LV10044B - Transdermal composition - Google Patents
Transdermal composition Download PDFInfo
- Publication number
- LV10044B LV10044B LVP-92-07A LV920007A LV10044B LV 10044 B LV10044 B LV 10044B LV 920007 A LV920007 A LV 920007A LV 10044 B LV10044 B LV 10044B
- Authority
- LV
- Latvia
- Prior art keywords
- weight
- methyl
- propyl
- propynylamine
- transdermal
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims description 24
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims abstract description 30
- 239000007788 liquid Substances 0.000 claims abstract description 25
- 238000002360 preparation method Methods 0.000 claims abstract description 19
- 229920000642 polymer Polymers 0.000 claims abstract description 10
- 150000003839 salts Chemical class 0.000 claims abstract description 9
- 239000007787 solid Substances 0.000 claims abstract description 9
- MEZLKOACVSPNER-UHFFFAOYSA-N selegiline Chemical compound C#CCN(C)C(C)CC1=CC=CC=C1 MEZLKOACVSPNER-UHFFFAOYSA-N 0.000 claims abstract 4
- MUDUXRHPVDVWHU-UHFFFAOYSA-N 1-(4-fluorophenyl)-n-methyl-n-prop-2-ynylpropan-2-amine Chemical compound C#CCN(C)C(C)CC1=CC=C(F)C=C1 MUDUXRHPVDVWHU-UHFFFAOYSA-N 0.000 claims abstract 3
- 239000004094 surface-active agent Substances 0.000 claims abstract 2
- 239000004480 active ingredient Substances 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 9
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 5
- 239000004973 liquid crystal related substance Substances 0.000 claims description 2
- -1 polyoxyethylene Polymers 0.000 claims 4
- 239000004976 Lyotropic liquid crystal Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000003995 emulsifying agent Substances 0.000 claims 1
- 239000002736 nonionic surfactant Substances 0.000 claims 1
- 229960004063 propylene glycol Drugs 0.000 abstract description 9
- 235000013772 propylene glycol Nutrition 0.000 abstract description 9
- 230000002535 lyotropic effect Effects 0.000 abstract description 8
- 239000012752 auxiliary agent Substances 0.000 abstract 1
- MEZLKOACVSPNER-GFCCVEGCSA-N selegiline Chemical compound C#CCN(C)[C@H](C)CC1=CC=CC=C1 MEZLKOACVSPNER-GFCCVEGCSA-N 0.000 description 25
- 102000010909 Monoamine Oxidase Human genes 0.000 description 19
- 108010062431 Monoamine oxidase Proteins 0.000 description 19
- 230000000694 effects Effects 0.000 description 17
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 10
- 241000700159 Rattus Species 0.000 description 7
- 241000282887 Suidae Species 0.000 description 7
- 210000004556 brain Anatomy 0.000 description 7
- 229960003946 selegiline Drugs 0.000 description 7
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 description 6
- 238000004128 high performance liquid chromatography Methods 0.000 description 6
- 230000005764 inhibitory process Effects 0.000 description 6
- 239000002245 particle Substances 0.000 description 6
- 239000011505 plaster Substances 0.000 description 6
- 208000018737 Parkinson disease Diseases 0.000 description 5
- 229920002685 Polyoxyl 35CastorOil Polymers 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 238000005259 measurement Methods 0.000 description 5
- QUANRIQJNFHVEU-UHFFFAOYSA-N oxirane;propane-1,2,3-triol Chemical compound C1CO1.OCC(O)CO QUANRIQJNFHVEU-UHFFFAOYSA-N 0.000 description 5
- 239000008389 polyethoxylated castor oil Substances 0.000 description 5
- 238000010521 absorption reaction Methods 0.000 description 4
- 210000001772 blood platelet Anatomy 0.000 description 4
- 230000001804 emulsifying effect Effects 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 239000002674 ointment Substances 0.000 description 4
- 241000282472 Canis lupus familiaris Species 0.000 description 3
- 206010012289 Dementia Diseases 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- 210000005013 brain tissue Anatomy 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000002500 effect on skin Effects 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 210000005228 liver tissue Anatomy 0.000 description 3
- 239000000758 substrate Substances 0.000 description 3
- 229920001285 xanthan gum Polymers 0.000 description 3
- 239000000230 xanthan gum Substances 0.000 description 3
- 229940082509 xanthan gum Drugs 0.000 description 3
- 235000010493 xanthan gum Nutrition 0.000 description 3
- 208000024827 Alzheimer disease Diseases 0.000 description 2
- 238000010241 blood sampling Methods 0.000 description 2
- 238000009792 diffusion process Methods 0.000 description 2
- 150000004676 glycans Chemical class 0.000 description 2
- 239000003883 ointment base Substances 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 241000772991 Aira Species 0.000 description 1
- 229920000742 Cotton Polymers 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 1
- 101100406879 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) par-2 gene Proteins 0.000 description 1
- 229920000604 Polyethylene Glycol 200 Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 241000282898 Sus scrofa Species 0.000 description 1
- 239000011149 active material Substances 0.000 description 1
- 238000002306 biochemical method Methods 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019994 cava Nutrition 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001149 cognitive effect Effects 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 230000002825 dopamine reuptake Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000003557 neuropsychological effect Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 229940066675 ricinoleate Drugs 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 238000010792 warming Methods 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K9/1274—Non-vesicle bilayer structures, e.g. liquid crystals, tubules, cubic phases or cochleates; Sponge phases
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dispersion Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (3)
- LV 10044 TRANSDERMĀLS ĀRSTNIECISKS SASTĀVS PATENTA FORMULA 1. Bezūdens transdermals preparāts, kas 20-100 % liotropiska šķidra kristāla struktūrā satur: optiski aktīvu vai racemisku N-metil-N-(fenil-2-pro- pil)-2-propinilamīnu vai N-metil-N-(l-(4-fluorfenil)-2-propil)-2-propinilamīnu vai to farmaceitiski 5 -15 sv.% 40 - 70 sv.% 10 - 20 sv.% 2 - 30 sv.% 2-20 sv.% 0.5 - 2 sv.% piemērotus sāļus šķidru polioksietilēnu dētu polioksietilēnu nejonogēnu virsmas aktīvu vielu propilēnglikolu, ja vēlams polimēru, kura a vērtība ir > 0.6, un, ja vēlams kvantitatīvi sasniegt 100 %, citu palīgvielu, tādu kā emulgatoru
- 2. Metode bezūdens transdermāla preparāta iegūšanai, atšķirīga ar to, ka maisījums, kas satur 40 - 70 sv.% šķidra polioksietilēna un 10 - 20 sv.% cieta polioksietilēna, 2-30 sv.% nejonogēnas virsmas aktīvas vielas un 2 - 20 sv.% propilēnglikola, tiek inokulēts ar 5 -15 sv.% optiski aktīva vai racemiska N-metil-N-(fenil-2-propil)-2-propinilamīna, vai N-metil-N-(l-(4-fluorfenil)-2-propil)-2-propinilamīna vai to farmaceitiski piemērotu sāļu, lai iegūtu šķidra kristāla struktūras liotropisku preparātu, kuram, ja vēlams, ir pievienoti 0.5 - 2.0 sv.% polimēra, kura a vērtība ir > 0.6, un, lai kvantitatīvi sasniegtu 100 sv.%, citas palīgvielas.
- 3. Metode transdermāla preparāta , kas satur 5 -15 sv.% optiski aktīva vai racemiska N-metil-N-(l-fenil-2-propil)-2-propinilamīna vai N-metil-N-(l-(4-fluorfenil)-2-propil)-2-propinilamīna vai to farmaceitiski piemērotu sāļu, efektivitātes palielināšanai, atšķirīga ar to, ka aktīvo sastāvdaļu pielieto uz ādas virsmas 20 -100 % liotropiska šķidra kristāla preparāta formā.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU911229A HU209605B (en) | 1991-04-15 | 1991-04-15 | Process for production of wather-free transdermal preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| LV10044A LV10044A (lv) | 1994-05-10 |
| LV10044B true LV10044B (en) | 1995-02-20 |
Family
ID=10953442
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LVP-92-07A LV10044B (en) | 1991-04-15 | 1992-04-09 | Transdermal composition |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US5380761A (lv) |
| EP (1) | EP0509761B1 (lv) |
| JP (1) | JP2547151B2 (lv) |
| KR (1) | KR950008766B1 (lv) |
| AT (1) | ATE142486T1 (lv) |
| AU (1) | AU648886B2 (lv) |
| BG (1) | BG61637B1 (lv) |
| CA (1) | CA2065134A1 (lv) |
| CZ (1) | CZ281261B6 (lv) |
| DE (1) | DE69213536T2 (lv) |
| DK (1) | DK0509761T3 (lv) |
| EC (1) | ECSP920873A (lv) |
| EE (1) | EE03038B1 (lv) |
| ES (1) | ES2092031T3 (lv) |
| FI (1) | FI101677B (lv) |
| GR (1) | GR3021505T3 (lv) |
| HK (1) | HK1003977A1 (lv) |
| HR (1) | HRP920570A2 (lv) |
| HU (2) | HU209605B (lv) |
| IE (1) | IE921019A1 (lv) |
| IL (1) | IL101487A (lv) |
| LT (1) | LT3044B (lv) |
| LV (1) | LV10044B (lv) |
| MX (1) | MX9201732A (lv) |
| NO (1) | NO303903B1 (lv) |
| NZ (1) | NZ242335A (lv) |
| PH (1) | PH29992A (lv) |
| PL (1) | PL173234B1 (lv) |
| RO (1) | RO109603B1 (lv) |
| RU (1) | RU2088617C1 (lv) |
| SK (1) | SK278666B6 (lv) |
| TW (1) | TW198690B (lv) |
| UA (1) | UA26892C2 (lv) |
| YU (1) | YU48552B (lv) |
| ZA (1) | ZA922355B (lv) |
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|---|---|---|---|---|
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| AU679937B2 (en) * | 1992-11-18 | 1997-07-17 | Johnson & Johnson Consumer Products, Inc. | Extrudable compositions for topical or transdermal drug delivery |
| US5817336A (en) * | 1993-04-02 | 1998-10-06 | Orion-Yhtyma Oy | Composition containing selegiline |
| DE4428444A1 (de) * | 1994-08-11 | 1996-02-15 | Dresden Arzneimittel | Verwendung von Selegilin zur Behandlung von epileptischen Erkrankungen |
| HU223475B1 (hu) * | 1994-10-24 | 2004-07-28 | Chinoin Gyógyszer és Vegyészeti Termékek Gyára Rt. | Selegilint tartalmazó liposzoma-készítmény és eljárás ennek előállítására |
| US6299901B1 (en) | 1995-01-13 | 2001-10-09 | Somerset Pharmaceuticals, Inc. | Methods and pharmaceutical compositions employing desmethylselegiline |
| US6033682A (en) | 1995-01-13 | 2000-03-07 | Somerset Pharmaceuticals, Inc. | S(+) desmethylselegiline and its use in therapeutic methods and pharmaceutical compositions |
| US6348208B1 (en) | 1995-01-13 | 2002-02-19 | Somerset Pharmaceuticals, Inc. | Methods and pharmaceutical compositions employing desmethylselegiline |
| US6319954B1 (en) | 1995-01-13 | 2001-11-20 | Somerset Pharmaceuticals, Inc. | S-(+)-desmethylselegiline and its use in the therapeutic methods and pharmaceutical compositions |
| US6316022B1 (en) | 1995-06-07 | 2001-11-13 | Noven Pharmaceuticals, Inc. | Transdermal compositions containing low molecular weight drugs which are liquid at room temperatures |
| IL122484A0 (en) | 1995-06-07 | 1998-06-15 | Noven Pharma | Transdermal compositions containing low molecular weight drugs which are liquid at room temperatures |
| HUP9601442A3 (en) * | 1995-07-25 | 1999-03-29 | Panacea Biotec Ltd | Nes antinflammatory and analgetic pharmaceutical compositions, containing nimesulid for transdermal use, and process for producing them |
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| DE19743323C2 (de) * | 1997-09-30 | 2000-05-25 | Iip Inst Fuer Ind Pharmazie Fo | Feste Arzneimittelzusammensetzung auf der Grundlage von Selegilin |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US468218A (en) | 1892-02-02 | Door-securer | ||
| HU187775B (en) * | 1982-07-14 | 1986-02-28 | Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt,Hu | New process for producing propargile-amines of pharmaceutical activity |
| US4861800A (en) * | 1987-08-18 | 1989-08-29 | Buyske Donald A | Method for administering the drug deprenyl so as to minimize the danger of side effects |
| US4868218A (en) * | 1987-08-18 | 1989-09-19 | Buyske Donald A | Method of treating depression |
| IL88099A (en) * | 1987-11-06 | 1992-02-16 | Chinoin Gyogyszer Es Vegyeszet | Lyotropic liquid crystalline compositions |
| GB8807504D0 (en) * | 1988-03-29 | 1988-05-05 | Sandoz Ltd | Improvements in/relating to organic compounds |
| DE68926506T2 (de) | 1988-07-29 | 1996-10-31 | Michelson Gary K | Rückgratretraktor |
| US5053227A (en) * | 1989-03-22 | 1991-10-01 | Cygnus Therapeutic Systems | Skin permeation enhancer compositions, and methods and transdermal systems associated therewith |
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1991
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1992
- 1992-03-30 IE IE101992A patent/IE921019A1/en not_active Application Discontinuation
- 1992-03-31 ZA ZA922355A patent/ZA922355B/xx unknown
- 1992-04-03 IL IL10148792A patent/IL101487A/en not_active IP Right Cessation
- 1992-04-03 CA CA002065134A patent/CA2065134A1/en not_active Abandoned
- 1992-04-07 PH PH44168A patent/PH29992A/en unknown
- 1992-04-08 RO RO92-200487A patent/RO109603B1/ro unknown
- 1992-04-09 LV LVP-92-07A patent/LV10044B/en unknown
- 1992-04-13 NZ NZ242335A patent/NZ242335A/en unknown
- 1992-04-13 SK SK1110-92A patent/SK278666B6/sk unknown
- 1992-04-13 KR KR1019920006147A patent/KR950008766B1/ko not_active Expired - Fee Related
- 1992-04-13 CZ CS921110A patent/CZ281261B6/cs unknown
- 1992-04-14 AU AU14849/92A patent/AU648886B2/en not_active Ceased
- 1992-04-14 BG BG96232A patent/BG61637B1/bg unknown
- 1992-04-14 AT AT92303341T patent/ATE142486T1/de active
- 1992-04-14 DE DE69213536T patent/DE69213536T2/de not_active Expired - Fee Related
- 1992-04-14 YU YU38492A patent/YU48552B/sh unknown
- 1992-04-14 MX MX9201732A patent/MX9201732A/es unknown
- 1992-04-14 NO NO921481A patent/NO303903B1/no unknown
- 1992-04-14 EP EP92303341A patent/EP0509761B1/en not_active Expired - Lifetime
- 1992-04-14 ES ES92303341T patent/ES2092031T3/es not_active Expired - Lifetime
- 1992-04-14 DK DK92303341.9T patent/DK0509761T3/da active
- 1992-04-14 RU SU925011496A patent/RU2088617C1/ru active
- 1992-04-15 JP JP4095681A patent/JP2547151B2/ja not_active Expired - Lifetime
- 1992-04-15 PL PL92294240A patent/PL173234B1/pl unknown
- 1992-04-15 FI FI921690A patent/FI101677B/fi active
- 1992-04-23 TW TW081103203A patent/TW198690B/zh active
- 1992-08-28 LT LTIP176A patent/LT3044B/lt not_active IP Right Cessation
- 1992-09-28 HR HR920570A patent/HRP920570A2/hr not_active Application Discontinuation
- 1992-10-15 EC EC1992000873A patent/ECSP920873A/es unknown
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1993
- 1993-06-14 UA UA93002168A patent/UA26892C2/uk unknown
- 1993-10-20 US US08/140,279 patent/US5380761A/en not_active Expired - Fee Related
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1994
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1995
- 1995-06-16 HU HU95P/P00215P patent/HU211544A9/hu unknown
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