CN104069082A - Potassium aspartate tablet and preparation method thereof - Google Patents
Potassium aspartate tablet and preparation method thereof Download PDFInfo
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- CN104069082A CN104069082A CN201310095733.3A CN201310095733A CN104069082A CN 104069082 A CN104069082 A CN 104069082A CN 201310095733 A CN201310095733 A CN 201310095733A CN 104069082 A CN104069082 A CN 104069082A
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- aspartic acid
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Abstract
The invention relates to a potassium aspartate tablet and a preparation method thereof. The potassium aspartate tablet comprises a tablet core and a coating, wherein the tablet core contains potassium aspartate and pharmaceutically acceptable adjuvant. The adjuvant comprises waxy adjuvant and other adjuvant. The tablet comprises, by weight, 30 to 90% of potassium aspartate and 0.5 to 20% of the waxy adjuvant, wherein the waxy adjuvant is one or more selected from the group consisting of glyceryl stearate, glyceryl monostearate, stearic acid, Chinese wax, beeswax and octadecanol. Compared with a potassium aspartate tablet without the above-mentioned adjuvant, the potassium aspartate tablet provided by the invention has the following advantages: in the preparation process of the potassium aspartate tablet, material hygroscopicity is obviously reduced, compressibility is obviously improved, stability of the finished tablet is enhanced, and preparation difficulty and production cost of the potassium aspartate tablet are decreased.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of aspartic acid sheet and preparation method thereof.
Background technology
L-ASPARTIC ACID potassium is a kind of kalium replenishment preparation, and its molecular formula is C
4h
6kNO
41/2H
2o, structural formula is:
Potassium is intracellular main cation, essential by cells survival, has multiple physiological action.98% potassium is present in cell, and extracellular fluid only contains 2%.Potassium in extracellular fluid mainly exists with ionic condition, outside in intracellular fluid, potassium exists divided by ionic condition, and a part and protein bound, another part combines with sugar and phosphate.Potassium at cellular metabolism, maintain intracellular fluid osmotic pressure, keep the aspects such as maintaining of transmission, muscle contraction, myocardial excitability, self-disciplining and the conductivity of acid-base balance inside and outside cell, neural impulse and normal organ function all to play an important role.
Aspartic Acid, as the precursor of oxaloacetic acid in body, plays an important role in tricarboxylic acid cycle, and participates in ornithine cycle, makes ammonia and carbon dioxide in conjunction with generating carbamide, the content of ammonia and carbon dioxide in reduction blood.Aspartic Acid and cellular affinity are strong, can be used as the carrier of potassium ion, and potassium ion is returned in cell, promote cell depolarization and cellular metabolism, maintain its normal function.
Many reasons can cause hypokalemia clinically, as reasons such as the hypokalemia causing after hypoalimentation, vomiting, severe diarrhea, application row potassium diuretic, mistake potassium nephropathy and prolonged application glucocorticoid and supplementary hypertonic glucose.Low potassium can affect the resting potential of myocardial cell membrane, inspires difference conduction and reentry phenomenon, forms severe arrhythmia, increases the incidence rate of digitalism; Can cause the neuromuscular disorders such as myasthenia, paralysis, respiratory insufficiency, also can cause rhabdomyolysis, electrocardiographic abnormality and intestinal obstruction simultaneously.Long-term hypokalemia causes injury of renal tubular (hypokalemia nephropathy).
Aspartic acid is the kind that Italian pharmacopeia is recorded, and also records in the 32nd edition large pharmacopeia of Martindale (The 32th Edition Martindial Pharmacopeia) and " Japanese pharmaceuticals collection ".There are many pharmacy corporation production this product in Japan, tablet, powder and the injection of Tian Bian drugmaker production this product, the tablet of republicanism Pharmaceutical, colleague's medicine production this product etc.
Aspartic acid sheet regular size is 0.3g, and drug loading is larger, and aspartic acid raw material has and very strong draw moistly, and its compressibility is also very poor, and material moisture absorption sticking very easily occurs in tabletting process, the problem of tablet sliver.
Summary of the invention
The present invention is based on aspartic acid sheet material moisture absorption sticking very easily occurs in tabletting process, the situation of tablet sliver, through repetition test research, finally draws a kind of Aspartic Acid potassium tablets and preparation method thereof.Aspartic acid sheet of the present invention is in its preparation process, and the hygroscopicity of material obviously reduces, and compressibility obviously improves, the stability of finished product increases, and reduces aspartic acid sheet and prepares difficulty and production cost.
Aspartic acid sheet of the present invention, comprises label and coating, and described label contains aspartic acid and pharmaceutically acceptable adjuvant, and this pharmaceutically acceptable adjuvant comprises waxiness adjuvant.By adding waxiness adjuvant, can obviously improve in tabletting process, the problem of the material moisture absorption, and increase compressibility.
In addition, label also comprises other appropriate adjuvants.
Wherein, described waxiness adjuvant is one or more in tristerin, glyceryl monostearate, stearic acid, Cera Chinensis, Cera Flava, octadecanol.
Other described adjuvants comprise the adjuvants such as filler, disintegrating agent, binding agent, fluidizer, and specifically, filler can be selected from one or more of sucrose, mannitol, starch, microcrystalline Cellulose, lactose, dextrin etc.; Disintegrating agent can be selected from one or more of hydroxypropyl cellulose, carboxymethyl starch sodium, polyvinylpolypyrrolidone etc.; One or more of the optional ethanol-water solution from polyvidone, hydroxypropyl emthylcellulose, dehydrated alcohol, various concentration of binding agent etc.; Fluidizer can be selected from one or more of Pulvis Talci, differential silica gel etc.
Specifically, label comprises following composition, and its content is to account for the percentage ratio of label weight:
Aspartic acid 30～90%;
Waxiness adjuvant 0.5～20%;
Other adjuvant surpluses.
Preferably, the content of the each ingredient of label is (to account for the percentage ratio of label weight):
Aspartic acid 50～70%;
Waxiness adjuvant 5～10%;
Other adjuvant surpluses.
In addition, aspartic acid sheet of the present invention, also comprises coating, and the weight of described coating is 1.0～5.0% of label weight.Coated tablet can reduce the hygroscopicity of aspartic acid sheet, increases the stability of tablet.
The present invention also provides a kind of preparation method of this aspartic acid sheet, comprises the steps:
(1) label of the aspartic acid sheet described in preparation;
(2) at the coated film coating of described wicking surface.
Wherein, in step (1), adopt wet granule compression tablet legal system for described label.Concrete steps are: take waxiness adjuvant, add appropriate ethanol, heating for dissolving, as binding agent; Take the adjuvant mix homogeneously such as aspartic acid and filler, disintegrating agent and other binding agents, add the above-mentioned solution making, stir, the granulation of sieving, dry, granulate, adds fluidizer mix homogeneously; Tabletting.
Waxiness adjuvant of the present invention, not only can reduce the hygroscopicity of material, also has the effect of lubricant and binding agent concurrently: can reduce ejection force as lubricant, can improve the phenomenon of sliver as binding agent simultaneously.
Advantage of the present invention is: compared with prior art, aspartic acid sheet of the present invention can significantly reduce the hygroscopicity of the front material of tabletting, improves the compressibility of material, reduces the hygroscopicity of tablet, thereby increase the stability of finished product, reduce aspartic acid sheet and prepare difficulty and production cost.
Brief description of the drawings
Fig. 1: the sucting wet curve (25 DEG C) of aspartic acid
Fig. 2: aspartic acid of the present invention is stripping curve figure in water from film-making and reference preparation
Fig. 3: aspartic acid of the present invention is stripping curve figure in pH1.2 hydrochloric acid solution from film-making and reference preparation
Fig. 4: aspartic acid of the present invention is stripping curve figure in pH4.0 phosphate buffer from film-making and reference preparation
Fig. 5: aspartic acid of the present invention is stripping curve figure in pH6.8 phosphate buffer from film-making and reference preparation
Detailed description of the invention
Further illustrate the present invention below by specific embodiment, following embodiment is that the simple modifications that essence according to the present invention is carried out the present invention all belongs to the scope of protection of present invention for the present invention instead of limitation of the present invention are described.
embodiment 1
Prescription composition:
Preparation method:
(1) configuration of binding agent: take stearic acid 30g, add in 210g ethanol (95%), heating is dissolved stearic acid, as binding agent;
(2) granulate: take aspartic acid, microcrystalline Cellulose mix homogeneously, add binding agent, stir, with 18 order nylon screens granulations; Dry 4 hours of 60 DEG C of heated-air circulation ovens; 16 order granulate, add Pulvis Talci mix homogeneously;
(3) tabletting: use rotary tablet machine, tabletting, the heavily about 0.5g of sheet;
(4) coating: use Opadry (trade name is blocked happy Kanggong department and manufactured) coating, taking plain sheet as benchmark, stomach dissolved type moisture-proofing coating weightening finish 3%.
In the present embodiment:
(1) stearic acid consumption in Core formulation is 6%, and stearic acid is hydrophobic material, after mixing, reduces aspartic acid surface area with aspartic acid, reduces the hygroscopicity of mixed material.
(2) stearic fusing point is lower, in the process of tabletting, melts, and is impregnated in unclassified stores, increases the adhesion of storeroom, prevents sliver, has the effect of binding agent.
(3) stearic acid is wax material, has the effect of lubricant.
Stearic acid not only can reduce the hygroscopicity of material in this prescription, also can be used as lubricant and reduces ejection force, also can be used as binding agent and improve the phenomenon of sliver.
embodiment 2
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 3%.
Prescription composition:
embodiment 3
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 3%.
Prescription composition:
embodiment 4
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 3%.
Prescription composition:
embodiment 5
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 3%.
Prescription composition:
embodiment 6
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 3%.
Prescription composition:
embodiment 7
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 5%.
Prescription composition:
embodiment 8
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 4%.
Prescription composition:
embodiment 9
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 1%.
Prescription composition:
embodiment 10
According to the method for recording in embodiment 1, utilize following prescription composition to prepare aspartic acid sheet.Result is taking plain sheet as benchmark, and stomach dissolved type moisture-proofing coating increases weight approximately 3%.
Prescription composition:
experimental example 1
the mensuration of material sucting wet curve
1. test specimen
Aspartic acid raw material (pulverizing 100 mesh sieves); Stearic acid (pulverizing 100 mesh sieves); Octadecanol (pulverizing 100 mesh sieves)
2. experimental technique
(1) configure respectively the saturated solution of different salt, put in exsiccator, make to reach in closed environment certain humidity.
(2) take the about 3.0g of aspartic acid raw material, put in weighing botle, tiling makes thickness be less than 5mm, puts in each exsiccator, places 10 days, and taking-up is weighed, and calculates moisture absorption weightening finish.
(3) with method by aspartic acid and stearic acid in the ratio ground and mixed of 9:1 evenly after, take about 3.0g, put in weighing botle, tiling makes thickness be less than 5mm, puts in each exsiccator, places 10 days, taking-up is weighed, and calculates moisture absorption and increases weight.
(4) with method by aspartic acid and octadecanol in the ratio ground and mixed of 9:1 evenly after, take about 3.0g, put in weighing botle, tiling makes thickness be less than 5mm, puts in each exsiccator, places 10 days, taking-up is weighed, and calculates moisture absorption and increases weight.
3. result of the test
Experimental result is in table 1, Fig. 1.
table 1 moisture absorption weightening finish experimental result
According to experimental result, aspartic acid raw material critical relative humidity is about 59%, after mixing stearic acid and octadecanol, moisture absorption obviously reduces, and critical relative humidity is increased to 65%, 63%, and stearic acid or octadecanol and aspartic acid raw material mixing energy obviously improve the hygroscopicity of aspartic acid raw material.
experimental example 2
the determination experiment of dissolution
1. sample
Aspartic acid sheet of the present invention, prepares according to the embodiment of the present invention 1.
2. experimental technique
Measure aspartic acid sheet dissolution with two annex X C of Chinese Pharmacopoeia version in 2010 the second method., the results are shown in Figure shown in 2～5 as dissolution medium taking water, pH1.2 hydrochloric acid solution, pH4.0 phosphate buffer, pH6.8 phosphate buffer (by Japanese official method configuration) 900ml respectively.
3. experimental result
Known referring to Fig. 2～5, aspartic acid sheet of the present invention and reference stripping curve are consistent substantially.
Claims (8)
1. an aspartic acid sheet, comprise label and coating, described label contains aspartic acid and pharmaceutically acceptable adjuvant, it is characterized in that this pharmaceutically acceptable adjuvant comprises waxiness adjuvant, this label contains aspartic acid 30～90% by weight percentage, waxiness adjuvant 0.5～20%.
2. aspartic acid sheet according to claim 1, is characterized in that containing in described label aspartic acid 50～70%, waxiness adjuvant 5～10%.
3. aspartic acid sheet according to claim 1, is characterized in that, described waxiness adjuvant is one or more in tristerin, glyceryl monostearate, stearic acid, Cera Chinensis, Cera Flava, octadecanol.
4. aspartic acid sheet according to claim 1, is characterized in that, label also contains appropriate other adjuvants.
5. aspartic acid sheet according to claim 4, is characterized in that, described other adjuvants comprise filler, disintegrating agent, binding agent, fluidizer etc.
6. aspartic acid sheet according to claim 1, is characterized in that, the weight of described coating is 1.0～5.0% of label weight.
7. according to the preparation method of the arbitrary described aspartic acid sheet of claim 1～6, comprise the steps:
(1) label of the aspartic acid sheet described in preparation;
(2) at the coated film coating of described wicking surface.
8. method according to claim 7, is characterized in that, adopts wet granule compression tablet legal system for described label in step (1), and concrete steps are: take waxiness adjuvant, add appropriate ethanol, heating for dissolving, as binding agent; Take the adjuvant mix homogeneously such as aspartic acid and filler, disintegrating agent and other binding agents, add the above-mentioned solution making, stir, the granulation of sieving, dry, granulate, adds fluidizer mix homogeneously; 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 true CN104069082A (en) | 2014-10-01 |
| CN104069082B CN104069082B (en) | 2017-12-05 |
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Cited By (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 |
Non-Patent Citations (1)
| Title |
|---|
| 张志荣: "《药剂学》", 31 December 2007 * |
Cited By (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 |
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|---|---|
| CN104069082B (en) | 2017-12-05 |
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