CN105769853A - Vildagliptin pharmaceutical composition - Google Patents
Vildagliptin pharmaceutical composition Download PDFInfo
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- CN105769853A CN105769853A CN201410812302.9A CN201410812302A CN105769853A CN 105769853 A CN105769853 A CN 105769853A CN 201410812302 A CN201410812302 A CN 201410812302A CN 105769853 A CN105769853 A CN 105769853A
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- vildagliptin
- pharmaceutical composition
- lactose
- microcrystalline cellulose
- disintegrating agent
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Abstract
The invention discloses a vildagliptin pharmaceutical composition, comprising vildagliptin, a filler, a disintegrating agent and a lubricant. Through selection of the filler with specific components, the vildagliptin pharmaceutical composition has good stability; the vildagliptin pharmaceutical composition is more obviously advantaged in improvement of product yield, cost reduction, realization of industrialization and better clinical application; the dissolving-out rate of vildagliptin can be effectively improved; and the bi0availability of vildagliptin is obviously enhanced.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to vildagliptin pharmaceutical composition and preparation method thereof.
Background technology
Vildagliptin, its chemistry is by name: (2S)-1-[2-[(3-hydroxyl three ring [3.3.1.13,7] last of the ten Heavenly stems-1-base) amino] acetyl group]-2-Pyrrolidinecarbonitile (having another name called 1-[2-(3-hydroxy-adamant-1-amino)-acetyl group] pyrrolidine-2 (S)-nitrile), molecular weight: 303.40.Its structural formula is as follows:
Indication:For improving the glycemic control of type 2 diabetes mellitus patient.
The oral solid formulation that prior art exists is generally of dissolution difference, the problems such as bioavailability is not high, and the present inventor is through the research to prior art, have been surprisingly found that, apply special adjuvant, vildagliptin pharmaceutical composition prepared by special process, reliable in quality, dissolution rate is fast, not only successfully solve the problem that vildagliptin is unstable, and be prone to industrialization, reduce production cost, easy to implement, remarkable in economical benefits.
Summary of the invention
The first object of the present invention is in that to provide a kind of vildagliptin pharmaceutical composition, and this vildagliptin pharmaceutical composition, to good stability, to improving product yield, reduces cost, it is achieved industrialization, is better applied to clinic, has more obvious advantage.
The second object of the present invention is in that the preparation method providing vildagliptin pharmaceutical composition of the present invention, and the method is simple, and prepared vildagliptin pharmaceutical composition, steady quality is reliable.
For realizing the first object of the present invention, present inventors have surprisingly found that the pharmaceutical composition of a kind of vildagliptin, said composition contains vildagliptin, disintegrating agent, microcrystalline Cellulose and lactose, and the weight ratio of microcrystalline Cellulose and lactose is 1-2.5.
Specifically, the present invention containing the pharmaceutical composition of vildagliptin, component and percentage by weight that it contains be:
Vildagliptin 15-25%
Disintegrating agent 4-10%
Microcrystalline Cellulose 30-50%
Lactose 20-30%
Wherein, described disintegrating agent is selected from polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose or one or more in CCMS-Na.Preferred disintegrating agent is selected from carboxymethyl starch sodium.
Microcrystalline Cellulose and lactose are the filleies of the present invention, can contain appropriate lubricant as required, for instance can contain one or both the mixture in appropriate micropowder silica gel or magnesium stearate.
The preparation method of the pharmaceutical composition more than containing vildagliptin is: the adjuvant taking vildagliptin and formula ratio is pulverized, and sieves for subsequent use；Vildagliptin is mixed homogeneously with adjuvant mixture；Measure mixture content of dispersion, calculate tablet weight, tabletting, coating and get final product.
One of preferred version of the present invention is:
Vildagliptin 25%
Carboxymethyl starch sodium 10%
Microcrystalline Cellulose 30%
Lactose 30%
Magnesium stearate 5%
Another preferred scheme of the present invention is:
Vildagliptin 20%
Carboxymethyl starch sodium 4%
Microcrystalline Cellulose 50%
Lactose 20%
Magnesium stearate 6%
The concrete preparation method of above-mentioned vildagliptin pharmaceutical composition comprises the steps:
1)Prepare: carboxymethyl starch sodium, lactose, microcrystalline Cellulose and magnesium stearate are dried 4 hours under 80 DEG C of conditions, standby；
2)By the lactose of recipe quantity, microcrystalline Cellulose and vildagliptin, put in container, after mix homogeneously, be ground to granularity at 80 ± 10um, standby；
3)By 2) item mixs homogeneously with carboxymethyl starch sodium and the magnesium stearate of recipe quantity；
4)Tabletting: regulate suitable stiff and tablet weight, carry out tabletting；
5)Packaging: adopt aluminium-plastic bubble plate packing machine to pack；
6)Warehouse-in.
On the basis of existing pharmaceutical adjunct and preparation technology, the present inventor finds through substantial amounts of experimental study, filler is selected, find two kinds of necessary proportion relations of filler, when to make vildagliptin pharmaceutical composition be above-mentioned formula and preparation technology, described pharmaceutical composition quality is effectively ensured.
Compared with prior art, present invention have the advantage that
1) vildagliptin pharmaceutical composition provided by the present invention is for improving the yield of this product, reducing production cost, and being better applied to clinical treatment has very big help.
2) new vildagliptin compositions provided by the present invention is through industrialized great production and study on the stability, it was demonstrated that constant product quality.
3) preparation method of new vildagliptin compositions provided by the present invention, the method is simple, prepared vildagliptin pharmaceutical composition reliable in quality.
4) new vildagliptin compositions provided by the present invention, dissolution is fast, has higher bioavailability, is rapidly reached and needs concentration.
Detailed description of the invention
Following example are only used for explaining the present invention rather than the restriction present invention.Unless otherwise indicated, the experiment condition in the embodiment of the present invention is the experiment condition that this area is conventional.
Embodiment 1
Every 1000 described vildagliptin pharmaceutical compositions, its formula consists of:
Vildagliptin 50g
Carboxymethyl starch sodium 20g
Microcrystalline Cellulose 60g
Lactose 60g
Magnesium stearate 10g
Preparation technology:
1)Prepare: carboxymethyl starch sodium, lactose, microcrystalline Cellulose and magnesium stearate are dried 4 hours under 80 DEG C of conditions, standby；
2)By the lactose of recipe quantity, microcrystalline Cellulose and vildagliptin, put in container, after mix homogeneously, be ground to granularity at 80 ± 10um, standby；
3)By 2) item mixs homogeneously with carboxymethyl starch sodium and the magnesium stearate of recipe quantity；
4)Tabletting: regulate suitable stiff and tablet weight, carry out tabletting；
5)Packaging: adopt aluminium-plastic bubble plate packing machine to pack；
6)Warehouse-in.
Embodiment 2
Every 1000 described vildagliptin pharmaceutical compositions, its formula consists of:
Vildagliptin 50g
Carboxymethyl starch sodium 10g
Microcrystalline Cellulose 125g
Lactose 50g
Magnesium stearate 15g
Preparation technology: with embodiment 1.
Embodiment 3
Every 1000 described vildagliptin pharmaceutical compositions, its formula consists of:
Vildagliptin 50g
Carboxymethyl starch sodium 20g
Microcrystalline Cellulose 80g
Lactose 40g
Magnesium stearate 10g
Preparation technology: with embodiment 1.
Comparative example 1
Every 1000 described vildagliptin pharmaceutical compositions, its formula consists of:
Vildagliptin 50g
Carboxymethyl starch sodium 5g
Microcrystalline Cellulose 60g
Lactose 20g
Magnesium stearate 10g
Purified Water q. s
Preparation method: vildagliptin, microcrystalline Cellulose, lactose, carboxymethyl starch sodium are tentatively mixed, pulverized 80 mesh sieves；Add appropriate purified water, soft material processed to said mixture, cross 20 mesh sieves and granulate；Dry, add magnesium stearate, tabletting, to obtain final product.
Test example 1
This test example is in that to investigate the stability of vildagliptin compositions provided by the present invention.
The accelerated test of vildagliptin pharmaceutical composition
Method and comparative example 1 according to embodiment of the present invention 1-3 prepare vildagliptin pharmaceutical composition, at 40 DEG C ± 2 DEG C, the condition of RH75% ± 5% is placed 6 months, period respectively at the 1st, 2,3, sampling in 6 months, survey according to stability check item visual inspection, and compare with 0 day data.
1, project is investigated
High spot reviews: character, have related substance and content.
2, accelerated test result
Above conclusion (of pressure testing) is it can be seen that embodiments of the invention 1-3 places 6 months stability better when accelerated test, and impurity content is few, has good dissolution simultaneously.
Test example 2
Adopt 2010 editions annex XC dissolution method the second method (slurry processes) 75rpm of Chinese Pharmacopoeia.Using the Ph4.5 acetate buffer 900mL containing 0.2%SDS as dissolution medium, the stripping curve of the tablet of detection embodiment of the present invention 1-3 and comparative example 1 preparation, result is as follows:
Testing result illustrates, the sample adopting the method for the present invention to prepare, and has quick dissolution rate.
Claims (7)
1. a vildagliptin pharmaceutical composition, said composition contains vildagliptin, disintegrating agent, microcrystalline Cellulose and lactose, it is characterised in that the weight ratio of microcrystalline Cellulose and lactose is 1-2.5.
2. vildagliptin pharmaceutical composition according to claim 1, it is characterised in that the percentage by weight of described each component is:
Vildagliptin 15-25%
Disintegrating agent 4-10%
Microcrystalline Cellulose 30-50%
Lactose 20-30%.
3. vildagliptin pharmaceutical composition according to claim 1 and 2, it is characterised in that described disintegrating agent is selected from one or both in carboxymethyl starch sodium or polyvinylpolypyrrolidone.
4. vildagliptin pharmaceutical composition according to claim 3, it is characterised in that possibly together with one or both in magnesium stearate or micropowder silica gel.
5. vildagliptin pharmaceutical composition according to claim 4, it is characterised in that described component and percentage by weight be:
Vildagliptin 25%
Disintegrating agent 10%
Microcrystalline Cellulose 30%
Lactose 30%
Magnesium stearate 5%.
6. vildagliptin pharmaceutical composition according to claim 4, it is characterised in that described component and percentage by weight be:
Vildagliptin 20%
Disintegrating agent 4%
Microcrystalline Cellulose 50%
Lactose 20%
Magnesium stearate 6%.
7. a preparation method for the vildagliptin pharmaceutical composition according to claim 4-6 any one, the method comprises the steps:
1)Prepare: disintegrating agent, lactose, microcrystalline Cellulose and magnesium stearate are dried 4 hours under 80 DEG C of conditions, standby；
2)By the lactose of recipe quantity, microcrystalline Cellulose and vildagliptin, put in container, after mix homogeneously, be ground to granularity at 80 ± 10um, standby；
3)By 2) item mixs homogeneously with disintegrating agent and the magnesium stearate of recipe quantity；
4)Tabletting: regulate suitable stiff and tablet weight, carry out tabletting；
5)Packaging: adopt aluminium-plastic bubble plate packing machine to pack；
6)Warehouse-in.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410812302.9A CN105769853A (en) | 2014-12-24 | 2014-12-24 | Vildagliptin pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410812302.9A CN105769853A (en) | 2014-12-24 | 2014-12-24 | Vildagliptin pharmaceutical composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105769853A true CN105769853A (en) | 2016-07-20 |
Family
ID=56377941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410812302.9A Pending CN105769853A (en) | 2014-12-24 | 2014-12-24 | Vildagliptin pharmaceutical composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105769853A (en) |
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2014
- 2014-12-24 CN CN201410812302.9A patent/CN105769853A/en active Pending
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| PB01 | Publication | ||
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160720 |