WO1985002124A1 - Procede et installation pour le degagement transdermique commande d'elements actifs, en particulier de medicaments - Google Patents

Procede et installation pour le degagement transdermique commande d'elements actifs, en particulier de medicaments Download PDF

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Publication number
WO1985002124A1
WO1985002124A1 PCT/CH1984/000178 CH8400178W WO8502124A1 WO 1985002124 A1 WO1985002124 A1 WO 1985002124A1 CH 8400178 W CH8400178 W CH 8400178W WO 8502124 A1 WO8502124 A1 WO 8502124A1
Authority
WO
WIPO (PCT)
Prior art keywords
skin
heating
medicament
housing
temperature
Prior art date
Application number
PCT/CH1984/000178
Other languages
German (de)
English (en)
Inventor
Konrad Hammacher
Original Assignee
Innovadata Ag
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 Innovadata Ag filed Critical Innovadata Ag
Publication of WO1985002124A1 publication Critical patent/WO1985002124A1/fr

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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N1/00—Electrotherapy; Circuits therefor
    • A61N1/02—Details
    • A61N1/04—Electrodes
    • A61N1/0404—Electrodes for external use
    • A61N1/0408—Use-related aspects
    • A61N1/0428—Specially adapted for iontophoresis, e.g. AC, DC or including drug reservoirs

Definitions

  • the invention relates to a method for the controlled transdermal delivery or application of active substances, in particular medication, and a device for carrying out the method. 5 It is known that certain medications
  • active pharmaceutical ingredients can be supplied to a patient by bringing them into contact with a point on the surface of his skin. Such medications are able to diffuse through the intact skin into the cutaneous and subcutaneous blood vessels and get from there into the bloodstream.
  • One difficulty with this so-called transdermal delivery of medicaments is to control the dosage, ie the amount of medication supplied to the patient's bloodstream within a certain time, ie to set it to a specific, predetermined value. This difficulty is due to the fact that the rate of penetration of such drugs through the skin into the blood vessels depends on a number of parameters which are difficult to control, such as the physiological nature of the skin, the degree of blood flow to the cutaneous and subcutaneous tissue, the skin temperature and skin hydration.
  • One measure proposed to solve this problem is to provide an external diffusion barrier for the medicament which specifies the amount of the medication supplied to the skin.
  • transdermal therapeutic systems have a semipermeable membrane between a medication reservoir and the skin, which serves as a diffusion barrier. The diffusion rate of the medicament through this membrane is considerable
  • the dosage of the drug is primarily controlled by its delivery through the membrane and is only slightly dependent on the properties of the skin.
  • OMPI -like systems to lie in such medicaments which: at "'a daily dose of 10 mg nor sufficient the ⁇ Commissionic effects show Another disadvantage of these systems is that the dosage of the drug can not be varied over time, such Variabili ⁇ .. It would be desirable to adapt the amount of medication supplied to the particular needs of the patient.
  • the invention is based on the object of proposing an improved method and a device for the transdermal delivery of medicaments which do not have the disadvantages of the known methods and with which in particular a time-variable dosage of a certain medicament is possible.
  • the invention consists in that the rate of release of the active substance is controlled by the fact that the temperature of the skin at the supply point is set to predetermined values by external action.
  • the method is carried out with the aid of a heating and / or cooling body which can be brought into heat-conducting contact with the medicament and the upper surface of the skin in order to change the change in temperature, the rate of penetration of the medicament into the blood circulation to the respective one
  • the corresponding value can be adapted to requirements.
  • the invention is based on the fact that diffusion processes, in the present case the diffusion of substances through the skin, are accelerated at elevated temperatures or delayed at reduced temperatures. It is known that even small changes in skin temperature speed greatly influence the diffusion rates' of some substances through the skin. Through the use of Heat or, where appropriate, heat withdrawal, therefore, offers the possibility of influencing the rate of penetration of a medicament through the skin into the bloodstream and thus the dosage of a medicament supplied transdermally and adapting it to certain requirements within certain limits. This enables a number of improvements and expansions of the field of application of systems for the transdermal delivery of medicaments, as will be explained in the following. The invention is partly explained in more detail below with reference to the drawing. In the drawing:
  • FIGS. 2 and 3 the schematic structure of a
  • Heating or cooling device
  • the invention offers the possibility of expanding the applicability of the transdermal therapeutic systems known today to medicaments which are therapeutically effective only in higher doses. While the limit of the applicability of the systems known today is, as already mentioned, for medications which are effective at a daily dose of about 10 mg, 5 systems can be constructed according to the concept of the invention which supply medication in much higher amounts Allow dosages.
  • the delivery rate of the drug can be controlled in the same Q manner as in the previously known systems.
  • the skin at the drug delivery point is heated to a constant temperature of 43 ° C. This temperature can be known from the skin without damage over a period of several hours up to a be tolerated for days.
  • the invention offers the possibility of constructing therapeutic systems which allow the supply of a defined amount of a medicament without the use of a diffusion barrier. This can be achieved by bringing an intended amount of a medication into contact with the heated skin surface and by completely absorbing this amount of the skin within a certain time. By selecting the suitable temperature of the radiator, the rate of absorption of the medicament and thus the time within which the medicament is completely absorbed by the skin can be adapted to the respective requirements.
  • Another advantage of the invention is that the speed at which a medicament is fed into the bloodstream can be changed in a relatively simple manner. For example,
  • CMPI by switching the heating on and off or by selecting different temperatures, achieve that a medicament is taken up by the skin at a higher or lower speed within a certain, desired time period.
  • the possibility of such a change is particularly advantageous if, at the start of the administration of a medicament, a higher feed rate is required in order to build up the required concentration of the medicament in the body more quickly while
  • Section shown embodiment of a device for performing the method shows a housing 1 made of electrically and thermally insulating plastic.
  • the housing is e.g. round or cylindrical and its lower part 1 * serves as a bearing surface on the
  • a heater 2 preferably made of metal, is accommodated in the interior of the housing.
  • the heating element 2 contains the actual heating device and, if necessary, a temperature control device . (see Fig. 2).
  • the cable 3 contains electrical connections for the heating
  • a cavity 4 serves to hold an active ingredient or medicament.
  • the drug can be introduced into this cavity in the following forms, for example: - Viscose ointment or gel
  • Tablet that has a melting point of about 30-40 ° C; i.e. the tablet is placed in the cavity in solid form and melts after the heating is switched on.
  • a 10th double-sided adhesive film 5 is provided on the lower housing parts 1 'for fastening the device to the skin 6.
  • FIG. 1 shows a possible heating device (or heating and / or cooling device) for use in a device according to FIG. 1.
  • This 15 consists e.g. from a metal disc 21, e.g. made of brass, an electrical insulation layer 22, e.g. Lacquer, an actual heating element 23, e.g. a thick film resistor, a cable 24 with electrical connections to the heating element 23, a cylindrical bore 25 in the metal disc 21, a thermistor 26 accommodated therein for regulating the temperature and finally a cable 27 with the electrical connections for the thermistor 26.
  • the thermal construction '30 intended element of the device can be used not only as heating, but also as a cooling element. None changes in the basic structure of the facility.
  • the invention can also be used, for example, in combination with iontophoresis, heating / cooling elements and with diagnostic-therapeutic "closed-loop"methods;
  • Iontophoresis which is currently being tested for the transdermal introduction of medication, can also be improved by a combination with thermal elements according to the invention.
  • Such thermal components can e.g.
  • PELTIER elements in which both heat and cold can be generated on the skin by reversing the polarity of the electrical circuit. In addition to the heat effect already described, cooling the skin and the associated blood vessels
  • the critical melting point of a medication for example, is in the range of the skin temperature (e.g. 30-34 C).
  • this medicament is then converted from the crystalline to the active liquid aggregate state. Then is the necessary thera-
  • 25 effects e.g. If a coronary circulatory disorder (angina pectoris attack) is remedied, the temperature is regulated below 30 degrees C, whereby the drug is converted into the solid crystalline state, and further transdermal absorption is prevented.
  • a coronary circulatory disorder angina pectoris attack
  • thermo components with the control via, for example, electronic control circuits allows the transdermal supply of a medicament to be adapted to the needs of the organism in a timely manner.
  • microprocessors also lends itself to this.
  • a medicament in combination can be appropriately transdermally supplied to the respective need by the use of thermal components according to the invention in a "closed-loop" process .

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Media Introduction/Drainage Providing Device (AREA)
  • Electrotherapy Devices (AREA)

Abstract

Dans un procédé d'application, respectivement d'introduction transdermique de médicaments, on influe sur la vitesse de dégagement en influant sur la température de la peau à l'endroit du dégagement et en la réglant à une valeur prédéterminée. Une installation pour réaliser ledit procédé prévoit un support, ayant par exemple la forme d'un boîtier (1), dans lequel est introduit un dispositif de chauffage et/ou de refroidissement (2) et dans lequel un médicament peut être placé; cela permet le passage temporaire d'une dose quantitative d'un médicament dans le système de circulation sanguine.
PCT/CH1984/000178 1983-11-10 1984-11-07 Procede et installation pour le degagement transdermique commande d'elements actifs, en particulier de medicaments WO1985002124A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH607483A CH662740A5 (de) 1983-11-10 1983-11-10 Einrichtung zur gesteuerten transdermalen zufuehrung von pharmazeutischen wirkstoffen.
CH6074/83-8 1983-11-10

Publications (1)

Publication Number Publication Date
WO1985002124A1 true WO1985002124A1 (fr) 1985-05-23

Family

ID=4303828

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CH1984/000178 WO1985002124A1 (fr) 1983-11-10 1984-11-07 Procede et installation pour le degagement transdermique commande d'elements actifs, en particulier de medicaments

Country Status (3)

Country Link
EP (1) EP0161275A1 (fr)
CH (1) CH662740A5 (fr)
WO (1) WO1985002124A1 (fr)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988001520A1 (fr) * 1986-09-05 1988-03-10 Young Hun Suh Appareil de thermotherapie utilisant un corps en pierre ou en ceramique produisant un rayonnement dans l'ultraviolet lointain
WO1988007392A1 (fr) * 1987-03-26 1988-10-06 Intrinsic Ag Procede de regulation d'un signal, installation pour electrotherapie et agencement d'electrodes
EP0555510A1 (fr) * 1992-02-14 1993-08-18 Drug Delivery Systems Inc. Appareil électrique d'application transdermique de médicaments avec un neutralisateur et méthode d'application
US5328453A (en) * 1988-12-21 1994-07-12 Drug Delivery Systems Inc. Method for enhancing transdermal drug delivery of electrical drug applicators
EP0682496A1 (fr) * 1993-01-11 1995-11-22 AXELGAARD, Jens Systeme medical a electrodes
WO1997026940A1 (fr) * 1996-01-25 1997-07-31 Vesture Corporation Applicateur medical et procede
EP1117357A1 (fr) * 1998-09-29 2001-07-25 Zars, Inc. Procedes et dispositifs servant a ameliorer l'administration de composes actifs sur le plan pharmaceutique
WO2002058678A2 (fr) * 2001-01-23 2002-08-01 Lts Lohmann Therapie-Systeme Ag Dispositifs et procedes permettant l'application transdermique assistee par impulsions thermique, de substances actives
EP1267764A1 (fr) * 2000-02-29 2003-01-02 Zars, Inc. Timbre transdermique contenant un dispositif chauffant commande
EP1280485A1 (fr) * 2000-02-29 2003-02-05 Zars, Inc. Timbre transdermique pour medicament ameliore
US9186334B2 (en) 2009-05-04 2015-11-17 Nuvo Research Inc. Heat assisted lidocaine and tetracaine for transdermal analgesia
US9186273B2 (en) 2009-05-04 2015-11-17 Nuvo Research Inc. Methods of treating pains associated with neuroma, nerve entrapment, and other conditions

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6048337A (en) * 1992-01-07 2000-04-11 Principal Ab Transdermal perfusion of fluids
WO1994028854A1 (fr) * 1993-06-11 1994-12-22 Koeltringer Peter Procede et dispositif permettant de traiter des tissus du corps
WO1995015783A1 (fr) * 1993-12-07 1995-06-15 Principal Ab Dispositif destine aux procedes de perfusion transdermique

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE141142C (fr) *
US1573116A (en) * 1924-09-02 1926-02-16 Kobayashi Tsurukichi Thermatologic electrode
GB336741A (en) * 1929-09-09 1930-10-23 Yoshi Kono Moxa curative instrument
CH536637A (fr) * 1971-04-23 1973-05-15 Schofield Janet Installation pour le traitement de l'obésité
FR2285902A2 (fr) * 1974-07-10 1976-04-23 Laguerre Rene Soutien-gorges et slips tonifiants
WO1980001139A1 (fr) * 1978-12-06 1980-06-12 Svedman Paul Dispositif de traitement des tissus, par exemple de la peau
DE2931610A1 (de) * 1979-08-03 1981-02-05 Walter Landsrath Heftpflaster

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE141142C (fr) *
US1573116A (en) * 1924-09-02 1926-02-16 Kobayashi Tsurukichi Thermatologic electrode
GB336741A (en) * 1929-09-09 1930-10-23 Yoshi Kono Moxa curative instrument
CH536637A (fr) * 1971-04-23 1973-05-15 Schofield Janet Installation pour le traitement de l'obésité
FR2285902A2 (fr) * 1974-07-10 1976-04-23 Laguerre Rene Soutien-gorges et slips tonifiants
WO1980001139A1 (fr) * 1978-12-06 1980-06-12 Svedman Paul Dispositif de traitement des tissus, par exemple de la peau
DE2931610A1 (de) * 1979-08-03 1981-02-05 Walter Landsrath Heftpflaster

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988001520A1 (fr) * 1986-09-05 1988-03-10 Young Hun Suh Appareil de thermotherapie utilisant un corps en pierre ou en ceramique produisant un rayonnement dans l'ultraviolet lointain
WO1988007392A1 (fr) * 1987-03-26 1988-10-06 Intrinsic Ag Procede de regulation d'un signal, installation pour electrotherapie et agencement d'electrodes
US5328453A (en) * 1988-12-21 1994-07-12 Drug Delivery Systems Inc. Method for enhancing transdermal drug delivery of electrical drug applicators
EP0555510A1 (fr) * 1992-02-14 1993-08-18 Drug Delivery Systems Inc. Appareil électrique d'application transdermique de médicaments avec un neutralisateur et méthode d'application
EP0682496A1 (fr) * 1993-01-11 1995-11-22 AXELGAARD, Jens Systeme medical a electrodes
EP0682496A4 (fr) * 1993-01-11 1998-09-23 Jens Axelgaard Systeme medical a electrodes.
WO1997026940A1 (fr) * 1996-01-25 1997-07-31 Vesture Corporation Applicateur medical et procede
EP1117357A4 (fr) * 1998-09-29 2006-05-03 Zars Inc Procedes et dispositifs servant a ameliorer l'administration de composes actifs sur le plan pharmaceutique
EP1117357A1 (fr) * 1998-09-29 2001-07-25 Zars, Inc. Procedes et dispositifs servant a ameliorer l'administration de composes actifs sur le plan pharmaceutique
EP1267764A1 (fr) * 2000-02-29 2003-01-02 Zars, Inc. Timbre transdermique contenant un dispositif chauffant commande
EP1280485A1 (fr) * 2000-02-29 2003-02-05 Zars, Inc. Timbre transdermique pour medicament ameliore
EP1267764A4 (fr) * 2000-02-29 2006-11-29 Zars Inc Timbre transdermique contenant un dispositif chauffant commande
EP1280485A4 (fr) * 2000-02-29 2006-11-29 Zars Inc Timbre transdermique pour medicament ameliore
WO2002058678A2 (fr) * 2001-01-23 2002-08-01 Lts Lohmann Therapie-Systeme Ag Dispositifs et procedes permettant l'application transdermique assistee par impulsions thermique, de substances actives
WO2002058678A3 (fr) * 2001-01-23 2002-12-05 Lohmann Therapie Syst Lts Dispositifs et procedes permettant l'application transdermique assistee par impulsions thermique, de substances actives
US9186334B2 (en) 2009-05-04 2015-11-17 Nuvo Research Inc. Heat assisted lidocaine and tetracaine for transdermal analgesia
US9186273B2 (en) 2009-05-04 2015-11-17 Nuvo Research Inc. Methods of treating pains associated with neuroma, nerve entrapment, and other conditions

Also Published As

Publication number Publication date
EP0161275A1 (fr) 1985-11-21
CH662740A5 (de) 1987-10-30

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