CA2303132C - Formulation intranasale contenant de la scopolamine et methode de traitement du mal des transports - Google Patents
Formulation intranasale contenant de la scopolamine et methode de traitement du mal des transports Download PDFInfo
- Publication number
- CA2303132C CA2303132C CA002303132A CA2303132A CA2303132C CA 2303132 C CA2303132 C CA 2303132C CA 002303132 A CA002303132 A CA 002303132A CA 2303132 A CA2303132 A CA 2303132A CA 2303132 C CA2303132 C CA 2303132C
- Authority
- CA
- Canada
- Prior art keywords
- formulation
- scopolamine
- intranasal
- upright
- inverted
- 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
- 239000000203 mixture Substances 0.000 title claims abstract description 216
- 238000009472 formulation Methods 0.000 title claims abstract description 190
- 229960002646 scopolamine Drugs 0.000 title claims abstract description 73
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 title claims abstract description 72
- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 title claims abstract description 72
- 229930000680 A04AD01 - Scopolamine Natural products 0.000 title claims abstract description 71
- 201000003152 motion sickness Diseases 0.000 title claims abstract description 15
- STECJAGHUSJQJN-FWXGHANASA-N scopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-FWXGHANASA-N 0.000 title claims abstract 8
- 238000000034 method Methods 0.000 title description 5
- 239000004372 Polyvinyl alcohol Substances 0.000 claims abstract description 66
- 229920002451 polyvinyl alcohol Polymers 0.000 claims abstract description 66
- 150000003839 salts Chemical class 0.000 claims abstract description 18
- 239000003349 gelling agent Substances 0.000 claims abstract description 17
- 229960004499 scopolamine hydrobromide Drugs 0.000 claims abstract description 16
- WTGQALLALWYDJH-MOUKNHLCSA-N scopolamine hydrobromide (anhydrous) Chemical compound Br.C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 WTGQALLALWYDJH-MOUKNHLCSA-N 0.000 claims abstract description 16
- 206010028813 Nausea Diseases 0.000 claims abstract description 12
- 230000008693 nausea Effects 0.000 claims abstract description 12
- 206010047700 Vomiting Diseases 0.000 claims abstract description 11
- 230000008673 vomiting Effects 0.000 claims abstract description 11
- 239000003937 drug carrier Substances 0.000 claims abstract description 10
- 239000000227 bioadhesive Substances 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 8
- 230000036470 plasma concentration Effects 0.000 claims description 8
- 239000003755 preservative agent Substances 0.000 claims description 8
- 239000004094 surface-active agent Substances 0.000 claims description 8
- 229920001661 Chitosan Polymers 0.000 claims description 7
- 235000010443 alginic acid Nutrition 0.000 claims description 7
- 229920000615 alginic acid Polymers 0.000 claims description 7
- 239000002562 thickening agent Substances 0.000 claims description 7
- 229920002307 Dextran Polymers 0.000 claims description 6
- 229920002472 Starch Polymers 0.000 claims description 6
- 239000003623 enhancer Substances 0.000 claims description 6
- 229920000058 polyacrylate Polymers 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- 208000024891 symptom Diseases 0.000 claims description 6
- 239000012458 free base Substances 0.000 claims description 4
- 230000002335 preservative effect Effects 0.000 claims description 4
- 239000000853 adhesive Substances 0.000 claims description 3
- 230000001070 adhesive effect Effects 0.000 claims description 3
- 239000003963 antioxidant agent Substances 0.000 claims description 3
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims 3
- 229940072056 alginate Drugs 0.000 claims 3
- 235000019846 buffering salt Nutrition 0.000 claims 3
- 229920000591 gum Polymers 0.000 claims 3
- 239000008107 starch Substances 0.000 claims 3
- 230000003078 antioxidant effect Effects 0.000 claims 2
- 239000006172 buffering agent Substances 0.000 claims 2
- 239000006184 cosolvent Substances 0.000 claims 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 abstract description 59
- 239000008194 pharmaceutical composition Substances 0.000 abstract description 3
- STECJAGHUSJQJN-VJQRDGCPSA-N chembl3084722 Chemical compound C1([C@@H](CO)C(=O)O[C@@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-VJQRDGCPSA-N 0.000 description 64
- 229940068984 polyvinyl alcohol Drugs 0.000 description 58
- 229920000609 methyl cellulose Polymers 0.000 description 25
- 239000001923 methylcellulose Substances 0.000 description 25
- 229960002900 methylcellulose Drugs 0.000 description 25
- 239000000047 product Substances 0.000 description 24
- 235000010981 methylcellulose Nutrition 0.000 description 23
- 239000003814 drug Substances 0.000 description 19
- 229940079593 drug Drugs 0.000 description 17
- 239000000872 buffer Substances 0.000 description 16
- 230000015556 catabolic process Effects 0.000 description 16
- 238000006731 degradation reaction Methods 0.000 description 16
- 239000002253 acid Substances 0.000 description 14
- 239000000499 gel Substances 0.000 description 14
- VBSTXRUAXCTZBQ-UHFFFAOYSA-N 1-hexyl-4-phenylpiperazine Chemical compound C1CN(CCCCCC)CCN1C1=CC=CC=C1 VBSTXRUAXCTZBQ-UHFFFAOYSA-N 0.000 description 13
- JACRWUWPXAESPB-QMMMGPOBSA-N Tropic acid Natural products OC[C@H](C(O)=O)C1=CC=CC=C1 JACRWUWPXAESPB-QMMMGPOBSA-N 0.000 description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 11
- 238000010521 absorption reaction Methods 0.000 description 11
- 229940100652 nasal gel Drugs 0.000 description 11
- LACQPOBCQQPVIT-SEYKEWMNSA-N scopolamine hydrobromide trihydrate Chemical compound O.O.O.Br.C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 LACQPOBCQQPVIT-SEYKEWMNSA-N 0.000 description 10
- 239000000243 solution Substances 0.000 description 10
- -1 salt Scopolamine Hydrobromide Chemical class 0.000 description 8
- 230000003247 decreasing effect Effects 0.000 description 6
- 239000007857 degradation product Substances 0.000 description 6
- 229960000686 benzalkonium chloride Drugs 0.000 description 5
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 5
- 229920002678 cellulose Polymers 0.000 description 5
- 239000001913 cellulose Substances 0.000 description 5
- 235000011187 glycerol Nutrition 0.000 description 5
- 101150064066 CTSL gene Proteins 0.000 description 4
- 241000124008 Mammalia Species 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 230000008859 change Effects 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 210000004379 membrane Anatomy 0.000 description 4
- 239000012528 membrane Substances 0.000 description 4
- 239000008213 purified water Substances 0.000 description 4
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 4
- 239000001509 sodium citrate Substances 0.000 description 4
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 4
- 229940001584 sodium metabisulfite Drugs 0.000 description 4
- 235000010262 sodium metabisulphite Nutrition 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 229960004106 citric acid Drugs 0.000 description 3
- 238000011835 investigation Methods 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 229960000999 sodium citrate dihydrate Drugs 0.000 description 3
- 230000002459 sustained effect Effects 0.000 description 3
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- 230000003444 anaesthetic effect Effects 0.000 description 2
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- 238000010494 dissociation reaction Methods 0.000 description 2
- 230000005593 dissociations Effects 0.000 description 2
- 239000003906 humectant Substances 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- MYWUZJCMWCOHBA-VIFPVBQESA-N methamphetamine Chemical compound CN[C@@H](C)CC1=CC=CC=C1 MYWUZJCMWCOHBA-VIFPVBQESA-N 0.000 description 2
- 210000002850 nasal mucosa Anatomy 0.000 description 2
- 239000007922 nasal spray Substances 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 235000010356 sorbitol Nutrition 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 241000220479 Acacia Species 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
- 229920002701 Polyoxyl 40 Stearate Polymers 0.000 description 1
- 241000220010 Rhode Species 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 208000012886 Vertigo Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000012670 alkaline solution Substances 0.000 description 1
- 125000000129 anionic group Chemical group 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 150000007514 bases Chemical class 0.000 description 1
- 239000003637 basic solution Substances 0.000 description 1
- 229960001716 benzalkonium Drugs 0.000 description 1
- CYDRXTMLKJDRQH-UHFFFAOYSA-N benzododecinium Chemical compound CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 CYDRXTMLKJDRQH-UHFFFAOYSA-N 0.000 description 1
- 239000003833 bile salt Substances 0.000 description 1
- 229940093761 bile salts Drugs 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000003093 cationic surfactant Substances 0.000 description 1
- 238000002144 chemical decomposition reaction Methods 0.000 description 1
- 229960004926 chlorobutanol Drugs 0.000 description 1
- BSQIVYOSLFLSGE-OZVSTBQFSA-N cid_657297 Chemical compound [O-][N+]([O-])=O.C1([C@@H](CO)C(=O)OC2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)C)=CC=CC=C1 BSQIVYOSLFLSGE-OZVSTBQFSA-N 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000010579 first pass effect Methods 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- LZCOQTDXKCNBEE-IKIFYQGPSA-N methscopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)C)=CC=CC=C1 LZCOQTDXKCNBEE-IKIFYQGPSA-N 0.000 description 1
- 229960001107 methscopolamine nitrate Drugs 0.000 description 1
- YLGXILFCIXHCMC-JHGZEJCSSA-N methyl cellulose Chemical compound COC1C(OC)C(OC)C(COC)O[C@H]1O[C@H]1C(OC)C(OC)C(OC)OC1COC YLGXILFCIXHCMC-JHGZEJCSSA-N 0.000 description 1
- 229960003730 methylcellulose (4000 cps) Drugs 0.000 description 1
- 229960001383 methylscopolamine Drugs 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 210000003097 mucus Anatomy 0.000 description 1
- 210000003928 nasal cavity Anatomy 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229940066429 octoxynol Drugs 0.000 description 1
- 229920002113 octoxynol Polymers 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 201000006302 peripheral vertigo Diseases 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 229960003424 phenylacetic acid Drugs 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229940099429 polyoxyl 40 stearate Drugs 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- JACRWUWPXAESPB-UHFFFAOYSA-N tropic acid Chemical compound OCC(C(O)=O)C1=CC=CC=C1 JACRWUWPXAESPB-UHFFFAOYSA-N 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Otolaryngology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
L'invention concerne des formulations pharmaceutiques contenant de la scopolamine, et plus particulièrement des formulations de gel intranasal comprenant du bromhydrate de scopolamine dans un excipient pharmaceutiquement acceptable, de préférence un gel intranasal. Cette formulation a un pH égal ou inférieur à environ 4,0, de préférence égal ou inférieur à 3,5 et une concentration en sel inférieure à environ 200 mM, et la solution de gel contient du poly[alcool de vinyle] comme agent gélifiant. Ces formulations intranasales sont particulièrement utiles pour la prévention et/ou le traitement des nausées et/ou des vomissements associés par exemple au mal des transports.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5865197P | 1997-09-11 | 1997-09-11 | |
| US60/058,651 | 1997-09-11 | ||
| PCT/US1998/018953 WO1999012544A1 (fr) | 1997-09-11 | 1998-09-11 | Formulation intranasale contenant de la scopolamine et methode de traitement du mal des transports |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2303132A1 CA2303132A1 (fr) | 1999-03-18 |
| CA2303132C true CA2303132C (fr) | 2002-07-09 |
Family
ID=22018094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002303132A Expired - Fee Related CA2303132C (fr) | 1997-09-11 | 1998-09-11 | Formulation intranasale contenant de la scopolamine et methode de traitement du mal des transports |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1027049A4 (fr) |
| JP (1) | JP2002516815A (fr) |
| AU (1) | AU742878B2 (fr) |
| CA (1) | CA2303132C (fr) |
| WO (1) | WO1999012544A1 (fr) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2423354C (fr) * | 2000-09-20 | 2009-12-15 | Lee Shahinian Jr. | Preparations et medications nasales, inhalables et ophtalmiques locales a conservation spontanee |
| ATE535525T1 (de) | 2006-03-31 | 2011-12-15 | Wako Pure Chem Ind Ltd | Cyaninfarbstoff vom pyrazoltyp |
| EP2119797B1 (fr) | 2007-01-31 | 2012-04-11 | Wako Pure Chemical Industries, Ltd. | Procede de detection d'une amplification ou d'une deletion dans un fragment d'adn genomique |
| US20250057853A1 (en) * | 2023-08-04 | 2025-02-20 | Repurposed Therapeutics, Inc. | Compositions and methods for the treatment of motion sickness and emesis |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1164227B (it) * | 1983-05-13 | 1987-04-08 | Angeli Inst Spa | Composizione farmaceutica atta alla somministrazione nasale di sali quaternari d'ammonio ed attivita' anticolinergica |
| US7765615B2 (en) * | 2007-03-28 | 2010-08-03 | Michael Robert Eastwood | Chest protector in sports medicine |
-
1998
- 1998-09-11 JP JP2000510441A patent/JP2002516815A/ja not_active Withdrawn
- 1998-09-11 WO PCT/US1998/018953 patent/WO1999012544A1/fr not_active Ceased
- 1998-09-11 EP EP98946945A patent/EP1027049A4/fr not_active Ceased
- 1998-09-11 CA CA002303132A patent/CA2303132C/fr not_active Expired - Fee Related
- 1998-09-11 AU AU93850/98A patent/AU742878B2/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP1027049A4 (fr) | 2001-09-05 |
| EP1027049A1 (fr) | 2000-08-16 |
| CA2303132A1 (fr) | 1999-03-18 |
| AU742878B2 (en) | 2002-01-17 |
| JP2002516815A (ja) | 2002-06-11 |
| AU9385098A (en) | 1999-03-29 |
| WO1999012544A1 (fr) | 1999-03-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |