NZ562032A - Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissues - Google Patents
Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissuesInfo
- Publication number
- NZ562032A NZ562032A NZ562032A NZ56203206A NZ562032A NZ 562032 A NZ562032 A NZ 562032A NZ 562032 A NZ562032 A NZ 562032A NZ 56203206 A NZ56203206 A NZ 56203206A NZ 562032 A NZ562032 A NZ 562032A
- Authority
- NZ
- New Zealand
- Prior art keywords
- retinal
- composition
- ocular
- disease
- eye
- Prior art date
Links
- 239000003862 glucocorticoid Substances 0.000 title claims abstract description 36
- 238000002560 therapeutic procedure Methods 0.000 title description 5
- 230000000149 penetrating effect Effects 0.000 title description 2
- 239000000203 mixture Substances 0.000 claims abstract description 175
- 239000003814 drug Substances 0.000 claims abstract description 64
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 30
- KBPLFHHGFOOTCA-UHFFFAOYSA-N 1-Octanol Chemical compound CCCCCCCCO KBPLFHHGFOOTCA-UHFFFAOYSA-N 0.000 claims abstract description 18
- 125000002252 acyl group Chemical group 0.000 claims abstract description 17
- 150000002148 esters Chemical class 0.000 claims abstract description 12
- 238000005192 partition Methods 0.000 claims abstract description 12
- 238000004519 manufacturing process Methods 0.000 claims abstract description 11
- 239000007943 implant Substances 0.000 claims description 83
- 229920000642 polymer Polymers 0.000 claims description 56
- 239000002245 particle Substances 0.000 claims description 40
- 230000002207 retinal effect Effects 0.000 claims description 37
- 230000001225 therapeutic effect Effects 0.000 claims description 36
- 230000001939 inductive effect Effects 0.000 claims description 25
- 208000017442 Retinal disease Diseases 0.000 claims description 24
- 239000000725 suspension Substances 0.000 claims description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 18
- 229920002988 biodegradable polymer Polymers 0.000 claims description 18
- 239000004621 biodegradable polymer Substances 0.000 claims description 18
- 208000002780 macular degeneration Diseases 0.000 claims description 18
- 208000002367 Retinal Perforations Diseases 0.000 claims description 17
- 210000001525 retina Anatomy 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 15
- -1 furoyl Chemical group 0.000 claims description 15
- 239000004633 polyglycolic acid Substances 0.000 claims description 15
- 229950008885 polyglycolic acid Drugs 0.000 claims description 15
- 208000001344 Macular Edema Diseases 0.000 claims description 14
- 208000029977 White Dot Syndromes Diseases 0.000 claims description 14
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims description 12
- 201000011190 diabetic macular edema Diseases 0.000 claims description 12
- 208000004644 retinal vein occlusion Diseases 0.000 claims description 12
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 11
- 206010025415 Macular oedema Diseases 0.000 claims description 11
- 206010038923 Retinopathy Diseases 0.000 claims description 11
- 210000000981 epithelium Anatomy 0.000 claims description 11
- 201000010230 macular retinal edema Diseases 0.000 claims description 11
- 206010046851 Uveitis Diseases 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 9
- 206010038848 Retinal detachment Diseases 0.000 claims description 9
- 239000004626 polylactic acid Substances 0.000 claims description 9
- 230000004264 retinal detachment Effects 0.000 claims description 9
- 208000031886 HIV Infections Diseases 0.000 claims description 8
- 208000037357 HIV infectious disease Diseases 0.000 claims description 8
- 206010038897 Retinal tear Diseases 0.000 claims description 8
- 230000001154 acute effect Effects 0.000 claims description 8
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 8
- 239000007787 solid Substances 0.000 claims description 8
- 208000010412 Glaucoma Diseases 0.000 claims description 7
- 208000000208 Wet Macular Degeneration Diseases 0.000 claims description 7
- 230000002062 proliferating effect Effects 0.000 claims description 7
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 6
- 208000014882 Carotid artery disease Diseases 0.000 claims description 6
- 206010063664 Presumed ocular histoplasmosis syndrome Diseases 0.000 claims description 6
- 206010038910 Retinitis Diseases 0.000 claims description 6
- 208000007014 Retinitis pigmentosa Diseases 0.000 claims description 6
- 201000005485 Toxoplasmosis Diseases 0.000 claims description 6
- 229920002674 hyaluronan Polymers 0.000 claims description 6
- 229960003160 hyaluronic acid Drugs 0.000 claims description 6
- 208000015181 infectious disease Diseases 0.000 claims description 6
- 229920000728 polyester Polymers 0.000 claims description 6
- 238000001356 surgical procedure Methods 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 208000006379 syphilis Diseases 0.000 claims description 6
- 230000001982 uveitic effect Effects 0.000 claims description 6
- 108010010803 Gelatin Proteins 0.000 claims description 5
- 201000007527 Retinal artery occlusion Diseases 0.000 claims description 5
- 201000007737 Retinal degeneration Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 206010014801 endophthalmitis Diseases 0.000 claims description 5
- 229920000159 gelatin Polymers 0.000 claims description 5
- 239000008273 gelatin Substances 0.000 claims description 5
- 235000019322 gelatine Nutrition 0.000 claims description 5
- 235000011852 gelatine desserts Nutrition 0.000 claims description 5
- 239000000049 pigment Substances 0.000 claims description 5
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims description 5
- 229920001610 polycaprolactone Polymers 0.000 claims description 5
- 230000009885 systemic effect Effects 0.000 claims description 5
- 208000002691 Choroiditis Diseases 0.000 claims description 4
- 102000008186 Collagen Human genes 0.000 claims description 4
- 108010035532 Collagen Proteins 0.000 claims description 4
- 208000026350 Inborn Genetic disease Diseases 0.000 claims description 4
- 229910019142 PO4 Inorganic materials 0.000 claims description 4
- 229920001710 Polyorthoester Polymers 0.000 claims description 4
- 208000003971 Posterior uveitis Diseases 0.000 claims description 4
- 208000027073 Stargardt disease Diseases 0.000 claims description 4
- 229920001436 collagen Polymers 0.000 claims description 4
- 208000016361 genetic disease Diseases 0.000 claims description 4
- 230000001575 pathological effect Effects 0.000 claims description 4
- 239000010452 phosphate Substances 0.000 claims description 4
- 230000000472 traumatic effect Effects 0.000 claims description 4
- 102100028187 ATP-binding cassette sub-family C member 6 Human genes 0.000 claims description 3
- 206010002329 Aneurysm Diseases 0.000 claims description 3
- 208000005598 Angioid Streaks Diseases 0.000 claims description 3
- 208000031104 Arterial Occlusive disease Diseases 0.000 claims description 3
- 206010003571 Astrocytoma Diseases 0.000 claims description 3
- 208000009137 Behcet syndrome Diseases 0.000 claims description 3
- 201000007795 Bietti crystalline corneoretinal dystrophy Diseases 0.000 claims description 3
- 208000003569 Central serous chorioretinopathy Diseases 0.000 claims description 3
- 208000033825 Chorioretinal atrophy Diseases 0.000 claims description 3
- 208000005590 Choroidal Neovascularization Diseases 0.000 claims description 3
- 206010070957 Choroidal haemangioma Diseases 0.000 claims description 3
- 206010060823 Choroidal neovascularisation Diseases 0.000 claims description 3
- 206010053567 Coagulopathies Diseases 0.000 claims description 3
- 206010010356 Congenital anomaly Diseases 0.000 claims description 3
- 206010058202 Cystoid macular oedema Diseases 0.000 claims description 3
- 206010048843 Cytomegalovirus chorioretinitis Diseases 0.000 claims description 3
- 208000019878 Eales disease Diseases 0.000 claims description 3
- 208000001351 Epiretinal Membrane Diseases 0.000 claims description 3
- 208000028506 Familial Exudative Vitreoretinopathies Diseases 0.000 claims description 3
- 208000002927 Hamartoma Diseases 0.000 claims description 3
- 201000002563 Histoplasmosis Diseases 0.000 claims description 3
- 206010020772 Hypertension Diseases 0.000 claims description 3
- 206010020880 Hypertrophy Diseases 0.000 claims description 3
- 206010058558 Hypoperfusion Diseases 0.000 claims description 3
- 206010022557 Intermediate uveitis Diseases 0.000 claims description 3
- 206010022941 Iridocyclitis Diseases 0.000 claims description 3
- 206010025412 Macular dystrophy congenital Diseases 0.000 claims description 3
- 208000035719 Maculopathy Diseases 0.000 claims description 3
- 206010027476 Metastases Diseases 0.000 claims description 3
- 208000009857 Microaneurysm Diseases 0.000 claims description 3
- 208000010164 Multifocal Choroiditis Diseases 0.000 claims description 3
- 208000006123 Myiasis Diseases 0.000 claims description 3
- 206010065119 Necrotising herpetic retinopathy Diseases 0.000 claims description 3
- 206010069385 Ocular ischaemic syndrome Diseases 0.000 claims description 3
- 206010065700 Ocular sarcoidosis Diseases 0.000 claims description 3
- 208000003435 Optic Neuritis Diseases 0.000 claims description 3
- 206010065373 Papillophlebitis Diseases 0.000 claims description 3
- 208000004788 Pars Planitis Diseases 0.000 claims description 3
- 208000034247 Pattern dystrophy Diseases 0.000 claims description 3
- 208000018262 Peripheral vascular disease Diseases 0.000 claims description 3
- 201000004613 Pseudoxanthoma elasticum Diseases 0.000 claims description 3
- 206010064714 Radiation retinopathy Diseases 0.000 claims description 3
- 208000008709 Retinal Telangiectasis Diseases 0.000 claims description 3
- 201000001949 Retinal Vasculitis Diseases 0.000 claims description 3
- 208000032430 Retinal dystrophy Diseases 0.000 claims description 3
- 206010038915 Retinitis viral Diseases 0.000 claims description 3
- 201000000582 Retinoblastoma Diseases 0.000 claims description 3
- 206010038935 Retinopathy sickle cell Diseases 0.000 claims description 3
- 206010039705 Scleritis Diseases 0.000 claims description 3
- 208000014286 Serpiginous choroiditis Diseases 0.000 claims description 3
- 208000022758 Sorsby fundus dystrophy Diseases 0.000 claims description 3
- 208000036038 Subretinal fibrosis Diseases 0.000 claims description 3
- 206010043189 Telangiectasia Diseases 0.000 claims description 3
- 206010044269 Toxocariasis Diseases 0.000 claims description 3
- 201000001408 X-linked juvenile retinoschisis 1 Diseases 0.000 claims description 3
- 208000017441 X-linked retinoschisis Diseases 0.000 claims description 3
- 208000023564 acute macular neuroretinopathy Diseases 0.000 claims description 3
- 201000004612 anterior uveitis Diseases 0.000 claims description 3
- 229920000249 biocompatible polymer Polymers 0.000 claims description 3
- 206010072959 birdshot chorioretinopathy Diseases 0.000 claims description 3
- 208000015294 blood coagulation disease Diseases 0.000 claims description 3
- 210000001185 bone marrow Anatomy 0.000 claims description 3
- 201000005845 branch retinal artery occlusion Diseases 0.000 claims description 3
- 201000005667 central retinal vein occlusion Diseases 0.000 claims description 3
- 208000027129 choroid disease Diseases 0.000 claims description 3
- 201000008615 cone dystrophy Diseases 0.000 claims description 3
- 208000006623 congenital stationary night blindness Diseases 0.000 claims description 3
- 201000010206 cystoid macular edema Diseases 0.000 claims description 3
- 208000001763 cytomegalovirus retinitis Diseases 0.000 claims description 3
- 201000006902 exudative vitreoretinopathy Diseases 0.000 claims description 3
- 230000002538 fungal effect Effects 0.000 claims description 3
- 230000001631 hypertensive effect Effects 0.000 claims description 3
- 208000014674 injury Diseases 0.000 claims description 3
- 208000019420 lymphoid neoplasm Diseases 0.000 claims description 3
- 208000029233 macular holes Diseases 0.000 claims description 3
- 230000009401 metastasis Effects 0.000 claims description 3
- 201000002165 neuroretinitis Diseases 0.000 claims description 3
- 208000008940 ocular tuberculosis Diseases 0.000 claims description 3
- 208000008798 osteoma Diseases 0.000 claims description 3
- 230000000649 photocoagulation Effects 0.000 claims description 3
- 239000002745 poly(ortho ester) Substances 0.000 claims description 3
- 201000004849 posterior scleritis Diseases 0.000 claims description 3
- 201000002267 posterior uveal melanoma Diseases 0.000 claims description 3
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims description 3
- 208000023558 pseudoxanthoma elasticum (inherited or acquired) Diseases 0.000 claims description 3
- 208000034503 punctate inner choroidopathy Diseases 0.000 claims description 3
- 201000007714 retinoschisis Diseases 0.000 claims description 3
- 208000009056 telangiectasis Diseases 0.000 claims description 3
- 230000008733 trauma Effects 0.000 claims description 3
- 201000008827 tuberculosis Diseases 0.000 claims description 3
- 230000003074 vasoproliferative effect Effects 0.000 claims description 3
- 201000007790 vitelliform macular dystrophy Diseases 0.000 claims description 3
- 208000008069 Geographic Atrophy Diseases 0.000 claims description 2
- 208000032398 Retinal pigment epitheliopathy Diseases 0.000 claims description 2
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 208000019672 acute posterior multifocal placoid pigment epitheliopathy Diseases 0.000 claims description 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 2
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 201000005849 central retinal artery occlusion Diseases 0.000 claims description 2
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 230000017074 necrotic cell death Effects 0.000 claims 1
- 210000001508 eye Anatomy 0.000 description 98
- 239000000463 material Substances 0.000 description 55
- 238000012377 drug delivery Methods 0.000 description 47
- 238000000034 method Methods 0.000 description 45
- 229940079593 drug Drugs 0.000 description 32
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 description 25
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 25
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 25
- 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 description 25
- 229940124597 therapeutic agent Drugs 0.000 description 25
- 239000003795 chemical substances by application Substances 0.000 description 24
- 238000002347 injection Methods 0.000 description 24
- 239000007924 injection Substances 0.000 description 24
- 210000004155 blood-retinal barrier Anatomy 0.000 description 22
- 230000004378 blood-retinal barrier Effects 0.000 description 22
- 230000015556 catabolic process Effects 0.000 description 22
- 150000001875 compounds Chemical class 0.000 description 22
- 229960003957 dexamethasone Drugs 0.000 description 22
- 150000003431 steroids Chemical class 0.000 description 21
- 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 description 20
- 210000001519 tissue Anatomy 0.000 description 20
- 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 20
- 229960002117 triamcinolone acetonide Drugs 0.000 description 20
- 230000000694 effects Effects 0.000 description 18
- 210000002164 blood-aqueous barrier Anatomy 0.000 description 17
- 230000004420 blood-aqueous barrier Effects 0.000 description 17
- 239000000872 buffer Substances 0.000 description 16
- 239000003755 preservative agent Substances 0.000 description 16
- 241000283973 Oryctolagus cuniculus Species 0.000 description 15
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 description 14
- 239000000243 solution Substances 0.000 description 14
- 210000002159 anterior chamber Anatomy 0.000 description 13
- 238000004090 dissolution Methods 0.000 description 13
- 238000001125 extrusion Methods 0.000 description 13
- 230000000699 topical effect Effects 0.000 description 13
- 229920000858 Cyclodextrin Polymers 0.000 description 12
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 12
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 12
- 239000011159 matrix material Substances 0.000 description 12
- 229940037128 systemic glucocorticoids Drugs 0.000 description 12
- 210000004127 vitreous body Anatomy 0.000 description 12
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 11
- 229920001577 copolymer Polymers 0.000 description 11
- 239000007788 liquid Substances 0.000 description 11
- 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 11
- 229920000954 Polyglycolide Polymers 0.000 description 10
- 229940092705 beclomethasone Drugs 0.000 description 10
- 241000282414 Homo sapiens Species 0.000 description 9
- 239000013078 crystal Substances 0.000 description 9
- 238000009472 formulation Methods 0.000 description 9
- 230000001965 increasing effect Effects 0.000 description 9
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 9
- 230000002335 preservative effect Effects 0.000 description 9
- 229960005294 triamcinolone Drugs 0.000 description 9
- 206010061218 Inflammation Diseases 0.000 description 8
- 239000002253 acid Substances 0.000 description 8
- 210000001742 aqueous humor Anatomy 0.000 description 8
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 8
- 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 description 8
- 229960000289 fluticasone propionate Drugs 0.000 description 8
- 230000004054 inflammatory process Effects 0.000 description 8
- 239000002953 phosphate buffered saline Substances 0.000 description 8
- 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 description 8
- 239000003981 vehicle Substances 0.000 description 8
- 102000003676 Glucocorticoid Receptors Human genes 0.000 description 7
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 7
- 239000012530 fluid Substances 0.000 description 7
- 230000002829 reductive effect Effects 0.000 description 7
- 239000011780 sodium chloride Substances 0.000 description 7
- 235000012431 wafers Nutrition 0.000 description 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 6
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 6
- 239000003246 corticosteroid Substances 0.000 description 6
- 230000003628 erosive effect Effects 0.000 description 6
- 229960000890 hydrocortisone Drugs 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- WCDDVEOXEIYWFB-VXORFPGASA-N (2s,3s,4r,5r,6r)-3-[(2s,3r,5s,6r)-3-acetamido-5-hydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5,6-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@@H]1C[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O)[C@H](O)[C@H]1O WCDDVEOXEIYWFB-VXORFPGASA-N 0.000 description 5
- 208000002177 Cataract Diseases 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 5
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 5
- 229950000210 beclometasone dipropionate Drugs 0.000 description 5
- 230000004438 eyesight Effects 0.000 description 5
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide 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]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 description 5
- 229940014041 hyaluronate Drugs 0.000 description 5
- 230000004410 intraocular pressure Effects 0.000 description 5
- 239000012071 phase Substances 0.000 description 5
- 239000008363 phosphate buffer Substances 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 150000003839 salts Chemical class 0.000 description 5
- 102100022258 Disks large homolog 5 Human genes 0.000 description 4
- 101100063489 Homo sapiens DLG5 gene Proteins 0.000 description 4
- 239000004372 Polyvinyl alcohol Substances 0.000 description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 4
- 230000008901 benefit Effects 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- QBWCMBCROVPCKQ-UHFFFAOYSA-N chlorous acid Chemical compound OCl=O QBWCMBCROVPCKQ-UHFFFAOYSA-N 0.000 description 4
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 4
- 210000003161 choroid Anatomy 0.000 description 4
- CBGUOGMQLZIXBE-XGQKBEPLSA-N clobetasol propionate 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)CCl)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CBGUOGMQLZIXBE-XGQKBEPLSA-N 0.000 description 4
- 210000004087 cornea Anatomy 0.000 description 4
- 229960001334 corticosteroids Drugs 0.000 description 4
- 229940097362 cyclodextrins Drugs 0.000 description 4
- 238000006731 degradation reaction Methods 0.000 description 4
- 238000009792 diffusion process Methods 0.000 description 4
- OSVXSBDYLRYLIG-UHFFFAOYSA-N dioxidochlorine(.) Chemical compound O=Cl=O OSVXSBDYLRYLIG-UHFFFAOYSA-N 0.000 description 4
- 239000000835 fiber Substances 0.000 description 4
- 150000004676 glycans Chemical class 0.000 description 4
- 238000000227 grinding Methods 0.000 description 4
- 229920001519 homopolymer Polymers 0.000 description 4
- 238000002513 implantation Methods 0.000 description 4
- 239000004310 lactic acid Substances 0.000 description 4
- 235000014655 lactic acid Nutrition 0.000 description 4
- 239000011859 microparticle Substances 0.000 description 4
- 239000004005 microsphere Substances 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 210000001328 optic nerve Anatomy 0.000 description 4
- 239000001301 oxygen Substances 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 239000008188 pellet Substances 0.000 description 4
- 229920000747 poly(lactic acid) Polymers 0.000 description 4
- 229920001282 polysaccharide Polymers 0.000 description 4
- 239000005017 polysaccharide Substances 0.000 description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 description 4
- 229960005205 prednisolone Drugs 0.000 description 4
- 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 4
- 238000012545 processing Methods 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 238000006467 substitution reaction Methods 0.000 description 4
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
- FBRAWBYQGRLCEK-AVVSTMBFSA-N Clobetasone butyrate 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)CCl)(OC(=O)CCC)[C@@]1(C)CC2=O FBRAWBYQGRLCEK-AVVSTMBFSA-N 0.000 description 3
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 241000282412 Homo Species 0.000 description 3
- JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 description 3
- FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 description 3
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 3
- HYRKAAMZBDSJFJ-LFDBJOOHSA-N Paramethasone acetate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)COC(C)=O)(O)[C@@]2(C)C[C@@H]1O HYRKAAMZBDSJFJ-LFDBJOOHSA-N 0.000 description 3
- 239000004793 Polystyrene Substances 0.000 description 3
- AKUJBENLRBOFTD-HIBZCRSPSA-N [2-[(9r,10s,11s,13s,16r,17r)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)C1C1C[C@@H](C)[C@@](C(=O)COC(C)=O)(O)[C@@]1(C)C[C@@H]2O AKUJBENLRBOFTD-HIBZCRSPSA-N 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 239000013543 active substance Substances 0.000 description 3
- 230000004888 barrier function Effects 0.000 description 3
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate 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)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 description 3
- 239000006172 buffering agent Substances 0.000 description 3
- 229960004703 clobetasol propionate Drugs 0.000 description 3
- 238000007906 compression Methods 0.000 description 3
- 230000006835 compression Effects 0.000 description 3
- 238000005520 cutting process Methods 0.000 description 3
- BOBLHFUVNSFZPJ-JOYXJVLSSA-N diflorasone diacetate 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)COC(C)=O)(OC(C)=O)[C@@]2(C)C[C@@H]1O BOBLHFUVNSFZPJ-JOYXJVLSSA-N 0.000 description 3
- 238000013265 extended release Methods 0.000 description 3
- 230000002209 hydrophobic effect Effects 0.000 description 3
- 230000006872 improvement Effects 0.000 description 3
- 238000001990 intravenous administration Methods 0.000 description 3
- DMKSVUSAATWOCU-HROMYWEYSA-N loteprednol etabonate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)OCCl)(OC(=O)OCC)[C@@]1(C)C[C@@H]2O DMKSVUSAATWOCU-HROMYWEYSA-N 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 229910052751 metal Inorganic materials 0.000 description 3
- 239000002184 metal Substances 0.000 description 3
- 238000003801 milling Methods 0.000 description 3
- 239000002395 mineralocorticoid Substances 0.000 description 3
- 239000000178 monomer Substances 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- 102000006255 nuclear receptors Human genes 0.000 description 3
- 108020004017 nuclear receptors Proteins 0.000 description 3
- 230000035515 penetration Effects 0.000 description 3
- 229920002223 polystyrene Polymers 0.000 description 3
- 239000001103 potassium chloride Substances 0.000 description 3
- 235000011164 potassium chloride Nutrition 0.000 description 3
- VJZLQIPZNBPASX-OJJGEMKLSA-L prednisolone sodium phosphate Chemical compound [Na+].[Na+].O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)COP([O-])([O-])=O)[C@@H]4[C@@H]3CCC2=C1 VJZLQIPZNBPASX-OJJGEMKLSA-L 0.000 description 3
- 102000005962 receptors Human genes 0.000 description 3
- 108020003175 receptors Proteins 0.000 description 3
- 230000004044 response Effects 0.000 description 3
- 210000003786 sclera Anatomy 0.000 description 3
- 239000003270 steroid hormone Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- DTOUUUZOYKYHEP-UHFFFAOYSA-N 1,3-bis(2-ethylhexyl)-5-methyl-1,3-diazinan-5-amine Chemical compound CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 DTOUUUZOYKYHEP-UHFFFAOYSA-N 0.000 description 2
- ZOCUOMKMBMEYQV-GSLJADNHSA-N 9alpha-Fluoro-11beta,17alpha,21-trihydroxypregna-1,4-diene-3,20-dione 21-acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O ZOCUOMKMBMEYQV-GSLJADNHSA-N 0.000 description 2
- 208000004142 Acute Retinal Necrosis Syndrome Diseases 0.000 description 2
- XKRFYHLGVUSROY-UHFFFAOYSA-N Argon Chemical compound [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 description 2
- 201000004569 Blindness Diseases 0.000 description 2
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- 239000004155 Chlorine dioxide Substances 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 239000004375 Dextrin Substances 0.000 description 2
- 229920001353 Dextrin Polymers 0.000 description 2
- 206010012692 Diabetic uveitis Diseases 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 238000012369 In process control Methods 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 206010030043 Ocular hypertension Diseases 0.000 description 2
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 2
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 description 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 description 2
- 229920001244 Poly(D,L-lactide) Polymers 0.000 description 2
- LRJOMUJRLNCICJ-JZYPGELDSA-N Prednisolone acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O LRJOMUJRLNCICJ-JZYPGELDSA-N 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 2
- 229920002125 Sokalan® Polymers 0.000 description 2
- 229940022663 acetate Drugs 0.000 description 2
- 239000008351 acetate buffer Substances 0.000 description 2
- DJHCCTTVDRAMEH-DUUJBDRPSA-N alclometasone dipropionate Chemical compound C([C@H]1Cl)C2=CC(=O)C=C[C@]2(C)[C@@H]2[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 DJHCCTTVDRAMEH-DUUJBDRPSA-N 0.000 description 2
- 150000001299 aldehydes Chemical class 0.000 description 2
- 150000001408 amides Chemical class 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 239000011324 bead Substances 0.000 description 2
- 229960000686 benzalkonium chloride Drugs 0.000 description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 2
- 229960002537 betamethasone Drugs 0.000 description 2
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone 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-DVTGEIKXSA-N 0.000 description 2
- CIWBQSYVNNPZIQ-XYWKZLDCSA-N betamethasone dipropionate 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)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CIWBQSYVNNPZIQ-XYWKZLDCSA-N 0.000 description 2
- 238000006065 biodegradation reaction Methods 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 150000007942 carboxylates Chemical class 0.000 description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 2
- 235000019398 chlorine dioxide Nutrition 0.000 description 2
- 229910001919 chlorite Inorganic materials 0.000 description 2
- 229910052619 chlorite group Inorganic materials 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 239000007979 citrate buffer Substances 0.000 description 2
- 229960005465 clobetasone butyrate Drugs 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000012141 concentrate Substances 0.000 description 2
- 238000009833 condensation Methods 0.000 description 2
- 230000005494 condensation Effects 0.000 description 2
- 239000000562 conjugate Substances 0.000 description 2
- 239000000599 controlled substance Substances 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 239000007857 degradation product Substances 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- CIWBQSYVNNPZIQ-PKWREOPISA-N dexamethasone dipropionate 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)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CIWBQSYVNNPZIQ-PKWREOPISA-N 0.000 description 2
- 235000019425 dextrin Nutrition 0.000 description 2
- 206010012601 diabetes mellitus Diseases 0.000 description 2
- 229960004154 diflorasone Drugs 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 208000011325 dry age related macular degeneration Diseases 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 239000003623 enhancer Substances 0.000 description 2
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 2
- 208000030533 eye disease Diseases 0.000 description 2
- 229960001347 fluocinolone acetonide Drugs 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 229940115747 halobetasol Drugs 0.000 description 2
- 229960004867 hexetidine Drugs 0.000 description 2
- 238000004128 high performance liquid chromatography Methods 0.000 description 2
- 230000003301 hydrolyzing effect Effects 0.000 description 2
- 238000010965 in-process control Methods 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 238000003780 insertion Methods 0.000 description 2
- 230000037431 insertion Effects 0.000 description 2
- 229940063199 kenalog Drugs 0.000 description 2
- 150000002576 ketones Chemical class 0.000 description 2
- 239000004816 latex Substances 0.000 description 2
- 229920000126 latex Polymers 0.000 description 2
- 239000003446 ligand Substances 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- 229960004584 methylprednisolone Drugs 0.000 description 2
- 230000005012 migration Effects 0.000 description 2
- 238000013508 migration Methods 0.000 description 2
- 239000004570 mortar (masonry) Substances 0.000 description 2
- 229960000865 paramethasone acetate Drugs 0.000 description 2
- 239000004632 polycaprolactone Substances 0.000 description 2
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 2
- 239000004810 polytetrafluoroethylene Substances 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 238000011176 pooling Methods 0.000 description 2
- 229960002800 prednisolone acetate Drugs 0.000 description 2
- 229960002943 prednisolone sodium phosphate Drugs 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 210000001747 pupil Anatomy 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 230000004258 retinal degeneration Effects 0.000 description 2
- 229940061341 retisert Drugs 0.000 description 2
- QTTRZHGPGKRAFB-OOKHYKNYSA-N rimexolone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CC)(C)[C@@]1(C)C[C@@H]2O QTTRZHGPGKRAFB-OOKHYKNYSA-N 0.000 description 2
- 238000000926 separation method Methods 0.000 description 2
- 229910001220 stainless steel Inorganic materials 0.000 description 2
- 239000010935 stainless steel Substances 0.000 description 2
- 238000011146 sterile filtration Methods 0.000 description 2
- 230000001954 sterilising effect Effects 0.000 description 2
- 238000004659 sterilization and disinfection Methods 0.000 description 2
- 238000013268 sustained release Methods 0.000 description 2
- 239000012730 sustained-release form Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 238000007910 systemic administration Methods 0.000 description 2
- ZMANZCXQSJIPKH-UHFFFAOYSA-N triethylamine Natural products CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 2
- BDSYKGHYMJNPAB-LICBFIPMSA-N ulobetasol 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)CCl)(OC(=O)CC)[C@@]2(C)C[C@@H]1O BDSYKGHYMJNPAB-LICBFIPMSA-N 0.000 description 2
- 239000003643 water by type Substances 0.000 description 2
- RVBSTEHLLHXILB-QODHSQIYSA-N (6r,8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-6,11,17-trihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one Chemical compound C1([C@H](O)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]2(C)C[C@@H]1O RVBSTEHLLHXILB-QODHSQIYSA-N 0.000 description 1
- SHJZUHWENQCCJH-YQAXKJAASA-N (8s,9r,10s,11s,13s,14s)-9-fluoro-11-hydroxy-10,13-dimethyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthrene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 SHJZUHWENQCCJH-YQAXKJAASA-N 0.000 description 1
- IKGBPSZWCRRUQS-DTAAKRQUSA-N (8s,9r,10s,11s,13s,14s,16s,17r)-17-acetyl-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(C)=O)(O)[C@@]1(C)C[C@@H]2O IKGBPSZWCRRUQS-DTAAKRQUSA-N 0.000 description 1
- BHDHELFREODRJK-XRYUJSLGSA-N (8s,9r,10s,13s,14s,17r)-9-fluoro-17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,12,14,15,16-octahydro-1h-cyclopenta[a]phenanthrene-3,11-dione Chemical compound O=C1CC[C@]2(C)[C@@]3(F)C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 BHDHELFREODRJK-XRYUJSLGSA-N 0.000 description 1
- JVTAAEKCZFNVCJ-UWTATZPHSA-M (R)-lactate Chemical compound C[C@@H](O)C([O-])=O JVTAAEKCZFNVCJ-UWTATZPHSA-M 0.000 description 1
- OGCKUGCNRAHIPG-UHFFFAOYSA-N 1-hydroxyoctan-2-one Chemical compound CCCCCCC(=O)CO OGCKUGCNRAHIPG-UHFFFAOYSA-N 0.000 description 1
- FUFLCEKSBBHCMO-UHFFFAOYSA-N 11-dehydrocorticosterone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 FUFLCEKSBBHCMO-UHFFFAOYSA-N 0.000 description 1
- FTMJFHVKAXPFIY-UHFFFAOYSA-N 2,2-dichloro-N-[1,3-dihydroxy-1-(3-nitrophenyl)propan-2-yl]acetamide Chemical compound OCC(NC(=O)C(Cl)Cl)C(O)c1cccc(c1)[N+]([O-])=O FTMJFHVKAXPFIY-UHFFFAOYSA-N 0.000 description 1
- BFUUJUGQJUTPAF-UHFFFAOYSA-N 2-(3-amino-4-propoxybenzoyl)oxyethyl-diethylazanium;chloride Chemical compound [Cl-].CCCOC1=CC=C(C(=O)OCC[NH+](CC)CC)C=C1N BFUUJUGQJUTPAF-UHFFFAOYSA-N 0.000 description 1
- QTQGHKVYLQBJLO-UHFFFAOYSA-N 4-methylbenzenesulfonate;(4-methyl-1-oxo-1-phenylmethoxypentan-2-yl)azanium Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.CC(C)CC(N)C(=O)OCC1=CC=CC=C1 QTQGHKVYLQBJLO-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- MYYIMZRZXIQBGI-HVIRSNARSA-N 6alpha-Fluoroprednisolone 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]3C[C@H](F)C2=C1 MYYIMZRZXIQBGI-HVIRSNARSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Natural products CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 1
- 229920000178 Acrylic resin Polymers 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
- 108010088751 Albumins Proteins 0.000 description 1
- 102000009027 Albumins Human genes 0.000 description 1
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 description 1
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 description 1
- 229920001450 Alpha-Cyclodextrin Polymers 0.000 description 1
- 102100032187 Androgen receptor Human genes 0.000 description 1
- 238000012371 Aseptic Filling Methods 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 229920001661 Chitosan Polymers 0.000 description 1
- ARPLCFGLEYFDCN-CDACMRRYSA-N Clocortolone acetate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(Cl)[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)COC(C)=O)[C@@]2(C)C[C@@H]1O ARPLCFGLEYFDCN-CDACMRRYSA-N 0.000 description 1
- MFYSYFVPBJMHGN-ZPOLXVRWSA-N Cortisone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 MFYSYFVPBJMHGN-ZPOLXVRWSA-N 0.000 description 1
- MFYSYFVPBJMHGN-UHFFFAOYSA-N Cortisone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)(O)C(=O)CO)C4C3CCC2=C1 MFYSYFVPBJMHGN-UHFFFAOYSA-N 0.000 description 1
- ITRJWOMZKQRYTA-RFZYENFJSA-N Cortisone acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)CC2=O ITRJWOMZKQRYTA-RFZYENFJSA-N 0.000 description 1
- 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 1
- 229930182843 D-Lactic acid Natural products 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
- JVTAAEKCZFNVCJ-UWTATZPHSA-N D-lactic acid Chemical compound C[C@@H](O)C(O)=O JVTAAEKCZFNVCJ-UWTATZPHSA-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
- 206010048474 Fat redistribution Diseases 0.000 description 1
- WJOHZNCJWYWUJD-IUGZLZTKSA-N Fluocinonide 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]3OC(C)(C)O[C@@]3(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O WJOHZNCJWYWUJD-IUGZLZTKSA-N 0.000 description 1
- 208000036119 Frailty Diseases 0.000 description 1
- 208000002705 Glucose Intolerance Diseases 0.000 description 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- YCISZOVUHXIOFY-HKXOFBAYSA-N Halopredone acetate Chemical compound C1([C@H](F)C2)=CC(=O)C(Br)=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2CC[C@](OC(C)=O)(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O YCISZOVUHXIOFY-HKXOFBAYSA-N 0.000 description 1
- 101000946124 Homo sapiens Lipocalin-1 Proteins 0.000 description 1
- FOGXJPFPZOHSQS-AYVLZSQQSA-N Hydrocortisone butyrate propionate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)CC)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O FOGXJPFPZOHSQS-AYVLZSQQSA-N 0.000 description 1
- DLVOSEUFIRPIRM-KAQKJVHQSA-N Hydrocortisone cypionate Chemical compound O=C([C@@]1(O)CC[C@H]2[C@H]3[C@@H]([C@]4(CCC(=O)C=C4CC3)C)[C@@H](O)C[C@@]21C)COC(=O)CCC1CCCC1 DLVOSEUFIRPIRM-KAQKJVHQSA-N 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- PIWKPBJCKXDKJR-UHFFFAOYSA-N Isoflurane Chemical compound FC(F)OC(Cl)C(F)(F)F PIWKPBJCKXDKJR-UHFFFAOYSA-N 0.000 description 1
- 239000000232 Lipid Bilayer Substances 0.000 description 1
- 102100034724 Lipocalin-1 Human genes 0.000 description 1
- 241000406668 Loxodonta cyclotis Species 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- HUXCOHMTWUSXGY-GAPIFECDSA-N Meclorisone dibutyrate 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)CCC)(OC(=O)CCC)[C@@]1(C)C[C@@H]2Cl HUXCOHMTWUSXGY-GAPIFECDSA-N 0.000 description 1
- GZENKSODFLBBHQ-ILSZZQPISA-N Medrysone Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@H](C(C)=O)CC[C@H]21 GZENKSODFLBBHQ-ILSZZQPISA-N 0.000 description 1
- 208000000592 Nasal Polyps Diseases 0.000 description 1
- 206010029113 Neovascularisation Diseases 0.000 description 1
- 208000022873 Ocular disease Diseases 0.000 description 1
- 208000021957 Ocular injury Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 239000004952 Polyamide Substances 0.000 description 1
- 229920002732 Polyanhydride Polymers 0.000 description 1
- 229920000148 Polycarbophil calcium Polymers 0.000 description 1
- HUMXXHTVHHLNRO-KAJVQRHHSA-N Prednisolone tebutate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)CC(C)(C)C)(O)[C@@]1(C)C[C@@H]2O HUMXXHTVHHLNRO-KAJVQRHHSA-N 0.000 description 1
- 241000283080 Proboscidea <mammal> Species 0.000 description 1
- 208000002158 Proliferative Vitreoretinopathy Diseases 0.000 description 1
- 208000007135 Retinal Neovascularization Diseases 0.000 description 1
- 206010038934 Retinopathy proliferative Diseases 0.000 description 1
- 229920002385 Sodium hyaluronate Polymers 0.000 description 1
- 208000002847 Surgical Wound Diseases 0.000 description 1
- 102000040945 Transcription factor Human genes 0.000 description 1
- 108091023040 Transcription factor Proteins 0.000 description 1
- TZIZWYVVGLXXFV-FLRHRWPCSA-N Triamcinolone hexacetonide 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)COC(=O)CC(C)(C)C)[C@@]1(C)C[C@@H]2O TZIZWYVVGLXXFV-FLRHRWPCSA-N 0.000 description 1
- 208000021017 Weight Gain Diseases 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- ITYMTTQVNYAJAA-OCUNRLNVSA-N [(8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] propanoate 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)(OC(=O)CC)[C@@]1(C)C[C@@H]2O ITYMTTQVNYAJAA-OCUNRLNVSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000004308 accommodation Effects 0.000 description 1
- 229960000583 acetic acid Drugs 0.000 description 1
- 150000001242 acetic acid derivatives Chemical class 0.000 description 1
- 208000024716 acute asthma Diseases 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 210000000577 adipose tissue Anatomy 0.000 description 1
- 210000004404 adrenal cortex Anatomy 0.000 description 1
- 230000001919 adrenal effect Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 229960002478 aldosterone Drugs 0.000 description 1
- 229940072056 alginate Drugs 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 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
- 125000000217 alkyl group Chemical group 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 108010080146 androgen receptors Proteins 0.000 description 1
- 150000008064 anhydrides Chemical class 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 229910052786 argon Inorganic materials 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 206010003549 asthenia Diseases 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 229940038482 beclomethasone dipropionate monohydrate Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000019445 benzyl alcohol Nutrition 0.000 description 1
- 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 1
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229940098773 bovine serum albumin Drugs 0.000 description 1
- NLAMRLZPVVKXTK-UHFFFAOYSA-N but-1-enyl acetate Chemical class CCC=COC(C)=O NLAMRLZPVVKXTK-UHFFFAOYSA-N 0.000 description 1
- 235000010410 calcium alginate Nutrition 0.000 description 1
- 239000000648 calcium alginate Substances 0.000 description 1
- 229960002681 calcium alginate Drugs 0.000 description 1
- OKHHGHGGPDJQHR-YMOPUZKJSA-L calcium;(2s,3s,4s,5s,6r)-6-[(2r,3s,4r,5s,6r)-2-carboxy-6-[(2r,3s,4r,5s,6r)-2-carboxylato-4,5,6-trihydroxyoxan-3-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate Chemical compound [Ca+2].O[C@@H]1[C@H](O)[C@H](O)O[C@@H](C([O-])=O)[C@H]1O[C@H]1[C@@H](O)[C@@H](O)[C@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@H](O2)C([O-])=O)O)[C@H](C(O)=O)O1 OKHHGHGGPDJQHR-YMOPUZKJSA-L 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 150000001721 carbon Chemical group 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 150000001733 carboxylic acid esters Chemical class 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 229920002301 cellulose acetate Polymers 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 150000001793 charged compounds Chemical class 0.000 description 1
- 229940045110 chitosan Drugs 0.000 description 1
- 239000013611 chromosomal DNA Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 229960002842 clobetasol Drugs 0.000 description 1
- 229960001146 clobetasone Drugs 0.000 description 1
- 229960004299 clocortolone Drugs 0.000 description 1
- 229960001357 clocortolone pivalate Drugs 0.000 description 1
- SXYZQZLHAIHKKY-GSTUPEFVSA-N clocortolone pivalate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(Cl)[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)COC(=O)C(C)(C)C)[C@@]2(C)C[C@@H]1O SXYZQZLHAIHKKY-GSTUPEFVSA-N 0.000 description 1
- 229940125898 compound 5 Drugs 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- BMCQMVFGOVHVNG-TUFAYURCSA-N cortisol 17-butyrate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CO)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O BMCQMVFGOVHVNG-TUFAYURCSA-N 0.000 description 1
- FZCHYNWYXKICIO-FZNHGJLXSA-N cortisol 17-valerate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O FZCHYNWYXKICIO-FZNHGJLXSA-N 0.000 description 1
- ALEXXDVDDISNDU-JZYPGELDSA-N cortisol 21-acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O ALEXXDVDDISNDU-JZYPGELDSA-N 0.000 description 1
- RYJIRNNXCHOUTQ-OJJGEMKLSA-L cortisol sodium phosphate Chemical compound [Na+].[Na+].O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)COP([O-])([O-])=O)[C@@H]4[C@@H]3CCC2=C1 RYJIRNNXCHOUTQ-OJJGEMKLSA-L 0.000 description 1
- 229960004544 cortisone Drugs 0.000 description 1
- 229960003290 cortisone acetate Drugs 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 229940022769 d- lactic acid Drugs 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 238000003795 desorption Methods 0.000 description 1
- 229960002593 desoximetasone Drugs 0.000 description 1
- VWVSBHGCDBMOOT-IIEHVVJPSA-N desoximetasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@H](C(=O)CO)[C@@]1(C)C[C@@H]2O VWVSBHGCDBMOOT-IIEHVVJPSA-N 0.000 description 1
- YNNURTVKPVJVEI-GSLJADNHSA-N dichlorisone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2Cl YNNURTVKPVJVEI-GSLJADNHSA-N 0.000 description 1
- 229950009888 dichlorisone Drugs 0.000 description 1
- 150000005690 diesters Chemical group 0.000 description 1
- 229960002124 diflorasone diacetate Drugs 0.000 description 1
- 229960004091 diflucortolone Drugs 0.000 description 1
- OGPWIDANBSLJPC-RFPWEZLHSA-N diflucortolone 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@H](C(=O)CO)[C@@]2(C)C[C@@H]1O OGPWIDANBSLJPC-RFPWEZLHSA-N 0.000 description 1
- NJDNXYGOVLYJHP-UHFFFAOYSA-L disodium;2-(3-oxido-6-oxoxanthen-9-yl)benzoate Chemical compound [Na+].[Na+].[O-]C(=O)C1=CC=CC=C1C1=C2C=CC(=O)C=C2OC2=CC([O-])=CC=C21 NJDNXYGOVLYJHP-UHFFFAOYSA-L 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- BORBLDJNKYHVJP-FXBDTBDDSA-N dolichodial Chemical compound C[C@H]1CC[C@H](C(=C)C=O)[C@@H]1C=O BORBLDJNKYHVJP-FXBDTBDDSA-N 0.000 description 1
- 229950001255 doxibetasol Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000003255 drug test Methods 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 208000024519 eye neoplasm Diseases 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 229950002335 fluazacort Drugs 0.000 description 1
- BYZCJOHDXLROEC-RBWIMXSLSA-N fluazacort Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)=N[C@@]3(C(=O)COC(=O)C)[C@@]1(C)C[C@@H]2O BYZCJOHDXLROEC-RBWIMXSLSA-N 0.000 description 1
- 229960003469 flumetasone Drugs 0.000 description 1
- WXURHACBFYSXBI-GQKYHHCASA-N flumethasone 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)CO)(O)[C@@]2(C)C[C@@H]1O WXURHACBFYSXBI-GQKYHHCASA-N 0.000 description 1
- 229940042902 flumethasone pivalate Drugs 0.000 description 1
- JWRMHDSINXPDHB-OJAGFMMFSA-N flumethasone pivalate 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)COC(=O)C(C)(C)C)(O)[C@@]2(C)C[C@@H]1O JWRMHDSINXPDHB-OJAGFMMFSA-N 0.000 description 1
- 229940043075 fluocinolone Drugs 0.000 description 1
- 229960000785 fluocinonide Drugs 0.000 description 1
- 239000007850 fluorescent dye Substances 0.000 description 1
- 229960001048 fluorometholone Drugs 0.000 description 1
- FAOZLTXFLGPHNG-KNAQIMQKSA-N fluorometholone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@]2(F)[C@@H](O)C[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FAOZLTXFLGPHNG-KNAQIMQKSA-N 0.000 description 1
- YRFXGQHBPBMFHW-SBTZIJSASA-N fluorometholone acetate Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@]2(F)[C@@H](O)C[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 YRFXGQHBPBMFHW-SBTZIJSASA-N 0.000 description 1
- 229960001629 fluorometholone acetate Drugs 0.000 description 1
- YLRFCQOZQXIBAB-RBZZARIASA-N fluoxymesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1CC[C@](C)(O)[C@@]1(C)C[C@@H]2O YLRFCQOZQXIBAB-RBZZARIASA-N 0.000 description 1
- 229960001751 fluoxymesterone Drugs 0.000 description 1
- 229960000618 fluprednisolone Drugs 0.000 description 1
- 239000012737 fresh medium Substances 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 239000012362 glacial acetic acid Substances 0.000 description 1
- 230000004110 gluconeogenesis Effects 0.000 description 1
- 230000004153 glucose metabolism Effects 0.000 description 1
- 230000004190 glucose uptake Effects 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- GGXMRPUKBWXVHE-MIHLVHIWSA-N halometasone Chemical compound C1([C@@H](F)C2)=CC(=O)C(Cl)=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]2(C)C[C@@H]1O GGXMRPUKBWXVHE-MIHLVHIWSA-N 0.000 description 1
- 229960002475 halometasone Drugs 0.000 description 1
- 229950008940 halopredone Drugs 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 208000034737 hemoglobinopathy Diseases 0.000 description 1
- AKRQHOWXVSDJEF-UHFFFAOYSA-N heptane-1-sulfonic acid Chemical compound CCCCCCCS(O)(=O)=O AKRQHOWXVSDJEF-UHFFFAOYSA-N 0.000 description 1
- 229960001067 hydrocortisone acetate Drugs 0.000 description 1
- 229960001524 hydrocortisone butyrate Drugs 0.000 description 1
- 229960003331 hydrocortisone cypionate Drugs 0.000 description 1
- 229960002846 hydrocortisone probutate Drugs 0.000 description 1
- 229960004204 hydrocortisone sodium phosphate Drugs 0.000 description 1
- 229960001401 hydrocortisone sodium succinate Drugs 0.000 description 1
- 229960000631 hydrocortisone valerate Drugs 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
- 150000001261 hydroxy acids Chemical class 0.000 description 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 230000004377 improving vision Effects 0.000 description 1
- 238000007925 in vitro drug release testing Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 description 1
- 238000001746 injection moulding Methods 0.000 description 1
- 210000004692 intercellular junction Anatomy 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 229960002857 isoflupredone Drugs 0.000 description 1
- 229960003317 isoflupredone acetate Drugs 0.000 description 1
- 229960002725 isoflurane Drugs 0.000 description 1
- 229940116871 l-lactate Drugs 0.000 description 1
- 150000003893 lactate salts Chemical class 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 150000002634 lipophilic molecules Chemical class 0.000 description 1
- 239000007791 liquid phase Substances 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 208000018769 loss of vision Diseases 0.000 description 1
- 231100000864 loss of vision Toxicity 0.000 description 1
- 229940080267 lotemax Drugs 0.000 description 1
- 229960001798 loteprednol Drugs 0.000 description 1
- 229960003744 loteprednol etabonate Drugs 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 238000004949 mass spectrometry Methods 0.000 description 1
- 229950001137 meclorisone Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- 229960001011 medrysone Drugs 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 150000002734 metacrylic acid derivatives Chemical class 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 229960001293 methylprednisolone acetate Drugs 0.000 description 1
- PLBHSZGDDKCEHR-LFYFAGGJSA-N methylprednisolone acetate Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(C)=O)CC[C@H]21 PLBHSZGDDKCEHR-LFYFAGGJSA-N 0.000 description 1
- 229960000334 methylprednisolone sodium succinate Drugs 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 208000021971 neovascular inflammatory vitreoretinopathy Diseases 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000004112 neuroprotection Effects 0.000 description 1
- 201000008106 ocular cancer Diseases 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 150000002895 organic esters Chemical class 0.000 description 1
- 150000002905 orthoesters Chemical class 0.000 description 1
- 229960002858 paramethasone Drugs 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 238000005453 pelletization Methods 0.000 description 1
- 235000019371 penicillin G benzathine Nutrition 0.000 description 1
- 229940056360 penicillin g Drugs 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 238000005191 phase separation Methods 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
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 238000002428 photodynamic therapy Methods 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 229920002627 poly(phosphazenes) Polymers 0.000 description 1
- 229920002492 poly(sulfone) Polymers 0.000 description 1
- 229920002401 polyacrylamide Polymers 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920002647 polyamide Polymers 0.000 description 1
- 239000004417 polycarbonate Substances 0.000 description 1
- 229920000515 polycarbonate Polymers 0.000 description 1
- 229950005134 polycarbophil Drugs 0.000 description 1
- 229920000570 polyether Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
- 150000003077 polyols Chemical class 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 239000011118 polyvinyl acetate Substances 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 229960004259 prednisolone tebutate Drugs 0.000 description 1
- 229960004618 prednisone Drugs 0.000 description 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 238000009516 primary packaging Methods 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000006785 proliferative vitreoretinopathy Effects 0.000 description 1
- 229960001371 proparacaine hydrochloride Drugs 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- 125000001453 quaternary ammonium group Chemical group 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 239000000700 radioactive tracer Substances 0.000 description 1
- 210000001927 retinal artery Anatomy 0.000 description 1
- 210000003583 retinal pigment epithelium Anatomy 0.000 description 1
- 230000004233 retinal vasculature Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 229960001487 rimexolone Drugs 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 230000011218 segmentation Effects 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 238000002798 spectrophotometry method Methods 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 201000005428 steroid-induced glaucoma Diseases 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 230000002889 sympathetic effect Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 150000007970 thio esters Chemical class 0.000 description 1
- 102000004217 thyroid hormone receptors Human genes 0.000 description 1
- 108090000721 thyroid hormone receptors Proteins 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 210000001585 trabecular meshwork Anatomy 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 230000007723 transport mechanism Effects 0.000 description 1
- 229960004221 triamcinolone hexacetonide Drugs 0.000 description 1
- 238000009281 ultraviolet germicidal irradiation Methods 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 229940055059 vexol Drugs 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000007966 viscous suspension Substances 0.000 description 1
- 230000004393 visual impairment Effects 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Classifications
-
- 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
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
- A61K31/728—Hyaluronic acid
-
- 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
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- 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
-
- 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
- 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
- A61K9/0051—Ocular inserts, ocular implants
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- 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
-
- 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
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
- A61P27/14—Decongestants or antiallergics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72820905P | 2005-10-18 | 2005-10-18 | |
| PCT/US2006/040429 WO2007047607A2 (en) | 2005-10-18 | 2006-10-17 | Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissues |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ562032A true NZ562032A (en) | 2011-11-25 |
Family
ID=37872252
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ562032A NZ562032A (en) | 2005-10-18 | 2006-10-17 | Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissues |
Country Status (11)
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6375972B1 (en) | 2000-04-26 | 2002-04-23 | Control Delivery Systems, Inc. | Sustained release drug delivery devices, methods of use, and methods of manufacturing thereof |
| US7431710B2 (en) | 2002-04-08 | 2008-10-07 | Glaukos Corporation | Ocular implants with anchors and methods thereof |
| US20090148527A1 (en) * | 2007-12-07 | 2009-06-11 | Robinson Michael R | Intraocular formulation |
| AU2004296376B2 (en) | 2003-12-05 | 2010-03-04 | Bristol-Myers Squibb Company | Inhibitors of type 2 vascular endothelial growth factor receptors |
| US20080220049A1 (en) * | 2003-12-05 | 2008-09-11 | Adnexus, A Bristol-Myers Squibb R&D Company | Compositions and methods for intraocular delivery of fibronectin scaffold domain proteins |
| US20090082321A1 (en) * | 2007-09-21 | 2009-03-26 | Allergan, Inc. | Steroid containing drug delivery systems |
| CN101394834A (zh) | 2005-10-18 | 2009-03-25 | 阿勒根公司 | 用糖皮质激素衍生物选择性渗透后段组织来治疗眼睛 |
| BRPI0719597A2 (pt) | 2006-11-22 | 2013-12-17 | Adnexus A Bristol Myers Squibb R & D Company | Produtos terapêuticos objetivados baseados em proteínas manipuladas para receptores de quinases de tirosina, incluindo igf-ir |
| US11078262B2 (en) * | 2007-04-30 | 2021-08-03 | Allergan, Inc. | High viscosity macromolecular compositions for treating ocular conditions |
| PT2214646T (pt) * | 2007-10-05 | 2021-09-29 | Univ Wayne State | Dendrímeros para libertação sustentada de compostos |
| US8353862B2 (en) | 2007-11-02 | 2013-01-15 | Allergan, Inc. | Drug delivery systems and methods |
| WO2009102421A2 (en) | 2008-02-14 | 2009-08-20 | Bristol-Myers Squibb Company | Targeted therapeutics based on engineered proteins that bind egfr |
| JP2011520961A (ja) | 2008-05-22 | 2011-07-21 | ブリストル−マイヤーズ スクイブ カンパニー | 多価フィブロネクチンをベースとする足場ドメインタンパク質 |
| TWI496582B (zh) | 2008-11-24 | 2015-08-21 | 必治妥美雅史谷比公司 | 雙重專一性之ｅｇｆｒ／ｉｇｆｉｒ結合分子 |
| US9636255B2 (en) | 2009-02-13 | 2017-05-02 | Dose Medical Corporation | Uveoscleral drug delivery implant and methods for implanting the same |
| US20100247606A1 (en) * | 2009-03-25 | 2010-09-30 | Allergan, Inc. | Intraocular sustained release drug delivery systems and methods for treating ocular conditions |
| US10206813B2 (en) | 2009-05-18 | 2019-02-19 | Dose Medical Corporation | Implants with controlled drug delivery features and methods of using same |
| EP2515864A4 (en) * | 2009-12-23 | 2013-09-11 | Psivida Inc | DELAYED RELEASE DELIVERY DEVICES |
| US9562089B2 (en) | 2010-05-26 | 2017-02-07 | Bristol-Myers Squibb Company | Fibronectin based scaffold proteins having improved stability |
| US9668915B2 (en) | 2010-11-24 | 2017-06-06 | Dose Medical Corporation | Drug eluting ocular implant |
| US10463687B2 (en) * | 2011-01-20 | 2019-11-05 | Cornell University | Treatments for retinal disorders |
| US10501779B2 (en) * | 2011-05-12 | 2019-12-10 | President And Fellows Of Harvard College | Oligonucleotide trapping |
| US10245178B1 (en) | 2011-06-07 | 2019-04-02 | Glaukos Corporation | Anterior chamber drug-eluting ocular implant |
| EP2847207B1 (en) | 2012-05-08 | 2019-03-27 | Nicox Ophthalmics, Inc. | Fluticasone propionate nanocrystals |
| US8765725B2 (en) | 2012-05-08 | 2014-07-01 | Aciex Therapeutics, Inc. | Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof |
| US9815865B2 (en) | 2013-01-07 | 2017-11-14 | Nicox Ophthalmics, Inc. | Preparations of hydrophobic therapeutic agents, methods of manufacture and use thereof |
| US10517759B2 (en) | 2013-03-15 | 2019-12-31 | Glaukos Corporation | Glaucoma stent and methods thereof for glaucoma treatment |
| WO2015168347A1 (en) | 2014-04-30 | 2015-11-05 | The Johns Hopkins University | Dendrimer compositions and their use in treatment of diseases of the eye |
| JP6655610B2 (ja) | 2014-05-29 | 2020-02-26 | グローコス コーポレーション | 制御された薬物送達機能を備えるインプラント及びそれを使用する方法 |
| CN115350285A (zh) | 2014-08-13 | 2022-11-18 | 约翰霍普金斯大学 | 树枝状聚合物到脑肿瘤的选择性传递 |
| WO2017040853A1 (en) | 2015-09-02 | 2017-03-09 | Glaukos Corporation | Drug delivery implants with bi-directional delivery capacity |
| US11564833B2 (en) | 2015-09-25 | 2023-01-31 | Glaukos Corporation | Punctal implants with controlled drug delivery features and methods of using same |
| US20180293360A1 (en) * | 2015-10-07 | 2018-10-11 | Genentech, Inc. | Systems and methods for predicting vitreal half-life of therapeutic agent-polymer conjugates |
| JP7003110B2 (ja) | 2016-04-20 | 2022-01-20 | ドーズ メディカル コーポレーション | 生体吸収性眼球薬物送達デバイス |
| CN106983733A (zh) * | 2017-03-08 | 2017-07-28 | 江苏富泽药业有限公司 | 曲安奈德plga缓释微球注射剂、其制备方法及其在制备治疗骨关节炎疼痛药物中的应用 |
| WO2019055028A1 (en) * | 2017-09-15 | 2019-03-21 | Kala Pharmaceuticals, Inc. | PARTICLES, COMPOSITIONS AND METHODS FOR OPHTHALMIC APPLICATIONS AND / OR OTHER APPLICATIONS |
| IL293606A (en) | 2019-12-04 | 2022-08-01 | Ashvattha Therapeutics Inc | Dendrimer preparations and methods of administering a drug to the eye |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4521210A (en) * | 1982-12-27 | 1985-06-04 | Wong Vernon G | Eye implant for relieving glaucoma, and device and method for use therewith |
| US4851521A (en) | 1985-07-08 | 1989-07-25 | Fidia, S.P.A. | Esters of hyaluronic acid |
| EP0244178A3 (en) | 1986-04-28 | 1989-02-08 | Iolab, Inc | Intraocular dosage compositions and method of use |
| US4997652A (en) * | 1987-12-22 | 1991-03-05 | Visionex | Biodegradable ocular implants |
| US4853224A (en) * | 1987-12-22 | 1989-08-01 | Visionex | Biodegradable ocular implants |
| US5164188A (en) * | 1989-11-22 | 1992-11-17 | Visionex, Inc. | Biodegradable ocular implants |
| KR0185215B1 (ko) * | 1990-11-30 | 1999-05-01 | 요시다 쇼오지 | 서방성 안구삽입용 약제 |
| WO1995003009A1 (en) * | 1993-07-22 | 1995-02-02 | Oculex Pharmaceuticals, Inc. | Method of treatment of macular degeneration |
| WO1995003807A1 (en) | 1993-07-27 | 1995-02-09 | The University Of Sydney | Treatment of age-related macular degeneration |
| US5540930A (en) | 1993-10-25 | 1996-07-30 | Pharmos Corporation | Suspension of loteprednol etabonate for ear, eye, or nose treatment |
| US5443505A (en) * | 1993-11-15 | 1995-08-22 | Oculex Pharmaceuticals, Inc. | Biocompatible ocular implants |
| ES2078175B1 (es) * | 1993-12-31 | 1996-10-16 | Cusi Lab | Formulacion farmaceutica conteniendo clobetasona y tobramicina y sus aplicaciones. |
| US5646136A (en) | 1994-01-04 | 1997-07-08 | Duke University | Methods of inhibiting angiogenesis and tumor growth, and treating ophthalmologic conditions with angiostatic and therapeutic steroids |
| US6369116B1 (en) * | 1995-06-02 | 2002-04-09 | Oculex Pharmaceuticals, Inc. | Composition and method for treating glaucoma |
| US5869079A (en) * | 1995-06-02 | 1999-02-09 | Oculex Pharmaceuticals, Inc. | Formulation for controlled release of drugs by combining hydrophilic and hydrophobic agents |
| ES2253787T3 (es) | 1996-11-05 | 2006-06-01 | The Children's Medical Center Corporation | Composiciones para inhibicion de la angiogenesis que comprenden talidomida y un nsaid. |
| WO1999007418A2 (en) * | 1997-08-11 | 1999-02-18 | Allergan Sales, Inc. | Sterile bioerodible implant device with improved biocompatability and method |
| US6331313B1 (en) * | 1999-10-22 | 2001-12-18 | Oculex Pharmaceticals, Inc. | Controlled-release biocompatible ocular drug delivery implant devices and methods |
| AUPQ496500A0 (en) * | 2000-01-06 | 2000-02-03 | University Of Sydney, The | Kit |
| US6726918B1 (en) * | 2000-07-05 | 2004-04-27 | Oculex Pharmaceuticals, Inc. | Methods for treating inflammation-mediated conditions of the eye |
| AU3649502A (en) * | 2000-11-29 | 2002-06-11 | Oculex Pharm Inc | Methods for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor |
| US20030185892A1 (en) | 2001-08-17 | 2003-10-02 | Bell Steve J. D. | Intraocular delivery compositions and methods |
| ATE426638T1 (de) | 2001-12-12 | 2009-04-15 | Rhodia Chimie Sa | Formulierung enthaltend eine anionische verbindung, ein polyionisches polymer und ein copolymer |
| US6873524B2 (en) * | 2002-08-15 | 2005-03-29 | Audavi Corporation | Data storage device |
| US20050048099A1 (en) * | 2003-01-09 | 2005-03-03 | Allergan, Inc. | Ocular implant made by a double extrusion process |
| CN1750828A (zh) * | 2003-02-20 | 2006-03-22 | 爱尔康公司 | 类固醇治疗眼病患者的用途 |
| US20050101582A1 (en) * | 2003-11-12 | 2005-05-12 | Allergan, Inc. | Compositions and methods for treating a posterior segment of an eye |
| CA2553381C (en) * | 2004-01-20 | 2011-03-22 | Allergan, Inc. | Compositions for localized therapy of the eye, comprising preferably triamcinolone acetonide and hyaluronic acid |
| US8119154B2 (en) * | 2004-04-30 | 2012-02-21 | Allergan, Inc. | Sustained release intraocular implants and related methods |
| CN101394834A (zh) * | 2005-10-18 | 2009-03-25 | 阿勒根公司 | 用糖皮质激素衍生物选择性渗透后段组织来治疗眼睛 |
| JP2007309763A (ja) | 2006-05-18 | 2007-11-29 | Sumitomo Electric Ind Ltd | 電線の表面欠陥検出装置 |
-
2006
- 2006-10-17 CN CNA2006800164791A patent/CN101394834A/zh active Pending
- 2006-10-17 NZ NZ562032A patent/NZ562032A/en unknown
- 2006-10-17 BR BRPI0613401A patent/BRPI0613401B8/pt active IP Right Grant
- 2006-10-17 MX MX2012007846A patent/MX339797B/es unknown
- 2006-10-17 EP EP06826056.1A patent/EP1937210B1/en active Active
- 2006-10-17 KR KR1020077028609A patent/KR101430760B1/ko active IP Right Grant
- 2006-10-17 WO PCT/US2006/040429 patent/WO2007047607A2/en active Application Filing
- 2006-10-17 MX MX2007012061A patent/MX2007012061A/es active IP Right Grant
- 2006-10-17 AU AU2006304416A patent/AU2006304416B2/en active Active
- 2006-10-17 CA CA2602577A patent/CA2602577C/en active Active
- 2006-10-17 JP JP2008536724A patent/JP5745208B2/ja active Active
- 2006-10-18 US US11/550,642 patent/US8062657B2/en active Active
-
2011
- 2011-11-17 US US13/299,215 patent/US8840872B2/en active Active
-
2013
- 2013-10-11 JP JP2013213746A patent/JP2014028855A/ja not_active Withdrawn
-
2014
- 2014-08-19 US US14/463,034 patent/US9259429B2/en active Active
-
2016
- 2016-02-15 US US15/043,750 patent/US9820995B2/en active Active
-
2017
- 2017-11-20 US US15/818,089 patent/US10188665B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US10188665B2 (en) | 2019-01-29 |
| CA2602577A1 (en) | 2007-04-26 |
| MX2007012061A (es) | 2007-12-13 |
| US20140357609A1 (en) | 2014-12-04 |
| AU2006304416B2 (en) | 2013-03-28 |
| US20160158249A1 (en) | 2016-06-09 |
| EP1937210B1 (en) | 2017-05-31 |
| CN101394834A (zh) | 2009-03-25 |
| BRPI0613401B8 (pt) | 2021-05-25 |
| CA2602577C (en) | 2015-03-31 |
| BRPI0613401B1 (pt) | 2020-08-04 |
| BRPI0613401A2 (pt) | 2011-01-11 |
| MX339797B (es) | 2016-06-10 |
| US8062657B2 (en) | 2011-11-22 |
| US9259429B2 (en) | 2016-02-16 |
| US20120065178A1 (en) | 2012-03-15 |
| US20180125861A1 (en) | 2018-05-10 |
| KR101430760B1 (ko) | 2014-08-19 |
| JP2014028855A (ja) | 2014-02-13 |
| JP2009511632A (ja) | 2009-03-19 |
| EP1937210A2 (en) | 2008-07-02 |
| WO2007047607A3 (en) | 2007-11-15 |
| KR20080055749A (ko) | 2008-06-19 |
| US20070088014A1 (en) | 2007-04-19 |
| US9820995B2 (en) | 2017-11-21 |
| US8840872B2 (en) | 2014-09-23 |
| JP5745208B2 (ja) | 2015-07-08 |
| WO2007047607A2 (en) | 2007-04-26 |
| AU2006304416A1 (en) | 2007-04-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10188665B2 (en) | Ocular therapy using glucocorticoid derivatives selectively penetrating posterior segment tissues | |
| CA2700072C (en) | Steroid containing drug delivery systems | |
| US20190015425A1 (en) | Ocular implant made by a double extrusion proces | |
| US20140010823A1 (en) | Method for determining optimum intraocular locations for drug delivery systems | |
| US20050271705A1 (en) | Retinoid-containing sustained release intraocular drug delivery system and related methods | |
| EP1991205A1 (en) | Ocular therapy using sirtuin-activating agents | |
| AU2014201844B2 (en) | Ocular implant made by a double extrusion process |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) | ||
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 3 YEARS UNTIL 17 OCT 2016 BY COMPUTER PACKAGES INC Effective date: 20131026 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2017 BY COMPUTER PACKAGES INC Effective date: 20161001 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2018 BY COMPUTER PACKAGES INC Effective date: 20171003 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2019 BY COMPUTER PACKAGES INC Effective date: 20181002 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2020 BY COMPUTER PACKAGES INC Effective date: 20191001 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2021 BY COMPUTER PACKAGES INC Effective date: 20201001 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2022 BY THOMSON REUTERS Effective date: 20210902 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2023 BY THOMSON REUTERS Effective date: 20220902 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 17 OCT 2024 BY THOMSON REUTERS Effective date: 20230904 |