LT3201B - Memantine-containing solid pharmaceutical dosage forms having an extended two-stage release profile and production thereof - Google Patents
Memantine-containing solid pharmaceutical dosage forms having an extended two-stage release profile and production thereof Download PDFInfo
- Publication number
- LT3201B LT3201B LTIP839A LTIP839A LT3201B LT 3201 B LT3201 B LT 3201B LT IP839 A LTIP839 A LT IP839A LT IP839 A LTIP839 A LT IP839A LT 3201 B LT3201 B LT 3201B
- Authority
- LT
- Lithuania
- Prior art keywords
- water
- insoluble
- casein
- pharmaceutical composition
- salt
- Prior art date
Links
- 239000002552 dosage form Substances 0.000 title claims abstract description 19
- 229960004640 memantine Drugs 0.000 title claims abstract description 12
- 239000007787 solid Substances 0.000 title claims abstract description 12
- 238000004519 manufacturing process Methods 0.000 title claims abstract description 8
- BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 title claims abstract 4
- BECPQYXYKAMYBN-UHFFFAOYSA-N casein, tech. Chemical compound NCCCCC(C(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(CC(C)C)N=C(O)C(CCC(O)=O)N=C(O)C(CC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(C(C)O)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=N)N=C(O)C(CCC(O)=O)N=C(O)C(CCC(O)=O)N=C(O)C(COP(O)(O)=O)N=C(O)C(CCC(O)=N)N=C(O)C(N)CC1=CC=CC=C1 BECPQYXYKAMYBN-UHFFFAOYSA-N 0.000 claims abstract description 58
- 239000000203 mixture Substances 0.000 claims abstract description 52
- 239000004480 active ingredient Substances 0.000 claims abstract description 28
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 26
- 239000011159 matrix material Substances 0.000 claims abstract description 23
- 108010076119 Caseins Proteins 0.000 claims abstract description 20
- 150000003839 salts Chemical class 0.000 claims abstract description 12
- 108010033929 calcium caseinate Proteins 0.000 claims abstract description 11
- 239000005018 casein Substances 0.000 claims abstract description 9
- 235000021240 caseins Nutrition 0.000 claims abstract description 9
- 238000000034 method Methods 0.000 claims abstract description 9
- 230000008569 process Effects 0.000 claims abstract description 5
- 239000003814 drug Substances 0.000 claims description 34
- 229940079593 drug Drugs 0.000 claims description 33
- 229940088598 enzyme Drugs 0.000 claims description 27
- 108090000790 Enzymes Proteins 0.000 claims description 26
- 102000004190 Enzymes Human genes 0.000 claims description 26
- 102000011632 Caseins Human genes 0.000 claims description 18
- 150000001768 cations Chemical class 0.000 claims description 13
- 230000002051 biphasic effect Effects 0.000 claims description 10
- 229940080237 sodium caseinate Drugs 0.000 claims description 10
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 8
- 239000011575 calcium Substances 0.000 claims description 8
- 229910052791 calcium Inorganic materials 0.000 claims description 8
- 108010019160 Pancreatin Proteins 0.000 claims description 7
- 108090000284 Pepsin A Proteins 0.000 claims description 7
- 102000057297 Pepsin A Human genes 0.000 claims description 7
- -1 cation salt Chemical class 0.000 claims description 7
- 238000011065 in-situ storage Methods 0.000 claims description 7
- 229940055695 pancreatin Drugs 0.000 claims description 7
- 229940111202 pepsin Drugs 0.000 claims description 7
- 239000007909 solid dosage form Substances 0.000 claims description 5
- 239000006187 pill Substances 0.000 claims description 3
- 238000013268 sustained release Methods 0.000 claims description 3
- 239000012730 sustained-release form Substances 0.000 claims description 3
- 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 abstract description 4
- 239000011734 sodium Substances 0.000 abstract description 4
- 229910052708 sodium Inorganic materials 0.000 abstract description 4
- 229940071162 caseinate Drugs 0.000 description 42
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 26
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 20
- 235000019359 magnesium stearate Nutrition 0.000 description 13
- 239000003826 tablet Substances 0.000 description 13
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 11
- 230000000694 effects Effects 0.000 description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 11
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 10
- 229960001948 caffeine Drugs 0.000 description 10
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 10
- 239000013543 active substance Substances 0.000 description 9
- 239000000654 additive Substances 0.000 description 9
- 239000012530 fluid Substances 0.000 description 9
- 238000009472 formulation Methods 0.000 description 9
- 230000002496 gastric effect Effects 0.000 description 9
- 239000002609 medium Substances 0.000 description 9
- LDDHMLJTFXJGPI-UHFFFAOYSA-N memantine hydrochloride Chemical compound Cl.C1C(C2)CC3(C)CC1(C)CC2(N)C3 LDDHMLJTFXJGPI-UHFFFAOYSA-N 0.000 description 9
- 238000007906 compression Methods 0.000 description 8
- 230000006835 compression Effects 0.000 description 8
- 229960005069 calcium Drugs 0.000 description 7
- 230000008859 change Effects 0.000 description 7
- 238000004090 dissolution Methods 0.000 description 7
- 238000013265 extended release Methods 0.000 description 7
- 210000002784 stomach Anatomy 0.000 description 7
- 229910002016 Aerosil® 200 Inorganic materials 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 210000000936 intestine Anatomy 0.000 description 6
- 238000003556 assay Methods 0.000 description 5
- 239000012738 dissolution medium Substances 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 238000005469 granulation Methods 0.000 description 5
- 230000003179 granulation Effects 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 230000002035 prolonged effect Effects 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 229910002012 Aerosil® Inorganic materials 0.000 description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 4
- 239000001110 calcium chloride Substances 0.000 description 4
- 229960002713 calcium chloride Drugs 0.000 description 4
- 229910001628 calcium chloride Inorganic materials 0.000 description 4
- 238000013270 controlled release Methods 0.000 description 4
- 238000005516 engineering process Methods 0.000 description 4
- 229960001680 ibuprofen Drugs 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 230000036470 plasma concentration Effects 0.000 description 4
- 235000018102 proteins Nutrition 0.000 description 4
- 102000004169 proteins and genes Human genes 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 230000000968 intestinal effect Effects 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 229910052749 magnesium Inorganic materials 0.000 description 3
- 239000011777 magnesium Substances 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 229920001223 polyethylene glycol Polymers 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 239000007916 tablet composition Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 229920003084 Avicel® PH-102 Polymers 0.000 description 2
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 2
- 239000011149 active material Substances 0.000 description 2
- 230000000996 additive effect Effects 0.000 description 2
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 2
- 235000010443 alginic acid Nutrition 0.000 description 2
- 229920000615 alginic acid Polymers 0.000 description 2
- 229940035676 analgesics Drugs 0.000 description 2
- 239000000730 antalgic agent Substances 0.000 description 2
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
- 229960003563 calcium carbonate Drugs 0.000 description 2
- 239000004227 calcium gluconate Substances 0.000 description 2
- 229960004494 calcium gluconate Drugs 0.000 description 2
- 235000013927 calcium gluconate Nutrition 0.000 description 2
- MKJXYGKVIBWPFZ-UHFFFAOYSA-L calcium lactate Chemical compound [Ca+2].CC(O)C([O-])=O.CC(O)C([O-])=O MKJXYGKVIBWPFZ-UHFFFAOYSA-L 0.000 description 2
- 239000001527 calcium lactate Substances 0.000 description 2
- 229960002401 calcium lactate Drugs 0.000 description 2
- 235000011086 calcium lactate Nutrition 0.000 description 2
- 229940078480 calcium levulinate Drugs 0.000 description 2
- ZCCIPPOKBCJFDN-UHFFFAOYSA-N calcium nitrate Chemical compound [Ca+2].[O-][N+]([O-])=O.[O-][N+]([O-])=O ZCCIPPOKBCJFDN-UHFFFAOYSA-N 0.000 description 2
- 159000000007 calcium salts Chemical class 0.000 description 2
- UGZVNIRNPPEDHM-SBBOJQDXSA-L calcium;(2s,3s,4s,5r)-2,3,4,5-tetrahydroxyhexanedioate Chemical compound [Ca+2].[O-]C(=O)[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O UGZVNIRNPPEDHM-SBBOJQDXSA-L 0.000 description 2
- NEEHYRZPVYRGPP-UHFFFAOYSA-L calcium;2,3,4,5,6-pentahydroxyhexanoate Chemical compound [Ca+2].OCC(O)C(O)C(O)C(O)C([O-])=O.OCC(O)C(O)C(O)C(O)C([O-])=O NEEHYRZPVYRGPP-UHFFFAOYSA-L 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 238000009792 diffusion process Methods 0.000 description 2
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- 239000007888 film coating Substances 0.000 description 2
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- 210000004051 gastric juice Anatomy 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
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- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 229960002003 hydrochlorothiazide Drugs 0.000 description 2
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- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- PXDJXZJSCPSGGI-UHFFFAOYSA-N palmityl palmitate Chemical compound CCCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC PXDJXZJSCPSGGI-UHFFFAOYSA-N 0.000 description 2
- XQYZDYMELSJDRZ-UHFFFAOYSA-N papaverine Chemical compound C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 XQYZDYMELSJDRZ-UHFFFAOYSA-N 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
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- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 description 1
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- TWBNMYSKRDRHAT-RCWTXCDDSA-N (S)-timolol hemihydrate Chemical compound O.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1 TWBNMYSKRDRHAT-RCWTXCDDSA-N 0.000 description 1
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 description 1
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 description 1
- GCKMFJBGXUYNAG-UHFFFAOYSA-N 17alpha-methyltestosterone Natural products C1CC2=CC(=O)CCC2(C)C2C1C1CCC(C)(O)C1(C)CC2 GCKMFJBGXUYNAG-UHFFFAOYSA-N 0.000 description 1
- FSVJFNAIGNNGKK-UHFFFAOYSA-N 2-[cyclohexyl(oxo)methyl]-3,6,7,11b-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4-one Chemical compound C1C(C2=CC=CC=C2CC2)N2C(=O)CN1C(=O)C1CCCCC1 FSVJFNAIGNNGKK-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 229930008281 A03AD01 - Papaverine Natural products 0.000 description 1
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- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
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- AZDRQVAHHNSJOQ-UHFFFAOYSA-N alumane Chemical class [AlH3] AZDRQVAHHNSJOQ-UHFFFAOYSA-N 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
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- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 description 1
- 229960003805 amantadine Drugs 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
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- IZMJMCDDWKSTTK-UHFFFAOYSA-N quinoline yellow Chemical compound C1=CC=CC2=NC(C3C(C4=CC=CC=C4C3=O)=O)=CC=C21 IZMJMCDDWKSTTK-UHFFFAOYSA-N 0.000 description 1
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- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
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- 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 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2063—Proteins, e.g. gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
-
- 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
- A61K9/1658—Proteins, e.g. albumin, gelatin
-
- 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
- A61K9/2068—Compounds of unknown constitution, e.g. material from plants or animals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Botany (AREA)
- Zoology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4225730A DE4225730C2 (de) | 1992-08-04 | 1992-08-04 | Verfahren zur Herstellung von festen Arzneiformkörpern mit protrahierter 2-Stufen-Freisetzung |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| LTIP839A LTIP839A (lt) | 1994-08-25 |
| LT3201B true LT3201B (en) | 1995-03-27 |
Family
ID=6464804
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LTIP839A LT3201B (en) | 1992-08-04 | 1993-08-04 | Memantine-containing solid pharmaceutical dosage forms having an extended two-stage release profile and production thereof |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US5382601A (es) |
| EP (1) | EP0582186B1 (es) |
| JP (1) | JP3560244B2 (es) |
| CN (1) | CN1086708A (es) |
| AT (1) | ATE176866T1 (es) |
| AU (1) | AU669731B2 (es) |
| CA (1) | CA2141691C (es) |
| DE (2) | DE4225730C2 (es) |
| DK (1) | DK0582186T3 (es) |
| ES (1) | ES2128369T3 (es) |
| GR (1) | GR3030227T3 (es) |
| IL (1) | IL106580A (es) |
| LT (1) | LT3201B (es) |
| LV (1) | LV10182B (es) |
| MX (1) | MX9304675A (es) |
| WO (1) | WO1994003158A1 (es) |
| ZA (1) | ZA935614B (es) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5817336A (en) * | 1993-04-02 | 1998-10-06 | Orion-Yhtyma Oy | Composition containing selegiline |
| AUPN605795A0 (en) * | 1995-10-19 | 1995-11-09 | F.H. Faulding & Co. Limited | Analgesic pharmaceutical composition |
| US6139872A (en) * | 1996-08-14 | 2000-10-31 | Henkel Corporation | Method of producing a vitamin product |
| US6057373A (en) * | 1997-05-22 | 2000-05-02 | Synchroneuron, Llc | Methods of treating tardive dyskinesia and other movement disorders using NMDA receptor antagonists |
| US5866585A (en) * | 1997-05-22 | 1999-02-02 | Synchroneuron, Llc | Methods of treating tardive dyskinesia using NMDA receptor antagonists |
| AU3860797A (en) * | 1997-07-16 | 1999-02-10 | Antrin Research Limited | Pharmaceutical formulations for oral administration |
| US5840334A (en) * | 1997-08-20 | 1998-11-24 | Fuisz Technologies Ltd. | Self-binding shearform compositions |
| US5980941A (en) * | 1997-08-20 | 1999-11-09 | Fuisz Technologies Ltd. | Self-binding shearform compositions |
| US6294583B1 (en) * | 1998-01-13 | 2001-09-25 | Synchroneuron, Llc | Methods of treating tardive dyskinesia and other movement disorders |
| US5952389A (en) * | 1998-01-13 | 1999-09-14 | Synchroneuron | Methods of treating tardive dyskinesia and other movement disorders |
| DE19809242A1 (de) * | 1998-03-05 | 1999-09-09 | Basf Ag | Verfahren zur Herstellung von festen, sphärischen Formkörpern, enthaltend pharmazeutische Wirkstoffe in einer Bindemittelmatrix |
| DE19814257A1 (de) | 1998-03-31 | 1999-10-07 | Asta Medica Ag | Brauseformulierungen |
| US6444702B1 (en) | 2000-02-22 | 2002-09-03 | Neuromolecular, Inc. | Aminoadamantane derivatives as therapeutic agents |
| US20040122090A1 (en) * | 2001-12-07 | 2004-06-24 | Lipton Stuart A. | Methods for treating neuropsychiatric disorders with nmda receptor antagonists |
| EP1852113A3 (en) * | 2000-12-07 | 2008-03-12 | Neuromolecular Inc. | Methods for treating neuropsychiatric disorders with NMDA receptors antagonists |
| AU2005209310B2 (en) * | 2004-01-29 | 2011-01-06 | Neuromolecular, Inc. | Combination of a NMDA receptor antagonist and a MAO-inhibitor or a GADPH-inhibitor for the treatment of central nervous system-related conditions |
| US20050245460A1 (en) * | 2004-02-13 | 2005-11-03 | Meyerson Laurence R | Methods and compositions for the treatment of epilepsy, seizure disorders, and other CNS disorders |
| WO2005079756A2 (en) * | 2004-02-13 | 2005-09-01 | Neuromolecular, Inc. | Combination of a nmda receptor antagonist and an anti-depressive drug mao-inhibitor or a gadph-inhibitor for the treatment of psychiatric conditions |
| KR100901927B1 (ko) * | 2004-06-17 | 2009-06-10 | 메르츠 파마 게엠베하 운트 코. 카가아 | 메만타인 또는 네라멕산의 직접 압축으로 제조된 마실수 있는 즉시 방출형 제제 |
| US20060002999A1 (en) | 2004-06-17 | 2006-01-05 | Forest Laboratories, Inc. | Immediate release formulations of 1-aminocyclohexane compounds, memantine and neramexane |
| CN1968684A (zh) * | 2004-06-17 | 2007-05-23 | 森林实验室公司 | 美金刚的调释制剂 |
| EP2601937A1 (en) * | 2004-06-17 | 2013-06-12 | Merz Pharma GmbH & Co. KGaA | Drinkable immediate release tablet made with direct compression of memantine or neramexane |
| MX2007006120A (es) * | 2004-11-23 | 2007-12-07 | Adamas Pharmaceuticals Inc | Metodo y composicion para administrar a un sujeto un antagonista del receptor de nmda. |
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- 1993-07-28 ES ES93112018T patent/ES2128369T3/es not_active Expired - Lifetime
- 1993-07-28 AT AT93112018T patent/ATE176866T1/de active
- 1993-07-28 DE DE59309388T patent/DE59309388D1/de not_active Expired - Lifetime
- 1993-07-28 DK DK93112018T patent/DK0582186T3/da active
- 1993-07-28 EP EP93112018A patent/EP0582186B1/de not_active Expired - Lifetime
- 1993-08-03 IL IL106580A patent/IL106580A/en not_active IP Right Cessation
- 1993-08-03 MX MX9304675A patent/MX9304675A/es unknown
- 1993-08-03 ZA ZA935614A patent/ZA935614B/xx unknown
- 1993-08-04 AU AU47069/93A patent/AU669731B2/en not_active Expired
- 1993-08-04 LT LTIP839A patent/LT3201B/lt not_active IP Right Cessation
- 1993-08-04 CA CA002141691A patent/CA2141691C/en not_active Expired - Lifetime
- 1993-08-04 CN CN93116211A patent/CN1086708A/zh active Pending
- 1993-08-04 JP JP50501594A patent/JP3560244B2/ja not_active Expired - Fee Related
- 1993-08-04 WO PCT/EP1993/002074 patent/WO1994003158A1/en not_active Ceased
- 1993-08-04 LV LVP-93-1013A patent/LV10182B/en unknown
-
1999
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| US4665081A (en) | 1982-12-02 | 1987-05-12 | Takada Seiyaku Kabushiki Kaisha | Solid nifedipine preparations and a process for preparing same |
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| EP0447100A1 (en) | 1990-03-06 | 1991-09-18 | Kelco International Limited | Controlled release formulation |
Also Published As
| Publication number | Publication date |
|---|---|
| US5382601A (en) | 1995-01-17 |
| CA2141691C (en) | 2002-04-09 |
| LV10182B (en) | 1995-04-20 |
| DE4225730A1 (de) | 1994-02-10 |
| AU669731B2 (en) | 1996-06-20 |
| WO1994003158A1 (en) | 1994-02-17 |
| LV10182A (lv) | 1994-10-20 |
| ATE176866T1 (de) | 1999-03-15 |
| AU4706993A (en) | 1994-03-03 |
| ES2128369T3 (es) | 1999-05-16 |
| DE59309388D1 (de) | 1999-04-01 |
| JP3560244B2 (ja) | 2004-09-02 |
| JPH07509479A (ja) | 1995-10-19 |
| EP0582186B1 (de) | 1999-02-24 |
| CA2141691A1 (en) | 1994-02-17 |
| GR3030227T3 (en) | 1999-08-31 |
| MX9304675A (es) | 1994-03-31 |
| LTIP839A (lt) | 1994-08-25 |
| ZA935614B (en) | 1995-02-03 |
| CN1086708A (zh) | 1994-05-18 |
| DK0582186T3 (da) | 1999-09-27 |
| EP0582186A1 (de) | 1994-02-09 |
| IL106580A0 (en) | 1993-12-08 |
| DE4225730C2 (de) | 2003-04-30 |
| IL106580A (en) | 1998-02-08 |
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| Date | Code | Title | Description |
|---|---|---|---|
| TK9A | Rectifications: patents |
Free format text: MERZ + CO. GMBH & CO., ECKENHEIMER LANDSTRASSE 100-104, D-6000 FRANKFURT AM MAIN 1, DE, 19951128 |
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| PD9A | Change of patent owner |
Owner name: MERZ PHARMA GMBH & CO. KGAA,DE Effective date: 20021017 |
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| MK9A | Expiry of a patent |
Effective date: 20130804 |