TR202009724A2 - FORMULATION OF CYTAGLIPTIN IN ORAL DISTRIBUTION TABLET - Google Patents
FORMULATION OF CYTAGLIPTIN IN ORAL DISTRIBUTION TABLETInfo
- Publication number
- TR202009724A2 TR202009724A2 TR2020/09724A TR202009724A TR202009724A2 TR 202009724 A2 TR202009724 A2 TR 202009724A2 TR 2020/09724 A TR2020/09724 A TR 2020/09724A TR 202009724 A TR202009724 A TR 202009724A TR 202009724 A2 TR202009724 A2 TR 202009724A2
- Authority
- TR
- Turkey
- Prior art keywords
- sitagliptin
- tablet formulation
- sodium
- feature
- orally disintegrating
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 68
- 238000009472 formulation Methods 0.000 title claims abstract description 47
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims abstract description 54
- 229960004034 sitagliptin Drugs 0.000 claims abstract description 51
- 150000003839 salts Chemical class 0.000 claims abstract description 21
- 239000003826 tablet Substances 0.000 claims abstract description 16
- 238000000034 method Methods 0.000 claims abstract description 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 7
- 239000007919 dispersible tablet Substances 0.000 claims abstract description 6
- 239000006191 orally-disintegrating tablet Substances 0.000 claims description 21
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 16
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 11
- 229960000913 crospovidone Drugs 0.000 claims description 11
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 11
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 11
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 10
- 239000003085 diluting agent Substances 0.000 claims description 10
- 229940049920 malate Drugs 0.000 claims description 10
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 10
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 9
- 229930195725 Mannitol Natural products 0.000 claims description 9
- 239000000594 mannitol Substances 0.000 claims description 9
- 235000010355 mannitol Nutrition 0.000 claims description 9
- 108010011485 Aspartame Proteins 0.000 claims description 8
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 8
- 239000000605 aspartame Substances 0.000 claims description 8
- 235000010357 aspartame Nutrition 0.000 claims description 8
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 8
- 229960003438 aspartame Drugs 0.000 claims description 8
- 235000003599 food sweetener Nutrition 0.000 claims description 8
- 235000019359 magnesium stearate Nutrition 0.000 claims description 8
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 8
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 8
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 8
- 239000003765 sweetening agent Substances 0.000 claims description 8
- 239000000454 talc Substances 0.000 claims description 7
- 229910052623 talc Inorganic materials 0.000 claims description 7
- 229940033134 talc Drugs 0.000 claims description 7
- 235000012222 talc Nutrition 0.000 claims description 7
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 6
- 239000007884 disintegrant Substances 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 5
- 239000011734 sodium Substances 0.000 claims description 5
- 229910052708 sodium Inorganic materials 0.000 claims description 5
- 239000007916 tablet composition Substances 0.000 claims description 5
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 4
- 229960001031 glucose Drugs 0.000 claims description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims description 4
- 239000003456 ion exchange resin Substances 0.000 claims description 4
- 229920003303 ion-exchange polymer Polymers 0.000 claims description 4
- 239000000377 silicon dioxide Substances 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 235000010356 sorbitol Nutrition 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 229940032147 starch Drugs 0.000 claims description 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 3
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 3
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 3
- 239000008103 glucose Substances 0.000 claims description 3
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 3
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 3
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 3
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 3
- 239000000811 xylitol Substances 0.000 claims description 3
- 235000010447 xylitol Nutrition 0.000 claims description 3
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 3
- 229960002675 xylitol Drugs 0.000 claims description 3
- PNXSHNOORJKXDW-SBSPUUFOSA-N (3r)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5h-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochloride Chemical compound Cl.C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F PNXSHNOORJKXDW-SBSPUUFOSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims description 2
- 239000004386 Erythritol Substances 0.000 claims description 2
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 2
- 239000005715 Fructose Substances 0.000 claims description 2
- 229930091371 Fructose Natural products 0.000 claims description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 2
- WINXNKPZLFISPD-UHFFFAOYSA-M Saccharin sodium Chemical compound [Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 WINXNKPZLFISPD-UHFFFAOYSA-M 0.000 claims description 2
- 239000004376 Sucralose Substances 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 2
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 claims description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 2
- 239000000783 alginic acid Substances 0.000 claims description 2
- 235000010443 alginic acid Nutrition 0.000 claims description 2
- 229920000615 alginic acid Polymers 0.000 claims description 2
- 229960001126 alginic acid Drugs 0.000 claims description 2
- 150000004781 alginic acids Chemical class 0.000 claims description 2
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims description 2
- 239000001506 calcium phosphate Substances 0.000 claims description 2
- 159000000007 calcium salts Chemical class 0.000 claims description 2
- 239000000378 calcium silicate Substances 0.000 claims description 2
- 229910052918 calcium silicate Inorganic materials 0.000 claims description 2
- 229960003340 calcium silicate Drugs 0.000 claims description 2
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims description 2
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 claims description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 claims description 2
- 229940096516 dextrates Drugs 0.000 claims description 2
- 239000008121 dextrose Substances 0.000 claims description 2
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims description 2
- 229940038472 dicalcium phosphate Drugs 0.000 claims description 2
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims description 2
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims description 2
- RRPFCKLVOUENJB-UHFFFAOYSA-L disodium;2-aminoacetic acid;carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O.NCC(O)=O RRPFCKLVOUENJB-UHFFFAOYSA-L 0.000 claims description 2
- 239000002270 dispersing agent Substances 0.000 claims description 2
- 229960000878 docusate sodium Drugs 0.000 claims description 2
- 235000019414 erythritol Nutrition 0.000 claims description 2
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 2
- 229940009714 erythritol Drugs 0.000 claims description 2
- 229960002737 fructose Drugs 0.000 claims description 2
- -1 glidants Substances 0.000 claims description 2
- 239000008240 homogeneous mixture Substances 0.000 claims description 2
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims description 2
- 239000008101 lactose Substances 0.000 claims description 2
- 229960001375 lactose Drugs 0.000 claims description 2
- 229960000502 poloxamer Drugs 0.000 claims description 2
- 229920001983 poloxamer Polymers 0.000 claims description 2
- 229920001282 polysaccharide Polymers 0.000 claims description 2
- 239000005017 polysaccharide Substances 0.000 claims description 2
- 150000004804 polysaccharides Chemical class 0.000 claims description 2
- 239000011591 potassium Substances 0.000 claims description 2
- 229910052700 potassium Inorganic materials 0.000 claims description 2
- 229960003975 potassium Drugs 0.000 claims description 2
- 238000003825 pressing Methods 0.000 claims description 2
- 229960004115 sitagliptin phosphate Drugs 0.000 claims description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
- 239000011780 sodium chloride Substances 0.000 claims description 2
- 229960002668 sodium chloride Drugs 0.000 claims description 2
- 229960001462 sodium cyclamate Drugs 0.000 claims description 2
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims description 2
- 239000008109 sodium starch glycolate Substances 0.000 claims description 2
- 229940079832 sodium starch glycolate Drugs 0.000 claims description 2
- 229920003109 sodium starch glycolate Polymers 0.000 claims description 2
- 229960002920 sorbitol Drugs 0.000 claims description 2
- 235000019408 sucralose Nutrition 0.000 claims description 2
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- RTZRUVMEWWPNRR-UHFFFAOYSA-N tert-butyl n-(3-iodo-1h-pyrrolo[2,3-b]pyridin-5-yl)carbamate Chemical compound CC(C)(C)OC(=O)NC1=CN=C2NC=C(I)C2=C1 RTZRUVMEWWPNRR-UHFFFAOYSA-N 0.000 claims description 2
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- 235000010493 xanthan gum Nutrition 0.000 claims description 2
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- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
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- 229920002774 Maltodextrin Polymers 0.000 claims 2
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- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 1
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- 239000001530 fumaric acid Substances 0.000 claims 1
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims 1
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- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims 1
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- 229910000021 magnesium carbonate Inorganic materials 0.000 claims 1
- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims 1
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims 1
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Classifications
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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Abstract
Mevcut buluş; sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu ve en az bir farmasötik olarak kabul edilebilir eksipiyan içeren ağızda dağılan bir tablet formülasyonu ile ilgilidir. Ayrıca mevcut buluş, söz konusu ağızda dağılan tableti hazırlama yöntemi de sunmaktadır.The present invention; relates to an orally dispersible tablet formulation comprising sitagliptin or a pharmaceutically acceptable salt of sitagliptin and at least one pharmaceutically acceptable excipient. Furthermore, the present invention provides a method of preparing said orodispersible tablet.
Description
TARFNAME SITAGLIPTININ AGIZDA DAGILAN TABLET FORMÜLASYONU Teknik Alan Mevcut bulus; sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu ve en az bir farmasötik olarak kabul edilebilir eksipiyan içeren agizda dagilan bir tablet formülasyonu ile ilgilidir. Ayrica mevcut bulus, söz konusu agizda dagilan tableti hazirlama yöntemi de sunmaktadir. DESCRIPTION ORAL DISSOLVABLE TABLET FORMULATION OF SITAGLIPTIIN Technical Field Present invention; sitagliptin or a pharmaceutically acceptable salt of sitagliptin and most An orodispersible tablet containing a small amount of pharmaceutically acceptable excipient It's about formulation. Moreover, the present invention is based on the preparation of the said orally disintegrating tablet. It also offers the method.
Teknigin Bilinen Durumu Diabetes mellitus, sekresyon degisimi sonucunda insülin etkisinin azaldigi veya yok oldugu ve/veya insülin aktivitesinin azaldigi bir grup karbonhidrat metabolizmasi bozuklugudur. Tip 1 ve Tip 2 olmak üzere iki ana diyabet tipi bulunmaktadir: Tip 1 diyabet, pankreasin insülin üreten hücrelerinin (beta hücreleri) hasar görmesi nedeniyle olusur. Tip 1 diyabette ise pankreas az insülin üretimi yapar veya hiç yapmaz, böylece seker, enerji olarak kullanilmak üzere vücut hücrelerine giremez. Tip 1 diyabetli kisiler, kan sekerini kontrol etmek için insülin enjeksiyonlari kullanmalidir. Known Status of the Technique Diabetes mellitus is a condition in which the effect of insulin decreases or disappears as a result of secretion changes. It is a group of carbohydrate metabolism disorders in which insulin and/or insulin activity is reduced. Type 1 There are two main types of diabetes: Type 2 and Type 2: Type 1 diabetes is caused by damage to the insulin-producing cells of the pancreas (beta cells). consists of In type 1 diabetes, the pancreas produces little or no insulin, so sugar, It cannot enter body cells to be used as energy. People with type 1 diabetes, blood sugar Must use insulin injections to control
Tip 2 diyabette pankreas insülin üretir, ancak üretilen insülin ya yetersiz kalir ya da düzgün etki göstermez. Bu diyabet tipi en çok 40 yasin üzerindeki ve asiri kilolu kisilerde görülür. Tip 2 diyabet bazen diyet, kilo kontrolü ve egzersiz kombinasyonu ile kontrol altina alinabilir. In type 2 diabetes, the pancreas produces insulin, but the insulin produced is either insufficient or not produced properly. does not show any effect. This type of diabetes is most common in people over the age of 40 and in people who are overweight. Medicine Type 2 diabetes can sometimes be controlled with a combination of diet, weight control and exercise.
Bununla birlikte, oral glikoz düsürücü ilaçlar veya insülin enjeksiyonlarindan olusan bir tedavi uygulanabilir. However, a treatment consisting of oral glucose-lowering medications or insulin injections applicable.
Sitagliptin, tip 2 diabetes mellituslu eriskinlerde diyet ve egzersize ek olarak glisemik kontrolü iyilestirmede endikedir. Dipeptidil peptidaz-4 (DPP-4) inhibitör sinifinin oral bir antihiperglisemik ajanidir. DPP-4 inhibitörleri, inkretin hormonunu yikima ugratan bir enzim olan DPP-4'ün etkisini bloke ederek etki gösterir. Vücutta glukagon benzeri peptit-1 (GLP-1) ve glikoz bagimli insulinotropik peptit (GIP) olarak adlandirilan iki tür inkretin hormonu bulunmaktadir. Bu hormonlar, gida alimina yanit olarak vücut tarafindan dogal olarak üretilir. Sitagliptin improves glycemic control as an adjunct to diet and exercise in adults with type 2 diabetes mellitus. It is indicated for healing. It is an oral drug of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. It is an antihyperglycemic agent. DPP-4 inhibitors, an enzyme that destroys the incretin hormone It works by blocking the effect of DPP-4. Glucagon-like peptide-1 (GLP-1) in the body and two types of incretin hormones called glucose-dependent insulinotropic peptide (GIP). There are. These hormones are produced naturally by the body in response to food intake.
Görevi, vücudun yalnizca ihtiyaci oldugunda daha fazla insülin üretmesine yardimci olmak ve gerekmediginde karaciger tarafindan üretilen glikoz miktarini azaltmaktir. Sitagliptin, DPP-4'e baglanarak onun GLP-1 ve GIP'ye ayrilmasini önleyerek etki gösterir. Böylece vücuttaki bu hormon düzeyleri artar ve böylelikle kan sekerini kontrol etme üzerindeki etkileri de yükselir. pirazin-'I' (8H)-yI]-1- (2,4,5-trifluor0fenil) butan-Z-amin) ve sitagliptinin kimyasal yapisi Formül 1'de gösterilmektedir. Its job is to help the body produce more insulin only when it needs it. It is to reduce the amount of glucose produced by the liver when it is not needed. Sitagliptin to DPP-4 It acts by binding to GLP-1 and GIP and preventing it from being broken down into GIP-1 and GIP. Thus, this in the body hormone levels increase and thus their effect on controlling blood sugar increases. Chemical structure of pyrazine-'I' (8H)-yl]-1- (2,4,5-trifluorophenyl)butane-Z-amine) and sitagliptin Formula It is shown in 1.
Formül 1. Sitagliptin Januvia® denilen Sitagliptin içeren film kapli tabletler, ABD'de Merck tarafindan pazarlanmaktadir. Januvia® tablet, sirasiyla 25, 50 veya 100 mg, serbest baza karsilik gelen Önceki teknikte, Sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu içeren tablet veya kapsül gibi konvansiyonel formlar yer almaktadir. Formula 1. Sitagliptin Film-coated tablets containing Sitagliptin, called Januvia®, are available from Merck in the USA. is marketed. Januvia® tablet, 25, 50 or 100 mg respectively, corresponding to the free base In the prior art, Sitagliptin or a pharmaceutically acceptable salt of sitagliptin There are conventional forms such as tablets or capsules containing
Konvansiyonel tablet dozaj formlari tercih edilen uygulama yolu olmasina karsin yasli, yataga bagimli, koopere olmayan, bulanti yasayan ve su alimi az olan hastalar gibi bazi hasta gruplari ve disfaji bulunan, yutma güçlügü yasayan hastalar, bu dozaj formlarini kullanirken problem yasamaktadir. Ek olarak hastalar, seyahat ederken kolaylikla su bulamayabilir ve bu da konvansiyonel tablet dozaj formlarinin kullanimini kisitlamaktadir. Antidiyabetik ilaçlar kronik olarak reçete edildiginden, böyle bir problem yüksek düzeyde hasta uyumsuzluguna neden olabilir. Although conventional tablet dosage forms are the preferred route of administration, elderly, bedridden Some patients, such as dependent, uncooperative, nauseated and low water intake patients, groups and patients with dysphagia and difficulty swallowing when using these dosage forms. is having a problem. Additionally, patients may not be able to easily find water while traveling, which It also restricts the use of conventional tablet dosage forms. antidiabetic drugs Since it is prescribed chronically, such a problem leads to high levels of patient non-compliance. why could it be.
Bu nedenle agizda dagilan tablet formülasyonlari konvansiyonel tablet dozaj formlarina göre en iyi alternatifi sunmaktadir. Tükürük ile temas ettiginde veya az miktarda su ile hizla dagilan agizda dagilan tablet kompozisyonlari, daha iyi hasta uyumu saglama potansiyeli ile daha yüksek rahatlik ve uygulama kolayligi sunmaktadir. Özellikle, konvansiyonel tabletleri veya kapsülleri yutmada güçlük çeken geriatrik hastalar ve nörodejeneratif hastaliklari olanlar için ekstra avantaj saglamaktadir. Hastanin ihtiyaci oldugunda kullanimi kolay ve hizli olacaktir. For this reason, orally disintegrating tablet formulations are more effective than conventional tablet dosage forms. offers the best alternative. Upon contact with saliva or quickly rinsed with a small amount of water. Orally dispersible tablet compositions have the potential to provide better patient compliance. It offers greater comfort and ease of application. In particular, conventional tablets or geriatric patients and those with neurodegenerative diseases who have difficulty swallowing capsules It provides an extra advantage for Easy and fast to use when the patient needs it It will happen.
Bulusun Ayrintili Açiklamasi Bulusun ana amaci, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu içeren ve suya ihtiyaç duymadan oral yoldan alinabilen, böylece hasta için kullanimi kolay bir tablet sunulmasidir. Mevcut bulusta, agizda dagilan tablet formu kullanilmaktadir. Bu sekilde, hem hasta için kullanimi kolay olan hem de istenen dissolüsyon profiline sahip bir form elde edilmis olmaktadir. Detailed Description of the Invention The main object of the invention is to provide sitagliptin or a pharmaceutically acceptable salt of sitagliptin. It contains a tablet that can be taken orally without the need for water, making it easy for the patient to use. tablet is presented. In the present invention, the orally disintegrating tablet form is used. In this way, A form that is both easy to use for the patient and has the desired dissolution profile is obtained. has been done.
Mevcut bulusun baska bir amaci, hastanin kolay kullanimi için arzu edilen stabiliteyi ve iyi bir tat saglamaktir. Another object of the present invention is to provide the desired stability and good fit for easy use by the patient. is to provide taste.
Bulusun bir uygulamasina göre agizda dagilan tablet formülasyonu, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu ve en az bir farmasötik olarak kabul edilebilir eksipiyan içermektedir. Bulusun formülasyonu, hizli emilen ve istenen dissolüsyon hizini elde etmek için stabiliteden ödün vermek zorunda kalmadan tasarlanmis olup, bu da; sitagliptin kaynagi olarak sitagliptin veya sitagliptinim farmasötik olarak kabul edilebilir bir tuzunun kullanilmasinin ve agizda dagilan tablet formunun kullanilmasinin sasirtici sekilde koordine etkisi ile iliskilendirilmistir. According to an embodiment of the invention, the orally disintegrating tablet formulation is sitagliptin or a pharmaceutically acceptable salt of sitagliptin and at least one pharmaceutically acceptable Contains acceptable excipients. The formulation of the invention provides rapid absorption and desired dissolution. It was designed without having to compromise stability to achieve speed, which means; sitagliptin or sitagliptinum as a pharmaceutically acceptable source of sitagliptin Surprisingly, using its salt and orally dispersing tablet form It is associated with the coordination effect.
Mevcut bulus; sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu içeren ve üç dakika içinde hizla dagilacak olan agizda dagilan bir tablet sunmaktadir. Bu kompozisyonlar kabul edilebilir bir tada sahiptir ve uygulama sonrasi agizda hos bir tat ile birlikte minimum düzeyde kalinti birakirlar. Mevcut bulus ayrica söz konusu agizda dagilan tabletin hazirlanmasina yönelik prosesler sunmaktadir. Ayrica, söz konusu agizda dagilan tabletin uygulanmasi diyabet tedavisi için bir yöntem saglamaktadir. Present invention; containing sitagliptin or a pharmaceutically acceptable salt of sitagliptin and offers a mouth-dispersible tablet that will disperse rapidly within three minutes. This The compositions have an acceptable taste and a pleasant aftertaste after application. Together they leave minimal residue. The present invention also provides for said mouth dispersing It offers processes for the preparation of tablets. Also, the disintegration in the mouth in question Administration of the tablet provides a method for treating diabetes.
Bulusun bir uygulamasina göre, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzu, formülasyonda agirlikça %20.0 ila %50.0 miktarinda bulunmaktadir. According to one embodiment of the invention, sitagliptin or sitagliptin is pharmaceutically acceptable A salt is present in the formulation in an amount of 20.0% to 50.0% by weight.
Bulusun bir uygulamasina göre, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir Bulusun bir uygulamasina göre, sitagliptinin farmasötik olarak kabul edilebilir bir tuzu, sitagliptin fosfat veya sitagliptin hidroklorür veya sitagliptin malattir. Tercihen, sitagliptinin farmasötik olarak kabul edilebilir bir tuzu sitagliptin malattir. According to one embodiment of the invention, sitagliptin or sitagliptin is pharmaceutically acceptable According to one embodiment of the invention, a pharmaceutically acceptable salt of sitagliptin is sitagliptin phosphate or sitagliptin hydrochloride or sitagliptin malate. Preferably, sitagliptin A pharmaceutically acceptable salt of it is sitagliptin malate.
Bununla birlikte, dagilma, stabilite, sikistirilabilirlik ve tat maskeleme gibi çesitli farkli sebepler ve gereklilikler yüzünden tüm etkin maddeler için agizda dagilan formülasyonlarin gelistirilmesi kolay degildir. Dozaj formu oral kavitede tükürük ile temasta kisa sürede dagilmalidir. Dolayisiyla, bu kompozisyonlar gözenekli bir yapiya sahip olmalidir. Agizda dagilan tabletler, daha yüksek gözenek elde etmek için konvansiyonel tabletlere göre daha düsük sikistirma kuvvetleri uygulanarak basilmaktadir. Bununla birlikte, bu gözenekli olma özelligi, neme ve kolay kirilmaya karsi çok hassastir ve stabilite problemlerine yol açabilir. However, various different factors such as dispersion, stability, compressibility and taste masking are required. For reasons and requirements, orodispersible formulations for all active ingredients It was not easy to develop. The dosage form is rapidly dissolved in contact with saliva in the oral cavity. It must be dispersed. Therefore, these compositions must have a porous structure. in mouth Dispersible tablets are larger than conventional tablets to achieve higher porosity. It is pressed by applying low compression forces. However, this porosity It is very sensitive to moisture and easy breakage and may cause stability problems.
Tüm bu gereklilikleri yerine getirmek için, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunun agizda dagilan tablet formülasyonunun uygun dagilim süresi ve yüksek stabilite sergileyecek sekilde uygun gözenekli yapida olmasi için eksipiyan seçimi dikkatli yapilmalidir. To fulfill all these requirements, sitagliptin or sitagliptin pharmaceutically acceptable The orodispersible tablet formulation of a soluble salt has a suitable dispersion time and high Excipient selection should be careful to ensure that it has a suitable porous structure to exhibit stability. should be done.
Mevcut bulusun bir uygulamasina göre, formülasyon; seyrelticiler, dagiticilar, glidantlar, edilebilir en az bir eksipiyan içermektedir. According to an embodiment of the present invention, the formulation; diluents, dispersants, glidants, contains at least one acceptable excipient.
Uygun seyrelticiler; mannitol, mikrokristalin selüloz, sorbitol, sükroz, inorganik tuzlar, kalsiyum tuzlari, polisakkaritler, dekstroz, dikalsiyum fosfat, sodyum klorür, dekstratlar, karbonat, nisasta, sodyum karbonat, sodyum bikarbonat veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable diluents; mannitol, microcrystalline cellulose, sorbitol, sucrose, inorganic salts, calcium salts, polysaccharides, dextrose, dicalcium phosphate, sodium chloride, dextrates, containing baking soda, starch, sodium carbonate, sodium bicarbonate or mixtures thereof is selected from the group.
Mevcut bulusun bir uygulamasina göre seyreltici miktari, formülasyonda agirlikça %450 ila Mevcut bulusun bir uygulamasina göre seyreltici, mannitol veya mikrokristalin selüloz veya bunlarin karisimlaridir. According to one embodiment of the present invention, the amount of diluent is 450 to 450% by weight in the formulation. According to one embodiment of the present invention, the diluent is mannitol or microcrystalline cellulose or are mixtures of these.
Mannitol, hos tadi ve agizda biraktigi his ile birlestiginde neme duyarli formülasyonlar için en uygun seyrelticilerden biridir. Mannitol, neme duyarli formülasyonlarda kullanilan etkisiz, nem çekici olmayan bir seyrelticidir. Mannitol, combined with its pleasant taste and mouthfeel, is best suited for moisture-sensitive formulations. It is one of the suitable diluents. Mannitol is an inert, moisture-absorbing agent used in moisture-sensitive formulations. It is an unattractive diluent.
Uygun dagiticilar; krospovidon, aljinik asit, iyon degistirici reçineler, magnezyum alüminyum silika, sodyum dodesil sülfat, kroskarmeloz sodyum, sodyum karboksimetil nisasta, karboksi metil selüloz kalsiyum, dokusat sodyum, sodyum nisasta glikolat, sodyum glisin karbonat, sodyum Iauril sülfat, düsük sübstitüye HPC (hidroksi propil selüloz), poliakrilin potasyum, poloksamer, ksantan zamki, kalsiyum silikat, iyon degistirici reçineler ve bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable distributors; crospovidone, alginic acid, ion exchange resins, magnesium aluminum silica, sodium dodecyl sulfate, croscarmellose sodium, sodium carboxymethyl starch, carboxy methyl cellulose calcium, docusate sodium, sodium starch glycolate, sodium glycine carbonate, sodium Iauryl sulfate, low substituted HPC (hydroxy propyl cellulose), polyacrylic potassium, poloxamer, xanthan gum, calcium silicate, ion exchange resins and their is selected from the group containing mixtures.
Mevcut bulusun bir uygulamasina göre, dagiticilarin miktari formülasyonda agirlikça %50 ila Mevcut bulusun bir baska uygulamasina göre dagitici, krospovidondur. According to one embodiment of the present invention, the amount of disintegrants in the formulation is 50 to 50% by weight. According to another embodiment of the present invention, the disintegrant is crospovidone.
Mevcut bulusun bir uygulamasina göre, gözenekli ODT yapisi saglamak için bu bulusun formülasyonunda dagitici olarak krospovidon kullanilmaktadir. Ayrica formülasyonda kullanilan krospovidon, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunun dagilma süresini uzatmakta, böylece istenen dissolüsyon profilinin elde edilmesini saglamaktadir. According to an embodiment of the present invention, the present invention is used to provide porous ODT structure. Crospovidone is used as a disintegrant in its formulation. Also in the formulation The crospovidone, sitagliptin or sitagliptin used is pharmaceutically acceptable. It prolongs the dispersion time of the salt, thus achieving the desired dissolution profile. It provides.
Bu bulusta, sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunun agizda dagilan tablet formülasyonu, dagitici (özellikle krospovidon) kullanimi sayesinde 1 dakikadan daha az, tercihen 30 saniyeden daha az bir sürede dagilmaktadir. In this invention, sitagliptin or a pharmaceutically acceptable salt of sitagliptin is administered orally. The dispersible tablet formulation can be used in less than 1 minute thanks to the use of disintegrants (especially crospovidone). It dissipates in less time, preferably in less than 30 seconds.
Uygun glidantlar; talk, koloidal silikon dioksit, koloidal susuz silika, alüminyum silikat veya bunlarin karisimlarini içeren bir gruptan seçilmektedir. Suitable glidants; talc, colloidal silicon dioxide, colloidal anhydrous silica, aluminum silicate or is selected from a group containing mixtures thereof.
Mevcut bulusun bir uygulamasina göre glidant miktari, formülasyonda agirlikça %001 ila Mevcut bulusun bir baska uygulamasina göre glidant, talktir. According to one embodiment of the present invention, the amount of glidant can range from 001 to 100% by weight in the formulation. According to another embodiment of the present invention, the glidant is talc.
Uygun Iubrikanlar; magnezyum stearat, sodyum stearil fumarati kalsiyum stearat, sodyum palmitostearat, hidrojene bitkisel yag, çinko stearat veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable Iubricans; magnesium stearate, sodium stearyl fumarate calcium stearate, sodium from the group containing palmitostearate, hydrogenated vegetable oil, zinc stearate or mixtures thereof is selected.
Mevcut bulusun bir uygulamasina göre Iubrikan miktari, formülasyonda agirlikça %001 ila Mevcut bulusun bir uygulamasina göre Iubrikan, magnezyum stearattir. According to one embodiment of the present invention, the amount of lubricant can range from 001 to 100% by weight in the formulation. According to one embodiment of the present invention, the lubricant is magnesium stearate.
Mevcut bulusun bir uygulamasina göre, dagiticilar Iubrikanlara spesifik bir oranda kullanilmaktadir. Oran. formülasyonun agirliginca 1.0 ila 12.0 araligindadir, tercihen formülasyonun agirliginca 7.0 ile 10.0 araligindadir. Sasirtici bir sekilde, bu oran ile formülasyonun ODT'Iere basilmasi için arzu edilen akiskanligin elde edildigi bulunmustur. According to one embodiment of the present invention, disintegrants are added to the lubricants at a specific rate. is used. Ratio. in the range of 1.0 to 12.0 by weight of the formulation, preferably It is between 7.0 and 10.0 by weight of the formulation. Surprisingly, with this ratio It was found that the desired fluidity was achieved for pressing the formulation into ODTs.
Agizda dagilan tablet, ilaç dille dogrudan temas ettiginde hizla dagilacak sekilde tasarlandigindan, bu kompozisyonlarin kabul edilebilirligi arttirmak için etkin maddenin tadini etkin sekilde maskelemek, formülasyon gelistiricileri için bir zorluk olarak kalmaya devam etmektedir. The orally disintegrating tablet is designed to disperse rapidly when the medicine comes into direct contact with the tongue. Since these compositions are designed to enhance the taste of the active ingredient to increase acceptability, Effectively masking remains a challenge for formulation developers It does.
Bulusun bir uygulamasina göre, kullanilan tatlandiricilar, hasta kompliansinin saglanmasi için etkin madde ile etkilesime girmeyen tatlandiricilar kullanilarak iyilestirilmistir. According to an embodiment of the invention, the sweeteners used are designed to ensure patient compliance. It has been improved by using sweeteners that do not interact with the active ingredient.
Uygun tatlandiricilar; aspartam, sükraloz, sakarin, sodyum siklamat, glikoz, Iaktoz, fruktoz, sorbitol, ksilitol, eritritol veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable sweeteners; aspartame, sucralose, saccharin, sodium cyclamate, glucose, lactose, fructose, sorbitol, xylitol, erythritol, or mixtures thereof.
Mevcut bulusun bir uygulamasina göre tatlandiricilarin miktari, formülasyonda agirlikça Mevcut bulusun bir baska uygulamasina göre tatlandirici, aspartamdir. According to one embodiment of the present invention, the amount of sweeteners by weight in the formulation is According to another embodiment of the present invention, the sweetener is aspartame.
Burada elde edilen agizda dagilan tablet formülasyonu, tükürük ile temas eder etmez bukkal kavitede hizla dagilir ve hos bir tada sahiptir (agizda hos kremamsi bir tat birakir) ve midede hizli, esasen eksiksiz bir doz salinimi saglar. The orally disintegrating tablet formulation obtained here is absorbed buccally as soon as it comes into contact with saliva. It disperses quickly in the cavity and has a pleasant taste (leaves a pleasant creamy taste in the mouth) Provides rapid, essentially complete dose release.
Mevcut bulusun bir uygulamasina göre agizda dagilan tablet formülasyonu, sunlari içermektedir; - Agirlikça %20.0-50.0 sitagliptin malat - Agirlikça %25.0-40.0 mannitol - Agirlikça %5.0-20.0 krospovidon - Agirlikça %20.0-30.0 mikrokristalin selüloz - Agirlikça %0.01-3.0 magnezyum stearat - Agirlikça %0.0'l-3.0 talk - Agirlikça %0.05-4.0 aspartam. The orally disintegrating tablet formulation according to an embodiment of the present invention includes: It includes; - 20.0-50.0% sitagliptin malate by weight - 25.0-40.0% mannitol by weight - 5.0-20.0% crospovidone by weight - 20.0-30.0% microcrystalline cellulose by weight - 0.01-3.0% magnesium stearate by weight - 0.01-3.0% talc by weight - 0.05-4.0% aspartame by weight.
Mevcut bulusun bir uygulamasina göre mevcut bulusa ait agizda dagilan tablet formülasyonu, direkt baski, kuru granülasyon veya islak granülasyon gibi konvansiyonel tekniklerle hazirlanabilir. Orally disintegrating tablet of the present invention according to an embodiment of the present invention formulation, direct printing, dry granulation or wet granulation can be prepared using techniques.
Mevcut bulusun bir uygulamasina göre agizda dagilan tablet formülasyonu, direkt baski ile hazi rlanmaktadir. Örnek 1: Sitagliptin veya sitagliptinin farmasötik olarak kabul edilebilir bir tuzunu içeren ODT formülasyonu Içerik maddeleri Agirlikça (%) Sitagliptin veya sitagliptinin farmasötik olarak 28.0 - 37.0 kabul edilebilir bir tuzu Seyrelticiler 45.0 - 70.0 Dagiticilar 5.0 - 20.0 Glidantlar 0.01 - 3.0 Lubrikanlar 0.01 - 3.0 Tatlandiricilar 0.05 - 4.0 TOPLAM 100 Örnek 2: Sitagliptin malat içeren ODT formülasyonu Içerik maddeleri Agirlikça (%) Sitagliptin malat 33.2 Mannitol 32.0 Krospovidon 7.5 Mikrokristalin selüloz 25.0 Magnezyum stearat 0.75 Aspartam 1.3 TOPLAM 100 Örnek 2 için proses; - Karisimin sitagliptin malat, mannitol, krospovidon, mikrokristalin selüloz, talk, aspartam ilave edildikten sonra homojen bir karisim elde edilene kadar karistirilmasi, - Magnezyum stearat eklenmesi ve ardindan karistirilmasi, - Karisimin agizda dagilan tablet olusturmak üzere basilmasi. According to an embodiment of the present invention, the orally disintegrating tablet formulation is produced by direct pressure. is being prepared. Example 1: Sitagliptin or a pharmaceutically acceptable salt of sitagliptin ODT formulation containing ingredients By weight (%) Sitagliptin or sitagliptin pharmaceutically 28.0 - 37.0 an acceptable salt Diluents 45.0 - 70.0 Distributors 5.0 - 20.0 Glidants 0.01 - 3.0 Lubricants 0.01 - 3.0 Sweeteners 0.05 - 4.0 TOTAL 100 Example 2: ODT formulation containing sitagliptin malate ingredients By weight (%) Sitagliptin malate 33.2 Mannitol 32.0 Crospovidone 7.5 Microcrystalline cellulose 25.0 Magnesium stearate 0.75 Aspartame 1.3 TOTAL 100 Process for example 2; - The mixture contains sitagliptin malate, mannitol, crospovidone, microcrystalline cellulose, talc, After adding aspartame, mixing until a homogeneous mixture is obtained, - Adding magnesium stearate and then mixing, - Compressing the mixture to form a tablet that dissolves in the mouth.
Claims (1)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2020/09724A TR202009724A2 (en) | 2020-06-23 | 2020-06-23 | FORMULATION OF CYTAGLIPTIN IN ORAL DISTRIBUTION TABLET |
| EP21830086.1A EP4167969A4 (en) | 2020-06-23 | 2021-05-07 | An orally disintegrating tablet formulation comprising sitagliptin |
| PCT/TR2021/050440 WO2021262114A1 (en) | 2020-06-23 | 2021-05-07 | An orally disintegrating tablet formulation comprising sitagliptin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| TR2020/09724A TR202009724A2 (en) | 2020-06-23 | 2020-06-23 | FORMULATION OF CYTAGLIPTIN IN ORAL DISTRIBUTION TABLET |
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| WO2010012781A2 (en) * | 2008-07-29 | 2010-02-04 | Medichem, S.A. | New crystalline salt forms of a 5,6,7,8-tetrahydro-1,2,4- triazolo[4,3-a]pyrazine derivative |
| US8183373B2 (en) * | 2010-03-31 | 2012-05-22 | Teva Pharmaceutical Industries Ltd. | Solid state forms of sitagliptin salts |
| TR201721700A2 (en) * | 2017-12-26 | 2019-07-22 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | DISTRIBUTED FORMULATIONS OF SAXAGLIPT IN THE MOUTH |
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| WO2021262114A1 (en) | 2021-12-30 |
| EP4167969A4 (en) | 2024-04-17 |
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