WO2009070829A1 - Non-aqueous oil-based fentanyl compositions for transmucosal administration - Google Patents

Non-aqueous oil-based fentanyl compositions for transmucosal administration Download PDF

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Publication number
WO2009070829A1
WO2009070829A1 PCT/AU2008/001779 AU2008001779W WO2009070829A1 WO 2009070829 A1 WO2009070829 A1 WO 2009070829A1 AU 2008001779 W AU2008001779 W AU 2008001779W WO 2009070829 A1 WO2009070829 A1 WO 2009070829A1
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Prior art keywords
oil
fentanyl
composition
active agent
solvent
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Application number
PCT/AU2008/001779
Other languages
French (fr)
Inventor
Alexander James Kelly
Original Assignee
Krius Pty Ltd
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
Priority claimed from AU2007906641A external-priority patent/AU2007906641A0/en
Application filed by Krius Pty Ltd filed Critical Krius Pty Ltd
Publication of WO2009070829A1 publication Critical patent/WO2009070829A1/en

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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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect

Definitions

  • the invention described herein relates generally to anesthesia and analgesia.
  • the invention is directed to transmucosal administration of a non-aqueous composition containing fentanyl or its derivatives, including nasal administration, although the scope of the invention is not necessarily limited thereto.
  • Fentanyls are extensively used for anesthesia and analgesia, most often in the operating room and intensive care unit.
  • Fentanyl transdermal patch is used in chronic pain management.
  • Fentanyl patches work by releasing fentanyl into body fats, which then slowly release the drug into the blood stream over 72 hours, allowing for long lasting relief from pain.
  • Fentanyl lozenges are a solid formulation of fentanyl citrate on a stick in the form of a lollipop that dissolves slowly in the mouth for transmucosal absorption. These lozenges are intended for opioid-tolerant individuals and are effective in treating breakthrough cancer pain.
  • Small fentanyl buccal pellets have also been developed. These are effervescent tablets placed in the cheek and is absorbed through the buccal mucosa. One advantage of such tablets is claimed to be quicker absorption into the bloodstream at lower dosage levels.
  • Fentanyl is frequently given intrathecally as part of spinal anesthesia or epidurally for epidural anesthesia and analgesia. It is also used as a sedative.
  • fentanyl administered transmucosally or intranasally is effective in the relief of postoperative pain and cancer pain.
  • Transmucosal and intranasal delivery of low concentrations and low doses of fentanyl have been performed.
  • Transmucosal and nasal routes would therefore be suitable for use in patients requiring rapid relief from severe pain.
  • General advantages of transmucosal and nasal application aiming at systemic effect are ease of self-administration, supporting a health- economic argument and the self-care concept. In addition, first pass liver metabolism and gastro-intestinal metabolism are avoided.
  • WO2002/009707 describes intranasal delivery of fentanyl in aqueous solutions. Although effective, fentanyl and derivatives are not particularly soluble in water. In addition, absorption of the active agent from an aqueous solution is not optimal.
  • the invention provides compositions of fentanyl and derivatives in non-aqueous formulation with unexpected advantages over the compositions disclosed in the prior art.
  • the invention provides a composition for transmucosal administration, the composition comprising a solution of at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl in at least one non-aqueous oil-based solvent.
  • the invention provides a method of treating pain in a subject, the method comprising transmucosal administration of a composition comprising at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl, in a non-aqueous oil-based solvent.
  • the composition comprises fentanyl or a derivative thereof, such as alfentanyl, sulfentanyl, remifentanyl, carfentanyl and ohmefentanyl, or the salts of fentanyl and the derivatives.
  • the composition comprises a mixture of fentanyl and one or more fentanyl derivative.
  • the concentration of active agent in the composition can be any practicable concentration but is preferably from l ⁇ g/ml to 100mg/ml.
  • the solvent of the invention can be any practicable non-aqueous oil-based solvent, such as vegetable oils, for example olive oil, almond oil, peppermint oil, macadamia oil, eucalyptus oil, canola oil, cottonseed oil, peanut oil and soybean oil; or other equivalents of a pharmacopoeial nature, for example paraffin liquid, glycerine, polyethylene glycol, polypropylene glycol.
  • the solvent of the invention is preferably glycerine (glycerol), paraffin liquid, olive oil or almond oil.
  • the composition can further comprise a fragrance component, such as an ester, scented oil, or artificial scent.
  • a fragrance component such as an ester, scented oil, or artificial scent.
  • the composition can also further comprise a preservative such as benzyl alcohol, LiquaPar® Oil (ISP Corporation), benzalkonium chloride, EDTA, benzethonium chloride, chlorobutanol, parabens and phenoxyethanol, to allow for inclusion of the composition in a device for multi-dose administration.
  • a preservative such as benzyl alcohol, LiquaPar® Oil (ISP Corporation), benzalkonium chloride, EDTA, benzethonium chloride, chlorobutanol, parabens and phenoxyethanol.
  • the preservative is LiquaPar® Oil, parabens, benzyl alcohol or benzalkonium chloride.
  • Transmucosal administration can be effected by any practicable manner, but is preferable effected by nasal administration.
  • the nasal administration of the composition can be effected in any practicable manner, including by swab, droplets, or spray.
  • the composition is preferably administered by spray, from a suitable spray device.
  • the device can be of any appropriate configuration, and is preferably a device which delivers a spray volume of between 1 ⁇ l and 1 ml per actuation of the device.
  • An example of such a device is a Valois® VP7 pump, or the Valois FreepodTM system.
  • the invention therefore provides a composition of fentanyl or derivatives thereof with enhanced solubility, drug delivery and drug uptake, which necessitates lower doses of the active and consequent lower incidence of side effects.
  • the non-aqueous oil-based solvent also increases the stability of the active in solution, ensuring a longer shelf-life and preservation of activity of the composition.
  • fragrance acts as an identifier for both healthcare workers and patients to increase safety of administration and patient compliance.
  • composition is packaged in a glass vial of Type 1 clear or amber glass of volume from 0.1 milliliter up to 100 milliliters of the type typically used for an injection pharmaceutical.
  • composition may also be packaged in a single use device of the type manufactured by Valois or equivalent such as the Valois MonodoseTM or DolphinTM.
  • a single use device of the type manufactured by Valois or equivalent such as the Valois MonodoseTM or DolphinTM.
  • volume of a single-use container is between 0.1 and 2 milliliters
  • Fentanyl is highly lipid soluble and stable in such a non-aqueous liquid phase. It has an octanol-water partition coefficient (drug lipid-solubility study method) several thousand times higher than morphine, a readily water soluble opiate drug.
  • Fentanyl's high solubility in non-aqueous solutions can improve the uptake of the drug via the transmucosal and particularly the nasal route.
  • fentanyl citrate Using a non-aqueous system allows the form ⁇ lator to use the exact quantity of fentanyl base for formulation, thereby reducing errors and reducing salts of addition for some water- soluble versions of fentanyl, for example fentanyl citrate.
  • a non-aqueous formulation is retained for a prolonged period on the mucosa, particularly the nasal mucosa, when compared to an aqueous formulation.
  • a non-aqueous formulation can mask the unpleasant taste experienced at the back of the throat upon application of an opioid-containing nasal spray.
  • a non-aqueous formulation ensures the drug cannot be easily misused by mixing with other solutions, for example a non-aqueous solution of fentanyl would not be miscible with an alcoholic drink and therefore a potential 'date-rape' victim would be alerted to the presence of that formulation in such a drink.
  • Non-aqueous based transmucosal and nasal sprays have more comfortable feel on administration, avoiding the "cold" feeling of an aqueous system.
  • Non-aqueous formulations can assist with inclusion of a fragrance to improve drug safety and compliance. It is clear from the foregoing that the invention provides an improved composition of fentanyl and/or its derivatives for transmucosal administration.
  • the invention provides a composition of fentanyl or derivatives thereof with enhanced solubility, drug delivery and drug uptake, which necessitates lower doses of the active and consequent lower incidence of side effects. Stability of the active in solution is also increased.
  • optional inclusion of a fragrance acts as an identifier for both healthcare workers and patients to increase safety of administration and patient compliance.
  • optimal inclusion of a preservative allows for provision of a multi-dose formulation.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Otolaryngology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention provides a composition and method of treating pain using the composition, the composition comprising a solution of at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl in at least one non-aqueous oil-based solvent for transmucosal administration.

Description

NON-AQUEOUS OIL-BASED FENTANYL COMPOSITIONS FOR TRANSMUCOSAL ADMINISTRATION
TECHNICAL FIELD
The invention described herein relates generally to anesthesia and analgesia. In particular, the invention is directed to transmucosal administration of a non-aqueous composition containing fentanyl or its derivatives, including nasal administration, although the scope of the invention is not necessarily limited thereto.
BACKGROUND ART
Fentanyls are extensively used for anesthesia and analgesia, most often in the operating room and intensive care unit. Fentanyl transdermal patch is used in chronic pain management. Fentanyl patches work by releasing fentanyl into body fats, which then slowly release the drug into the blood stream over 72 hours, allowing for long lasting relief from pain.
Fentanyl lozenges are a solid formulation of fentanyl citrate on a stick in the form of a lollipop that dissolves slowly in the mouth for transmucosal absorption. These lozenges are intended for opioid-tolerant individuals and are effective in treating breakthrough cancer pain.
Small fentanyl buccal pellets have also been developed. These are effervescent tablets placed in the cheek and is absorbed through the buccal mucosa. One advantage of such tablets is claimed to be quicker absorption into the bloodstream at lower dosage levels.
Fentanyl is frequently given intrathecally as part of spinal anesthesia or epidurally for epidural anesthesia and analgesia. It is also used as a sedative.
It has been shown that fentanyl administered transmucosally or intranasally is effective in the relief of postoperative pain and cancer pain. Transmucosal and intranasal delivery of low concentrations and low doses of fentanyl have been performed.
Animal data shows rapid occurring absorption by use of the transmucosal and particularly the nasal route. Transmucosal and nasal routes would therefore be suitable for use in patients requiring rapid relief from severe pain. General advantages of transmucosal and nasal application aiming at systemic effect are ease of self-administration, supporting a health- economic argument and the self-care concept. In addition, first pass liver metabolism and gastro-intestinal metabolism are avoided.
WO2002/009707 describes intranasal delivery of fentanyl in aqueous solutions. Although effective, fentanyl and derivatives are not particularly soluble in water. In addition, absorption of the active agent from an aqueous solution is not optimal.
Therefore, there would be an advantage if it were possible to provide a composition for transmucosal administration of fentanyl and its derivatives, which may overcome at least some of the above-mentioned disadvantages or provide a useful or commercial choice.
SUMMARY OF THE INVENTION The invention provides compositions of fentanyl and derivatives in non-aqueous formulation with unexpected advantages over the compositions disclosed in the prior art.
In a first embodiment, the invention provides a composition for transmucosal administration, the composition comprising a solution of at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl in at least one non-aqueous oil-based solvent.
In a second embodiment, the invention provides a method of treating pain in a subject, the method comprising transmucosal administration of a composition comprising at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl, in a non-aqueous oil-based solvent. With regard to the first and second embodiments as defined above, the composition comprises fentanyl or a derivative thereof, such as alfentanyl, sulfentanyl, remifentanyl, carfentanyl and ohmefentanyl, or the salts of fentanyl and the derivatives. Optionally, the composition comprises a mixture of fentanyl and one or more fentanyl derivative.
The concentration of active agent in the composition can be any practicable concentration but is preferably from lμg/ml to 100mg/ml.
The solvent of the invention can be any practicable non-aqueous oil-based solvent, such as vegetable oils, for example olive oil, almond oil, peppermint oil, macadamia oil, eucalyptus oil, canola oil, cottonseed oil, peanut oil and soybean oil; or other equivalents of a pharmacopoeial nature, for example paraffin liquid, glycerine, polyethylene glycol, polypropylene glycol. The solvent of the invention is preferably glycerine (glycerol), paraffin liquid, olive oil or almond oil.
The composition can further comprise a fragrance component, such as an ester, scented oil, or artificial scent. The addition of a fragrance ensures that a user of the composition knows when it has been administered. In addition, the composition can then not be administered without subject knowledge, and patient compliance is improved due to a pleasant smell on application of the composition.
The composition can also further comprise a preservative such as benzyl alcohol, LiquaPar® Oil (ISP Corporation), benzalkonium chloride, EDTA, benzethonium chloride, chlorobutanol, parabens and phenoxyethanol, to allow for inclusion of the composition in a device for multi-dose administration. Preferably, the preservative is LiquaPar® Oil, parabens, benzyl alcohol or benzalkonium chloride.
Transmucosal administration can be effected by any practicable manner, but is preferable effected by nasal administration.
The nasal administration of the composition can be effected in any practicable manner, including by swab, droplets, or spray. The composition is preferably administered by spray, from a suitable spray device. The device can be of any appropriate configuration, and is preferably a device which delivers a spray volume of between 1 μl and 1 ml per actuation of the device. An example of such a device is a Valois® VP7 pump, or the Valois Freepod™ system.
The invention therefore provides a composition of fentanyl or derivatives thereof with enhanced solubility, drug delivery and drug uptake, which necessitates lower doses of the active and consequent lower incidence of side effects. The non-aqueous oil-based solvent also increases the stability of the active in solution, ensuring a longer shelf-life and preservation of activity of the composition.
The optional inclusion of a fragrance acts as an identifier for both healthcare workers and patients to increase safety of administration and patient compliance.
In order that the invention may be more readily understood and put into practice, one or more preferred embodiments thereof will now be described, by way of example only. - A -
DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS Examples Formulations of the invention are made in the following manner:
1. Preserved Formulations: Fentanyl 2.5 mg
LiquaPar Oil 0.02 mL
Olive Oil q.s.5.0 mL
Fentanyl 5.0 mg
LiquaPar Oil 0.02 mL Olive Oil q.s.5.0 mL
Fentanyl 2.5 mg
LiquaPar Oil 0.02 mL
Vanillin BP 25.0 mg
Almond Oil q.s.5.0 mL Fentanyl 5.0 mg
LiquaPar Oil 0.02 mL
Vanillin BP 25.0 mg
Almond Oil q.s.5.0 mL
2. Unpreserved Formulations: Fentanyl 2.5 mg
Vanillin BP 25.0 mg
Glycerol q.s.5.0 mL
Fentanyl 5.0 mg
Vanillin BP 25.0 mg Glycerol q.s.5.0 mL
3. Pediatric Formulations:
Fentanyl 1.0 mg
Vanillin BP 25.0 mg Glycerol q.s.5.0 mL
Fentanyl 1.0 mg
LiquaPar Oil 0.02 mL
Vanillin BP 25.0 mg Almond Oil q.s.5.0 mL
The composition is packaged in a glass vial of Type 1 clear or amber glass of volume from 0.1 milliliter up to 100 milliliters of the type typically used for an injection pharmaceutical.
The composition may also be packaged in a single use device of the type manufactured by Valois or equivalent such as the Valois Monodose™ or Dolphin™. Typically the volume of a single-use container is between 0.1 and 2 milliliters
Efficacy and Uses of Formulations
Fentanyl is highly lipid soluble and stable in such a non-aqueous liquid phase. It has an octanol-water partition coefficient (drug lipid-solubility study method) several thousand times higher than morphine, a readily water soluble opiate drug.
Fentanyl's high solubility in non-aqueous solutions can improve the uptake of the drug via the transmucosal and particularly the nasal route.
Using a non-aqueous system allows the formύlator to use the exact quantity of fentanyl base for formulation, thereby reducing errors and reducing salts of addition for some water- soluble versions of fentanyl, for example fentanyl citrate.
A non-aqueous formulation is retained for a prolonged period on the mucosa, particularly the nasal mucosa, when compared to an aqueous formulation.
A non-aqueous formulation can mask the unpleasant taste experienced at the back of the throat upon application of an opioid-containing nasal spray. A non-aqueous formulation ensures the drug cannot be easily misused by mixing with other solutions, for example a non-aqueous solution of fentanyl would not be miscible with an alcoholic drink and therefore a potential 'date-rape' victim would be alerted to the presence of that formulation in such a drink. Non-aqueous based transmucosal and nasal sprays have more comfortable feel on administration, avoiding the "cold" feeling of an aqueous system.
Non-aqueous formulations can assist with inclusion of a fragrance to improve drug safety and compliance. It is clear from the foregoing that the invention provides an improved composition of fentanyl and/or its derivatives for transmucosal administration. The invention provides a composition of fentanyl or derivatives thereof with enhanced solubility, drug delivery and drug uptake, which necessitates lower doses of the active and consequent lower incidence of side effects. Stability of the active in solution is also increased. In addition, optional inclusion of a fragrance acts as an identifier for both healthcare workers and patients to increase safety of administration and patient compliance. Also, optimal inclusion of a preservative allows for provision of a multi-dose formulation.
The foregoing embodiments are illustrative only of the principles of the invention, and various modifications and changes will readily occur to those skilled in the art. The invention is capable of being practiced and carried out in various ways and in other embodiments. It is also to be understood that the terminology employed herein is for the purpose of description and should not be regarded as limiting.
The term "comprise" and variants of the term such as "comprises" or "comprising" are used herein to denote the inclusion of a stated integer or stated integers but not to exclude any other integer or any other integers, unless in the context or usage an exclusive interpretation of the term is required.
Any reference to publications cited in this specification is not an admission that the disclosures constitute common general knowledge in Australia.

Claims

The claims defining the invention are as follows:
1. A composition for transmucosal administration, the composition comprising a solution of at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl,l in at least one non-aqueous oil-based solvent.
2. The composition of claim 1 wherein the at least one active agent is selected from the group consisting of fentanyl, alfentanyl, sulfentanyl, remifentanyl, ohmefantanyl and carfentanyl in at least one non-aqueous oil-based solvent.
3. The composition of claim 1 or claim 2 wherein the concentration of the active agent is from lμg/ml to lOOmg/ml.
4. The composition of any one of claims 1 to 3 wherein the at least one solvent is a plant oil. 7
5. The composition of claim 4 wherein the at least one solvent is selected from the group consisting of olive oil, almond oil, peppermint oil, macadamia oil, eucalyptus oil, canola oil, cottonseed oil, peanut oil, coconut oil, castor oil(s), grapeseed oil, soybean oil, other vegetable and nut oils.
6. The composition of any one of claims 1 to 3 wherein the at least one solvent is selected from the group consisting of a glycol, paraffin liquid and glycerine.
7. The composition of any one of claims 1 to 6 further comprising a fragrance.
8. The composition of claim 7 further comprising a preservative.
9. The composition of any one of claims 1 to 8 wherein the administration is intranasal.
10. A method of treating pain in a subject, the method comprising transmucosal administration of a composition comprising at least one active agent selected from the group consisting of fentanyl, a derivative of fentanyl and an analogue of fentanyl, in a non-aqueous oil-based solvent.
1 1. The method of claim 10 wherein the at least one active agent is selected from the group consisting of fentanyl, alfentanyl, sulfentanyl, remifentanyl, carfentanyl and ohmefentanyl in a non-aqueous oil-based solvent.
12. The method of claim 10 or claim 11 wherein the concentration of the active agent is from lμg/ml to lOOmg/ml.
13. The method of any one of claims 10 to 12 wherein the solvent is a plant oil.
14. The method of claim 13 wherein the at least one solvent is selected from the group consisting of olive oil, almond oil, peppermint oil, macadamia oil, eucalyptus oil, canola oil, cottonseed oil, peanut oil, coconut oil, castor oils, grapeseed oil,soybean oil, other vegetable oils, and other nut oils.
15. The method of any one of claims 10 to 12 wherein the at least one solvent is selected from the group consisting of a glycol, paraffin liquid and glycerine.
16. The method of any one of claims 10 to 15 further comprising a fragrance.
17. The method of claim 16 further comprising a preservative.
18. The method of any one of claims 10 to 17 wherein the administration is intranasal.
19. The method of claim 18 wherein administration is via a spray device.
20. The method of claim 19 wherein the spray device delivers a unit-dose of the active agent upon actuation of between 0.00 ImL to 2mL.
21. The method of claim 19 wherein the spray device delivers a multi-dose of the active agent upon actuation of between 0.00 ImL to 2mL.
PCT/AU2008/001779 2007-12-05 2008-12-02 Non-aqueous oil-based fentanyl compositions for transmucosal administration WO2009070829A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AU2007906641A AU2007906641A0 (en) 2007-12-05 Novel Compositions
AU2007906641 2007-12-05

Publications (1)

Publication Number Publication Date
WO2009070829A1 true WO2009070829A1 (en) 2009-06-11

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8017627B2 (en) 2000-07-31 2011-09-13 Nycomed Danmark Aps Fentanyl composition for nasal administration
GB2481728A (en) * 2010-06-30 2012-01-04 Londonpharma Ltd Formulations and delivery devices for the sublingual administration of opioids
GB2534624A (en) * 2014-08-21 2016-08-03 Simon Corbitt Terence Formulations for transmucosal delivery

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002009707A1 (en) * 2000-07-31 2002-02-07 Nycomed Danmark A/S Fentanyl composition for nasal administration
US20040115133A1 (en) * 2000-05-10 2004-06-17 Wermeling Daniel P. Intranasal opioid compositions
WO2005117830A1 (en) * 2004-06-04 2005-12-15 Camurus Ab Liquid depot formulations
US20070225379A1 (en) * 2001-08-03 2007-09-27 Carrara Dario Norberto R Transdermal delivery of systemically active central nervous system drugs

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040115133A1 (en) * 2000-05-10 2004-06-17 Wermeling Daniel P. Intranasal opioid compositions
WO2002009707A1 (en) * 2000-07-31 2002-02-07 Nycomed Danmark A/S Fentanyl composition for nasal administration
US20070225379A1 (en) * 2001-08-03 2007-09-27 Carrara Dario Norberto R Transdermal delivery of systemically active central nervous system drugs
WO2005117830A1 (en) * 2004-06-04 2005-12-15 Camurus Ab Liquid depot formulations

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8017627B2 (en) 2000-07-31 2011-09-13 Nycomed Danmark Aps Fentanyl composition for nasal administration
US8158651B2 (en) 2000-07-31 2012-04-17 Nycomed Danmark Aps Fentanyl composition for nasal administration
US8653107B2 (en) 2000-07-31 2014-02-18 Takeda Pharma A/S Fentanyl composition for nasal administration
GB2481728A (en) * 2010-06-30 2012-01-04 Londonpharma Ltd Formulations and delivery devices for the sublingual administration of opioids
WO2012001411A3 (en) * 2010-06-30 2012-03-29 Londonpharma Ltd Pharmaceutical compositions for sublingual delivery of opioids
GB2481728B (en) * 2010-06-30 2012-05-23 Londonpharma Ltd Formulations and delivery devices for the sublingual administration of opioids
EP2653152A1 (en) * 2010-06-30 2013-10-23 Londonpharma Ltd. Pharmaceutical compositions for sublingual delivery of opioids
GB2534624A (en) * 2014-08-21 2016-08-03 Simon Corbitt Terence Formulations for transmucosal delivery

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