WO2017142442A1 - Compositions pharmaceutiques pour la prévention et le traitement des troubles du sommeil - Google Patents

Compositions pharmaceutiques pour la prévention et le traitement des troubles du sommeil Download PDF

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Publication number
WO2017142442A1
WO2017142442A1 PCT/RU2017/000077 RU2017000077W WO2017142442A1 WO 2017142442 A1 WO2017142442 A1 WO 2017142442A1 RU 2017000077 W RU2017000077 W RU 2017000077W WO 2017142442 A1 WO2017142442 A1 WO 2017142442A1
Authority
WO
WIPO (PCT)
Prior art keywords
melatonin
sleep
composition
doxylamine succinate
insomnia
Prior art date
Application number
PCT/RU2017/000077
Other languages
English (en)
Russian (ru)
Inventor
Владимир Викторович НЕСТЕРУК
Кирилл Константинович Сыров
Original Assignee
Общество С Ограниченной Ответственностью "Валента-Интеллект"
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 Общество С Ограниченной Ответственностью "Валента-Интеллект" filed Critical Общество С Ограниченной Ответственностью "Валента-Интеллект"
Priority to KR1020187023412A priority Critical patent/KR20180101539A/ko
Priority to CN201780009565.8A priority patent/CN108697645A/zh
Priority to BR112018016725A priority patent/BR112018016725A2/pt
Priority to EA201891647A priority patent/EA201891647A1/ru
Priority to MX2018009921A priority patent/MX2018009921A/es
Publication of WO2017142442A1 publication Critical patent/WO2017142442A1/fr
Priority to HK18114767.2A priority patent/HK1255631A1/zh

Links

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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy

Definitions

  • Insomnia is a clinical syndrome characterized by the presence of repeated disturbances in the initiation, duration, totality and / or quality of sleep that occur despite the presence of a sufficient amount of time and conditions for sleep. This syndrome is manifested by violations of daytime activity of various kinds.
  • This disorder manifests itself in various forms: fatigue, impaired attention, concentration or remembering information, social dysfunction, mood disorders, irritability, daytime sleepiness, decreased motivation and initiative, a tendency to mistakes at the wheel and at work, muscle tension, headache, disorders of the gastrointestinal tract, anxiety about the state of your sleep.
  • a tendency to mistakes at the wheel and at work muscle tension, headache, disorders of the gastrointestinal tract, anxiety about the state of your sleep.
  • Doxylamine succinate is more effective in presomnic disorders, i.e. problems preceding the onset of sleep. This means that intrasomnic disorders are distributed as follows:
  • melatonin is a neuropeptide synthesized by the pineal gland and having a unique effect on the human and animal organisms. Melatonin is involved in the organization of daily periodism and in the regulation of cyclic processes, acting as an intermediary between the pacemaker mechanism of suprachiasmatic nuclei (SCN) and peripheral organs.
  • SCN suprachiasmatic nuclei
  • the pineal gland along with the SCN of the hypothalamus is included in the so-called biological clock system of the body, which plays a key role in the mechanisms of “counting internal time” and aging [Arushanyan EB, 2005; Anisimov V.N., 2007].
  • melatonin is the only therapeutically active agent in an amount of from 0.0025 to 50 mg in a drug of the same purpose.
  • melatonin acts as a sleep initiator, in combination with various active substances selected from anxiolytics, antidepressants, hypnotics (both benzodiazepines and nonbenzodiazepines), sedatives, antihypertensives, analgesics, antipsychotic drugs, dopaminergic agonists, anti-anxiolytic drugs.
  • Doxylamine succinate is not mentioned among these agents. It is also necessary to state that, as a sleep initiator, melatonin does not have such a pronounced and effective agent.
  • Excipients used in solid dosage forms may further include colorants and pigments, taste masking agents, flavors, sweeteners and adsorbents.
  • Diluents are used to increase the size of the tablet when the amount of active drug substance is not high. Diluents include lactose, in the form of alpha-lactose or beta-lactose.
  • lactose monohydrate is about 20-40% by weight of the composition
  • microcrystalline cellulose is about 10-15%
  • gelatinized starch is about 5-10%
  • sodium carboxymethyl cellulose is about 1-5%
  • polyvinylpyrrolidone is about 1-5%
  • magnesium stearate is from about 0.1-2.0%.
  • Melatonin in an amount of 2 mg mixed with sifted hydroxypropyl methylcellulose (HPMC) 100 mg, a complex compound of microcrystalline cellulose (MCC) 50 mg and silicon dioxide 2 mg are loaded into the mixer based on the dosage in a tablet.
  • the mixture of dry components is mixed for about 10 minutes (the rotation speed of the main mixer is 80 + 1 10 rpm.
  • the sieved magnesium stearate 1 mg is added to the mixture of dry components and mixing is continued for 3 minutes (rotation speed of the main mixer 80 + 1 10 r / min)
  • doxylamine succinate in the amount of 15 mg is added to the tablet mass, further mixed and discharged from the mixer, then transferred to the tabletting step. Tableting is carried out on a RTM-41 M rotary press using round punches (deep sphere).
  • Core tablets are sent to the film-coating step. Apply a film coating to the tablet cores on a BGB-10 apparatus using an aqueous suspension of OPADRY II powder with a mass concentration of 19% ⁇ 1%.
  • Magnesium stearate is sieved through an ASTM # 60 sieve shaker.
  • the pre-compacted mixture was transferred to a roller press, which was put into operation.
  • the lower and upper punches 8 * 13 mm are mounted on a tablet press to determine the limit of the corresponding compressive strength.

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne la médecine et plus particulièrement et l'industrie chimique et pharmaceutique et porte sur des médicaments utilisés pour le traitement des troubles du sommeil. La composition pharmaceutique pour déclencher et maintenir le processus de sommeil et assurer la prévention chez les animaux et l'humain des états qui s'accompagnent de troubles de sommeil de différente nature, caractérisée en ce qu'elle comprend du succinate de Doxilamine et de la mélatonine à libération prolongée dans des quantités efficaces. Les résultats techniques sont les suivants : effets thérapeutiques synergiques, filiation biologique et effets secondaires réduits.
PCT/RU2017/000077 2016-02-18 2017-02-16 Compositions pharmaceutiques pour la prévention et le traitement des troubles du sommeil WO2017142442A1 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
KR1020187023412A KR20180101539A (ko) 2016-02-18 2017-02-16 수면장애를 예방 및 치료하기 위한 약제학적 조성물
CN201780009565.8A CN108697645A (zh) 2016-02-18 2017-02-16 用于预防和治疗睡眠障碍的药物组合物
BR112018016725A BR112018016725A2 (pt) 2016-02-18 2017-02-16 composição farmacêutica para prevenir e tratar transtornos do sono
EA201891647A EA201891647A1 (ru) 2016-02-18 2017-02-16 Фармацевтическая композиция для профилактики и лечения нарушений сна
MX2018009921A MX2018009921A (es) 2016-02-18 2017-02-16 Composición farmacéutica para prevenir y tratar trastornos del sueño.
HK18114767.2A HK1255631A1 (zh) 2016-02-18 2018-11-19 用於預防和治療睡眠障礙的藥物組合物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2016105535A RU2620855C1 (ru) 2016-02-18 2016-02-18 Фармацевтическая композиция для профилактики и лечения нарушений сна
RU2016105535 2016-02-18

Publications (1)

Publication Number Publication Date
WO2017142442A1 true WO2017142442A1 (fr) 2017-08-24

Family

ID=59032329

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2017/000077 WO2017142442A1 (fr) 2016-02-18 2017-02-16 Compositions pharmaceutiques pour la prévention et le traitement des troubles du sommeil

Country Status (9)

Country Link
KR (1) KR20180101539A (fr)
CN (1) CN108697645A (fr)
BR (1) BR112018016725A2 (fr)
CL (1) CL2018002337A1 (fr)
EA (1) EA201891647A1 (fr)
HK (1) HK1255631A1 (fr)
MX (1) MX2018009921A (fr)
RU (1) RU2620855C1 (fr)
WO (1) WO2017142442A1 (fr)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014138162A1 (fr) * 2013-03-05 2014-09-12 Requis Pharmaceuticals Inc. Préparations pour le traitement de troubles respiratoires liés au sommeil

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050164987A1 (en) * 2003-12-24 2005-07-28 Barberich Timothy J. Melatonin combination therapy for improving sleep quality
US9700548B2 (en) * 2011-06-09 2017-07-11 Requis Pharmaceuticals Inc. Antihistamines combined with dietary supplements for improved health
FR3000896B1 (fr) * 2013-01-14 2016-08-26 Philippe Perovitch Forme galenique pour l'administration de principe(s) actif(s) permettant l'induction acceleree du sommeil et/ou le traitement des troubles du sommeil

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014138162A1 (fr) * 2013-03-05 2014-09-12 Requis Pharmaceuticals Inc. Préparations pour le traitement de troubles respiratoires liés au sommeil

Also Published As

Publication number Publication date
KR20180101539A (ko) 2018-09-12
MX2018009921A (es) 2018-11-09
EA201891647A1 (ru) 2018-12-28
CN108697645A (zh) 2018-10-23
RU2620855C1 (ru) 2017-05-30
BR112018016725A2 (pt) 2019-04-30
HK1255631A1 (zh) 2019-08-23
CL2018002337A1 (es) 2018-11-30

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