RU2003102615A - COMPOSITIONS AND COMPOUNDS FOR THE DELIVERY OF ACTIVE AGENTS - Google Patents

COMPOSITIONS AND COMPOUNDS FOR THE DELIVERY OF ACTIVE AGENTS

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Publication number
RU2003102615A
RU2003102615A RU2003102615/04A RU2003102615A RU2003102615A RU 2003102615 A RU2003102615 A RU 2003102615A RU 2003102615/04 A RU2003102615/04 A RU 2003102615/04A RU 2003102615 A RU2003102615 A RU 2003102615A RU 2003102615 A RU2003102615 A RU 2003102615A
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RU
Russia
Prior art keywords
active agent
insulin
biologically active
hormone
interferon
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RU2003102615/04A
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Russian (ru)
Other versions
RU2326110C2 (en
Inventor
Джон Дж. ВЕЙДНЕР
Брюс Ф. ВАРИАНО
Шингай МАДЖЕРУ
Сатай БХАНКАРКАР
Вильям Е. БЭЙ
Лин ШИФИЛДЗ
Original Assignee
Емисфир Текнолоджис, Инк.
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Application filed by Емисфир Текнолоджис, Инк. filed Critical Емисфир Текнолоджис, Инк.
Publication of RU2003102615A publication Critical patent/RU2003102615A/en
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Publication of RU2326110C2 publication Critical patent/RU2326110C2/en

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Claims (20)

1. Соединение формулы1. The compound of the formula
Figure 00000001
Figure 00000001
 и его соли.and its salts. 2. Соединение, содержащее (А) активный агент и (Б)соединение формулы2. A compound containing (A) an active agent and (B) a compound of the formula
Figure 00000002
Figure 00000002
 его соль или их смесь.its salt or a mixture thereof. 3. Соединение по п.2, отличающееся тем, что активный агент выбран из группы, включающей биологически активный агент, химически активный агент и их сочетание.3. The compound according to claim 2, characterized in that the active agent is selected from the group comprising a biologically active agent, a chemically active agent, and a combination thereof. 4. Соединение по п.3, отличающееся тем, что биологически активный агент содержит по меньшей мере один белок, полипетптид, пептид, гормон, полисахарид, мукополисахарид, углевод или липид.4. The compound according to claim 3, characterized in that the biologically active agent contains at least one protein, polypetitis, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate or lipid. 5. Соединение по п.4, отличающееся тем, что биологически активный агент выбран из группы, включающей гормоны роста, гормоны роста человека, рекомбинантные гормоны роста человека, гормоны роста быка, гормоны роста свиньи, гормоны, выделяющие гормоны роста, интерфероны, α-интерферон, β-интерферон, γ-интерферон, интерлейкин-1, интрелейкин-2, инсулин, инсулин свиньи, инсулин быка, инсулин человека, рекомбинантный инсулин человека, инсулиноподобный фактор-1 роста, гепарин, нефракционированный гепарин, гепариноиды, дерматаны, хондроитины, гепарин с низкой молекулярной массой, гепарин с очень низкой молекулярной массой и гепарин со сверхнизкой молекулярной массой, кальцитонин, кальцитонин лосося, кальцитонин угря, кальцитонин человека, эритропоэтин (ЕРО), предсердный naturetic фактор, антигены, моноклональные антитела, соматостатин, ингибиторы протеазы, адренокортикотропин, гормон, выделяющий гонадотропин, окситоцин, гормон, выделяющий лейтинизирующий гормон, гормон, стимулирующий фолликулы, глюкоцереброзидазу, тромбопоэтин, филграстим, простагландины, циклоспорин, вазопрессин, кромолин натрия, натриевый хромогликат, двунатриевый хромогликат, ванкомицин, десферриоксамин, паратироидный гормон, фрагменты паратироидного гормона, противомикробные, противогрибковые агенты, витамины, аналоги, фрагменты, миметики или производные этих соединений, модифицированные полиэтиленгликолем, а также их любые сочетания.5. The compound according to claim 4, characterized in that the biologically active agent is selected from the group comprising growth hormones, human growth hormones, recombinant human growth hormones, bull growth hormones, pig growth hormones, hormones that secrete growth hormones, interferons, α- interferon, β-interferon, γ-interferon, interleukin-1, intreleukin-2, insulin, pig insulin, bovine insulin, human insulin, recombinant human insulin, insulin-like growth factor-1, heparin, unfractionated heparin, heparinoids, dermatans, chondroitins heparin n low molecular weight, very low molecular weight heparin and ultra low molecular weight heparin, calcitonin, salmon calcitonin, eel calcitonin, human calcitonin, erythropoietin (EPO), atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, protease inhibitors, adrenocortin secreting gonadotropin, oxytocin, hormone secreting leutinizing hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoietin, filgrastim, prostaglandins, cyclosporine, vasopressin, cromol sodium in, sodium chromoglycate, disodium chromoglycate, vancomycin, desferrioxamine, parathyroid hormone, fragments of parathyroid hormone, antimicrobial, antifungal agents, vitamins, analogues, fragments, mimetics or derivatives of these compounds, modified with polyethylene glycol, as well as any combinations thereof. 6. Соединение по п.3, отличающееся тем, что биологически активный агент включает инсулин, гормон роста человека, интерферон, кромолин натрия или их сочетание.6. The compound according to claim 3, characterized in that the biologically active agent includes insulin, human growth hormone, interferon, cromolin sodium, or a combination thereof. 7. Соединение по п.3, отличающееся тем, что биологически активный агент включает инсулин.7. The compound according to claim 3, characterized in that the biologically active agent includes insulin. 8. Соединение по п.3, отличающееся тем, что биологически активный агент включает интерферон.8. The compound according to claim 3, characterized in that the biologically active agent comprises interferon. 9. Стандартная дозированная форма, содержащая (А) состав по п.2 и (Б) (а)наполнитель, (б)разбавитель, (в) дезинтегратор, (г) смазочное вещество, (д) пластификатор, (е)краситель, (ж) дозировочный носитель или (з) их любое сочетание.9. A standard dosage form containing (A) the composition according to claim 2 and (B) (a) a filler, (b) a diluent, (c) a disintegrant, (d) a lubricant, (e) a plasticizer, (e) a dye, (g) a dosage carrier; or (h) any combination thereof. 10. Стандартная дозированная форма по п.9, отличающаяся тем, что активный агент выбран из группы, включающей биологически активный агент, химически активный агент и их сочетание.10. The unit dosage form of claim 9, wherein the active agent is selected from the group comprising a biologically active agent, a chemically active agent, and a combination thereof. 11. Стандартная дозированная форма по п.10, отличающаяся тем, что биологически активный агент содержит по меньшей мере один белок, полипептид, пептид, гормон, полисахарид, мукополисахарид, углевод или липид.11. The unit dosage form of claim 10, wherein the biologically active agent contains at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate or lipid. 12. Стандартная дозированная форма по п.10, отличающаяся тем, что биологически активный агент выбран из группы, включающей гормоны роста, гормоны роста человека, рекомбинантные гормоны роста человека, гормоны роста быка, гормоны роста свиньи, гормоны, выделяющие гормоны роста, интерфероны, α-интерферон, β-интерферон, γ-интерферон, интерлейкин-1, интрелейкин-2, инсулин, инсулин быка, инсулин свиньи, инсулин человека, рекомбинантный инсулин человека, инсулиноподобный фактор-1 роста, гепарин, нефракционированный гепарин, гепариноиды, дерматаны, хондроитины, гепарин с низкой молекулярной массой, гепарин с очень низкой молекулярной массой и гепарин со сверхнизкой молекулярной массой, кальцитонин, кальцитонин лосося, кальцитонин угря, кальцитонин человека, эритропоэтин, предсердный naturetic фактор, антигены, моноклональные антитела, соматостатин, ингибиторы протеазы, адренокортикотропин, гормон, выделяющий гонадотропин, окситоцин, гормон, выделяющий лейтинизирующий гормон, гормон, стимулирующий фолликулы, глюкоцереброзидазу, тромбопоэтин, филграстим, простагландины, циклоспорин, вазопрессин, кромолин натрия, натриевый хромогликат, двунатриевый хромогликат, ванкомицин, десферриоксамин, паратироидный гормон, фрагменты паратироидного гормона, противомикробные, противогрибковые агенты, витамины, аналоги, фрагменты, миметики или производные этих соединений, модифицированные полиэтиленгликолем, а также их любые сочетания.12. The unit dosage form of claim 10, wherein the biologically active agent is selected from the group consisting of growth hormones, human growth hormones, recombinant human growth hormones, bull growth hormones, pig growth hormones, hormones secreting growth hormones, interferons, α-interferon, β-interferon, γ-interferon, interleukin-1, intreleukin-2, insulin, bovine insulin, human insulin, human insulin, recombinant human insulin, insulin-like growth factor-1, heparin, unfractionated heparin, heparinoids, dermatans, ho ndroitins, heparin with a low molecular weight, heparin with a very low molecular weight and heparin with an ultra low molecular weight, calcitonin, salmon calcitonin, eel calcitonin, human calcitonin, erythropoietin, atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, inhibitors, inhibitors gonadotropin releasing hormone, oxytocin, leutinizing hormone releasing hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoietin, filgrastim, prostaglandins, cyclosporin, va opressin, cromolyn sodium, sodium cromoglycate, disodium cromoglycate, vancomycin, desferrioxamine, parathyroid hormone, fragments of parathyroid hormone, antimicrobials, antifungal agents, vitamins, analogs, fragments, mimetics or derivatives of these compounds modified with polyethylene glycol, and any combination thereof. 13. Стандартная дозированная форма по п.10, отличающаяся тем, что биологически активный агент включает инсулин, гормон роста человека, интерферон, кромолин натрия или их сочетание.13. The unit dosage form of claim 10, wherein the biologically active agent comprises insulin, human growth hormone, interferon, cromolin sodium, or a combination thereof. 14. Стандартная дозированная форма по п.9, отличающаяся тем, что биологически активный агент включает инсулин.14. The unit dosage form of claim 9, wherein the biologically active agent comprises insulin. 15. Стандартная дозированная форма по п.9, отличающаяся тем, что биологически активный агент включает интерферон.15. The standard dosage form according to claim 9, characterized in that the biologically active agent comprises interferon. 16. Стандартная дозированная форма по п.9, отличающаяся тем, что стандартная дозированная форма имеет форму таблетки, капсулы, частиц, порошка, саше или жидкости.16. The unit dosage form of claim 9, wherein the unit dosage form is in the form of a tablet, capsule, particle, powder, sachet or liquid. 17. Стандартная дозированная форма по п.9, отличающаяся тем, что дозирующий носитель представляет собой жидкость, выбранную из группы, включающей воду, 25%-ный водный пропиленгликоль, фосфатный буфер, 1,2-пропандиол, этанол, а также их любое сочетание.17. The standard dosage form according to claim 9, characterized in that the dosage carrier is a liquid selected from the group consisting of water, 25% aqueous propylene glycol, phosphate buffer, 1,2-propanediol, ethanol, as well as any combination thereof . 18. Способ введения биологически активного агента животному, которое нуждается в этом агенте, при этом указанный способ включает пероральное введение указанному животному соединения по п.3.18. A method of administering a biologically active agent to an animal that needs this agent, said method comprising orally administering to said animal a compound according to claim 3. 19. Способ получения состава, включающий смешивание (A) по меньшей мере одного активного агента, (Б) соединения по п.1 и, (B) возможно, дозировочного носителя.19. A method of obtaining a composition comprising mixing (A) at least one active agent, (B) a compound according to claim 1, and (B) optionally a dosage carrier. 20. Способ лечения заболевания, включающий введение соединения по п.3 животному, которое нуждается в этом соединении.20. A method of treating a disease, comprising administering a compound of claim 3 to an animal that needs the compound.
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