CA2543482A1 - Inhalable pharmaceutical formulations employing lactose anhydrate and methods of administering the same - Google Patents
Inhalable pharmaceutical formulations employing lactose anhydrate and methods of administering the same Download PDFInfo
- Publication number
- CA2543482A1 CA2543482A1 CA002543482A CA2543482A CA2543482A1 CA 2543482 A1 CA2543482 A1 CA 2543482A1 CA 002543482 A CA002543482 A CA 002543482A CA 2543482 A CA2543482 A CA 2543482A CA 2543482 A1 CA2543482 A1 CA 2543482A1
- Authority
- CA
- Canada
- Prior art keywords
- lactose
- pharmaceutical formulation
- medicament
- formulation
- inhalation device
- 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.)
- Abandoned
Links
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 title claims abstract description 118
- 239000008101 lactose Substances 0.000 title claims abstract description 114
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 69
- 238000000034 method Methods 0.000 title claims description 41
- 239000003814 drug Substances 0.000 claims abstract description 55
- 239000000203 mixture Substances 0.000 claims description 162
- 238000009472 formulation Methods 0.000 claims description 120
- 239000000843 powder Substances 0.000 claims description 64
- GIIZNNXWQWCKIB-UHFFFAOYSA-N Serevent Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1 GIIZNNXWQWCKIB-UHFFFAOYSA-N 0.000 claims description 30
- -1 anti-infilammatories Substances 0.000 claims description 29
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 claims description 29
- 229910052925 anhydrite Inorganic materials 0.000 claims description 27
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 27
- 229960000289 fluticasone propionate Drugs 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 21
- 229940125388 beta agonist Drugs 0.000 claims description 20
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 19
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 claims description 16
- 229960005018 salmeterol xinafoate Drugs 0.000 claims description 16
- 229960004017 salmeterol Drugs 0.000 claims description 14
- 239000012453 solvate Substances 0.000 claims description 14
- 229960002052 salbutamol Drugs 0.000 claims description 13
- 150000002148 esters Chemical class 0.000 claims description 12
- 229960002848 formoterol Drugs 0.000 claims description 10
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 10
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims description 9
- 239000000443 aerosol Substances 0.000 claims description 9
- 229960004436 budesonide Drugs 0.000 claims description 9
- BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 claims description 9
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 claims description 8
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 claims description 8
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 claims description 8
- 229960000676 flunisolide Drugs 0.000 claims description 8
- 229960002714 fluticasone Drugs 0.000 claims description 8
- 229940071648 metered dose inhaler Drugs 0.000 claims description 8
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 claims description 8
- 229960000195 terbutaline Drugs 0.000 claims description 8
- 229940112141 dry powder inhaler Drugs 0.000 claims description 7
- MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 claims description 7
- 229960001664 mometasone Drugs 0.000 claims description 7
- 229960005294 triamcinolone Drugs 0.000 claims description 7
- 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 7
- 230000004584 weight gain Effects 0.000 claims description 7
- 235000019786 weight gain Nutrition 0.000 claims description 7
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 claims description 6
- 229910021653 sulphate ion Inorganic materials 0.000 claims description 6
- 229940035676 analgesics Drugs 0.000 claims description 5
- 239000000730 antalgic agent Substances 0.000 claims description 5
- 229950000210 beclometasone dipropionate Drugs 0.000 claims description 5
- 229940124630 bronchodilator Drugs 0.000 claims description 5
- 239000000168 bronchodilator agent Substances 0.000 claims description 5
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 5
- 229940088597 hormone Drugs 0.000 claims description 5
- 239000005556 hormone Substances 0.000 claims description 5
- 229960002720 reproterol Drugs 0.000 claims description 5
- WVLAAKXASPCBGT-UHFFFAOYSA-N reproterol Chemical compound C1=2C(=O)N(C)C(=O)N(C)C=2N=CN1CCCNCC(O)C1=CC(O)=CC(O)=C1 WVLAAKXASPCBGT-UHFFFAOYSA-N 0.000 claims description 5
- 208000023504 respiratory system disease Diseases 0.000 claims description 5
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 claims description 4
- AKNNEGZIBPJZJG-MSOLQXFVSA-N (-)-noscapine Chemical compound CN1CCC2=CC=3OCOC=3C(OC)=C2[C@@H]1[C@@H]1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-MSOLQXFVSA-N 0.000 claims description 4
- YREYLAVBNPACJM-UHFFFAOYSA-N 2-(tert-butylamino)-1-(2-chlorophenyl)ethanol Chemical compound CC(C)(C)NCC(O)C1=CC=CC=C1Cl YREYLAVBNPACJM-UHFFFAOYSA-N 0.000 claims description 4
- LSLYOANBFKQKPT-DIFFPNOSSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]benzene-1,3-diol Chemical compound C([C@@H](C)NC[C@H](O)C=1C=C(O)C=C(O)C=1)C1=CC=C(O)C=C1 LSLYOANBFKQKPT-DIFFPNOSSA-N 0.000 claims description 4
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical class O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims description 4
- HUYWAWARQUIQLE-UHFFFAOYSA-N Isoetharine Chemical compound CC(C)NC(CC)C(O)C1=CC=C(O)C(O)=C1 HUYWAWARQUIQLE-UHFFFAOYSA-N 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 4
- VQDBNKDJNJQRDG-UHFFFAOYSA-N Pirbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=N1 VQDBNKDJNJQRDG-UHFFFAOYSA-N 0.000 claims description 4
- BNPSSFBOAGDEEL-UHFFFAOYSA-N albuterol sulfate Chemical compound OS(O)(=O)=O.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 BNPSSFBOAGDEEL-UHFFFAOYSA-N 0.000 claims description 4
- AKNNEGZIBPJZJG-UHFFFAOYSA-N alpha-noscapine Natural products CN1CCC2=CC=3OCOC=3C(OC)=C2C1C1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-UHFFFAOYSA-N 0.000 claims description 4
- 230000000954 anitussive effect Effects 0.000 claims description 4
- 230000002924 anti-infective effect Effects 0.000 claims description 4
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 4
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims description 4
- 229940125715 antihistaminic agent Drugs 0.000 claims description 4
- 239000000739 antihistaminic agent Substances 0.000 claims description 4
- 229960005475 antiinfective agent Drugs 0.000 claims description 4
- 239000003434 antitussive agent Substances 0.000 claims description 4
- 229940124584 antitussives Drugs 0.000 claims description 4
- 229960004620 bitolterol Drugs 0.000 claims description 4
- FZGVEKPRDOIXJY-UHFFFAOYSA-N bitolterol Chemical compound C1=CC(C)=CC=C1C(=O)OC1=CC=C(C(O)CNC(C)(C)C)C=C1OC(=O)C1=CC=C(C)C=C1 FZGVEKPRDOIXJY-UHFFFAOYSA-N 0.000 claims description 4
- 239000000812 cholinergic antagonist Substances 0.000 claims description 4
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims description 4
- 229960003957 dexamethasone Drugs 0.000 claims description 4
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims description 4
- IZEKFCXSFNUWAM-UHFFFAOYSA-N dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 claims description 4
- 239000002934 diuretic Substances 0.000 claims description 4
- 229940030606 diuretics Drugs 0.000 claims description 4
- DLNKOYKMWOXYQA-UHFFFAOYSA-N dl-pseudophenylpropanolamine Natural products CC(N)C(O)C1=CC=CC=C1 DLNKOYKMWOXYQA-UHFFFAOYSA-N 0.000 claims description 4
- 229960002179 ephedrine Drugs 0.000 claims description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 4
- 229960001022 fenoterol Drugs 0.000 claims description 4
- 229960001268 isoetarine Drugs 0.000 claims description 4
- 229960001317 isoprenaline Drugs 0.000 claims description 4
- LMOINURANNBYCM-UHFFFAOYSA-N metaproterenol Chemical compound CC(C)NCC(O)C1=CC(O)=CC(O)=C1 LMOINURANNBYCM-UHFFFAOYSA-N 0.000 claims description 4
- PLPRGLOFPNJOTN-UHFFFAOYSA-N narcotine Natural products COc1ccc2C(OC(=O)c2c1OC)C3Cc4c(CN3C)cc5OCOc5c4OC PLPRGLOFPNJOTN-UHFFFAOYSA-N 0.000 claims description 4
- 229960004708 noscapine Drugs 0.000 claims description 4
- 229960002657 orciprenaline Drugs 0.000 claims description 4
- 229960001802 phenylephrine Drugs 0.000 claims description 4
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 claims description 4
- 229960000395 phenylpropanolamine Drugs 0.000 claims description 4
- DLNKOYKMWOXYQA-APPZFPTMSA-N phenylpropanolamine Chemical compound C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 claims description 4
- 229960005414 pirbuterol Drugs 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 4
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 4
- 102000004169 proteins and genes Human genes 0.000 claims description 4
- 108090000623 proteins and genes Proteins 0.000 claims description 4
- 229960001457 rimiterol Drugs 0.000 claims description 4
- IYMMESGOJVNCKV-SKDRFNHKSA-N rimiterol Chemical compound C([C@@H]1[C@@H](O)C=2C=C(O)C(O)=CC=2)CCCN1 IYMMESGOJVNCKV-SKDRFNHKSA-N 0.000 claims description 4
- IXTCZMJQGGONPY-XJAYAHQCSA-N rofleponide Chemical compound C1([C@@H](F)C2)=CC(=O)CC[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3O[C@@H](CCC)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O IXTCZMJQGGONPY-XJAYAHQCSA-N 0.000 claims description 4
- 229950004432 rofleponide Drugs 0.000 claims description 4
- 229940065721 systemic for obstructive airway disease xanthines Drugs 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical compound O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 claims description 4
- 229940110309 tiotropium Drugs 0.000 claims description 4
- 229960000859 tulobuterol Drugs 0.000 claims description 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 3
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 3
- 208000006673 asthma Diseases 0.000 claims description 3
- 206010057190 Respiratory tract infections Diseases 0.000 claims description 2
- 208000011479 upper respiratory tract disease Diseases 0.000 claims description 2
- 229940092705 beclomethasone Drugs 0.000 claims 6
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 claims 6
- QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- ULSIYEODSMZIPX-UHFFFAOYSA-N phenylethanolamine Chemical class NCC(O)C1=CC=CC=C1 ULSIYEODSMZIPX-UHFFFAOYSA-N 0.000 claims 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 164
- 229960001375 lactose Drugs 0.000 description 103
- 229960004977 anhydrous lactose Drugs 0.000 description 61
- 238000003860 storage Methods 0.000 description 41
- 150000004682 monohydrates Chemical class 0.000 description 32
- 239000002245 particle Substances 0.000 description 32
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 24
- 239000010419 fine particle Substances 0.000 description 21
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 19
- 230000008859 change Effects 0.000 description 18
- 229960001021 lactose monohydrate Drugs 0.000 description 15
- 239000002274 desiccant Substances 0.000 description 13
- 239000000463 material Substances 0.000 description 13
- 230000000704 physical effect Effects 0.000 description 13
- 238000004519 manufacturing process Methods 0.000 description 11
- 239000004480 active ingredient Substances 0.000 description 10
- 238000011049 filling Methods 0.000 description 10
- 150000002597 lactoses Chemical class 0.000 description 10
- 239000002585 base Substances 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- 230000000694 effects Effects 0.000 description 8
- 230000018044 dehydration Effects 0.000 description 7
- 238000006297 dehydration reaction Methods 0.000 description 7
- 239000000126 substance Substances 0.000 description 6
- GUBGYTABKSRVRQ-DCSYEGIMSA-N Beta-Lactose Chemical compound OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-DCSYEGIMSA-N 0.000 description 5
- 230000007613 environmental effect Effects 0.000 description 5
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- 230000000241 respiratory effect Effects 0.000 description 5
- 229940021597 salmeterol and fluticasone Drugs 0.000 description 5
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- 229930195724 β-lactose Natural products 0.000 description 5
- 238000004817 gas chromatography Methods 0.000 description 4
- 230000001965 increasing effect Effects 0.000 description 4
- 210000004072 lung Anatomy 0.000 description 4
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- 238000001179 sorption measurement Methods 0.000 description 4
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- 238000002411 thermogravimetry Methods 0.000 description 4
- 238000012384 transportation and delivery Methods 0.000 description 4
- 238000011282 treatment Methods 0.000 description 4
- RQBBDIIWJKBGAP-UHFFFAOYSA-N 1-hydroxy-4-[[2-hydroxy-5-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenyl]methyl]naphthalene-2-carboxylic acid Chemical compound C=1C=C(O)C(CC=2C3=CC=CC=C3C(O)=C(C(O)=O)C=2)=CC=1C(O)CNCCCCCCOCCCCC1=CC=CC=C1 RQBBDIIWJKBGAP-UHFFFAOYSA-N 0.000 description 3
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- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
- 229930195727 α-lactose Natural products 0.000 description 3
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- 239000004812 Fluorinated ethylene propylene Substances 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
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- 238000004458 analytical method Methods 0.000 description 2
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- 238000002144 chemical decomposition reaction Methods 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
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- 238000000113 differential scanning calorimetry Methods 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- VLARUOGDXDTHEH-UHFFFAOYSA-L disodium cromoglycate Chemical compound [Na+].[Na+].O1C(C([O-])=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C([O-])=O)O2 VLARUOGDXDTHEH-UHFFFAOYSA-L 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 229920000840 ethylene tetrafluoroethylene copolymer Polymers 0.000 description 2
- 230000001747 exhibiting effect Effects 0.000 description 2
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- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[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 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- GMVPRGQOIOIIMI-DWKJAMRDSA-N prostaglandin E1 Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(O)=O GMVPRGQOIOIIMI-DWKJAMRDSA-N 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 206010039083 rhinitis Diseases 0.000 description 1
- 239000005060 rubber Substances 0.000 description 1
- 231100000279 safety data Toxicity 0.000 description 1
- CQRYARSYNCAZFO-UHFFFAOYSA-N salicyl alcohol Chemical compound OCC1=CC=CC=C1O CQRYARSYNCAZFO-UHFFFAOYSA-N 0.000 description 1
- 239000000523 sample Substances 0.000 description 1
- DEIYFTQMQPDXOT-UHFFFAOYSA-N sildenafil citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 DEIYFTQMQPDXOT-UHFFFAOYSA-N 0.000 description 1
- 229960002639 sildenafil citrate Drugs 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000012385 systemic delivery Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
- 229940040944 tetracyclines Drugs 0.000 description 1
- BFKJFAAPBSQJPD-UHFFFAOYSA-N tetrafluoroethene Chemical group FC(F)=C(F)F BFKJFAAPBSQJPD-UHFFFAOYSA-N 0.000 description 1
- 238000002076 thermal analysis method Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 229960001540 vardenafil hydrochloride Drugs 0.000 description 1
- 239000011800 void material Substances 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 238000004804 winding Methods 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- 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
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Otolaryngology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51507703P | 2003-10-28 | 2003-10-28 | |
| US60/515,077 | 2003-10-28 | ||
| PCT/US2004/035129 WO2005044187A2 (en) | 2003-10-28 | 2004-10-22 | Inhalable pharmaceutical formulations employing lactose anhydrate and methods of administering the same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2543482A1 true CA2543482A1 (en) | 2005-05-19 |
Family
ID=34572801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002543482A Abandoned CA2543482A1 (en) | 2003-10-28 | 2004-10-22 | Inhalable pharmaceutical formulations employing lactose anhydrate and methods of administering the same |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20070053843A1 (https=) |
| EP (1) | EP1686960A4 (https=) |
| JP (1) | JP2007509941A (https=) |
| CA (1) | CA2543482A1 (https=) |
| IL (1) | IL175032A0 (https=) |
| WO (1) | WO2005044187A2 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0501956D0 (en) * | 2005-01-31 | 2005-03-09 | Arrow Internat | Nebulizer formulation |
| GB0520794D0 (en) * | 2005-10-12 | 2005-11-23 | Innovata Biomed Ltd | Inhaler |
| CN101744792B (zh) * | 2008-12-17 | 2013-04-17 | 张凯 | 氟替卡松丙酸酯和沙美特罗昔萘酸酯复方干粉吸入剂及其制备工艺 |
| US9925282B2 (en) | 2009-01-29 | 2018-03-27 | The General Hospital Corporation | Cromolyn derivatives and related methods of imaging and treatment |
| US8834931B2 (en) | 2009-12-25 | 2014-09-16 | Mahmut Bilgic | Dry powder formulation containing tiotropium for inhalation |
| TR200909788A2 (tr) * | 2009-12-25 | 2011-07-21 | Bi̇lgi̇ç Mahmut | Tiotropyum içeren inhalasyona uygun kuru toz formülasyonu |
| EP2533765A2 (en) * | 2010-01-29 | 2012-12-19 | Mahmut Bilgic | Pharmaceutical compositions comprising formoterol and mometasone |
| TR201000685A2 (tr) * | 2010-01-29 | 2011-08-22 | Bi̇lgi̇ç Mahmut | Salmeterol ve flutikazon içeren farmasötik preparatlar. |
| US10105316B2 (en) | 2012-07-05 | 2018-10-23 | Arven llac Sanayi Ve Ticaret A.S. | Inhalation compositions comprising muscarinic receptor antagonist |
| WO2014007770A2 (en) * | 2012-07-05 | 2014-01-09 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Inhalation compositions comprising corticosteroid and sorbitol |
| US10111957B2 (en) | 2012-07-05 | 2018-10-30 | Arven Ilac Snayi ve Ticaret A.S. | Inhalation compositions comprising glucose anhydrous |
| AU2014261538A1 (en) * | 2013-04-29 | 2015-12-10 | Sanofi Sa | Inhalable pharmaceutical compositions and the inhaler devices containing them |
| TW201516023A (zh) | 2013-09-30 | 2015-05-01 | Daiichi Sankyo Co Ltd | 使用噴霧乾燥法之Ｄ－甘露醇α型結晶之選擇性製造方法 |
| CN110305095A (zh) * | 2013-10-22 | 2019-10-08 | 综合医院公司 | 色甘酸衍生物以及成像和治疗的相关方法 |
| WO2016037166A1 (en) * | 2014-09-07 | 2016-03-10 | Yu Zhang | Novel anti-oxidant compositions and methods of delivery |
| MX392636B (es) | 2014-10-31 | 2025-03-24 | Glaxosmithkline Ip Dev Ltd | Formulacion en polvo. |
| JP2019524865A (ja) | 2016-08-31 | 2019-09-05 | ザ ジェネラル ホスピタル コーポレイション | 神経変性疾患と関連する神経炎症におけるマクロファージ／ミクログリア |
| MX2021006869A (es) | 2018-12-10 | 2021-07-02 | Massachusetts Gen Hospital | Esteres de cromolin y usos de los mismos. |
| WO2021207060A1 (en) | 2020-04-06 | 2021-10-14 | The General Hospital Corporation | Methods of treatment of coronavirus-induced inflammation conditions |
| WO2022146914A1 (en) | 2020-12-28 | 2022-07-07 | The General Hospital Corporation | Cromolyn derivatives and uses thereof |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4778054A (en) * | 1982-10-08 | 1988-10-18 | Glaxo Group Limited | Pack for administering medicaments to patients |
| AU591152B2 (en) * | 1985-07-30 | 1989-11-30 | Glaxo Group Limited | Devices for administering medicaments to patients |
| US6536427B2 (en) * | 1990-03-02 | 2003-03-25 | Glaxo Group Limited | Inhalation device |
| GB9004781D0 (en) * | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| SK280968B6 (sk) * | 1990-03-02 | 2000-10-09 | Glaxo Group Limited | Balenie medikamentu na použite v inhalačnom prístroji |
| PE44995A1 (es) * | 1994-01-27 | 1995-12-18 | Schering Corp | Furoato de mometasona para el tratamiento de las enfermedades pulmonares y de las vias respiratorias |
| GB9404945D0 (en) * | 1994-03-15 | 1994-04-27 | Glaxo Group Ltd | Pharmaceutical composition |
| HU219899B (hu) * | 1995-04-14 | 2001-09-28 | Glaxo Wellcome Inc. | Inhalálóberendezés flutikaszon-propionát adagolására mért dózisban |
| TR199701169T1 (xx) * | 1995-04-14 | 1998-03-21 | Glaxo Wellcome Inc. | Salmeterol i�in �l��lm�� doz inhaleri. |
| US6258341B1 (en) * | 1995-04-14 | 2001-07-10 | Inhale Therapeutic Systems, Inc. | Stable glassy state powder formulations |
| TR199701170T1 (xx) * | 1995-04-14 | 1998-02-21 | Glaxo Wellcome Inc. | Beklometazon dipropionat i�in �l��lm�� doz inhaleri. |
| HU219900B (hu) * | 1995-04-14 | 2001-09-28 | Glaxo Wellcome Inc. | Mért dózist adagoló inhalálóberendezés |
| GB9606188D0 (en) * | 1996-03-23 | 1996-05-29 | Danbiosyst Uk | Pollysaccharide microspheres for the pulmonary delivery of drugs |
| GB9626960D0 (en) * | 1996-12-27 | 1997-02-12 | Glaxo Group Ltd | Valve for aerosol container |
| GB9700226D0 (en) * | 1997-01-08 | 1997-02-26 | Glaxo Group Ltd | Inhalation device |
| US6495167B2 (en) * | 1997-03-20 | 2002-12-17 | Schering Corporation | Preparation of powder agglomerates |
| WO1998041193A1 (en) * | 1997-03-20 | 1998-09-24 | Schering Corporation | Preparation of powder agglomerates |
| EP0876814A1 (en) * | 1997-05-07 | 1998-11-11 | "PHARLYSE", Société Anonyme | Dry powder inhaler excipient, process for its preparation and pharmaceutical compositions containing it |
| TW533865U (en) * | 1997-06-10 | 2003-05-21 | Glaxo Group Ltd | Dispenser for dispensing medicament and actuation indicating device |
| GB2329939A (en) * | 1997-06-26 | 1999-04-07 | Glaxo Group Ltd | Self-lubricating valve stem for aerosol containers |
| PL200941B1 (pl) * | 1998-11-13 | 2009-02-27 | Jagotec Ag | Suchy proszkowy preparat inhalacyjny |
| US6390291B1 (en) * | 1998-12-18 | 2002-05-21 | Smithkline Beecham Corporation | Method and package for storing a pressurized container containing a drug |
| DK1292303T3 (da) * | 2000-02-17 | 2004-09-06 | Teva Pharma | Stabil farmaceutisk formulering omfattende torsemidmodifikation II |
-
2004
- 2004-10-22 JP JP2006538128A patent/JP2007509941A/ja active Pending
- 2004-10-22 CA CA002543482A patent/CA2543482A1/en not_active Abandoned
- 2004-10-22 WO PCT/US2004/035129 patent/WO2005044187A2/en not_active Ceased
- 2004-10-22 US US10/595,449 patent/US20070053843A1/en not_active Abandoned
- 2004-10-22 EP EP04796175A patent/EP1686960A4/en not_active Withdrawn
-
2006
- 2006-04-20 IL IL175032A patent/IL175032A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL175032A0 (en) | 2008-04-13 |
| US20070053843A1 (en) | 2007-03-08 |
| WO2005044187A3 (en) | 2006-03-23 |
| WO2005044187A2 (en) | 2005-05-19 |
| EP1686960A2 (en) | 2006-08-09 |
| EP1686960A4 (en) | 2007-03-07 |
| JP2007509941A (ja) | 2007-04-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |