RU2019118034A - Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли - Google Patents

Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли Download PDF

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RU2019118034A
RU2019118034A RU2019118034A RU2019118034A RU2019118034A RU 2019118034 A RU2019118034 A RU 2019118034A RU 2019118034 A RU2019118034 A RU 2019118034A RU 2019118034 A RU2019118034 A RU 2019118034A RU 2019118034 A RU2019118034 A RU 2019118034A
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fentanyl
biodegradable
mucoadhesive
polymeric
agent according
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RU2019118034A
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Нирадж Васишт
Эндрю Финн
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БайоДеливери Сейенсиз Интэнэшнл, Инк.
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7007Drug-containing films, membranes or sheets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect

Claims (45)

1. Способ доставки фентанила субъекту, включающий:
введение мукоадгезивного биоразлагаемого средства для трансмукозальной доставки лекарства к слизистой оболочке рта субъекта, при этом указанное средство доставки содержит:
биоразлагаемый мукоадгезивный слой, содержащий фентанил в полимерной диффузионной среде, причем указанная полимерная диффузионная среда имеет pH от 6,5 до 8,5; и
полимерную барьерную среду, прилегающую к указанному мукоадгезивному слою, при этом при применении на буккальной поверхности обеспечивается однонаправленный градиент диффузии фентанила,
при этом общая биодоступность фентанила составляет по меньшей мере 60%; и
при этом доставка фентанила происходит менее чем за 30 минут.
2. Способ по п. 1, в котором общая биодоступность фентанила составляет по меньшей мере 70%.
3. Способ по п. 1, в котором полимерная диффузионная среда содержит по меньшей мере один пленкообразующий водоразлагаемый адгезивный полимер и по меньшей мере один биоразлагаемый полимер.
4. Способ по п. 1, в котором указанная полимерная барьерная среда содержит по меньшей мере один пленкообразующий водоразлагаемый полимер.
5. Способ по п. 1, в котором полимерная дуффузионная среда имеет pH от 7 до 7,5.
6. Способ по п. 1, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит опиоидный антагонист.
7. Способ по п. 1, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит третий слой или покрытие.
8. Способ по п. 1, в котором полимерная дуффузионная среда имеет pH, забуференный до значений от 6,5 до 8,5.
9. Способ по п. 1, в котором полимерная диффузионная среда имеет pH, забуференный до значений от 7 до 7,5.
10. Способ по п. 8, в котором общая биодоступность фентанила составляет по меньшей мере 70%.
11. Способ по п. 8, в котором полимерная диффузионная среда содержит по меньшей мере один пленкообразующий водоразлагаемый адгезивный полимер и по меньшей мере один биоадгезивный полимер.
12. Способ по п. 8, в котором указанная полимерная барьерная среда содержит по меньшей мере один пленкообразующий водоразлагаемый полимер.
13. Способ по п. 8, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит опиоидный антагонист.
14. Способ по п. 8, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит третий слой или покрытие.
15. Средство для доставки фентанила субъекту, содержащее:
биоразлагаемый мукоадгезивный слой, содержащий фентанил в полимерной диффузионной среде, причем указанная полимерная диффузионная среда имеет рН от 6,5 до 8,5, и
полимерную барьерную среду, прилегающую к указанному мукоадгезивному слою, при этом при применении на буккальной поверхности субъекта обеспечивается однонаправленный градиент диффузии фентанила и
причем при применении на буккальной поверхности общая биодоступность фентанила составляет по меньшей мере 60%; и
при этом доставка фентанила происходит менее чем за 30 минут.
16. Средство по п. 15, в котором общая биодоступность фентанила составляет по меньшей мере 70%.
17. Средство по п. 15, в котором полимерная дуффузионная среда содержит по меньшей мере один пленкообразующий водоразлагаемый полимер и по меньшей мере один биоразлагаемый полимер.
18. Средство по п. 15, в котором указанная полимерная барьерная среда содержит по меньшей мере один пленкообразующий водоразлагаемый полимер.
19. Средство по п. 15, в котором полимерная дуффузионная среда имеет pH от 7 до 7,5.
20. Средство по п. 15, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит опиоидный антагонист.
21. Средство по п. 15, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит третий слой или покрытие.
22. Средство по п. 15, в котором полимерная дуффузионная среда имеет pH, забуференный до значений от 6,5 до 8,5.
23. Средство по п. 15, в котором полимерная диффузионная среда имеет pH, забуференный до значений от 7 до 7,5.
24. Средство по п. 22, в котором общая биодоступность фентанила составляет по меньшей мере 70%.
25. Средство по п. 22, в котором полимерная диффузионная среда содержит по меньшей мере один пленкообразующий водоразлагаемый адгезивный полимер и по меньшей мере один биоразлагаемый полимер.
26. Средство по п. 22, в котором указанная полимерная барьерная среда содержит по меньшей мере один пленкообразующий водоразлагаемый полимер.
27. Средство по п. 22, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит опиоидный антагонист.
28. Средство по п. 27, в котором указанный опиоидный антагонист представляет собой налоксон.
29. Средство по п. 22, в котором указанное мукоадгезивное биоразлагаемое средство для трансмукозальной доставки лекарства дополнительно содержит третий слой или покрытие.
30. Способ лечения боли, включающий:
адгезивное прикрепление мукоадгезивного биоразлагаемого средства доставки лекарства к буккальной поверхности субъекта, при этом указанное средство доставки содержит:
биоразлагаемый мукоадгезивный слой, содержащий терапевтически эффективное для лечения боли количество фентанила в полимерной диффузионной среде, причем указанная полимерная диффузионная среда имеет pH, забуференный до значений от 6,5 до 8,5, и
полимерную барьерную среду, прилегающую к указанному мукоадгезивному слою, при этом при применении на буккальной поверхности обеспечивается однонаправленный градиент диффузии фентанила,
при этом указанная трансмукозальная доставка фентанила по меньшей мере на 50% осуществляется за счет прямой трансбуккальной абсорбции,
при этом общая биодоступность фентанила составляет по меньшей мере 70%; и
при этом доставка фентанила происходит менее чем за 30 минут.
RU2019118034A 2006-07-21 2019-06-10 Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли RU2019118034A (ru)

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US83272506P 2006-07-21 2006-07-21
US83272606P 2006-07-21 2006-07-21
US60/832,725 2006-07-21
US60/832,726 2006-07-21
US83950406P 2006-08-23 2006-08-23
US60/839,504 2006-08-23

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RU2009106177/15A RU2504377C2 (ru) 2006-07-21 2007-07-23 Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли
RU2013141051/15A RU2013141051A (ru) 2006-07-21 2013-09-06 Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли
RU2019118034A RU2019118034A (ru) 2006-07-21 2019-06-10 Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли

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RU2013141051/15A RU2013141051A (ru) 2006-07-21 2013-09-06 Способ трансмукозальной доставки лекарства, средство трансмукозальной доставки лекарства (варианты) и способ лечения боли

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US (12) US20100015183A1 (ru)
EP (3) EP2054031B1 (ru)
JP (2) JP5448814B2 (ru)
KR (2) KR101230804B1 (ru)
CN (2) CN101511337B (ru)
AU (1) AU2007275581B2 (ru)
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CA (1) CA2658585C (ru)
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IL (2) IL196529A (ru)
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RU (3) RU2504377C2 (ru)
SI (1) SI2054031T1 (ru)
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