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
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
• • 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
  • A61K31/66—Phosphorus compounds
• • 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
  • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
  • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
  • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/04—Centrally acting analgesics, e.g. opioids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/34—Tobacco-abuse
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P35/00—Antineoplastic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P5/00—Drugs for disorders of the endocrine system
  • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
  • A61P5/30—Oestrogens
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
  • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure

Definitions

• the skin is the largest organ of the body, which functions to protect the internal organs from external chemical, physical and pathological hazards. Normal skin is divided into three layers: the epidermis, the dermis, and subcutaneous tissue.
• the outer cornified layer of the epidermis, the stratum corneum possesses properties of strength, flexibility, high electrical impedance and dryness that retards penetration and proliferation of microorganisms.
• the stratum corneum is also the principle barrier to transdermal drug absorption. There is a layer of sebum protecting the skin which has not commonly been considered to be a barrier to drug transport.
• a diffusing drug molecule When travelling through the skin, a diffusing drug molecule has a number of potential transport routes available. These include appendageal such as eccrine, follicular or epidermal such as inter or intra cellular. Current theories regarding the transport route point to two possible mechanisms: (i) passive transcellular and (ii) intracellular epidermal transport. Evidence also exists that active transport systems in the skin are important to regulate homeostasis and that this process operates to move compounds across membranes and throughout the dermis. Active transport mechanisms have not been considered or exploited as a drug delivery pathway, as the absorption process is believed to be largely a permeation process.
• Transdermal delivery devices include diffusion controlled polymeric membrane reservoir delivery systems. Such devices, often in the form of patches, aim to maintain a constant rate of drug release over an extended period of time under steady state conditions, which is sometimes referred to as "zero-order release” or "zero-order kinetics". Such patches usually consist of one or more rate controlling membranes surrounding a drug solution operating to maintain a constant rate of drug release. This is generally achieved by using membrane devices, microcapsules, liposomes and hollow fibres in various polymeric materials including silicone rubber, ethylene vinylacetate, cellulose acetate, copolymers, polyurethanes and hydrogels.
• transdermal delivery systems Another limitation to transdermal delivery systems is the difficulty in formulating a drug compound that is both sufficiently lipid soluble to absorb through phospholipid membranes yet water soluble to move in the aqueous cytosol and usually hydrophilic suspension media. Drug molecules need to pass both lipophilic and hydrophillic barriers in traversing the skin. This is difficult to achieve and can slow dermal transport.
• transdermal delivery system is used herein to refer to sustained release systems designed to alter absorption kinetics in favor of zero order release.
• R 1 is chosen from the group comprising straight or branched chain mixed alkyl radicals from C6 to C22 and carbonyl derivatives thereof;
• the device is a patch, poultice, gel, cream, plaster or other sustained- release system designed to alter absorption kinetics in towards zero order release.
• a method for improving the efficacy of a pharmaceutical hydroxy compound formulation comprising:
• ISP Corporation Procedure Combine Phase A items minus the carbomer and lauryliminodipropionic acid tocopheryl phosphate. When a solution is obtained, disperse carbomer in this solution. Begin heating Phase A to 70-75°C with adequate agitation. Disperse lauryliminodipropionic acid tocopheryl phosphate in carbomer mucilage with sweep agitation. Combine Phase B items and heat to 75- 80°C with adequate agitation. With Phase A uniform and at 70-75°C and Phase B uniform and at 75-80°C, add Phase B to Phase A with adequate agitation. Allow AB to cool to 50°C and then add Phase C solution to AB. Continue adequate agitation of ABC until 45°C is reached. Add Phase D to ABC. Continue adequate agitation until 35°C is reached.
• Each formulation was applied to the dorsal skin of an anaesthetised rat in an area of approximately 4 cm 2 marked with an indelible felt tip marker.
• Application of approximately 30 mg of formulation (containing 0.17 ⁇ g of E or EP) was applied to the site with a curved glass rod applicator. The formulation was 'rubbed' in until it appeared to have been absorbed into the skin, which took between 5-10 min. Any changes in the consistency of the formulation during this procedure were noted.
• the amount of formulation applied and the area of the application site were weighed for each animal.
• Each formulation was applied to the dorsal skin of an anaesthetized rat in an area of approximately 4 cm 2 marked with an indelible felt tip marker.
• Application of approximately 30 mg of formulation (containing 1 ⁇ g of T or TP) was applied to the site with a curved glass rod applicator. The formulation was 'rubbed' in until it appeared to have been absorbed into the skin, which took between 5 to 10 min. Any changes in the consistency of the formulation during this procedure were noted.
• Atropine sulfate and atropine phosphate formulated in phosphate buffer and given intravenously (IV) each to two rats at 2mg/kg resulted similar increases in heart rates.
• the baseline heart rate of a rat was approx. 350 bpm and increased to 450 bpm within 15 minutes after administration of atropine (either atropine phosphate or atropine sulfate). Approximately two hours later, normal heart rates were restored. This is regarded as a significant change in pulse rate.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• General Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Epidemiology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Dermatology (AREA)
• Biomedical Technology (AREA)
• Hospice & Palliative Care (AREA)
• Endocrinology (AREA)
• Addiction (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Cardiology (AREA)
• Neurology (AREA)
• Neurosurgery (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Diabetes (AREA)
• Otolaryngology (AREA)
• Reproductive Health (AREA)
• Pain & Pain Management (AREA)
• Psychiatry (AREA)
• Heart & Thoracic Surgery (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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• 2002
  • 2002-12-13 EP EP02784914A patent/EP1460995B1/en not_active Expired - Lifetime
  • 2002-12-13 AU AU2002350272A patent/AU2002350272B1/en not_active Ceased
  • 2002-12-13 DE DE60238276T patent/DE60238276D1/de not_active Expired - Lifetime
  • 2002-12-13 AT AT02784914T patent/ATE487456T1/de not_active IP Right Cessation
  • 2002-12-13 MX MXPA04005361A patent/MXPA04005361A/es active IP Right Grant
  • 2002-12-13 CA CA2466536A patent/CA2466536C/en not_active Expired - Fee Related
  • 2002-12-13 CN CNA028249674A patent/CN1604772A/zh active Pending
  • 2002-12-13 WO PCT/AU2002/001686 patent/WO2003049774A1/en not_active Ceased
  • 2002-12-13 BR BR0215102-2A patent/BR0215102A/pt not_active IP Right Cessation
  • 2002-12-13 US US10/498,684 patent/US20050089495A1/en not_active Abandoned
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