JP2011528031A5 - - Google Patents
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- JP2011528031A5 JP2011528031A5 JP2011518059A JP2011518059A JP2011528031A5 JP 2011528031 A5 JP2011528031 A5 JP 2011528031A5 JP 2011518059 A JP2011518059 A JP 2011518059A JP 2011518059 A JP2011518059 A JP 2011518059A JP 2011528031 A5 JP2011528031 A5 JP 2011528031A5
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- 239000000758 substrate Substances 0.000 claims description 21
- 150000002632 lipids Chemical class 0.000 claims description 15
- 150000003904 phospholipids Chemical class 0.000 claims description 5
- 229940067631 Phospholipids Drugs 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims 8
- 239000011159 matrix material Substances 0.000 claims 6
- 230000000399 orthopedic Effects 0.000 claims 6
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol 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 4
- 239000004621 biodegradable polymer Substances 0.000 claims 4
- 229920002988 biodegradable polymer Polymers 0.000 claims 4
- 239000011248 coating agent Substances 0.000 claims 4
- 238000000576 coating method Methods 0.000 claims 4
- 210000000988 Bone and Bones Anatomy 0.000 claims 3
- 102000008186 Collagen Human genes 0.000 claims 3
- 108010035532 Collagen Proteins 0.000 claims 3
- 229960005188 collagen Drugs 0.000 claims 3
- 229920001436 collagen Polymers 0.000 claims 3
- 239000003960 organic solvent Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229940107161 Cholesterol Drugs 0.000 claims 2
- 229920000954 Polyglycolide Polymers 0.000 claims 2
- 239000003242 anti bacterial agent Substances 0.000 claims 2
- 230000003115 biocidal Effects 0.000 claims 2
- 239000002617 bone density conservation agent Substances 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 150000004665 fatty acids Chemical group 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 239000007943 implant Substances 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drugs Drugs 0.000 claims 2
- 229920000747 poly(lactic acid) polymer Polymers 0.000 claims 2
- 239000004633 polyglycolic acid Substances 0.000 claims 2
- 239000004626 polylactic acid Substances 0.000 claims 2
- 150000003432 sterols Chemical class 0.000 claims 2
- 235000003702 sterols Nutrition 0.000 claims 2
- 230000002459 sustained Effects 0.000 claims 2
- ZAKBPRIDLSBYQQ-VHSXEESVSA-N 1,2-diacyl-sn-glycero-3-phospho-(1'-sn-glycerol) Chemical compound CC(=O)OC[C@@H](OC(C)=O)COP(O)(=O)OC[C@@H](O)CO ZAKBPRIDLSBYQQ-VHSXEESVSA-N 0.000 claims 1
- 229940064005 Antibiotic throat preparations Drugs 0.000 claims 1
- 229940083879 Antibiotics FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Drugs 0.000 claims 1
- 229940042052 Antibiotics for systemic use Drugs 0.000 claims 1
- 229940042786 Antitubercular Antibiotics Drugs 0.000 claims 1
- 229910000684 Cobalt-chrome Inorganic materials 0.000 claims 1
- 229950003499 FIBRIN Drugs 0.000 claims 1
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 claims 1
- 102000009123 Fibrin Human genes 0.000 claims 1
- 108010073385 Fibrin Proteins 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 229940093922 Gynecological Antibiotics Drugs 0.000 claims 1
- 229960002897 Heparin Drugs 0.000 claims 1
- ZFGMDIBRIDKWMY-PASTXAENSA-N Heparin Chemical compound CC(O)=N[C@@H]1[C@@H](O)[C@H](O)[C@@H](COS(O)(=O)=O)O[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O[C@H]2[C@@H]([C@@H](OS(O)(=O)=O)[C@@H](O[C@@H]3[C@@H](OC(O)[C@H](OS(O)(=O)=O)[C@H]3O)C(O)=O)O[C@@H]2O)CS(O)(=O)=O)[C@H](O)[C@H]1O ZFGMDIBRIDKWMY-PASTXAENSA-N 0.000 claims 1
- 210000000282 Nails Anatomy 0.000 claims 1
- UNJJBGNPUUVVFQ-ZJUUUORDSA-N Phosphatidylserine Chemical compound CCCC(=O)O[C@H](COC(=O)CC)COP(O)(=O)OC[C@H](N)C(O)=O UNJJBGNPUUVVFQ-ZJUUUORDSA-N 0.000 claims 1
- 229910001069 Ti alloy Inorganic materials 0.000 claims 1
- 229960001295 Tocopherol Drugs 0.000 claims 1
- 229940024982 Topical Antifungal Antibiotics Drugs 0.000 claims 1
- 230000000843 anti-fungal Effects 0.000 claims 1
- 239000003429 antifungal agent Substances 0.000 claims 1
- 229940121375 antifungals Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 230000003416 augmentation Effects 0.000 claims 1
- 239000004622 biodegradable polyester Substances 0.000 claims 1
- 229920000229 biodegradable polyester Polymers 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 239000004568 cement Substances 0.000 claims 1
- 239000000919 ceramic Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- -1 cobalt chromium Chemical compound 0.000 claims 1
- 239000010952 cobalt-chrome Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 238000001704 evaporation Methods 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 229920000669 heparin Polymers 0.000 claims 1
- 239000008240 homogeneous mixture Substances 0.000 claims 1
- 229910052588 hydroxylapatite Inorganic materials 0.000 claims 1
- 230000002163 immunogen Effects 0.000 claims 1
- 229940079866 intestinal antibiotics Drugs 0.000 claims 1
- 239000000463 material Substances 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 229910052751 metal Inorganic materials 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000002365 multiple layer Substances 0.000 claims 1
- 229940005935 ophthalmologic Antibiotics Drugs 0.000 claims 1
- 230000002188 osteogenic Effects 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 201000001245 periodontitis Diseases 0.000 claims 1
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims 1
- 150000003905 phosphatidylinositols Chemical class 0.000 claims 1
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 150000003408 sphingolipids Chemical class 0.000 claims 1
- 239000010935 stainless steel Substances 0.000 claims 1
- 229910001220 stainless steel Inorganic materials 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 230000004936 stimulating Effects 0.000 claims 1
- 239000003356 suture material Substances 0.000 claims 1
- GUVRBAGPIYLISA-UHFFFAOYSA-N tantalum Chemical compound [Ta] GUVRBAGPIYLISA-UHFFFAOYSA-N 0.000 claims 1
- 229910052715 tantalum Inorganic materials 0.000 claims 1
- 235000010384 tocopherol Nutrition 0.000 claims 1
- 239000011732 tocopherol Substances 0.000 claims 1
- 229930003799 tocopherols Natural products 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 description 4
- 150000001982 diacylglycerols Chemical class 0.000 description 2
- 125000005265 dialkylamine group Chemical group 0.000 description 2
- 150000001985 dialkylglycerols Chemical class 0.000 description 2
- 150000008103 phosphatidic acids Chemical class 0.000 description 2
- 150000008104 phosphatidylethanolamines Chemical class 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
Description
他の実施形態では、本発明の組成物が更にペグ化(pegylated)脂質を含む。他の実施形態では、PEG部分が500〜5000ダルトンのMWを有する。他の実施形態では、PEG部分が他の任意の適切なMWを有する。適切なPEG修飾脂質の非限定的な例としては、メトキシ末端基を有するPEG部分、例えば以下に示すようなPEG修飾ホスファチジルエタノールアミンおよびホスファチジン酸（構造AおよびB）、PEG修飾ジアシルグリセロールおよびジアルキルグリセロール（構造CおよびD）、PEG修飾ジアルキルアミン（構造E）、およびPEG修飾1,2-ジアシルオキシプロパン-3-アミン（構造F）が挙げられる。他の実施形態では、PEG部分が当業界で用いる他の任意の末端基を有する。他の実施形態では、ペグ化脂質をPEG修飾ホスファチジルエタノールアミン、PEG修飾ホスファチジン酸、PEG修飾ジアシルグリセロール、PEG修飾ジアルキルグリセロール、PEG修飾ジアルキルアミンおよびPEG修飾1,2-ジアシルオキシプロパン-3-アミンからなる群から選択する。他の実施形態では、ペグ化脂質が当業界で既知の他の任意のペグ化リン脂質である。各可能性は本発明の別々の実施形態を表す。
ペグ化脂質は、基質組成物中に全脂質の10モル%未満の量で存在するのが好ましい。他の実施形態では、この割合が全脂質の9モル%未満である。他の実施形態では、この割合が8モル%未満である。他の実施形態では、この割合が7モル%未満である。他の実施形態では、この割合が6モル%未満である。他の実施形態では、この割合が5モル%未満である。他の実施形態では、この割合が4モル%未満である。他の実施形態では、この割合が3モル%未満である。他の実施形態では、この割合が2モル%未満である。他の実施形態では、この割合が1モル%未満である。各可能性は本発明の別々の実施形態を表す。
Claims (22)
- a.極性基を有する第1の脂質に関連する生分解性ポリマーと、
b.少なくとも14の炭素からなる炭化水素鎖を有する少なくとも1つのリン脂質を含む第2の脂質と、
c.少なくとも1つの薬学的活性物質とを含み、本質的に水が無く、前記薬学的活性物質の徐放を付与するのに適するようにした基質組成物。 - 前記リン脂質が、少なくとも14の炭素を有する脂肪酸部分を含むホスファチジルコリンである請求項1に記載の基質組成物。
- 前記生分解性ポリマーが、PLA（ポリ乳酸）、PGA（ポリグリコール酸）、PLGA（ポリ（乳酸−グリコール酸）からなる群から選択された生分解性ポリエステルである請求項1に記載の基質組成物。
- 前記薬学的活性物質が、抗生物質、抗真菌薬、非ステロイド抗炎症薬、ステロイド、抗癌剤、骨原性因子および骨吸収抑制剤から選択される請求項1に記載の基質組成物。
- 前記極性基を有する第1の脂質がステロールを含む請求項1に記載の基質組成物。
- 前記生分解性ポリマーに対する全脂質の質量比が、1.5:1〜9:1である請求項1に記載の基質組成物。
- 前記基質組成物が均質である請求項1に記載の基質組成物。
- トコフェロールを更に含む請求項1に記載の基質組成物。
- スフィンゴ脂質；14以上の炭素原子を有する遊離脂肪酸；ホスファチジルセリン、ホスファチジルグリセロールおよびホスファチジルイノシトールからなる群から選択される追加のリン脂質；並びに、コラーゲン分子、フィブリン分子およびヘパリンからなる群から選択される標的分子と相互作用可能な標的部分；からなる群から選択される化合物を更に含む請求項１に記載の基質組成物。
- ペグ化脂質を更に含む請求項1に記載の基質組成物。
- 前記ステロールがコレステロールである請求項5に記載の基質組成物。
- 前記コレステロールが前記基質組成物の総脂質含有量の5〜50モル%の量で存在する請求項11に記載の基質組成物。
- 前記薬学的活性物質の少なくとも50%がゼロ次速度過程で前記組成物から放出される薬学的活性物質の徐放用の請求項1に記載の基質組成物。
- 請求項1に記載の基質組成物を含むインプラント。
- 請求項1に記載の基質組成物を含む薬学的活性物質の徐放用の医薬組成物。
- 請求項1に記載の基質組成物を含み、薬学的活性物質が抗生物質、抗真菌薬および非ステロイド抗炎症薬から選択される、必要とする被検体の歯周炎の治療用医薬組成物。
- 請求項1に記載の基質組成物を含み、薬学的活性物質が骨原性因子および骨吸収抑制剤から選択される、必要とする被検体の骨増生の刺激用医薬組成物。
- 基板と、前記基板の少なくとも一部分上に堆積させた生体適合性コーティングとを備え、該生体適合性コーティングが請求項1に記載の基質組成物を含む医療装置。
- 前記生体適合性コーティングが多層を含む請求項18に記載の医療装置。
- 前記基板が、ヒドロキシアパタイト、ステンレス鋼、コバルトクロム、チタン合金、タンタル、セラミック、ゼラチンからなる群から選択される少なくとも1つの材料を含む請求項18に記載の医療装置。
- 整形外科用爪、整形外科用ねじ、整形外科用ステープル、整形外科用ワイヤ、整形外科用ピン、金属またはポリマーインプラント、骨充填材粒子、コラーゲンおよび非コラーゲンメンブレン、縫合材料、整形外科用セメント、スポンジから選択される基板のコーティング用の請求項1に記載の組成物の使用。
- 基質組成物を製造するに当たり、
a. 第1の揮発性有機溶媒に（i）生分解性ポリマーと、（ii）極性基を有する第1の脂質とを混合するステップと、
b. 第2の揮発性有機溶媒に（i）少なくとも1つの薬学的活性物質と、（ii）少なくとも14の炭素からなる炭化水素鎖を有するリン脂質から選択した第2の脂質とを混合するステップと、
c. 前記ステップ（a）および（b）で得られた生成物を混合して均質混合物を生成するステップと、
d. 前記揮発性有機溶媒を蒸発させて均質基質組成物を生成するステップとを備え、前記各ステップが実質的に水溶液の無いものである請求項1に記載の基質組成物の製造方法。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8028908P | 2008-07-14 | 2008-07-14 | |
| US61/080,289 | 2008-07-14 | ||
| US15478509P | 2009-02-24 | 2009-02-24 | |
| US61/154,785 | 2009-02-24 | ||
| PCT/IL2009/000701 WO2010007623A1 (en) | 2008-07-14 | 2009-07-14 | Sustained-release drug carrier composition |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015002177A Division JP2015129128A (ja) | 2008-07-14 | 2015-01-08 | 徐放性薬剤キャリア組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011528031A JP2011528031A (ja) | 2011-11-10 |
| JP2011528031A5 true JP2011528031A5 (ja) | 2012-08-23 |
| JP5681626B2 JP5681626B2 (ja) | 2015-03-11 |
Family
ID=41550058
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011518059A Active JP5681626B2 (ja) | 2008-07-14 | 2009-07-14 | 徐放性薬剤キャリア組成物 |
| JP2015002177A Ceased JP2015129128A (ja) | 2008-07-14 | 2015-01-08 | 徐放性薬剤キャリア組成物 |
| JP2016023906A Active JP6053083B2 (ja) | 2008-07-14 | 2016-02-10 | 徐放性薬剤キャリア組成物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015002177A Ceased JP2015129128A (ja) | 2008-07-14 | 2015-01-08 | 徐放性薬剤キャリア組成物 |
| JP2016023906A Active JP6053083B2 (ja) | 2008-07-14 | 2016-02-10 | 徐放性薬剤キャリア組成物 |
Country Status (11)
| Country | Link |
|---|---|
| US (6) | US8877242B2 (ja) |
| EP (1) | EP2299953B1 (ja) |
| JP (3) | JP5681626B2 (ja) |
| CN (2) | CN104274866B (ja) |
| AU (1) | AU2009272280B2 (ja) |
| CA (1) | CA2730340C (ja) |
| DK (1) | DK2299953T3 (ja) |
| ES (1) | ES2630805T3 (ja) |
| HK (1) | HK1205960A1 (ja) |
| PL (1) | PL2299953T3 (ja) |
| WO (1) | WO2010007623A1 (ja) |
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| US11731099B2 (en) | 2018-07-20 | 2023-08-22 | The Trustees Of Princeton University | Method for controlling encapsulation efficiency and burst release of water soluble molecules from nanoparticles and microparticles produced by inverse flash nanoprecipitation |
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