CA2455680A1 - Ophthalmic depot formulations for periocular or subconjunctival administration - Google Patents
Ophthalmic depot formulations for periocular or subconjunctival administration Download PDFInfo
- Publication number
- CA2455680A1 CA2455680A1 CA002455680A CA2455680A CA2455680A1 CA 2455680 A1 CA2455680 A1 CA 2455680A1 CA 002455680 A CA002455680 A CA 002455680A CA 2455680 A CA2455680 A CA 2455680A CA 2455680 A1 CA2455680 A1 CA 2455680A1
- Authority
- CA
- Canada
- Prior art keywords
- active agent
- formulation
- polymer
- formulation according
- depot
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- 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)
Abstract
The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctiv al administration.
Claims (16)
1. An ophthalmic depot formulation comprising an active agent for periocular or subconjunctival administration.
2. A formulation according to claim 1 comprising of microparticles of essentially pure active agent.
3. A formulation according to claim 1 wherein the active agent is embedded in a biocompatible pharmacologically acceptable polymer or a lipid encapsulating agent.
4. A formulation according to claim 1 or 3 wherein the polymer is a polylactide-co-glycolide ester of a polyol.
5. A formulation according to any one of claims 1, 3 or 4 wherein the polymer is a 40/60 to 60/40 polylactide-co-glycolide ester of a polyol.
6. A formulation according to any one of claims 1, and 3 to 5 comprising microparticles.
7. A formulation according to claim 6 wherein the external surface of the microparticles is substantially free of active agent.
8. A liquid formulation comprising a dissolved pharmaceutical acceptable polymer and a dissolved or dispersed active agent which formulation upon injection forms a depot at the injection site.
9. A formulation according to any preceding claim wherein the active agent is present in an amount of up to 300 mg per dose for single administration.
10. A formulation according to any preceding claim wherein the active agent is a staurosporine of formula (I), a phthalazine of formula (II) or an ophthalmically acceptable salt thereof.
11. A method for treating an ocular disease which comprises:
i) providing a depot formulation comprising an active agent, and ii) introducing said depot formulation periocularly or subconjunctivally.
i) providing a depot formulation comprising an active agent, and ii) introducing said depot formulation periocularly or subconjunctivally.
12. A method according to claim 11 wherein the active agent is embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent.
13. A method according to claim 11 or 12 wherein the active agent diffuses from said depot formulation to the site of said ocular disease.
14. A method according to any one of claims 11 to 13 wherein the active agent is maintained at an effective dosage for said ocular disease at the site of said ocular disease for an extended period of time.
15. A method according to any one of claims 11 to 14 wherein the active agent is maintained at an effective dosage for up to 3 months.
16. A microparticle comprising a staurosporine of formula (I), a phthalazine of formula (II) or an ophthalmically acceptable salt thereof embedded in a biocompatible pharma-cologically acceptable polymer or a lipid encapsulating agent.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0122318.9 | 2001-09-14 | ||
GBGB0122318.9A GB0122318D0 (en) | 2001-09-14 | 2001-09-14 | Organic compounds |
PCT/EP2002/010314 WO2003024420A1 (en) | 2001-09-14 | 2002-09-13 | Ophthalmic depot formulations for periocular or subconjunctival administration |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2455680A1 true CA2455680A1 (en) | 2003-03-27 |
CA2455680C CA2455680C (en) | 2010-07-20 |
Family
ID=9922147
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2455680A Expired - Fee Related CA2455680C (en) | 2001-09-14 | 2002-09-13 | Ophthalmic depot formulations for periocular or subconjunctival administration |
Country Status (25)
Country | Link |
---|---|
US (4) | US20040234611A1 (en) |
EP (1) | EP1429725B1 (en) |
JP (3) | JP2005504797A (en) |
KR (1) | KR20040030869A (en) |
CN (2) | CN102008428A (en) |
AT (1) | ATE389385T1 (en) |
AU (1) | AU2002342694B2 (en) |
BR (1) | BR0212475A (en) |
CA (1) | CA2455680C (en) |
CO (1) | CO5560548A2 (en) |
DE (1) | DE60225701T2 (en) |
EC (1) | ECSP044967A (en) |
ES (1) | ES2302849T3 (en) |
GB (1) | GB0122318D0 (en) |
HK (1) | HK1066733A1 (en) |
HU (1) | HU229453B1 (en) |
IL (2) | IL160027A0 (en) |
MX (1) | MXPA04002421A (en) |
NO (1) | NO333825B1 (en) |
NZ (1) | NZ531481A (en) |
PL (1) | PL203949B1 (en) |
PT (1) | PT1429725E (en) |
RU (1) | RU2316315C2 (en) |
WO (1) | WO2003024420A1 (en) |
ZA (1) | ZA200400524B (en) |
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US9657294B2 (en) | 2002-02-20 | 2017-05-23 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA) |
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- 2001-09-14 GB GBGB0122318.9A patent/GB0122318D0/en not_active Ceased
-
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- 2002-09-13 AT AT02779354T patent/ATE389385T1/en active
- 2002-09-13 CA CA2455680A patent/CA2455680C/en not_active Expired - Fee Related
- 2002-09-13 PT PT02779354T patent/PT1429725E/en unknown
- 2002-09-13 CN CN2010105534172A patent/CN102008428A/en active Pending
- 2002-09-13 MX MXPA04002421A patent/MXPA04002421A/en active IP Right Grant
- 2002-09-13 JP JP2003528517A patent/JP2005504797A/en not_active Withdrawn
- 2002-09-13 KR KR10-2004-7001255A patent/KR20040030869A/en active Search and Examination
- 2002-09-13 NZ NZ531481A patent/NZ531481A/en not_active IP Right Cessation
- 2002-09-13 PL PL368128A patent/PL203949B1/en not_active IP Right Cessation
- 2002-09-13 US US10/489,752 patent/US20040234611A1/en not_active Abandoned
- 2002-09-13 AU AU2002342694A patent/AU2002342694B2/en not_active Ceased
- 2002-09-13 DE DE60225701T patent/DE60225701T2/en not_active Expired - Lifetime
- 2002-09-13 RU RU2004111596/15A patent/RU2316315C2/en not_active IP Right Cessation
- 2002-09-13 ES ES02779354T patent/ES2302849T3/en not_active Expired - Lifetime
- 2002-09-13 HU HU0401568A patent/HU229453B1/en not_active IP Right Cessation
- 2002-09-13 IL IL16002702A patent/IL160027A0/en unknown
- 2002-09-13 WO PCT/EP2002/010314 patent/WO2003024420A1/en active IP Right Grant
- 2002-09-13 EP EP02779354A patent/EP1429725B1/en not_active Expired - Lifetime
- 2002-09-13 BR BR0212475-0A patent/BR0212475A/en not_active IP Right Cessation
- 2002-09-13 CN CNA028155742A patent/CN1538835A/en active Pending
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2004
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- 2004-01-23 ZA ZA200400524A patent/ZA200400524B/en unknown
- 2004-02-02 EC EC2004004967A patent/ECSP044967A/en unknown
- 2004-02-18 CO CO04013821A patent/CO5560548A2/en not_active Application Discontinuation
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- 2004-12-10 HK HK04109814A patent/HK1066733A1/en unknown
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2008
- 2008-08-20 US US12/194,617 patent/US20080305172A1/en not_active Abandoned
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2010
- 2010-10-01 JP JP2010224231A patent/JP2011026338A/en not_active Withdrawn
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2012
- 2012-06-14 US US13/523,537 patent/US20120269894A1/en not_active Abandoned
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2013
- 2013-01-07 US US13/735,076 patent/US20130122064A1/en not_active Abandoned
- 2013-05-09 JP JP2013099024A patent/JP2013147516A/en active Pending
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