ZA200410196B - Lasofoxifene tablet and its coating - Google Patents
Lasofoxifene tablet and its coating Download PDFInfo
- Publication number
- ZA200410196B ZA200410196B ZA200410196A ZA200410196A ZA200410196B ZA 200410196 B ZA200410196 B ZA 200410196B ZA 200410196 A ZA200410196 A ZA 200410196A ZA 200410196 A ZA200410196 A ZA 200410196A ZA 200410196 B ZA200410196 B ZA 200410196B
- Authority
- ZA
- South Africa
- Prior art keywords
- phenyl
- cellulose
- sodium
- cis
- tetrahydronaphthalen
- Prior art date
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- GXESHMAMLJKROZ-IAPPQJPRSA-N lasofoxifene Chemical compound C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 GXESHMAMLJKROZ-IAPPQJPRSA-N 0.000 title claims description 7
- 239000011248 coating agent Substances 0.000 title description 4
- 238000000576 coating method Methods 0.000 title description 4
- 229960002367 lasofoxifene Drugs 0.000 title description 3
- 239000000203 mixture Substances 0.000 claims description 27
- 150000001875 compounds Chemical class 0.000 claims description 20
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 18
- 239000000651 prodrug Substances 0.000 claims description 18
- 229940002612 prodrug Drugs 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 11
- 239000003085 diluting agent Substances 0.000 claims description 10
- 239000000377 silicon dioxide Substances 0.000 claims description 9
- 235000012239 silicon dioxide Nutrition 0.000 claims description 9
- 239000012453 solvate Substances 0.000 claims description 9
- 239000007884 disintegrant Substances 0.000 claims description 8
- 239000000314 lubricant Substances 0.000 claims description 8
- 239000000945 filler Substances 0.000 claims description 5
- 239000002775 capsule Substances 0.000 claims description 4
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 8
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 5
- 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 5
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 5
- 239000008108 microcrystalline cellulose Substances 0.000 claims 5
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 5
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 4
- 239000001913 cellulose Substances 0.000 claims 4
- 229960001681 croscarmellose sodium Drugs 0.000 claims 4
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 4
- 239000008101 lactose Substances 0.000 claims 4
- 235000019359 magnesium stearate Nutrition 0.000 claims 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 229920000881 Modified starch Polymers 0.000 claims 2
- 229920002472 Starch Polymers 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
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims 2
- 235000010980 cellulose Nutrition 0.000 claims 2
- 229920002678 cellulose Polymers 0.000 claims 2
- 239000008121 dextrose Substances 0.000 claims 2
- 235000019814 powdered cellulose Nutrition 0.000 claims 2
- 229920003124 powdered cellulose Polymers 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- 229940032147 starch Drugs 0.000 claims 2
- 239000000454 talc Substances 0.000 claims 2
- 229910052623 talc Inorganic materials 0.000 claims 2
- 229940033134 talc Drugs 0.000 claims 2
- 235000012222 talc Nutrition 0.000 claims 2
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- 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 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- 239000004375 Dextrin Substances 0.000 claims 1
- 229920001353 Dextrin Polymers 0.000 claims 1
- 239000005913 Maltodextrin Substances 0.000 claims 1
- 229920002774 Maltodextrin Polymers 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 229960003563 calcium carbonate Drugs 0.000 claims 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- 235000013539 calcium stearate Nutrition 0.000 claims 1
- 239000008116 calcium stearate Substances 0.000 claims 1
- 229940078456 calcium stearate Drugs 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 229960002086 dextran Drugs 0.000 claims 1
- 229940096516 dextrates Drugs 0.000 claims 1
- 235000019425 dextrin Nutrition 0.000 claims 1
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 1
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
- 229960001031 glucose Drugs 0.000 claims 1
- 229940075507 glyceryl monostearate Drugs 0.000 claims 1
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims 1
- 229940046813 glyceryl palmitostearate Drugs 0.000 claims 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 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 1
- FEWJPZIEWOKRBE-LWMBPPNESA-N levotartaric acid Chemical class OC(=O)[C@@H](O)[C@H](O)C(O)=O FEWJPZIEWOKRBE-LWMBPPNESA-N 0.000 claims 1
- -1 light mineral oil Chemical compound 0.000 claims 1
- 229940059904 light mineral oil Drugs 0.000 claims 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims 1
- 239000001095 magnesium carbonate Substances 0.000 claims 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims 1
- 239000000395 magnesium oxide Substances 0.000 claims 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims 1
- 229940035034 maltodextrin Drugs 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 235000010446 mineral oil Nutrition 0.000 claims 1
- 239000002480 mineral oil Substances 0.000 claims 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 claims 1
- 229960000540 polacrilin potassium Drugs 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- WVWZXTJUCNEUAE-UHFFFAOYSA-M potassium;1,2-bis(ethenyl)benzene;2-methylprop-2-enoate Chemical compound [K+].CC(=C)C([O-])=O.C=CC1=CC=CC=C1C=C WVWZXTJUCNEUAE-UHFFFAOYSA-M 0.000 claims 1
- 235000010413 sodium alginate Nutrition 0.000 claims 1
- 239000000661 sodium alginate Substances 0.000 claims 1
- 229940005550 sodium alginate Drugs 0.000 claims 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims 1
- 235000010234 sodium benzoate Nutrition 0.000 claims 1
- 239000004299 sodium benzoate Substances 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 239000008109 sodium starch glycolate Substances 0.000 claims 1
- 229920003109 sodium starch glycolate Polymers 0.000 claims 1
- 229940079832 sodium starch glycolate Drugs 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 229960004274 stearic acid Drugs 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 235000019731 tricalcium phosphate Nutrition 0.000 claims 1
- 239000000811 xylitol Substances 0.000 claims 1
- 235000010447 xylitol Nutrition 0.000 claims 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 1
- 229960002675 xylitol Drugs 0.000 claims 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims 1
- 229940057977 zinc stearate Drugs 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 description 31
- 239000002552 dosage form Substances 0.000 description 13
- 238000004519 manufacturing process Methods 0.000 description 13
- 238000000034 method Methods 0.000 description 13
- 238000002156 mixing Methods 0.000 description 8
- 229940095743 selective estrogen receptor modulator Drugs 0.000 description 7
- 239000000333 selective estrogen receptor modulator Substances 0.000 description 7
- 239000003814 drug Substances 0.000 description 6
- 239000002184 metal Substances 0.000 description 6
- 239000002245 particle Substances 0.000 description 6
- 238000009472 formulation Methods 0.000 description 5
- 238000001035 drying Methods 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 230000003647 oxidation Effects 0.000 description 4
- 238000007254 oxidation reaction Methods 0.000 description 4
- 230000003389 potentiating effect Effects 0.000 description 4
- 238000005550 wet granulation Methods 0.000 description 4
- 239000003086 colorant Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 229940126534 drug product Drugs 0.000 description 3
- 238000007908 dry granulation Methods 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000003605 opacifier Substances 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 239000000825 pharmaceutical preparation Substances 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- JWQYZECMEPOAPF-UHFFFAOYSA-N 1,2,3,4-tetrahydronaphthalen-2-ol Chemical class C1=CC=C2CC(O)CCC2=C1 JWQYZECMEPOAPF-UHFFFAOYSA-N 0.000 description 2
- 230000001680 brushing effect Effects 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 238000009826 distribution Methods 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 238000009513 drug distribution Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 2
- 239000004014 plasticizer Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 238000009827 uniform distribution Methods 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 201000009273 Endometriosis Diseases 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000025844 Prostatic disease Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 230000001174 ascending effect Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 239000000356 contaminant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000009828 non-uniform distribution Methods 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 150000002978 peroxides Chemical class 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229960004622 raloxifene Drugs 0.000 description 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 description 1
- 238000005204 segregation Methods 0.000 description 1
- 238000013207 serial dilution Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Classifications
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- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
-
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- 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
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—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
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39509002P | 2002-07-10 | 2002-07-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200410196B true ZA200410196B (en) | 2006-07-26 |
Family
ID=30115812
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| ZA200410196A ZA200410196B (en) | 2002-07-10 | 2004-12-17 | Lasofoxifene tablet and its coating |
Country Status (36)
| Country | Link |
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| US (2) | US20040057992A1 (es) |
| EP (1) | EP1534248B1 (es) |
| JP (2) | JP4446446B2 (es) |
| KR (1) | KR100782693B1 (es) |
| CN (1) | CN100344278C (es) |
| AP (1) | AP2005003201A0 (es) |
| AR (1) | AR040434A1 (es) |
| AT (1) | ATE550017T1 (es) |
| AU (1) | AU2003247017B2 (es) |
| BR (1) | BR0312563A (es) |
| CA (1) | CA2489407C (es) |
| CY (1) | CY1112892T1 (es) |
| DK (1) | DK1534248T3 (es) |
| EA (1) | EA007268B1 (es) |
| EC (1) | ECSP055528A (es) |
| ES (1) | ES2395123T3 (es) |
| HK (1) | HK1077747A1 (es) |
| HN (1) | HN2003000206A (es) |
| HR (1) | HRP20041196A2 (es) |
| IL (2) | IL165746A0 (es) |
| IS (1) | IS7594A (es) |
| MA (1) | MA27318A1 (es) |
| MX (1) | MXPA05000394A (es) |
| NO (1) | NO20050018L (es) |
| NZ (1) | NZ537278A (es) |
| OA (1) | OA12883A (es) |
| PA (1) | PA8576201A1 (es) |
| PE (1) | PE20040104A1 (es) |
| PL (1) | PL374913A1 (es) |
| PT (1) | PT1534248E (es) |
| SI (1) | SI1534248T1 (es) |
| TN (1) | TNSN05006A1 (es) |
| TW (1) | TW200406222A (es) |
| UY (1) | UY27886A1 (es) |
| WO (1) | WO2004006895A1 (es) |
| ZA (1) | ZA200410196B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8576201A1 (es) * | 2002-07-10 | 2004-05-26 | Pfizer Prod Inc | Composicion farmaceutica que tiene una distribucion y potencia uniforme de farmaco |
| US20050271717A1 (en) * | 2003-06-12 | 2005-12-08 | Alfred Berchielli | Pharmaceutical compositions of atorvastatin |
| US20040253305A1 (en) * | 2003-06-12 | 2004-12-16 | Luner Paul E. | Pharmaceutical compositions of atorvastatin |
| EP1871359A1 (en) * | 2005-04-07 | 2008-01-02 | Miso Sabovic | Delaying the ageing process and disorders caused by ageing |
| WO2006118137A1 (ja) * | 2005-04-26 | 2006-11-09 | Dainippon Sumitomo Pharma Co., Ltd. | ビグアナイド系薬物を含有する粒状製剤 |
| GB0516604D0 (en) * | 2005-08-12 | 2005-09-21 | Sandoz Ag | Rapidly dispersing/disintegrating compositions |
| CA2833706C (en) | 2005-11-11 | 2014-10-21 | Boehringer Ingelheim International Gmbh | Quinazoline derivatives for the treatment of cancer diseases |
| US9891239B2 (en) | 2007-02-23 | 2018-02-13 | Gilead Sciences, Inc. | Modulators of pharmacokinetic properties of therapeutics |
| CA2587805C (en) * | 2007-04-25 | 2014-02-18 | The Procter & Gamble Company | Improved vitamin d content uniformity in pharmaceutical dosage forms |
| US20100055180A1 (en) * | 2007-10-10 | 2010-03-04 | Mallinckrodt Baker, Inc. | Directly Compressible Granular Microcrystalline Cellulose Based Excipient, Manufacturing Process and Use Thereof |
| CA2702055C (en) * | 2007-10-10 | 2017-12-12 | Mallinckrodt Baker, Inc. | Directly compressible high functionality granular microcrystalline cellulose based excipient, manufacturing process and use thereof |
| WO2009135067A1 (en) * | 2008-05-01 | 2009-11-05 | Wyeth | Pharmaceutical polish formulations |
| US10039718B2 (en) * | 2008-05-02 | 2018-08-07 | Gilead Sciences, Inc. | Use of solid carrier particles to improve the processability of a pharmaceutical agent |
| SI2451445T1 (sl) | 2009-07-06 | 2019-07-31 | Boehringer Ingelheim International Gmbh | Postopek za sušenje BIBW2992, njegovih soli in trdnih farmacevtskih formulacij, ki obsegajo to aktivno sestavino |
| PT2753306T (pt) * | 2011-10-17 | 2020-11-11 | Lexicon Pharmaceuticals Inc | Formas de dosagem sólidas de 2-amino-3-(4-(2-amino-6-((r)-1- (4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2- trifluoroetoxi)pirimidin-4-il)fenil)propanoato de (s)-etilo |
| DK2851075T3 (da) | 2012-05-14 | 2022-01-31 | Shionogi & Co | Præparat, der indeholder 6,7-umættet -7-carbamoylmorphinanderivat |
| EP3043778B1 (en) * | 2013-09-13 | 2017-09-06 | Bayer Pharma Aktiengesellschaft | Pharmaceutical compositions containing refametinib |
| RU2539375C1 (ru) * | 2013-11-07 | 2015-01-20 | Общество С Ограниченной Ответственностью "Валента-Интеллект" | Фармацевтическая композиция в форме таблетки и способ ее получения |
| US9242965B2 (en) | 2013-12-31 | 2016-01-26 | Boehringer Ingelheim International Gmbh | Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors |
| CN103830196A (zh) * | 2014-03-14 | 2014-06-04 | 王志刚 | 一种酒石酸拉索昔芬分散片及其制备方法 |
| TWI535784B (zh) | 2014-08-26 | 2016-06-01 | 財團法人工業技術研究院 | 剪切增稠配方、及包含其之複合材料 |
| CN105434444B (zh) * | 2014-09-29 | 2021-02-05 | 上海奥奇医药科技有限公司 | 一种A-失碳-5α雄甾烷化合物的口服制剂 |
| PE20200478A1 (es) * | 2016-07-25 | 2020-03-03 | Canopy Growth Corp | Nuevas formulaciones y composiciones de cannabis en comprimidos y metodos para su elaboracion |
| ES2909576T3 (es) | 2016-10-11 | 2022-05-09 | Univ Duke | Tratamiento con lasofoxifeno del cáncer de mama ER+ |
| CN112261937B (zh) | 2018-04-10 | 2023-11-14 | 杜克大学 | 乳腺癌的拉索昔芬治疗 |
| CN114288258A (zh) * | 2022-02-18 | 2022-04-08 | 山东新时代药业有限公司 | 一种单硝酸异山梨酯片及其制备方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4182A (en) * | 1845-09-09 | Island | ||
| US4880636A (en) * | 1988-05-13 | 1989-11-14 | Franz Robert M | Film coated tablet of ranitidine HCl |
| US5552412A (en) * | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
| UA51676C2 (uk) * | 1995-11-02 | 2002-12-16 | Пфайзер Інк. | (-)цис-6(s)-феніл-5(r)[4-(2-піролідин-1-ілетокси)феніл]-5,6,7,8-тетрагідронафталін-2-ол d-тартрат, спосіб його одержання, спосіб лікування захворювань, що піддаються лікуванню агоністами естрогену, та фармацевтична композиція |
| TW442286B (en) * | 1996-02-28 | 2001-06-23 | Pfizer | New therapeutic uses of estrogen agonists |
| US6372457B1 (en) | 1997-01-14 | 2002-04-16 | Arkion Life Sciences Llc | Process and materials for production of glucosamine |
| KR200161927Y1 (ko) * | 1997-08-26 | 1999-12-01 | 윤종용 | 냉장고 |
| YU26700A (sh) * | 1999-05-24 | 2002-06-19 | Pfizer Products Inc. | Postupak za cis-1-(2-(4-(6-metoksi-2-fenil-1,2,3,4- tetrahidronaftalen-1-il)fenoksi)etil)pirolidin |
| US6436977B1 (en) * | 1999-09-29 | 2002-08-20 | Pfizer Inc. | Dosing regimens for lasofoxifene |
| US6419956B1 (en) * | 1999-12-30 | 2002-07-16 | Ancile Pharmaceuticals | Odor-masking coating for a pharmaceutical preparation |
| EP1145719A3 (en) * | 2000-03-10 | 2001-11-14 | Pfizer Products Inc. | Use a ferrous salt for inhibiting oxidative degradation of pharmaceutical formulations |
| AR029538A1 (es) * | 2000-07-06 | 2003-07-02 | Wyeth Corp | Composiciones farmaceuticas de agentes estrogenicos |
| CZ20032959A3 (cs) * | 2001-05-01 | 2004-01-14 | Pfizer Products Inc. | Způsob přípravy farmaceutické kompozice s nízkou dávkou léčiva mající rovnoměrnou distribuci a účinnost léčiva |
| PA8576201A1 (es) * | 2002-07-10 | 2004-05-26 | Pfizer Prod Inc | Composicion farmaceutica que tiene una distribucion y potencia uniforme de farmaco |
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2003
- 2003-06-23 PA PA20038576201A patent/PA8576201A1/es unknown
- 2003-06-30 PL PL03374913A patent/PL374913A1/xx not_active Application Discontinuation
- 2003-06-30 BR BR0312563-7A patent/BR0312563A/pt not_active IP Right Cessation
- 2003-06-30 PT PT03764059T patent/PT1534248E/pt unknown
- 2003-06-30 CN CNB038162881A patent/CN100344278C/zh not_active Expired - Fee Related
- 2003-06-30 CA CA002489407A patent/CA2489407C/en not_active Expired - Fee Related
- 2003-06-30 KR KR1020057000369A patent/KR100782693B1/ko active IP Right Grant
- 2003-06-30 EA EA200401583A patent/EA007268B1/ru not_active IP Right Cessation
- 2003-06-30 AT AT03764059T patent/ATE550017T1/de active
- 2003-06-30 NZ NZ537278A patent/NZ537278A/en unknown
- 2003-06-30 WO PCT/IB2003/003074 patent/WO2004006895A1/en not_active Application Discontinuation
- 2003-06-30 AP AP2005003201A patent/AP2005003201A0/xx unknown
- 2003-06-30 IL IL16574603A patent/IL165746A0/xx unknown
- 2003-06-30 MX MXPA05000394A patent/MXPA05000394A/es active IP Right Grant
- 2003-06-30 AU AU2003247017A patent/AU2003247017B2/en not_active Ceased
- 2003-06-30 ES ES03764059T patent/ES2395123T3/es not_active Expired - Lifetime
- 2003-06-30 EP EP03764059A patent/EP1534248B1/en not_active Expired - Lifetime
- 2003-06-30 DK DK03764059.6T patent/DK1534248T3/da active
- 2003-06-30 OA OA1200500007A patent/OA12883A/en unknown
- 2003-06-30 JP JP2004521001A patent/JP4446446B2/ja not_active Expired - Fee Related
- 2003-06-30 SI SI200332150T patent/SI1534248T1/sl unknown
- 2003-07-01 US US10/612,679 patent/US20040057992A1/en not_active Abandoned
- 2003-07-04 TW TW092118389A patent/TW200406222A/zh unknown
- 2003-07-07 HN HN2003000206A patent/HN2003000206A/es unknown
- 2003-07-07 PE PE2003000682A patent/PE20040104A1/es not_active Application Discontinuation
- 2003-07-08 UY UY27886A patent/UY27886A1/es not_active Application Discontinuation
- 2003-07-08 AR AR20030102454A patent/AR040434A1/es not_active Application Discontinuation
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2004
- 2004-12-13 IL IL165746A patent/IL165746A/en active IP Right Grant
- 2004-12-13 IS IS7594A patent/IS7594A/is unknown
- 2004-12-17 HR HR20041196A patent/HRP20041196A2/hr not_active Application Discontinuation
- 2004-12-17 ZA ZA200410196A patent/ZA200410196B/en unknown
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2005
- 2005-01-03 NO NO20050018A patent/NO20050018L/no not_active Application Discontinuation
- 2005-01-10 TN TNP2005000006A patent/TNSN05006A1/fr unknown
- 2005-01-10 MA MA28036A patent/MA27318A1/fr unknown
- 2005-01-10 EC EC2005005528A patent/ECSP055528A/es unknown
- 2005-11-04 HK HK05109850A patent/HK1077747A1/xx not_active IP Right Cessation
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2006
- 2006-11-09 JP JP2006303440A patent/JP2007031451A/ja active Pending
- 2006-12-22 US US11/615,511 patent/US7553500B2/en not_active Expired - Fee Related
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2012
- 2012-06-06 CY CY20121100504T patent/CY1112892T1/el unknown
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