NZ535455A - Controlled release dosage forms - Google Patents
Controlled release dosage formsInfo
- Publication number
- NZ535455A NZ535455A NZ535455A NZ53545503A NZ535455A NZ 535455 A NZ535455 A NZ 535455A NZ 535455 A NZ535455 A NZ 535455A NZ 53545503 A NZ53545503 A NZ 53545503A NZ 535455 A NZ535455 A NZ 535455A
- Authority
- NZ
- New Zealand
- Prior art keywords
- controlled release
- dosage form
- oral dosage
- release oral
- agent
- Prior art date
Links
- 238000013270 controlled release Methods 0.000 title claims abstract description 84
- 239000002552 dosage form Substances 0.000 title description 16
- 238000000576 coating method Methods 0.000 claims abstract description 63
- 239000008199 coating composition Substances 0.000 claims abstract description 48
- 239000011248 coating agent Substances 0.000 claims abstract description 47
- 239000006186 oral dosage form Substances 0.000 claims abstract description 45
- 239000006185 dispersion Substances 0.000 claims abstract description 28
- 229920001577 copolymer Polymers 0.000 claims abstract description 25
- 239000013543 active substance Substances 0.000 claims abstract description 24
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 24
- 238000000034 method Methods 0.000 claims abstract description 23
- 230000007935 neutral effect Effects 0.000 claims abstract description 19
- 229920000151 polyglycol Polymers 0.000 claims abstract description 19
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- 125000000524 functional group Chemical group 0.000 claims abstract description 15
- 238000002844 melting Methods 0.000 claims abstract description 15
- 230000008018 melting Effects 0.000 claims abstract description 15
- 230000008569 process Effects 0.000 claims abstract description 6
- 239000000203 mixture Substances 0.000 claims description 42
- 239000003795 chemical substances by application Substances 0.000 claims description 34
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 28
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims description 26
- 229960003105 metformin Drugs 0.000 claims description 24
- 239000000314 lubricant Substances 0.000 claims description 23
- 238000004090 dissolution Methods 0.000 claims description 22
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- 239000002202 Polyethylene glycol Substances 0.000 claims description 16
- -1 polyoxyethylene Polymers 0.000 claims description 16
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
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- 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 12
- 239000002518 antifoaming agent Substances 0.000 claims description 11
- TVYLLZQTGLZFBW-ZBFHGGJFSA-N (R,R)-tramadol Chemical compound COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-ZBFHGGJFSA-N 0.000 claims description 9
- 239000003085 diluting agent Substances 0.000 claims description 9
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 claims description 9
- 229940083037 simethicone Drugs 0.000 claims description 9
- 229960004380 tramadol Drugs 0.000 claims description 9
- TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 claims description 9
- 239000004353 Polyethylene glycol 8000 Substances 0.000 claims description 8
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- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims description 7
- 239000003911 antiadherent Substances 0.000 claims description 7
- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 6
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims description 6
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 5
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
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- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 4
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 4
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 4
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical group Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims description 4
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- 150000003839 salts Chemical class 0.000 claims description 4
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 3
- 239000001361 adipic acid Substances 0.000 claims description 3
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- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 3
- 235000013539 calcium stearate Nutrition 0.000 claims description 3
- 239000008116 calcium stearate Substances 0.000 claims description 3
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- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 3
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- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims description 3
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims description 3
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- 239000008363 phosphate buffer Substances 0.000 claims description 3
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 3
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- 239000004299 sodium benzoate Substances 0.000 claims description 3
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- 229920002517 Poloxamer 338 Polymers 0.000 claims description 2
- 150000005215 alkyl ethers Chemical class 0.000 claims description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 2
- 229910052782 aluminium Inorganic materials 0.000 claims description 2
- 229920003086 cellulose ether Polymers 0.000 claims description 2
- 235000003599 food sweetener Nutrition 0.000 claims description 2
- 150000004676 glycans Chemical class 0.000 claims description 2
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- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 2
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- 239000002594 sorbent Substances 0.000 claims description 2
- 239000003765 sweetening agent Substances 0.000 claims description 2
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 claims 4
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 claims 4
- 229920000136 polysorbate Polymers 0.000 claims 3
- 229950008882 polysorbate Drugs 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- 229960004329 metformin hydrochloride Drugs 0.000 claims 2
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims 1
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
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- MPQPXMRGNQJXGO-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxamide Chemical compound NC(=O)CC(O)(C(N)=O)CC(N)=O MPQPXMRGNQJXGO-UHFFFAOYSA-N 0.000 description 5
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- 2003-02-21 US US10/370,109 patent/US7780987B2/en not_active Expired - Lifetime
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- 2003-02-21 WO PCT/US2003/004867 patent/WO2003072089A1/en not_active Ceased
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