorption sticking, the feelings of tablet sliver easily occur in tableting processes for the present invention
Condition, studied by repetition test, finally draw a kind of L-aminobutanedioic acid potassium tablets and preparation method thereof.The aspartic acid of the present invention
In its preparation process, the hygroscopicity of material substantially reduces piece, and compressibility significantly improves, the increase of the stability of finished product, reduces door
Winter propylhomoserin potassium piece prepares difficulty and production cost.
The aspartic acid piece of the present invention, including label and coating, the label contain aspartic acid and pharmaceutically may be used
The auxiliary material of receiving, the pharmaceutically acceptable auxiliary material include waxy auxiliary material.By adding waxy auxiliary material, pressure can be obviously improved
During piece, the problem of the material moisture absorption, and increase compressibility.
In addition, label also includes other appropriate auxiliary materials.
Wherein, the waxy auxiliary material be tristerin, glycerin monostearate, stearic acid, insect wax, beeswax,
One or more in octadecyl alcolol.
Other described auxiliary materials include the auxiliary materials such as filler, disintegrant, adhesive, glidant, and specifically, filler can
One or more selected from sucrose, mannitol, starch, microcrystalline cellulose, lactose, dextrin etc.；Disintegrant may be selected from hydroxypropyl fibre
Tie up the one or more of element, sodium carboxymethyl starch, PVPP etc.；Adhesive may be selected from PVP, hydroxypropyl methyl fiber
Element, absolute ethyl alcohol, various concentration ethanol-water solution etc. one or more；Glidant may be selected from talcum powder, differential silica gel etc.
One or more.
Specifically, label includes following component, and its content is to account for the percentages of label weight：
Aspartic acid 30~90%；
Waxy auxiliary material 0.5~20%；
Other auxiliary material surpluses.
Preferably, the content of each part of label is（To account for the percentages of label weight）：
Aspartic acid 50~70%；
Waxy auxiliary material 5~10%；
Other auxiliary material surpluses.
In addition, the aspartic acid piece of the present invention, include coating, the weight of the coating be label weight 1.0~
5.0%.Coated tablet can reduce the hygroscopicity of aspartic acid piece, increase the stability of tablet.
The present invention also provides a kind of preparation method of the aspartic acid piece, comprises the following steps：
（1）Prepare the label of described aspartic acid piece；
（2）In the label Surface coating film coating.
Wherein, step（1）It is middle that the label is prepared using wet granule compression tablet method.Concretely comprise the following steps：Weigh waxy auxiliary
Material, ethanol in proper amount is added, dissolved by heating, as adhesive；Weigh aspartic acid and filler, disintegrant and other bondings
The auxiliary materials such as agent are well mixed, and are added solution obtained above, are stirred, and sieving granulation, are dried, whole grain, are added glidant and are mixed
Close uniform；Tabletting.
Waxy auxiliary material of the present invention, be not only able to reduce material hygroscopicity, while also have concurrently lubricant and
The effect of adhesive：Ejection force can be reduced as lubricant, the phenomenon of sliver can be improved as adhesive.
It is an advantage of the invention that：Compared with prior art, aspartic acid piece of the invention can significantly reduce thing before tabletting
The hygroscopicity of material, the compressibility of material is improved, reduce the hygroscopicity of tablet, so as to increase the stability of finished product, reduce door winter ammonia
Sour potassium piece prepares difficulty and production cost.
Brief description of the drawings
Fig. 1：The sucting wet curve of aspartic acid（25℃）
Fig. 2：Aspartic acid of the present invention is from film-making and reference preparation stripping curve figure in water
Fig. 3：Aspartic acid of the present invention is from film-making and reference preparation stripping curve figure in pH1.2 hydrochloric acid solutions
Fig. 4：Aspartic acid of the present invention is from film-making and reference preparation stripping curve figure in pH4.0 phosphate buffers
Fig. 5：Aspartic acid of the present invention is from film-making and reference preparation stripping curve figure in pH6.8 phosphate buffers
Embodiment
The present invention is further illustrated below by specific embodiment, following embodiments are to be used to illustrate rather than
Limitation of the present invention, claimed model is belonged to according to the simple modifications that the essence of the present invention is carried out to the present invention
Enclose.
Embodiment 1
Composition：
Preparation method：
（1）The configuration of adhesive：Stearic acid 30g is weighed, adds 210g ethanol（95%）In, heating dissolves stearic acid, makees
For adhesive；
（2）Granulation：Weigh aspartic acid, microcrystalline cellulose is well mixed, add adhesive, stir, with 18 mesh
Nylon screen is pelletized；The drying 4 hours of 60 DEG C of heated-air circulation oven；16 mesh whole grains, add talcum powder and be well mixed；
（3）Tabletting：Using rotary pelleting machine, tabletting, piece weighs about 0.5g；
（4）Coating：Use Opadry（Trade name, block happy Kanggong department manufacture）Coating, on the basis of plain piece, stomach dissolved type moisture-proofing
Coating weight gain 3%.
In the present embodiment：
（1）Stearic acid dosage in Core formulation is 6%, and stearic acid is hydrophobic material, after being mixed with aspartic acid,
Reduce aspartic acid surface area, reduce the hygroscopicity of mixed material.
（2）Stearic fusing point is relatively low, is melted during tabletting, is impregnated into unclassified stores, increases storeroom
Adhesion, sliver is prevented, there is adhesive.
（3）Stearic acid is wax material, has the function that lubricant.
Stearic acid is not only able to reduce the hygroscopicity of material in this prescription, and being alternatively arranged as lubricant reduces ejection force, also
The phenomenon of sliver can be improved as adhesive.
Embodiment 2
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 3%.
Composition：
Embodiment 3
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 3%.
Composition：
Embodiment 4
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 3%.
Composition：
Embodiment 5
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 3%.
Composition：
Embodiment 6
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 3%.
Composition：
Embodiment 7
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 5%.
Composition：
Embodiment 8
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 4%.
Composition：
Embodiment 9
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 1%.
Composition：
Embodiment 10
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result using plain piece as
Benchmark, stomach dissolved type moisture-proofing coating weight gain about 3%.
Composition：
Experimental example 1
The measure of material sucting wet curve
1. test specimen
Aspartic acid raw material（It crushed 100 mesh sieves）；Stearic acid（It crushed 100 mesh sieves）；Octadecyl alcolol（It crushed 100
Mesh sieve）
2. experimental method
（1）The saturated solution of different salt is respectively configured, puts in drier, makes to reach certain humidity in closed environment.
（2）Aspartic acid raw material about 3.0g is weighed, is put in measuring cup, tiling makes thickness be less than 5mm, puts each drier
In, place 10 days, taking-up is weighed, and calculates moisture absorption weightening.
（3）Aspartic acid and stearic acid are pressed 9 with method：After 1 ratio ground and mixed is uniform, about 3.0g is weighed, puts title
In measuring bottle, tiling makes thickness be less than 5mm, puts in each drier, places 10 days, and taking-up is weighed, and calculates moisture absorption weightening.
（4）Aspartic acid and octadecyl alcolol are pressed 9 with method：After 1 ratio ground and mixed is uniform, about 3.0g is weighed, puts title
In measuring bottle, tiling makes thickness be less than 5mm, puts in each drier, places 10 days, and taking-up is weighed, and calculates moisture absorption weightening.
3. result of the test
Experimental result is shown in Table 1, Fig. 1.
The moisture absorption of table 1 weightening experimental result
According to experimental result, aspartic acid raw material critical relative moisture is about 59%, after mixing stearic acid and octadecyl alcolol
Moisture absorption substantially reduces, and critical relative moisture is increased to 65%, 63%, and stearic acid or octadecyl alcolol and aspartic acid raw material hybrid energy are bright
The aobvious hygroscopicity for improving aspartic acid raw material.
Experimental example 2
The determination experiment of dissolution rate
1. sample
Aspartic acid piece of the present invention, is prepared according to the embodiment of the present invention 1.
2. experimental method
With Chinese Pharmacopoeia two the second methods of annex X C measure aspartic acid piece dissolution rates of version in 2010.Respectively with water,
PH1.2 hydrochloric acid solutions, pH4.0 phosphate buffers, pH6.8 phosphate buffers（Configured by Japanese official method）900ml is
Dissolution medium, as a result as shown in Fig. 2~5.
3. experimental result
It can be seen from Fig. 2~5, aspartic acid piece and reference stripping curve of the present invention are consistent substantially.
Claims (7)
1. a kind of aspartic acid piece, including label and coating, the label contains aspartic acid and pharmaceutically acceptable
Auxiliary material, it is characterised in that the pharmaceutically acceptable auxiliary material includes waxy auxiliary material, and the label by weight percentage contains a winter
Propylhomoserin potassium 30~90%, waxy auxiliary material 0.5~20%；Described waxy auxiliary material is that tristerin, stearic acid, worm are white
One or more in wax, beeswax, octadecyl alcolol.
2. aspartic acid piece according to claim 1, it is characterised in that in the label containing aspartic acid 50~
70%, waxy auxiliary material 5~10%.
3. aspartic acid piece according to claim 1, it is characterised in that label is also containing other appropriate auxiliary materials.
4. aspartic acid piece according to claim 3, it is characterised in that other described auxiliary materials include filler, disintegration
Agent, adhesive, glidant.
5. aspartic acid piece according to claim 1, it is characterised in that the weight of the coating is label weight
1.0~5.0%.
6. according to the preparation method of any described aspartic acid piece of Claims 1 to 5, comprise the following steps：
（1）Prepare the label of described aspartic acid piece；
（2）In the label Surface coating film coating.
7. according to the method for claim 6, it is characterised in that in step（1）It is middle that institute is prepared using wet granule compression tablet method
Label is stated, is concretely comprised the following steps：Waxy auxiliary material is weighed, adds ethanol in proper amount, is dissolved by heating, as adhesive；Weigh a winter ammonia
Sour potassium and filler, disintegrant and other adhesives are well mixed, and are added solution obtained above, are stirred, and cross sieve series
Grain, dry, whole grain, add glidant and be well mixed；Tabletting.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310095733.3A CN104069082B (en) | 2013-03-25 | 2013-03-25 | A kind of aspartic acid piece and preparation method thereof |
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| CN201310095733.3A CN104069082B (en) | 2013-03-25 | 2013-03-25 | A kind of aspartic acid piece and preparation method thereof |
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| CN104069082A CN104069082A (en) | 2014-10-01 |
| CN104069082B true CN104069082B (en) | 2017-12-05 |
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Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105982875A (en) * | 2014-12-27 | 2016-10-05 | 辽宁药联制药有限公司 | Venlafaxine sustained release preparation using waxy material as skeleton and having sustained release effect and preparation method thereof |
| CN107303287A (en) * | 2016-04-21 | 2017-10-31 | 辽宁药联制药有限公司 | A kind of preparation method of the moistureproof piller of aspartic acid |
| CN107432870A (en) * | 2016-05-25 | 2017-12-05 | 辽宁药联制药有限公司 | A kind of aspartic acid capsule and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1439629A (en) * | 2003-03-21 | 2003-09-03 | 于航 | Laevo potassium aspartate material and preparation therefrom and preparing method thereof |
| CN101234992A (en) * | 2008-03-10 | 2008-08-06 | 北京京卫信康医药科技发展有限公司 | Method for preparing aspartic acid |
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2013
- 2013-03-25 CN CN201310095733.3A patent/CN104069082B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1439629A (en) * | 2003-03-21 | 2003-09-03 | 于航 | Laevo potassium aspartate material and preparation therefrom and preparing method thereof |
| CN101234992A (en) * | 2008-03-10 | 2008-08-06 | 北京京卫信康医药科技发展有限公司 | Method for preparing aspartic acid |
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