PT98643B - Processo para a preparacao de uma composicao oftalmica em gotas contendo acido 3,4-dihidro-2,8-diisopropil-3-tioxo-2h-1,4-benzoxazina-4-acetico - Google Patents
Processo para a preparacao de uma composicao oftalmica em gotas contendo acido 3,4-dihidro-2,8-diisopropil-3-tioxo-2h-1,4-benzoxazina-4-acetico Download PDFInfo
- Publication number
- PT98643B PT98643B PT98643A PT9864391A PT98643B PT 98643 B PT98643 B PT 98643B PT 98643 A PT98643 A PT 98643A PT 9864391 A PT9864391 A PT 9864391A PT 98643 B PT98643 B PT 98643B
- Authority
- PT
- Portugal
- Prior art keywords
- process according
- composition
- cyclodextrin
- concentration
- water
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- CLDJCRWXLDLJLO-UHFFFAOYSA-N 2-[2,8-di(propan-2-yl)-3-sulfanylidene-1,4-benzoxazin-4-yl]acetic acid Chemical compound C1=CC=C2N(CC(O)=O)C(=S)C(C(C)C)OC2=C1C(C)C CLDJCRWXLDLJLO-UHFFFAOYSA-N 0.000 title 1
- 239000000203 mixture Substances 0.000 claims abstract description 74
- 229920000858 Cyclodextrin Polymers 0.000 claims abstract description 29
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims abstract description 12
- 150000003839 salts Chemical class 0.000 claims abstract description 10
- 150000001875 compounds Chemical class 0.000 claims description 39
- 238000000034 method Methods 0.000 claims description 18
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 claims description 15
- 239000004327 boric acid Substances 0.000 claims description 15
- 239000002738 chelating agent Substances 0.000 claims description 14
- 230000008569 process Effects 0.000 claims description 14
- 229920003169 water-soluble polymer Polymers 0.000 claims description 14
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 11
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 11
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 3
- 239000001913 cellulose Substances 0.000 claims description 3
- 229920002678 cellulose Polymers 0.000 claims description 3
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 3
- 239000001509 sodium citrate Substances 0.000 claims description 3
- 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 claims description 3
- 239000001488 sodium phosphate Substances 0.000 claims description 3
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 2
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 claims description 2
- 229920000642 polymer Polymers 0.000 claims description 2
- 229910000162 sodium phosphate Inorganic materials 0.000 claims description 2
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 claims description 2
- 229920001450 Alpha-Cyclodextrin Polymers 0.000 claims 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 claims 1
- 229940043377 alpha-cyclodextrin Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 238000010348 incorporation Methods 0.000 claims 1
- 239000003889 eye drop Substances 0.000 abstract description 24
- 229940012356 eye drops Drugs 0.000 abstract description 11
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 abstract description 2
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 24
- FAPWRFPIFSIZLT-UHFFFAOYSA-M sodium chloride Inorganic materials [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 15
- 229960000686 benzalkonium chloride Drugs 0.000 description 13
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- 206010015946 Eye irritation Diseases 0.000 description 12
- 231100000013 eye irritation Toxicity 0.000 description 12
- 239000008223 sterile water Substances 0.000 description 12
- 230000000052 comparative effect Effects 0.000 description 9
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical class OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 8
- 230000015572 biosynthetic process Effects 0.000 description 8
- 239000011780 sodium chloride Substances 0.000 description 8
- 239000000126 substance Substances 0.000 description 7
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 6
- 239000003814 drug Substances 0.000 description 6
- 239000011734 sodium Substances 0.000 description 5
- 229910052708 sodium Inorganic materials 0.000 description 5
- WRMNZCZEMHIOCP-UHFFFAOYSA-N 2-phenylethanol Chemical compound OCCC1=CC=CC=C1 WRMNZCZEMHIOCP-UHFFFAOYSA-N 0.000 description 4
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 4
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 4
- 239000012528 membrane Substances 0.000 description 4
- 231100000286 mucous membrane, eye irritation or corrosion testing Toxicity 0.000 description 4
- 208000002177 Cataract Diseases 0.000 description 3
- 206010012689 Diabetic retinopathy Diseases 0.000 description 3
- 239000001116 FEMA 4028 Substances 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 3
- 229960004853 betadex Drugs 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000011521 glass Substances 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- 206010023365 keratopathy Diseases 0.000 description 3
- 230000002335 preservative effect Effects 0.000 description 3
- 229940037001 sodium edetate Drugs 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 3
- 229940033663 thimerosal Drugs 0.000 description 3
- 208000002249 Diabetes Complications Diseases 0.000 description 2
- 206010012655 Diabetic complications Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 235000019445 benzyl alcohol Nutrition 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 239000006172 buffering agent Substances 0.000 description 2
- 229960004926 chlorobutanol Drugs 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000002198 insoluble material Substances 0.000 description 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 239000004334 sorbic acid Substances 0.000 description 2
- 235000010199 sorbic acid Nutrition 0.000 description 2
- 229940075582 sorbic acid Drugs 0.000 description 2
- 238000013112 stability test Methods 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- JEFOOEBNQUNOME-UHFFFAOYSA-N 2,8-di(propan-2-yl)-4H-1,4-benzoxazine-3-thione Chemical compound CC(C)C1Oc2c(NC1=S)cccc2C(C)C JEFOOEBNQUNOME-UHFFFAOYSA-N 0.000 description 1
- 102000016912 Aldehyde Reductase Human genes 0.000 description 1
- 108010053754 Aldehyde reductase Proteins 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 206010007749 Cataract diabetic Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 208000017442 Retinal disease Diseases 0.000 description 1
- 206010038923 Retinopathy Diseases 0.000 description 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 description 1
- 206010052428 Wound Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001340 alkali metals Chemical class 0.000 description 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
- 150000001342 alkaline earth metals Chemical class 0.000 description 1
- AZDRQVAHHNSJOQ-UHFFFAOYSA-N alumane Chemical class [AlH3] AZDRQVAHHNSJOQ-UHFFFAOYSA-N 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- 239000000043 antiallergic agent Substances 0.000 description 1
- 239000003899 bactericide agent 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
- 230000003115 biocidal effect Effects 0.000 description 1
- 229910021538 borax Inorganic materials 0.000 description 1
- 229960002645 boric acid Drugs 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- -1 compound sodium chloride Chemical class 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 201000007025 diabetic cataract Diseases 0.000 description 1
- 239000006196 drop Substances 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 1
- 235000019799 monosodium phosphate Nutrition 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 230000007823 neuropathy Effects 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- 229960002668 sodium chloride Drugs 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 229940079827 sodium hydrogen sulfite Drugs 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 235000011008 sodium phosphates Nutrition 0.000 description 1
- 239000004328 sodium tetraborate Substances 0.000 description 1
- 235000010339 sodium tetraborate Nutrition 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 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
Classifications
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
-
- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6949—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
- A61K47/6951—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
-
- 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
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nanotechnology (AREA)
- Ophthalmology & Optometry (AREA)
- General Engineering & Computer Science (AREA)
- Medical Informatics (AREA)
- Molecular Biology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Biotechnology (AREA)
- Biophysics (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP21482790 | 1990-08-13 | ||
| JP16285491 | 1991-07-03 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PT98643A PT98643A (pt) | 1992-07-31 |
| PT98643B true PT98643B (pt) | 1999-01-29 |
Family
ID=26488494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PT98643A PT98643B (pt) | 1990-08-13 | 1991-08-12 | Processo para a preparacao de uma composicao oftalmica em gotas contendo acido 3,4-dihidro-2,8-diisopropil-3-tioxo-2h-1,4-benzoxazina-4-acetico |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US5663170A (cg-RX-API-DMAC7.html) |
| EP (1) | EP0472327B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2769253B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR920003971A (cg-RX-API-DMAC7.html) |
| AT (1) | ATE121295T1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU633754B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2048942A1 (cg-RX-API-DMAC7.html) |
| DE (1) | DE69109021T2 (cg-RX-API-DMAC7.html) |
| DK (1) | DK0472327T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2071227T3 (cg-RX-API-DMAC7.html) |
| FI (1) | FI97777C (cg-RX-API-DMAC7.html) |
| HU (1) | HU207950B (cg-RX-API-DMAC7.html) |
| NO (1) | NO177845C (cg-RX-API-DMAC7.html) |
| PT (1) | PT98643B (cg-RX-API-DMAC7.html) |
| RU (1) | RU2068260C1 (cg-RX-API-DMAC7.html) |
| TW (1) | TW200402B (cg-RX-API-DMAC7.html) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0589020A4 (en) * | 1992-03-18 | 1994-07-06 | Coopervision Pharma | Verapamil hcl formulation and other ophthalmic solutions with buffer system for ocular administration |
| US5324718A (en) * | 1992-07-14 | 1994-06-28 | Thorsteinn Loftsson | Cyclodextrin/drug complexation |
| US5472954A (en) * | 1992-07-14 | 1995-12-05 | Cyclops H.F. | Cyclodextrin complexation |
| WO1994010976A1 (en) * | 1992-11-16 | 1994-05-26 | Ciba Vision Ag, Hettlingen | Polyvinyl alcohol/borate ophthalmic drug delivery system |
| US5494901A (en) * | 1993-01-05 | 1996-02-27 | Javitt; Jonathan C. | Topical compositions for the eye comprising a β-cyclodextrin derivative and a therapeutic agent |
| SE501482C2 (sv) * | 1993-06-24 | 1995-02-27 | Leiras Oy | Komposition för topisk administration av bispilokarpinsyradiestrar till ögat i form av en vattenlösning |
| JPH09500901A (ja) * | 1993-07-28 | 1997-01-28 | インサイト・ビジョン・インコーポレイテッド | 薬剤供給用懸濁液 |
| EP0777415A4 (en) * | 1994-07-11 | 1999-06-16 | David W Pate | COMPOSITIONS CONTAINING AN ANANDAMIDE ANALOG AND METHOD FOR TREATING INCREASED EYE PRESSURE USING IT |
| US5631297A (en) * | 1994-07-11 | 1997-05-20 | Pate; David W. | Anandamides useful for the treatment of intraocular hypertension, ophthalmic compositions containing the same and methods of use of the same |
| JP3297969B2 (ja) * | 1994-12-26 | 2002-07-02 | ライオン株式会社 | 点眼剤 |
| US5929115A (en) * | 1995-01-20 | 1999-07-27 | Wakamoto Pharmaceutical Co., Ltd. | Anti-inflammatory eye drop |
| CN1087169C (zh) * | 1995-01-20 | 2002-07-10 | 若素制药株式会社 | 抗炎症点眼剂 |
| JP2002241272A (ja) * | 1996-07-18 | 2002-08-28 | Mitsubishi Pharma Corp | 医薬処方組成物 |
| US6476004B1 (en) | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| JPH11209277A (ja) * | 1998-01-19 | 1999-08-03 | Yoshitomi Pharmaceut Ind Ltd | 医薬組成物 |
| GB9711643D0 (en) * | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| WO2000012137A1 (en) * | 1998-09-02 | 2000-03-09 | Allergan Sales, Inc. | Preserved cyclodextrin-containing compositions |
| EP1186302B1 (en) * | 1999-06-11 | 2005-05-18 | Sankyo Company, Limited | Ocular tension lowering composition for topical adminstration |
| JP2001125052A (ja) * | 1999-10-25 | 2001-05-11 | Lion Corp | コンタクトレンズ装着液 |
| WO2001097852A1 (en) * | 2000-06-19 | 2001-12-27 | Santen Pharmaceutical Co., Ltd. | Aseptics |
| US6468989B1 (en) | 2000-07-13 | 2002-10-22 | Dow Pharmaceutical Sciences | Gel compositions containing metronidazole |
| US6881726B2 (en) | 2001-12-24 | 2005-04-19 | Dow Pharmaceutical Sciences | Aqueous compositions containing metronidazole |
| WO2006137433A1 (ja) * | 2005-06-21 | 2006-12-28 | Wakamoto Pharmaceutical Co., Ltd. | レボカバスチンを可溶化させた水性薬剤 |
| US20100069335A1 (en) * | 2005-07-15 | 2010-03-18 | Rajiv Bhushan | Prevention and Treatment of Ophthalmic Complications of Diabetes |
| TWI692364B (zh) | 2012-03-26 | 2020-05-01 | 日商參天製藥股份有限公司 | 含有迪夸弗索之點眼液 |
| EP3784354A1 (en) * | 2018-04-27 | 2021-03-03 | Allergan, Inc. | Sodium chlorite compositions with enhanced anti-microbial efficacy and reduced toxicity |
| JP7470791B2 (ja) * | 2019-11-21 | 2024-04-18 | サムジン ファーマシューティカル カンパニー，リミテッド | 眼疾患の予防または治療用点眼組成物 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU602641B2 (en) * | 1986-04-17 | 1990-10-18 | Senju Pharmaceutical Co., Ltd. | Thiolactam-N-acetic acid derivatives, their production and use |
-
1991
- 1991-07-29 TW TW080105889A patent/TW200402B/zh active
- 1991-08-05 JP JP3195186A patent/JP2769253B2/ja not_active Expired - Lifetime
- 1991-08-08 DE DE69109021T patent/DE69109021T2/de not_active Expired - Fee Related
- 1991-08-08 ES ES91307275T patent/ES2071227T3/es not_active Expired - Lifetime
- 1991-08-08 AT AT91307275T patent/ATE121295T1/de active
- 1991-08-08 DK DK91307275.7T patent/DK0472327T3/da active
- 1991-08-08 AU AU81708/91A patent/AU633754B2/en not_active Ceased
- 1991-08-08 EP EP91307275A patent/EP0472327B1/en not_active Expired - Lifetime
- 1991-08-12 NO NO913136A patent/NO177845C/no unknown
- 1991-08-12 CA CA002048942A patent/CA2048942A1/en not_active Abandoned
- 1991-08-12 FI FI913811A patent/FI97777C/fi not_active IP Right Cessation
- 1991-08-12 RU SU915001489A patent/RU2068260C1/ru active
- 1991-08-12 PT PT98643A patent/PT98643B/pt not_active IP Right Cessation
- 1991-08-13 KR KR1019910013973A patent/KR920003971A/ko not_active Ceased
- 1991-08-13 HU HU912692A patent/HU207950B/hu not_active IP Right Cessation
-
1992
- 1992-07-13 US US07/912,580 patent/US5663170A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| FI97777B (fi) | 1996-11-15 |
| ATE121295T1 (de) | 1995-05-15 |
| FI913811L (fi) | 1992-02-14 |
| JPH05213757A (ja) | 1993-08-24 |
| FI913811A0 (fi) | 1991-08-12 |
| RU2068260C1 (ru) | 1996-10-27 |
| DE69109021T2 (de) | 1995-09-21 |
| TW200402B (cg-RX-API-DMAC7.html) | 1993-02-21 |
| HU207950B (en) | 1993-07-28 |
| DE69109021D1 (de) | 1995-05-24 |
| DK0472327T3 (da) | 1995-05-08 |
| PT98643A (pt) | 1992-07-31 |
| EP0472327B1 (en) | 1995-04-19 |
| NO177845B (no) | 1995-08-28 |
| HUT61196A (en) | 1992-12-28 |
| FI97777C (fi) | 1997-02-25 |
| US5663170A (en) | 1997-09-02 |
| NO913136L (no) | 1992-02-14 |
| AU8170891A (en) | 1992-02-20 |
| AU633754B2 (en) | 1993-02-04 |
| KR920003971A (ko) | 1992-03-27 |
| NO913136D0 (no) | 1991-08-12 |
| CA2048942A1 (en) | 1992-02-14 |
| HU912692D0 (en) | 1992-01-28 |
| ES2071227T3 (es) | 1995-06-16 |
| NO177845C (no) | 1995-12-06 |
| JP2769253B2 (ja) | 1998-06-25 |
| EP0472327A1 (en) | 1992-02-26 |
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| BB1A | Laying open of patent application |
Effective date: 19920327 |
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| FG3A | Patent granted, date of granting |
Effective date: 19981020 |
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| MM3A | Annulment or lapse |
Free format text: LAPSE DUE TO NON-PAYMENT OF FEES Effective date: 20000430 |