JP2005527584A5 - - Google Patents
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- JP2005527584A5 JP2005527584A5 JP2003583377A JP2003583377A JP2005527584A5 JP 2005527584 A5 JP2005527584 A5 JP 2005527584A5 JP 2003583377 A JP2003583377 A JP 2003583377A JP 2003583377 A JP2003583377 A JP 2003583377A JP 2005527584 A5 JP2005527584 A5 JP 2005527584A5
- Authority
- JP
- Japan
- Prior art keywords
- less
- composition
- megestrol
- chloride
- mpa
- 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
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- 239000000203 mixture Substances 0.000 claims description 123
- RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 claims description 76
- 229960001786 megestrol Drugs 0.000 claims description 63
- 238000009472 formulation Methods 0.000 claims description 18
- 229960004296 megestrol acetate Drugs 0.000 claims description 13
- 239000013543 active substance Substances 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 8
- 239000007788 liquid Substances 0.000 claims description 6
- 239000002105 nanoparticle Substances 0.000 claims description 4
- 239000006185 dispersion Substances 0.000 claims description 3
- 239000002552 dosage form Substances 0.000 claims description 2
- 239000003381 stabilizer Substances 0.000 claims 42
- -1 sorbitan ester Chemical class 0.000 claims 30
- 238000000034 method Methods 0.000 claims 27
- 239000002245 particle Substances 0.000 claims 27
- 244000060011 Cocos nucifera Species 0.000 claims 12
- 235000013162 Cocos nucifera Nutrition 0.000 claims 12
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims 8
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 8
- 229920000642 polymer Polymers 0.000 claims 8
- AISMNBXOJRHCIA-UHFFFAOYSA-N trimethylazanium;bromide Chemical compound Br.CN(C)C AISMNBXOJRHCIA-UHFFFAOYSA-N 0.000 claims 8
- 239000000654 additive Substances 0.000 claims 7
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 7
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 7
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 6
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 6
- 125000002091 cationic group Chemical group 0.000 claims 6
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 6
- 230000000052 comparative effect Effects 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims 4
- BSTPEQSVYGELTA-UHFFFAOYSA-N 2-(dimethylamino)ethanol;hydrobromide Chemical compound [Br-].C[NH+](C)CCO BSTPEQSVYGELTA-UHFFFAOYSA-N 0.000 claims 4
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 4
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 4
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 4
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 claims 4
- 238000010521 absorption reaction Methods 0.000 claims 4
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 claims 4
- 150000001412 amines Chemical class 0.000 claims 4
- 150000001413 amino acids Chemical group 0.000 claims 4
- 229960000686 benzalkonium chloride Drugs 0.000 claims 4
- JBIROUFYLSSYDX-UHFFFAOYSA-M benzododecinium chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 JBIROUFYLSSYDX-UHFFFAOYSA-M 0.000 claims 4
- 229920002678 cellulose Polymers 0.000 claims 4
- 239000001913 cellulose Substances 0.000 claims 4
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims 4
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical group [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims 4
- 229940107161 cholesterol Drugs 0.000 claims 4
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
- 239000003246 corticosteroid Substances 0.000 claims 4
- 125000005131 dialkylammonium group Chemical group 0.000 claims 4
- 235000014113 dietary fatty acids Nutrition 0.000 claims 4
- 235000015872 dietary supplement Nutrition 0.000 claims 4
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims 4
- YHAIUSTWZPMYGG-UHFFFAOYSA-L disodium;2,2-dioctyl-3-sulfobutanedioate Chemical compound [Na+].[Na+].CCCCCCCCC(C([O-])=O)(C(C([O-])=O)S(O)(=O)=O)CCCCCCCC YHAIUSTWZPMYGG-UHFFFAOYSA-L 0.000 claims 4
- 229960000878 docusate sodium Drugs 0.000 claims 4
- DDXLVDQZPFLQMZ-UHFFFAOYSA-M dodecyl(trimethyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)C DDXLVDQZPFLQMZ-UHFFFAOYSA-M 0.000 claims 4
- 239000000194 fatty acid Substances 0.000 claims 4
- 229930195729 fatty acid Natural products 0.000 claims 4
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 4
- 150000004820 halides Chemical class 0.000 claims 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 4
- HICYUNOFRYFIMG-UHFFFAOYSA-N n,n-dimethyl-1-naphthalen-1-ylmethanamine;hydrochloride Chemical compound [Cl-].C1=CC=C2C(C[NH+](C)C)=CC=CC2=C1 HICYUNOFRYFIMG-UHFFFAOYSA-N 0.000 claims 4
- 150000003904 phospholipids Chemical class 0.000 claims 4
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 4
- 229920005604 random copolymer Polymers 0.000 claims 4
- 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 4
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical compound O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims 3
- 102000016943 Muramidase Human genes 0.000 claims 3
- 108010014251 Muramidase Proteins 0.000 claims 3
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 claims 3
- 230000000202 analgesic effect Effects 0.000 claims 3
- 239000004325 lysozyme Substances 0.000 claims 3
- 229960000274 lysozyme Drugs 0.000 claims 3
- 235000010335 lysozyme Nutrition 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 229940044551 receptor antagonist Drugs 0.000 claims 3
- 239000002464 receptor antagonist Substances 0.000 claims 3
- MJYQFWSXKFLTAY-OVEQLNGDSA-N (2r,3r)-2,3-bis[(4-hydroxy-3-methoxyphenyl)methyl]butane-1,4-diol;(2r,3r,4s,5s,6r)-6-(hydroxymethyl)oxane-2,3,4,5-tetrol Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O.C1=C(O)C(OC)=CC(C[C@@H](CO)[C@H](CO)CC=2C=C(OC)C(O)=CC=2)=C1 MJYQFWSXKFLTAY-OVEQLNGDSA-N 0.000 claims 2
- 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 2
- JVAZJLFFSJARQM-RMPHRYRLSA-N (2r,3r,4s,5s,6r)-2-hexoxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound CCCCCCO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O JVAZJLFFSJARQM-RMPHRYRLSA-N 0.000 claims 2
- TZCPCKNHXULUIY-RGULYWFUSA-N 1,2-distearoyl-sn-glycero-3-phosphoserine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCCCCCCCCCCCC TZCPCKNHXULUIY-RGULYWFUSA-N 0.000 claims 2
- QAQSNXHKHKONNS-UHFFFAOYSA-N 1-ethyl-2-hydroxy-4-methyl-6-oxopyridine-3-carboxamide Chemical compound CCN1C(O)=C(C(N)=O)C(C)=CC1=O QAQSNXHKHKONNS-UHFFFAOYSA-N 0.000 claims 2
- RMAJTXKOOKJAAV-UHFFFAOYSA-N 2,2-dihydroxyethyl(methyl)azanium;bromide Chemical compound [Br-].C[NH2+]CC(O)O RMAJTXKOOKJAAV-UHFFFAOYSA-N 0.000 claims 2
- DBRHJJQHHSOXCQ-UHFFFAOYSA-N 2,2-dihydroxyethyl(methyl)azanium;chloride Chemical compound [Cl-].C[NH2+]CC(O)O DBRHJJQHHSOXCQ-UHFFFAOYSA-N 0.000 claims 2
- LKAWQFHWVVSFTR-UHFFFAOYSA-N 2-(methylamino)ethanol;hydrochloride Chemical compound [Cl-].C[NH2+]CCO LKAWQFHWVVSFTR-UHFFFAOYSA-N 0.000 claims 2
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims 2
- MPNXSZJPSVBLHP-UHFFFAOYSA-N 2-chloro-n-phenylpyridine-3-carboxamide Chemical compound ClC1=NC=CC=C1C(=O)NC1=CC=CC=C1 MPNXSZJPSVBLHP-UHFFFAOYSA-N 0.000 claims 2
- YJHSJERLYWNLQL-UHFFFAOYSA-N 2-hydroxyethyl(dimethyl)azanium;chloride Chemical compound Cl.CN(C)CCO YJHSJERLYWNLQL-UHFFFAOYSA-N 0.000 claims 2
- BZSJQMAZLOWECR-UHFFFAOYSA-N 2-methylprop-2-enoate trimethylazanium bromide Chemical compound [Br-].C[NH+](C)C.C(C(=C)C)(=O)[O-].C[NH+](C)C BZSJQMAZLOWECR-UHFFFAOYSA-N 0.000 claims 2
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims 2
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical group NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims 2
- 244000144927 Aloe barbadensis Species 0.000 claims 2
- 235000002961 Aloe barbadensis Nutrition 0.000 claims 2
- 241000416162 Astragalus gummifer Species 0.000 claims 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 2
- 102000055006 Calcitonin Human genes 0.000 claims 2
- 108060001064 Calcitonin Proteins 0.000 claims 2
- CXRFDZFCGOPDTD-UHFFFAOYSA-M Cetrimide Chemical compound [Br-].CCCCCCCCCCCCCC[N+](C)(C)C CXRFDZFCGOPDTD-UHFFFAOYSA-M 0.000 claims 2
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims 2
- 229920002567 Chondroitin Polymers 0.000 claims 2
- 244000303965 Cyamopsis psoralioides Species 0.000 claims 2
- 229920002307 Dextran Polymers 0.000 claims 2
- RUPBZQFQVRMKDG-UHFFFAOYSA-M Didecyldimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCC[N+](C)(C)CCCCCCCCCC RUPBZQFQVRMKDG-UHFFFAOYSA-M 0.000 claims 2
- 229940122858 Elastase inhibitor Drugs 0.000 claims 2
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 2
- 108010010803 Gelatin Proteins 0.000 claims 2
- ZWZWYGMENQVNFU-UHFFFAOYSA-N Glycerophosphorylserin Natural products OC(=O)C(N)COP(O)(=O)OCC(O)CO ZWZWYGMENQVNFU-UHFFFAOYSA-N 0.000 claims 2
- CTKINSOISVBQLD-UHFFFAOYSA-N Glycidol Chemical compound OCC1CO1 CTKINSOISVBQLD-UHFFFAOYSA-N 0.000 claims 2
- 229920000084 Gum arabic Polymers 0.000 claims 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 2
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 2
- UPYKUZBSLRQECL-UKMVMLAPSA-N Lycopene Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1C(=C)CCCC1(C)C)C=CC=C(/C)C=CC2C(=C)CCCC2(C)C UPYKUZBSLRQECL-UKMVMLAPSA-N 0.000 claims 2
- JEVVKJMRZMXFBT-XWDZUXABSA-N Lycophyll Natural products OC/C(=C/CC/C(=C\C=C\C(=C/C=C/C(=C\C=C\C=C(/C=C/C=C(\C=C\C=C(/CC/C=C(/CO)\C)\C)/C)\C)/C)\C)/C)/C JEVVKJMRZMXFBT-XWDZUXABSA-N 0.000 claims 2
- YJPIGAIKUZMOQA-UHFFFAOYSA-N Melatonin Natural products COC1=CC=C2N(C(C)=O)C=C(CCN)C2=C1 YJPIGAIKUZMOQA-UHFFFAOYSA-N 0.000 claims 2
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims 2
- JVAZJLFFSJARQM-UHFFFAOYSA-N O-n-hexyl beta-D-glucopyranoside Natural products CCCCCCOC1OC(CO)C(O)C(O)C1O JVAZJLFFSJARQM-UHFFFAOYSA-N 0.000 claims 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 239000004721 Polyphenylene oxide Substances 0.000 claims 2
- 229920001214 Polysorbate 60 Polymers 0.000 claims 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 235000021355 Stearic acid Nutrition 0.000 claims 2
- 229930006000 Sucrose Natural products 0.000 claims 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 2
- 239000000150 Sympathomimetic Substances 0.000 claims 2
- 244000269722 Thea sinensis Species 0.000 claims 2
- 229920001615 Tragacanth Polymers 0.000 claims 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims 2
- NJSSICCENMLTKO-HRCBOCMUSA-N [(1r,2s,4r,5r)-3-hydroxy-4-(4-methylphenyl)sulfonyloxy-6,8-dioxabicyclo[3.2.1]octan-2-yl] 4-methylbenzenesulfonate Chemical compound C1=CC(C)=CC=C1S(=O)(=O)O[C@H]1C(O)[C@@H](OS(=O)(=O)C=2C=CC(C)=CC=2)[C@@H]2OC[C@H]1O2 NJSSICCENMLTKO-HRCBOCMUSA-N 0.000 claims 2
- SZYSLWCAWVWFLT-UTGHZIEOSA-N [(2s,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-[(2r,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-2-yl]methyl octadecanoate Chemical compound O([C@@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@]1(COC(=O)CCCCCCCCCCCCCCCCC)O[C@H](CO)[C@@H](O)[C@@H]1O SZYSLWCAWVWFLT-UTGHZIEOSA-N 0.000 claims 2
- 235000010489 acacia gum Nutrition 0.000 claims 2
- 239000000205 acacia gum Substances 0.000 claims 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 2
- 239000002253 acid Substances 0.000 claims 2
- 229960005305 adenosine Drugs 0.000 claims 2
- 229940072056 alginate Drugs 0.000 claims 2
- 229920000615 alginic acid Polymers 0.000 claims 2
- 235000010443 alginic acid Nutrition 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000006177 alkyl benzyl group Chemical group 0.000 claims 2
- 150000005215 alkyl ethers Chemical class 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000005211 alkyl trimethyl ammonium group Chemical group 0.000 claims 2
- 235000011399 aloe vera Nutrition 0.000 claims 2
- 102000004305 alpha Adrenergic Receptors Human genes 0.000 claims 2
- 108090000861 alpha Adrenergic Receptors Proteins 0.000 claims 2
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims 2
- 235000001014 amino acid Nutrition 0.000 claims 2
- SWLVFNYSXGMGBS-UHFFFAOYSA-N ammonium bromide Chemical compound [NH4+].[Br-] SWLVFNYSXGMGBS-UHFFFAOYSA-N 0.000 claims 2
- 235000019270 ammonium chloride Nutrition 0.000 claims 2
- 239000002269 analeptic agent Substances 0.000 claims 2
- 239000010775 animal oil Substances 0.000 claims 2
- 125000000129 anionic group Chemical group 0.000 claims 2
- 230000000507 anthelmentic effect Effects 0.000 claims 2
- 230000003288 anthiarrhythmic effect Effects 0.000 claims 2
- 230000001430 anti-depressive effect Effects 0.000 claims 2
- 230000003178 anti-diabetic effect Effects 0.000 claims 2
- 230000003474 anti-emetic effect Effects 0.000 claims 2
- 230000003110 anti-inflammatory effect Effects 0.000 claims 2
- 230000001022 anti-muscarinic effect Effects 0.000 claims 2
- 230000001355 anti-mycobacterial effect Effects 0.000 claims 2
- 239000000883 anti-obesity agent Substances 0.000 claims 2
- 230000001754 anti-pyretic effect Effects 0.000 claims 2
- 230000002921 anti-spasmodic effect Effects 0.000 claims 2
- 239000000043 antiallergic agent Substances 0.000 claims 2
- 239000003416 antiarrhythmic agent Substances 0.000 claims 2
- 239000003146 anticoagulant agent Substances 0.000 claims 2
- 229940127219 anticoagulant drug Drugs 0.000 claims 2
- 239000000935 antidepressant agent Substances 0.000 claims 2
- 229940005513 antidepressants Drugs 0.000 claims 2
- 239000003472 antidiabetic agent Substances 0.000 claims 2
- 239000002111 antiemetic agent Substances 0.000 claims 2
- 239000003429 antifungal agent Substances 0.000 claims 2
- 229940121375 antifungal agent Drugs 0.000 claims 2
- 229940030225 antihemorrhagics Drugs 0.000 claims 2
- 239000002220 antihypertensive agent Substances 0.000 claims 2
- 229940127088 antihypertensive drug Drugs 0.000 claims 2
- 239000003926 antimycobacterial agent Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 229940041181 antineoplastic drug Drugs 0.000 claims 2
- 229940125710 antiobesity agent Drugs 0.000 claims 2
- 239000003963 antioxidant agent Substances 0.000 claims 2
- 235000006708 antioxidants Nutrition 0.000 claims 2
- 239000002221 antipyretic Substances 0.000 claims 2
- 239000003200 antithyroid agent Substances 0.000 claims 2
- 229940043671 antithyroid preparations Drugs 0.000 claims 2
- 239000003434 antitussive agent Substances 0.000 claims 2
- 229940124584 antitussives Drugs 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 239000002249 anxiolytic agent Substances 0.000 claims 2
- 239000002830 appetite depressant Substances 0.000 claims 2
- 239000003212 astringent agent Substances 0.000 claims 2
- KHSLHYAUZSPBIU-UHFFFAOYSA-M benzododecinium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 KHSLHYAUZSPBIU-UHFFFAOYSA-M 0.000 claims 2
- UUZYBYIOAZTMGC-UHFFFAOYSA-M benzyl(trimethyl)azanium;bromide Chemical compound [Br-].C[N+](C)(C)CC1=CC=CC=C1 UUZYBYIOAZTMGC-UHFFFAOYSA-M 0.000 claims 2
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| JP2005527584A JP2005527584A (ja) | 2005-09-15 |
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| DK (1) | DK1494649T3 (enExample) |
| ES (1) | ES2380318T3 (enExample) |
| PT (1) | PT1494649E (enExample) |
| WO (1) | WO2003086354A1 (enExample) |
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| US9101540B2 (en) | 2002-04-12 | 2015-08-11 | Alkermes Pharma Ireland Limited | Nanoparticulate megestrol formulations |
| CA2544627A1 (en) * | 2003-11-05 | 2005-05-19 | Elan Pharma International Ltd. | Nanoparticulate compositions having a peptide as a surface stabilizer |
| US20050131079A1 (en) * | 2003-12-10 | 2005-06-16 | Pujara Chetan P. | Cefdinir oral suspension |
| DE602004027515D1 (de) * | 2004-12-01 | 2010-07-15 | Par Pharmaceuticals Inc | Verwendung von Megestrolacetat zur Verbesserung der Herzfunktion und zur Behandlung von Herzinsuffizienz |
| ATE511835T1 (de) * | 2005-02-17 | 2011-06-15 | Hadasit Med Res Service | Biophosphonate zur behandlung von endometriose |
| EP1871345B1 (en) | 2005-04-12 | 2012-08-01 | Elan Pharma International Limited | Nanoparticulate erlotinib formulations |
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| EA200800099A1 (ru) * | 2005-06-22 | 2008-06-30 | Элан Фарма Интернэшнл Лтд. | Композиции наночастиц мегестрола |
| EP1749531B1 (en) | 2005-08-03 | 2015-07-22 | Par Pharmaceuticals, Inc. | Use of an oral suspension comprising megestrol acetate for the treatment of bronchial asthma |
| BRPI0714173A2 (pt) * | 2006-07-12 | 2012-12-25 | Elan Pharma Int Ltd | composiÇço nanoparticulada estÁvel,mÉtodos para preparar a composiÇço, para prevenir e/ou tratar estados de doenÇas, sintomas, sÍndromes e condiÇÕes do sistema nervoso central, para melhorar ou manter a biodisponibilidade de modafinil, e para tratar distérbio com base neurolàgica, composiÇço farmacÊutica, e forma de dosagem |
| EP2101735A2 (en) * | 2006-11-28 | 2009-09-23 | Marinus Pharmaceuticals, Inc. | Nanoparticulate formulations and methods for the making and use thereof |
| CN101730547A (zh) * | 2007-04-24 | 2010-06-09 | 阿卡西亚制药有限公司 | 用于治疗肌肉丧失的β2激动剂和妊娠素的药物组合 |
| US9993427B2 (en) | 2013-03-14 | 2018-06-12 | Biorest Ltd. | Liposome formulation and manufacture |
| CN114746083A (zh) * | 2019-12-02 | 2022-07-12 | 默克专利股份有限公司 | 活性药物成分的纳米悬浮液在载体上的沉积 |
| CN111904931B (zh) * | 2020-07-06 | 2022-09-20 | 中国人民解放军军事科学院军事医学研究院 | 一种醋酸甲地孕酮纳米晶口服混悬液及其制备方法和其应用 |
| EP4221693A1 (en) | 2020-09-29 | 2023-08-09 | Millicent Pharma Limited | Orodispersible formulations |
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-
2003
- 2003-04-14 EP EP03723991A patent/EP1494649B1/en not_active Expired - Lifetime
- 2003-04-14 EP EP10010939.6A patent/EP2263650A3/en not_active Withdrawn
- 2003-04-14 DK DK03723991.0T patent/DK1494649T3/da active
- 2003-04-14 JP JP2003583377A patent/JP4865990B2/ja not_active Expired - Fee Related
- 2003-04-14 WO PCT/US2003/011277 patent/WO2003086354A1/en not_active Ceased
- 2003-04-14 CA CA2481390A patent/CA2481390C/en not_active Expired - Fee Related
- 2003-04-14 AT AT03723991T patent/ATE539737T1/de active
- 2003-04-14 AU AU2003230885A patent/AU2003230885A1/en not_active Abandoned
- 2003-04-14 PT PT03723991T patent/PT1494649E/pt unknown
- 2003-04-14 ES ES03723991T patent/ES2380318T3/es not_active Expired - Lifetime
-
2010
- 2010-06-21 JP JP2010140607A patent/JP2010248220A/ja not_active Withdrawn
-
2012
- 2012-03-26 CY CY20121100307T patent/CY1113036T1/el unknown
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