CN105125575B - A kind of preparation method for treating hyperphosphatemia disease drug - Google Patents
A kind of preparation method for treating hyperphosphatemia disease drug Download PDFInfo
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- CN105125575B CN105125575B CN201510487315.8A CN201510487315A CN105125575B CN 105125575 B CN105125575 B CN 105125575B CN 201510487315 A CN201510487315 A CN 201510487315A CN 105125575 B CN105125575 B CN 105125575B
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Abstract
The present invention relates to a kind of pharmaceutical composition for treating hyperphospheremia and preparation method thereof, pharmaceutical composition of the invention is chewable tablet, and the composition of wherein each component is as follows：
Description
Technical field：
The present invention relates to a kind of preparation method for treating hyperphosphatemia disease drug, it is more particularly to a kind of treat high phosphoric acid
The preparation method that salt mass formed by blood stasis drug passes through dry granulation.
Background technology：
Hyperphospheremia is a peculiar problem with chronic renal insufficiency or chronic kidney disease (CKD) patient.
About 70% patient that kidney dialysis treatment is carried out with end-stage renal disease (ESRD) needs to treat hyperphospheremia.The illness can be led
Serious bone problem and skin and the metastatic calcification of major organs are caused, and related to significant morbidity and mortality.
Conventional dialysis can not reduce phosphate level in blood, therefore level increases at any time.Raised phosphate level is using drink
Eclipse limit system and phosphate binders combine what is treated.
WO96/30029 discloses seleced lanthanum carbonate hydrates and can be applied through gastrointestinal tract, treats person having renal failure
Hyperphosphatemia.WO2005/018651 discloses a kind of masticable lanthanum preparation, the lanthanum chemical combination including pharmacy effective dose
Object and at least one masticable pharmaceutically acceptable excipient, further relate to a kind of tablet or powder of the lanthanum compound comprising pharmacy effective dose
Last pharmaceutical preparation includes composition of pharmaceutical preparation of lanthanum compound and preparation method thereof, i.e., is obtained using the method for powder vertical compression
Tablet.
Lanthanum compound in lanthanum carbonate chewable tablets is lanthanum carbonate hydrates, has following formula：La2(CO3)3·nH2O, wherein n
Be worth is 3 to 6.
Lanthanum carbonate chewable tablets is a kind of drug listed at present, but its formula and preparation method be not open, this hair
A person of good sense has found lanthanum carbonate hydrates poor fluidity during lanthanum carbonate hydrates is used to prepare chewable tablets, meanwhile, every lanthanum contains
It measures as 250-500mg, using the method for powder vertical compression, fragment is more, yield is low, is not easy to transport and preserve, and powder is through granulation
The method of tabletting can reduce the generation of fragment again, improve yield, since lanthanum carbonate hydrates are the medicines that have specific hydration status
Object, using the method for wet granulation, i.e., lanthanum carbonate hydrates need to through being mixed with auxiliary material, water wetting, granulation, by high temperature drying,
Lanthanum carbonate hydrates can be degraded to basic carbonate lanthanum, have larger impact to the stability of drug.Dry granulation can be to avoid this side
Hard-packed particle is being made compared with dry method under strong pressure in drug by the defects of face.And Particulate Air content is low, mobility
It is easy to tabletting well.But experiment finds that dry granulation is for lanthanum carbonate hydrates, because hydrone content therein is larger, and
And crystal structure is soft, tablet hardness is not high, while places and be susceptible to pitted skin after a certain period of time.
The present invention is by research, it is proposed that a kind of solution to the problem.
The present invention squeezes in blocks, warp by adding in polylactic acid in the auxiliary material of formula, after fine drug powder is mixed with auxiliary material
Concussion is broken for particle, then carry out tabletting.This method technical process is simple, it is not necessary to time saving and can by the process that granulation is dry
Ensure medicine stability.
Invention content：
The present invention relates to a kind of pharmaceutical composition for treating hyperphospheremia and preparation method thereof, wherein the treatment is high
The drug of phosphate mass formed by blood stasis is lanthanum carbonate hydrates.
The pharmaceutical composition of the present invention, is chewable tablet, the composition of wherein each component is as follows：
The chewing tablet recipe of wherein 250mg specifications (in terms of lanthanum) is as follows：
The chewing tablet recipe of wherein 500mg specifications (in terms of lanthanum) is as follows：
Wherein described glucose can use dextrates such as：The replacements such as fructose, barley-sugar, mannitol.
Wherein described silica can be colloidal silicon dioxide,
Wherein lanthanum carbonate hydrates have following formula：La2(CO3)3·nH2O, wherein n values are 3 to 6, preferably 4-5.
The invention also includes the preparation method of the pharmaceutical composition of the present invention, step is as follows：
Lanthanum carbonate hydrates with polylactic acid, glucose, silica are uniformly mixed, put into dry granulating machine, through concussion
It is broken for midbody particle, midbody particle and magnesium stearate is uniformly mixed, pressure 1000 to obtain the final product.
In the preparation method of the lanthanum carbonate chewable tablets of the present invention, wherein the squeeze pressure 2MPa to 8MPa, lanthanum carbonate
Grain heap density is 0.6g/ml to 0.9g/ml；Particle is broken for through shaking, 20% to 30% below 60 mesh of drug granule grain size；60
More than mesh screening retention 70% to 80%.
The present invention passes through dry granulation：1. select specific extrusion pressure 2. comprehensive to the selection of broken rear grain diameter etc.
Technological means causes the lanthanum carbonate chewable tablets prepared to be easy to tabletting, and in the case of similary dose, technically prevents because of water
Divide and pass through X-ray powder diffraction point with the tendency that heat affecting lanthanum carbonate hydrates Partial digestion is basic carbonate lanthanum, products made thereby
Analysis does not detect the generation of basic carbonate lanthanum polymorphic I and basic carbonate lanthanum polymorphs, and drug filling is suitable in production process
Profit improves production controllable degree, while tablet hardness improves, and places and is generated after a certain period of time without pitted skin.
Specific embodiment：
Finer description is done to the present invention by the following examples.But these embodiments are only limitted to illustrate the present invention,
Any type of limitation is not formed to the present invention.
Embodiment 1
A. the following raw material is weighed in proportion：
Wherein lanthanum carbonate hydrates, the water content having are approximately equal to 4 to 5 mole of water.
B. by 954g lanthanum carbonate hydrates and 10g polylactic acid, 1000g dextrates, the mixing of 40g colloidal silicon dioxides
Uniformly, particle, squeeze pressure 4MPa is made in input dry granulating machine, and drug tabletting heap density is 0.8g/ml；It is broken through shaking
For particle, select 30% below 60 mesh of grain diameter；More than 60 mesh screenings retention 70%；
C. drug granule and 20g magnesium stearates are uniformly mixed, tabletting is to get lanthanum carbonate chewable tablets.
Embodiment 2
A. the following raw material is weighed in proportion：
Wherein lanthanum carbonate is hydration, and the water content having is approximately equal to 4 to 5 mole of water.
B. by 477g lanthanum carbonates and 5g polylactic acid, 500g glucose, 20g colloidal silicon dioxides are uniformly mixed, and put into dry method
Particle, squeeze pressure 4MPa is made in granulator, and drug tabletting heap density is 0.8g/ml；Particle, selection are broken for through concussion
30% below grain 60 mesh of grain size；More than 60 mesh screenings retention 70%；
C. drug granule and 10g magnesium stearates are uniformly mixed, tabletting is to get lanthanum carbonate chewable tablets.
Embodiment 3
A. the following raw material is weighed in proportion：
Wherein lanthanum carbonate hydrates, the water content having are approximately equal to 4 to 5 mole of water.
B. 954g lanthanum carbonate hydrates with 1000g dextrates, 40g colloidal silicon dioxides are uniformly mixed, put into
Particle, squeeze pressure 4MPa is made in dry granulating machine, and drug tabletting heap density is 0.8g/ml；Particle is broken for through concussion, is selected
It selects 30% below 60 mesh of grain diameter；More than 60 mesh screenings retention 70%；
C. drug granule and 20g magnesium stearates are uniformly mixed, tabletting is to get lanthanum carbonate chewable tablets.
Example 4
A. the following raw material is weighed in proportion：
Wherein lanthanum carbonate is hydration, and the water content having is approximately equal to 4 to 5 mole of water.
B. 477g lanthanum carbonates are uniformly mixed with 500g glucose, 20g colloidal silicon dioxides, input dry granulating machine is made
Particle, squeeze pressure 4MPa, drug tabletting heap density are 0.8g/ml；Particle is broken for through concussion, selects 60 mesh of grain diameter
Below 30%；More than 60 mesh screenings retention 70%；
C. drug granule and 10g magnesium stearates are uniformly mixed, tabletting is to get lanthanum carbonate chewable tablets.
Below by the advantageous effect of description of test technical solution provided by the present invention, to embodiment 1,2 and control
Lanthanum carbonate chewable tablets prepared by embodiment 3,4 carries out quality testing, at the same arrange 1,2,3,4 product of embodiment 40 DEG C/
Accelerated test and the long term test under the conditions of 25 DEG C/60%RH under the conditions of 75%RH investigate the variation of each inspection project, institute's total
According to as shown in table 1-3：
0 day inspection result of 1 embodiment 1-4 lanthanum carbonate chewable tablets of table
2 embodiment 1-4 lanthanum carbonate chewable tablets 500mg accelerated test 6 months under the conditions of 40 DEG C, 75%RH of table
3 embodiment 1-4 lanthanum carbonate chewable tablets 500mg long term test 6 months under the conditions of 25 DEG C, 60%RH of table
By more than inspection data it is found that lanthanum content and carbonate content meet mark in the obtained lanthanum carbonate chewable tablets of the present invention
Standard, basic carbonate lanthanum polymorphic I and basic carbonate lanthanum polymorphs do not detect.By accelerating examination under the conditions of 40 DEG C/75%RH
It tests with after 25 DEG C/60%RH conditions long term test 6 months, every test rating meets quality standard, explanation without significant changes
Sample quality prepared by the present invention is fine, has good stability.Compared to comparative example 3,4, hardness reduction is small, does not occur fiber crops
Point.
The present invention is described in detail according to the above embodiments, it should be noted that above embodiment is only
It illustrates the present invention.Under the premise of the spirit and essence without departing from invention, those skilled in the art can design
Go out a variety of alternatives and improvement project of the present invention, should be understood within protection scope of the present invention.
Claims (3)
1. a kind of preparation method for treating hyperphospheremia chewable tablet, wherein the composition of the tablet each component is as follows：
Wherein lanthanum carbonate hydrates have following formula：La2(CO3)3·nH2O, wherein n values are 3 to 6；
Preparation method, step are as follows：By lanthanum carbonate hydrates and polylactic acid, glucose, silica are uniformly mixed, and input is dry
Method granulator is broken for midbody particle through concussion, midbody particle and magnesium stearate is uniformly mixed, and presses 1000 to obtain the final product,
Squeeze pressure is 2MPa to 8MPa wherein in tableting processes, and lanthanum carbonate granular pile density is 0.6g/ml to 0.9g/ml；Through concussion
Particle is broken for, 20% to 30% below 60 mesh of drug granule grain size；More than 60 mesh screenings retention 70% to 80%.
2. the chewing tablet recipe of preparation method according to claim 1, wherein 250mg specifications is as follows：
3. the chewing tablet recipe of preparation method according to claim 1, wherein 500mg specifications is as follows：
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| CN201510487315.8A CN105125575B (en) | 2015-08-07 | 2015-08-07 | A kind of preparation method for treating hyperphosphatemia disease drug |
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| CN105125575B true CN105125575B (en) | 2018-06-08 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN111419811A (en) * | 2020-05-20 | 2020-07-17 | 北京华睿鼎信科技有限公司 | Tenofovir alafenamide fumarate composition |
| CN113244179B (en) * | 2021-05-21 | 2023-01-13 | 浙江仟源海力生制药有限公司 | Lanthanum carbonate tablet with good stability, preparation method and application thereof |
| CN114794467B (en) * | 2022-04-12 | 2023-08-04 | 广州市巴菲巴健康产业有限公司 | Fruit and vegetable ferment chewable tablet as well as preparation method and application thereof |
| CN117046760B (en) * | 2023-10-13 | 2023-12-26 | 湖南明瑞制药股份有限公司 | Preparation, detection and separation method of lanthanum carbonate chewable tablets |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996030029A1 (en) * | 1995-03-25 | 1996-10-03 | Johnson Matthey Public Limited Company | Pharmaceutical composition containing selected lanthanum carbonate hydrates |
| CN103237543A (en) * | 2010-12-01 | 2013-08-07 | 夏尔有限责任公司 | Capsule and powder formulations containing lanthanum compounds |
| CN103494781A (en) * | 2013-08-30 | 2014-01-08 | 哈药集团技术中心 | Montelukast sodium chewing tablet prescription and preparation process thereof |
| CN104434854A (en) * | 2014-12-10 | 2015-03-25 | 哈药集团技术中心 | Minodronic acid tablet and preparation process thereof |
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2015
- 2015-08-07 CN CN201510487315.8A patent/CN105125575B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996030029A1 (en) * | 1995-03-25 | 1996-10-03 | Johnson Matthey Public Limited Company | Pharmaceutical composition containing selected lanthanum carbonate hydrates |
| CN103237543A (en) * | 2010-12-01 | 2013-08-07 | 夏尔有限责任公司 | Capsule and powder formulations containing lanthanum compounds |
| CN103494781A (en) * | 2013-08-30 | 2014-01-08 | 哈药集团技术中心 | Montelukast sodium chewing tablet prescription and preparation process thereof |
| CN104434854A (en) * | 2014-12-10 | 2015-03-25 | 哈药集团技术中心 | Minodronic acid tablet and preparation process thereof |
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