[go: up one dir, main page]

WO1989004179A1 - Formulations pharmaceutiques pour administration transcutanee - Google Patents

Formulations pharmaceutiques pour administration transcutanee Download PDF

Info

Publication number
WO1989004179A1
WO1989004179A1 PCT/EP1988/000958 EP8800958W WO8904179A1 WO 1989004179 A1 WO1989004179 A1 WO 1989004179A1 EP 8800958 W EP8800958 W EP 8800958W WO 8904179 A1 WO8904179 A1 WO 8904179A1
Authority
WO
WIPO (PCT)
Prior art keywords
active
dmi
dimethylisosorbide
emulsion
transdermal administration
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.)
Ceased
Application number
PCT/EP1988/000958
Other languages
English (en)
Inventor
Luciano Cocchi
Simos Contos
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Also Laboratori SAS Di Dr P Sorbini and C
Original Assignee
Also Laboratori SAS Di Dr P Sorbini and C
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Also Laboratori SAS Di Dr P Sorbini and C filed Critical Also Laboratori SAS Di Dr P Sorbini and C
Publication of WO1989004179A1 publication Critical patent/WO1989004179A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • A61K9/70—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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches

Definitions

  • the present invention concerns pharmaceutical compositions for the transdermal application of active principles.
  • transdermal administration of pharmacologicaly active substances has recently been more and more widely studied in order to obtain a controlled release of drugs, mainly for particular kind of drugs with short half-life, asking for repeated administration over a certain period of time.
  • Example of drugs presently used by transdermal route are nitroglycerine, ⁇ copolamine, clonidine, some anti-inflammatory drugs and some hormones.
  • plasters wherein the active principle is suitably absorbed in a reservoir and is made available therefrom, optionally through a membrane, for the cutaneous absorption.
  • a problem common to the known formulations consists in the high variability of absorption according to the chemico-physical characteristics of each active principle. This asks for the need of developing new and different formulations suitable for the single active principle.
  • Dimethylsulfoxide for instance, is used to make the diffusion of the active principles through the horny layer easier, but it does not provide an ideal solution because of its toxicity.
  • GB 2146525, E-A 120262 and DD 217989 disclose pharmaceutical formulations suited for the transdermal administration which may contain, inter alia, also DMI as a solvent, in admixture with different vehicles or solvents contributing to the transdermal administration system.
  • DMI is therefore used only as a hydrophilic solvent and always in combination with other excipients or ve-hicle-s.
  • JP-A-60-64418 discloses the USE of DMI as an agent for promoting the absorption of active principles through the skin.
  • DMI is never used as single component but it is used in weight percentages ranging from 5 to 50%. Values outside this range are said to be "snrpreferred", tbecause higher percentages would cause a lowering of cohesivenes ⁇ of the particular tape formulation.
  • the amount of drug to be contained in the tape preparation according to said JP-A- is from 1 to 1000 ⁇ g/cm 2 .
  • compositions suitable for the transdermal administration of active principle consisting of a solution or an emulsion of said active principle in dimethylisosorbide or in a dimethyl isosorbide-water mixture wherein the content of dimethylisosorbide is higher than 50% by weight of the total mixture and is preferably higher than 60%.
  • the formulations according to the invention allow an effective absorbtion of a wide variety of active principles, even of very different chemico-physical characteristics, and they are prepared in an easy, inexp- ensive way.
  • the invention provides plasters having the formulations of the invention absorbed on a suitable material.
  • the active principles which may be used according to the present invention belong to different therapeutic cathegories.
  • both steroidal and non steroidal antiinf lammatory agents calcium-antagonists, ⁇ -blockers, ⁇ -blockers, ⁇ -agonists, calcium blockers, ergot alkaloids, anti-hist aminics, anti-cholinergics, mucolytics, anti-oxidizing agents (vitamins, enzymes ⁇ uch a ⁇ superoxidismutase), bacterial extracts, thymic hormones, cardiac glycosides, pharmacologically active peptides, active principles of vegetal .kind, GingKo biloba, physiological substances (carnitine, taurine, glutathion, cerebrosides, phospholipids etc).
  • the amount of the active principles in the formulations of the invention depends on the activity and on the .absorption characteristics of the considered compounds: it will be anyhow determined by usual methods, relying on the average knowledge in the art.
  • the preparation of solutions or emulsion ⁇ of the different active principles is carried out by usual methods; for the solutions, the percent of hydratation of DMI will be ⁇ elected according to the hydrophilic degree of the active principle. Active principle ⁇ in saline form, for instance, will be solubilized with higher amounts of water, up to about 50%.
  • the di ⁇ solution temperature should not be higher than 40-50°C, in order to avoid degradation of the active principle .
  • solution of the active principle obtained as abov e described is added to sai base emulsion prepared from usual and compatible substances, preferably at a temp erature lower than 40°C, first in a mixer under vacuum and then in a piston homogenizer.
  • solutions or emul ⁇ ion ⁇ may be the further worked for the preparation of pharmaceutical forms suited for the topical administation, such as those described in "Remington's Pharmaceutical Sciences Handbook",hack Pub. CO., N.Y., U.S.A.
  • a compatible material for instance a viscosa-rayon non-wowen material, collagene or other natural or synthetic fibres unsoluble in DMI.
  • the carrier system according to the invention allows the preparation of solutions up to 60% of solid active principle and up to 90% for active principles in liquid form.
  • the plasters may comprise up to 1-1,5 ml of solution or emulsion
  • the maximum amount of active principle comprised in the plasters of the invention reaches about 600-900 mg, which is by far higher than that allowable by the known prior-art formulations.
  • the composition, form, size and materials of the plaster may change according to the active principle, to the application zone, and to packaging and/or presentation needs, etc.
  • the numeral 1 shows a first sheet, for example of aluminum, PVC or other material, to be applied on the skin during the drug release.
  • the absorption zone of the emulsion or solution of the active principle is indicated by 2 whereas 3 shows a ring of expanded or foamed material coated with acrylic or siliconic hypoallergenic adhesive.
  • a protective ring 4 covers the adhesive side of the ring 3; two thermosealed aluminum or plastic rings limit the zone 2 and the plaster's perimeter, respectively.
  • the numeral 6 shows the upper closure sheet, which can be of the same of different material as the sheet 1, to be discarded immediately before use.
  • a siliconic film or other suitable membrane may be placed between the zone 2 and the adhesive ring 3, in order to enhance the gradual release of the active principle.

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Dermatology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Formulations pharmaceutiques, notamment sous forme d'emplâtres, pour l'administration transcutanée de principes actifs, renfermant comme activeur d'absorption du diméthylisosorbide dans des quantités supérieures à 50 % en poids.
PCT/EP1988/000958 1987-11-03 1988-10-26 Formulations pharmaceutiques pour administration transcutanee Ceased WO1989004179A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT22501A/87 1987-11-03
IT22501/87A IT1223343B (it) 1987-11-03 1987-11-03 Formulazioni farmaceutiche per somministrazione transdermica

Publications (1)

Publication Number Publication Date
WO1989004179A1 true WO1989004179A1 (fr) 1989-05-18

Family

ID=11197124

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1988/000958 Ceased WO1989004179A1 (fr) 1987-11-03 1988-10-26 Formulations pharmaceutiques pour administration transcutanee

Country Status (3)

Country Link
AU (1) AU2617288A (fr)
IT (1) IT1223343B (fr)
WO (1) WO1989004179A1 (fr)

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992000725A1 (fr) * 1990-07-13 1992-01-23 Farcon Ag Compositions pharmaceutiques liquides de traitement oral presentant une activite anti-inflammatoire
WO1995022322A1 (fr) * 1994-02-18 1995-08-24 Schering Aktiengesellschaft Systemes therapeutiques transdermiques contenant des steroides sexuels
WO1999016434A1 (fr) * 1997-09-26 1999-04-08 Sam Yang Co., Ltd. Systeme d'administration transdermique de medicament pour agent analgesique et anti-inflammatoire comportant du sel de diclofenac-diethylammonium et procede de fabrication correspondant
AU724308B2 (en) * 1994-02-18 2000-09-14 Schering Aktiengesellschaft Transdermal therapeutic systems that contain sex steroids
WO2004002444A3 (fr) * 2002-06-27 2004-03-11 Holden Dev Ltd Plate-forme pour formulations transdermiques
US7258871B2 (en) 2000-10-20 2007-08-21 Neurobiotec Gmbh Combination of a transdermal therapeutic system and an oral and/or parenteral preparation containing dopamine agonists for the treatment of dopaminergic disease states
EP2088154A1 (fr) 2004-03-09 2009-08-12 Ironwood Pharmaceuticals, Inc. Procédés et compositions pour le traitement de troubles gastro-intestinaux
WO2010059836A1 (fr) 2008-11-20 2010-05-27 Decode Genetics Ehf Composés bicycliques substitués à pont aza pour maladie cardiovasculaire et du système nerveux central
WO2010084499A2 (fr) 2009-01-26 2010-07-29 Israel Institute For Biological Research Composés spiro hétérocycliques bicycliques
EP2476680A1 (fr) 2008-01-11 2012-07-18 Albany Molecular Research, Inc. Pyridoindoles à substitution (1-azinone)
EP2628727A2 (fr) 2007-11-21 2013-08-21 Decode Genetics EHF Inhibiteurs de PDE4 biaryle pour le traitement de troubles pulmonaires et cardiovasculaires

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4082881A (en) * 1976-12-23 1978-04-04 E. R. Squibb & Sons, Inc. Topical and other type pharmaceutical formulations containing isosorbide carrier
LU84514A1 (fr) * 1982-12-09 1984-10-22 Oreal Composition stable pour corticotherapie locale contenant a l'etat solubilise de l'hydrocortisone
EP0137278A2 (fr) * 1983-09-12 1985-04-17 Schering Aktiengesellschaft Composition pour application percutanée de substances actives pharmaceutiques
GB2150024A (en) * 1983-11-21 1985-06-26 May & Baker Ltd Anthelmintic compositions

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4082881A (en) * 1976-12-23 1978-04-04 E. R. Squibb & Sons, Inc. Topical and other type pharmaceutical formulations containing isosorbide carrier
LU84514A1 (fr) * 1982-12-09 1984-10-22 Oreal Composition stable pour corticotherapie locale contenant a l'etat solubilise de l'hydrocortisone
EP0137278A2 (fr) * 1983-09-12 1985-04-17 Schering Aktiengesellschaft Composition pour application percutanée de substances actives pharmaceutiques
GB2150024A (en) * 1983-11-21 1985-06-26 May & Baker Ltd Anthelmintic compositions

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992000725A1 (fr) * 1990-07-13 1992-01-23 Farcon Ag Compositions pharmaceutiques liquides de traitement oral presentant une activite anti-inflammatoire
WO1995022322A1 (fr) * 1994-02-18 1995-08-24 Schering Aktiengesellschaft Systemes therapeutiques transdermiques contenant des steroides sexuels
US5904931A (en) * 1994-02-18 1999-05-18 Schering Aktiengesellschaft Transdermal therapeutic systems that contain sex steroids and dimethyl isosorbide
AU724308B2 (en) * 1994-02-18 2000-09-14 Schering Aktiengesellschaft Transdermal therapeutic systems that contain sex steroids
WO1999016434A1 (fr) * 1997-09-26 1999-04-08 Sam Yang Co., Ltd. Systeme d'administration transdermique de medicament pour agent analgesique et anti-inflammatoire comportant du sel de diclofenac-diethylammonium et procede de fabrication correspondant
US7258871B2 (en) 2000-10-20 2007-08-21 Neurobiotec Gmbh Combination of a transdermal therapeutic system and an oral and/or parenteral preparation containing dopamine agonists for the treatment of dopaminergic disease states
WO2004002444A3 (fr) * 2002-06-27 2004-03-11 Holden Dev Ltd Plate-forme pour formulations transdermiques
EP2088154A1 (fr) 2004-03-09 2009-08-12 Ironwood Pharmaceuticals, Inc. Procédés et compositions pour le traitement de troubles gastro-intestinaux
EP2628727A2 (fr) 2007-11-21 2013-08-21 Decode Genetics EHF Inhibiteurs de PDE4 biaryle pour le traitement de troubles pulmonaires et cardiovasculaires
EP2674417A2 (fr) 2007-11-21 2013-12-18 Decode Genetics EHF Inhibiteurs de PDE4 biaryle pour le traitement de l'inflammation
EP2476680A1 (fr) 2008-01-11 2012-07-18 Albany Molecular Research, Inc. Pyridoindoles à substitution (1-azinone)
WO2010059836A1 (fr) 2008-11-20 2010-05-27 Decode Genetics Ehf Composés bicycliques substitués à pont aza pour maladie cardiovasculaire et du système nerveux central
WO2010084499A2 (fr) 2009-01-26 2010-07-29 Israel Institute For Biological Research Composés spiro hétérocycliques bicycliques

Also Published As

Publication number Publication date
IT1223343B (it) 1990-09-19
AU2617288A (en) 1989-06-01
IT8722501A0 (it) 1987-11-03

Similar Documents

Publication Publication Date Title
US6562368B2 (en) Transdermal administration of oxybutynin using hydroxide-releasing agents as permeation enhancers
US4933184A (en) Menthol enhancement of transdermal drug delivery
US5834010A (en) Triacetin as a penetration enhancer for transdermal delivery of a basic drug
KR101612901B1 (ko) 경피흡수 의약조성물, 의약조성물 저장유닛 및 이것을 이용하는 경피흡수제제
US5314694A (en) Transdermal formulations, methods and devices
AU651165B2 (en) Subsaturated transdermal drug delivery device exhibiting enhanced drug flux
EP0644746B1 (fr) Utilisation de glycerine pour moderer un apport medicamenteux transdermique
KR100267442B1 (ko) 아세틸살리실산을 함유하는 혈전증 치료용 및 암 예방용 경피적 투여시스템
US5019395A (en) Compositions with enhanced penetration
IE83582B1 (en) Subsaturated transdermal drug delivery device exhibiting enhanced drug flux
US4931283A (en) Menthol enhancement of transdermal drug delivery
CA1238275A (fr) Augmentation par le menthol de l'absorption transdermique de medicament
IE62871B1 (en) Compositions with enhanced penetration
WO1989004179A1 (fr) Formulations pharmaceutiques pour administration transcutanee
US4788064A (en) Transdermal delivery system
US5139786A (en) Topical formulations
SK126093A3 (en) Lanoline derivatives as a penetration-promoting substances
GB2256135A (en) Transdermal administration of 4-substituted imidazoles
EP1239846A2 (fr) Administration transdermique de phenylpropanolamine
JPH05310568A (ja) カプトプリル含有経皮吸収製剤
MXPA97007868A (es) La triacetina como incrementador de penetraciontransdermica
HK1084320B (en) Triacetin as a transdermal penetration enhancer
HK1013790B (en) Systems for administering drugs transdermally using sorbitan esters as skin permeation enhancers
HK1013803B (en) Subsaturated transdermal drug delivery device exhibiting enhanced drug flux

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AU BB BG BR DK FI HU JP KP KR LK MC MG MW NO RO SD SU US

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): AT BE BJ CF CG CH CM DE FR GA GB IT LU ML MR NL SE SN TD TG