JP2010534234A - オキシカルバゼピンを含む制御放出固体製剤を調製する方法、およびその方法により得られる製剤 - Google Patents
オキシカルバゼピンを含む制御放出固体製剤を調製する方法、およびその方法により得られる製剤 Download PDFInfo
- Publication number
- JP2010534234A JP2010534234A JP2010517499A JP2010517499A JP2010534234A JP 2010534234 A JP2010534234 A JP 2010534234A JP 2010517499 A JP2010517499 A JP 2010517499A JP 2010517499 A JP2010517499 A JP 2010517499A JP 2010534234 A JP2010534234 A JP 2010534234A
- Authority
- JP
- Japan
- Prior art keywords
- water
- oxcarbazepine
- excipient
- controlled release
- active ingredient
- 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.)
- Granted
Links
- 238000000034 method Methods 0.000 title claims abstract description 31
- 229960001816 oxcarbazepine Drugs 0.000 title claims abstract description 23
- CTRLABGOLIVAIY-UHFFFAOYSA-N oxcarbazepine Chemical compound C1C(=O)C2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 CTRLABGOLIVAIY-UHFFFAOYSA-N 0.000 title claims abstract description 23
- 239000007787 solid Substances 0.000 title claims abstract description 11
- 238000013270 controlled release Methods 0.000 title claims abstract description 10
- 239000000203 mixture Substances 0.000 title claims description 29
- 238000009472 formulation Methods 0.000 title description 9
- 239000008203 oral pharmaceutical composition Substances 0.000 claims abstract description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 23
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical group CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 15
- 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 10
- 229930195725 Mannitol Natural products 0.000 claims description 10
- 239000002552 dosage form Substances 0.000 claims description 10
- 239000000594 mannitol Substances 0.000 claims description 10
- 235000010355 mannitol Nutrition 0.000 claims description 10
- 239000002244 precipitate Substances 0.000 claims description 9
- 150000003626 triacylglycerols Chemical class 0.000 claims description 8
- 238000009826 distribution Methods 0.000 claims description 7
- 239000008187 granular material Substances 0.000 claims description 7
- 239000002904 solvent Substances 0.000 claims description 7
- 239000003960 organic solvent Substances 0.000 claims description 6
- 239000002245 particle Substances 0.000 claims description 6
- 229920001817 Agar Polymers 0.000 claims description 5
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 5
- 239000008272 agar Substances 0.000 claims description 5
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 5
- 238000001556 precipitation Methods 0.000 claims description 5
- 230000008569 process Effects 0.000 claims description 5
- 239000000811 xylitol Substances 0.000 claims description 5
- 229960002675 xylitol Drugs 0.000 claims description 5
- 235000010447 xylitol Nutrition 0.000 claims description 5
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 5
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 4
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 4
- 239000001856 Ethyl cellulose Substances 0.000 claims description 4
- 229920002774 Maltodextrin Polymers 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 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 4
- 239000007900 aqueous suspension Substances 0.000 claims description 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 4
- 229920001249 ethyl cellulose Polymers 0.000 claims description 4
- 239000000835 fiber Substances 0.000 claims description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 4
- 229920000609 methyl cellulose Polymers 0.000 claims description 4
- 235000010981 methylcellulose Nutrition 0.000 claims description 4
- 239000001923 methylcellulose Substances 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 108010010803 Gelatin Proteins 0.000 claims description 3
- 239000005913 Maltodextrin Substances 0.000 claims description 3
- 108010011756 Milk Proteins Proteins 0.000 claims description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 3
- 108010073771 Soybean Proteins Proteins 0.000 claims description 3
- 239000001506 calcium phosphate Substances 0.000 claims description 3
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 3
- 229960001714 calcium phosphate Drugs 0.000 claims description 3
- 235000011010 calcium phosphates Nutrition 0.000 claims description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 3
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 3
- 238000007906 compression Methods 0.000 claims description 3
- 230000006835 compression Effects 0.000 claims description 3
- 239000008273 gelatin Substances 0.000 claims description 3
- 229920000159 gelatin Polymers 0.000 claims description 3
- 235000019322 gelatine Nutrition 0.000 claims description 3
- 235000011852 gelatine desserts Nutrition 0.000 claims description 3
- GVALZJMUIHGIMD-UHFFFAOYSA-H magnesium phosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 claims description 3
- 239000004137 magnesium phosphate Substances 0.000 claims description 3
- 229910000157 magnesium phosphate Inorganic materials 0.000 claims description 3
- 229960002261 magnesium phosphate Drugs 0.000 claims description 3
- 235000010994 magnesium phosphates Nutrition 0.000 claims description 3
- 229940035034 maltodextrin Drugs 0.000 claims description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 3
- 229940001941 soy protein Drugs 0.000 claims description 3
- 239000000454 talc Substances 0.000 claims description 3
- 229910052623 talc Inorganic materials 0.000 claims description 3
- 229940033134 talc Drugs 0.000 claims description 3
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 3
- 244000099147 Ananas comosus Species 0.000 claims description 2
- 235000007119 Ananas comosus Nutrition 0.000 claims description 2
- 102000014171 Milk Proteins Human genes 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- 235000021239 milk protein Nutrition 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims 1
- 229940050549 fiber Drugs 0.000 claims 1
- 229960001855 mannitol Drugs 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 description 27
- 229940079593 drug Drugs 0.000 description 11
- 239000003814 drug Substances 0.000 description 11
- 235000014113 dietary fatty acids Nutrition 0.000 description 10
- 239000000194 fatty acid Substances 0.000 description 10
- 229930195729 fatty acid Natural products 0.000 description 10
- 150000004665 fatty acids Chemical class 0.000 description 10
- -1 alkyl ether sulfates Chemical class 0.000 description 8
- 210000002784 stomach Anatomy 0.000 description 8
- 239000004615 ingredient Substances 0.000 description 7
- 230000000144 pharmacologic effect Effects 0.000 description 7
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 6
- 159000000003 magnesium salts Chemical class 0.000 description 6
- 239000011591 potassium Substances 0.000 description 6
- 229910052700 potassium Inorganic materials 0.000 description 6
- 239000000047 product Substances 0.000 description 6
- 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 description 5
- 239000002671 adjuvant Substances 0.000 description 5
- 150000001298 alcohols Chemical class 0.000 description 5
- 125000004432 carbon atom Chemical group C* 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 238000002156 mixing Methods 0.000 description 5
- 229920001983 poloxamer Polymers 0.000 description 5
- 239000011734 sodium Substances 0.000 description 5
- 229910052708 sodium Inorganic materials 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 235000010419 agar Nutrition 0.000 description 4
- 230000003111 delayed effect Effects 0.000 description 4
- 150000002148 esters Chemical class 0.000 description 4
- 230000036470 plasma concentration Effects 0.000 description 4
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 4
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 4
- 235000013311 vegetables Nutrition 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 229920001400 block copolymer Polymers 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 238000000576 coating method Methods 0.000 description 3
- 239000013078 crystal Substances 0.000 description 3
- HQQADJVZYDDRJT-UHFFFAOYSA-N ethene;prop-1-ene Chemical group C=C.CC=C HQQADJVZYDDRJT-UHFFFAOYSA-N 0.000 description 3
- 239000002736 nonionic surfactant Substances 0.000 description 3
- 229940057838 polyethylene glycol 4000 Drugs 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 238000009827 uniform distribution Methods 0.000 description 3
- 239000001993 wax Chemical class 0.000 description 3
- LDMOEFOXLIZJOW-UHFFFAOYSA-N 1-dodecanesulfonic acid Chemical compound CCCCCCCCCCCCS(O)(=O)=O LDMOEFOXLIZJOW-UHFFFAOYSA-N 0.000 description 2
- QTDIEDOANJISNP-UHFFFAOYSA-N 2-dodecoxyethyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOCCOS(O)(=O)=O QTDIEDOANJISNP-UHFFFAOYSA-N 0.000 description 2
- HKQRNFNHJGCLST-UHFFFAOYSA-N 2-hexadecoxyethyl hydrogen sulfate Chemical class CCCCCCCCCCCCCCCCOCCOS(O)(=O)=O HKQRNFNHJGCLST-UHFFFAOYSA-N 0.000 description 2
- MCDQYEUDJIBGFS-UHFFFAOYSA-N 2-octadecoxyethyl hydrogen sulfate Chemical class CCCCCCCCCCCCCCCCCCOCCOS(O)(=O)=O MCDQYEUDJIBGFS-UHFFFAOYSA-N 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- 241000196324 Embryophyta Species 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- 229920002907 Guar gum Polymers 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- 229920001213 Polysorbate 20 Polymers 0.000 description 2
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 2
- HVWGGPRWKSHASF-UHFFFAOYSA-N Sulfuric acid, monooctadecyl ester Chemical compound CCCCCCCCCCCCCCCCCCOS(O)(=O)=O HVWGGPRWKSHASF-UHFFFAOYSA-N 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- 229940023476 agar Drugs 0.000 description 2
- 239000003945 anionic surfactant Substances 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 238000005119 centrifugation Methods 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000007907 direct compression Methods 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 description 2
- 239000003995 emulsifying agent Substances 0.000 description 2
- 150000004676 glycans Chemical class 0.000 description 2
- 239000000665 guar gum Substances 0.000 description 2
- 229960002154 guar gum Drugs 0.000 description 2
- 235000010417 guar gum Nutrition 0.000 description 2
- SSILHZFTFWOUJR-UHFFFAOYSA-M hexadecane-1-sulfonate Chemical compound CCCCCCCCCCCCCCCCS([O-])(=O)=O SSILHZFTFWOUJR-UHFFFAOYSA-M 0.000 description 2
- LPTIRUACFKQDHZ-UHFFFAOYSA-N hexadecyl sulfate;hydron Chemical compound CCCCCCCCCCCCCCCCOS(O)(=O)=O LPTIRUACFKQDHZ-UHFFFAOYSA-N 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 150000002484 inorganic compounds Chemical class 0.000 description 2
- 229910010272 inorganic material Inorganic materials 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 235000013336 milk Nutrition 0.000 description 2
- 239000008267 milk Substances 0.000 description 2
- 210000004080 milk Anatomy 0.000 description 2
- CACRRXGTWZXOAU-UHFFFAOYSA-N octadecane-1-sulfonic acid Chemical compound CCCCCCCCCCCCCCCCCCS(O)(=O)=O CACRRXGTWZXOAU-UHFFFAOYSA-N 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 235000005985 organic acids Nutrition 0.000 description 2
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 2
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 2
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 description 2
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 2
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 2
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 2
- 235000010988 polyoxyethylene sorbitan tristearate Nutrition 0.000 description 2
- 239000001816 polyoxyethylene sorbitan tristearate Substances 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 235000018102 proteins Nutrition 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- URLJMZWTXZTZRR-UHFFFAOYSA-N sodium myristyl sulfate Chemical compound CCCCCCCCCCCCCCOS(O)(=O)=O URLJMZWTXZTZRR-UHFFFAOYSA-N 0.000 description 2
- 229950005425 sodium myristyl sulfate Drugs 0.000 description 2
- 239000007909 solid dosage form Substances 0.000 description 2
- 229960000391 sorbitan trioleate Drugs 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- MYOWBHNETUSQPA-UHFFFAOYSA-N tetradecane-1-sulfonic acid Chemical compound CCCCCCCCCCCCCCS(O)(=O)=O MYOWBHNETUSQPA-UHFFFAOYSA-N 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- SWPLMYYBIPGCRH-UHFFFAOYSA-N 2-tetradecoxyethyl hydrogen sulfate Chemical class CCCCCCCCCCCCCCOCCOS(O)(=O)=O SWPLMYYBIPGCRH-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 229910000497 Amalgam Inorganic materials 0.000 description 1
- 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 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 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 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- ZNOZWUKQPJXOIG-XSBHQQIPSA-L [(2r,3s,4r,5r,6s)-6-[[(1r,3s,4r,5r,8s)-3,4-dihydroxy-2,6-dioxabicyclo[3.2.1]octan-8-yl]oxy]-4-[[(1r,3r,4r,5r,8s)-8-[(2s,3r,4r,5r,6r)-3,4-dihydroxy-6-(hydroxymethyl)-5-sulfonatooxyoxan-2-yl]oxy-4-hydroxy-2,6-dioxabicyclo[3.2.1]octan-3-yl]oxy]-5-hydroxy-2-( Chemical compound O[C@@H]1[C@@H](O)[C@@H](OS([O-])(=O)=O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H]2OC[C@H]1O[C@H](O[C@H]1[C@H]([C@@H](CO)O[C@@H](O[C@@H]3[C@@H]4OC[C@H]3O[C@H](O)[C@@H]4O)[C@@H]1O)OS([O-])(=O)=O)[C@@H]2O ZNOZWUKQPJXOIG-XSBHQQIPSA-L 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 229960003965 antiepileptics Drugs 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 238000006065 biodegradation reaction Methods 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 238000000975 co-precipitation Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 235000013681 dietary sucrose Nutrition 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 208000014617 hemorrhoid Diseases 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000005342 ion exchange Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- 229960002160 maltose Drugs 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 150000002482 oligosaccharides Chemical class 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 229920000151 polyglycol Polymers 0.000 description 1
- 239000010695 polyglycol Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- PANBYUAFMMOFOV-UHFFFAOYSA-N sodium;sulfuric acid Chemical compound [Na].OS(O)(=O)=O PANBYUAFMMOFOV-UHFFFAOYSA-N 0.000 description 1
- 208000018556 stomach disease Diseases 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000009492 tablet coating Methods 0.000 description 1
- 239000002700 tablet coating Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Classifications
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/009—Sachets, pouches characterised by the material or function of the envelope
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Abstract
Description
投与頻度が一日一回を超え、患者が投与に対応しない危険性が高くなり、よって、治療の効能に悪影響が及ぶ。
薬理効果を得るのに必要な有効血中濃度を直ちに得るための、薬物の迅速放出;
有効成分の血中濃度の変動の充分な縮小;
単回投与で終日保護するのに充分長い期間有効であって、それにより、投与頻度を低下させ、患者の完全な順守を容易にする、血中濃度。
錠剤の場合の硬度、寸法、形状等のような、固体剤形の技術的特徴;
有効成分の粒径プロフィール、すなわち、有効成分の結晶の粒径分布範囲のみならず、対応する量;
結晶形;
賦形剤としての組成、および、種々の百分率での溶解促進剤または遅延剤;
顆粒または錠剤の被覆。
前述の目的を達成するために、制御放出製剤に関する多くの特許が試みられてきた。
a)オキシカルバゼピンと、モノ−、ジ−およびトリグリセリドの混合物とを、水混和性有機溶媒:エタノール、メタノール、ジオキサン、ジメチルホルムアミドおよびジメチルスルホキシドに溶解させる工程、
b)水不溶性賦形剤の水性懸濁液を、a)で得られた溶液に添加する工程、
c)任意の水溶性賦形剤を、b)で得られた湿潤沈殿物に添加し、得られる混合物を造粒する工程、および
d)c)で得られた顆粒を、医薬投与剤形に圧縮または分布させる工程、
を含んでなる、オキシカルバゼピンの制御放出固体経口医薬製剤の調製方法に関する。
本発明の目的は、適切なマトリクス中における薬物の分散の最大均一性を保証すると共に、結果として、一定の生物学的効率および治療効能を保証する、オキシカルバゼピンの固体経口制御(促進または遅延)放出剤形を製造することである。
多糖類:微結晶性セルロースおよびそれらの誘導体、例えば、メチルセルロース、ヒドロキシプロピルメチルセルロース、エチルセルロースおよびパイナップル繊維。
単、二およびオリゴ糖類:マンニトール、キシリトール、ポリエチレングリコール、カルボキシメチルセルロースナトリウム、種々の分子量のマルトデキストリン、グアーガム、寒天およびそれらの混合物。
乳化剤、すなわち、有効成分の水中への分散および湿潤性のためのアジュバント;
溶解が困難なオキシカルバゼピンの水和形の形成の阻害剤;
錠剤または顆粒結合/分解特性を有する圧縮アジュバント;
有効成分の放出を遅延させる特性を有するバインダー。
アニオン性界面活性剤:ナトリウム、カリウムまたはマグネシウム塩、硫酸n−ドデシル、硫酸n−テトラデシル、硫酸n−ヘキサデシル、硫酸n−オクタデシル;アルキルエーテル硫酸塩、例えば、硫酸n−ドデシルオキシエチル、硫酸n−テトラデシルオキシエチル、硫酸n−ヘキサデシルオキシエチルおよび硫酸n−オクタデシルオキシエチルのナトリウム、カリウムまたはマグネシウム塩。
オキシカルバゼピンが、ジメチルホルムアミドまたは、水と混和性の溶媒に溶解される;
モノ−、ジ−およびトリグリセリドの混合物のような、前記溶媒に可溶性であるが水には不溶性である化合物を、オキシカルバゼピンと一緒に溶解する;
有機溶媒と水の両方に不溶性の化合物は、水中に懸濁され、オキシカルバゼピンと共沈して、コアセルベートを得る;
水溶性成分を湿潤沈殿物に添加しそれと充分に混合して、それにより、共沈物中に存在する水に溶解すると共に湿潤顆粒を与える;ここで、全ての成分は最大の均一性で分布している。
予めジメチルホルムアミドに溶解された、炭素原子数18の鎖を有する植物脂肪酸のモノ−、ジ−およびトリグリセリドの混合物120gを含むジメチルホルムアミド12リッター中に、窒素雰囲気下に60℃で、オキシカルバゼピン1200gを溶解する。
マンニトール120gをキシリトール120gに置き換えて、実施例1に記載の手順を行う。
マンニトール120gのうちの30gをポリエチレングリコール4000の30gに置き換えて、実施例1に記載の手順を行う。
マンニトール120gをキシリトール105gおよびカルボキシメチルセルロースナトリウム塩15gに置き換えて、実施例1に記載の手順を行う。
マンニトール120gをマルトデキストリン(分子量25000)120gに置き換えて、実施例1に記載の手順を行う。
モノ−、ジ−およびトリグリセリドの混合物120gが、炭素原子数6の鎖を有する植物脂肪酸からなることを除いて、実施例1に記載の手順を行う。
モノ−、ジ−およびトリグリセリドの混合物120gが、炭素原子数12の鎖を有する植物脂肪酸からなることを除いて、実施例1に記載の手順を行う。
マンニトール120gをポリエチレングリコール4000の100gおよびポリオキシエチレンソルビタンモノオレエート60の20gに置き換えて、実施例1に記載の手順を行う。
マンニトール120gをポリエチレングリコール4000の100gおよびポリオキシエチレンソルビタンモノオレエート80の20gに置き換えて、実施例1に記載の手順を行う。
マンニトール120gを寒天120gに置き換えて、実施例1に記載の手順を行う。
Claims (9)
- a)オキシカルバゼピンと、モノ−、ジ−およびトリグリセリドの混合物とを、水と混和性の有機溶媒に溶解させる工程、
b)水不溶性賦形剤の水性懸濁液を、a)で得られた溶液に添加する工程、
c)任意の水溶性賦形剤を、b)で得られた湿潤沈殿物に添加し、得られる混合物を造粒する工程、および
d)c)で得られた顆粒を、医薬投与剤形に圧縮または分布させる工程、
を含んでなる、オキシカルバゼピンの制御放出固体経口医薬製剤の調製方法。 - 工程b)が、0〜8℃の温度で行われる請求項1に記載の方法。
- 得られた微結晶性共沈物が平均粒径分布が約50μmである請求項2に記載の方法。
- 水と混和性の有機溶媒がジメチルホルムアミドである請求項1〜3のいずれかに記載の方法。
- 水不溶性賦形剤が、微結晶性セルロースおよびそれらの誘導体、メチルセルロース、ヒドロキシプロピルメチルセルロース、エチルセルロース、パイナップル繊維、タルク、コロイド状二酸化ケイ素、リン酸カルシウム、リン酸マグネシウム、乳タンパク、大豆タンパクおよびゼラチンから選択される請求項1〜4のいずれかに記載の方法。
- 工程c)で添加すべき水溶性賦形剤がマンニトール、キシリトール、マルトデキストリン、ナトリウムカルボキシメチルセルロース、ポリエチレングリコール、寒天およびそれらの混合物から選択される請求項1〜5のいずれかに記載の方法。
- 請求項1〜6のいずれかに記載の方法により得られる医薬組成物。
- カプセル、錠剤、およびサシェ中顆粒の形態である、請求項7に記載の組成物。
- 水不溶性賦形剤の水性懸濁液を用いて、水混和性溶媒からのオキシカルバゼピンの沈殿により得られるオキシカルバゼピンコアセルベート。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT001502A ITMI20071502A1 (it) | 2007-07-25 | 2007-07-25 | Procedimento per la preparazione di formulazioni solide a rilascio controllato contenenti oxcarbazepina e formulazioni ottenibili con tale procedimento |
ITMI2007A001502 | 2007-07-25 | ||
PCT/IB2008/001904 WO2009013594A2 (en) | 2007-07-25 | 2008-07-23 | Process for the preparation of controlled-release solid formulations containing oxcarbazepine, and formulations obtainable by said process |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2010534234A true JP2010534234A (ja) | 2010-11-04 |
JP5340285B2 JP5340285B2 (ja) | 2013-11-13 |
Family
ID=40134070
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010517499A Expired - Fee Related JP5340285B2 (ja) | 2007-07-25 | 2008-07-23 | オキシカルバゼピンを含む制御放出固体製剤を調製する方法、およびその方法により得られる製剤 |
Country Status (9)
Country | Link |
---|---|
US (2) | US20100226944A1 (ja) |
EP (1) | EP2170285B1 (ja) |
JP (1) | JP5340285B2 (ja) |
KR (1) | KR101519612B1 (ja) |
CN (1) | CN101754750A (ja) |
ES (1) | ES2515167T3 (ja) |
IL (1) | IL203433A (ja) |
IT (1) | ITMI20071502A1 (ja) |
WO (1) | WO2009013594A2 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TR201008460A1 (tr) * | 2010-10-15 | 2012-05-21 | Sanovel İlaç San.Ve Ti̇c.A.Ş. | Eslikarbazepinin saşe formülasyonları. |
WO2014078435A1 (en) | 2012-11-14 | 2014-05-22 | W. R. Grace & Co.-Conn. | Compositions containing a biologically active material and a non-ordered inorganic oxide |
KR102172273B1 (ko) * | 2019-10-31 | 2020-10-30 | 주식회사 삼양사 | 점성 저감화 환 제조용 조성물 |
CN111481521B (zh) * | 2020-04-14 | 2021-04-02 | 上海奥科达生物医药科技有限公司 | 一种奥卡西平缓释制剂、制备方法及其应用 |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2003043602A1 (en) * | 2001-11-20 | 2003-05-30 | Korea Dds Pharmaceutical Co., Ltd. | Solid dispersions containing substituted cyclodextrin and insoluble drug and their preparations |
JP2004529966A (ja) * | 2001-05-18 | 2004-09-30 | ランバクシー ラボラトリーズ リミテッド | オキシカルバゼピン製剤 |
WO2007029093A2 (en) * | 2005-09-05 | 2007-03-15 | Ranbaxy Laboratories Limited | Pharmaceutical dosage forms of oxcarbazepine |
WO2007141806A1 (en) * | 2006-06-02 | 2007-12-13 | Jubilant Organosys Ltd | Pharmaceutical formulations comprising oxcarbazepine and methods thereof |
WO2008092046A2 (en) * | 2007-01-26 | 2008-07-31 | Isp Investments Inc. | Amorphous oxcarbazepine and the production thereof |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA953078B (en) * | 1994-04-28 | 1996-01-05 | Alza Corp | Effective therapy for epilepsies |
ATE286725T1 (de) * | 1998-10-01 | 2005-01-15 | Novartis Pharma Gmbh | Neue oral anzuwendende arzneizubereitungen für rivastigmine mit kontrollierter wirkstoffabgabe |
WO2002064557A2 (en) * | 2001-02-12 | 2002-08-22 | Teva Pharmaceutical Industries Ltd. | New crystal forms of oxcarbazepine and processes for their preparation |
AUPR573001A0 (en) * | 2001-06-15 | 2001-07-12 | Glaxo Wellcome Australia Ltd | Lymphatic drug delivery system |
US20040185095A1 (en) * | 2002-05-31 | 2004-09-23 | Hanshermann Franke | Pharmaceutical composition containing oxcarbazepine and having a controlled active substance release |
JP5243247B2 (ja) * | 2005-07-28 | 2013-07-24 | アイエスピー インヴェストメンツ インコーポレイテッド | スプレー乾燥された粉体及び粒状化された材料の特性の改良方法、並びにそれによって製造した製品 |
-
2007
- 2007-07-25 IT IT001502A patent/ITMI20071502A1/it unknown
-
2008
- 2008-07-23 JP JP2010517499A patent/JP5340285B2/ja not_active Expired - Fee Related
- 2008-07-23 CN CN200880100020A patent/CN101754750A/zh active Pending
- 2008-07-23 US US12/670,273 patent/US20100226944A1/en not_active Abandoned
- 2008-07-23 WO PCT/IB2008/001904 patent/WO2009013594A2/en active Application Filing
- 2008-07-23 EP EP08788908.5A patent/EP2170285B1/en not_active Not-in-force
- 2008-07-23 KR KR1020107001632A patent/KR101519612B1/ko not_active IP Right Cessation
- 2008-07-23 ES ES08788908.5T patent/ES2515167T3/es active Active
-
2010
- 2010-01-21 IL IL203433A patent/IL203433A/en not_active IP Right Cessation
-
2012
- 2012-12-03 US US13/692,576 patent/US20130095149A1/en not_active Abandoned
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2004529966A (ja) * | 2001-05-18 | 2004-09-30 | ランバクシー ラボラトリーズ リミテッド | オキシカルバゼピン製剤 |
WO2003043602A1 (en) * | 2001-11-20 | 2003-05-30 | Korea Dds Pharmaceutical Co., Ltd. | Solid dispersions containing substituted cyclodextrin and insoluble drug and their preparations |
WO2007029093A2 (en) * | 2005-09-05 | 2007-03-15 | Ranbaxy Laboratories Limited | Pharmaceutical dosage forms of oxcarbazepine |
WO2007141806A1 (en) * | 2006-06-02 | 2007-12-13 | Jubilant Organosys Ltd | Pharmaceutical formulations comprising oxcarbazepine and methods thereof |
WO2008092046A2 (en) * | 2007-01-26 | 2008-07-31 | Isp Investments Inc. | Amorphous oxcarbazepine and the production thereof |
Also Published As
Publication number | Publication date |
---|---|
US20100226944A1 (en) | 2010-09-09 |
CN101754750A (zh) | 2010-06-23 |
ITMI20071502A1 (it) | 2009-01-26 |
EP2170285A2 (en) | 2010-04-07 |
KR20100041780A (ko) | 2010-04-22 |
KR101519612B1 (ko) | 2015-05-12 |
JP5340285B2 (ja) | 2013-11-13 |
ES2515167T3 (es) | 2014-10-29 |
EP2170285B1 (en) | 2014-10-01 |
WO2009013594A2 (en) | 2009-01-29 |
US20130095149A1 (en) | 2013-04-18 |
WO2009013594A3 (en) | 2009-08-13 |
IL203433A (en) | 2016-03-31 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP6934932B2 (ja) | アンドロゲン受容体アンタゴニストの固体医薬組成物 | |
RU2590979C2 (ru) | Составы l-ментола, состоящие из множества частиц, и связанные с ними способы | |
EP2645996A2 (de) | Verfahren zur herstellung einer ppi-haltigen pharmazeutischen zubereitung | |
WO2013034040A1 (zh) | 塞来昔布固体分散体及其制备方法 | |
FR2585570A1 (fr) | Procede de preparation d'une forme granulaire a liberation retardee d'un principe actif et forme granulaire obtenue | |
WO2015121472A1 (en) | Pharmaceutical composition comprising apixaban | |
JP5340285B2 (ja) | オキシカルバゼピンを含む制御放出固体製剤を調製する方法、およびその方法により得られる製剤 | |
EP3003277B1 (en) | Process for the preparation of a pharmaceutical composition comprising rivaroxaban | |
RU2351352C2 (ru) | Твердая нанокомпозиция для доставки биологически активных веществ | |
US20120027822A1 (en) | Process for Producing Rapidly Disintegrating Spheroids (Pellets), Granules and/or Mixtures Thereof | |
US8062664B2 (en) | Process for preparing formulations of lipid-regulating drugs | |
CN115919793A (zh) | 一种奥利司他胶囊制剂及其制备方法 | |
US20230310401A1 (en) | Pharmaceutical Composition Containing Dabigatran Etexilate And Preparation Method Thereof | |
EP1895990A2 (en) | Formulations containing pantoprazole free acid and its salts | |
Walavalkar et al. | Formulation and Evaluation of Capsule Loaded With Gastro-Resistant Microspheres of Pantoprazole and Gastroretentive Sustained Release Floating Tablet of Itopride Hydrochloride | |
WO2001051031A2 (en) | Enteric coated pharmaceutical formulation | |
US20060177512A1 (en) | Process for preparing formulations of lipid-regulating drugs | |
WO2010092260A2 (fr) | Compositions pharmaceutiques du 6-oxo-6.7.8,9.10.11-hexahydrocyclohepta mchromen-3-yl sulfamate | |
Swathi et al. | PHARMACEUTICAL SCIENCES | |
JPH08175997A (ja) | マレイン酸イルソグラジン経口投与用製剤およびその製造法 | |
EP3383368A1 (en) | Product comprising hydrolized collagen and at least one amorphous micronized drug, process for the preparation thereof and related uses in medical field | |
SK15612000A3 (sk) | Perorálne tablety s riadeným uvoľňovaním farmaceuticky akceptovateľných solí metoprololu a spôsob ich prípravy | |
MXPA06000111A (es) | Proceso para preparar formulaciones de farmacos que regulan lipidos. | |
KR20060011341A (ko) | 펠로디핀 서방성 제제의 제조방법 | |
SK278560B6 (en) | The healing preparation containing morphine sulphate and preparation method thereof |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20110530 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20130416 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20130702 |
|
TRDD | Decision of grant or rejection written | ||
A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20130730 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20130806 |
|
R150 | Certificate of patent or registration of utility model |
Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
LAPS | Cancellation because of no payment of annual fees |