WO2010064047A1 - Utilisation de sabcomeline pour le traitement de l'add ou de l'adhd - Google Patents

Utilisation de sabcomeline pour le traitement de l'add ou de l'adhd Download PDF

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Publication number
WO2010064047A1
WO2010064047A1 PCT/GB2009/051644 GB2009051644W WO2010064047A1 WO 2010064047 A1 WO2010064047 A1 WO 2010064047A1 GB 2009051644 W GB2009051644 W GB 2009051644W WO 2010064047 A1 WO2010064047 A1 WO 2010064047A1
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Prior art keywords
sabcomeline
treatment
add
adhd
agent
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PCT/GB2009/051644
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English (en)
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Argeris Karabelas
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Minster Research Limited
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Publication of WO2010064047A1 publication Critical patent/WO2010064047A1/fr

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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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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

Definitions

  • the present invention relates to the treatment of attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), to the treatment of cognitive impairment associated with ADD or ADHD, and to sabcomeline, pharmaceutically acceptable salts thereof, and compositions comprising sabcomeline for use in said treatments.
  • ADD attention deficit disorder
  • ADHD attention deficit hyperactivity disorder
  • sabcomeline pharmaceutically acceptable salts thereof, and compositions comprising sabcomeline for use in said treatments.
  • US Patent No. 5,278,170 discloses a series of compounds, including sabcomeline, which enhance cholinergic neuronal activity via functional action at muscarinic M1/M4 receptors within the central nervous system, and are said to be useful in the treatment or prophylaxis of dementia.
  • Sabcomeline otherwise known /?-(Z)- ⁇ -(methoxyimino)- ⁇ - (1-azabicyclo[2.2.2]oct-3-yl)acetonitrile is currently being investigated for a range of conditions, including schizophrenia, and cognitive decline and negative symptoms associated with schizophrenia.
  • International patent application WO 96/12486 refers to the use of sabcomeline in the treatment of Alzheimer's disease.
  • International patent application WO 00/03717 refers to the use of sabcomeline in the treatment of psychosis or other neuropsychiatric symptoms in patients with Alzheimer's disease with severe behavioural disturbance.
  • International patent application WO 01/76571 refers to the use of sabcomeline in the treatment of anxiety.
  • International patent application WO 2006/067496 refers to combinations of sabcomeline with a neuroleptic agent for the treatment of psychotic disorders.
  • International patent application WO 2006/067494 refers to the use of sabcomeline and combinations with mood stabilising or anti-manic agents for the treatment of bipolar disorders.
  • Attention deficit/hyperactivity disorder is a prevalent disorder in children and is characterised by behaviour that is significantly more inattentive or hyperactive than that of a child's peers of a similar age. The disorder has been found to have a strong genetic contribution (Bellgrove, M. A. et. al., Genetics of cognitive defects in ADHD: clues for novel treatment methods, Expert Rev. Neurotherapeutics, 2008, 8(4), 553-561 ).
  • Cognitive function refers to the general ability to organise, process, and recall information. Cognitive tasks may be subdivided into a large number of more specific functions, depend ing on the natu re of the information remembered and the circumstances of its recall. In addition, there are many functions commonly associated with cognition such as the ability to execute complex sequences of tasks. i Manifestations of cognitive impairment in ADD and ADHD may be characterised by deficits in working memory, attention/vigilance, such as spatial selective attention and attentional asymmetry, executive function (verbal learning and memory, visual learning and memory, speed of processing, reasoning and problem solving) and social cognition.
  • the present invention provides for the use of sabcomeline, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable composition of sabcomeline or said salt, in the manufacture of a medicament for the treatment of ADD or ADHD.
  • the treatment may be acute or prophylactic.
  • the present invention provides a method for the treatment of ADD or ADHD comprising administering to a patient in need thereof a pharmaceutically effective amount of sabcomeline, or a pharmaceutically acceptable salt thereof , o r a pharmaceutically acceptable composition of sabcomeline or said salt.
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADHD, comprising administering to a patient in need thereof a pharmaceutically effective amount of sabcomeline, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable composition of sabcomeline or said salt.
  • the present invention provides for sabcomeline, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable composition of sabcomeline or said salt, for use in the treatment of ADD or ADHD.
  • the treatment may be acute or prophylactic.
  • the present invention provides for sabcomeline, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable composition of sabcomeline or said salt, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • polymorphs, solvates, and radiolabeled derivatives of sabcomeline and pharmaceutically acceptable compositions thereof are also included within the scope of the present invention.
  • References to sabcomeline include such polymorphs, solvates and radiolabeled derivatives thereof.
  • Treatment with sabcomeline may be conducted at a dose of between 10 ⁇ g and 200 ⁇ g.
  • the dose is between 20 ⁇ g and 100 ⁇ g. More preferably, the dose is between 25 ⁇ g and 50 ⁇ g.
  • the dose may be administered as a single dose or twice daily.
  • the sabcomeline is administered at a dose of 25 ⁇ g twice daily.
  • sabcomeline is administered to the patient at dose ranges of 20 to 50 ⁇ g total daily dose with titration to optimal dose in the range 10 to 200 ⁇ g total daily dose.
  • sabcomeline is preferably used in the form of a pharmaceutically acceptable salt, typically the hydrochloride salt, but alternative salts of sabcomeline with pharmaceutically acceptable acids may also be utilised in therapeutic administration, for example salts derived from sabcomeline free base and acids including, but not limited to, hydrobromic acid, phosphoric acid, acetic acid, fumaric acid, maleic acid, salicylic acid, citric acid, lactic acid, oxalic acid and p-toluene sulphonic acid.
  • References to sabcomeline include pharmaceutically acceptable salts thereof and pharmaceutically acceptable compositions of sabcomeline or said salt.
  • Sabcomeline may be delivered alone, but will generally be delivered in the form of a pharmaceutically acceptable composition thereof, which comprises sabcomeline and one or more pharmaceutically acceptable diluents or carriers selected with regard to the intended route of administration.
  • Sabcomeline may be administered either independently or in combination with another suitable medication.
  • sabcomeline may be administered in combination with at least one neuroprotective agent and/or neuroleptic agent (which may be a typical or atypical antipsychotic agent).
  • neuroleptic agent which may be a typical or atypical antipsychotic agent.
  • the combinations, uses and methods of treatment of the invention may also provide advantages in treatment of patients who fail to respond adequately or who are resistant to other known treatments.
  • a neuroprotective agent may be defined as a compound which is intended to help limit the damage suffered by a nerve or neural tissue such as, for example, spinal cord, brain or nerve, when the blood supply is cut off or there is a traumatic injury.
  • psychotic disorders or diseases may be due in part to the abnormalities of neurons or synaptic function or architecture such as to cause a breakdown of neural integrity. It is believed that neuroprotective agents help prevent or stop the breakdown of neurons and neural integrity. Administering a neuroprotective agent alters the underlying pathology affecting integrity of neural function.
  • Neuroprotective agents include, but are not limited to, some types of antioxidants, antiinflammatories and anti-manic / mood stabiliser agents such as lithium.
  • the neuroprotective agent is selected from the group consisting of anti-oxidants, for example Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and anti-inflammatories such as non-steroidal anti-inflammatory, cyclo-oxygenase-2 (cox-2) inhibitors and statins.
  • the chosen neuroprotective agent is also an antipsychotic (typical or atypical)
  • antipsychotic typically or atypical
  • the clinical utility of the combination of sabcomeline and antipsychotic may vary between different members of the atypical antipsychotic drug class, depending on their different affinities for various sub-types of neurochemical receptors.
  • members of the atypical antipsychotic class may vary in their affinity for muscarinic and histamine receptor subtypes.
  • atypical antipsychotics at muscarinic receptor subtypes are such that properties of negligible affinity, weak agonist activity and weak antagonist activity have been reported amongst the various members of the atypical antipsychotic drug class.
  • the M1/M4 receptor agonist properties of sabcomeline may enhance functional cholinergic activity and, when administered in combination, provide benefit by: i) enhancing functional cholinergic activity in combination with an atypical antipsychotic that itself has little or no affinity for muscarinic receptors (e.g. risperidone); ii) providing additive functional cholinergic activity in combination with an atypical antipsychotic drug that has weak muscarinic receptor agonist effects (e.g.
  • clozapine or N-desmethylclozapine iii) competing for muscarinic receptors and thereby reducing the anticholinergic functional effects of an atypical antipsychotic drug that possesses muscarinic receptor antagonist properties (e.g. olanzapine ).
  • drugs with 5-HT 6 receptor antagonist and an adrenergic ⁇ 2 receptor antagonist properties may also be of benefit.
  • Some atypical antipsychotics also have these benefits.
  • a particular example of a neuroprotective agent useful in the invention is lithium, trade name Priadel, oral tablet or liquid, 100 to IOOOmg titrated to plasma level.
  • neuroleptic refers to drugs which have the effect on cognition and behaviour of antipsychotic drugs that reduce confusion, delusions, hallucinations, and psychomotor agitation in patients with psychoses.
  • neuroleptic agents include, but are not limited to: typical antipsychotic drugs, including phenothiazines, further divided into the aliphatics, piperidines, and piperazines, thioxanthenes (e.g., droperidol), butyrophenones (e.g. haloperidol), dibenzoxazepines (e.g. loxapine), dihydroindolones (e.g.
  • benzisoxazoles e.g. risperidone
  • olanzapine quetiapine
  • osanetant osanetant and ziprasidone
  • a particular example of a neuroleptic agent useful in the invention and its typical route of administration and dosage ranges that are preferred is olanzapine, trade name Zyprexa, oral tablet, 5 to 20 mg.
  • Particularly preferred neuroleptic agents for use in the invention are olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant.
  • the most preferred neuroleptic agent is risperidone.
  • the present invention provides for the use of sabcomeline, in combination with at least one neuroprotective agent and/or neuroleptic agent for the treatment of ADD or ADHD.
  • the treatment may be acute or prophylactic.
  • the present invention provides a method for the treatment of ADD or ADHD comprising administering to a patient in need thereof a pharmaceutically effective amount of sabcomeline in combination with at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADHD, comprising administering to a patient in need thereof a pharmaceutically effective amount of sabcomeline in combination with at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADHD, comprising administering to a patient in need thereof a pharmaceutically effective amount of sabcomeline in combination with at least one neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal antiinflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium.
  • EPA eicosapentaenoic acid
  • DHA docosahexaenoic acid
  • non-steroidal antiinflammatories cyclo-oxygenase-2 (cox-2) inhibitors
  • statins and lithium selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal antiinflammatories, cyclo-oxygenase-2 (cox-2) inhibitor
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADHD, comprising administering to a patient in need thereof a pharmaceutically effective amount of sabcomeline in combination with at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant.
  • sabcomeline in combination with at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant.
  • the present invention provides for a combination of sabcomeline and at least one neuroprotective agent and/or neuroleptic agent, for use in the treatment of ADD or ADHD.
  • the present invention provides for a combination of sabcomeline and at least one neuroprotective agent and/or neuroleptic agent, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • the present invention provides for a combination of sabcomeline and at least one neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal antiinflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • a neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal antiinflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • the present invention provides for a combination of sabcomeline and at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • the present invention provides for the use of sabcomeline for the treatment of ADD or ADH D by adjunctive therapeutic administration to a patient receiving therapeutic administration of at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides a method for the treatment of ADD or ADHD comprising adjunctive therapeutic administration of sabcomeline to a patient receiving therapeutic administration of at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADH D, comprising adjunctive therapeutic administration of sabcomeline to a patient receiving therapeutic administration of at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADHD, comprising adjunctive therapeutic administration of sabcomeline to a patient receiving therapeutic administration of at least one neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal anti-inflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium.
  • EPA eicosapentaenoic acid
  • DHA docosahexaenoic acid
  • non-steroidal anti-inflammatories cyclo-oxygenase-2 (cox-2) inhibitors
  • statins and lithium selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal anti-inflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statin
  • the present invention provides a method for the treatment of cognitive impairment associated with ADD or ADHD, comprising adjunctive therapeutic administration of sabcomeline to a patient receiving therapeutic administration of at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant.
  • sabcomeline to a patient receiving therapeutic administration of at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant.
  • the present invention provides for sabcomeline for use in the treatment of ADD or ADH D by adjunctive therapeutic administration to a patient receiving therapeutic administration of at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides for sabcomeline for use in the treatment of cognitive impairment associated with ADD or ADH D by adjunctive therapeutic administration to a patient receiving therapeutic administration of at least one neuroprotective agent and/or neuroleptic agent.
  • the present invention provides for sabcomeline for use in the treatment of cognitive impairment associated with ADD or ADHD by adjunctive therapeutic administration to a patient receiving therapeutic administration of at least one neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal anti-inflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • Vitamin E eicosapentaenoic acid
  • DHA docosahexaenoic acid
  • non-steroidal anti-inflammatories cyclo-oxygenase-2 (cox-2) inhibitors, statins
  • the present provides for sabcomeline for use in the treatment of cognitive impairment associated with ADD or ADH D by adjunctive therapeutic administration to a patient receiving therapeutic administration of at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant
  • the present invention provides for a kit for use in the treatment of ADD or ADHD, comprising sabcomeline and at least one neuroprotective agent and/or neuroleptic as a combined preparation for separate, simultaneous or sequential administration to a patient.
  • the present invention provides for a kit for use in the treatment of cognitive impairment associated with ADD or ADHD, comprising sabcomeline and at least one neuroprotective agent and/or neuroleptic as a combined preparation for separate, simultaneous or sequential administration to a patient.
  • the present invention provides for a kit for use in the treatment of cognitive impairment associated with ADD or ADHD comprising sabcomeline and at least one neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal anti- inflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • sabcomeline at least one neuroprotective agent selected from Vitamin E, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and non-steroidal anti- inflammatories, cyclo-oxygenase-2 (cox-2) inhibitors, statins and lithium, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • EPA eicosapentaenoic acid
  • DHA docosahexa
  • the present provides for a kit for use in the treatment of cognitive impairment associated with ADD or ADHD comprising sabcomeline and at least one neuroleptic agent selected from olanzapine, risperidone, quetiapine, aripiprazole, haloperidol, clozapine, ziprasidone and osanetant, for use in the treatment of cognitive impairment associated with ADD or ADHD.
  • the cognitive symptoms that may suitably be treated by sabcomeline or combinations comprising sabcomeline include deficits in working memory, attention/vigilance, such as spatial selective attention and attentional asymmetry, executive function (verbal learning and memory, visual learning and memory, speed of processing, reasoning and problem solving) and social cognition.
  • the sabcomeline, neuroprotective agent and/or neuroleptic agent may be administered, by weight, in the ranges 10 ⁇ g to 200 ⁇ g, 0.0 to 5 ⁇ g, and 0.0 to 5 ⁇ g respectively. Such dosages are typically given once every 12 hours for 3 weeks before being re-assessed by a physician.
  • the sabcomeline is administered in the range between 20 ⁇ g to 100 ⁇ g. More preferably, the sabcomeline is administered in the range between 25 ⁇ g to 50 ⁇ g.
  • adjunctive administration is meant the concurrent or overlapping administration of each of the components in the form of separate pharmaceutical compositions or devices.
  • This regime of therapeutic administration of two or more therapeutic agents is referred to generally by those skilled in the art and herein as adjunctive therapeutic administration; it is also known as add-on therapeutic administration.
  • sabcomeline is administered in the form of a pharmaceutical composition, such as a composition for oral, including sub-lingual, intranasal, rectal, topical, parenteral (especially intravenous), or ocular administration.
  • a pharmaceutical composition such as a composition for oral, including sub-lingual, intranasal, rectal, topical, parenteral (especially intravenous), or ocular administration.
  • compositions suitable for the delivery of sabcomeline and methods for their preparation will be readily apparent to those skilled in the art. Such compositions and methods for their preparation may be found, for example, in Remington's Pharmaceutical Sciences, 19th Edition (Mack Publishing Company, 1995).
  • compositions suitable for oral administration include solid formulations such as tablets, capsules containing particulates, liquids, or powders, lozenges (including liquid-filled), chews, multi- and nano-particulates, gels, solid solution, liposome, films, ovules, sprays and liquid formulations.
  • Solid formulations such as tablets, capsules containing particulates, liquids, or powders, lozenges (including liquid-filled), chews, multi- and nano-particulates, gels, solid solution, liposome, films, ovules, sprays and liquid formulations.
  • Liquid formulations include suspensions, solutions, syrups and elixirs. Liquid formulations may also be prepared by the reconstitution of a solid, for example, from a sachet.
  • compositions for oral administration may be formulated to be immediate and/or modified release.
  • Modified release formulations include delayed-, sustained-, pulsed-, controlled-, targeted and programmed release.
  • compositions suitable for parenteral administration include injectable and infusible aqueous or oily blends, mixtures, suspensions, solutions, emulsions and low-viscosity gel preparations.
  • Compositions for parenteral administration may be formulated to be immediate and/or modified release. Modified release formulations include delayed-, sustained-, pulsed-, controlled-, targeted and programmed release.
  • Sabcomeline may also be administered intranasally or by inhalation, typically in the form of a dry powder from a dry powder inhaler, or as an aerosol spray.
  • Sabcomeline may also be administered rectally or vaginally, for example, in the form of a suppository, pessary, or enema.
  • the sabcomeline compositions may also be in the form of fast-dispersing dosage forms such as those described in Expert Opinion in Therapeutic Patents, 1 1 (6), 981 -986, by Liang and Chen (2001 ) and Verma RK et.al . Current Status of Drug Delivery Technologies and Future Directions, Pharmaceutical Technology On-Line, 2001 , 25(2), 1-14.
  • Such dosage forms are also known as oral fast-dissolving, rapid-dissolve, rapid- melt, mouth-dissolving and fast-disintegrating tablet.
  • the composition may be in solid form which melts on contact with the tongue of the patient, for example in the form of disintegrating tablets sold under the trade name ZYDIS ® (RP Scherer, UK).
  • the composition may be in the form of the EFVDAS (effervescent drug absorption system, Elan Corporation), Fast Melt (highly porous microfine matrix tablet, Elan Corporation), Flashdose (floss matrix utilising shearform technology, (Fuisz Technologies, USA), Flashtab (orodispersible multiparticulate tablet, Prographarm, France), Multiflash (fast disintegrating multi-unit, multiparticulate tablet, Prographarm), Orasolv (effervescent dispersed microcapsule tablet, Cima Labs Inc, USA), Wowtab tablets (Yamanouchi Pharma Technologies, USA), LYOC (freeze dried fast dispersing tablets, Farmalyoc, France) or Quicksolve (freeze dried fast dispersing tablets, Janssen Pharamceutica, USA).
  • EFVDAS effervescent drug absorption system, Elan Corporation
  • Fast Melt highly porous microfine matrix tablet, Elan Corporation
  • Flashdose floss matrix utilising shearform technology, (Fuisz Technologies,
  • Suitable formulation technologies may include INDAS (insoluble drug absorption system, Elan Corporation), which utilises a stabilised amorphous form of the drug with enhanced solubility, NanoCrystal technology (Elan Corporation), which utilises nanoparticles of the drug, typically having a particle size of less than 400nm in diameter, or SoftGel (RP Scherer), which utilises a soft gelatin capsule formulation.
  • INDAS insoluble drug absorption system
  • Elan Corporation nanoCrystal technology
  • SoftGel RP Scherer
  • the formulation technologies described herein may advantageously provide more rapid drug dissolution and absorption. For those compositions that disintegrate in the oral cavity, such as beneath the tongue, the rate of absorption may be increased and first- pass metabolism effects reduced.

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Abstract

La présente invention porte sur le traitement du trouble déficitaire de l'attention (ADD), de l'hyperactivité avec déficit de l'attention (ADHD), sur le traitement de la déficience cognitive associée à l'ADD ou à l'ADHD, et sur la sabcomeline, les sels pharmaceutiquement acceptables de celle-ci, et sur des compositions comprenant la sabcomeline destinées à être utilisées dans lesdits traitements.
PCT/GB2009/051644 2008-12-03 2009-12-03 Utilisation de sabcomeline pour le traitement de l'add ou de l'adhd WO2010064047A1 (fr)

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US10238643B2 (en) 2009-07-22 2019-03-26 PureTech Health LLC Methods and compositions for treatment of disorders ameliorated by muscarinic receptor activation
US10265311B2 (en) 2009-07-22 2019-04-23 PureTech Health LLC Methods and compositions for treatment of disorders ameliorated by muscarinic receptor activation
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