RU2008102651A - Замедленное высвобождение противоинфекционных агентов - Google Patents
Замедленное высвобождение противоинфекционных агентов Download PDFInfo
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- RU2008102651A RU2008102651A RU2008102651/15A RU2008102651A RU2008102651A RU 2008102651 A RU2008102651 A RU 2008102651A RU 2008102651/15 A RU2008102651/15 A RU 2008102651/15A RU 2008102651 A RU2008102651 A RU 2008102651A RU 2008102651 A RU2008102651 A RU 2008102651A
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- lipid
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- infective
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- amikacin
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- 230000002924 anti-infective effect Effects 0.000 title claims abstract 10
- 150000002632 lipids Chemical class 0.000 claims abstract 59
- 239000002626 anti infective formulation Substances 0.000 claims abstract 29
- 239000000203 mixture Substances 0.000 claims abstract 23
- 238000009472 formulation Methods 0.000 claims abstract 21
- 229960005475 antiinfective agent Drugs 0.000 claims abstract 17
- 239000004599 antimicrobial Substances 0.000 claims abstract 17
- 229960004821 amikacin Drugs 0.000 claims abstract 7
- LKCWBDHBTVXHDL-RMDFUYIESA-N amikacin Chemical compound O([C@@H]1[C@@H](N)C[C@H]([C@@H]([C@H]1O)O[C@@H]1[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O1)O)NC(=O)[C@@H](O)CCN)[C@H]1O[C@H](CN)[C@@H](O)[C@H](O)[C@H]1O LKCWBDHBTVXHDL-RMDFUYIESA-N 0.000 claims abstract 7
- 239000002502 liposome Substances 0.000 claims abstract 5
- 150000003904 phospholipids Chemical class 0.000 claims abstract 5
- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 claims abstract 4
- 229930182566 Gentamicin Natural products 0.000 claims abstract 4
- 229940126575 aminoglycoside Drugs 0.000 claims abstract 4
- 229960002518 gentamicin Drugs 0.000 claims abstract 4
- 239000012678 infectious agent Substances 0.000 claims abstract 4
- 229960000707 tobramycin Drugs 0.000 claims abstract 4
- NLVFBUXFDBBNBW-PBSUHMDJSA-N tobramycin Chemical compound N[C@@H]1C[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N NLVFBUXFDBBNBW-PBSUHMDJSA-N 0.000 claims abstract 4
- 150000003431 steroids Chemical class 0.000 claims abstract 3
- 239000003795 chemical substances by application Substances 0.000 claims abstract 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 6
- KILNVBDSWZSGLL-KXQOOQHDSA-N 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCC KILNVBDSWZSGLL-KXQOOQHDSA-N 0.000 claims 4
- 229930182558 Sterol Natural products 0.000 claims 3
- 235000012000 cholesterol Nutrition 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 230000002685 pulmonary effect Effects 0.000 claims 3
- 150000003432 sterols Chemical class 0.000 claims 3
- 235000003702 sterols Nutrition 0.000 claims 3
- 241000186365 Mycobacterium fortuitum Species 0.000 claims 2
- 241001135516 Burkholderia gladioli Species 0.000 claims 1
- 241000020731 Burkholderia multivorans Species 0.000 claims 1
- 241001136175 Burkholderia pseudomallei Species 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 241001600125 Delftia acidovorans Species 0.000 claims 1
- 241000588914 Enterobacter Species 0.000 claims 1
- 241000588724 Escherichia coli Species 0.000 claims 1
- 241000606790 Haemophilus Species 0.000 claims 1
- 241000588748 Klebsiella Species 0.000 claims 1
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims 1
- 241001502334 Mycobacterium avium complex bacterium Species 0.000 claims 1
- 241000187478 Mycobacterium chelonae Species 0.000 claims 1
- 241000186364 Mycobacterium intracellulare Species 0.000 claims 1
- 241000186363 Mycobacterium kansasii Species 0.000 claims 1
- 241000187492 Mycobacterium marinum Species 0.000 claims 1
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 1
- 241000187917 Mycobacterium ulcerans Species 0.000 claims 1
- 241000187494 Mycobacterium xenopi Species 0.000 claims 1
- 241000589516 Pseudomonas Species 0.000 claims 1
- 241000589540 Pseudomonas fluorescens Species 0.000 claims 1
- 241000589776 Pseudomonas putida Species 0.000 claims 1
- 241000607720 Serratia Species 0.000 claims 1
- 241000736110 Sphingomonas paucimobilis Species 0.000 claims 1
- 241000295644 Staphylococcaceae Species 0.000 claims 1
- 206010041925 Staphylococcal infections Diseases 0.000 claims 1
- 241000191967 Staphylococcus aureus Species 0.000 claims 1
- 241000193998 Streptococcus pneumoniae Species 0.000 claims 1
- 241000607734 Yersinia <bacteria> Species 0.000 claims 1
- 208000015688 methicillin-resistant staphylococcus aureus infectious disease Diseases 0.000 claims 1
- 229960003085 meticillin Drugs 0.000 claims 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 claims 1
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
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Abstract
1. Липидная противоинфекционная препаративная форма, включающая липидную препаративную форму и противоинфекционный агент, в которой соотношение липида и противоинфекционного агента составляет 1:1 или менее. ! 2. Липидная противоинфекционная препаративная форма по п. 1, в которой соотношение липида и противоинфекционного агента составляет менее 0,75:1. ! 3. Липидная противоинфекционная препаративная форма по п. 1, в которой соотношение липида и противоинфекционного агента составляет менее 0,5:1. ! 4. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой аминогликозид. ! 5. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой аминогликозид, выбранный из следующих агентов: амикацина, гентамицина или тобрамицина. ! 6. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой амикацин. ! 7. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой гентамицин. ! 8. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой тобрамицин. ! 9. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма представляет собой липосому. ! 10. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает фосфолипид. ! 11. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает стероид. ! 12. Липидная противоинфекционная препаративная
Claims (23)
1. Липидная противоинфекционная препаративная форма, включающая липидную препаративную форму и противоинфекционный агент, в которой соотношение липида и противоинфекционного агента составляет 1:1 или менее.
2. Липидная противоинфекционная препаративная форма по п. 1, в которой соотношение липида и противоинфекционного агента составляет менее 0,75:1.
3. Липидная противоинфекционная препаративная форма по п. 1, в которой соотношение липида и противоинфекционного агента составляет менее 0,5:1.
4. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой аминогликозид.
5. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой аминогликозид, выбранный из следующих агентов: амикацина, гентамицина или тобрамицина.
6. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой амикацин.
7. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой гентамицин.
8. Липидная противоинфекционная препаративная форма по п. 1, в которой противоинфекционный агент представляет собой тобрамицин.
9. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма представляет собой липосому.
10. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает фосфолипид.
11. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает стероид.
12. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает стерол.
13. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает дипальмитоилфосфатидилхолин (DPPC).
14. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает холестерин.
15. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает фосфолипид и стероид.
16. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает фосфолипид и стерол.
17. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма включает DPPC и холестерин.
18. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная препаративная форма представляет собой липосому, а противоинфекционный агент представляет собой амикацин.
19. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная композиция представляет собой липосому, противоинфекционный агент представляет собой амикацин, а липидная препаративная форма включает в себя фосфолипид и стерол.
20. Липидная противоинфекционная препаративная форма по п. 1, в которой липидная композиция представляет собой липосому, противоинфекционный агент представляет собой амикацин, а липидная препаративная форма включает DPPC и холестерин.
21. Способ лечения легочной инфекции у пациента, включающий введение пациенту терапевтически эффективного количества липидной противоинфекционной препаративной формы по п.1.
22. Способ по п.21, в котором легочная инфекция представляет собой рseudomonas, P.aeruginosa, P.paucimobilis, P.putida, P.fluorescens и P.acidovorans, стафилококки, резистентные к метициллину Staphylococcus aureus (MRSA), стрептококки, Streptococcus pneumoniae, Escherichia coli, Klebsiella, Enterobacter, Serratia, Haemophilus, Yersinia pesos, Burkholderia pseudomallei, B.cepaсia, B.gladioli, B.multivorans, B.vietnamiensis, Mycobacterium tuberculosis, комплекс M.avium (MAC), M.avium, M.intracellulare, M.kansasii, M.xenopi, M.marinum, M.ulcerans, комплексом M.fortuitum, M.fortuitum или M.chelonei.
23. Способ лечения легочной инфекции у пациента, вызванной муковисцидозом, включающий введение пациенту терапевтически эффективного количества липидной противоинфекционной препаративной формы по п. 1.
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