RU2006104983A - Доставка активного лекарства к дальней области глаза посредством субконъюнктивальной или периокулярной доставки пролекарства - Google Patents
Доставка активного лекарства к дальней области глаза посредством субконъюнктивальной или периокулярной доставки пролекарства Download PDFInfo
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- RU2006104983A RU2006104983A RU2006104983/14A RU2006104983A RU2006104983A RU 2006104983 A RU2006104983 A RU 2006104983A RU 2006104983/14 A RU2006104983/14 A RU 2006104983/14A RU 2006104983 A RU2006104983 A RU 2006104983A RU 2006104983 A RU2006104983 A RU 2006104983A
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- Prior art keywords
- active drug
- prodrug
- eye
- active
- drug
- Prior art date
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- 229940079593 drug Drugs 0.000 claims 21
- 239000003814 drug Substances 0.000 claims 21
- 238000000034 method Methods 0.000 claims 18
- 229940002612 prodrug Drugs 0.000 claims 12
- 239000000651 prodrug Substances 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 238000002347 injection Methods 0.000 claims 6
- 239000007924 injection Substances 0.000 claims 6
- 239000005557 antagonist Substances 0.000 claims 5
- 210000004127 vitreous body Anatomy 0.000 claims 4
- HVAUUPRFYPCOCA-AREMUKBSSA-N 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCOC[C@@H](OC(C)=O)COP([O-])(=O)OCC[N+](C)(C)C HVAUUPRFYPCOCA-AREMUKBSSA-N 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 108010003541 Platelet Activating Factor Proteins 0.000 claims 3
- 239000011859 microparticle Substances 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000007774 longterm Effects 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 229940127557 pharmaceutical product Drugs 0.000 claims 2
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims 1
- 206010048843 Cytomegalovirus chorioretinitis Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- 201000007737 Retinal degeneration Diseases 0.000 claims 1
- 206010038848 Retinal detachment Diseases 0.000 claims 1
- 206010038934 Retinopathy proliferative Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- OGQICQVSFDPSEI-UHFFFAOYSA-N Zorac Chemical compound N1=CC(C(=O)OCC)=CC=C1C#CC1=CC=C(SCCC2(C)C)C2=C1 OGQICQVSFDPSEI-UHFFFAOYSA-N 0.000 claims 1
- 239000000674 adrenergic antagonist Substances 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 1
- 230000003532 cataractogenesis Effects 0.000 claims 1
- 239000000064 cholinergic agonist Substances 0.000 claims 1
- 210000003161 choroid Anatomy 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 208000001763 cytomegalovirus retinitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940052760 dopamine agonists Drugs 0.000 claims 1
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 239000004005 microsphere Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 210000001328 optic nerve Anatomy 0.000 claims 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 210000001525 retina Anatomy 0.000 claims 1
- 230000004264 retinal detachment Effects 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 210000003583 retinal pigment epithelium Anatomy 0.000 claims 1
- 150000004492 retinoid derivatives Chemical class 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 210000003786 sclera Anatomy 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 230000002459 sustained effect Effects 0.000 claims 1
- 229960000565 tazarotene Drugs 0.000 claims 1
- 210000001760 tenon capsule Anatomy 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
Classifications
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- 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
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K31/203—Retinoic acids ; Salts thereof
-
- 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
-
- 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
- A61P27/12—Ophthalmic agents for cataracts
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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)
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (20)
1. Способ продолжительной доставки активного лекарства в дальнюю область глаза млекопитающего для лечения или предотвращения заболевания или состояния, поражающего указанного млекопитающего, где указанное заболевание или состояние можно излечить или предотвратить действием указанного лекарства на дальнюю область глаза, включающий субконъюнктивальное или периокулярное введение эффективного количества пролекарства, представляющего собой эфирное производное активного лекарства, причем активное лекарство более чем в 10 раз активней пролекарства.
2. Способ по п.1, в котором активное лекарство или пролекарство катарактогенно.
3. Способ по п.1, в котором активное лекарство представляет собой карбоновую кислоту или ее соль.
4. Способ по п.1, в котором активное лекарство выбрано из группы, включающей ретиноиды, простагландины, антагонисты альфа-2-адренорецепторов, антагонисты бета-адренорецепторов, дофаминергические агонисты, холинергические агонисты, ингибиторы тирозин-киназы, противовоспалительные средства, кортикостероиды, N-метил-D-аспартат-антагонисты (NMDA-антагонисты), противоопухолевые средства и антигистамины.
5. Способ по п.1, в котором активное лекарство является спиртом.
6. Способ по п.1, в котором активное лекарство является ретиноидом.
7. Способ по п.1, в котором активное лекарство является тазаротеновой кислотой.
8. Способ по п.1, в котором пролекарство представляет собой тазаротен.
9. Способ по п.1, в котором пролекарство представляет собой эфир фосфор- или серосодержащей кислоты.
10. Способ по п.1, где пролекарство содержится в системе полимерных микрочастиц, пригодной для улучшения продолжительной направленной доставки указанного активного лекарства.
11. Способ по п.10, где указанной системой полимерных микрочастиц является суспензия микросфер из поли(лактидгликолид)а.
12. Способ по п.1, где указанная дальняя область глаза включает увеальный тракт, стекловидное тело, сетчатку, хориоид, зрительный нерв или пигментный эпителий сетчатки.
13. Способ по п.1, где указанное заболевание или состояние представляет собой пигментную дегенерацию сетчатки, пролиферативную ретинопатию стекловидного тела, возрастную дегенерацию желтого пятна, диабетическую ретинопатию, диабетический отек пятна, отслойку сетчатки, разрыв сетчатки, увеит или цитомегаловирусный ретинит.
14. Способ по п.1, в котором пролекарство вводят путем инъекции.
15. Способ по п.1, в котором пролекарство вводят субконъюнктивально, в склеру, супра-хориоидально, под тенонову капсулу, ретробульбарно или перибульбарно.
16. Способ по п.1, в котором введение лекарства осуществляют субконъюнктивально.
17. Способ по п.1, в котором активное лекарство не является антагонистом фактора активации тромбоцитов.
18. Способ лечения или предупреждения заболевания или состояния, где лечение или предупреждение вышеуказанного заболевания или состояния достигается действием активного лекарства на дальнюю область глаза пораженного млекопитающего, при котором осуществляют введение эффективного количества пролекарства, представляющего собой эфир карбоновой кислоты активного лекарства, субконъюнктивальной или периокулярной инъекцией, причем пролекарство содержится в системе полимерных микрочастиц, пригодной для улучшения продолжительной доставки указанного активного лекарства, и при этом активное лекарство более чем в 10 раз активней пролекарства и не является антагонистом фактора активации тромбоцитов.
19. Фармацевтический продукт, включающий
а) композицию, содержащую эффективную концентрацию пролекарства, представляющего собой эфирное производное активного лекарства, причем воздействие указанного лекарства на дальнюю часть глаза млекопитающих эффективно при лечении или предупреждении заболевания или состояния, затрагивающего указанную дальнюю область глаза, и при этом активное лекарство более чем в 10 раз активней пролекарства, и
б) подходящую упаковку, содержащую инструкцию по применению, в которой указано, что продукт следует применять для лечения вышеуказанного заболевания или состояния посредством периокулярной или субконъюнктивальной инъекции, причем в инструкции не указано, что продукт следует вводить инъекцией в стекловидное тело или внутрь глаза, или же в инструкции указано или советуется предпочтительное введение субконъюнктивальной или периокулярной инъекцией по сравнению с инъекцией в стекловидное тело либо внутрь глаза.
20. Фармацевтический продукт по п.19, в котором активное лекарство не является антагонистом фактора активации тромбоцитов.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/617,468 | 2003-07-10 | ||
| US10/617,468 US20050009910A1 (en) | 2003-07-10 | 2003-07-10 | Delivery of an active drug to the posterior part of the eye via subconjunctival or periocular delivery of a prodrug |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2006104983A true RU2006104983A (ru) | 2006-06-27 |
| RU2353393C2 RU2353393C2 (ru) | 2009-04-27 |
Family
ID=33564972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2006104983/14A RU2353393C2 (ru) | 2003-07-10 | 2004-07-07 | Доставка активного лекарства к дальней области глаза посредством субконъюнктивальной или периокулярной доставки пролекарства |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20050009910A1 (ru) |
| EP (1) | EP1644047A2 (ru) |
| JP (1) | JP2007528851A (ru) |
| KR (1) | KR20060033008A (ru) |
| CN (1) | CN1882362A (ru) |
| AU (1) | AU2004260645B2 (ru) |
| BR (1) | BRPI0412496A (ru) |
| CA (1) | CA2531753A1 (ru) |
| IL (1) | IL172583A (ru) |
| MX (1) | MXPA06000408A (ru) |
| NO (1) | NO20056174L (ru) |
| NZ (2) | NZ582376A (ru) |
| PL (1) | PL380169A1 (ru) |
| RU (1) | RU2353393C2 (ru) |
| WO (1) | WO2005011741A2 (ru) |
| ZA (1) | ZA200510129B (ru) |
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| US20050101582A1 (en) | 2003-11-12 | 2005-05-12 | Allergan, Inc. | Compositions and methods for treating a posterior segment of an eye |
| US20050250737A1 (en) * | 2003-11-12 | 2005-11-10 | Allergan, Inc. | Therapeutic ophthalmic compositions containing retinal friendly excipients and related methods |
| CA2549161A1 (en) * | 2003-12-02 | 2005-06-23 | Allergan, Inc. | Prevention and/or reduction of photoreceptor degeneration with retinoids |
| US8871224B2 (en) * | 2003-12-09 | 2014-10-28 | Allergan, Inc. | Botulinum toxin therapy for skin disorders |
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| US20050220734A1 (en) * | 2004-04-02 | 2005-10-06 | Allergan, Inc. | Therapy for melanin related afflictions |
| US7771742B2 (en) | 2004-04-30 | 2010-08-10 | Allergan, Inc. | Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods |
| AU2005240078A1 (en) * | 2004-04-30 | 2005-11-17 | Allergan, Inc. | Retinoid-containing sustained release intraocular drug delivery systems and related methods of manufacturing |
| WO2005107708A1 (en) | 2004-04-30 | 2005-11-17 | Allergan, Inc. | Biodegradable intravitreal tyrosine kinase inhibitors implants |
| AU2011211380B9 (en) * | 2004-04-30 | 2014-05-08 | Allergan, Inc. | Biodegradable intravitreal tyrosine kinase inhibitor implants |
| US20060089590A1 (en) * | 2004-10-27 | 2006-04-27 | John Higuchi | Methods and devices for sustained in-vivo release of an active agent |
| PL1959925T3 (pl) * | 2005-12-02 | 2017-05-31 | (Osi) Eyetech, Inc. | Mikrocząstki o kontrolowanym uwalnianiu |
| US20070202186A1 (en) | 2006-02-22 | 2007-08-30 | Iscience Interventional Corporation | Apparatus and formulations for suprachoroidal drug delivery |
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| EP1864668B1 (en) | 2006-06-01 | 2012-11-21 | Novagali Pharma S.A. | Use of prodrugs for ocular intravitreous administration |
| US10022348B2 (en) | 2009-05-20 | 2018-07-17 | Sun Pharmaceutical Industries Limited | Topical solution of isotretinoin |
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| US20120157499A1 (en) | 2012-06-21 |
| WO2005011741A2 (en) | 2005-02-10 |
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| WO2005011741A3 (en) | 2005-04-14 |
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| CN1882362A (zh) | 2006-12-20 |
| EP1644047A2 (en) | 2006-04-12 |
| AU2004260645B2 (en) | 2010-03-11 |
| ZA200510129B (en) | 2007-02-28 |
| IL172583A (en) | 2011-02-28 |
| NZ582376A (en) | 2012-02-24 |
| MXPA06000408A (es) | 2006-03-17 |
| BRPI0412496A (pt) | 2006-09-19 |
| IL172583A0 (en) | 2006-04-10 |
| AU2004260645A1 (en) | 2005-02-10 |
| NO20056174L (no) | 2006-01-25 |
| NZ544027A (en) | 2010-07-30 |
| CA2531753A1 (en) | 2005-02-10 |
| PL380169A1 (pl) | 2007-01-08 |
| RU2353393C2 (ru) | 2009-04-27 |
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