CN106389364A - Trajenta tablet composition and preparation method thereof - Google Patents
Trajenta tablet composition and preparation method thereof Download PDFInfo
- Publication number
- CN106389364A CN106389364A CN201610956027.7A CN201610956027A CN106389364A CN 106389364 A CN106389364 A CN 106389364A CN 201610956027 A CN201610956027 A CN 201610956027A CN 106389364 A CN106389364 A CN 106389364A
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- CN
- China
- Prior art keywords
- gelieting
- compositionss
- macrogol
- lactose
- polyvidone
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
Abstract
The invention relates to a Trajenta tablet composition and a preparation method thereof, and belongs to the technical field of medicines. The Trajenta tablet composition is technically characterized in that every 1000 pieces of composition contain 5g of Trajenta, 80 to 150g of mannitol, 10 to 25g of polyethylene glycol 8000, 15 to 20g of lactose, 10 to 46g of pregelatinized starch, 5 to 16g of povidone k30, and 1.8g of magnesium stearate, wherein the particle size of the Trajenta is D90=10 to 50mu m. By adopting the technical scheme, the tablet composition with high dissolution rate is provided.
Description
Technical field
The present invention relates to a kind of Linagliptin Tablets agent compositionss and preparation method thereof, belong to pharmaceutical technology field.
Background technology
Li Gelieting（Linagliptin, structural formula is as follows）It is a kind of potent, selectivity dipeptidyl peptidase 4（DPP-
4）Inhibitor, DPP-4 can degrade gut incretin hormones sample polypeptide -1（GLP-1）And glucose dependency pancreotropic hormone is many
Peptide（GIP）.Li Gelieting is capable of the concentration of increased activity gut incretin hormones, stimulates islets of langerhans in the way of glucose dependency
Element release, reduces Plasma Glucagon Level in circulation.Additionally, GLP-1 can also reduce the glucagon secretion of pancreatic alpha cells,
Hepatic glucose output reduces.
Li Gelieting（linagliptin）Structural formula
Linagliptin Tablets are used in combination with metformin and sulfonylurea drugs, coordinate diet control and motion, can be used for 2 types of growing up
The glycemic control of diabeticss, for pharmacokineticss, Li Gelieting is administered orally latter 1.5 hours and can reach peak serum concentration,
Effective half-life is about 12 hours, will not cause the accumulation of medicine by daily single.About 90% Li Gelieting is arranged with prototype
Let out, can be used for the diabeticss having renal dysfunction, and dose titration need not be carried out.Pharmacokinetics research show liver
Injured patient need not adjust dosage.Li Gelieting absorbs and is not affected by taking food（After experimenter's feed and aobvious under fasted conditions
Similar pharmacokinetic results are shown）.For products characteristics, Li Gelieting belongs to micromolecular compound, be one kind very
Unique non-peptidomimetic class DPP-4 precisely combines, and selectivity is higher.
Li Gelieting dissolves in methyl alcohol, slightly molten in ethanol, almost insoluble in water, and in water, dissolubility is only 0.9mg/
ml.Additionally, Li Gelieting crude drug is all unstable under illumination and hot conditionss, especially in conventional wet granulation oven drying bar
Under part, high temperature impurity increases comparatively fast.
Chinese patent CN 101437493A（200780016227.3）In the medicine attempting the selected DPP-IV inhibitor of preparation
It has been observed that the DPP-IV inhibitor with primary amino radical or secondary amino group shows and such as Microcrystalline Cellulose, hydroxyl second in compositionss
Acid-starch sodium, cross-linking sodium carboxymethyl cellulose, tartaric acid, citric acid, glucose, Fructose, sucrose, Lactose, maltodextrin permitted
The incompatibility of many usual excipients, degradation problem.Although compound itself and its stable, it is used with solid dosage formss
The impurity reaction of multiple excipient and excipient.This all give prepare excellent preparation bring unfavorable.
Content of the invention
Goal of the invention：It is an object of the invention to provide a kind of qualified Linagliptin Tablets agent of high-dissolution.
It has been found that when preparing Li Gelieting compositionss, only using Mannitol, Pregelatinized Starch, polyvidone
, as filling out adjuvant, prepared slice, thin piece is although dissolution is up to standard, but easily goes out for k30, aerosil and magnesium stearate
The situation of existing fragment.Through repetition test it is achieved that the present invention.
The technical scheme is that：A kind of Linagliptin Tablets agent compositionss are it is characterised in that the compositionss of every 1000
In contain favourable Ge Lieting 5g, Mannitol 80-150g, Macrogol 8000 10-25g, Lactose 15-20g, Pregelatinized Starch 10-
46g, polyvidone k30 5-16g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=10-50 μm.
The technical scheme is that：A kind of Linagliptin Tablets agent compositionss are it is characterised in that the compositionss of every 1000
In contain favourable Ge Lieting 5g, Mannitol 90-130g, Macrogol 8000 13-22g, Lactose 15-20g, Pregelatinized Starch 15-
40g, polyvidone k30 8-13g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=15-40 μm.
The technical scheme is that：A kind of Linagliptin Tablets agent compositionss are it is characterised in that the compositionss of every 1000
In contain favourable Ge Lieting 5g, Mannitol 90g, Macrogol 8000 13g, Lactose 15g, Pregelatinized Starch 15g, polyvidone k30
8g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=20 μm.
The technical scheme is that：A kind of Linagliptin Tablets agent compositionss are it is characterised in that the compositionss of every 1000
In contain favourable Ge Lieting 5g, Mannitol 130g, Macrogol 8000 22g, Lactose 20g, Pregelatinized Starch 40g, polyvidone k30
13g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=30 μm.
The technical scheme is that：A kind of Linagliptin Tablets agent compositionss are it is characterised in that the compositionss of every 1000
In contain favourable Ge Lieting 5g, Mannitol 100g, Macrogol 8000 18g, Lactose 18g, Pregelatinized Starch 30g, polyvidone k30
10g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=40 μm.
The preparation method of the present composition it is characterised in that
The first step adopts jet mill to pulverize, and Li Gelieting is crushed to D90=10-50 μm.
Second step weighs the Li Gelieting of recipe quantity, mixs homogeneously with the Macrogol 8000 of recipe quantity.
3rd step weighs other adjuvants of recipe quantity, mixes with second step gained compounding substances.
4th step tabletting, 8mm scrobicula stamping, hardness 60-80N.
Beneficial effects of the present invention：Technical solution of the present invention provides a kind of high-dissolution tablet composition, and solves
Fragment problems.Through reasonable compatibility, solve CN 101437493A（200780016227.3）Incompatibility described in patent and fall
Solution problem.
Embodiment 1, Li Gelieting 5g, Mannitol 80g, Macrogol 8000 25g, Lactose 15g, Pregelatinized Starch 46g,
Polyvidone k30 5g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=10 μm, side as described in technical scheme
Method prepares 1000.
Embodiment 2, Li Gelieting 5g, Mannitol 150g, Macrogol 8000 10g, Lactose 20g, Pregelatinized Starch 10g,
Polyvidone k30 16g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=50 μm, side as described in technical scheme
Method prepares 1000, prepares 1000 by technical scheme methods described.
Embodiment 3, Li Gelieting 5g, Mannitol 90g, Macrogol 8000 13g, Lactose 15g, Pregelatinized Starch 15g,
Polyvidone k30 8g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=20 μm, side as described in technical scheme
Method prepares 1000.
Embodiment 4, Li Gelieting 5g, Mannitol 130g, Macrogol 8000 22g, Lactose 20g, Pregelatinized Starch 40g,
Polyvidone k30 13g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=30 μm, side as described in technical scheme
Method prepares 1000.
Embodiment 5, Li Gelieting 5g, Mannitol 100g, Macrogol 8000 18g, Lactose 18g, Pregelatinized Starch 30g,
Polyvidone k30 10g, magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=40 μm, side as described in technical scheme
Method prepares 1000.
Reference examples 1：Weigh the Li Gelieting 5g of recipe quantity（D90=10μm）, Mannitol 80g, Pregelatinized Starch 46g, poly-
Dimension ketone k30 8g, magnesium stearate 1.8g, mix homogeneously, make 1000.（Reference implementation example 1）
Reference examples 2：Weigh the Li Gelieting 5g of recipe quantity（D90=20μm）, Mannitol 90g, Pregelatinized Starch 15g, polyvidone
K30 8g, magnesium stearate 1.8g, mix homogeneously, make 1000.（Reference implementation example 3）
Reference examples 3：Weigh recipe quantity Li Gelieting 5g（D90=30μm）, Mannitol 130g, Pregelatinized Starch 40g, polyvidone k30
13g, magnesium stearate 1.8g, mix homogeneously, make 1000.（Reference implementation example 4）
Test example 1, by embodiment 1-5 and reference examples 1-3 sample, measure 30min dissolution in hydrochloric acid medium, dissolution measures
Condition is：Basket method, 50 turns, dissolution volume is 900ml.Concrete data is shown in Table 1.
Table 1
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Reference examples 1 | Reference examples 2 | Reference examples 3 | |
| 30min dissolution in 1.0 media | 99 | 99 | 100 | 98.6 | 99 | 85 | 80 | 83 |
Test result indicate that：Embodiment of the present invention 1-5 product has higher dissolution.
Test example 2, embodiment 1-5 and reference examples 1-3 sample are respectively taken 20, observe the complete of embodiment and reference examples slice, thin piece
Degree.The quantity of imperfect slice, thin piece is recorded in table 2.
Table 2
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Reference examples 1 | Reference examples 2 | Reference examples 3 | |
| 0 day number of tiles | No fragment | No fragment | No fragment | No fragment | No fragment | 3 imperfect | 3 imperfect | 3 imperfect |
| 6 months number of tiles | No fragment | No fragment | No fragment | No fragment | No fragment | 5 imperfect | 4 imperfect | 4 imperfect |
Table 2 data illustrates embodiment of the present invention sample, and slice, thin piece is stable.
Test example 3 measures the relevant content of material of embodiment 1-5 and reference examples 1-3 sample respectively.Result is recorded in table 3.
Table 3
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Reference examples 1 | Reference examples 2 | Reference examples 3 | |
| Relevant content of material, % | 0.10 | 0.10 | 0.08 | 0.08 | 0.10 | 0.10 | 0.10 | 0.11 |
The table 3 data explanation relevant content of material of technical solution of the present invention products obtained therefrom is inconspicuous with reference examples difference.
Claims (6)
1. a kind of Linagliptin Tablets agent compositionss are it is characterised in that contain favourable Ge Lieting 5g, manna in the compositionss of every 1000
Alcohol 80-150g, Macrogol 8000 10-25g, Lactose 15-20g, Pregelatinized Starch 10-46g, polyvidone k30 5-16g, firmly
Fatty acid magnesium 1.8g, wherein, the particle size range of Li Gelieting is D90=10-50 μm.
2. tablet composition described in claim 1 is it is characterised in that contain favourable Ge Lieting 5g, sweet in the compositionss of every 1000
Dew alcohol 90-130g, Macrogol 8000 13-22g, Lactose 15-20g, Pregelatinized Starch 15-40g, polyvidone k30 8-13g,
Magnesium stearate 1.8g, wherein, the particle size range of Li Gelieting is D90=15-40 μm.
3. tablet composition described in claim 1 is it is characterised in that contain favourable Ge Lieting 5g, sweet in the compositionss of every 1000
Dew alcohol 90g, Macrogol 8000 13g, Lactose 15g, Pregelatinized Starch 15g, polyvidone k30 8g, magnesium stearate 1.8g, its
In, the particle size range of Li Gelieting is D90=20 μm.
4. tablet composition described in claim 1 is it is characterised in that contain favourable Ge Lieting 5g, sweet in the compositionss of every 1000
Dew alcohol 130g, Macrogol 8000 22g, Lactose 20g, Pregelatinized Starch 40g, polyvidone k30 13g, magnesium stearate 1.8g,
Wherein, the particle size range of Li Gelieting is D90=30 μm.
5. tablet composition described in claim 1 is it is characterised in that contain favourable Ge Lieting 5g, sweet in the compositionss of every 1000
Dew alcohol 100g, Macrogol 8000 18g, Lactose 18g, Pregelatinized Starch 30g, polyvidone k30 10g, magnesium stearate 1.8g,
Wherein, the particle size range of Li Gelieting is D90=40 μm.
6. tablet composition described in claim 1 preparation method it is characterised in that
The first step adopts jet mill to pulverize, and Li Gelieting is crushed to D90=10-50 μm；
Second step weighs the Li Gelieting of recipe quantity, mixs homogeneously with the Macrogol 8000 of recipe quantity；
3rd step weighs other adjuvants of recipe quantity, mixes with second step gained compounding substances；
4th step tabletting, 8mm scrobicula stamping, hardness 60-80N.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201610956027.7A CN106389364A (en) | 2016-10-28 | 2016-10-28 | Trajenta tablet composition and preparation method thereof |
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| CN201610956027.7A CN106389364A (en) | 2016-10-28 | 2016-10-28 | Trajenta tablet composition and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106389365A (en) * | 2016-10-28 | 2017-02-15 | 迪沙药业集团有限公司 | Trajenta tablet composition |
| CN115501195A (en) * | 2022-10-20 | 2022-12-23 | 北京惠之衡生物科技有限公司 | Linagliptin tablet and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014080384A1 (en) * | 2012-11-26 | 2014-05-30 | Ranbaxy Laboratories Limited | Pharmaceutical composition of linagliptin |
| CN105456270A (en) * | 2014-08-27 | 2016-04-06 | 石药集团中奇制药技术（石家庄）有限公司 | Dipeptidyl peptidase IV inhibitor pharmaceutical composition, use and preparation method thereof |
| CN106389365A (en) * | 2016-10-28 | 2017-02-15 | 迪沙药业集团有限公司 | Trajenta tablet composition |
-
2016
- 2016-10-28 CN CN201610956027.7A patent/CN106389364A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014080384A1 (en) * | 2012-11-26 | 2014-05-30 | Ranbaxy Laboratories Limited | Pharmaceutical composition of linagliptin |
| CN105456270A (en) * | 2014-08-27 | 2016-04-06 | 石药集团中奇制药技术（石家庄）有限公司 | Dipeptidyl peptidase IV inhibitor pharmaceutical composition, use and preparation method thereof |
| CN106389365A (en) * | 2016-10-28 | 2017-02-15 | 迪沙药业集团有限公司 | Trajenta tablet composition |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106389365A (en) * | 2016-10-28 | 2017-02-15 | 迪沙药业集团有限公司 | Trajenta tablet composition |
| CN115501195A (en) * | 2022-10-20 | 2022-12-23 | 北京惠之衡生物科技有限公司 | Linagliptin tablet and preparation method thereof |
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