WO2018087779A1 - Système d'administration transdermique et dispositif de pulvérisation - Google Patents

Système d'administration transdermique et dispositif de pulvérisation Download PDF

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Publication number
WO2018087779A1
WO2018087779A1 PCT/IN2017/050519 IN2017050519W WO2018087779A1 WO 2018087779 A1 WO2018087779 A1 WO 2018087779A1 IN 2017050519 W IN2017050519 W IN 2017050519W WO 2018087779 A1 WO2018087779 A1 WO 2018087779A1
Authority
WO
WIPO (PCT)
Prior art keywords
delivery system
transdermal delivery
transdermal
spray device
drug
Prior art date
Application number
PCT/IN2017/050519
Other languages
English (en)
Inventor
Geena Malhotra
Original Assignee
Cipla Limited
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 Cipla Limited filed Critical Cipla Limited
Publication of WO2018087779A1 publication Critical patent/WO2018087779A1/fr

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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/08—Solutions
    • 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
    • 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
    • A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M35/00—Devices for applying media, e.g. remedies, on the human body
    • A61M35/003—Portable hand-held applicators having means for dispensing or spreading integral media
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
    • A61M2037/0007—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin having means for enhancing the permeation of substances through the epidermis, e.g. using suction or depression, electric or magnetic fields, sound waves or chemical agents

Definitions

  • the invention generally relates to transdermal drug delivery system and devices therefor.
  • Oral drug delivery is the most preferred route of delivery system having advantage of unit dosage form along with feasibility of dose titration.
  • oral route has potential drawbacks including formulation of poorly soluble drugs, first-pass metabolism, patient compliance for paediatric and geriatric population, dose missing and at times intentional skipping of medications. This has led to exploration of other routes for drug delivery and transdermal route has emerged one of the promising approaches for drug delivery.
  • Transdermal drug delivery systems have the potential advantage of overcoming first- pass metabolism, systemic drug delivery, ease of formulation for poorly water soluble drug, dose reduction, ease of acceptance in paediatric and geriatric population and physical intervention/termination of medicament in between the treatment if required.
  • transdermal spray delivery systems are widely being explored owing to the advantage of immediate action and its penetration to the subsequent skin layers.
  • One of the prominent examples are the anti-inflammatory medicament sprays which provide quick relief from pain in conditions such as sports injury and muscle pull while executing daily activities.
  • transdermal spray has been successfully adapted to delivery of therapeutic medicaments in conditions such as anti-psychotic and steroidal drugs.
  • one of the potential problems associated with transdermal patches are the local irritation at the site of application.
  • discomforts like erythema, itching, and local edema are frequently observed with these systems which are primarily caused by adhesive, polymers or other excipients used in patch formulation.
  • Allergic reactions too are observed in few patients. Many patients feel the transdermal patches to be non-aesthetic in appeal.
  • the present invention as embodied and broadly described herein provides a transdermal spray device and a transdermal delivery system maintained by the device.
  • the device comprises means for storing and dispensing of a transdermal delivery system, and at least one UV light source for initiating a curing procedure of the transdermal delivery system in relation to the dispensing action.
  • the transdermal delivery system in turn comprises a drug or combination of drugs along with at least one UV curable monomer and a solvent system.
  • Figure 1 illustrates a front view of a device for storing and dispensing the transdermal delivery system in accordance with the teachings of the invention
  • Figure 2 illustrates a side view of the device shown in Figure 1.
  • the present invention provides a transdermal delivery system comprising of a drug or combination of drugs along with at least one UV curable monomer and a photoinitiator in a solvent system.
  • the transdermal delivery system is deliverable from a transdermal spray device which has a UV light source coupled therewith.
  • the actuation of the device sprays the transdermal delivery system on to skin which in situ and eventually gets cured after exposure to UV light emitted by the device to form a thin, transparent and robust drug- polymer film on the skin which retains for prolonged period of time and provide sustained drug release.
  • the novel transdermal spray device is coupled with UV light source which facilitates curing of sprayed monomer into a polymer having higher adhesiveness to the body surface.
  • the transdermal delivery system comprises drug or combination of drugs, UV curable monomer(s) and organic solvent(s).
  • the transdermal delivery system may further comprise photoinitiators, plasticizers (or alternatively referred to as film forming agent), permeability enhancers, antioxidants, release retarding agent etc.
  • the drug can be selected from a group comprising of scopolamine, nitroglycerine, clonidine, isosorbide dinitrate, rivastigmine, rotigotine, propranolol hydrochloride, timolol maleate, clonazepam, verapamil, diclofenac sodium, naproxen sodium, ibuprofen, ketoprofen, indomethacin, piroxicam, ketorolac, tromethamine, nimesulide, hydrocortisone or esters thereof, dexamethasone, fluocinolone acetonide, betamethasone, estradiol, norethisterone, testosterone, progesterone, salbutamol, bambuterol, salmeterol xinafoate, fluticasone propionate, mometasone furoate, budesonide, beclomethasone dipropionate, sodium cromoglycate, iso
  • drug can be selected from a group comprising of Nicotine, amphetamine, methamphetamine, methyphenidate, scopolamine, isosorbide dinitrate, rivastigmine, rotigotine, estradiol, norethisterone, testosterone, progesterone, zolmitriptan, sumatriptan, loperamide, alprostadil, melatonin.
  • the UV curable monomer can be selected from a group comprising of acrylate derivatives which includes but not limited to ⁇ , ⁇ '- Methylenebis(acrylamide), acrylamide, 4-acetoxyphenethyl acrylate, acryloyl chloride, 2- hydroxyethyl methacrylate, bis- glycidyl methacrylate, triethylene glycol monomethacrylate (TEGMA), urethane dimethacrylate (UDMA) etc.
  • acrylate derivatives which includes but not limited to ⁇ , ⁇ '- Methylenebis(acrylamide), acrylamide, 4-acetoxyphenethyl acrylate, acryloyl chloride, 2- hydroxyethyl methacrylate, bis- glycidyl methacrylate, triethylene glycol monomethacrylate (TEGMA), urethane dimethacrylate (UDMA) etc.
  • the photoinitiator can be selected from a group comprising of camphorquinone, lucirin, Irgacure 651, Irgacure 184, Irgacure 2959, Irgacure 907 and Darocur MBF etc.
  • a ready-made mixed composition of acrylate based monomers and photoinitiators will be used.
  • One of the example of such ready-made mixed composition is, but not limiting to, Helioseal ® F.
  • the plasticizers (or alternatively referred to as film forming agent) can be selected from a group comprising of Kollidone VA64, triethyl citrate, dimethyl isosorbide, acetyltributyl citrate, castor oil, propylene glycol, and polyethylene glycol or any other two or more of the above in combination.
  • the permeability enhancers can be selected from a group comprising of Octyl salicylate, dimethyl sulfoxide, dimethyl formamide, or isopropyl myristate, Tween 80, sodium lauryl sulfate, oleic acid, octyl dimethyl paraamino benzoic acid (Padimate O), polyhydric alcohol, propylene glycol, diethylene monoethyl ether EP (Transcutol) or any two or more of the above in combination.
  • the antioxidants can be selected from a group comprising of Vitamin E, propyl gallate, butylated hydroxyanisole, butylated hydroxytoluene, ascorbic acid, tocotrienols, carotenoids etc.
  • the release retarding agent can be selected from a group comprising of Eudragit RSPO, copolymer of methyl methacrylate and butyl methacrylate (Plastoid B ® ), a copolymer of dimethylamine ethyl methacrylate and a neutral methacrylic acid ester (Eudragit E 100 ® ), ammonio methacrylate copolymer type B (Eudragit RS ® , USP/NF), ammonio methacrylate copolymer type A (Eudragit RL , USP/NF), methacrylic acid copolymer type A (Eudragit L100 ® , USP/NF), methacrylic acid copolymer type B (Eudragit S 100 ® , USP/NF), polyvinyl acetate, cellulose acetate, polyvinyl alcohol, povidone vinyl acetate, hydroxyl propyl methyl cellulose, hydroxyl ethy
  • the solvent can be selected from a group comprising of ethanol, methanol, acetone, ethyl acetate, chloroform, dichloro methane or any other two or more of the above in combination.
  • the transdermal delivery system comprises 1 to 30 %w/v of drug or combination of drugs. In an embodiment of the invention, the transdermal delivery system comprises 1 to 20 %w/v of UV curable monomers.
  • the transdermal delivery system comprises 1 to 10 %w/v of photoinitiator(s).
  • the transdermal delivery system comprises 1 to
  • plasticizers or film forming agent
  • the transdermal delivery system comprises 1 to 8 %w/v of permeability enhancer.
  • the transdermal delivery system comprises 0.1 to 3 %w/v of antioxidant(s).
  • the transdermal delivery system comprises 1 to 10 %w/v of release retarding agent(s).
  • a remaining portion of the transdermal delivery system is constituted by solvent.
  • the process comprises addition and solubilisation of the drug, the UV curable monomer and photo initiator, optionally other elements such as plasticizer, permeability enhancer, antioxidant, and release retarding agent in a sequential manner in the solvent with the aid of stirring. These ingredients are added in the weight percentage as mentioned above.
  • the resulting transdermal delivery system from such process is a clear solution.
  • the final volume makeup of the transdermal delivery system is performed using the solvent.
  • transdermal delivery system prepared using different combinations of drug, the UV curable monomer and photo initiator, optionally other elements such as plasticizer, permeability enhancer, antioxidant, and release retarding agent in the solvent.
  • the transdermal spray device for storing and dispensing of the transdermal delivery system is described in detail with reference to figures 1 and 2.
  • the transdermal spray device is illustrated in figures 1 and 2 as a hand-held dispensing device (100).
  • the transdermal spray device (100) comprises means (101, 102, 103) for storing and dispensing of the transdermal delivery system.
  • the transdermal delivery system comprises a drug or combination of drugs along with at least one UV curable monomer and a solvent system.
  • the means (101, 102, 103) is constituted by a hollow body (101) adapted to receive the transdermal delivery system, which may be in fluid state (including a viscous state).
  • the hollow body (101) may be adapted to receive a container including the transdermal delivery system.
  • the means comprises a nozzle (102), which is in fluid flow communication with the transdermal delivery system, and a nozzle actuator mechanism (103), which upon actuation dispenses the transdermal delivery system via an outlet port of the nozzle (102).
  • the nozzle (102) dispenses the transdermal delivery system in form of a spray.
  • the nozzle (102) may be adapted to deliver a metered-quantity of the transdermal delivery system in response to actuation of the nozzle actuator mechanism (103).
  • the hollow body (101) may additionally define a wall (104) surrounding the nozzle (102).
  • the transdermal spray device (100) comprises one or more UV-light emitting sources (105), which may be placed on the wall (104) such that the UV-light emitting source (105) illuminates a space defined between the nozzle (102) and the wall (104).
  • the hollow body may additionally include a UV-light source actuator mechanism (106).
  • the wall (104) may additionally help in controlling a spray pattern (107) of the transdermal delivery system dispensed by the nozzle (102).
  • the transdermal spray device (100) can be further provided with a closure cap detachably mountable on the wall (104). In operation, the transdermal spray device upon receiving an actuation (i.e.
  • the UV light source (105) initiates a curing procedure of the dispensed transdermal delivery system through emission of a UV radiation.
  • the emission of UV radiation may be triggered manually by a user through the actuator-mechanism (106). In other scenario, such emission may be automatically triggered. Nevertheless, whether automatic or manual, the emission of UV radiation is always in relation to the dispensing, since the emission of UV radiation is timed either alongside the dispensing or post elapse of a brief pre-determined time-interval after said dispensing. In other words, the dispensing and the emission of UV radiation depict different yet connected events of a same operation.
  • transdermal delivery system as described above and the transdermal spray device allows for the realizing one or more of the following advantages.
  • Enhance therapeutic outcome & prolonged drug action The dissolved form of the drug in the solvent systems facilitates the drug permeation through stratum corneum and further augment the permeability through deeper layers of skin.
  • the in silico polymerization process occurs eventually which helps entrapment the drug in the cured polymeric layer.
  • This scenario confers an additional release retardant effect and may even enhance this effect along with other release retardant polymers. This effect would help govern the release profile of the drug for desired duration which would not be practically possible with general topical sprays.
  • the system in addition would provide robustness and skin adhesive capability to bestow therapeutic action for longer duration.
  • the topical spray is non-occlusive and helps reduce the problem of skin irritation associated with transdermal patches.
  • Enhance patient's compliance The product eliminates the need of repeated use which offers a patient convenient dosage regimen.
  • Dose flexibility Installation of metered dose dispensing accessories in the spray device will help facilitate dispensing of desired dose of formulation on to the skin as per patients requirement.
  • Aesthetic appeal In addition, the transparent layer enhances the aesthetic appeal of the system compared to transdermal patches. While specific language has been used to describe the disclosure, any limitations arising on account of the same are not intended. As would be apparent to a person in the art, various working modifications may be made to the disclosure in order to implement the inventive concept as taught herein.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Dispersion Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un dispositif de pulvérisation transdermique et un système d'administration transdermique maintenu par le dispositif. Le dispositif comprend des moyens (101, 102, 103) pour le stockage et la distribution d'un système d'administration transdermique, et au moins une source de lumière UV (105) pour initier une procédure de durcissement du système d'administration transdermique par rapport à l'action de distribution. Le système d'administration transdermique comprend à son tour un médicament ou une combinaison de médicaments avec au moins un monomère durcissable par UV et un système de solvant.
PCT/IN2017/050519 2016-11-11 2017-11-10 Système d'administration transdermique et dispositif de pulvérisation WO2018087779A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN201621038615 2016-11-11
IN201621038615 2016-11-11

Publications (1)

Publication Number Publication Date
WO2018087779A1 true WO2018087779A1 (fr) 2018-05-17

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019140087A1 (fr) * 2018-01-10 2019-07-18 Celista Pharmaceuticals Llc Pulvérisation transdermique de testostérone avec film

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020122771A1 (en) * 2000-09-23 2002-09-05 Troy Holland Spray hydrogel wound dressings
US6723077B2 (en) * 2001-09-28 2004-04-20 Hewlett-Packard Development Company, L.P. Cutaneous administration system
US6958154B2 (en) * 1998-08-20 2005-10-25 3M Innovative Properties Company Spray on bandage and drug delivery system
US20090145452A1 (en) * 2006-05-11 2009-06-11 Living Proof, Inc. Devices and methods of use for treatment of skin and hair
US20090194474A1 (en) * 2008-02-05 2009-08-06 L V M H Recherche Fluid Dispenser Device and a Dispensing Method
US20130032610A1 (en) * 2011-08-01 2013-02-07 Aptar France S.A.S. Fluid dispenser
US20150209808A1 (en) * 2014-01-24 2015-07-30 The Procter & Gamble Company Package for Light Activated Treatment Composition
US20150250922A1 (en) * 2014-03-07 2015-09-10 Megan Cole Polymeric hydrogel for accelerating wound healing
US20160067252A1 (en) * 2013-03-15 2016-03-10 Strategic Science & Technologies, Llc Transdermal delivery of sildenafil and other phosphodiesterase type 5 inhibitors

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6958154B2 (en) * 1998-08-20 2005-10-25 3M Innovative Properties Company Spray on bandage and drug delivery system
US20020122771A1 (en) * 2000-09-23 2002-09-05 Troy Holland Spray hydrogel wound dressings
US6723077B2 (en) * 2001-09-28 2004-04-20 Hewlett-Packard Development Company, L.P. Cutaneous administration system
US20090145452A1 (en) * 2006-05-11 2009-06-11 Living Proof, Inc. Devices and methods of use for treatment of skin and hair
US20090194474A1 (en) * 2008-02-05 2009-08-06 L V M H Recherche Fluid Dispenser Device and a Dispensing Method
US20130032610A1 (en) * 2011-08-01 2013-02-07 Aptar France S.A.S. Fluid dispenser
US20160067252A1 (en) * 2013-03-15 2016-03-10 Strategic Science & Technologies, Llc Transdermal delivery of sildenafil and other phosphodiesterase type 5 inhibitors
US20150209808A1 (en) * 2014-01-24 2015-07-30 The Procter & Gamble Company Package for Light Activated Treatment Composition
US20150250922A1 (en) * 2014-03-07 2015-09-10 Megan Cole Polymeric hydrogel for accelerating wound healing

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019140087A1 (fr) * 2018-01-10 2019-07-18 Celista Pharmaceuticals Llc Pulvérisation transdermique de testostérone avec film
US11523994B2 (en) 2018-01-10 2022-12-13 Celista Pharmaceuticals Llc Testosterone transdermal spray with film

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