TWI455708B - 經由醫藥裝置輸送高親脂性劑 - Google Patents

經由醫藥裝置輸送高親脂性劑 Download PDF

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TWI455708B
TWI455708B TW95110143A TW95110143A TWI455708B TW I455708 B TWI455708 B TW I455708B TW 95110143 A TW95110143 A TW 95110143A TW 95110143 A TW95110143 A TW 95110143A TW I455708 B TWI455708 B TW I455708B
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agent
lipophilic
lipophilic agent
stent
medical device
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TW200722064A (en
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Keith R Cromack
John L Toner
Sandra E Burke
Richard W Krasula
Lewis B Schwartz
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Abbott Lab
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L31/00Materials for other surgical articles, e.g. stents, stent-grafts, shunts, surgical drapes, guide wires, materials for adhesion prevention, occluding devices, surgical gloves, tissue fixation devices
    • A61L31/08Materials for coatings
    • A61L31/10Macromolecular materials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F2/00Filters implantable into blood vessels; Prostheses, i.e. artificial substitutes or replacements for parts of the body; Appliances for connecting them with the body; Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
    • A61F2/02Prostheses implantable into the body
    • A61F2/04Hollow or tubular parts of organs, e.g. bladders, tracheae, bronchi or bile ducts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F2/00Filters implantable into blood vessels; Prostheses, i.e. artificial substitutes or replacements for parts of the body; Appliances for connecting them with the body; Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
    • A61F2/82Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61L31/00Materials for other surgical articles, e.g. stents, stent-grafts, shunts, surgical drapes, guide wires, materials for adhesion prevention, occluding devices, surgical gloves, tissue fixation devices
    • A61L31/14Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
    • A61L31/16Biologically active materials, e.g. therapeutic substances
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F2/00Filters implantable into blood vessels; Prostheses, i.e. artificial substitutes or replacements for parts of the body; Appliances for connecting them with the body; Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
    • A61F2/02Prostheses implantable into the body
    • A61F2/04Hollow or tubular parts of organs, e.g. bladders, tracheae, bronchi or bile ducts
    • A61F2002/044Oesophagi or esophagi or gullets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F2/00Filters implantable into blood vessels; Prostheses, i.e. artificial substitutes or replacements for parts of the body; Appliances for connecting them with the body; Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
    • A61F2/02Prostheses implantable into the body
    • A61F2/04Hollow or tubular parts of organs, e.g. bladders, tracheae, bronchi or bile ducts
    • A61F2002/047Urethrae
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F2250/00Special features of prostheses classified in groups A61F2/00 - A61F2/26 or A61F2/82 or A61F9/00 or A61F11/00 or subgroups thereof
    • A61F2250/0058Additional features; Implant or prostheses properties not otherwise provided for
    • A61F2250/0067Means for introducing or releasing pharmaceutical products into the body
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/20Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials
    • A61L2300/216Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials with other specific functional groups, e.g. aldehydes, ketones, phenols, quaternary phosphonium groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/20Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials
    • A61L2300/22Lipids, fatty acids, e.g. prostaglandins, oils, fats, waxes
    • A61L2300/222Steroids, e.g. corticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/60Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a special physical form
    • A61L2300/606Coatings

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Claims (102)

  1. 一種用於輸送親脂性劑之系統,其包含:一醫藥裝置;能穿透體內腔之第一親脂性劑,其中該第一親脂性劑之傳遞係數達至至少約5,000(μg/mL)-1 之量,其中該第一親脂性劑與該醫藥裝置結合,其中該醫藥裝置可被置放在該體內腔鄰近處;且該醫藥裝置可將治療有效量之該第一親脂性劑輸送至受檢者內之所要區域,該所要區域與該醫藥裝置所置放之體內腔非直接相鄰;其中該第一親脂性劑為具有如下結構之化合物之一: 其中該體內腔包含血管壁及冠狀動脈中之至少一者;其中該醫藥裝置為一血管內醫藥裝置;其中在長達約5天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約15μg/g至約150μg/g之範圍,在自約5天至長達約15天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約15μg/g至約80μg/g之範圍,及在自15天直至約28天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約5μg/g至約60μg/g之範圍。
  2. 如請求項1之系統,其進一步包含至少一種醫藥學上可接受之載劑或賦形劑,其中該醫藥裝置與該醫藥學上可接受之載劑或賦形劑結合。
  3. 如請求項2之系統,其中該醫藥學上可接受之載劑或賦形劑為聚合物。
  4. 如請求項2之系統,其中該醫藥學上可接受之載劑或賦形劑為劑。
  5. 如請求項1之系統,其中該醫藥裝置可被置放在包括冠狀動脈之該體內腔鄰近處,其中將治療有效量之該第一親 脂性劑輸送至該等冠狀動脈內且使其擴散至心包囊內。
  6. 如請求項5之系統,其中該系統提供該第一親脂性劑達至心肌之大體上均勻的藥物輸送。
  7. 如請求項5之系統,其中該系統適用於治療及/或預防受檢者中之血管疾病。
  8. 如請求項3之系統,其中該第一親脂性劑係藉由包含下列之機制所輸送:聚合物水合作用、繼之該第一親脂性劑之溶解,且其中此後將該第一親脂性劑輸送至該體內腔內。
  9. 如請求項3之系統,其中該第一親脂性劑係藉由包含下列之機制所輸送:控制該第一親脂性劑達至該體內腔之溶離速率的親脂性劑/聚合物基質。
  10. 如請求項1之系統,其進一步包含至少一種第二親脂性劑。
  11. 如請求項1之系統,其進一步包含至少一種親脂性前藥。
  12. 如請求項1之系統,其進一步包含至少一種親脂性穿透增強劑。
  13. 如請求項12之系統,其中該親脂性穿透增強劑為醫藥劑。
  14. 如請求項10之系統,其中與該第一親脂性劑組合之該第二親脂性劑之濃度係以治療有效量輸送至該體內腔。
  15. 如請求項1之系統,其進一步包含至少一種有益劑。
  16. 如請求項1之系統,其中該第一親脂性劑包括大於20,000P之分配係數。
  17. 如請求項1之系統,其中該第一親脂性劑包括大於20,000 P之分配係數且該第一親脂性劑具有小於約30μg/mL之溶解度。
  18. 如請求項16之系統,其中該第一親脂性劑包括至少約4.3之LogP。
  19. 如請求項1之系統,其中該系統包含具有至少約10,000(μg/mL)-1之傳遞係數的第一親脂性劑。
  20. 如請求項1之系統,其中該系統包含具有至少約15,000(μg/mL)-1之傳遞係數的第一親脂性劑。
  21. 如請求項1之系統,其中該第一親脂性劑在包含遠端心肌、無支架之心肌、下側心肌、無支架及遠端冠狀動脈中之至少一者之該受檢者中的目標區域內可達至治療顯著之濃度,且在整個28天時期內保持彼等濃度。
  22. 如請求項1之系統,其中該醫藥裝置可永久或暫時性地植入受檢者中。
  23. 如請求項1之系統,其中該第一親脂性劑呈非晶形形態。
  24. 如請求項1之系統,其進一步包含有益劑,該有益劑包括抗血栓藥、抗凝血劑、抗血小板劑、抗脂劑、血栓溶解劑、抗增殖劑、消炎藥、抑制增生劑、平滑肌細胞抑制劑、抗生素、生長因子抑制劑、細胞黏著抑制劑、細胞黏著促進劑、抗有絲分裂劑、抗纖維蛋白藥、抗氧化劑、抗癌藥、促進內皮細胞恢復之劑、基質金屬蛋白酶抑制劑、抗癌藥、抗代謝劑、抗過敏性物質、病毒載體、核酸、單株抗體、酪胺酸激酶抑制劑、反義化合物、寡核苷酸、細胞滲透增強劑及其任何組合中之至少一者。
  25. 如請求項1之系統,其進一步包含有益劑,該有益劑包括降血糖劑、降血脂劑、蛋白質、核酸、適用於刺激紅血球生成之劑、血管生成劑、抗潰瘍/抗逆流劑及抗噁心劑/抗嘔劑、PPAR-α促效劑及其任何組合中之至少一者。
  26. 如請求項1之系統,其進一步包含有益劑,該有益劑包括肝素鈉、LMW肝素、類肝素、水蛭素、阿加曲班(argatroban)、弗斯可林(forskolin)、伐普立若司(vapriprost)、前列環素及前列環素類似物、葡聚糖、D-苯丙胺酸-脯胺酸-精胺酸-氯甲基酮(合成抗凝血酵素)、糖蛋白IIb/IIIa(血小板膜受體拮抗劑抗體)、重組水蛭素、凝血酶抑制劑、吲哚美辛(indomethacin)、水楊酸苯酯、β-雌二醇、長春鹼(vinblastine)、ABT-627(阿曲生坦(astrasentan))、睾固酮、孕酮、紫杉醇(paclitaxel)、甲胺喋呤(methotrexate)、福莫司汀(fotemustine)、RPR-101511A、環孢素A、長春新鹼(vincristine)、卡維地洛(carvediol)、長春地辛(vindesine)、雙嘧達莫(dipyridamole)、甲胺喋呤、葉酸、血栓反應素模擬劑、雌二醇、地塞米松(dexamethasone)、甲泛葡胺(metrizamide)、碘帕醇(iopamidol)、碘海醇(iohexol)、碘普胺(iopromide)、碘比醇(iobitridol)、碘美普爾(iomeprol)、碘噴托(iopentol)、碘佛醇(ioversol)、碘昔蘭(ioxilan)、碘克沙醇(iodixanol)、碘曲蘭(iotrolan)及其前藥、類似物、衍生物及任何組合中之至少一者。
  27. 如請求項1之系統,其中該醫藥裝置包括選自由下列者組成之群的冠狀動脈內醫藥裝置:用於受檢者脈管系統中 之支架、藥物輸送導管、移植物及藥物輸送氣球。
  28. 如請求項1之系統,其中該醫藥裝置包括選自由下列者組成之群的支架:周邊支架、周邊冠狀動脈支架、可降解冠狀動脈支架、不可降解冠狀動脈支架、自膨脹型支架、氣球膨脹之支架及食管支架。
  29. 如請求項1之系統,其中該醫藥裝置係選自由下列者組成之群:動脈-靜脈移植物、繞道移植物、血管植入物及移植物及靜脈內導管。
  30. 如請求項10之系統,其中該第二親脂性劑為具有下列結構之化合物中之至少一者:
  31. 如請求項1之系統,其中使該第一親脂性劑可不斷地輸送至心外膜及/或心包囊。
  32. 一種醫藥裝置,其包含:與該醫藥裝置結合之治療有效量之第一親脂性劑,其中該第一親脂性劑能穿透體內腔,其中該第一親脂性劑之傳遞係數達至至少約5,000(μg/mL)-1之量;且其中該醫藥裝置可被置放至受檢者體內腔之鄰近處,且可將治療有效量之該第一親脂性劑輸送至受檢者內之所要區域,該所要區域與該醫藥裝置所置放之體內腔非直接相鄰;其中該第一親脂性劑為具有如下結構之化合物之一: 其中該體內腔包含血管壁及冠狀動脈中之至少一者;其中該醫藥裝置為一血管內醫藥裝置;其中在長達約5天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約15μg/g至約150μg/g之範圍,在自約5天至長達約15天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約15μg/g至約80μg/g之範圍,及在自15天直至約28天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約5μg/g至約60μg/g之範圍。
  33. 如請求項32之裝置,其進一步包含至少一種醫藥學上可接受之載劑或賦形劑,其中該醫藥裝置與該醫藥學上可 接受之載劑或賦形劑結合。
  34. 如請求項33之裝置,其中該醫藥學上可接受之載劑或賦形劑係以塗層形式與該醫藥裝置結合。
  35. 如請求項33之裝置,其中該醫藥學上可接受之載劑或賦形劑為聚合物。
  36. 如請求項33之裝置,其中該醫藥學上可接受之載劑或賦形劑為劑。
  37. 如請求項33之裝置,其中該醫藥學上可接受之載劑或賦形劑包含下列性質中之至少一者,該等下列性質包括:生物可降解性、生物相容性及合成性。
  38. 如請求項32之裝置,其中該醫藥裝置可被置放於包括冠狀動脈之該體內腔鄰近處,其中將治療有效量之該第一親脂性劑輸送至該等冠狀動脈內且使其擴散至心包囊內。
  39. 如請求項38之裝置,其中該醫藥裝置提供該第一親脂性劑達至心肌之大體上均勻的藥物輸送。
  40. 如請求項38之裝置,其中該第一親脂性劑適用於治療及/或預防受檢者中之血管疾病。
  41. 如請求項35之裝置,其中該第一親脂性劑係藉由包含下列之機制所輸送:聚合物水合作用、繼之該第一親脂性劑之溶解,且其中此後將該第一親脂性劑輸送至該體內腔內。
  42. 如請求項35之裝置,其中該第一親脂性劑係藉由包含下列之機制所輸送:控制該第一親脂性劑達至該體內腔之 溶離速率的親脂性劑/聚合物基質。
  43. 如請求項32之裝置,其進一步包含至少一種第二親脂性劑。
  44. 如請求項32之裝置,其進一步包含至少一種親脂性前藥。
  45. 如請求項32之裝置,其進一步包含至少一種親脂性穿透增強劑。
  46. 如請求項45之裝置,其中該親脂性穿透增強劑為醫藥劑。
  47. 如請求項43之裝置,其中與該第一親脂性劑組合之該第二親脂性劑之濃度係以治療有效量輸送至該體內腔。
  48. 如請求項32之裝置,其中該第一親脂性劑為佐他若莫司。
  49. 如請求項32之裝置,其進一步包含至少一種有益劑。
  50. 如請求項32之裝置,其中該第一親脂性劑包括大於20,000P之分配係數。
  51. 如請求項32之裝置,其中該第一親脂性劑包括大於20,000P之分配係數且該第一親脂性劑具有小於約30μg/mL之溶解度。
  52. 如請求項50之裝置,其中該第一親脂性劑包括至少約4.3之LogP。
  53. 如請求項32之裝置,其中該裝置包含具有至少約15μg/mL之溶解度的第一親脂性劑。
  54. 如請求項32之裝置,其中該裝置包含具有至少約10,000(μg/mL)-1之傳遞係數的第一親脂性劑。
  55. 如請求項32之裝置,其中該裝置包含具有至少約15,000(μg/mL)-1之傳遞係數的第一親脂性劑。
  56. 如請求項32之裝置,其中該第一親脂性劑在包含遠端心肌、無支架之心肌、下側心肌、無支架及遠端冠狀動脈中之至少一者之該受檢者中的目標區域內可達至治療顯著之濃度,且在整個28天時期內保持彼等濃度。
  57. 如請求項32之裝置,其中使該醫藥裝置永久或暫時性地植入受檢者體內。
  58. 如請求項32之裝置,其中該第一親脂性劑呈非晶形形態。
  59. 如請求項32之裝置,其進一步包含有益劑,該有益劑包括抗血栓藥、抗凝血劑、抗血小板劑、抗脂劑、血栓溶解劑、抗增殖劑、消炎藥、抑制增生劑、平滑肌細胞抑制劑、抗生素、生長因子抑制劑、細胞黏著抑制劑、細胞黏著促進劑、抗有絲分裂劑、抗纖維蛋白藥、抗氧化劑、抗癌藥、促進內皮細胞恢復之劑、基質金屬蛋白酶抑制劑、抗癌藥、抗代謝劑、抗過敏性物質、病毒載體、核酸、單株抗體、酪胺酸激酶抑制劑、反義化合物、寡核苷酸、細胞滲透增強劑及其任何組合中之至少一者。
  60. 如請求項32之裝置,其進一步包含有益劑,該有益劑包括降血糖劑、降血脂劑、蛋白質、核酸、適用於刺激紅血球生成之劑、血管生成劑、抗潰瘍/抗逆流劑及抗噁心劑/抗嘔劑、PPAR-α促效劑及其任何組合中之至少一者。
  61. 如請求項32之裝置,其進一步包含有益劑,該有益劑包括肝素鈉、LMW肝素、類肝素、水蛭素、阿加曲班、弗斯可林、伐普立若司、前列環素及前列環素類似物、葡聚糖、D-苯丙胺酸-脯胺酸-精胺酸-氯甲基酮(合成抗凝血 酵素)、糖蛋白IIb/IIIa(血小板膜受體拮抗劑抗體)、重組水蛭素、凝血酶抑制劑、吲哚美辛、水楊酸苯酯、β-雌二醇、長春鹼、ABT-627(阿曲生坦)、睾固酮、孕酮、紫杉醇、甲胺喋呤、福莫司汀、RPR-101511A、環孢素A、長春新鹼、卡維地洛、長春地辛、雙嘧達莫、甲胺喋呤、葉酸、血栓反應素模擬劑、雌二醇、地塞米松、甲泛葡胺、碘帕醇、碘海醇、碘普胺、碘比醇、碘美普爾、碘噴托、碘佛醇、碘昔蘭、碘克沙醇、碘曲蘭及其前藥、類似物、衍生物及任何組合中之至少一者。
  62. 如請求項32之裝置,其中該醫藥裝置包括選自由下列者組成之群的冠狀動脈內醫藥裝置:用於受檢者脈管系統中之支架、藥物輸送導管、移植物及藥物輸送氣球。
  63. 如請求項32之裝置,其中該醫藥裝置包括選自由下列者組成之群的支架:周邊支架、周邊冠狀動脈支架、可降解冠狀動脈支架、不可降解冠狀動脈支架、自膨脹型支架、氣球膨脹之支架及食管支架。
  64. 如請求項32之裝置,其中該醫藥裝置係選自由下列者組成之群:動脈-靜脈移植物、繞道移植物、血管植入物及移植物及靜脈內導管。
  65. 如請求項43之裝置,其中該第二親脂性劑為具有下列結構之化合物中之至少一者:
  66. 如請求項38之裝置,其中該第一親脂性劑可不斷地輸送至心外膜及/或心包囊。
  67. 一種支架,其包含:與該支架結合之治療有效量之第一親脂性劑,其中該第一親脂性劑能穿透體內腔,其中該第一親脂性劑之傳遞係數達至至少約5,000(μg/mL)-1之量;且其中該支架可被置放至受檢者體內腔之鄰近處且可將治療有效量之該第一親脂性劑輸送至受檢者內之所要區域,該所要區域與該支架所置放之體內腔非直接相鄰; 其中該第一親脂性劑為具有如下結構之化合物之一: 其中該體內腔包含血管壁及冠狀動脈中之至少一者;其中在長達約5天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約15μg/g至約150μg/g之範圍,在自約5天至長達約15天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約15μg/g至約80μg/g之範圍,及在自15天直至約28天之時期內該第一親脂性劑進入該體內腔之輸送劑量為約5μg/g至約60μg/g之範圍。
  68. 如請求項67之支架,其進一步包含至少一種醫藥學上可接受之載劑或賦形劑,其中該支架與該醫藥學上可接受 之載劑或賦形劑結合。
  69. 如請求項68之支架,其中該醫藥學上可接受之載劑或賦形劑係以塗層形式與該支架結合。
  70. 如請求項68之支架,其中該醫藥學上可接受之載劑或賦形劑為聚合物。
  71. 如請求項68之支架,其中該醫藥學上可接受之載劑或賦形劑為劑。
  72. 如請求項68之支架,其中該醫藥學上可接受之載劑或賦形劑包含下列性質中之至少一者,該等下列性質包括:生物可降解性、生物相容性或合成性。
  73. 如請求項67之支架,其可被置放於包括冠狀動脈之該體內腔鄰近處,其中將治療有效量之該第一親脂性劑輸送至該等冠狀動脈內且使其擴散至心包囊內。
  74. 如請求項73之支架,其提供該第一親脂性劑達至心肌之大體上均勻的藥物輸送。
  75. 如請求項73之支架,其中該第一親脂性劑適用於治療及/或預防受檢者中之血管疾病。
  76. 如請求項70之支架,其中該第一親脂性劑係藉由包含下列之機制所輸送:聚合物水合作用、繼之該第一親脂性劑之溶解,且其中此後將該第一親脂性劑輸送至該體內腔內。
  77. 如請求項70之支架,其中該第一親脂性劑係藉由包含下列之機制所輸送:控制該第一親脂性劑達至該體內腔之溶離速率的親脂性劑/聚合物基質。
  78. 如請求項67之支架,其進一步包含至少一種第二親脂性劑。
  79. 如請求項67之支架,其進一步包含至少一種親脂性前藥。
  80. 如請求項67之支架,其進一步包含至少一種親脂性穿透增強劑。
  81. 如請求項80之支架,其中該親脂性穿透增強劑為醫藥劑。
  82. 如請求項78之支架,其中與該第一親脂性劑組合之該第二親脂性劑之濃度係以治療有效量輸送至該體內腔。
  83. 如請求項81之支架,其中該第一親脂性劑為佐他若莫司。
  84. 如請求項67之支架,其進一步包含至少一種有益劑。
  85. 如請求項67之支架,其中該第一親脂性劑包括大於20,000P之分配係數。
  86. 如請求項67之支架,其中該第一親脂性劑包括大於20,000P之分配係數且該第一親脂性劑具有小於約30μg/mL之溶解度。
  87. 如請求項85之支架,其中該第一親脂性劑包括至少約4.3之LogP。
  88. 如請求項67之支架,其中該支架包含具有至少約15μg/mL之溶解度的第一親脂性劑。
  89. 如請求項67之支架,其中該支架包含具有至少約10,000(μg/mL)-1之傳遞係數的第一親脂性劑。
  90. 如請求項67之支架,其中該支架包含具有至少約15,000(μg/mL)-1之傳遞係數的第一親脂性劑。
  91. 如請求項67之支架,其中該第一親脂性劑在包含遠端心 肌、無支架之心肌、下側心肌、無支架及遠端冠狀動脈中之至少一者之該受檢者中的目標區域內可達至治療顯著之濃度,且在整個28天時期內保持彼等濃度。
  92. 如請求項67之支架,其中該支架可永久或暫時性地植入受檢者體內。
  93. 如請求項67之支架,其中該第一親脂性劑呈非晶形形態。
  94. 如請求項67之支架,其進一步包含有益劑,該有益劑包括抗血栓藥、抗凝血劑、抗血小板劑、抗脂劑、血栓溶解劑、抗增殖劑、消炎藥、抑制增生劑、平滑肌細胞抑制劑、抗生素、生長因子抑制劑、細胞黏著抑制劑、細胞黏著促進劑、抗有絲分裂劑、抗纖維蛋白藥、抗氧化劑、抗癌藥、促進內皮細胞恢復之劑、基質金屬蛋白酶抑制劑、抗癌藥、抗代謝劑、抗過敏性物質、病毒載體、核酸、單株抗體、酪胺酸激酶抑制劑、反義化合物、寡核苷酸、細胞滲透增強劑及其任何組合中之至少一者。
  95. 如請求項67之支架,其進一步包含有益劑,該有益劑包括降血糖劑、降血脂劑、蛋白質、核酸、適用於刺激紅血球生成之劑、血管生成劑、抗潰瘍/抗逆流劑及抗噁心劑/抗嘔劑、PPAR-α促效劑及其任何組合中之至少一者。
  96. 如請求項67之支架,其進一步包含有益劑,該有益劑包括肝素鈉、LMW肝素、類肝素、水蛭素、阿加曲班、弗斯可林、伐普立若司、前列環素及前列環素類似物、葡聚糖、D-苯丙胺酸-脯胺酸-精胺酸-氯甲基酮(合成抗凝血酵素)、糖蛋白IIb/IIIa(血小板膜受體拮抗劑抗體)、重組 水蛭素、凝血酶抑制劑、吲哚美辛、水楊酸苯酯、β-雌二醇、長春鹼、ABT-627(阿曲生坦)、睾固酮、孕酮、紫杉醇、甲胺喋呤、福莫司汀、RPR-101511A、環孢素A、長春新鹼、卡維地洛、長春地辛、雙嘧達莫、甲胺喋呤、葉酸、血栓反應素模擬劑、雌二醇、地塞米松、甲泛葡胺、碘帕醇、碘海醇、碘普胺、碘比醇、碘美普爾、碘噴托、碘佛醇、碘昔蘭、碘克沙醇、碘曲蘭及其前藥、類似物、衍生物及任何組合中之至少一者。
  97. 如請求項67之支架,其中該支架包括選自由下列者組成之群的支架:周邊支架、周邊冠狀動脈支架、可降解冠狀動脈支架、不可降解冠狀動脈支架、自膨脹型支架、氣球膨脹之支架及食管支架。
  98. 如請求項78之支架,其中該第二親脂性劑為具有下列結構之化合物中之至少一者:
  99. 如請求項73之支架,其中該第一親脂性劑可不斷地輸送至心外膜及/或心包囊。
  100. 如請求項1之系統,其可用於改良涉及置放一醫藥裝置在體內腔中以治療及/或預防鄰近疾病或保持該體內腔之開通之受檢者中之開通。
  101. 如請求項32之醫藥裝置,其可用於改良涉及置放一醫藥裝置在體內腔中以治療及/或預防鄰近疾病或保持該體內腔之開通之受檢者中之開通。
  102. 如請求項67之支架,其可用於改良涉及置放一醫藥裝置在體內腔中以治療及/或預防鄰近疾病或保持該體內腔之開通之受檢者中之開通。
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