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Us 2017 / 0239276 A1 US 20170239276A1 ( 19) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2017/ 0239276 A1 MUTLU et al. ( 43 ) Pub . Date: Aug . 24 , 2017 ( 54 ) PHARMACEUTICAL COMBINATIONS OF ( 30 ) Foreign Application Priority Data SITAGLIPTIN Sep. 5 , 2014 ( TR ) .. .. .. .. .. 2014 / 10448 (71 ) Applicant : SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETI, Publication Classification ISTANBUL ( TR ) (51 ) Int. Cl. ( 72 ) Inventors : ONUR MUTLU , ISTANBUL ( TR ) ; A61K 31/ 64 (2006 .01 ) ALI TÜRKYILMAZ , ISTANBUL A61K 9 / 20 ( 2006 . 01 ) ( TR ) ; GÜLAY YELKEN , ISTANBUL A61K 9 / 28 ( 2006 . 01 ) ( TR ); MEHTAP SAYDAM , A61K 31/ 4985 ( 2006 . 01 ) ISTANBUL ( TR ) (52 ) U . S . CI. CPC .. .. .. A61K 31 /64 ( 2013 .01 ) ; A61K 31 /4985 ( 21 ) Appl. No. : (2013 .01 ) ; A61K 9 / 2027 ( 2013 .01 ) ; A61K 15 / 507, 946 9 /2054 ( 2013 .01 ) ; A61K 9 / 28 (2013 .01 ) ( 22 ) PCT Filed : Sep . 4 , 2015 (57 ) ABSTRACT (86 ) PCT NONo . : PCT /EP2015 /070251 A pharmaceutical combination comprising sitagliptin or a $ 371 ( c ) ( 1 ) , pharmaceutically acceptable salt thereof in combination ( 2 ) Date : Mar. 1 , 2017 with a sulfonylurea . US 2017 /0239276 A1 Aug . 24 , 2017 PHARMACEUTICAL COMBINATIONS OF 4 - ( 2 , 4 , 5 - trifluorophenyl) butan - 1 - one or (2R ) - 4 - oxo - 4 - [ 3 SITAGLIPTIN ( trifluoromethyl) - 5 ,6 - dihydro [ 1, 2 , 4 ] triazolo [ 4 , 3 - a ]pyrazin FIELD OF INVENTION 7 (8H )- yl )- 1 - ( 2 ,4 ,5 -trifluorophenyl ) butan - 2 - amine) and its [0001 ] The present invention relates to a pharmaceutical chemical structure is shown in the Formula I . combination comprising sitagliptin or a pharmaceutically [0004 ] Sitagliptin is licensed in the US and EU under the acceptable salt thereof in combination with a sulfonylurea name of JANUVIA in the strength of 100 mg, 50 mg, and 25 and at least one pharmaceutically acceptable excipient. mg. The recommended dose is 100 mg once daily . [ 0005 ] DPP -4 inhibitors , especially sitagliptin have a BACKGROUND OF INVENTION novel mechanism of action , and many studies are available [0002 ] Sitagliptin is indicated as an adjunct to diet and which shows their efficacy and safety in monotherapy or exercise to improve glycemic control in adults with type 2 combination therapy . When the single sitagliptin alone does diabetes mellitus . It is an oral antihyperglycemic of the not provide adequate glycemic control, sulfonylureas are the dipeptidyl peptidase - 4 (DPP - 4 ) inhibitor class . DPP - 4 most common co - administered drugs of it . inhibitors work by blocking the action of DPP - 4 , an enzyme [0006 ] Sitagliptin increase plasma GLP - 1 concentration which destroys the hormone incretin . There are two types of and elevate cellular cAMP levels in pancreatic beta - cells incretin hormones found in the body, called glucagon -like leading to potentiate insulin secretion , whereas sulfonylurea peptide - 1 (GLP - 1 ) and glucose - dependent insulinotropic drugs stimulate insulin secretion as a result of elevation of peptide (GIP ) . These hormones are naturally produced by cytosolic Ca2+ concentration in the beta - cells . Therefore , the body in response to food intake . Their function is to help they both help to reduce blood glucose levels in different the body produce more insulin only when it is needed and pathways in type 2 diabetes patients and it is anticipated that reduce the amount of glucose being produced by the liver a combination therapy of sitagliptin and sulfonylurea may when it is not needed . Sitagliptin works by binding to DPP - 4 synergistically stimulate insulin secretion and effectively and preventing it from breaking down the GLP - 1 and GIP . ameliorate hyperglycemia in type 2 diabetes mellitus . This increases the levels of these hormones in the body and [0007 ] Sulfonylureas are divided into two categories : first so increases their effect on controlling blood sugar . generation drugs are comprising tolbutamide , chlorprop amide , tolazamide, acetohexamide and carbutamide; and Formula I second generation drugs are comprising glimepiride, gliclaz ide, glyburide ( glibenclamide ), glipizide, glibornuride, gliq uidone, glisoxepide and glyclopyramide . F [ 0008 ] Glimepiride is a second generation sulfonylurea . It is used as an adjuvant to reduce blood sugar level in “ diabetes mellitus type II ” patients . As do all other sulfo Zl nylureas , it enhances the secretion of insulin from pancreatic beta cells and provides an insulin - like effect . The chemical name of glimepiride is 1 - {{ p -( 2 - (3 -ethyl - 4 -methyl - 2 - oxo - 3 pyrroline- 1 -carboxamide ) ethyl ) phenyl } sulfonyl ) - 3 - (trans [ 0003 ] It is named as (3R ) - 3 - amino - 1 - ( 3 - ( trifluorom 4 -methylcyclohexyl ) urea and the chemical structure is ethyl) - 6 , 8 -dihydro -5H - [ 1 , 2 , 4 ] triazolo [ 4 , 3 - a ]pyrazin - 7 - yl ] - shown in Formula II . Formula II H3C =0 H CH ; H3C — CH2 NH – CH2 – CH2 – – SO - NH 1- C?NH. XX - US 2017 /0239276 A1 Aug . 24 , 2017 [ 0009 ] Glimepiride is marketed under the trademark tilayer tablet , mini tablet , capsule , gelatin capsule , oral AMARYL® in 1 , 2 , and 4 mg dosage forms. It is used as an granule , powder, sachet or a pellet. adjunct to diet and exercise to improve glycemic control in [ 0020 ] In one embodiment, the sulfonylurea in the phar adults with type 2 diabetes mellitus . maceutical combination of this present invention is selected [0010 ] In prior art , glimepiride molecule was first dis from the group comprising glimepiride, gliclazide, glipizide , closed in the patent EP0031058 . glibenclamide (glyburide ) , glibornuride , gliquidone , glisox [0011 ] Gliclazide N - ( 4 -methylbenzenesulfonyl ) - N - ( 3 epide , glyclopyramide, tolbutamide, chlorpropamide , tolaz azabicyclo [ 3 . 3 . 0 ] - oct - 3 - yl ) urea ) , one type of second genera amide, acetohexamide and carbutamide or pharmaceutically tion sulfonylureas, is an active agent which has antidiabetic acceptable salts thereof. More preferably, the sulfonylurea is properties and its chemical structure is illustrated with glimepiride or gliclazide. Formula III. [0021 ] In one embodiment , sulfonylureas used in the pharmaceutical combination of this present invention com prise first generation sulfonylureas and second generation Formula III sulfonylureas . [ 0022 ] According to this embodiment , first generation sulfonylureas comprise tolbutamide , chlorpropamide , tola zamide , acetohexamide and carbutamide ; second generation sulfonylureas comprise glimepiride, gliclazide, glipizide , glibenclamide ( glyburide ), glibornuride , gliquidone , glisox N epide and glyclopyramide . [0023 ]. While combining more than one molecule in one dosage form is increasing the patients ' quality of life , many [ 0012 ] Gliclazide has been administered in the form of 80 challenges also occur such as the physicochemical compat mg conventional tablets . It is recommended to be adminis ibility between the different active agents and / or between the tered one tablet twice a day . active agents and the excipients used ; and the therapeutical [0013 ] The formulation of gliclazide was first disclosed in compatibility between the two active agents regarding their the patent document U . S . Pat . No . 3 , 501, 495 (SCIENCE pharmacokinetic and / or pharmaceutical properties in order UNION ET CIE . SOC . ), with hypoglycemic properties , and that the posology of the combined formulation allows to is orally used in the treatment of diabetes mellitus. obtain safe and efficient plasma levels of both pharmaco [ 0014 ] In prior art, there are many pharmaceutical com logical agents . bination studies about sitagliptin . For instance , WO 2009 / 10024 ] It is well known that drugs even used in the same 099734 discloses pharmaceutical compositions providing an therapeutic area cannot always be combined in a dosage extended release ofmetformin and an immediate release of form . The scientific literature is full of examples wherein sitagliptin . The tablet core is comprised ofmetformin and an compounds of different classes, which are used to treat the extended release excipient (HPMC ) (Hydroxypropyl meth same indications , cannot be combined into safe and effica ylcellulose ) . The tablet core is then coated with immediate cious dosage forms thereby resulting in incompatible drug release polymer comprising sitagliptin . However , in prior combinations . The reasons for this unexpected lack of art , no study has been done in terms of sitagliptin and compatibility are varied ; however, it is often found that the sulfonylurea combinations . incompatible drug combinations result in increased side [ 0015 ] There is a need in the art for a pharmaceutical effects , unwanted drug interactions or additional side effects . formulation or a dosage form that is to combine sitagliptin More specifically , when sitagliptin is used in combination and sulfonylureas . However , some problems may be with a sulfonylurea , they may cause hypoglycemia as an occurred while combining these two antidiabetic drugs such additional side effect. Therefore , a lower dose of sulfony as, additional undesired side effects , physicochemical lurea is required to reduce the risk of hypoglycemia . incompatibility and therapeutical incompatibility problems. [0025 ] According to this embodiment, sitagliptin or a [0016 ] In this present invention , a pharmaceutical combi pharmaceutically acceptable salt thereof is present in an nation comprising sitagliptin or a pharmaceutically accept amount of between 1 . 5 - 90 % , preferably 15 -50 % and more able
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