CN1267087C - 药物片剂 - Google Patents
药物片剂 Download PDFInfo
- Publication number
- CN1267087C CN1267087C CNB038035804A CN03803580A CN1267087C CN 1267087 C CN1267087 C CN 1267087C CN B038035804 A CNB038035804 A CN B038035804A CN 03803580 A CN03803580 A CN 03803580A CN 1267087 C CN1267087 C CN 1267087C
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- China
- Prior art keywords
- tablet
- acid
- agent
- agents
- drug
- 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.)
- Expired - Fee Related
Links
- 239000003814 drug Substances 0.000 claims abstract description 78
- 229940079593 drug Drugs 0.000 claims abstract description 70
- 238000000576 coating method Methods 0.000 claims abstract description 38
- 239000011248 coating agent Substances 0.000 claims abstract description 37
- 229920002148 Gellan gum Polymers 0.000 claims abstract description 24
- 235000010492 gellan gum Nutrition 0.000 claims abstract description 23
- 239000000216 gellan gum Substances 0.000 claims abstract description 23
- 239000002245 particle Substances 0.000 claims abstract description 13
- 239000007787 solid Substances 0.000 claims abstract description 12
- 239000011159 matrix material Substances 0.000 claims abstract description 8
- -1 (S) -N- [ [3- [5- (3-pyridinyl) thiophen-2-yl ] -2-oxo-5-oxazolidinyl ] methyl ] acetamide hydrochloride Chemical compound 0.000 claims description 77
- 239000000203 mixture Substances 0.000 claims description 31
- 239000003795 chemical substances by application Substances 0.000 claims description 27
- 150000001875 compounds Chemical class 0.000 claims description 22
- 239000002253 acid Substances 0.000 claims description 20
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 16
- 239000011247 coating layer Substances 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims description 11
- 229960001680 ibuprofen Drugs 0.000 claims description 11
- 229910052760 oxygen Inorganic materials 0.000 claims description 11
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims description 11
- 239000003242 anti bacterial agent Substances 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 10
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 9
- 125000003545 alkoxy group Chemical group 0.000 claims description 9
- 229940111134 coxibs Drugs 0.000 claims description 9
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 9
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 229960000890 hydrocortisone Drugs 0.000 claims description 8
- 229960001797 methadone Drugs 0.000 claims description 8
- MITFXPHMIHQXPI-UHFFFAOYSA-N Oraflex Chemical compound N=1C2=CC(C(C(O)=O)C)=CC=C2OC=1C1=CC=C(Cl)C=C1 MITFXPHMIHQXPI-UHFFFAOYSA-N 0.000 claims description 7
- SNPPWIUOZRMYNY-UHFFFAOYSA-N bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 claims description 7
- 229960001058 bupropion Drugs 0.000 claims description 7
- RZEKVGVHFLEQIL-UHFFFAOYSA-N celecoxib Chemical compound C1=CC(C)=CC=C1C1=CC(C(F)(F)F)=NN1C1=CC=C(S(N)(=O)=O)C=C1 RZEKVGVHFLEQIL-UHFFFAOYSA-N 0.000 claims description 7
- 229960000590 celecoxib Drugs 0.000 claims description 7
- RZJQGNCSTQAWON-UHFFFAOYSA-N rofecoxib Chemical compound C1=CC(S(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)C(=O)OC1 RZJQGNCSTQAWON-UHFFFAOYSA-N 0.000 claims description 7
- 229960000371 rofecoxib Drugs 0.000 claims description 7
- 229940124597 therapeutic agent Drugs 0.000 claims description 7
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 claims description 6
- FZERHIULMFGESH-UHFFFAOYSA-N N-phenylacetamide Chemical compound CC(=O)NC1=CC=CC=C1 FZERHIULMFGESH-UHFFFAOYSA-N 0.000 claims description 6
- 239000002246 antineoplastic agent Substances 0.000 claims description 6
- 239000002221 antipyretic Substances 0.000 claims description 6
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims description 6
- MNJVRJDLRVPLFE-UHFFFAOYSA-N etoricoxib Chemical compound C1=NC(C)=CC=C1C1=NC=C(Cl)C=C1C1=CC=C(S(C)(=O)=O)C=C1 MNJVRJDLRVPLFE-UHFFFAOYSA-N 0.000 claims description 6
- 229960004945 etoricoxib Drugs 0.000 claims description 6
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 claims description 6
- 125000005843 halogen group Chemical group 0.000 claims description 6
- CPJSUEIXXCENMM-UHFFFAOYSA-N phenacetin Chemical compound CCOC1=CC=C(NC(C)=O)C=C1 CPJSUEIXXCENMM-UHFFFAOYSA-N 0.000 claims description 6
- ZQBAKBUEJOMQEX-UHFFFAOYSA-N phenyl salicylate Chemical compound OC1=CC=CC=C1C(=O)OC1=CC=CC=C1 ZQBAKBUEJOMQEX-UHFFFAOYSA-N 0.000 claims description 6
- 229960002895 phenylbutazone Drugs 0.000 claims description 6
- VYMDGNCVAMGZFE-UHFFFAOYSA-N phenylbutazonum Chemical compound O=C1C(CCCC)C(=O)N(C=2C=CC=CC=2)N1C1=CC=CC=C1 VYMDGNCVAMGZFE-UHFFFAOYSA-N 0.000 claims description 6
- IWELDVXSEVIIGI-UHFFFAOYSA-N piperazin-2-one Chemical compound O=C1CNCCN1 IWELDVXSEVIIGI-UHFFFAOYSA-N 0.000 claims description 6
- 230000005586 smoking cessation Effects 0.000 claims description 6
- LNPDTQAFDNKSHK-UHFFFAOYSA-N valdecoxib Chemical compound CC=1ON=C(C=2C=CC=CC=2)C=1C1=CC=C(S(N)(=O)=O)C=C1 LNPDTQAFDNKSHK-UHFFFAOYSA-N 0.000 claims description 6
- 229960002004 valdecoxib Drugs 0.000 claims description 6
- 230000004584 weight gain Effects 0.000 claims description 6
- 235000019786 weight gain Nutrition 0.000 claims description 6
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 5
- 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 5
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical group O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims description 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 5
- 201000001880 Sexual dysfunction Diseases 0.000 claims description 5
- 239000000730 antalgic agent Substances 0.000 claims description 5
- 229940125684 antimigraine agent Drugs 0.000 claims description 5
- 239000002282 antimigraine agent Substances 0.000 claims description 5
- 239000002876 beta blocker Substances 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 5
- 229960000991 ketoprofen Drugs 0.000 claims description 5
- 229960005489 paracetamol Drugs 0.000 claims description 5
- 229960004662 parecoxib Drugs 0.000 claims description 5
- TZRHLKRLEZJVIJ-UHFFFAOYSA-N parecoxib Chemical compound C1=CC(S(=O)(=O)NC(=O)CC)=CC=C1C1=C(C)ON=C1C1=CC=CC=C1 TZRHLKRLEZJVIJ-UHFFFAOYSA-N 0.000 claims description 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 5
- 229960003712 propranolol Drugs 0.000 claims description 5
- WVYADZUPLLSGPU-UHFFFAOYSA-N salsalate Chemical compound OC(=O)C1=CC=CC=C1OC(=O)C1=CC=CC=C1O WVYADZUPLLSGPU-UHFFFAOYSA-N 0.000 claims description 5
- 231100000872 sexual dysfunction Toxicity 0.000 claims description 5
- 229960004380 tramadol Drugs 0.000 claims description 5
- 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 5
- 229960005294 triamcinolone Drugs 0.000 claims description 5
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 claims description 5
- ZFKBWSREWJOSSJ-VIFPVBQESA-N (2s)-6,8-dichloro-2-(trifluoromethyl)-2h-chromene-3-carboxylic acid Chemical compound ClC1=CC(Cl)=C2O[C@H](C(F)(F)F)C(C(=O)O)=CC2=C1 ZFKBWSREWJOSSJ-VIFPVBQESA-N 0.000 claims description 4
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 claims description 4
- 201000004384 Alopecia Diseases 0.000 claims description 4
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 claims description 4
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims description 4
- VOXIUXZAOFEFBL-UHFFFAOYSA-N Voacangin Natural products CCC1CC2CN3CC1C(C2)(OC(=O)C)c4[nH]c5ccc(OC)cc5c4C3 VOXIUXZAOFEFBL-UHFFFAOYSA-N 0.000 claims description 4
- 229960001413 acetanilide Drugs 0.000 claims description 4
- 230000000202 analgesic effect Effects 0.000 claims description 4
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 4
- 230000001754 anti-pyretic effect Effects 0.000 claims description 4
- 239000003146 anticoagulant agent Substances 0.000 claims description 4
- 239000002220 antihypertensive agent Substances 0.000 claims description 4
- 239000000164 antipsychotic agent Substances 0.000 claims description 4
- NPAKNKYSJIDKMW-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=NC3=CC=C[CH]C3=C12 NPAKNKYSJIDKMW-UHFFFAOYSA-N 0.000 claims description 4
- 229960004195 carvedilol Drugs 0.000 claims description 4
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 claims description 4
- 239000000812 cholinergic antagonist Substances 0.000 claims description 4
- JQVDAXLFBXTEQA-UHFFFAOYSA-N dibutylamine Chemical compound CCCCNCCCC JQVDAXLFBXTEQA-UHFFFAOYSA-N 0.000 claims description 4
- 229960000616 diflunisal Drugs 0.000 claims description 4
- HUPFGZXOMWLGNK-UHFFFAOYSA-N diflunisal Chemical compound C1=C(O)C(C(=O)O)=CC(C=2C(=CC(F)=CC=2)F)=C1 HUPFGZXOMWLGNK-UHFFFAOYSA-N 0.000 claims description 4
- 229960000920 dihydrocodeine Drugs 0.000 claims description 4
- RBOXVHNMENFORY-DNJOTXNNSA-N dihydrocodeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC RBOXVHNMENFORY-DNJOTXNNSA-N 0.000 claims description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 4
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims description 4
- 239000003172 expectorant agent Substances 0.000 claims description 4
- 229960004369 flufenamic acid Drugs 0.000 claims description 4
- LPEPZBJOKDYZAD-UHFFFAOYSA-N flufenamic acid Chemical compound OC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 LPEPZBJOKDYZAD-UHFFFAOYSA-N 0.000 claims description 4
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims description 4
- HSIBGVUMFOSJPD-CFDPKNGZSA-N ibogaine Chemical compound N1([C@@H]2[C@H]3C[C@H](C1)C[C@@H]2CC)CCC1=C3NC2=CC=C(OC)C=C12 HSIBGVUMFOSJPD-CFDPKNGZSA-N 0.000 claims description 4
- OLOCMRXSJQJJPL-UHFFFAOYSA-N ibogaine Natural products CCC1CC2CC3C1N(C2)C=Cc4c3[nH]c5ccc(OC)cc45 OLOCMRXSJQJJPL-UHFFFAOYSA-N 0.000 claims description 4
- AREITJMUSRHSBK-UHFFFAOYSA-N ibogamine Natural products CCC1CC2C3CC1CN2CCc4c3[nH]c5ccccc45 AREITJMUSRHSBK-UHFFFAOYSA-N 0.000 claims description 4
- 229960000905 indomethacin Drugs 0.000 claims description 4
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 claims description 4
- 229960003907 linezolid Drugs 0.000 claims description 4
- TYZROVQLWOKYKF-ZDUSSCGKSA-N linezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCOCC1 TYZROVQLWOKYKF-ZDUSSCGKSA-N 0.000 claims description 4
- 238000002483 medication Methods 0.000 claims description 4
- 229960002237 metoprolol Drugs 0.000 claims description 4
- IUBSYMUCCVWXPE-UHFFFAOYSA-N metoprolol Chemical compound COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 IUBSYMUCCVWXPE-UHFFFAOYSA-N 0.000 claims description 4
- 229960002715 nicotine Drugs 0.000 claims description 4
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 229960000482 pethidine Drugs 0.000 claims description 4
- RGZSQWQPBWRIAQ-CABCVRRESA-N (-)-alpha-Bisabolol Chemical compound CC(C)=CCC[C@](C)(O)[C@H]1CCC(C)=CC1 RGZSQWQPBWRIAQ-CABCVRRESA-N 0.000 claims description 3
- SSEBTPPFLLCUMN-CYBMUJFWSA-N (1r)-2-(tert-butylamino)-1-(7-ethyl-1-benzofuran-2-yl)ethanol Chemical compound CCC1=CC=CC2=C1OC([C@H](O)CNC(C)(C)C)=C2 SSEBTPPFLLCUMN-CYBMUJFWSA-N 0.000 claims description 3
- 239000001500 (2R)-6-methyl-2-[(1R)-4-methyl-1-cyclohex-3-enyl]hept-5-en-2-ol Substances 0.000 claims description 3
- NXQMNKUGGYNLBY-GFCCVEGCSA-N (2r)-1-(3-methylphenoxy)-3-(propan-2-ylamino)propan-2-ol Chemical compound CC(C)NC[C@@H](O)COC1=CC=CC(C)=C1 NXQMNKUGGYNLBY-GFCCVEGCSA-N 0.000 claims description 3
- METKIMKYRPQLGS-GFCCVEGCSA-N (R)-atenolol Chemical compound CC(C)NC[C@@H](O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-GFCCVEGCSA-N 0.000 claims description 3
- 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 claims description 3
- XILVEPYQJIOVNB-UHFFFAOYSA-N 2-[3-(trifluoromethyl)anilino]benzoic acid 2-(2-hydroxyethoxy)ethyl ester Chemical compound OCCOCCOC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 XILVEPYQJIOVNB-UHFFFAOYSA-N 0.000 claims description 3
- SGUAFYQXFOLMHL-UHFFFAOYSA-N 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide Chemical compound C=1C=C(O)C(C(N)=O)=CC=1C(O)CNC(C)CCC1=CC=CC=C1 SGUAFYQXFOLMHL-UHFFFAOYSA-N 0.000 claims description 3
- YTRMTPPVNRALON-UHFFFAOYSA-N 2-phenyl-4-quinolinecarboxylic acid Chemical compound N=1C2=CC=CC=C2C(C(=O)O)=CC=1C1=CC=CC=C1 YTRMTPPVNRALON-UHFFFAOYSA-N 0.000 claims description 3
- IYNWSQDZXMGGGI-NUEKZKHPSA-N 3-hydroxymorphinan Chemical compound C1CCC[C@H]2[C@H]3CC4=CC=C(O)C=C4[C@]21CCN3 IYNWSQDZXMGGGI-NUEKZKHPSA-N 0.000 claims description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 3
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- NPBVQXIMTZKSBA-UHFFFAOYSA-N Chavibetol Natural products COC1=CC=C(CC=C)C=C1O NPBVQXIMTZKSBA-UHFFFAOYSA-N 0.000 claims description 3
- OIRAEJWYWSAQNG-UHFFFAOYSA-N Clidanac Chemical compound ClC=1C=C2C(C(=O)O)CCC2=CC=1C1CCCCC1 OIRAEJWYWSAQNG-UHFFFAOYSA-N 0.000 claims description 3
- 239000005770 Eugenol Substances 0.000 claims description 3
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- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims description 3
- SBDNJUWAMKYJOX-UHFFFAOYSA-N Meclofenamic Acid Chemical compound CC1=CC=C(Cl)C(NC=2C(=CC=CC=2)C(O)=O)=C1Cl SBDNJUWAMKYJOX-UHFFFAOYSA-N 0.000 claims description 3
- BLXXJMDCKKHMKV-UHFFFAOYSA-N Nabumetone Chemical compound C1=C(CCC(C)=O)C=CC2=CC(OC)=CC=C21 BLXXJMDCKKHMKV-UHFFFAOYSA-N 0.000 claims description 3
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims description 3
- ONBWJWYUHXVEJS-ZTYRTETDSA-N Normorphine Chemical compound C([C@@H](NCC1)[C@@H]2C=C[C@@H]3O)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 ONBWJWYUHXVEJS-ZTYRTETDSA-N 0.000 claims description 3
- 239000008896 Opium Substances 0.000 claims description 3
- UVMRYBDEERADNV-UHFFFAOYSA-N Pseudoeugenol Natural products COC1=CC(C(C)=C)=CC=C1O UVMRYBDEERADNV-UHFFFAOYSA-N 0.000 claims description 3
- NGFMICBWJRZIBI-JZRPKSSGSA-N Salicin Natural products O([C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@H](CO)O1)c1c(CO)cccc1 NGFMICBWJRZIBI-JZRPKSSGSA-N 0.000 claims description 3
- 239000000695 adrenergic alpha-agonist Substances 0.000 claims description 3
- 125000000304 alkynyl group Chemical group 0.000 claims description 3
- 229960004663 alminoprofen Drugs 0.000 claims description 3
- FPHLBGOJWPEVME-UHFFFAOYSA-N alminoprofen Chemical compound OC(=O)C(C)C1=CC=C(NCC(C)=C)C=C1 FPHLBGOJWPEVME-UHFFFAOYSA-N 0.000 claims description 3
- 229960002133 almotriptan Drugs 0.000 claims description 3
- RGZSQWQPBWRIAQ-LSDHHAIUSA-N alpha-Bisabolol Natural products CC(C)=CCC[C@@](C)(O)[C@@H]1CCC(C)=CC1 RGZSQWQPBWRIAQ-LSDHHAIUSA-N 0.000 claims description 3
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Abstract
提供一种药物片剂,该片剂包括芯和粘附于芯的包衣层,其中(a)芯包括分散在基质中的水溶性染料的固体颗粒,和(b)包衣层包括胶凝糖胶。该片剂适用于经口或口内给药,例如用于传送片芯内含有的药物到患者。片剂具有斑点外观,从而使片剂能容易地被识别。
Description
技术领域
本发明涉及可口服的药物剂型,尤其是片剂。
背景技术
片剂是药物口服给药中最常见并且最方便的药物剂型。可通过外观包括大小、形状、表面结构、斑纹和颜色容易地识别是片剂重要的功能属性。这种易识别性在减少配药错误和使正服用多种药物的患者区分他们在不同时间或以不同频率服用的药物方面非常重要。目前大量药物被制成片剂,而这些药物中的多种以不同剂量浓度配制,因此任何新片剂具有独特的外观变得更重要但也更难于保证。
尤其是片剂配方设计师可用的易区分颜色的范围是相当有限的。已通过使用杂色、双色或多色片剂在一定程度上缓解了这个问题。但是,在本领域中仍需要具有独特表面色型的片剂。
在为包衣片剂时,颜色可为表面包衣层的属性。例如,一系列不透明色素可用于掺入到片剂包衣组合物如基于乙基纤维素的组合物中;这些色素往往赋予包衣片剂纯白色或有色外观。或者,表面包衣层可为光洁和透明的,包衣片剂的颜色由包衣层下面片芯的颜色控制。
Nivaggioli等人的美国专利US 6326028公开了包括胶凝糖胶(gellangum)的片剂包衣层,这里引入作为参考。这种包衣层据说能用于口服片剂,并能在外观、识别性、口感、减尘(reduced dust)、稳定性、颜色和/或吞服性方面带来益处。
国际专利公布WO01/10406公开了被认为可适用于柠檬酸西地那非的宽范围给药途径包括口腔和舌下途径的组合物,这里引入作为参考。公开的优选组合物据说包括溶液、凝胶、半固体、混悬液、计量剂量物(metereddose device)、透皮贴片或薄膜。此专利指出这种组合物可包括凝胶体系,例如胶凝糖胶0.5%-10%。
国际专利公布WO02/05820公开了包括柠檬酸西地那非的膜剂型,这里引入作为参考。通过将柠檬酸西地那非的固体分散体和水溶性糖与水胶体和任选的其它成分混合来制备这些剂型,当放在粘膜表面时,据说能形成随后崩解并溶解放出西地那非的包衣层。在被认为可用于这种薄膜剂型的水胶体中列举了胶凝糖胶钠盐。
Levin的美国专利US 6291506公开了可通过将眼用药卡维地洛悬浮到试剂如能提高角膜与药物接触时间的胶凝糖胶中来配制制剂用于眼给药。其中还考虑了其它可能的给药模式。权利要求包括通过选择给药途径包括舌下给药来给药的方法。
发明概述
本发明提供一种药物片剂,该片剂包括芯和粘附于芯的包衣层,其中(a)芯包括分散在基质中的水溶性染料的固体颗粒,和(b)包衣层包括胶凝糖胶。
该片剂尤其适用于经口或口内给药,例如,用于将片芯内含有的药物给药到患者如人类患者。这里的术语“经口”是指经由口给药,包括吞服片剂而片剂在口内没有大量的预先崩解,从而使药物的吸收一般发生在胃肠道内。这里的术语“口内”是指通过放置片剂在患者口中给药,片剂在口中崩解和/或溶解,从而使药物的吸收一般至少部分经由口腔粘膜发生。对于口内给药,可将片剂放入或放到口的任何一个部位上,但优选在舌下或口腔空间内放置片剂。
或者将片剂溶解或分散到液体介质中并作为饮剂吞服,介质优选水。
本发明的片剂具有与众不同的斑点(speckled)外观。不受理论约束,可认为在用包含胶凝糖胶的水溶性包衣组合物包衣芯的过程中,与包衣组合物接触的染料颗粒部分溶解,导致颜色“渗出”到每个这种颗粒所在处的包衣层上。当包衣层干燥时,颜色就变成固定的。得益于胶凝糖胶的高光洁表面结构使斑点图形更明显并使其更吸引人或更精致。这将在下文中更充分地描述,本发明片剂的斑点图形特征的多种变体是可能的并且是行得通的,这为正设法制备易识别片剂的配方设计师增加了新的选择。
作为另外的优点,本发明片剂的斑点图形能使有时因处理条件变化而产生的任何小的变色区域不明显。
本发明的其它特征、优点和益处将在随后的描述中显现。
发明详述
本发明的片剂可为安慰剂片剂,即在其芯中不含药物或其它活性剂。优选地,本发明的片剂在芯中含有治疗和/或预防有效量的药物,更优选地,通过经口或口内施用方便地给药。
例如,本发明片剂的芯中存在的药物可选自以下示例性种类:ACE抑制剂;α-肾上腺素能激动剂;β-肾上腺素能激动剂;αβ-肾上腺素能阻滞剂;β-肾上腺素能阻滞剂(β阻滞剂);醇抑制剂;醛醣还原酶抑制剂;醛固酮拮抗剂;氨基酸;同化剂(anabolics);镇痛药(麻醉药和非麻醉药);麻醉剂;减食欲药;抗酸剂;驱虫剂;抗粉刺剂(antiacne agent);抗过敏剂;抗雄性激素药;抗心绞痛药;抗不安药;抗心律失常药(antiarrythmics);平喘药;抗菌药和抗生素;抗脱发和抗秃顶药;抗变形虫药;抗体;抗胆碱能药;抗凝血剂和血液稀释剂(blood thinner);抗结肠炎药;抗惊厥药;抗膀胱炎药;抗抑郁药;抗糖尿病药;止泻药;抗利尿药;解毒药;止吐药;抗雌激素药;抗气胀药;抗真菌药;抗原;抗青光眼药;抗组胺药;抗机能亢进药(antihyperactive);抗高脂蛋白血症药;抗高血压药;抗甲状腺机能亢进药;抗低血压药;抗甲状腺机能减退药;抗感染药;抗炎药(甾族的和非甾族的);抗疟疾药;抗偏头痛药;抗肿瘤药;抗肥胖药;抗帕金森病药和抗运动障碍药;抗肺炎药;抗原虫药;抗痒药(antipruritics);抗牛皮癣药;抗精神病药;退热药;抗风湿药;抗分泌药;抗休克药;抗痉挛药;抗血栓形成药;抗癌药;镇咳药;抗溃疡药;抗病毒药;抗焦虑药;杀菌药;骨增密剂;支气管扩张药;钙通道阻滞剂;碳酸酐酶抑制剂;强心剂和心脏兴奋剂;化学治疗剂;利胆剂;类胆碱能药物;慢性疲劳综合症治疗药;CNS兴奋剂;促凝剂;避孕药;囊性纤维化治疗药;减充血剂;利尿剂;多巴胺受体激动剂;多巴胺受体拮抗剂;酶;雌激素;祛痰药;胃机能亢进治疗药;糖皮质激素;止血剂;HMG CoA还原酶抑制剂;激素;安眠药;免疫调节剂;免疫抑制剂;轻泻剂;口腔和牙周疾病用药;缩瞳药;单胺氧化酶抑制剂;粘液溶解剂;多发性硬化治疗药;肌肉松弛药;散瞳药;抗麻醉药;NMDA受体拮抗剂;寡核苷酸;眼用药;催产药;肽;多肽和蛋白质;多糖;孕激素;前列腺素;蛋白酶抑制剂;呼吸促进剂;镇静剂;五羟色胺摄取抑制剂;性激素(包括雄性激素);戒烟药;平滑肌松弛药;平滑肌兴奋剂;血栓溶解剂;安定药;尿酸化剂;尿失禁治疗药;血管扩张剂;血管保护剂;和它们的组合。
应认识到这里对具体药物化合物的任何引用都包括那种化合物的互变异构体、立体异构体、盐和前体药物,并且不特指药物的任何一种固态形式。
在一种实施方式中,片芯中含有的药物为戒烟药,例如烟碱、烟碱代谢物或有助于戒烟的非烟碱如丁氨苯丙酮(bupropion)或伊菠加因(ibogaine)。
例如,戒烟药可选自烟碱和其代谢物(如可铁宁、去甲可铁宁、降烟碱、烟碱N-氧化物、可铁宁N-氧化物、3-羟基可铁宁和5-羟基可铁宁)、伊菠加因、丁氨苯丙酮和它们的代谢物(如丁氨苯丙酮赤-和苏-氨基醇、丁氨苯丙酮赤氨基二醇和羟基丁氨苯丙酮)、洛贝林(lobeline)、司来吉兰(selegiline)、利培酮(risperidone)和其9-羟基代谢物、去甲司来吉兰、取代的吡啶衍生物(如1-[(6-氯-3-吡啶基)甲基]-2-咪唑烷、1-[(6-氯-3-吡啶基)甲基]-2-咪唑并噻唑和它们的类似物)、甲基莰基胺(methcamylamine)、去甲丙咪嗪(desipramine)、氟西汀、罗匹尼罗(ropinirole)、三甲噻方(trimethaphan)、右旋樟脑磺酸三甲噻方(trimethaphan camsylate)、多虑平(doxepin)、2-(3-氯代苯基)-3,5,5-三甲基-2-吗啉醇、抗焦虑药(如异戊酰胺)、γ-乙烯基GABA(GVG)、地棘蛙素(epibatidine)和其衍生物、7-氮杂双环-[2.2.1]-庚烷和-庚烯化合物、纳曲酮(naltrexone)、纳美芬(nalmefene)、氯胺酮(ketamine)、六甲双铵(hexamethonium)、血安定(pentolinium)、二氢-β-刺桐碱(erythroidine)、刺桐定、d-管箭毒碱、潘必啶(pempidine)、氯化氯异吲哚铵(chlorisondamine)、金刚烷(amantadine)胺、杂氧(hetero-oxy)链烷胺、亚苄基-和亚肉桂基-新烟碱、氮杂吲哚-乙胺衍生物、N-(吡啶基甲基)-亚杂环胺(heterocyclylideneamine)和NK-1受体拮抗剂(如9-溴-1,2,3,4,5,6-六氢-1,5-桥亚甲基-吡啶并[1,2-a][1,5]二氮芳辛-8-酮)。
在另一种实施方式中,片芯中含有的药物为抗菌药。例如这类药物可为抗生素,如氨基糖苷类(aminoglycoside)、霉素(amphenicol)、袢霉素(ansamycin)、碳青霉烯(carbapenem)、头孢菌素、头霉素、单酰胺菌素(monobactam)、氧头孢烯(oxacephem)、青霉素、林肯酰胺(lincosamide)、大环内酯、多肽或四环素;或合成的抗菌药,如2,4-二氨基嘧啶、硝基呋喃、噁唑烷酮、喹诺酮或其类似物、磺胺或砜。本发明中优选的抗菌药包括以下示例:丁胺卡那霉素、阿奇霉素(azithromycin)、头孢克肟(cefixime)、头孢哌酮(cefoperazone)、头孢噻肟(cefotaxime)、头孢噻甲羧肟(ceftazidime)、头孢三嗪(ceftriaxone)、氯霉素、环丙沙星、氯林霉素(clindamycin)、多粘菌素E(colistin)、domeclocycline、强力霉素、红霉素、庆大霉素、林可霉素(lincomycin)、利奈唑胺(linezolid)、磺胺米隆、甲烯土霉素、二甲胺四环素、新霉素、诺氟沙星、氧氟沙星、土霉素、吡利霉素(pirlimycin)、多粘菌素B、乙胺嘧啶、磺胺嘧啶银、磺胺醋酰(sulfacetamide)、磺胺异噁唑、四环素、妥布霉素、甲氧苄氨嘧啶和它们的组合。在一种实施方式中,片芯中存在的抗菌药为噁唑烷酮(oxazolidinone),例如选自(S)-N-[[3-[3-氟-4-[4-(羟乙酰基)-1-哌嗪基]苯基]-2-氧代-5-噁唑烷基]甲基]乙酰胺(依哌唑胺eperezolid))、(S)-N-[[3-[3-氟-4-[4-(吗啉基)苯基]-2-氧代-5-噁唑烷基]甲基]乙酰胺(利奈唑胺linezolid)、N-[(5S)-3-[3-氟-4-[4-(2-氟乙基)-3-氧代-1-哌嗪基]苯基-2-氧代-5-噁唑烷基]甲基]乙酰胺、(S)-N-[[3-[5-(3-吡啶基)噻吩-2-基]-2-氧代-5-噁唑烷基]甲基]乙酰胺和(S)-N-[[3-[5-(4-吡啶基)吡啶-2-基]-2-氧代-5-噁唑烷基]甲基]乙酰胺盐酸盐。
在另一种实施方式中,片芯中含有的药物为抗偏头痛药。例如这类药剂为烷基黄嘌呤(alkylxanthine),例如咖啡因;多巴胺D2受体激动剂,如阿吡必利(alpiropride)或麦角乙脲(lisuride);GABAA受体调节剂,如加奈索酮(ganaxolone);5-羟色胺(5-HT)受体激动剂,如阿莫曲坦(almotriptan)、依立曲坦(eletriptan)、氟伐曲坦(frovatriptan)、纳拉曲坦(naratriptan)、雷扎曲坦(rizatriptan)、舒马曲坦(sumatriptan)或佐米曲坦(zolmitriptan);麦角或其衍生物,如麦角胺或二氢麦角胺;或血管调节剂(vasomodulator),如多他利嗪(dotarizine)、二甲替嗪(fonazine)或洛美利嗪(lomerizine)。
在另一种实施方式中,片芯中含有的药物用于治疗或预防眼科疾病。
例如这类眼用药可为抗菌药,例如选自上面列出的那些种类。
或者或另外地,这类眼用药例如可为抗青光眼药或降眼压药,如(a)α-肾上腺素能激动剂或类交感神经药,如adrenolone、阿可乐定(apraclonidine)、溴莫尼定(brimonidine)或地匹福林(dipivefrin);(b)β-肾上腺素能阻滞剂,如醋丁洛尔、阿达洛尔(adaprolol)、烯丙洛尔(alprenolol)、阿替洛尔(atenolol)、倍他洛尔(betaxolol)、布非洛尔(bufetolol)、丁呋洛尔(bufuralol)、布尼洛尔(bunitrolol)、丁萘酮心安(bunolol)、布拉洛尔(bupranolol)、卡替洛尔(carteolol)、卡维洛尔(carvedilol)、西他洛尔(cetamolol)、右旋普萘洛尔(dexpropanolol)、拉贝洛尔(labetalol)、左布诺洛尔(levobunolol)、美替洛尔(metipranolol)、美托洛尔(metoprolol)、纳多洛尔(nadolol)、硝苯洛尔(nifenalol)、心得平(oxyprenolol)、环戊丁心安(penbutolol)、吲哚洛尔(pindolol)、心得宁(practolol)、萘心定(pronethalol)、普萘洛尔(propranolol)、索他洛尔(sotalol)、噻吗洛尔(timolol)、胺甲苯心安(tolamolol)、托利洛尔(toliprolol)或vaninolol;(c)碳酸酐酶抑制剂,如醋唑磺胺或多尔唑胺(dorzolamide);或(d)前列腺素或其类似物,如PGF2α类似物如比马前列素(bimatoprost)、适利达(latanoprost)、曲沃前列素(trayoprost)和乌诺前列酮异丙酯(unorpostone isopropyl)。
或者或另外地,这类眼用药可例如为缩瞳剂如卡巴可、毒扁豆碱或毛果芸香碱。
或者或另外地,这类眼用药可例如为抗炎药,如NSAID,更优选选择性COX-2抑制剂,例如选自上面列出的那些。
在另一实施方式中,片芯中含有的药物为止痛药、退热药或抗炎药,如醋氯酚酸(aceclofenac)、醋炎痛(acemetacin)、e-乙酰氨基己酸、扑热息痛(acetaminophen)、水杨酸对乙酰氨苯酯(acetaminosalol)、乙酰苯胺(acetanilide)、乙酰水杨酸(阿司匹林)、S-钴酰胺蛋氨酸(S-adenosylmethionine)、阿氯酚酸(alclofenac)、阿氯米松(alclometasone)、阿芬太尼(alfentanil)、阿尔孕酮(algestone)、烯丙苯哌啶(allylprodine)、阿明洛芬(alminoprofen)、阿洛普令(aloxiprin)、阿法罗定(alphaprodine)、双(乙酰水杨酸)铝、安西缩松(amcinonide)、氨芬酸(amfenac)、氨基氯噻噁嗪(aminochlorthenoxazin)、3-氨基-4-羟基丁酸、2-氨基-4-甲基吡啶、氨基普罗皮纶(aminopropylon)、氨基比林、阿米曲林(amixetrine)、水杨酸铵、安吡昔康(ampiroxicam)、呱氨托美丁(amtolmetin guacil)、阿尼利定(anileridine)、安替比林(antipyrine)、安拉非宁(antrafenine)、炎爽痛(apazone)、倍氯米松、苄吲酸、贝诺酯(benorylate)、苯噁洛芬、苄哌吡酮(benzpiperylon)、炎痛静(benzydamine)、苄吗啡(benzylmorphine)、贝尔洛芬(bermoprofen)、倍他米松(betamethasone)、苯晴米特(bezitramide)、α-没药醇(α-bisabolol)、溴芬酸(bromfenac)、对-溴乙酰苯胺、5-溴水杨酸乙酸酯、溴水杨醇(bromosaligenin)、丁西丁(bucetin)、氯环己苯酰丙酸(bucloxic acid)、布可龙(bucolome)、布地缩松(budesonide)、丁苯羟酸(bufexamac)、丁丙二苯肼(bumadizon)、丁丙诺啡(buprenorphine)、丁醋苯胺(butacetin)、布替布芬(butibufen)、布托啡诺(butophanol)、卡马西平(carbamazepine)、卡必芬(carbiphene)、卡布洛芬(carprofen)、卡沙兰(carsalam)、塞来昔布(celecoxib)、氯丁醇、氯泼尼松(chloroprednisone)、氯乙苯噁嗪酮(chlorthenoxazin)、水杨酸胆碱、辛可芬(cinchophen)、桂美辛(cinmetacin)、曲马朵(ciramadol)、环氯茚酸(clidanac)、氯倍他索(clobetasol)、氯可托龙(clocortolone)、氯美辛(clometacin)、氯尼他秦(clonitazene)、氯胺烟酸(clonixin)、氯苯吡咯酸(clopirac)、氯泼尼醇(cloprednol)、丁香、可待因(codeine)、可待因甲基溴、磷酸可待因、硫酸可待因、可的松(cortisone)、可的伐唑(cortivazol)、巴酰丙酰胺(cropropamide)、巴酰乙酰胺(crotethamide)、去氟可特(deflazacort)、二氢去氧吗啡(desomorphine)、丙缩羟强龙(desonide)、去羟米松(desoximetasone)、地塞米松(dexamethasone)、右旋二苯哌啶二噁烷(dexoxadrol)、吗散痛(dextromoramide)、地佐辛(dezocine)、双胺丙酰胺(diampromide)、双氯芬酸(diclofenac)、二苯酰胺吡唑(difenamizole)、联苯吡胺(difenpiramide)、二氟拉松(diflorasone)、二氟米松(diflucortolone)、双氟尼酸(diflunisal)、醋丁二氟龙(difluprednate)、二氢可待因、醋氢可待酮、二氢吗啡、乙酰水杨酸二氢铝、苯醋胺乙酯(dimenoxadol)、美沙醇(dimepheptanol)、二甲嗯丁胺(dimethylthiambutene)、吗苯丁酯(dioxaphetyl butyrate)、二苯哌己酮(dipipanone)、diprocetyl、安乃近(dipyrone)、双苯唑醇(ditazol)、哚昔康(droxicam)、依莫法宗(emorfazone)、苯乙氨茴酸(enfenamic acid)、甘草次酸(enoxolone)、嘧啶唑(epirizole)、依他佐辛(eptazocine)、依特柳酯(etersalate)、乙柳酰胺(ethenzamide)、依索庚嗪(ethoheptazine)、乙氧二氨偶氮苯(ethoxazene)、甲乙嗯丁胺(ethylmethylthiambutene)、乙基吗啡、依托度酸(etodolac)、依托非那酯(etofenamate)、依托尼秦(etonitazene)、依托昔布(etoricoxib)、丁香酚(eugenol)、联苯乙酸(felbinac)、芬布芬(fenbufen)、氯苯噻唑乙酸(fenclozic acid)、芬多沙(fendosal)、苯氧苯丙酸(fenoprofen)、芬太尼(fentanyl)、芬替酸(fentiazac)、非普地醇(fepradinol)、戊烯保泰松(feprazone)、氟喹氨苯酯(floctafenine)、氟噁米松(fluazacort)、氟二氯松(flucloronide)、氟灭酸(flufenamic acid)、二氟美松(flumethasone)、9-去氟肤轻松(flunisolide)、氟胺烟酸(flunixin)、氟诺洛芬(flunoxaprofen)、醋酸氟轻松(fluocinolone acetonide)、氟轻松(fluocinonide)、氟考丁酯(fluocortin butyl)、氟考龙(fluocortolone)、氟苯乙砜(fluoresone)、氟甲龙(fluorometholone)、氟培龙(fluperolone)、氟吡汀(flupirtine)、氟泼尼定(fluprednidene)、氟强的松龙(fluprednisolone)、氟丙喹宗(fluproquazone)、丙酮缩氟氢羟龙(flurandrenolide)、氟比洛芬(flurbiprofen)、醛基缩松(formocortal)、磷酸柳酯(fbsfosal)、龙胆酸(gentisic acid)、格拉非宁(glafenine)、葡卡美新(glucametacin)、水杨酸二醇酯、愈创兰油烃(guaiazulene)、氯氟松(halcinonide)、氯二氟美松(halometasone)、溴氟龙(haloprednone)、氢可酮(hydrocodone)、氢可松氨酯(hydrocortamate)、氢化可的松(hydrocortisone)、二氢吗啡酮(hydromorphone)、羟哌替啶(hydroxypethidine)、异丁苯乙酸(ibufenac)、布洛芬(ibuprofen)、布洛新(ibuproxam)、水杨酸咪唑、消炎痛(indomethacin)、吲哚洛芬(indoprofen)、三苯唑酸(isofezolac)、isoladol、异美沙酮(isomethadone)、异尼克辛(isonixin)、伊索克酸(isoxepac)、伊索昔康(isoxicam)、凯托米酮(ketobemidone)、酮洛芬(ketoprofen)、痛力克(ketorolac)、乳酰对异氧苯胺(p-lactophenetide)、利非他明(lefetamine)、羟甲左吗喃(levorphanol)、洛芬太尼(lofentanil)、氯苯唑酸(lonazolac)、氯诺昔康(lornoxicam)、洛索洛芬(loxoprofen)、赖氨酸阿司匹林、马泼尼酮(mazipredone)、甲氯灭酸(meclofenamic acid)、甲羟松(medrysone)、甲灭酸(mefenamic acid)、度冷丁(meperidine)、甲泼尼松(meprednisone)、哌替啶(meptazinol)、美沙拉明(mesalamine)、美他佐辛(metazocine)、美沙酮(methadone)、甲氧异丁嗪(methotrimeprazine)、甲基强的松龙(methylprednisolone)、甲噻吩嗪乙酸(metiazinic acid)、甲氧苯啉(metofoline)、甲基二氢吗啡酮(metopon)、布他酮(mofebutazone)、莫苯唑酸(mofezolac)、苯吗比林(morazone)、吗啡、盐酸吗啡、硫酸吗啡、水杨酸吗啉、麦罗啡(myrophine)、那布米酮(nabumetone)、纳布啡(nalbuphine)、水杨酸-l-萘酯、萘普生(naproxen)、那碎因(narceine)、平痛新(nefopam)、尼可吗啡(nicomorphine)、尼芬那宗(nifenazone)、尼氟灭酸(niflumic acid)、尼美舒利(nimesulide)、5’-硝基-2’-丙氧基乙酰苯胺、去甲左啡烷(norlevorphanol)、去甲美沙酮(normethadone)、去甲吗啡(normorphine)、诺匹哌酮(norpipanone)、偶氮水杨酸(olsalazine)、阿片(opium)、奥沙西罗(oxaceprol)、吲肟酸(oxametacine)、噁丙嗪(oxaprozin)、羟考酮(oxycodone)、羟吗啡酮(oxymorphone)、羟保泰松(oxyphenbutazone)、阿片全碱(papaveretum)、对氟米松(paramethasone)、胍苯叉芴(paranyline)、帕瑞昔布(parecoxib)、帕沙米特(parsalmide)、镇痛新(pentazocine)、哌立索唑(perisoxal)、非那西丁(phenacetin)、苯吗庚酮(phenadoxone)、非那佐辛(phenazocine)、盐酸非那吡啶(phenazopyridine)、非诺可(phenocoll)、苯哌利定(phenoperidine)、非诺吡酮(phenopyrazone)、乙酰水杨酸苯酯、苯基保泰松(phenylbutazone)、水杨酸苯酯、苯吡氨醇(phenyramidol)、吡酮洛芬(piketoprofen)、去痛定(piminodine)、哌保松(pipebuzone)、哌立酮(piperylone)、哌洛芬(piprofen)、吡拉唑酸(pirazolac)、氰苯双哌酰胺(piritramide)、炎痛喜康(piroxicam)、普拉洛芬(pranoprofen)、泼尼卡酯(prednicarbate)、强的松龙(prednisolone)、强的松(prednisone)、强的松龙戊酸酯(prednival)、泼尼立定(prednylidene)、丙谷炎痛(proglumetacin)、普罗庚嗪(proheptazine)、二甲哌替啶(promedol)、丙帕他莫(propacetamol)、丙吡胺(propiram)、丙氧吩(propoxyphene)、异丙安替比林(propyphenazone)、普罗喹宗(proquazone)、吩噻嗪丙酸(protizinic acid)、普罗沙唑(proxazole)、雷米那酮(ramifenazone)、雷米芬太尼(remifentanil)、甲硫酸吡嘧乙酯(rimazolium metilsulfate)、罗非昔布(rofecoxib)、乙酰水杨酰胺(salacetamide)、水杨苷(salicin)、水杨酰胺(salicylamide)、水杨酰胺邻乙酸、水杨酸、水杨酸硫酸酯、双水杨酸酯、沙维林(salverine)、西美曲特(simetride)、舒芬太尼(sufentanil)、柳氮磺胺吡啶(sulfasalazine)、舒林酸(sulindac)、超氧化物歧化酶、舒洛芬(suprofen)、琥保松(suxibuzone)、他尼氟酯(talniflumate)、替尼达普(tenidap)、替诺昔康(tenoxicam)、特罗氨酯(terofenamate)、粉防己碱(tetrandrine)、噻唑啉酮丁氮酮(thiazolinobutazone)、噻洛芬酸(tiaprofenicacid)、噻拉米特(tiaramide)、替利定(tilidine)、替诺立定(tinoridine)、氢可的松(tixocortol)、托灭酸(tolfenamic acid)、痛灭定(tolmetin)、曲马多(tramadol)、去炎松(triamcinolone)、tropesin、戊地昔布(valdecoxib)、维米醇(viminol)、联苯丁酸(xenbucin)、肟环苯丙酸(ximoprofen)、扎托洛芬(zaltoprofen)或佐美酸(zomepirac)。
在一具体实施方式中,这种药物为选择性COX-2抑制剂,例如为式(I)所示的化合物或其前体药物或其可药用盐:
A为选自部分不饱和或不饱和的杂环以及部分不饱和或不饱和的碳环的取代基,优选地,杂环基团选自吡唑基、呋喃酮基、异噁唑基、吡啶基、环戊烯酮基(cyclopentenonyl)和哒嗪酮基;
X为O、S或CH2;
n为0或1;
R11为至少一种选自杂环、环烷基、环烯基和芳基的取代基,并任选地被一个或多个取代基在可取代位取代,取代基选自烷基、卤代烷基、氰基、羧基、烷氧羰基、羟基、羟烷基、卤代烷氧基、氨基、烷基氨基、芳基氨基、硝基、烷氧基烷基、烷基亚磺酰基、卤原子、烷氧基和烷硫基;
R12为甲基、氨基或氨基羰基烷基;
R13为一个或多个选自下列基团的基团:氢(hydrido)、卤原子、烷基、烯基、炔基、氧基、氰基、羧基、氰基烷基、杂环氧基、烷氧基、烷硫基、烷基羰基、环烷基、芳基、卤代烷基、杂环基、环烯基、芳烷基、杂环烷基、酰基、烷硫基烷基(alkylthioalkyl)、羟烷基、烷氧基羰基、芳基羰基、芳烷基羰基、芳烯基、烷氧基烷基、芳硫基烷基(arylthioalkyl)、芳氧基烷基、芳烷硫基烷基、芳烷氧基烷基、烷氧基芳烷氧基烷基、烷氧基羰基烷基、氨基羰基、氨基羰基烷基、烷基氨基羰基、N-芳基氨基羰基、N-烷基-N-芳基氨基羰基、烷基氨基羰基烷基、羧基烷基、烷基氨基、N-芳基氨基、N-芳烷基氨基、N-烷基-N-芳烷基氨基、N-烷基-N-芳基氨基、氨基烷基、烷基氨基烷基、N-芳基氨基烷基、N-芳烷基氨基烷基、N-烷基-N-芳烷基氨基烷基、N-烷基-N-芳基氨基烷基、芳氧基、芳烷氧基、芳硫基、芳烷硫基、烷基亚磺酰基、烷基磺酰基、氨基磺酰基、烷基氨基磺酰基、N-芳基氨基磺酰基、芳基磺酰基和N-烷基-N-芳基氨基磺酰基,R13任选地被一个或多个取代基在可取代位取代,取代基选自烷基、卤代烷基、氰基、羧基、烷氧基羰基、羟基、羟烷基、卤代烷氧基、氨基、烷基氨基、芳基氨基、硝基、烷氧基烷基、烷基亚磺酰基、卤原子、烷氧基和烷硫基;和R14选自氢和卤原子。
在根据本发明实施方式的优选组合物中,选择性COX-2抑制剂为式(II)所示的化合物:
其中R15为甲基、氨基或酰亚胺基(imide group),R16为氢或C1-4烷基或烷氧基,X为N或CR17,其中R17为氢或卤原子,并且Y和Z独立地为碳或氮原子,它们是五元或六元环的相邻原子,所述环未被取代,或在一个或多个位置被氧、卤原子、甲基或卤代甲基取代。优选的这类五至六元环为在不超过一个位置被取代的环戊烯酮、呋喃酮、甲基吡唑、异噁唑和吡啶环。
在根据本发明实施方式的另一优选组合物中,选择性COX-2抑制剂为具有式(III)的化合物或其前体药物或其可药用盐:
其中X″为O、S或N-低级烷基;R18为低级卤代烷基;R19为氢或卤;R20为氢、卤原子、低级烷基、低级烷氧基或卤代烷氧基、低级芳烷基羰基、低级二烷基氨基磺酰基、低级烷基氨基磺酰基、低级芳烷基氨基磺酰基、低级杂芳烷基氨基磺酰基或5或6元含氮的杂环磺酰基;R21和R22独立地为氢、卤原子、低级烷基、低级烷氧基或芳基。
式(III)代表的尤其有用的化合物为(S)-6,8-二氯-2-(三氟甲基)-2H-1-苯并吡喃-3-羧酸。在根据本发明实施方式的又一优选组合物中,选择性COX-2抑制剂为5-烷基-2-芳基氨基苯乙酸或其衍生物。尤其有用的这类化合物为5-甲基-2-(2′-氯-6′-氟苯胺基)苯乙酸和其可药用盐。
例如,在本发明的组合物中,可用塞来昔布(celecoxib)、deracoxib、戊地昔布(valdecoxib)、帕瑞昔布(parecoxib)、罗非昔布(rofecoxib)、依托昔布(etoricoxib)、2-(3,5-二氟苯基)-3-[4-(甲基磺酰基)苯基]-2-环戊烯-1-酮、(S)-6,8-二氯-2-(三氟甲基)-2H-1-苯并吡喃-3-羧酸、2-(3,4-二氟苯基)-4-(3-羟基-3-甲基-1-丁氧基)-5-[4-(甲基磺酰基)苯基]-3-(2H)-哒嗪酮和它们的盐。
例如,选择性COX-2抑制剂或其前体药物可选自塞来昔布、戊地昔布、帕瑞昔布、罗非昔布、依托昔布、(S)-6,8-二氯-2-(三氟甲基)-2H-1-苯并吡喃-3.-羧酸和它们的盐。
在另一实施方式中,片芯中含有的药物用于治疗和/或预防男性和/或女性患者的性功能障碍。这类药物可为例如(a)磷酸二酯酶5型(PDE5)抑制剂,如西地那非(sildenafil)、他达拉非(tadalafil)或泛地那非(vardenafil),(b)环GMP磷酸二酯酶抑制剂,(c)环AMP活化剂,(d)α-肾上腺素能拮抗剂,如酚妥拉明(phentolamine)或育亨宾(yohimbine),或(e)多巴胺能激动剂,如阿扑吗啡(apomorphine)。这类药物可为下面式(V)代表的化合物。或者,片芯中含有的药物可不同于在治疗和/或预防性功能障碍中使用的药物。作为另外的替换方案,片芯中含有的药物可用于治疗和/或预防性功能障碍但不同于下面式(V)代表的化合物。
在示例性组合物中,用于例如治疗帕金森病或性功能障碍的药物存在于片芯中,并为式(V)代表的化合物或其可药用盐:
其中,
R1、R2和R3相同或不同,为H、C1-6烷基(任选被苯基取代)、C3-5烯基或炔基或C3-10环烷基,或R3同上所述,R1和R2与相连的N原子成环形成吡咯烷基、哌啶基、吗啉基、4-甲基哌嗪基或咪唑基;、
X为H、F、Cl、Br、I、OH、C1-6烷基或烷氧基、CN、氨甲酰、羧基或(C1-6烷基)羰基;
A为CH、CH2、CHF、CHCl、CHBr、CHI、CHCH3、C=O、C=S、CSCH3、C=NH、CNH2、CNHCH3、CNHCOOCH3、CNHCN、SO2或N;
B为CH、CH2、CHF、CHCl、CHBr、CHI、C=O、N、NH或NCH3,n为0或1;并且
D为CH、CH2、CHF、CHCl、CHBr、CHI、C=O、O、N、NH或NCH3。优选式(V)代表的化合物或其盐为水溶性的。
式(V)代表的化合物的可药用盐包括但不限于下列酸的盐:盐酸、氢溴酸、硫酸、甲磺酸、磷酸、硝酸、苯甲酸、柠檬酸、酒石酸、富马酸和马来酸,和式CH3-(CH2)n-COOH和HOOC-(CH2)n-COOH的单羧酸和二羧酸,其中n为0至4,例如丙二酸。
尤其优选的盐为盐酸盐和马来酸盐,即(Z)-2-丁烯二酸盐。
可通过本来已知的方法制备式(V)的化合物和它们的盐,包括本文引用的专利文献中描述的方法。但是,本发明不受制备治疗药所用的方法的限制。
优选的式(V)的化合物为Moon等人的美国专利US5273975中一般地或特定地描述的那些。尤其优选的化合物为式(VI)代表的化合物和其可药用盐:
O或S。
可通过现有技术中已知的任何合适方法制备符合本发明用的片芯。根据本发明的芯包括分散有水溶性染料固体颗粒的基质。任何合适的赋形剂都能形成基质。对于经口片剂,基质一般包括稀释剂或载体,例如乳糖和/或淀粉,并还可包括另外的赋形剂如粘合剂、崩解剂、润湿剂等。对于口内片剂,基质一般包括水溶性糖,例如甘露醇和/或麦芽糖。如果药物存在于芯中,则药物也分散在基质中。
片剂最终的外观部分取决于水溶性染料的选择和染料固体颗粒的数量和大小。例如,较大颗粒产生的斑点图形往往比较小颗粒产生的斑点图形具有更大的颜色块;较大量颗粒产生的斑点图形往往比较少量颗粒产生的斑点图形能覆盖片剂表面的更大部分。水溶性大的染料往往比水溶性小的染料产生更大和/或更少的分散颜色块。
芯中可任意地存在一种以上水溶性染料的固体颗粒,以为片剂提供双色或多色斑点外观。
用包含胶凝糖胶的包衣组合物包衣芯,这在下面更充分地描述。包衣层一般的存在量表示为增重约0.1%-约5%,但可根据需要使用更大或更小的量。优选地,胶凝糖胶构成包衣层重量的约25%-100%,更优选约50%-100%。
优选地,包衣层为赋形剂包衣层。这里的“赋形剂包衣层”是指至少在为芯施用包衣层时仅由赋形剂材料组成的包衣层,也就是说在其中基本上不含药物。应认识到在生产和贮存过程中,可能会发生从本发明片剂芯到包衣层的一定程度的药物迁移,但这通常是微不足道的。因此,药物(如果在片剂中存在的话)主要被限制在芯上,在这里它不会与胶凝糖胶混合。
可在包衣组合物中使用任何胶凝糖胶,但优选使用脱酰基的胶凝糖胶,如商标为KelcogelTM的市售品。包衣组合物中可任选地存在一种或多种其它的胶和/或生物聚合物,如藻酸盐。
包衣组合物包括已在其中溶解或分散了胶凝糖胶和任选的一种或多种其它赋形剂的可喷涂介质,优选水。优选地,包衣组合物的总固体浓度为约1wt%-约10wt%,并且胶凝糖胶浓度为约1wt%-约5wt%。
包衣组合物中存在的其它赋形剂可包括:一种或多种缓冲剂,一般地浓度为约0.03wt%-约3wt%;一种或多种增塑剂,一般地浓度为约0.03wt%-约3wt%;和/或一种或多种分散剂和/或乳化剂,一般地浓度为约0.03wt%-约3wt%。合适的缓冲剂的例子为柠檬酸钠。合适的增塑剂的例子为丙二醇。合适的分散剂或乳化剂的例子为卵磷脂。如果需要,还可在包衣组合物中包括调味剂。
可通过任何适当的方法制备包衣组合物,包括将胶凝糖胶和任选的其它赋形剂溶解到介质中,介质优选水。添加顺序不重要。优选将水加热至例如约55℃-约85℃的温度。在搅拌下加入胶凝糖胶和其它赋形剂(如果有的话)直到所有成分均匀分散。优选在搅拌和随后的喷涂过程中将得到的包衣液体保持在高温(elevated temperature)。
将待包衣的片芯放在合适的包衣装置内,例如包衣锅,并优选预热至约50℃-约70℃的床温。在由一个本领域技术人员就能容易优化的条件下将包衣液体喷涂到片剂上。连续进行喷涂直到已施用了与增重为约0.1%-约5%相当的包衣液量。在从包衣锅中卸出前,优选将得到的包衣片剂冷却至室温或约20℃-约35℃。
包衣和冷却条件也会影响最终片剂的精确颜色图形。例如,如果在低温下进行包衣和/或如果缓慢冷却,则芯内的固体染料颗粒就长时间暴露于水,因而一般会产生具有较大颜色块的斑点图形。
含有盐如sumanirole或(R)-5,6-二氢-5-(甲基氨基)-4H-咪唑并[4,5-ij]-喹啉-2(1H)-硫酮的马来酸盐作为活性剂的本发明的示例性舌下片剂具有组成为以下的芯:
活性剂 0.1-3%游离碱当量
甘露醇 50-90%
山梨糖醇粉末 10-40%
羟丙基纤维素 0-10%
黄原胶 0-5%
调味剂 0-0.5%
水溶性染料 0-0.5%
胶态二氧化硅 0-1%
硬脂酸镁 0.5-5%所有百分比均以重量计。
含有盐如sumanirole或(R)-5,6-二氢-5-(甲基氨基)-4H-咪唑并[4,5-ij]-喹啉-2(1H)-硫酮的马来酸盐作为活性剂的本发明的另一示例性舌下片剂具有组成为以下的芯:
活性剂 0.1-3%游离碱当量
乳糖一水合物 50-85%
预胶化淀粉 10-45%
黄原胶 0-5%
调味剂 0-0.5%
水溶性染料 0-0.5%
胶态二氧化硅 0-1%
硬脂酸镁 0.5-5%
所有百分比均以重量计。
含有盐如sumanirole或(R)-5,6-二氢-5-(甲基氨基)-4H-咪唑并[4,5-ij]-喹啉-2(1H)-硫酮的马来酸盐作为活性剂的本发明的又一示例性舌下片剂具有组成为以下的芯:
活性剂 0.1-3%游离碱当量
微晶纤维素 30-70%
预胶化淀粉 25-65%
交联羧甲基纤维素钠 0-10%
黄原胶 0-5%
调味剂 0-0.5%
水溶性染料 0-0.5%
胶态二氧化硅 0-1%
硬脂酸镁 0.5-5%所有百分比均以重量计。
实施例
下面的实施例举例说明本发明,但不应被看作是对其的限制。在这些实施例中,“化合物Z”是指(R)-5,6-二氢-5-(甲基氨基)-4H-咪唑并[4,5-ij]-喹啉-2(1H)-硫酮马来酸盐。除非另外指明,所有百分比均以重量计。
实施例1
制备具有以下组成的舌下片剂制剂:
化合物Z 1.11%
AvicelTM PH-101(微晶纤维素) 46.71%
Colorcon淀粉1500(预胶化淀粉) 44.00%
交联羧甲基纤维素钠NF 5.00%
胶态二氧化硅NF 0.50%
桂皮调味剂 0.14%
薄荷调味剂 0.04%
染料(樱桃色#1632,Crompton&Knowles) 0.50%
硬脂酸镁 2.00%
在高剪切混合器内混合预胶化淀粉和染料2分钟,或直到混合均匀。然后在高剪切混合器内得到的混合物上逐一地放置以下成分:化合物Z;微晶纤维素;胶态二氧化硅;交联羧甲基纤维素钠。再继续在高剪切混合器内的混合2分钟。如果染料不能充分地分散到得到的混合物中,则以1分钟的增量继续混合直到观察到良好的染料分散。然后取出混合物的一小部分并用手与硬脂酸镁混合形成硬脂酸镁预混合料。将这种预混合料与调味剂一起加入到高剪切混合器内,并混合1分钟形成润滑的片剂原料。
从高剪切混合器中卸出润滑的片剂原料,并贮存到干燥密闭的密封容器中直到开始制片剂。通过使用12/32英寸(约9mm)的稍微弯曲的Plain/Plain工具压缩成以下规格来制备片剂:
片剂重量 180mg
硬度 3-4SCU
脆碎度 <0.5%
实施例2
按照下面的过程用胶凝糖胶包衣层包衣按实施例1制备的舌下片剂。
制备具有以下组成的包衣液:
胶凝糖胶(KelcogelTM) 2.00%
柠檬酸钠 0.13%
丙二醇 0.40%
卵磷脂 0.20%
去离子水 97.27%
将去离子水加热至70℃。在搅拌下加入其它成分直到所有成分均匀分散。在搅拌和随后的喷涂过程中将得到的固体含量为2.73%的包衣液保持在70℃温度。
将700g的实施例1的片剂放到12英寸(约300mm)的包衣锅中,并预热至60℃的床温。在以下条件下将包衣液喷涂到片剂上:
出口空气温度 50-60℃
锅速 16rpm
空气流速 30-35cfm(0.84-0.98m3/分钟)
雾化空气压力 10psi(69kPa)
蠕动泵速度(setting): 15-20g/min
连续进行喷涂直到已施用了与增重为1.2%相当的包衣液量。在从包衣锅中卸出前,将得到的包衣片剂冷却至30℃。
片剂具有诱人的带樱桃红斑点的高亮光外观。
实施例3
制备具有以下组成的舌下片剂制剂:
化合物Z 1.05%
甘露醇,颗粒 70.00%
山梨糖醇 16.57%
羟丙基纤维素,LH-11型 7.00%
黄原胶 2.50%
胶态二氧化硅NF 0.50%
桂皮调味剂 0.14%
薄荷调味剂 0.04%
染料(樱桃色#1632,Crompton&Knowles) 0.20%
硬脂酸镁 2.00%
在高剪切混合器内混合甘露醇和染料2分钟或直到混合均匀。然后在高剪切混合器内得到的混合物上逐一地放置以下成分:化合物Z;山梨糖醇;羟丙基纤维素;黄原酸胶;胶态二氧化硅。再继续在高剪切混合器内的混合2分钟。如果染料不能充分地分散到整个得到的混合物中,则以1分钟的增量继续混合直到观察到良好的染料分散。然后取出混合物的一小部分并用手与硬脂酸镁混合形成硬脂酸镁预混合料。将这种预混合料与调味剂一起加入到高剪切混合器内,并混合1分钟形成润滑的片剂原料。
从高剪切混合器中卸出润滑的片剂原料,并贮存到干燥密闭的密封容器中直到开始制片剂。通过使用12/32英寸(约9mm)的稍微弯曲的Plain/Plain工具压缩成以下规格来制备片剂:
片剂重量 190mg
硬度3-4 SCU
脆碎度 <0.5%
实施例4
按照下面的过程用胶凝糖胶包衣层包衣按实施例3制备的舌下片剂。
制备具有以下组成的包衣液:
胶凝糖胶(KelcogelTM) 2.00%
柠檬酸钠 0.13%
丙二醇 0.40%
卵磷脂(LipoidTMLS-100) 0.20%
调味剂 0.30%
去离子水 96.97%
将去离子水加热至70℃。在搅拌下加入其它成分直到所有成分均匀分散。在搅拌和随后的喷涂过程中将得到的固体含量为3.03%的包衣液保持在70℃温度。
将700g实施例1的片剂放到12英寸(约300mm)的包衣锅中,并预热至60℃的床温。在以下条件下将包衣液喷涂到片剂上:
出口空气温度 50-60℃
锅速 16rpm
空气流速 30-35cfm(0.84-0.98m3/分钟)
雾化空气压力 10psi(69kPa)
蠕动泵速度: 15-20g/min
连续进行喷涂直到已施用了与增重为1.36%相当的包衣液量。在从包衣锅中卸出前,将得到的包衣片剂冷却至30℃。
片剂具有诱人的带樱桃红斑点的高亮光外观。
实施例5
制备具有以下组成的舌下片剂制剂:
化合物Z 0.43%
AvicelTM PH-101(微晶纤维素) 47.39%
Colorcon淀粉1500(预胶化淀粉) 44.00%
交联羧甲基纤维素钠NF 5.00%
胶态二氧化硅NF 0.50%
桂皮调味剂 0.14%
薄荷调味剂 0.04%
染料(樱桃色#1632,Crompton&Knowles) 0.50%
硬脂酸镁 2.00%
在高剪切混合器内混合预胶化淀粉和染料2分钟或直到混合均匀。然后在高剪切混合器内得到的混合物上逐一地放置以下成分:化合物Z;微晶纤维素;胶态二氧化硅;交联羧甲基纤维素钠。再继续在高剪切混合器内的混合2分钟。如果染料不能充分地分散到整个得到的混合物中,则以1分钟的增量继续混合直到观察到良好的染料分散。然后取出混合物的一小部分并用手与硬脂酸镁混合形成硬脂酸镁预混合料。将这种预混合料与调味剂一起用手过#20目药用筛,然后加入到高剪切混合器内,并混合1分钟形成润滑的片剂原料。
从高剪切混合器中卸出润滑的片剂原料,并贮存到干燥密闭的密封容器中直到开始制片剂。通过使用12/32英寸(约9mm)的稍微弯曲的Plain/Plain工具压缩成以下规格来制备片剂:
片剂重量 180mg
硬度 3.5-4SCU
脆碎度 <0.8%
实施例6
按照下面的过程用胶凝糖胶包衣层包衣按实施例5制备的舌下片剂。
制备具有以下组成的包衣液:
胶凝糖胶(KelcogelTM) 2.00%
柠檬酸钠 0.13%
丙二醇 0.40%
卵磷脂(LipoidTMLS-100) 0.20%
热桂皮调味剂 0.30%
去离子水 96.97%
将去离子水加热至70℃。在搅拌下加入其它成分直到所有成分均匀分散。在搅拌和随后的喷涂过程中将得到的固体含量为3.03%的包衣液保持在70℃温度。
将7000g实施例5的片剂放到24英寸(约600mm)的包衣锅中,并预热至60℃的床温。在以下条件下将包衣液喷涂到片剂上:
出口空气温度 48-55℃
锅速 10-14rpm,优选14rpm
空气流速 300-400cfm(8.5-11.3m3/分钟)
雾化空气压力 20-35psi(138-242kPa),
优选约20psi
蠕动泵速度: 15-40g/min/枪(2喷枪系统),
优选30-40g/min/枪
片剂床温 37-50℃,优选约40℃
连续进行喷涂直到已施用了与增重为2.04%相当的包衣液量。在从包衣锅中卸出前,将得到的包衣片剂冷却至30℃。
片剂具有诱人的带樱桃红斑点的高亮光外观。
Claims (29)
1.一种药物片剂,该片剂包括片芯和粘附于片芯的包衣层,其中(a)片芯包括分散在基质中的水溶性染料的固体颗粒,(b)包衣层包括胶凝糖胶;且该片剂具有斑点表面外观。
2.权利要求1所述的片剂,其中片芯包含治疗和/或预防有效量的药物。
3.权利要求2所述的片剂,其中药物选自ACE抑制剂;α-肾上腺素能激动剂;β-肾上腺素能激动剂;α-肾上腺素能阻滞剂;β-肾上腺素能阻滞剂;醇抑制剂;醛醣还原酶抑制剂;醛固酮拮抗剂;氨基酸;同化剂;麻醉药和非麻醉药类型的镇痛药;麻醉剂;减食欲药;抗酸剂;驱虫剂;抗粉刺剂;抗过敏剂;抗雄性激素药;抗心绞痛药;抗不安药;抗心律失常药;平喘药;抗菌药和抗生素;抗脱发和抗秃顶药;抗变形虫药;抗体;抗胆碱能药;抗凝血剂和血液稀释剂;抗结肠炎药;抗惊厥药;抗膀胱炎药;抗抑郁药;抗糖尿病药;止泻药;抗利尿药;解毒药;止吐药;抗雌激素药;抗气胀药;抗真菌药;抗原;抗青光眼药;抗组胺药;抗机能亢进药;抗高脂蛋白血症药;抗高血压药;抗甲状腺机能亢进药;抗低血压药;抗甲状腺机能减退药;抗感染药;甾族的和非甾族的抗炎药;抗疟疾药;抗偏头痛药;抗肿瘤药;抗肥胖药;抗帕金森病药和抗运动障碍药;抗肺炎药;抗原虫药;抗痒药;抗牛皮癣药;抗精神病药;退热药;抗风湿药;抗分泌药;抗休克药;抗痉挛药;抗血栓形成药;抗癌药;镇咳药;抗溃疡药;抗病毒药;抗焦虑药;杀菌药;骨增密剂;支气管扩张药;钙通道阻滞剂;碳酸酐酶抑制剂;强心剂和心脏兴奋剂;化学治疗剂;利胆剂;类胆碱能药物;慢性疲劳综合症治疗药;CNS兴奋剂;促凝剂;避孕药;囊性纤维化治疗药;减充血剂;利尿剂;多巴胺受体激动剂;多巴胺受体拮抗剂;酶;雌激素;祛痰药;胃机能亢进治疗药;糖皮质激素;止血剂;HMG CoA还原酶抑制剂;激素;安眠药;免疫调节剂;免疫抑制剂;轻泻剂;口腔和牙周疾病用药;缩瞳药;单胺氧化酶抑制剂;粘液溶解剂;多发性硬化治疗药;肌肉松弛药;散瞳药;抗麻醉药;NMDA受体拮抗剂;寡核苷酸;眼用药;催产药;肽;多肽和蛋白质;多糖;孕激素;前列腺素;蛋白酶抑制剂;呼吸促进剂;镇静剂;五羟色胺摄取抑制剂;性激素,其包括雄性激素;戒烟药;平滑肌松弛药;平滑肌兴奋剂;血栓溶解剂;安定药;尿酸化剂;尿失禁治疗药;血管扩张剂;血管保护剂;和它们的混合物。
4.权利要求2所述的片剂,其中药物为戒烟药。
5.权利要求4所述的片剂,其中戒烟药选自丁氨苯丙酮、伊菠加因、烟碱及其代谢物。
6.权利要求2所述的片剂,其中药物为抗菌药。
7.权利要求6所述的片剂,其中抗菌药为噁唑烷酮。
8.权利要求7所述的片剂,其中噁唑烷酮选自依哌唑胺、利奈唑胺、N-[(5S)-3-[3-氟-4-[4-(2-氟乙基)-3-氧代-1-哌嗪基]苯基-2-氧代-5-噁唑烷基]甲基]乙酰胺、(S)-N-[[3-[5-(3-吡啶基)噻吩-2-基]-2-氧代-5-噁唑烷基]甲基]乙酰胺和(S)-N-[[3-[5-(4-吡啶基)吡啶-2-基]-2-氧代-5-噁唑烷基]甲基]乙酰胺盐酸盐。
9.权利要求2所述的片剂,其中药物为抗偏头痛药。
10.权利要求9所述的片剂,其中抗偏头痛药为5-HT受体激动剂。
11.权利要求10所述的片剂,其中5-HT受体激动剂选自阿莫曲坦、依立曲坦、氟伐曲坦、纳拉曲坦、雷扎曲坦、舒马曲坦或佐米曲坦。
12.权利要求2所述的片剂,其中药物用于治疗或预防眼科疾病。
13.权利要求12所述的片剂,其中药物为抗青光眼药或降眼压药。
14.权利要求13所述的片剂,其中抗青光眼药或降眼压药选自adrenolone、阿可乐定、溴莫尼定、地匹福林、醋丁洛尔、阿达洛尔、烯丙洛尔、阿替洛尔、倍他洛尔、布非洛尔、丁呋洛尔、布尼洛尔、丁萘酮心安、布拉洛尔、卡替洛尔、卡维洛尔、西他洛尔、右旋普萘洛尔、拉贝洛尔、左布诺洛尔、美替洛尔、美托洛尔、纳多洛尔、硝苯洛尔、心得平、环戊丁心安、吲哚洛尔、心得宁、萘心定、普萘洛尔、索他洛尔、噻吗洛尔、胺甲苯心安、托利洛尔、vaninolol、醋唑磺胺、多尔唑胺、比马前列素、适利达、曲沃前列素、乌诺前列酮异丙酯和它们的组合。
15.权利要求2所述的片剂,其中药物为止痛药、退热药或抗炎药。
16.权利要求15所述的片剂,其中止痛药、退热药或抗炎药选自醋氯酚酸、醋炎痛、e-乙酰氨基己酸、扑热息痛、水杨酸对乙酰氨苯酯、乙酰苯胺、乙酰水杨酸、S-钴酰胺蛋氨酸、阿氯酚酸、阿氯米松、阿芬太尼、阿尔孕酮、烯丙苯哌啶、阿明洛芬、阿洛普令、阿法罗定、双(乙酰水杨酸)铝、安西缩松、氨芬酸、氨基氯噻噁嗪、3-氨基-4-羟基丁酸、2-氨基-4-甲基吡啶、氨基普罗皮纶、氨基比林、阿米曲林、水杨酸铵、安吡昔康、呱氨托美丁、阿尼利定、安替比林、安拉非宁、炎爽痛、倍氯米松、苄吲酸、贝诺酯、苯噁洛芬、苄哌吡酮、炎痛静、苄吗啡、贝尔洛芬、倍他米松、苯晴米特、α-没药醇、溴芬酸、对-溴乙酰苯胺、5-溴水杨酸乙酸酯、溴水杨醇、丁西丁、氯环己苯酰丙酸、布可龙、布地缩松、丁苯羟酸、丁丙二苯肼、丁丙诺啡、丁醋苯胺、布替布芬、布托啡诺、卡马西平、卡必芬、卡布洛芬、卡沙兰、塞来昔布、氯丁醇、氯泼尼松、氯乙苯噁嗪酮、水杨酸胆碱、辛可芬、桂美辛、曲马朵、环氯茚酸、氯倍他索、氯可托龙、氯美辛、氯尼他秦、氯胺烟酸、氯苯吡咯酸、氯泼尼醇、丁香、可待因、可待因甲基溴、磷酸可待因、硫酸可待因、可的松、可的伐唑、巴酰丙酰胺、巴酰乙酰胺、去氟可特、二氢去氧吗啡、丙缩羟强龙、去羟米松、地塞米松、右旋二苯哌啶二噁烷、吗散痛、地佐辛、双胺丙酰胺、双氯芬酸、二苯酰胺吡唑、联苯吡胺、二氟拉松、二氟米松、双氟尼酸、醋丁二氟龙、二氢可待因、醋氢可待酮、二氢吗啡、乙酰水杨酸二氢铝、苯醋胺乙酯、美沙醇、二甲嗯丁胺、吗苯丁酯、二苯哌己酮、diprocetyl、安乃近、双苯唑醇、哚昔康、依莫法宗、苯乙氨茴酸、甘草次酸、嘧啶唑、依他佐辛、依特柳酯、乙柳酰胺、依索庚嗪、乙氧二氨偶氮苯、甲乙嗯丁胺、乙基吗啡、依托度酸、依托非那酯、依托尼秦、依托昔布、丁香酚、联苯乙酸、芬布芬、氯苯噻唑乙酸、芬多沙、苯氧苯丙酸、芬太尼、芬替酸、非普地醇、戊烯保泰松、氟喹氨苯酯、氟噁米松、氟二氯松、氟灭酸、二氟美松、9-去氟肤轻松、氟胺烟酸、氟诺洛芬、醋酸氟轻松、氟轻松、氟考丁酯、氟考龙、氟苯乙砜、氟甲龙、氟培龙、氟吡汀、氟泼尼定、氟强的松龙、氟丙喹宗、丙酮缩氟氢羟龙、氟比洛芬、醛基缩松、磷酸柳酯、龙胆酸、格拉非宁、葡卡美新、水杨酸二醇酯、愈创兰油烃、氯氟松、氯二氟美松、溴氟龙、氢可酮、氢可松氨酯、氢化可的松、二氢吗啡酮、羟哌替啶、异丁苯乙酸、布洛芬、布洛新、水杨酸咪唑、消炎痛、吲哚洛芬、三苯唑酸、isoladol、异美沙酮、异尼克辛、伊索克酸、伊索昔康、凯托米酮、酮洛芬、痛力克、乳酰对异氧苯胺、利非他明、羟甲左吗喃、洛芬太尼、氯苯唑酸、氯诺昔康、洛索洛芬、赖氨酸阿司匹林、马泼尼酮、甲氯灭酸、甲羟松、甲灭酸、度冷丁、甲泼尼松、哌替啶、美沙拉明、美他佐辛、美沙酮、甲氧异丁嗪、甲基强的松龙、甲噻吩嗪乙酸、甲氧苯啉、甲基二氢吗啡酮、布他酮、莫苯唑酸、苯吗比林、吗啡、盐酸吗啡、硫酸吗啡、水杨酸吗啉、麦罗啡、那布米酮、纳布啡、水杨酸-1-萘酯、萘普生、那碎因、平痛新、尼可吗啡、尼芬那宗、尼氟灭酸、尼美舒利、5’-硝基-2’-丙氧基乙酰苯胺、去甲左啡烷、去甲美沙酮、去甲吗啡、诺匹哌酮、偶氮水杨酸、阿片、奥沙西罗、吲肟酸、噁丙嗪、羟考酮、羟吗啡酮、羟保泰松、阿片全碱、对氟米松、胍苯叉芴、帕瑞昔布、帕沙米特、镇痛新、哌立索唑、非那西丁、苯吗庚酮、非那佐辛、盐酸非那吡啶、非诺可、苯哌利定、非诺吡酮、乙酰水杨酸苯酯、苯基保泰松、水杨酸苯酯、苯吡氨醇、吡酮洛芬、去痛定、哌保松、哌立酮、哌洛芬、吡拉唑酸、氰苯双哌酰胺、炎痛喜康、普拉洛芬、泼尼卡酯、强的松龙、强的松、强的松龙戊酸酯、泼尼立定、丙谷炎痛、普罗庚嗪、二甲哌替啶、丙帕他莫、丙吡胺、丙氧吩、异丙安替比林、普罗喹宗、吩噻嗪丙酸、普罗沙唑、雷米那酮、雷米芬太尼、甲硫酸吡嘧乙酯、罗非昔布、乙酰水杨酰胺、水杨苷、水杨酰胺、水杨酰胺邻-乙酸、水杨酸、水杨酸硫酸酯、双水杨酸酯、沙维林、西美曲特、舒芬太尼、柳氮磺胺吡啶、舒林酸、超氧化物歧化酶、舒洛芬、琥保松、他尼氟酯、替尼达普、替诺昔康、特罗氨酯、粉防己碱、噻唑啉酮丁氮酮、噻洛芬酸、噻拉米特、替利定、替诺立定、氢可的松、托灭酸、痛灭定、曲马多、去炎松、tropesin、戊地昔布、维米醇、联苯丁酸、肟环苯丙酸、扎托洛芬和佐美酸。
17.权利要求15所述的片剂,其中止痛药、退热药或抗炎药为选择性COX-2抑制剂。
18.权利要求17所述的片剂,其中选择性COX-2抑制剂为下式化合物:
其中R15为甲基、氨基或酰亚胺基,R16为氢或C1-4烷基或烷氧基,X为N或CR17,其中R17为氢或卤原子,并且Y和Z独立地为碳或氮原子,它们是五元或六元环的相邻原子,所述环未被取代,或在一个或多个位置被氧、卤原子、甲基或卤代甲基取代。
19.权利要求17所述的片剂,其中选择性COX-2抑制剂选自塞采昔布、deracoxib、戊地昔布、帕瑞昔布、罗非昔布、依托昔布、2-(3,5-二氟苯基)-3-[4-(甲基磺酰基)苯基]-2-环戊烯-1-酮、(S)-6,8-二氯-2-(三氟甲基)-2H-1-苯并吡喃-3-羧酸、2-(3,4-二氟苯基)-4-(3-羟基-3-甲基-1-丁氧基)-5-[4-(甲基磺酰基)苯基]-3-(2H)-哒嗪酮和它们的盐。
20.权利要求2所述的片剂,其中药物为用于治疗和/或预防性功能障碍的药物。
21.权利要求20所述的片剂,其中药剂选自PDE5抑制剂、环AMP活化剂、α-肾上腺素能拮抗剂和多巴胺能激动剂。
22.权利要求20所述的片剂,其中药物为下式化合物或其可药用盐:
其中:
R1、R2和R3相同或不同,为H、任选被苯基取代的C1-6烷基、C3-5烯基或炔基或C3-10环烷基,或R3同上所述,R1和R2与相连的N原子成环形成吡咯烷基、哌啶基、吗啉基、4-甲基哌嗪基或咪唑基;、
X为H、F、Cl、Br、I、OH、C1-6烷基或烷氧基、CN、氨甲酰、羧基或C1-6烷基羰基;
A为CH、CH2、CHF、CHCl、CHBr、CHI、CHCH3、C=O、C=S、CSCH3、C=NH、CNH2、CNHCH3、CNHCOOCH3、CNHCN、SO2或N;
B为CH、CH2、CHF、CHCl、CHBr、CHI、C=O、N、NH或NCH3,n为0或1;并且
D为CH、CH2、CHF、CHCl、CHBr、CHI、C=O、O、N、NH或NCH3。
24.权利要求1所述的片剂,该片剂适于经口给药。
25.权利要求1所述的片剂,该片剂适于口内给药。
26.权利要求1所述的片剂,其中包衣层的存在量以增重表示为0.1-5%。
27.权利要求1所述的片剂,其中胶凝糖胶构成包衣层重量的25%-100%。
28.权利要求1所述的片剂,其中胶凝糖胶构成包衣层重量的50%-100%。
29.权利要求1所述的片剂,其中包衣层还包含至少一种选自缓冲剂、增塑剂、分散剂和乳化剂的其它赋形剂。
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NZ533957A (en) | 2006-02-24 |
ATE346591T1 (de) | 2006-12-15 |
WO2003066030A3 (en) | 2003-10-16 |
AU2003210930B2 (en) | 2007-01-04 |
DK1480624T3 (da) | 2007-03-12 |
BR0307593A (pt) | 2005-02-01 |
RU2004124065A (ru) | 2005-04-20 |
JP2005517693A (ja) | 2005-06-16 |
HK1074581A1 (en) | 2005-11-18 |
MXPA04006799A (es) | 2004-12-06 |
KR100661684B1 (ko) | 2006-12-26 |
EP1480624B1 (en) | 2006-11-29 |
KR20050002821A (ko) | 2005-01-10 |
DE60310039D1 (de) | 2007-01-11 |
ES2274248T3 (es) | 2007-05-16 |
CN1630512A (zh) | 2005-06-22 |
PL372250A1 (en) | 2005-07-11 |
NO20043716L (no) | 2004-09-06 |
JP4174426B2 (ja) | 2008-10-29 |
US20030180357A1 (en) | 2003-09-25 |
ZA200405556B (en) | 2005-08-10 |
EP1480624A2 (en) | 2004-12-01 |
WO2003066030A2 (en) | 2003-08-14 |
RU2273473C2 (ru) | 2006-04-10 |
AU2003210930A1 (en) | 2003-09-02 |
DE60310039T2 (de) | 2007-04-05 |
CA2474921A1 (en) | 2003-08-14 |
CO5611097A2 (es) | 2006-02-28 |
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