Classifications

• • 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
• • 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
  • A61K31/13—Amines
  • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
  • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• • 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
  • A61K31/16—Amides, e.g. hydroxamic acids
  • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• • 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
• • 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
  • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • 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
  • A61K9/0048—Eye, e.g. artificial tears
• • 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
  • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
  • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
• • 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
  • A61P17/00—Drugs for dermatological disorders
  • A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P23/00—Anaesthetics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P23/00—Anaesthetics
  • A61P23/02—Local anaesthetics
• • 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
  • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
  • A61P27/12—Ophthalmic agents for cataracts
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution

Definitions

• the present invention concerns the therapeutic field and more particularly the ophthalmologic field.
• compositions based on a parasympatholytic agent, an adrenergic substance and advantageously a local anaesthetic in the context of pre-operative treatment of the eye for a surgical operation on cataracts or laser treatment of the retina.
• active ingredients are to be administered simultaneously on or in the eye.
• the parasympatholytic agent is a mydriatic agent and preferably a derivative of tropic acid such as a tropic acid ester or a tropic acid amide or a cyclohexyl or cyclopentylacetic acid amide.
• parasympatholytic agents we shall notably mention cyclodrine, eucatropine, homatropine as well as atropine (benzylic ester of tropic acid), N-methyl hyoscine and especially tropicamide (N-ethyl 2-phenyl N-4 pyridyl methyl hydracrylamide or pyridyl methyl benzene acetamide).
• butocaine prilocaine, procaine, novocaine, tetracaine, ambucaine, amylocaine, bupivacaine, carticaine, butoxycaine, formocaine, mepivacaine, etidocaine, prilocaine, orthocaine, oxybuprocaine or benoxinate, and mainly lidocaine or diethylamino 2,6 dimethyl acetanilide, or one of its salts.
• noradrenaline phenylephrine, isoprenaline, dipivefrine, dimetrophine, norfenefrine, pholedrine or octedrine.
• compositions according to the invention are of major interest, notably in intracameral injection, for preparing the eye before a surgical operation or during the surgical operation, notably in the surgical treatment of cataracts.
• the volume of the intracameral chamber does not exceed 300 ⁇ l in man
• the volume of the composition injected should preferably be less than or equal to 200 ⁇ l, notably between 50 and 200 ⁇ l.
• compositions according to the invention can also be administered in a collyrium beforehand or during a laser intervention on the retina.
• 1 to 5 drops are instilled, which also represents a volume less than or equal to 200 ⁇ l.
• compositions according to the invention are capable of providing very rapid anaesthesia as well as nearly instantaneous, sizeable and sustainable dilation of the pupil for undertaking an examination of the pupil and the surgical operation as quickly as possible.
• anaesthesia is of long duration, so that the subject suffers little from the operation they undergo.
• Such a combination has the advantage of reinforcing the mydriatic effect of the parasympatholytic derivative, but without manifesting an overly long effect which leads to a decrease in vision essentially characterised by prolonged mydriasis.
• the effects of mydriasis mainly translate into disturbances of vision and balance.
• compositions according to the invention can be distinguished from those described in the prior art by a concentration of a sympathomimetic agent, for example phenylephrine, that is sharply reduced.
• a concentration of a sympathomimetic agent for example phenylephrine
• the concentration of the parasympatholytic agent is also reduced.
• a combination of just two mydriatic agents is thus distinguished from the solutions in the prior art by low concentrations of sympathomimetic agents, or even parasympatholytic agents.
• composition according to the invention also contains a local anaesthetic agent.
• compositions according to the invention contain between 0.001 and 0.6% parasympatholytic agent, between 0.04 and 0.5% sympathomimetic agent, and possibly between 0.2 and 3% local anaesthetic agent.
• a preferred composition contains between 0.01 and 0.5% parasympatholytic agent defined above, between 0.5 and 1.5% local anaesthetic and between 0.1 and 0.4% sympathomimetic agent.
• An ophthalmologic composition according to the invention contains between 0.015 and 0.025% parasympatholytic agent, advantageously tropicamide, between 0.75% and 1.25% lidocaine and between 0.2 and 0.4% phenylephrine in a single preparation.
• parasympatholytic agent advantageously tropicamide
• lidocaine between 0.2 and 0.4% phenylephrine
• Such a formulation is particularly well suited to injection into the anterior chamber of the eye before the surgical treatment of cataracts. For this, an incision is made at the time of the operation in the anterior chamber of the eye and the composition is injected into it. This preparation of the eye simultaneously causes mydriasis and local anaesthesia, allowing the later extraction of the lens under favourable conditions. In this precise case, a single injection of a volume of the preparation between 0.05 and 0.2 ml provides the desired effect.
• the concentrations of the pharmaceutical compositions instilled are advantageously adapted.
• the concentrations of the parasympatholytic agent and local anaesthetic agent will be significantly higher, in the higher values of the widest range of concentrations.
• the concentrations of the parasympatholytic agent will be between 0.1 and 0.25% and the concentration of the local anaesthetic agent will be between 2 and 3%.
• Such preparations being designed for a single use, the use of a preservative may not be necessary.
• the preparations according to the invention therefore may not contain any preservatives.
• the method of administration may also be different, proceeding with the instillation of the preparation on the treated eye in two to four times at one minute intervals. Thus, sedation of pain is ensured more immediately and for a longer time.
• the three active ingredients are dissolved or dispersed in an aqueous vehicle, advantageously sterile.
• the compositions according to the invention may come in liquid or solid form, for example in the form of collyriums, single-dose recipients, instillable preparations, ready-to-use or in freeze-dried form to be reconstituted with an aqueous solvent when used.
• compositions according to the invention may also come in a mixed form, for example one of the active ingredients being freeze-dried to be reconstituted by adding an aqueous solution containing the other active ingredients. It is also possible to have a bottle containing one of the solid active ingredients, covered by a frangible membrane above which can be found the solution containing the other active ingredients.
• the preparation according to the invention is to be administered by injection into the anterior chamber of the eye (intracameral zone).
• Said preparation could be presented in a single packaging for easy handling with total safety, then administered to the patient in a quantity of liquid less than 1 ml, typically between 50 and 200 ⁇ l.
• the preparation is used under the same conditions as in example 1.
• Said preparation will be presented in single-use packaging. This collyrium is particularly well suited to the treatment of pain during laser treatment.
• the collyriums according to the invention are to be instilled on the eye, in three times one drop during the same day.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Ophthalmology & Optometry (AREA)
• Pain & Pain Management (AREA)
• Emergency Medicine (AREA)
• Anesthesiology (AREA)
• Dermatology (AREA)
• Neurosurgery (AREA)
• Neurology (AREA)
• Biomedical Technology (AREA)
• Surgery (AREA)
• Dispersion Chemistry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

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• 2005
  • 2005-03-09 FR FR0502357A patent/FR2882930B1/fr active Active
• 2006
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  • 2006-03-09 WO PCT/FR2006/000528 patent/WO2006095095A1/fr active Application Filing
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