JP2005530712A5 - - Google Patents
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- JP2005530712A5 JP2005530712A5 JP2003577857A JP2003577857A JP2005530712A5 JP 2005530712 A5 JP2005530712 A5 JP 2005530712A5 JP 2003577857 A JP2003577857 A JP 2003577857A JP 2003577857 A JP2003577857 A JP 2003577857A JP 2005530712 A5 JP2005530712 A5 JP 2005530712A5
- Authority
- JP
- Japan
- Prior art keywords
- less
- composition
- chloride
- drugs
- bromide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000000203 mixture Substances 0.000 claims 59
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 26
- 229940121369 angiogenesis inhibitors Drugs 0.000 claims 26
- -1 purinomastert Chemical compound 0.000 claims 22
- 239000003381 stabilizer Substances 0.000 claims 13
- 239000003814 drug Substances 0.000 claims 12
- 239000002105 nanoparticle Substances 0.000 claims 12
- 229940079593 drugs Drugs 0.000 claims 10
- 239000002245 particle Substances 0.000 claims 10
- 235000013162 Cocos nucifera Nutrition 0.000 claims 6
- 240000007170 Cocos nucifera Species 0.000 claims 6
- 230000037098 T max Effects 0.000 claims 6
- 239000011780 sodium chloride Substances 0.000 claims 6
- AISMNBXOJRHCIA-UHFFFAOYSA-N trimethylazanium;bromide Chemical compound Br.CN(C)C AISMNBXOJRHCIA-UHFFFAOYSA-N 0.000 claims 5
- 230000035839 C max Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonium chloride Substances [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims 3
- 108010079709 Angiostatins Proteins 0.000 claims 3
- 102000012936 Angiostatins Human genes 0.000 claims 3
- 238000010521 absorption reaction Methods 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 229960001040 ammonium chloride Drugs 0.000 claims 3
- 235000019270 ammonium chloride Nutrition 0.000 claims 3
- 230000033115 angiogenesis Effects 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-M chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 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 2
- CQOQDQWUFQDJMK-SSTWWWIQSA-N 2-Methoxyestradiol Chemical compound C([C@@H]12)C[C@]3(C)[C@@H](O)CC[C@H]3[C@@H]1CCC1=C2C=C(OC)C(O)=C1 CQOQDQWUFQDJMK-SSTWWWIQSA-N 0.000 claims 2
- YJHSJERLYWNLQL-UHFFFAOYSA-N 2-hydroxyethyl(dimethyl)azanium;chloride Chemical compound Cl.CN(C)CCO YJHSJERLYWNLQL-UHFFFAOYSA-N 0.000 claims 2
- 229960000686 Benzalkonium Chloride Drugs 0.000 claims 2
- 102100016705 COL18A1 Human genes 0.000 claims 2
- 108010079505 Endostatins Proteins 0.000 claims 2
- KQPYUDDGWXQXHS-UHFFFAOYSA-N Juglone Chemical compound O=C1C=CC(=O)C2=C1C=CC=C2O KQPYUDDGWXQXHS-UHFFFAOYSA-N 0.000 claims 2
- OAIJSZIZWZSQBC-LWRKPGOESA-N Lycopene Natural products CC(C)=CCC\C(C)=C/C=C/C(/C)=C\C=C\C(\C)=C/C=C/C=C(/C)\C=C\C=C(\C)/C=C/C=C(/C)CCC=C(C)C OAIJSZIZWZSQBC-LWRKPGOESA-N 0.000 claims 2
- DYKFCLLONBREIL-KVUCHLLUSA-N Minocycline Chemical compound C([C@H]1C2)C3=C(N(C)C)C=CC(O)=C3C(=O)C1=C(O)[C@@]1(O)[C@@H]2[C@H](N(C)C)C(O)=C(C(N)=O)C1=O DYKFCLLONBREIL-KVUCHLLUSA-N 0.000 claims 2
- 229960004023 Minocycline Drugs 0.000 claims 2
- HICYUNOFRYFIMG-UHFFFAOYSA-N N,N-dimethyl-1-naphthalen-1-ylmethanamine;hydrochloride Chemical compound [Cl-].C1=CC=C2C(C[NH+](C)C)=CC=CC2=C1 HICYUNOFRYFIMG-UHFFFAOYSA-N 0.000 claims 2
- AAFYOVPTFNNVDN-UHFFFAOYSA-N N-methyl-N-phenacylnitrous amide Chemical compound O=NN(C)CC(=O)C1=CC=CC=C1 AAFYOVPTFNNVDN-UHFFFAOYSA-N 0.000 claims 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N Stearic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- 102000005353 Tissue Inhibitor of Metalloproteinase-1 Human genes 0.000 claims 2
- 108010031374 Tissue Inhibitor of Metalloproteinase-1 Proteins 0.000 claims 2
- LRFVTYWOQMYALW-UHFFFAOYSA-N Xanthine Natural products O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 235000001014 amino acid Nutrition 0.000 claims 2
- 150000001413 amino acids Chemical group 0.000 claims 2
- 239000000730 antalgic agent Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims 2
- FXJNQQZSGLEFSR-UHFFFAOYSA-M benzyl-dimethyl-tetradecylazanium;chloride;hydrate Chemical compound O.[Cl-].CCCCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 FXJNQQZSGLEFSR-UHFFFAOYSA-M 0.000 claims 2
- JBIROUFYLSSYDX-UHFFFAOYSA-M benzyl-dodecyl-dimethylazanium;chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 JBIROUFYLSSYDX-UHFFFAOYSA-M 0.000 claims 2
- 125000002091 cationic group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000000052 comparative effect Effects 0.000 claims 2
- 239000003246 corticosteroid Substances 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 235000015872 dietary supplement Nutrition 0.000 claims 2
- DDXLVDQZPFLQMZ-UHFFFAOYSA-M dodecyl(trimethyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)C DDXLVDQZPFLQMZ-UHFFFAOYSA-M 0.000 claims 2
- 235000013399 edible fruits Nutrition 0.000 claims 2
- 235000020937 fasting conditions Nutrition 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 claims 2
- 230000000051 modifying Effects 0.000 claims 2
- QDHHCQZDFGDHMP-UHFFFAOYSA-N monochloramine Chemical compound ClN QDHHCQZDFGDHMP-UHFFFAOYSA-N 0.000 claims 2
- JVAZJLFFSJARQM-YBXAARCKSA-N n-Hexyl-beta-D-glucopyranoside Natural products CCCCCCO[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O JVAZJLFFSJARQM-YBXAARCKSA-N 0.000 claims 2
- 230000000275 pharmacokinetic Effects 0.000 claims 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 235000018102 proteins Nutrition 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 2
- 230000000699 topical Effects 0.000 claims 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2R,3R,4S,5R,6S)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2S,3R,4S,5R,6R)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2R,3R,4S,5R,6R)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- WUWDLXZGHZSWQZ-WQLSENKSSA-N (3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one Chemical compound N1C(C)=CC(C)=C1\C=C/1C2=CC=CC=C2NC\1=O WUWDLXZGHZSWQZ-WQLSENKSSA-N 0.000 claims 1
- NBRQRXRBIHVLGI-OWXODZSWSA-N (4aS,5aR,12aR)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide Chemical compound C1C2=CC=CC(O)=C2C(O)=C(C2=O)[C@@H]1C[C@@H]1[C@@]2(O)C(O)=C(C(=O)N)C(=O)C1 NBRQRXRBIHVLGI-OWXODZSWSA-N 0.000 claims 1
- UEJJHQNACJXSKW-SECBINFHSA-N (R)-thalidomide Chemical compound O=C1C2=CC=CC=C2C(=O)N1[C@@H]1CCC(=O)NC1=O UEJJHQNACJXSKW-SECBINFHSA-N 0.000 claims 1
- UEJJHQNACJXSKW-VIFPVBQESA-N (S)-thalidomide Chemical compound O=C1C2=CC=CC=C2C(=O)N1[C@H]1CCC(=O)NC1=O UEJJHQNACJXSKW-VIFPVBQESA-N 0.000 claims 1
- RMAJTXKOOKJAAV-UHFFFAOYSA-N 2,2-dihydroxyethyl(methyl)azanium;bromide Chemical compound [Br-].C[NH2+]CC(O)O RMAJTXKOOKJAAV-UHFFFAOYSA-N 0.000 claims 1
- DBRHJJQHHSOXCQ-UHFFFAOYSA-N 2,2-dihydroxyethyl(methyl)azanium;chloride Chemical compound [Cl-].C[NH2+]CC(O)O DBRHJJQHHSOXCQ-UHFFFAOYSA-N 0.000 claims 1
- VKDGNNYJFSHYKD-UHFFFAOYSA-N 2,5-diamino-2-(difluoromethyl)pentanoic acid;hydron;chloride Chemical compound Cl.NCCCC(N)(C(F)F)C(O)=O VKDGNNYJFSHYKD-UHFFFAOYSA-N 0.000 claims 1
- BSTPEQSVYGELTA-UHFFFAOYSA-N 2-(dimethylamino)ethanol;hydrobromide Chemical compound [Br-].C[NH+](C)CCO BSTPEQSVYGELTA-UHFFFAOYSA-N 0.000 claims 1
- VUKAUDKDFVSVFT-UHFFFAOYSA-N 2-[6-[4,5-bis(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)-6-methoxyoxan-3-yl]oxy-4,5-dimethoxy-2-(methoxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)-5-methoxyoxane-3,4-diol Chemical compound COC1C(OC)C(OC2C(C(O)C(OC)C(CO)O2)O)C(COC)OC1OC1C(COCC(C)O)OC(OC)C(OCC(C)O)C1OCC(C)O VUKAUDKDFVSVFT-UHFFFAOYSA-N 0.000 claims 1
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims 1
- HPEGNLMTTNTJSP-UHFFFAOYSA-N 2-heptylsulfanyl-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound CCCCCCCSC1OC(CO)C(O)C(O)C1O HPEGNLMTTNTJSP-UHFFFAOYSA-N 0.000 claims 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N 2-stearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 claims 1
- LGZKGOGODCLQHG-CYBMUJFWSA-N 5-[(2R)-2-hydroxy-2-(3,4,5-trimethoxyphenyl)ethyl]-2-methoxyphenol Chemical compound C1=C(O)C(OC)=CC=C1C[C@@H](O)C1=CC(OC)=C(OC)C(OC)=C1 LGZKGOGODCLQHG-CYBMUJFWSA-N 0.000 claims 1
- CWSZBVAUYPTXTG-UHFFFAOYSA-N 5-[6-[[3,4-dihydroxy-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxymethyl]-3,4-dihydroxy-5-[4-hydroxy-3-(2-hydroxyethoxy)-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxyoxan-2-yl]oxy-6-(hydroxymethyl)-2-methyloxane-3,4-diol Chemical compound O1C(CO)C(OC)C(O)C(O)C1OCC1C(OC2C(C(O)C(OC)C(CO)O2)OCCO)C(O)C(O)C(OC2C(OC(C)C(O)C2O)CO)O1 CWSZBVAUYPTXTG-UHFFFAOYSA-N 0.000 claims 1
- OIRDTQYFTABQOQ-GAWUUDPSSA-N 9-β-D-XYLOFURANOSYL-ADENINE Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@H](O)[C@H]1O OIRDTQYFTABQOQ-GAWUUDPSSA-N 0.000 claims 1
- 229940035676 ANALGESICS Drugs 0.000 claims 1
- 229940005513 ANTIDEPRESSANTS Drugs 0.000 claims 1
- 241000186361 Actinobacteria <class> Species 0.000 claims 1
- OIRDTQYFTABQOQ-SXVXDFOESA-N Adenosine Natural products Nc1ncnc2c1ncn2[C@@H]3O[C@@H](CO)[C@H](O)[C@@H]3O OIRDTQYFTABQOQ-SXVXDFOESA-N 0.000 claims 1
- XKBGEWXEAPTVCK-UHFFFAOYSA-M Aliquat 336 Chemical compound [Cl-].CCCCCCCC[N+](C)(CCCCCCCC)CCCCCCCC XKBGEWXEAPTVCK-UHFFFAOYSA-M 0.000 claims 1
- 244000144927 Aloe barbadensis Species 0.000 claims 1
- 235000002961 Aloe barbadensis Nutrition 0.000 claims 1
- XSDQTOBWRPYKKA-UHFFFAOYSA-N Amiloride Chemical compound NC(=N)NC(=O)C1=NC(Cl)=C(N)N=C1N XSDQTOBWRPYKKA-UHFFFAOYSA-N 0.000 claims 1
- SWLVFNYSXGMGBS-UHFFFAOYSA-N Ammonium bromide Chemical compound [NH4+].[Br-] SWLVFNYSXGMGBS-UHFFFAOYSA-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
- 241000416162 Astragalus gummifer Species 0.000 claims 1
- XFILPEOLDIKJHX-QYZOEREBSA-N Batimastat Chemical compound C([C@@H](C(=O)NC)NC(=O)[C@H](CC(C)C)[C@H](CSC=1SC=CC=1)C(=O)NO)C1=CC=CC=C1 XFILPEOLDIKJHX-QYZOEREBSA-N 0.000 claims 1
- 229950001858 Batimastat Drugs 0.000 claims 1
- KHSLHYAUZSPBIU-UHFFFAOYSA-M Benzododecinium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 KHSLHYAUZSPBIU-UHFFFAOYSA-M 0.000 claims 1
- 210000004369 Blood Anatomy 0.000 claims 1
- 210000001772 Blood Platelets Anatomy 0.000 claims 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 1
- 229940078456 CALCIUM STEARATE Drugs 0.000 claims 1
- 229940084030 CARBOXYMETHYLCELLULOSE CALCIUM Drugs 0.000 claims 1
- 229960004015 Calcitonin Drugs 0.000 claims 1
- 102400000113 Calcitonin Human genes 0.000 claims 1
- 108060001064 Calcitonin Proteins 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L Calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- 241001214176 Capros Species 0.000 claims 1
- RZEKVGVHFLEQIL-UHFFFAOYSA-N Celecoxib Chemical compound C1=CC(C)=CC=C1C1=CC(C(F)(F)F)=NN1C1=CC=C(S(N)(=O)=O)C=C1 RZEKVGVHFLEQIL-UHFFFAOYSA-N 0.000 claims 1
- CXRFDZFCGOPDTD-UHFFFAOYSA-M Cetrimide Chemical compound [Br-].CCCCCCCCCCCCCC[N+](C)(C)C CXRFDZFCGOPDTD-UHFFFAOYSA-M 0.000 claims 1
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims 1
- 229960001927 Cetylpyridinium Chloride Drugs 0.000 claims 1
- YMKDRGPMQRFJGP-UHFFFAOYSA-M Cetylpyridinium chloride Chemical group [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims 1
- TYNQWWGVEGFKRU-AJDPQWBVSA-N Chaconine Chemical compound O([C@@H]1[C@@H](CO)O[C@H]([C@@H]([C@H]1O)O[C@H]1[C@@H]([C@H](O)[C@@H](O)[C@H](C)O1)O)O[C@@H]1CC2=CC[C@H]3[C@@H]4C[C@@H]5N6C[C@@H](C)CC[C@@H]6[C@H]([C@@H]5[C@@]4(C)CC[C@@H]3[C@@]2(C)CC1)C)[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O TYNQWWGVEGFKRU-AJDPQWBVSA-N 0.000 claims 1
- 229940107161 Cholesterol Drugs 0.000 claims 1
- 229960001231 Choline Drugs 0.000 claims 1
- DLGJWSVWTWEWBJ-HGGSSLSASA-N Chondroitin Chemical compound CC(O)=N[C@@H]1[C@H](O)O[C@H](CO)[C@H](O)[C@@H]1OC1[C@H](O)[C@H](O)C=C(C(O)=O)O1 DLGJWSVWTWEWBJ-HGGSSLSASA-N 0.000 claims 1
- 229920002567 Chondroitin Polymers 0.000 claims 1
- AMLYAMJWYAIXIA-VWNVYAMZSA-N Cilengitide Chemical compound N1C(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)N(C)C(=O)[C@H]1CC1=CC=CC=C1 AMLYAMJWYAIXIA-VWNVYAMZSA-N 0.000 claims 1
- 210000001072 Colon Anatomy 0.000 claims 1
- 229940064701 Corticosteroid nasal preparations for topical use Drugs 0.000 claims 1
- 229960001334 Corticosteroids Drugs 0.000 claims 1
- 240000005497 Cyamopsis tetragonoloba Species 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N D-sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229940039227 DIAGNOSTIC AGENTS Drugs 0.000 claims 1
- 229940030606 DIURETICS Drugs 0.000 claims 1
- 229940005501 DOPAMINERGIC AGENTS Drugs 0.000 claims 1
- JDRSMPFHFNXQRB-IBEHDNSVSA-N Decyl glucoside Chemical compound CCCCCCCCCCO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O JDRSMPFHFNXQRB-IBEHDNSVSA-N 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- MKXZASYAUGDDCJ-SZMVWBNQSA-N Dextromethorphan Chemical compound C1CCC[C@H]2[C@@]3([H])N(C)CC[C@]21C1=CC(OC)=CC=C1C3 MKXZASYAUGDDCJ-SZMVWBNQSA-N 0.000 claims 1
- 229960001985 Dextromethorphan Drugs 0.000 claims 1
- RUPBZQFQVRMKDG-UHFFFAOYSA-M Didecyldimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCC[N+](C)(C)CCCCCCCCCC RUPBZQFQVRMKDG-UHFFFAOYSA-M 0.000 claims 1
- APSBXTVYXVQYAB-UHFFFAOYSA-M Dioctyl sodium sulfosuccinate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims 1
- 229960000878 Docusate Sodium Drugs 0.000 claims 1
- VLCYCQAOQCDTCN-UHFFFAOYSA-N Eflornithine Chemical compound NCCCC(N)(C(F)F)C(O)=O VLCYCQAOQCDTCN-UHFFFAOYSA-N 0.000 claims 1
- 241000196324 Embryophyta Species 0.000 claims 1
- 229940089020 Evening primrose oil Drugs 0.000 claims 1
- 229960000304 Folic Acid Drugs 0.000 claims 1
- NGGMYCMLYOUNGM-CSDLUJIJSA-N Fumagillin Chemical compound C([C@H]([C@H]([C@@H]1[C@]2(C)[C@H](O2)CC=C(C)C)OC)OC(=O)\C=C\C=C\C=C\C=C\C(O)=O)C[C@@]21CO2 NGGMYCMLYOUNGM-CSDLUJIJSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 229960002442 Glucosamine Drugs 0.000 claims 1
- 229920000084 Gum arabic Polymers 0.000 claims 1
- 229940093922 Gynecological Antibiotics Drugs 0.000 claims 1
- NIDYWHLDTIVRJT-UJPOAAIJSA-N Heptyl-β-D-Glucopyranoside Chemical compound CCCCCCCO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O NIDYWHLDTIVRJT-UJPOAAIJSA-N 0.000 claims 1
- MCAHMSDENAOJFZ-BVXDHVRPSA-N Herbimycin Chemical compound N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](OC)[C@@H](OC)C[C@H](C)[C@@H](OC)C2=CC(=O)C=C1C2=O MCAHMSDENAOJFZ-BVXDHVRPSA-N 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
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- 239000003163 gonadal steroid hormone Substances 0.000 claims 1
- 235000009569 green tea Nutrition 0.000 claims 1
- 238000000227 grinding Methods 0.000 claims 1
- 230000012010 growth Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 230000002439 hemostatic Effects 0.000 claims 1
- 239000002874 hemostatic agent Substances 0.000 claims 1
- 235000008216 herbs Nutrition 0.000 claims 1
- IJSPVDBICDUTNQ-UHFFFAOYSA-H hexasodium;8-[[4-methyl-3-[[3-[[3-[[2-methyl-5-[(8-oxidoperoxysulfanyl-4,6-disulfonatonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonate Chemical compound [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[O-]S(=O)(=O)C1=CC(SOO[O-])=C2C(NC(=O)C3=CC=C(C(=C3)NC(=O)C=3C=C(NC(=O)NC=4C=C(C=CC=4)C(=O)NC=4C(=CC=C(C=4)C(=O)NC=4C5=C(C=C(C=C5C(=CC=4)S([O-])(=O)=O)S([O-])(=O)=O)S([O-])(=O)=O)C)C=CC=3)C)=CC=C(S([O-])(=O)=O)C2=C1 IJSPVDBICDUTNQ-UHFFFAOYSA-H 0.000 claims 1
- 238000000265 homogenisation Methods 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 claims 1
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims 1
- 239000012216 imaging agent Substances 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 229940079866 intestinal antibiotics Drugs 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 235000019136 lipoic acid Nutrition 0.000 claims 1
- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 claims 1
- 239000001656 lutein Substances 0.000 claims 1
- 235000012680 lutein Nutrition 0.000 claims 1
- 125000002635 lutein group Chemical group 0.000 claims 1
- 229960004999 lycopene Drugs 0.000 claims 1
- 235000012661 lycopene Nutrition 0.000 claims 1
- 239000001751 lycopene Substances 0.000 claims 1
- 239000004325 lysozyme Substances 0.000 claims 1
- 229960000274 lysozyme Drugs 0.000 claims 1
- 235000010335 lysozyme Nutrition 0.000 claims 1
- 229960004616 medroxyprogesterone Drugs 0.000 claims 1
- 229960002985 medroxyprogesterone acetate Drugs 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- VXBSKVAMQMBCCA-UHFFFAOYSA-M methyl sulfate;trimethyl(tetradecyl)azanium Chemical compound COS([O-])(=O)=O.CCCCCCCCCCCCCC[N+](C)(C)C VXBSKVAMQMBCCA-UHFFFAOYSA-M 0.000 claims 1
- BAVYZALUXZFZLV-UHFFFAOYSA-O methylammonium Chemical compound [NH3+]C BAVYZALUXZFZLV-UHFFFAOYSA-O 0.000 claims 1
- 230000011987 methylation Effects 0.000 claims 1
- 238000007069 methylation reaction Methods 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 235000020786 mineral supplement Nutrition 0.000 claims 1
- 239000003158 myorelaxant agent Substances 0.000 claims 1
- 239000002742 neurokinin 1 receptor antagonist Substances 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
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- 235000015097 nutrients Nutrition 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 229940005935 ophthalmologic Antibiotics Drugs 0.000 claims 1
- 230000003364 opioid Effects 0.000 claims 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N oxane Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 1
- 229940094443 oxytocics Prostaglandins Drugs 0.000 claims 1
- 239000000734 parasympathomimetic agent Substances 0.000 claims 1
- 230000000849 parathyroid Effects 0.000 claims 1
- 229960001639 penicillamine Drugs 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 235000021317 phosphate Nutrition 0.000 claims 1
- 150000003904 phospholipids Chemical class 0.000 claims 1
- 150000004714 phosphonium salts Chemical class 0.000 claims 1
- 108010024226 placental ribonuclease inhibitor Proteins 0.000 claims 1
- 239000000419 plant extract Substances 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 229920001987 poloxamine Polymers 0.000 claims 1
- 229920000371 poly(diallyldimethylammonium chloride) polymer Polymers 0.000 claims 1
- 229920003229 poly(methyl methacrylate) Polymers 0.000 claims 1
- 229920000570 polyether Polymers 0.000 claims 1
- 239000004926 polymethyl methacrylate Substances 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 239000006041 probiotic Substances 0.000 claims 1
- 230000000529 probiotic Effects 0.000 claims 1
- 235000018291 probiotics Nutrition 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 230000002685 pulmonary Effects 0.000 claims 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 claims 1
- 239000012217 radiopharmaceutical Substances 0.000 claims 1
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- 229920005604 random copolymer Polymers 0.000 claims 1
- 230000001624 sedative Effects 0.000 claims 1
- 239000000932 sedative agent Substances 0.000 claims 1
- 238000004062 sedimentation Methods 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- 239000003195 sodium channel blocking agent Substances 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 239000000021 stimulant Substances 0.000 claims 1
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- 229940065721 systemic for obstructive airway disease Xanthines Drugs 0.000 claims 1
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- 235000019529 tetraterpenoid Nutrition 0.000 claims 1
- 229960002663 thioctic acid Drugs 0.000 claims 1
- 102000002938 thrombospondin family Human genes 0.000 claims 1
- 108060008245 thrombospondin family Proteins 0.000 claims 1
- 108010021724 tonin Proteins 0.000 claims 1
- 229940083878 topical for treatment of hemorrhoids and anal fissures Corticosteroids Drugs 0.000 claims 1
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- 125000005208 trialkylammonium group Chemical group 0.000 claims 1
- FAGMGMRSURYROS-UHFFFAOYSA-M trihexadecyl(methyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+](C)(CCCCCCCCCCCCCCCC)CCCCCCCCCCCCCCCC FAGMGMRSURYROS-UHFFFAOYSA-M 0.000 claims 1
- SZYJELPVAFJOGJ-UHFFFAOYSA-N trimethylamine hydrochloride Chemical compound Cl.CN(C)C SZYJELPVAFJOGJ-UHFFFAOYSA-N 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
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- XTXRWKRVRITETP-UHFFFAOYSA-N vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 claims 1
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Claims (25)
- (a)約2000nm未満の有効平均粒径を有する血管新生抑制剤またはその塩の粒子;および
(b)その表面と結合した少なくとも1種の表面安定剤、
を含んでなるナノ粒子血管新生抑制剤組成物。 - 血管新生抑制剤が、2-メトキシエストラジオール、プリノマスタット、バチマスタット、BAY 12-9566、カルボキシアミドトリアゾール、CC-1088、デキストロメトルファン酢酸、ジメチルキサンテノン酢酸、EMD 121974、エンドスタチン、IM-862、マリマスタット、マトリックスメタロプロテイナーゼ、ペニシラミン、PTK787/ZK 222584、RPI.4610、スクアラミン、乳酸スクアラミン、SU5416、(+)-サリドマイド、S-サリドマイド、R-サリドマイド、TNP-470、コンブレタスタチン、パクリタキセル、タモキシフェン、COL-3、ネオバスタット、BMS-275291、SU6668、インターフェロン-α、抗VEGF抗体、Medi-522(Vitaxin II)、CAI、セレコキシブ、インターロイキン-12、IM862、アミロライド、アンギオスタチン(登録商標)タンパク質、アンギオスタチンK1-3、アンギオスタチンK1-5、カプロプリル、DL-α-ジフルオロメチルオルニチン、DL-α-ジフルオロメチルオルニチンHCl、His-Tag(登録商標) EndostatinTMタンパク質、フマギリン、ヘルビマイシンA、4-ヒドロキシフェニルレチンアミド、γ-インターフェロン、ジュグロン、ラミニン、ラミニンヘキサペプチド、ラミニンペンタペプチド、ラベンヅスチンA、メドロキシプロゲステロン、酢酸メドロキシプロゲステロン、ミノシクリン、ミノシクリンHCl、胎盤リボヌクレアーゼ抑制剤、スラミン、ナトリウム塩スラミン、ヒト血小板トロンボスポンジン、メタロプロテイナーゼ1の組織抑制剤、メタロプロテイナーゼ1の好中球顆粒球組織抑制剤、およびメタロプロテイナーゼ2のリューマチ様滑液繊維芽細胞組織抑制剤からなる群から選択される、請求項1に記載の組成物。
- 血管新生抑制剤が2-メトキシエストラジオールである、請求項1または請求項2に記載の組成物。
- 血管新生抑制剤が結晶相、無定形相、半結晶相、半無定形相、およびそれらの混合物からなる群から選択される、請求項1〜3のいずれか1項に記載の組成物。
- ナノ粒子血管新生抑制剤の有効平均粒径が約1900nm未満、約1800nm未満、約1700nm未満、約1600nm未満、約1500nm未満、約1400nm未満、約1300nm未満、約1200nm未満、約1100nm未満、約1000nm未満、約900nm未満、約800nm未満、約700nm未満、約600nm未満、約500nm未満、約400nm未満、約300nm未満、約250nm未満、約200nm未満、約100nm未満、約75nm未満、または約50nm未満からなる群から選択される、請求項1〜4のいずれか1項に記載の組成物。
- 組成物が、
(a)経口、肺、直腸、眼、結腸、非経口、槽内、腟内、腹腔内、局部、バッカル、経鼻、および局所投与からなる群から選択される投与用に製剤される;および/または
(b)分散液、ジェル、エーロゾル、軟膏、クリーム、制御放出製剤、高速融解製剤、凍結乾燥製剤、錠剤、カプセル、遅延放出製剤、長期放出製剤、パルス放出製剤、ならびに高速放出および制御放出混合製剤からなる群から選択される投与剤形に製剤される、
請求項1〜5のいずれか1項に記載の組成物。 - 組成物がさらに1以上の製薬上許容される賦形剤、担体、またはそれらの組合わせを含んでなる、請求項1〜6のいずれか1項に記載の組成物。
- (a)他の賦形剤を含まずに血管新生抑制剤と少なくとも1種の表面安定剤の全組合わせ重量を基準として、血管新生抑制剤が重量により約99.5%〜約0.001%、約95%〜約0.1%、および約90%〜約0.5%からなる群から選択される量で存在する、および/または
(b)他の賦形剤を含まずに少なくとも1種の血管新生抑制剤と少なくとも1種の表面安定剤の全組合わせ重量を基準として、少なくとも1種の表面安定剤が重量により約0.5%〜約99.999%、約5.0%〜約99.9%、および約10%〜約99.5%からなる群から選択される量で存在する、
請求項1〜7のいずれか1項に記載の組成物。 - 少なくとも2種の表面安定剤を含む、請求項1〜8のいずれか1項に記載の組成物。
- 表面安定剤が、非イオン表面安定剤、アニオン表面安定剤、カチオン表面安定剤、イオン表面安定剤、および双イオン表面安定剤からなる群から選択される、請求項1〜9のいずれか1項に記載の組成物。
- 少なくとも1種の表面安定剤が、セチルピリジニウムクロリド、ゼラチン、カゼイン、ホスファチド、デキストラン、グリセロール、アカシアゴム、コレステロール、トラガカント、ステアリン酸、塩化ベンザルコニウム、ステアリン酸カルシウム、モノステアリン酸グリセロール、セトステアリルアルコール、セトマクロゴル乳化ワックス、ソルビタンエステル、ポリオキシエチレンアルキルエーテル、ポリオキシエチレンヒマシ油誘導体、ポリオキシエチレンソルビタン脂肪酸エステル、ポリエチレングリコール、ドデシルトリメチルアンモニウムブロミド、ステアリン酸ポリオキシエチレン、コロイド二酸化シリコン、ホスフェート、ドデシル硫酸ナトリウム、カルボキシメチルセルロースカルシウム、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシメチルセルロースナトリウム、メチルセルロース、ヒドロキシエチルセルロース、フタル酸ヒドロキシプロピルメチル-セルロース、非結晶セルロース、ケイ酸マグネシウムアルミニウム、トリエタノールアミン、ポリビニルアルコール、ポリビニルピロリドン、4-(1,1,3,3-テトラメチルブチル)-フェノールとエチレンオキシドおよびホルムアルデヒドとのポリマー、ポロキサマー;ポロキサミン、帯電リン脂質、スルホコハク酸ジオクチル、スルホコハク酸ナトリウムのジアルキルエステル、ラウリル硫酸ナトリウム、アルキルアリールポリエーテルスルホネート、ステアリン酸スクロースとジステアリン酸スクロースの混合物、C18H37CH2C(O)N(CH3)-CH2(CHOH)4(CH20H)2、p-イソノニルフェノキシポリ-(グリシドール)、デカノイル-N-メチルグルカミド;n-デシルβ-D-グルコピラノシド;n-デシルβ-D-マルトピラノシド;n-ドデシルβ-D-グルコピラノシド;n-ドデシルβ-D-マルトシド;ヘプタノイル-N-メチルグルカミド;n-へプチル-β-D-グルコピラノシド;n-へプチルβ-D-チオグルコシド;n-へクシルβ-D-グルコピラノシド;ノナノイル-N-メチルグルカミド;n-ノイルβ-D-グルコピラノシド;オクタノイル-N-メチルグルカミド;n-オクチル-β-D-グルコピラノシド;オクチルβ-D-チオグルコピラノシド;リゾチーム、PEG-リン脂質、PEG-コレステロール、PEG-コレステロール誘導体、PEG-ビタミンA、PEG-ビタミンE、酢酸ビニルとビニルピロリドンのランダムコポリマー、カチオン性脂質、ポリメチルメタクリレートトリメチルアンモニウムブロミド、スルホニウム化合物、ポリビニルピロリドン-2-ジメチルアミノエチルメタクリレートジメチルサルフェート、ヘキサデシルトリメチルアンモニウムブロミド、ホスホニウム化合物、第4級アンモニウム化合物、ベンジル-ジ(2-クロロエチル)エチルアンモニウムブロミド、ココナッツトリメチルアンモニウムクロリド、ココナッツトリメチルアンモニウムブロミド、ココナッツメチルジヒドロキシエチルアンモニウムクロリド、ココナッツメチルジヒドロキシエチルアンモニウムブロミド、デシルトリエチルアンモニウムクロリド、デシルジメチルヒドロキシエチルアンモニウムクロリド、デシルジメチルヒドロキシエチルアンモニウムクロリドブロミド、C12-15ジメチルヒドロキシエチルアンモニウムクロリド、C12-15ジメチルヒドロキシエチルアンモニウムクロリドブロミド、ココナッツジメチルヒドロキシエチルアンモニウムクロリド、ココナッツジメチルヒドロキシエチルアンモニウムブロミド、ミリスチルトリメチルアンモニウムメチルサルフェート、ラウリルジメチルベンジルアンモニウムクロリド、ラウリルジメチルベンジルアンモニウムブロミド、ラウリルジメチル(エテノキシ)4アンモニウムクロリド、ラウリルジメチル(エテノキシ)4アンモニウムブロミド、N-アルキル(C12-18)ジメチルベンジルアンモニウムクロリド、N-アルキル(C14-18)ジメチルベンジルアンモニウムクロリド、N-テトラデシルジメチルベンジルアンモニウムクロリド一水和物、ジメチルジデシルアンモニウムクロリド、N-アルキルおよび(C12-14)ジメチル1-ナフチルメチルアンモニウムクロリド、ハロゲン化トリメチルアンモニウム、アルキル-トリメチルアンモニウム塩、ジアルキル-ジメチルアンモニウム塩、ラウリルトリメチルアンモニウムクロリド、エトキシル化アルキルアミドアルキルジアルキルアンモニウム塩、エトキシル化トリアルキルアンモニウム塩、ジアルキルベンゼンジアルキルアンモニウムクロリド、N-ジデシルジメチルアンモニウムクロリド、N-テトラデシルジメチルベンジルアンモニウムクロリド一水和物、N-アルキル(C12-14)ジメチル1-ナフチルメチルアンモニウムクロリド、ドデシルジメチルベンジルアンモニウムクロリド、ジアルキルベンゼンアルキルアンモニウムクロリド、ラウリルトリメチルアンモニウムクロリド、アルキルベンジルメチルアンモニウムクロリド、アルキルベンジルジメチルアンモニウムブロミド、C12トリメチルアンモニウムブロミド、C15トリメチルアンモニウムブロミド、C17トリメチルアンモニウムブロミド、ドデシルベンジルトリエチルアンモニウムクロリド、ポリ-ジアリルジメチルアンモニウムクロリド(DADMAC)、ジメチルアンモニウムクロリド、アルキルジメチルアンモニウムハロゲン化物、トリセチルメチルアンモニウムクロリド、デシルトリメチルアンモニウムブロミド、ドデシルトリエチルアンモニウムブロミド、テトラデシルトリメチルアンモニウムブロミド、メチルトリオクチルアンモニウムクロリド、POLYQUAT 10TM、テトラブチルアンモニウムブロミド、ベンジルトリメチルアンモニウムブロミド、コリンエステル、塩化ベンザルコニウム、ステアラルコニウムクロリド化合物、セチルピリジニウムブロミド、セチルピリジニウムクロリド、4級化ポリオキシエチルアルキルアミンのハロゲン化物塩、MIRAPOLTM、ALKAQUATTM、アルキルピリジニウム塩;アミン、アミン塩、アミンオキシド、イミドアゾリニウム塩、プロトン化第4級アクリルアミド、メチル化第4級ポリマー、およびカチオン性グアールからなる群から選択される、請求項1〜10のいずれか1項に記載の組成物。
- 組成物が生物接着性である、請求項11に記載の組成物。
- 組成物が1種以上の血管新生抑制剤を含む、請求項1〜12のいずれか1項に記載の組成物。
- さらに約2ミクロン未満の有効平均粒径を有する少なくとも1種のナノ粒子血管新生抑制剤組成物を含む組成物であって、上記のさらなるナノ粒子血管新生抑制剤組成物が請求項1に記載のナノ粒子血管新生抑制剤組成物の粒径と異なる有効平均粒径を有する、請求項1〜13のいずれか1項に記載の組成物。
- さらに少なくとも1種の非血管新生抑制剤活性薬を含む、請求項1〜14のいずれか1項に記載の組成物。
- (a)上記非血管新生抑制剤活性薬が、アミノ酸、タンパク質、ペプチド、ヌクレオチド、抗肥満薬、栄養補助食品、サプルメント食品、中枢神経系刺激薬、カロテノイド、副腎皮質ステロイド、エラスターゼ抑制剤、抗真菌薬、アルキルキサンチン、腫瘍治療薬、抗催吐薬、鎮痛薬、オピオイド、解熱剤、心血管薬、抗炎症薬、駆虫薬、抗不整脈薬、抗生物質、抗凝血薬、抗うつ薬、抗糖尿病薬、抗てんかん薬、抗ヒスタミン薬、血圧降下薬、抗ムスカリン薬、抗放線菌薬、抗悪性腫瘍薬、免疫抑制薬、抗甲状腺薬、抗ウイルス薬、抗不安薬、鎮静薬、収斂薬、α-アドレナリン受容体遮断薬、β-アドレナリン受容体遮断薬、血液製剤、代替血液、強心薬、造影剤、副腎皮質ステロイド、咳抑制薬、診断薬、画像診断薬、利尿薬、ドーパミン作動薬、止血剤、免疫薬、脂質調節薬、筋弛緩薬、副交感神経様作用薬、副甲状腺カルシトニンおよびビホスホン酸、プロスタグランジン、放射性医薬品、性ホルモン、抗アレルギー薬、刺激薬、食欲抑制薬、交感神経模倣薬、甲状腺薬、血管拡張薬、血管モジュレーター、キサンチン、μ受容体アンタゴニスト、κ受容体アンタゴニスト、非麻薬性鎮痛薬、モノアミン摂取抑制剤、アデノシン調節薬、カンナビノイド誘導体、サブスタンスPアンタゴニスト、ニューロキニン-1受容体アンタゴニスト、およびナトリウムチャネル遮断薬からなる群から選択される、および/または
(b)上記栄養補助食品が、ルテイン、葉酸、脂肪酸、果実エキス、植物エキス、ビタミンサプルメント、ミネラルサプルメント、ホスファチジルセリン、リポ酸、メラトニン、グルコサミン/コンドロイチン、アロエ・ベラ、ガッグル、グルタミン、アミノ酸、緑茶、リコペン、全食品、食品添加物、ハーブ、植物栄養剤、抗酸化剤、果実のフラボノイド成分、月見草油、アマ種子、魚油、海洋動物油、およびプロバイオティクスからなる群から選択される、
請求項15に記載の組成物。 - 投与すると組成物が再分散して、血管新生抑制剤粒子が約2ミクロン未満、約1900nm未満、約1800nm未満、約1700nm未満、約1600nm未満、約1500nm未満、約1400nm未満、約1300nm未満、約1200nm未満、約1100nm未満、約1000nm未満、約900nm未満、約800nm未満、約700nm未満、約600nm未満、約500nm未満、約400nm未満、約300nm未満、約250nm未満、約200nm未満、約150nm未満、約100nm未満、約75nm未満、または約50nm未満からなる群から選択される粒径を有する、請求項1〜16のいずれか1項に記載の組成物。
- (a)摂食のもとで投与したときに、絶食条件と比較して、組成物が有意差のある吸収レベルを生じない、および/または
(b)摂食のもとで投与したときに、絶食条件と比較して、組成物が有意差のある吸収速度(Tmax)を生じない、
請求項1〜17のいずれか1項に記載の組成物。 - (a)摂食のもとで投与したときの絶食状態と対比した本発明のナノ粒子血管新生抑制剤組成物の吸収の差が、約100%未満、約90%未満、約80%未満、約70%未満、約60%未満、約50%未満、約40%未満、約35%未満、約30%未満、約25%未満、約20%未満、約15%未満、または約10%未満、約5%未満、約3%未満からなる群から選択される、および/または
(b)摂食のもとで投与したときの絶食状態と対比した本発明のナノ粒子血管新生抑制剤組成物のTmaxの差が約100%未満、約90%未満、約80%未満、約70%未満、約60%未満、約50%未満、約40%未満、約30%未満、約20%未満、約15%未満、または約10%未満、約5%未満、約3%未満である、
請求項1〜18のいずれか1項に記載の組成物。 - (a)投与時に、Tmaxが同じ用量で投与した同じ血管新生抑制剤の通常の非ナノ粒子組成物のそれより小さい、および/または
(b)同じ用量で投与した同じ血管新生抑制剤の非ナノ粒子組成物との比較薬物動態試験において、ナノ粒子組成物が、血管新生抑制剤の非ナノ粒子組成物により示されるTmaxの約100%未満、約90%未満、約80%未満、約70%未満、約60%未満、約50%未満、約40%未満、約30%未満、約25%未満、約20%未満、約15%未満、および約10%未満からなる群から選択されるTmaxを示す、および/または
(c)投与後に、組成物が約2.5時間未満、約2.25時間未満、約2時間未満、約1.75時間未満、約1.5時間未満、約1.25時間未満、約1.0時間未満、約50分間未満、約40分間未満、約30分間未満、約25分間未満、約20分間未満、約15分間未満、または約10分間未満からなる群から選択されるTmaxを有する、
請求項1〜19のいずれか1項に記載の組成物。 - (a)投与時に、組成物のCmaxが同じ用量で投与した同じ血管新生抑制剤の通常の非ナノ粒子組成物のCmaxより大きい、および/または
(b)同じ用量で投与した同じ血管新生抑制剤の非ナノ粒子組成物との比較薬物動態試験において、ナノ粒子組成物が、血管新生抑制剤の非ナノ粒子組成物が示すCmaxより、約5%を超える、約10%を超える、約15%を超える、約20%を超える、約30%を超える、約40%を超える、約50%を超える、約60%を超える、約70%を超える、約80%を超える、約90%を超える、約100%を超える、約110%を超える、約120%を超える、約130%を超える、約140%を超える、または約150%を超える値からなる群から選択されるCmaxを示す、
請求項1〜20のいずれか1項に記載の組成物。 - 医薬の製造のための、請求項1〜21のいずれか1項に記載の組成物の使用。
- 上記医薬が、
(a)選択的血管新生抑制剤を必要とする症状を治療するために有用である、
(b)望ましくない血管新生により特徴づけられる哺乳類動物の疾患を治療するために有用である、
(c)腫瘍増殖を治療または予防するために有用である、あるいは
(d)癌増殖を治療または予防するために有用である、
請求項22の使用。 - 少なくとも1種の血管新生抑制剤の粒子と少なくとも1種の表面安定剤とを、約2ミクロン未満の有効平均粒径を有する血管新生抑制剤組成物を得るために十分な時間および条件のもとで接触させることを含む、血管新生抑制剤組成物を作製する方法。
- 上記の接触が、粉砕、湿式粉砕、均質化、または沈降を含む、請求項24に記載の方法。
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-
2003
- 2003-03-20 CA CA2479665A patent/CA2479665C/en not_active Expired - Fee Related
- 2003-03-20 EP EP03723781A patent/EP1490030B2/en not_active Expired - Lifetime
- 2003-03-20 AT AT03723781T patent/ATE343376T1/de not_active IP Right Cessation
- 2003-03-20 JP JP2003577857A patent/JP4842514B2/ja not_active Expired - Fee Related
- 2003-03-20 WO PCT/US2003/008546 patent/WO2003080027A1/en active IP Right Grant
- 2003-03-20 US US10/392,403 patent/US20040033267A1/en not_active Abandoned
- 2003-03-20 DE DE60309300T patent/DE60309300T3/de not_active Expired - Lifetime
- 2003-03-20 AU AU2003230691A patent/AU2003230691A1/en not_active Abandoned
-
2007
- 2007-10-30 US US11/928,278 patent/US20080107741A1/en not_active Abandoned
- 2007-10-30 US US11/928,250 patent/US20080050461A1/en not_active Abandoned
- 2007-10-30 US US11/928,289 patent/US20080226732A1/en not_active Abandoned
-
2008
- 2008-05-09 US US12/117,982 patent/US20080279949A1/en not_active Abandoned
-
2009
- 2009-11-24 JP JP2009266089A patent/JP2010077146A/ja not_active Withdrawn
-
2010
- 2010-08-27 US US12/870,722 patent/US20100322852A1/en not_active Abandoned
- 2010-08-27 US US12/870,745 patent/US20100322853A1/en not_active Abandoned
- 2010-08-27 US US12/870,749 patent/US20100329976A1/en not_active Abandoned
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