CO2019001110A2 - Improved composition of teneligliptin and metformin and process to prepare it - Google Patents
Improved composition of teneligliptin and metformin and process to prepare itInfo
- Publication number
- CO2019001110A2 CO2019001110A2 CONC2019/0001110A CO2019001110A CO2019001110A2 CO 2019001110 A2 CO2019001110 A2 CO 2019001110A2 CO 2019001110 A CO2019001110 A CO 2019001110A CO 2019001110 A2 CO2019001110 A2 CO 2019001110A2
- Authority
- CO
- Colombia
- Prior art keywords
- metformin
- improved
- teneligliptin
- pharmaceutical composition
- compressibility
- Prior art date
Links
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 title abstract 5
- 229960003105 metformin Drugs 0.000 title abstract 5
- 239000000203 mixture Substances 0.000 title abstract 3
- WGRQANOPCQRCME-PMACEKPBSA-N teneligliptin Chemical group O=C([C@H]1NC[C@H](C1)N1CCN(CC1)C1=CC(=NN1C=1C=CC=CC=1)C)N1CCSC1 WGRQANOPCQRCME-PMACEKPBSA-N 0.000 title abstract 3
- 229950000034 teneligliptin Drugs 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000003826 tablet Substances 0.000 abstract 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 238000007906 compression Methods 0.000 abstract 1
- 230000006835 compression Effects 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 abstract 1
- 239000008187 granular material Substances 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 239000000314 lubricant Substances 0.000 abstract 1
- 235000019359 magnesium stearate Nutrition 0.000 abstract 1
- 239000007935 oral tablet Substances 0.000 abstract 1
- 229940096978 oral tablet Drugs 0.000 abstract 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 1
- 229940069328 povidone Drugs 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
- 238000005550 wet granulation Methods 0.000 abstract 1
Classifications
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se refiere a una composición farmacéutica mejorada en la forma de comprimido oral recubierto, con Teneligliptina o sus sales farmacéuticamente aceptables y Metformina o sus sales farmacéuticamente aceptables para el tratamiento de diabetes mellitus tipo 2. Dicha composición farmacéutica es obtenida por granulación húmeda, utilizando Metformina molida a polvo fino y baja carga de excipientes, consistentes en un aglutinante, en este caso Povidona y Estearato de Magnesio como lubricante durante la compresión. El hecho de utilizar la Metformina molida, mejora notablemente la compresibilidad de la misma, permitiendo a su vez optimizar las condiciones operativas. La composición farmacéutica mejorada, comprendiendo la combinación de Teneligliptina y Metformina, comparada con ambos principios activos por separado, vehiculizados en la forma de comprimidos recubiertos, no mostro diferencias en la liberación in vitro (disolución), y por otro lado mejoró la compresibilidad del granulado y la friabilidad de los comprimidos. Los aspectos mencionados hacen que esta composición mejorada se diferencie de otras composiciones que contienen los mismos activos y que utilizan mayor número de excipientes, y es por consiguiente, el objeto principal de la presente invención.The present invention relates to an improved pharmaceutical composition in the form of an oral tablet coated with Teneligliptin or its pharmaceutically acceptable salts and Metformin or its pharmaceutically acceptable salts for the treatment of type 2 diabetes mellitus. Said pharmaceutical composition is obtained by wet granulation, using fine powdered ground Metformin and low excipient load, consisting of a binder, in this case Povidone and Magnesium Stearate as a lubricant during compression. The fact of using ground Metformin significantly improves its compressibility, allowing in turn to optimize operating conditions. The improved pharmaceutical composition, comprising the combination of Teneligliptin and Metformin, compared to both active ingredients separately, vehiculized in the form of coated tablets, showed no differences in in vitro release (dissolution), and on the other hand improved the compressibility of the granulate and the friability of the tablets. The mentioned aspects make this improved composition different from other compositions that contain the same assets and use a greater number of excipients, and is therefore the main object of the present invention.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MX2016010682A MX2016010682A (en) | 2016-08-17 | 2016-08-17 | Improved composition of teneligliptin and metformin and method for preparing same. |
| PCT/IB2017/053749 WO2018033808A1 (en) | 2016-08-17 | 2017-06-23 | Improved composition of teneligliptin and metformin and method for preparing same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2019001110A2 true CO2019001110A2 (en) | 2019-04-12 |
Family
ID=61196457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2019/0001110A CO2019001110A2 (en) | 2016-08-17 | 2019-02-05 | Improved composition of teneligliptin and metformin and process to prepare it |
Country Status (9)
| Country | Link |
|---|---|
| AR (1) | AR109253A1 (en) |
| BR (1) | BR112019002909A2 (en) |
| CL (1) | CL2019000273A1 (en) |
| CO (1) | CO2019001110A2 (en) |
| DO (1) | DOP2019000035A (en) |
| EC (2) | ECSP19010066A (en) |
| MX (1) | MX2016010682A (en) |
| PE (1) | PE20190402A1 (en) |
| WO (1) | WO2018033808A1 (en) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014080383A1 (en) * | 2012-11-26 | 2014-05-30 | Ranbaxy Laboratories Limited | Pharmaceutical composition of dipeptidyl peptidase-iv (dpp-iv) inhibitors in combination with other antidiabetics |
| WO2015132679A1 (en) * | 2014-03-05 | 2015-09-11 | Glenmark Pharmaceuticals Ltd | Teneligliptin compositions |
-
2016
- 2016-08-17 MX MX2016010682A patent/MX2016010682A/en unknown
-
2017
- 2017-06-23 PE PE2019000305A patent/PE20190402A1/en unknown
- 2017-06-23 WO PCT/IB2017/053749 patent/WO2018033808A1/en active Application Filing
- 2017-06-23 BR BR112019002909-5A patent/BR112019002909A2/en active Search and Examination
- 2017-07-04 AR ARP170101849A patent/AR109253A1/en unknown
-
2019
- 2019-02-01 CL CL2019000273A patent/CL2019000273A1/en unknown
- 2019-02-05 CO CONC2019/0001110A patent/CO2019001110A2/en unknown
- 2019-02-12 EC ECSENADI201910066A patent/ECSP19010066A/en unknown
- 2019-02-18 DO DO2019000035A patent/DOP2019000035A/en unknown
- 2019-06-25 EC ECSENADI201944926A patent/ECSP19044926A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018033808A1 (en) | 2018-02-22 |
| MX2016010682A (en) | 2018-02-16 |
| BR112019002909A2 (en) | 2019-05-21 |
| ECSP19044926A (en) | 2019-07-31 |
| AR109253A1 (en) | 2018-11-14 |
| ECSP19010066A (en) | 2019-11-30 |
| PE20190402A1 (en) | 2019-03-13 |
| CL2019000273A1 (en) | 2019-06-28 |
| DOP2019000035A (en) | 2019-06-30 |
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