WO2003077885A3 - Free-base formulations of local anesthetics - Google Patents

Free-base formulations of local anesthetics Download PDF

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Publication number
WO2003077885A3
WO2003077885A3 PCT/US2003/007424 US0307424W WO03077885A3 WO 2003077885 A3 WO2003077885 A3 WO 2003077885A3 US 0307424 W US0307424 W US 0307424W WO 03077885 A3 WO03077885 A3 WO 03077885A3
Authority
WO
WIPO (PCT)
Prior art keywords
formulation
free
local anesthetics
base formulations
disclosed
Prior art date
Application number
PCT/US2003/007424
Other languages
French (fr)
Other versions
WO2003077885A2 (en
Inventor
Allan L Wilcox
Keith R Bley
Larry Litle
Arturo Angel
Gene Jamieson
Naweed Muhammad
Wendye R Robbins
Original Assignee
Neurogesx Inc
Allan L Wilcox
Keith R Bley
Larry Litle
Arturo Angel
Gene Jamieson
Naweed Muhammad
Wendye R Robbins
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 Neurogesx Inc, Allan L Wilcox, Keith R Bley, Larry Litle, Arturo Angel, Gene Jamieson, Naweed Muhammad, Wendye R Robbins filed Critical Neurogesx Inc
Priority to AU2003225745A priority Critical patent/AU2003225745A1/en
Publication of WO2003077885A2 publication Critical patent/WO2003077885A2/en
Publication of WO2003077885A3 publication Critical patent/WO2003077885A3/en

Links

Classifications

    • 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
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
    • 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
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K9/70—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
    • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L17/00—Materials for surgical sutures or for ligaturing blood vessels ; Materials for prostheses or catheters
    • A61L17/005—Materials for surgical sutures or for ligaturing blood vessels ; Materials for prostheses or catheters containing a biologically active substance, e.g. a medicament or a biocide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/40—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
    • A61L2300/402—Anaestetics, analgesics, e.g. lidocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/80—Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a special chemical form
    • A61L2300/802—Additives, excipients, e.g. cyclodextrins, fatty acids, surfactants

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Materials Engineering (AREA)
  • Surgery (AREA)
  • Vascular Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

An anesthetic formulation and methods of use are disclosed. The formulation includes an oleaginous base vehicle, a free base anesthetic and a solubility enhancer. Further, the formulation may additionally include penetration enhancers, antioxydants, solubility enhancers, gelling agents, and antimicrobial agents. The inventive formulation may be incorporated into a drug delivery patch or a drug delivery gel. Methods of use and application are also disclosed.
PCT/US2003/007424 2002-03-12 2003-03-11 Free-base formulations of local anesthetics WO2003077885A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003225745A AU2003225745A1 (en) 2002-03-12 2003-03-11 Free-base formulations of local anesthetics

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US36476102P 2002-03-12 2002-03-12
US60/364,761 2002-03-12
US42521202P 2002-11-07 2002-11-07
US60/425,212 2002-11-07

Publications (2)

Publication Number Publication Date
WO2003077885A2 WO2003077885A2 (en) 2003-09-25
WO2003077885A3 true WO2003077885A3 (en) 2004-03-18

Family

ID=28045438

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/007424 WO2003077885A2 (en) 2002-03-12 2003-03-11 Free-base formulations of local anesthetics

Country Status (2)

Country Link
AU (1) AU2003225745A1 (en)
WO (1) WO2003077885A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2408933A (en) * 2003-12-12 2005-06-15 Reckitt Benckiser Healthcare Antimicrobial composition
US9283177B2 (en) * 2007-01-16 2016-03-15 Juventio, Llc Topical anesthetic for rapid local anesthesia and method of applying a topical anesthetic
EP2016935A1 (en) * 2007-07-09 2009-01-21 Intendis GmbH Pharmaceutical composition for topical application of poorly soluble compounds
US8119694B2 (en) 2008-08-15 2012-02-21 Arcion Therapeutics, Inc. High concentration local anesthetic formulations
AU2009298411B2 (en) 2008-10-02 2013-06-06 Mylan Inc. Method of making a multilayer adhesive laminate
CN103142458B (en) 2013-01-22 2015-09-09 莱普德制药有限公司 Without prescription and the preparation method of additive analgesia sustained release drug delivery systems
CN111840553A (en) * 2019-04-15 2020-10-30 湖州依诺唯新药物制剂有限公司 Lipid pharmaceutical preparation and application thereof

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1907392A (en) * 1931-02-28 1933-05-02 Stover Oscar Hayen Anesthetic
US3849569A (en) * 1965-12-02 1974-11-19 Glaxo Lab Ltd Composition containing procaine penicillin
US4118480A (en) * 1973-02-09 1978-10-03 Charles V. Stoelker Pharmaceutical preparation for treating hemorrhoids and anal fissures
JPH0977662A (en) * 1995-09-11 1997-03-25 Zeria Pharmaceut Co Ltd Ointment
JPH10147521A (en) * 1996-09-18 1998-06-02 Yuutoku Yakuhin Kogyo Kk Persistent cataplasm for reducing pain
EP1125578A1 (en) * 1998-10-05 2001-08-22 Yutoku Pharmaceutical Ind. Co. Ltd. Tape material for transcutaneous absorption
US20030049283A1 (en) * 2001-08-31 2003-03-13 Vandell Victor E. Scalp desensitizing formulation

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1907392A (en) * 1931-02-28 1933-05-02 Stover Oscar Hayen Anesthetic
US3849569A (en) * 1965-12-02 1974-11-19 Glaxo Lab Ltd Composition containing procaine penicillin
US4118480A (en) * 1973-02-09 1978-10-03 Charles V. Stoelker Pharmaceutical preparation for treating hemorrhoids and anal fissures
JPH0977662A (en) * 1995-09-11 1997-03-25 Zeria Pharmaceut Co Ltd Ointment
JPH10147521A (en) * 1996-09-18 1998-06-02 Yuutoku Yakuhin Kogyo Kk Persistent cataplasm for reducing pain
EP1125578A1 (en) * 1998-10-05 2001-08-22 Yutoku Pharmaceutical Ind. Co. Ltd. Tape material for transcutaneous absorption
US20030049283A1 (en) * 2001-08-31 2003-03-13 Vandell Victor E. Scalp desensitizing formulation

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 9722, Derwent World Patents Index; AN 1997-241644, XP002252060, "Ointment for haemorrhoidal diseases contain e.g poly-glycerol fatty acid ester and lidocaine" *
DATABASE WPI Week 9832, Derwent World Patents Index; AN 1998-371035, XP002252061, "Plaster for relief of continuous pain comprises adding lidocaine as active ingredient and oily component" *

Also Published As

Publication number Publication date
AU2003225745A1 (en) 2003-09-29
AU2003225745A8 (en) 2003-09-29
WO2003077885A2 (en) 2003-09-25

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