ZA200109517B - Pharmaceutical preparation containing the active substance diamorphine and its utilization in a method for treating opiate addiction. - Google Patents
Pharmaceutical preparation containing the active substance diamorphine and its utilization in a method for treating opiate addiction. Download PDFInfo
- Publication number
- ZA200109517B ZA200109517B ZA200109517A ZA200109517A ZA200109517B ZA 200109517 B ZA200109517 B ZA 200109517B ZA 200109517 A ZA200109517 A ZA 200109517A ZA 200109517 A ZA200109517 A ZA 200109517A ZA 200109517 B ZA200109517 B ZA 200109517B
- Authority
- ZA
- South Africa
- Prior art keywords
- active substance
- morphine
- diamorphine
- derivative
- opiate
- Prior art date
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Classifications
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- 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
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- 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
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
- A61K9/7061—Polyacrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19923551A DE19923551A1 (de) | 1999-05-21 | 1999-05-21 | Pharmazeutisches Präparat mit dem Wirkstoff Diamorphin und seine Verwendung in einem Verfahren zur Behandlung der Opiatsucht |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200109517B true ZA200109517B (en) | 2002-09-26 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200109517A ZA200109517B (en) | 1999-05-21 | 2001-11-19 | Pharmaceutical preparation containing the active substance diamorphine and its utilization in a method for treating opiate addiction. |
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| US (1) | US20050053647A1 (zh) |
| EP (1) | EP1183029B1 (zh) |
| JP (1) | JP4892148B2 (zh) |
| KR (1) | KR100742471B1 (zh) |
| CN (1) | CN100457107C (zh) |
| AR (1) | AR024013A1 (zh) |
| AT (1) | ATE300301T1 (zh) |
| AU (1) | AU772139B2 (zh) |
| BR (1) | BR0011286A (zh) |
| CA (1) | CA2372339C (zh) |
| CZ (1) | CZ301230B6 (zh) |
| DE (2) | DE19923551A1 (zh) |
| DK (1) | DK1183029T3 (zh) |
| ES (1) | ES2245311T3 (zh) |
| HU (1) | HUP0201349A3 (zh) |
| IL (2) | IL146277A0 (zh) |
| MX (1) | MXPA01011921A (zh) |
| NZ (1) | NZ515301A (zh) |
| PL (1) | PL196741B1 (zh) |
| PT (1) | PT1183029E (zh) |
| RU (1) | RU2254130C2 (zh) |
| TR (1) | TR200103302T2 (zh) |
| TW (1) | TWI241910B (zh) |
| WO (1) | WO2000071125A2 (zh) |
| ZA (1) | ZA200109517B (zh) |
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| DE19960154A1 (de) * | 1999-12-14 | 2001-07-12 | Lohmann Therapie Syst Lts | Flache Arzneizubereitung zur transmucosalen Verabreichung von Oxycodon oder einem vergleichbaren Wirkstoff in der Mundhöhle, für die Anwendung in der Schmerztherapie und Suchttherapie |
| US6958389B2 (en) * | 2000-09-08 | 2005-10-25 | San-Ei Gen F.F.I. Inc. | Tetraphenylbacteriochlorin derivatives and compositions containing the same |
| WO2003002071A2 (en) * | 2001-06-29 | 2003-01-09 | Lewandowski Leon J | Individualized addiction cessation therapy |
| DE10159745A1 (de) | 2001-12-05 | 2003-07-03 | Lohmann Therapie Syst Lts | Transdermales Therapeutisches System mit verbessertem Langzeittragekomfort |
| WO2003049774A1 (en) * | 2001-12-13 | 2003-06-19 | Vital Health Sciences Pty Ltd | Transdermal transport of compounds |
| DE10237057A1 (de) * | 2002-08-09 | 2004-03-25 | Grünenthal GmbH | Opioid-Rezeptor-Antagonisten in Pflasterformulierungen |
| AU2002950713A0 (en) | 2002-08-09 | 2002-09-12 | Vital Health Sciences Pty Ltd | Carrier |
| KR101341359B1 (ko) * | 2004-10-01 | 2013-12-13 | 램스코르 인코포레이티드 | 편리하게 이식가능한 서방형 약물 조성물 |
| EP1893159B1 (en) | 2005-06-17 | 2015-09-30 | Vital Health Sciences Pty Ltd. | A carrier comprising one or more di- and/or monophosphate derivatives of electron transfer agents |
| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| US20070148448A1 (en) * | 2005-12-28 | 2007-06-28 | Kimberly-Clark Worldwide, Inc. | Microencapsulated delivery vehicles including cooling agents |
| US20070145619A1 (en) * | 2005-12-28 | 2007-06-28 | Kimberly-Clark Worldwide, Inc. | Processes for producing microencapsulated delivery vehicles |
| US20070149435A1 (en) * | 2005-12-28 | 2007-06-28 | Kimberly-Clark Worldwide, Inc. | Cleansing composition including microencapsulated delivery vehicles |
| US7442439B2 (en) * | 2005-12-28 | 2008-10-28 | Kimberly-Clark Worldwide, Inc. | Microencapsulated heat delivery vehicles |
| US20070202185A1 (en) * | 2005-12-28 | 2007-08-30 | Kimberly-Clark Worldwide, Inc. | Microencapsulated Delivery Vehicles Having Fugitive Layers |
| US7914891B2 (en) * | 2005-12-28 | 2011-03-29 | Kimberly-Clark Worldwide, Inc. | Wipes including microencapsulated delivery vehicles and phase change materials |
| US20070145618A1 (en) * | 2005-12-28 | 2007-06-28 | Kimberly-Clark Worldwide, Inc. | Methods of making microencapsulated delivery vehicles |
| US20070148446A1 (en) * | 2005-12-28 | 2007-06-28 | Kimberly-Clark Worldwide, Inc. | Wipes including microencapsulated delivery vehicles and processes of producing the same |
| US20070148459A1 (en) * | 2005-12-28 | 2007-06-28 | Kimberly-Clark Worldwide, Inc. | Microencapsulated delivery vehicles |
| US7497351B2 (en) | 2006-05-30 | 2009-03-03 | Kimberly-Clark Worldwide, Inc. | Wet wipe dispensing system |
| US7654412B2 (en) * | 2006-05-30 | 2010-02-02 | Kimberly-Clark Worldwide, Inc. | Wet wipe dispensing system for dispensing warm wet wipes |
| US7648046B2 (en) * | 2006-05-30 | 2010-01-19 | Kimberly-Clark Worldwide, Inc. | Dispensing system for dispensing warm wet wipes |
| US7799352B2 (en) * | 2006-08-09 | 2010-09-21 | Korea Atomic Energy Research Institute | Therapeutic hydrogel for atopic dermatitis and preparation method thereof |
| US8192841B2 (en) * | 2006-12-14 | 2012-06-05 | Kimberly-Clark Worldwide, Inc. | Microencapsulated delivery vehicle having an aqueous core |
| WO2008136699A1 (fr) * | 2007-05-04 | 2008-11-13 | Igor Alexandrovich Bazikov | Patch transdermique à microcapsules et procédé de fabrication correspondant |
| BRPI0811319A2 (pt) | 2007-05-25 | 2015-02-10 | Tolmar Therapeutics Inc | Composição fluida, método de formação de uma composição fluida, implante biodegrádavel formado in situ, método de formação de um implante biodegradável in situ, kit, implante e método de trataento |
| US7924142B2 (en) * | 2008-06-30 | 2011-04-12 | Kimberly-Clark Worldwide, Inc. | Patterned self-warming wipe substrates |
| EP2531047A4 (en) | 2010-02-05 | 2014-03-19 | Phosphagenics Ltd | CARRIER WITH AN UNINUTRALIZED TOCOPHERYL PHOSPHATE |
| ES2829386T3 (es) | 2010-03-30 | 2021-05-31 | Phosphagenics Ltd | Parche de administración transdérmica |
| US9272044B2 (en) | 2010-06-08 | 2016-03-01 | Indivior Uk Limited | Injectable flowable composition buprenorphine |
| GB2513060B (en) | 2010-06-08 | 2015-01-07 | Rb Pharmaceuticals Ltd | Microparticle buprenorphine suspension |
| WO2012122586A1 (en) | 2011-03-15 | 2012-09-20 | Phosphagenics Limited | New composition |
| US20150231130A1 (en) | 2012-07-26 | 2015-08-20 | Wockhardt Limited | Pharmaceutical composition comprising diamorphine for intranasal administration |
| GB201404139D0 (en) | 2014-03-10 | 2014-04-23 | Rb Pharmaceuticals Ltd | Sustained release buprenorphine solution formulations |
| CN108601732A (zh) | 2015-12-09 | 2018-09-28 | 磷肌酸有限公司 | 药物制剂 |
| MX2019006845A (es) | 2016-12-21 | 2019-10-15 | Avecho Biotechnology Ltd | Proceso. |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3797494A (en) * | 1969-04-01 | 1974-03-19 | Alza Corp | Bandage for the administration of drug by controlled metering through microporous materials |
| US3760805A (en) * | 1971-01-13 | 1973-09-25 | Alza Corp | Osmotic dispenser with collapsible supply container |
| US3742951A (en) * | 1971-08-09 | 1973-07-03 | Alza Corp | Bandage for controlled release of vasodilators |
| US3996934A (en) * | 1971-08-09 | 1976-12-14 | Alza Corporation | Medical bandage |
| US3987790A (en) * | 1975-10-01 | 1976-10-26 | Alza Corporation | Osmotically driven fluid dispenser |
| US4031894A (en) * | 1975-12-08 | 1977-06-28 | Alza Corporation | Bandage for transdermally administering scopolamine to prevent nausea |
| US4626539A (en) * | 1984-08-10 | 1986-12-02 | E. I. Dupont De Nemours And Company | Trandermal delivery of opioids |
| DE3902013A1 (de) * | 1989-01-25 | 1990-09-20 | Knoll Ag | Pflaster zur transdermalen anwendung |
| DE3939376C1 (zh) * | 1989-11-29 | 1991-05-08 | Lts Lohmann Therapie-Systeme Gmbh & Co. Kg, 5450 Neuwied, De | |
| SE9003665D0 (sv) * | 1990-11-16 | 1990-11-16 | Kabivitrum Ab | Morphine prodrugs |
| AU1183092A (en) * | 1991-02-06 | 1992-09-07 | Guy Parent | Antalgic ointment |
| DE4238223C1 (de) * | 1992-11-12 | 1994-05-26 | Lohmann Therapie Syst Lts | Transdermales therapeutisches System zur Verabreichung von Physostigmin an die Haut und Verfahren zu dessen Herstellung |
| JPH0733681A (ja) * | 1993-05-18 | 1995-02-03 | Sekisui Chem Co Ltd | 経皮吸収貼付剤 |
| ES2168290T3 (es) * | 1993-11-23 | 2002-06-16 | Euro Celtique Sa | Metodo para preparar una composicion de liberacion sostenida. |
| EP0672416A1 (en) * | 1994-03-14 | 1995-09-20 | Euro-Celtique S.A. | Pharmaceutical composition comprising diamorphine |
| US5843480A (en) * | 1994-03-14 | 1998-12-01 | Euro-Celtique, S.A. | Controlled release diamorphine formulation |
| JPH08143458A (ja) * | 1994-11-17 | 1996-06-04 | Sekisui Chem Co Ltd | 経皮吸収貼付剤 |
| DE19642043A1 (de) * | 1995-10-23 | 1997-04-24 | Hexal Ag | Transdermales therapeutisches System (TTS) für die Verabreichung von Wirkstoffen zur Behandlung von Drogenabhängigkeit oder Drogensucht |
| GB9605867D0 (en) * | 1996-03-20 | 1996-05-22 | Svedman Paul | Transdermal device |
| DE19654468C1 (de) * | 1996-12-27 | 1998-01-22 | Lohmann Therapie Syst Lts | Extrem flexibles, dermal oder transdermal wirkendes Pflaster und Verfahren zu seiner Herstellung |
| US6143278A (en) * | 1998-02-23 | 2000-11-07 | Elkhoury; George F. | Topical application of opioid analgesic drugs such as morphine |
| DE19901085C2 (de) * | 1999-01-14 | 2003-12-18 | Lohmann Therapie Syst Lts | Transdermales therapeutisches System mit einer selbstklebenden Matrix, enthaltend organische Säure-Additionssalze von Alkaloiden des Morphin- bzw. Morphinantyps |
-
1999
- 1999-05-21 DE DE19923551A patent/DE19923551A1/de not_active Withdrawn
-
2000
- 2000-05-17 DE DE50010833T patent/DE50010833D1/de not_active Expired - Lifetime
- 2000-05-17 TR TR2001/03302T patent/TR200103302T2/xx unknown
- 2000-05-17 CN CNB008078823A patent/CN100457107C/zh not_active Expired - Fee Related
- 2000-05-17 BR BR0011286-0A patent/BR0011286A/pt not_active Application Discontinuation
- 2000-05-17 CZ CZ20014187A patent/CZ301230B6/cs not_active IP Right Cessation
- 2000-05-17 EP EP00929536A patent/EP1183029B1/de not_active Expired - Lifetime
- 2000-05-17 PL PL351681A patent/PL196741B1/pl not_active IP Right Cessation
- 2000-05-17 MX MXPA01011921A patent/MXPA01011921A/es active IP Right Grant
- 2000-05-17 PT PT00929536T patent/PT1183029E/pt unknown
- 2000-05-17 HU HU0201349A patent/HUP0201349A3/hu unknown
- 2000-05-17 CA CA002372339A patent/CA2372339C/en not_active Expired - Fee Related
- 2000-05-17 AU AU47577/00A patent/AU772139B2/en not_active Ceased
- 2000-05-17 WO PCT/EP2000/004458 patent/WO2000071125A2/de active IP Right Grant
- 2000-05-17 NZ NZ515301A patent/NZ515301A/xx not_active IP Right Cessation
- 2000-05-17 ES ES00929536T patent/ES2245311T3/es not_active Expired - Lifetime
- 2000-05-17 AT AT00929536T patent/ATE300301T1/de active
- 2000-05-17 JP JP2001505144A patent/JP4892148B2/ja not_active Expired - Fee Related
- 2000-05-17 DK DK00929536T patent/DK1183029T3/da active
- 2000-05-17 KR KR1020017014818A patent/KR100742471B1/ko not_active IP Right Cessation
- 2000-05-17 IL IL14627700A patent/IL146277A0/xx active IP Right Grant
- 2000-05-17 RU RU2001134016/15A patent/RU2254130C2/ru not_active IP Right Cessation
- 2000-05-18 TW TW089109605A patent/TWI241910B/zh not_active IP Right Cessation
- 2000-05-19 AR ARP000102385A patent/AR024013A1/es not_active Application Discontinuation
-
2001
- 2001-11-01 IL IL146277A patent/IL146277A/en not_active IP Right Cessation
- 2001-11-19 ZA ZA200109517A patent/ZA200109517B/en unknown
-
2004
- 2004-09-16 US US10/942,297 patent/US20050053647A1/en not_active Abandoned
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