ES2859629T3 - Formulaciones mejoradas - Google Patents
Formulaciones mejoradas Download PDFInfo
- Publication number
- ES2859629T3 ES2859629T3 ES10768760T ES10768760T ES2859629T3 ES 2859629 T3 ES2859629 T3 ES 2859629T3 ES 10768760 T ES10768760 T ES 10768760T ES 10768760 T ES10768760 T ES 10768760T ES 2859629 T3 ES2859629 T3 ES 2859629T3
- Authority
- ES
- Spain
- Prior art keywords
- fluticasone propionate
- formoterol fumarate
- micrograms
- total weight
- hfa
- 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.)
- Active
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 143
- 238000009472 formulation Methods 0.000 title claims abstract description 120
- 239000000443 aerosol Substances 0.000 claims abstract description 66
- 239000000725 suspension Substances 0.000 claims abstract description 64
- 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 abstract description 63
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 57
- 229960000289 fluticasone propionate Drugs 0.000 claims abstract description 56
- 239000002245 particle Substances 0.000 claims abstract description 52
- RATSWNOMCHFQGJ-TUYNVFRMSA-N (e)-but-2-enedioic acid;n-[2-hydroxy-5-[(1s)-1-hydroxy-2-[[(2s)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide;dihydrate Chemical compound O.O.OC(=O)\C=C\C(O)=O.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1 RATSWNOMCHFQGJ-TUYNVFRMSA-N 0.000 claims abstract description 36
- 229960003610 formoterol fumarate dihydrate Drugs 0.000 claims abstract description 36
- 239000000080 wetting agent Substances 0.000 claims abstract description 27
- 229940071648 metered dose inhaler Drugs 0.000 claims abstract description 26
- 230000008021 deposition Effects 0.000 claims abstract description 18
- 239000003380 propellant Substances 0.000 claims abstract description 17
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims abstract description 15
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 12
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 claims abstract description 5
- 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 claims description 40
- 238000009826 distribution Methods 0.000 claims description 22
- 229960000265 cromoglicic acid Drugs 0.000 claims description 21
- YFMFNYKEUDLDTL-UHFFFAOYSA-N 1,1,1,2,3,3,3-heptafluoropropane Chemical group FC(F)(F)C(F)C(F)(F)F YFMFNYKEUDLDTL-UHFFFAOYSA-N 0.000 claims description 17
- 239000010419 fine particle Substances 0.000 claims description 14
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 7
- 208000006673 asthma Diseases 0.000 claims description 7
- 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 6
- 239000000843 powder Substances 0.000 claims description 6
- 229960002052 salbutamol Drugs 0.000 claims description 6
- 238000011282 treatment Methods 0.000 claims description 6
- RQTOOFIXOKYGAN-UHFFFAOYSA-N nedocromil Chemical compound CCN1C(C(O)=O)=CC(=O)C2=C1C(CCC)=C1OC(C(O)=O)=CC(=O)C1=C2 RQTOOFIXOKYGAN-UHFFFAOYSA-N 0.000 claims description 4
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 claims description 3
- NDAUXUAQIAJITI-LBPRGKRZSA-N (R)-salbutamol Chemical compound CC(C)(C)NC[C@H](O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-LBPRGKRZSA-N 0.000 claims description 3
- 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 3
- 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 3
- 229960001022 fenoterol Drugs 0.000 claims description 3
- 229950008204 levosalbutamol Drugs 0.000 claims description 3
- 229960005414 pirbuterol Drugs 0.000 claims description 3
- 229960002720 reproterol Drugs 0.000 claims description 3
- 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 3
- 229940127211 short-acting beta 2 agonist Drugs 0.000 claims description 3
- 229960000195 terbutaline Drugs 0.000 claims description 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 2
- 201000010105 allergic rhinitis Diseases 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims description 2
- OBRNDARFFFHCGE-PERKLWIXSA-N (S,S)-formoterol fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1 OBRNDARFFFHCGE-PERKLWIXSA-N 0.000 claims 24
- 229960000193 formoterol fumarate Drugs 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 4
- 229960004398 nedocromil Drugs 0.000 claims 2
- 229940088679 drug related substance Drugs 0.000 description 27
- 229940079593 drug Drugs 0.000 description 21
- 239000003814 drug Substances 0.000 description 21
- 239000008186 active pharmaceutical agent Substances 0.000 description 19
- 238000000151 deposition Methods 0.000 description 17
- 238000000034 method Methods 0.000 description 13
- 238000012360 testing method Methods 0.000 description 13
- 238000003860 storage Methods 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- 238000004519 manufacturing process Methods 0.000 description 8
- 230000000694 effects Effects 0.000 description 6
- 210000004072 lung Anatomy 0.000 description 6
- 239000000463 material Substances 0.000 description 6
- 238000000576 coating method Methods 0.000 description 5
- -1 polyoxyethylene Polymers 0.000 description 5
- 230000007928 solubilization Effects 0.000 description 5
- 238000005063 solubilization Methods 0.000 description 5
- 239000013078 crystal Substances 0.000 description 4
- 238000011049 filling Methods 0.000 description 4
- 238000013101 initial test Methods 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- 230000036961 partial effect Effects 0.000 description 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 239000004094 surface-active agent Substances 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 229960002714 fluticasone Drugs 0.000 description 3
- 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 description 3
- 229960002848 formoterol Drugs 0.000 description 3
- 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 description 3
- 239000007788 liquid Substances 0.000 description 3
- 229910052751 metal Inorganic materials 0.000 description 3
- 239000002184 metal Substances 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- UDOFUJZUXCZXKD-VYAAASJMSA-N s-(fluoromethyl) (6s,8s,9r,10s,11s,13s,14s,16r,17r)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-17-carbothioate;n-[2-hydroxy-5-[1-hydroxy-2-[1-(4-methoxyphenyl)propan-2-ylamino]ethyl]phenyl Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1.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 UDOFUJZUXCZXKD-VYAAASJMSA-N 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
- 229910000838 Al alloy Inorganic materials 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 239000005642 Oleic acid Substances 0.000 description 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 2
- 238000001016 Ostwald ripening Methods 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 230000001070 adhesive effect Effects 0.000 description 2
- 239000000556 agonist Substances 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000003246 corticosteroid Substances 0.000 description 2
- 238000002788 crimping Methods 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 229920002313 fluoropolymer Polymers 0.000 description 2
- 238000012395 formulation development Methods 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- 230000007062 hydrolysis Effects 0.000 description 2
- 238000006460 hydrolysis reaction Methods 0.000 description 2
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 2
- 239000012633 leachable Substances 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 150000002739 metals Chemical class 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- 239000008249 pharmaceutical aerosol Substances 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 230000002000 scavenging effect Effects 0.000 description 2
- 230000006641 stabilisation Effects 0.000 description 2
- 238000011105 stabilization Methods 0.000 description 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- PFWLFWPASULGAN-UHFFFAOYSA-N 7-methylxanthine Chemical compound N1C(=O)NC(=O)C2=C1N=CN2C PFWLFWPASULGAN-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 description 1
- LUKZNWIVRBCLON-GXOBDPJESA-N Ciclesonide Chemical compound C1([C@H]2O[C@@]3([C@H](O2)C[C@@H]2[C@@]3(C[C@H](O)[C@@H]3[C@@]4(C)C=CC(=O)C=C4CC[C@H]32)C)C(=O)COC(=O)C(C)C)CCCCC1 LUKZNWIVRBCLON-GXOBDPJESA-N 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 229920011250 Polypropylene Block Copolymer Polymers 0.000 description 1
- 229920001213 Polysorbate 20 Polymers 0.000 description 1
- 229920001214 Polysorbate 60 Polymers 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical group CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- 239000004147 Sorbitan trioleate Substances 0.000 description 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 238000002441 X-ray diffraction Methods 0.000 description 1
- 229960004308 acetylcysteine Drugs 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 238000011374 additional therapy Methods 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 208000016709 aortopulmonary window Diseases 0.000 description 1
- 229960004814 apaflurane Drugs 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 238000013475 authorization Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
- 229940124748 beta 2 agonist Drugs 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229920001400 block copolymer Polymers 0.000 description 1
- 229940124630 bronchodilator Drugs 0.000 description 1
- 229960004436 budesonide Drugs 0.000 description 1
- 239000012876 carrier material Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 1
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 1
- 229960003728 ciclesonide Drugs 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 238000007599 discharging Methods 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 230000005713 exacerbation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 229960000676 flunisolide Drugs 0.000 description 1
- 239000004811 fluoropolymer Substances 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 230000008642 heat stress Effects 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 230000003301 hydrolyzing effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 229940125369 inhaled corticosteroids Drugs 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 238000010902 jet-milling Methods 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 150000002617 leukotrienes Chemical class 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 229960002744 mometasone furoate Drugs 0.000 description 1
- WOFMFGQZHJDGCX-ZULDAHANSA-N mometasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(Cl)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@H]1C)C(=O)CCl)C(=O)C1=CC=CO1 WOFMFGQZHJDGCX-ZULDAHANSA-N 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229960002969 oleic acid Drugs 0.000 description 1
- 235000021313 oleic acid Nutrition 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000007971 pharmaceutical suspension Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 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 description 1
- 239000002516 radical scavenger Substances 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 238000009666 routine test Methods 0.000 description 1
- 238000009781 safety test method Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 239000013049 sediment Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000012439 solid excipient Substances 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 230000035882 stress Effects 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
- 229960005294 triamcinolone Drugs 0.000 description 1
- 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 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 238000009736 wetting 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
- A61K9/008—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]
-
- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0918150.4A GB0918150D0 (en) | 2009-10-16 | 2009-10-16 | Improved formulations |
| PCT/EP2010/065569 WO2011045429A1 (en) | 2009-10-16 | 2010-10-15 | Improved formulations |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2859629T3 true ES2859629T3 (es) | 2021-10-04 |
Family
ID=41462451
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10768760T Active ES2859629T3 (es) | 2009-10-16 | 2010-10-15 | Formulaciones mejoradas |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20120263766A1 (enExample) |
| EP (2) | EP2488157B1 (enExample) |
| JP (2) | JP5818801B2 (enExample) |
| CN (1) | CN102573791B (enExample) |
| AU (1) | AU2010305695B2 (enExample) |
| BR (1) | BR112012008969B1 (enExample) |
| CA (1) | CA2776845C (enExample) |
| CL (1) | CL2012000948A1 (enExample) |
| CY (1) | CY1123918T1 (enExample) |
| DK (1) | DK2488157T3 (enExample) |
| ES (1) | ES2859629T3 (enExample) |
| GB (1) | GB0918150D0 (enExample) |
| HR (1) | HRP20210379T1 (enExample) |
| HU (1) | HUE054030T2 (enExample) |
| IL (2) | IL219162A0 (enExample) |
| LT (1) | LT2488157T (enExample) |
| MX (1) | MX372991B (enExample) |
| NZ (1) | NZ599900A (enExample) |
| PL (1) | PL2488157T3 (enExample) |
| PT (1) | PT2488157T (enExample) |
| RS (1) | RS61430B1 (enExample) |
| SI (1) | SI2488157T1 (enExample) |
| SM (1) | SMT202100150T1 (enExample) |
| WO (1) | WO2011045429A1 (enExample) |
| ZA (1) | ZA201202595B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100496608C (zh) * | 2001-03-30 | 2009-06-10 | 洁垢技术有限公司 | 药用气溶胶制剂 |
| GB0323684D0 (en) | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
| GB0918149D0 (en) * | 2009-10-16 | 2009-12-02 | Jagotec Ag | Improved medicinal aerosol formulation |
| GB0918150D0 (en) * | 2009-10-16 | 2009-12-02 | Jagotec Ag | Improved formulations |
| WO2013127738A1 (de) * | 2012-02-28 | 2013-09-06 | Boehringer Ingelheim International Gmbh | Neue treibgashaltige tiotropium-formulierung |
| RU2678992C2 (ru) | 2012-04-11 | 2019-02-05 | Сипла Лимитед | Фармацевтическая композиция, содержащая арформотерол и флутиказона фуроат |
| GB201321712D0 (en) * | 2013-12-09 | 2014-01-22 | Pharmachemie Bv | Dry Powder Inhaler |
| CN105963282B (zh) * | 2016-05-04 | 2019-04-19 | 四川普锐特医药科技有限责任公司 | 一种医用定量吸入气雾剂 |
| WO2018059390A1 (zh) * | 2016-09-29 | 2018-04-05 | 广东东阳光药业有限公司 | 药物组合物 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6596260B1 (en) | 1993-08-27 | 2003-07-22 | Novartis Corporation | Aerosol container and a method for storage and administration of a predetermined amount of a pharmaceutically active aerosol |
| EP1366777B1 (en) | 1995-04-14 | 2005-06-15 | SmithKline Beecham Corporation | Metered dose inhaler for salmeterol |
| DE69622166T2 (de) | 1995-04-14 | 2003-04-03 | Smithkline Beecham Corp., Philadelphia | Dosierinhalator für albuterol |
| JPH101442A (ja) * | 1996-06-12 | 1998-01-06 | Taisho Pharmaceut Co Ltd | 鼻炎用点鼻薬 |
| EP1393721B1 (en) * | 1997-03-20 | 2008-11-26 | Schering Corporation | Dosage form of powder agglomerates |
| GB9903759D0 (en) * | 1999-02-18 | 1999-04-14 | Novartis Ag | Organic compounds |
| EE05167B1 (et) * | 2000-05-22 | 2009-06-15 | Chiesi Farmaceutici S.P.A. | Stabiilsed farmatseutilised lahuspreparaadid survestatud doseerivatele inhalaatoritele |
| US20060257324A1 (en) * | 2000-05-22 | 2006-11-16 | Chiesi Farmaceutici S.P.A. | Pharmaceutical solution formulations for pressurised metered dose inhalers |
| AU2001289126A1 (en) | 2000-09-18 | 2002-04-02 | Glaxo Group Limited | Metered dose inhaler can coated two or more times with fluorocarbon polymers |
| CN1635870A (zh) * | 2000-10-09 | 2005-07-06 | 3M创新有限公司 | 药用气雾剂制剂 |
| CN100496608C (zh) * | 2001-03-30 | 2009-06-10 | 洁垢技术有限公司 | 药用气溶胶制剂 |
| US6667344B2 (en) * | 2001-04-17 | 2003-12-23 | Dey, L.P. | Bronchodilating compositions and methods |
| GB0201400D0 (en) * | 2002-01-22 | 2002-03-13 | Glaxo Group Ltd | Novel apparatus and process |
| EP1531866A1 (en) * | 2002-08-29 | 2005-05-25 | Cipla Ltd. | Pharmaceutical products and compositions comprising specific anticholinergic agents, beta-2 agonists and corticosteroids |
| GB0323684D0 (en) * | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
| GB0327727D0 (en) * | 2003-11-28 | 2003-12-31 | Quadrant Drug Delivery Ltd | Viral microparticles |
| GB0410399D0 (en) * | 2004-05-10 | 2004-06-16 | Arakis Ltd | The treatment of respiratory disease |
| GB0918150D0 (en) * | 2009-10-16 | 2009-12-02 | Jagotec Ag | Improved formulations |
-
2009
- 2009-10-16 GB GBGB0918150.4A patent/GB0918150D0/en not_active Ceased
-
2010
- 2010-10-15 AU AU2010305695A patent/AU2010305695B2/en active Active
- 2010-10-15 CN CN201080046305.6A patent/CN102573791B/zh active Active
- 2010-10-15 RS RS20210159A patent/RS61430B1/sr unknown
- 2010-10-15 NZ NZ599900A patent/NZ599900A/en unknown
- 2010-10-15 US US13/502,097 patent/US20120263766A1/en not_active Abandoned
- 2010-10-15 HR HRP20210379TT patent/HRP20210379T1/hr unknown
- 2010-10-15 WO PCT/EP2010/065569 patent/WO2011045429A1/en not_active Ceased
- 2010-10-15 PT PT107687600T patent/PT2488157T/pt unknown
- 2010-10-15 LT LTEP10768760.0T patent/LT2488157T/lt unknown
- 2010-10-15 MX MX2012004338A patent/MX372991B/es active IP Right Grant
- 2010-10-15 HU HUE10768760A patent/HUE054030T2/hu unknown
- 2010-10-15 SM SM20210150T patent/SMT202100150T1/it unknown
- 2010-10-15 JP JP2012533648A patent/JP5818801B2/ja active Active
- 2010-10-15 ES ES10768760T patent/ES2859629T3/es active Active
- 2010-10-15 EP EP10768760.0A patent/EP2488157B1/en active Active
- 2010-10-15 BR BR112012008969-2A patent/BR112012008969B1/pt active IP Right Grant
- 2010-10-15 SI SI201032050T patent/SI2488157T1/sl unknown
- 2010-10-15 DK DK10768760.0T patent/DK2488157T3/da active
- 2010-10-15 CA CA2776845A patent/CA2776845C/en active Active
- 2010-10-15 PL PL10768760T patent/PL2488157T3/pl unknown
- 2010-10-15 EP EP20213235.3A patent/EP3811928A1/en not_active Withdrawn
-
2012
- 2012-04-11 ZA ZA2012/02595A patent/ZA201202595B/en unknown
- 2012-04-13 CL CL2012000948A patent/CL2012000948A1/es unknown
- 2012-04-15 IL IL219162A patent/IL219162A0/en unknown
-
2015
- 2015-09-29 JP JP2015191177A patent/JP2016040286A/ja active Pending
-
2017
- 2017-03-21 US US15/464,879 patent/US20180296468A2/en not_active Abandoned
-
2019
- 2019-09-15 IL IL26936919A patent/IL269369A/en unknown
-
2021
- 2021-03-05 CY CY20211100190T patent/CY1123918T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20230364015A1 (en) | Process for providing particles with reduced electrostatic charges | |
| ES2468840T7 (es) | Terapia combinada para EPOC | |
| EP2488157B1 (en) | Improved formulations | |
| JP5289306B2 (ja) | 加圧式定量噴霧吸入器用の薬学的溶液製剤 | |
| ES2687345T3 (es) | Composición de solución en aerosol presurizado estable de una combinación de bromuro de glucopirronio y formoterol | |
| AU2023201307A1 (en) | Dry powder treprostinil for the treatment of pulmonary hypertension | |
| ES2526685T3 (es) | Medicamento inhalable que comprende tiotropio | |
| ES2472268T3 (es) | Formulaciones de aerosol que comprenden fumarato de formoterol dihidratado, un propelente, etanol y opcionalmente un esteroide, en las que el fumarato de formoterol dihidratado tiene un contenido de agua del 4,8-4,28% en peso | |
| ES2613754T3 (es) | Uso de glicopirrolato para tratar la taquicardia | |
| BR112015010601B1 (pt) | Composição farmacêutica e uso da composição | |
| ES2775606T3 (es) | Furoato de fluticasona en el tratamiento de la EPOC | |
| CN105101955A (zh) | 至少包含两种通过喷雾干燥以增加制剂稳定性而得到的干粉的组合物 | |
| CN107205936A (zh) | 包含至少一种通过喷雾干燥得到的增加制剂稳定性的干粉的组合物 | |
| ES2568913T3 (es) | Formulaciones farmacéuticas en aerosol de formoterol y dipropionato de beclometasona | |
| ES2973882T3 (es) | Formulaciones medicinales en aerosol mejoradas | |
| WO2017089404A1 (en) | Pharmaceutical composition | |
| AU2013203244B2 (en) | Improved formulations | |
| EA015353B1 (ru) | Применение солей тиотропия для лечения персистирующей астмы средней тяжести | |
| ES2701525T3 (es) | Un procedimiento para la preparación de formulaciones para inhalación | |
| HK1173076B (en) | Improved formulations | |
| HK1173076A (en) | Improved formulations |