CN104644580A - Pharmaceutical composition of teneligliptin - Google Patents
Pharmaceutical composition of teneligliptin Download PDFInfo
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- CN104644580A CN104644580A CN201310606266.6A CN201310606266A CN104644580A CN 104644580 A CN104644580 A CN 104644580A CN 201310606266 A CN201310606266 A CN 201310606266A CN 104644580 A CN104644580 A CN 104644580A
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- hydrobromic acid
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- gelatin
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Abstract
The invention relates to a pharmaceutical composition of teneligliptin and a preparation method of the pharmaceutical composition. The pharmaceutical composition of teneligliptin is characterized in that a corrigent in the pharmaceutical composition of teneligliptin is selected from gelatin and mannitol. The pharmaceutical composition is in the form of powder or particles, so that a preparation is good in stability, and bitter taste is masked; the pharmaceutical composition is relatively good in taste, rapid to disintegrate and absorb and convenient to carry.
Description
Technical field
The present invention relates to and a kind ofly containing hydrobromic acid pharmaceutical composition and preparation method thereof for Ge Lieting, hydrobromic acid is prepared into taste masking compositions for Ge Lieting, then add other adjuvant and be prepared into hydrobromic acid for Ge Lieting dispersible tablet.
Background technology
For Ge Lieting, its chemistry is by name: 3-[[(2S, 4S)-4-[4-(3-methyl isophthalic acid-phenyl-1H-pyrazoles-5-base)-1-piperazinyl]-2-pyrrolidinyl] formoxyl] Thiazolidine, molecular weight: 426.58.Its structural formula is as follows:
pharmacology type:the 7th DDP-4 inhibitor of whole world listing.
indication:for improving the glycemic control of type 2 diabetes mellitus patient.
usage and dosage:this product recommended dose is 20mg/ days, once a day, and oral administration.As effectively do not controlled patient blood glucose, dosage can increase to 40mg/ days, once a day.
For Ge Lieting Yuan Yan producer Shi Tianbian Mitsubishi Pharmaceutical Co., Ltd, in June, 2012 goes on the market in Japan, ratifies the glycemic control for improving type 2 diabetes mellitus patient.This product is applicable to the following situation that effectively can not control patient blood glucose: 1. diet, exercise therapy; 2. diet, exercise therapy coordinate sulfonylureas treatment; 3. diet, exercise therapy coordinate thiazolidinedione treatment.
Chinese patent CN 102711761 discloses a kind of solid preparation containing teneligliptin, described solid preparation comprises containing teneligliptin part independently, describedly contain teneligliptin or its salt or its solvate containing teneligliptin part, wherein the percentage composition of teneligliptin or its salt or its solvate is 1.5 to 10 times of the percentage composition that solid preparation is expected.
Pharmaceutical composition for Ge Lieting taste masking compositions prepared by the present invention, gelatin, mannitol is selected from for the correctives in Ge Lieting taste masking compositions, this pharmaceutical composition exists with the form of powder or granule, better stability of preparation can be made and mask bitterness, mouthfeel is better, disintegrate is fast, absorbs fast, easy to carry.
Therefore, the present inventor adopts special preparation technique to mask the mouthfeel of its bitterness, adopts proper auxiliary materials prepared composition discrete piece, overcomes and absorb the slow shortcoming of slow metabolism for Ge Lieting.
Summary of the invention
The object of this invention is to provide a kind of new hydrobromic acid for Ge Lieting combination of oral medication, it is characterized in that: containing hydrobromic acid for Ge Lieting taste masking compositions, filler, disintegrating agent, correctives and lubricant.
Another object of the present invention is to provide and a kind ofly utilizes described compositions to prepare hydrobromic acid for the method for Ge Lieting pharmaceutical composition.
According to an aspect of the present invention, described filler is selected from microcrystalline Cellulose, and described disintegrating agent is selected from cross-linking sodium carboxymethyl cellulose, and described correctives is selected from mannitol, and described lubricant is selected from magnesium stearate.
According to an aspect of the present invention, hydrobromic acid is provided to replace Ge Lieting taste masking compositions, described hydrobromic acid is selected from mannitol and gelatin and hydrobromic acid for Ge Lieting taste masking compositions to be prepared through special process for Ge Lieting and makes to be uniformly dispersed, and described hydrobromic acid replaces Ge Lieting and mannitol, the weight proportion of gelatin is: 1:2:5 or 1:6:4.
According to another aspect of the present invention, hydrobromic acid for the special process described in Ge Lieting taste masking compositions is: gelatin and mannitol are crossed 60 mesh sieves respectively, appropriate distilled water is added in gelatin, make Gelatin, under agitation add hydrobromic acid respectively for Ge Lieting and mannitol, put in 70 ~ 80 DEG C of water-baths and mix evaporate to dryness, pulverize, cross 50 mesh sieves, to obtain final product.
According to another aspect of the present invention, provide a kind of and prepare the method for hydrobromic acid for the pharmaceutical composition of Ge Lieting taste masking compositions, comprise the following steps:
1) gelatin, mannitol are crossed 60 mesh sieves respectively, in gelatin, add appropriate distilled water, make Gelatin, under agitation add hydrobromic acid respectively for Ge Lieting and mannitol, put in 70 ~ 80 DEG C of water-baths and mix evaporate to dryness, pulverize, cross 50 mesh sieves, for subsequent use;
2) microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, mannitol, fragrant citrus essence, magnesium stearate are sieved for subsequent use respectively;
3) by 1) in obtained hydrobromic acid for Ge Lieting taste masking compositions and 2) middle adjuvant mixs homogeneously, tabletting, to obtain final product.
Advantage of the present invention is technical maturity, simple to operate, is applicable to industrial large-scale production.
Advantage of the present invention is to adopt special process to prepare hydrobromic acid for Ge Lieting taste masking compositions, thus improves mouthfeel.
Advantage of the present invention is to adopt hydrobromic acid to prepare dispersible tablet for Ge Lieting taste masking compositions, makes its disintegrate rapid, overcomes and absorbs the slow shortcoming of slow metabolism.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, but the non-scope being only limitted to these embodiments of scope of the present invention should be understood.
embodiment 1
Hydrobromic acid is for the preparation of Ge Lieting taste masking compositions
Hydrobromic acid is for Ge Lieting 20g
Mannitol 40g
Gelatin 100g
Make 1000
Preparation technology: gelatin, mannitol are crossed 60 mesh sieves respectively, adds appropriate distilled water, make Gelatin in gelatin, under agitation adds hydrobromic acid respectively for Ge Lieting and mannitol, puts in 70 ~ 80 DEG C of water-baths and mix evaporate to dryness, pulverize, cross 50 mesh sieves, for subsequent use;
(2) hydrobromic acid is for the preparation of lattice row orally disintegration tablet
Hydrobromic acid is for Ge Lieting masked composition 100g
Microcrystalline Cellulose 60g
Cross-linking sodium carboxymethyl cellulose 24g
Mannitol 13.5g
Magnesium stearate 2.5g
Make 1000
Preparation technology: check weighing through double, mix homogeneously, tabletting by above-mentioned supplementary material amount, hardness, at 5-7kg, to obtain final product.
embodiment 2
(1) hydrobromic acid is for the preparation of Ge Lieting taste masking compositions
Hydrobromic acid is for Ge Lieting 20g
Mannitol 120g
Gelatin 80g
Make 1000
Preparation technology: gelatin, mannitol are crossed 60 mesh sieves respectively, adds appropriate distilled water, make Gelatin in gelatin, under agitation adds hydrobromic acid respectively for Ge Lieting and mannitol, puts in 70 ~ 80 DEG C of water-baths and mix evaporate to dryness, pulverize, cross 50 mesh sieves, for subsequent use;
(2) hydrobromic acid is for the preparation of lattice row orally disintegration tablet
Hydrobromic acid is for Ge Lieting masked composition 100g
Microcrystalline Cellulose 60g
Cross-linking sodium carboxymethyl cellulose 24g
Mannitol 13.5g
Magnesium stearate 2.5g
Make 1000
Preparation technology: check weighing through double, mix homogeneously, tabletting by above-mentioned supplementary material amount, hardness, at 5-7kg, to obtain final product.
test example 1
Select volunteer to carry out mouthfeel and dispersing uniformity time detecting to the sample of above-described embodiment, comprehensively its structure, averages, and mouthfeel and dispersing uniformity testing result are in table 1.
the mouthfeel of each embodiment of table 1 and dispersing uniformity
| Embodiment | Dispersing uniformity (second) | Taste |
| Embodiment 1 | 90 | ++ |
| Embodiment 2 | 85 | ++ |
[note] +++: fabulous ++: good+: general-: poor--: poor---: extreme difference
Conclusion: after hydrobromic acid is prepared into taste masking compositions for Ge Lieting and mannitol, gelatin by special process, effectively mask the zest of medicine, and on using the dispersing uniformity of said composition prepared composition discrete piece without impact, its preparation method is simple and easy to do simultaneously, cost is low, demonstrates this taste masking compositions and has excellent characteristic.
Claims (7)
1. a hydrobromic acid is for the Pharmaceutical composition of Ge Lieting, it is characterized in that: containing hydrobromic acid for Ge Lieting taste masking compositions, filler, disintegrating agent, correctives and lubricant, described hydrobromic acid is selected from mannitol, gelatin for Ge Lieting taste masking compositions, and hydrobromic acid for the weight proportion of Ge Lieting and mannitol, gelatin is: 1:2:5 or 1:6:4.
2. hydrobromic acid according to claim 1 is for the Pharmaceutical composition of Ge Lieting, it is characterized in that described filler is selected from microcrystalline Cellulose.
3. hydrobromic acid according to claim 1 is for the Pharmaceutical composition of Ge Lieting, it is characterized in that described disintegrating agent is selected from cross-linking sodium carboxymethyl cellulose.
4. hydrobromic acid according to claim 1 is for the Pharmaceutical composition of Ge Lieting, and it is characterized in that described correctives is selected from mannitol, described lubricant is selected from magnesium stearate.
5. hydrobromic acid according to claim 1 is for the Pharmaceutical composition of Ge Lieting, it is characterized in that this compositions is dispersible tablet.
6. hydrobromic acid according to claim 1 is for the Pharmaceutical composition of Ge Lieting, it is characterized in that each component is:
Weight ratio of constituents (%)
Hydrobromic acid is for Ge Lieting taste masking compositions 50%
Microcrystalline Cellulose 30%
Cross-linking sodium carboxymethyl cellulose 12%
Mannitol 6.75%
Magnesium stearate 1.25%.
7. hydrobromic acid according to claim 1 is for the preparation method of the Pharmaceutical composition of Ge Lieting, it is characterized in that comprising following preparation steps:
1) gelatin, mannitol are crossed 60 mesh sieves respectively, in gelatin, add appropriate distilled water, make Gelatin, under agitation add hydrobromic acid respectively for Ge Lieting and mannitol, put in 70 ~ 80 DEG C of water-baths and mix evaporate to dryness, pulverize, cross 50 mesh sieves, for subsequent use;
2) microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, magnesium stearate are sieved for subsequent use respectively;
3) by 1) in obtained hydrobromic acid for Ge Lieting taste masking compositions and 2) middle adjuvant mixs homogeneously, tabletting, to obtain final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310606266.6A CN104644580A (en) | 2013-11-25 | 2013-11-25 | Pharmaceutical composition of teneligliptin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310606266.6A CN104644580A (en) | 2013-11-25 | 2013-11-25 | Pharmaceutical composition of teneligliptin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104644580A true CN104644580A (en) | 2015-05-27 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310606266.6A Pending CN104644580A (en) | 2013-11-25 | 2013-11-25 | Pharmaceutical composition of teneligliptin |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106913535A (en) * | 2015-12-25 | 2017-07-04 | 江苏万邦生化医药股份有限公司 | A kind of DDP-4 inhibitor medicaments oral disintegrating tablet and preparation method thereof |
| WO2020209350A1 (en) * | 2019-04-12 | 2020-10-15 | 田辺三菱製薬株式会社 | Rapid disintegrating oral tablet for treatment of diabetes |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101632665A (en) * | 2009-09-01 | 2010-01-27 | 严洁 | Novel torasemide oral medicine composition |
| CN102008466A (en) * | 2010-11-29 | 2011-04-13 | 天津市汉康医药生物技术有限公司 | Febuxostat medicament composition and preparation method thereof |
| CN102711761A (en) * | 2009-12-18 | 2012-10-03 | 田边三菱制药株式会社 | Elution-stabilized preparation |
-
2013
- 2013-11-25 CN CN201310606266.6A patent/CN104644580A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101632665A (en) * | 2009-09-01 | 2010-01-27 | 严洁 | Novel torasemide oral medicine composition |
| CN102711761A (en) * | 2009-12-18 | 2012-10-03 | 田边三菱制药株式会社 | Elution-stabilized preparation |
| CN102008466A (en) * | 2010-11-29 | 2011-04-13 | 天津市汉康医药生物技术有限公司 | Febuxostat medicament composition and preparation method thereof |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106913535A (en) * | 2015-12-25 | 2017-07-04 | 江苏万邦生化医药股份有限公司 | A kind of DDP-4 inhibitor medicaments oral disintegrating tablet and preparation method thereof |
| WO2020209350A1 (en) * | 2019-04-12 | 2020-10-15 | 田辺三菱製薬株式会社 | Rapid disintegrating oral tablet for treatment of diabetes |
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