JP2009504778A5 - - Google Patents
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- JP2009504778A5 JP2009504778A5 JP2008527182A JP2008527182A JP2009504778A5 JP 2009504778 A5 JP2009504778 A5 JP 2009504778A5 JP 2008527182 A JP2008527182 A JP 2008527182A JP 2008527182 A JP2008527182 A JP 2008527182A JP 2009504778 A5 JP2009504778 A5 JP 2009504778A5
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- 239000000203 mixture Substances 0.000 claims 22
- 238000009472 formulation Methods 0.000 claims 9
- 230000000975 bioactive Effects 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 244000079386 endoparasites Species 0.000 claims 7
- 238000007920 subcutaneous administration Methods 0.000 claims 7
- XEKOWRVHYACXOJ-UHFFFAOYSA-N acetic acid ethyl ester Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 6
- 244000078703 ectoparasites Species 0.000 claims 5
- 229920000642 polymer Polymers 0.000 claims 5
- 239000002904 solvent Substances 0.000 claims 5
- 201000008297 typhoid fever Diseases 0.000 claims 5
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 241000243774 Trichinella Species 0.000 claims 4
- 241000223782 Ciliophora Species 0.000 claims 3
- LZCLXQDLBQLTDK-UHFFFAOYSA-N Ethyl lactate Chemical compound CCOC(=O)C(C)O LZCLXQDLBQLTDK-UHFFFAOYSA-N 0.000 claims 3
- 241000243795 Ostertagia Species 0.000 claims 3
- RUOJZAUFBMNUDX-UHFFFAOYSA-N Propylene carbonate Chemical compound CC1COC(=O)O1 RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 claims 3
- 229940116333 ethyl lactate Drugs 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 239000007788 liquid Substances 0.000 claims 3
- SECXISVLQFMRJM-UHFFFAOYSA-N n-methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 3
- BTANRVKWQNVYAZ-UHFFFAOYSA-N 2-Butanol Chemical compound CCC(C)O BTANRVKWQNVYAZ-UHFFFAOYSA-N 0.000 claims 2
- JYVLIDXNZAXMDK-UHFFFAOYSA-N 2-Pentanol Chemical compound CCCC(C)O JYVLIDXNZAXMDK-UHFFFAOYSA-N 0.000 claims 2
- AZSNMRSAGSSBNP-XPNPUAGNSA-N 22,23-dihydroavermectin B1a Chemical compound C1C[C@H](C)[C@@H]([C@@H](C)CC)O[C@@]21O[C@H](C\C=C(C)\[C@@H](O[C@@H]1O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C1)[C@@H](C)\C=C\C=C/1[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\1)O)C[C@H]4C2 AZSNMRSAGSSBNP-XPNPUAGNSA-N 0.000 claims 2
- 239000005660 Abamectin Substances 0.000 claims 2
- 241000244203 Caenorhabditis elegans Species 0.000 claims 2
- JBKVHLHDHHXQEQ-UHFFFAOYSA-N Caprolactam Chemical compound O=C1CCCCCN1 JBKVHLHDHHXQEQ-UHFFFAOYSA-N 0.000 claims 2
- FXHOOIRPVKKKFG-UHFFFAOYSA-N DMA Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 2
- 241000244160 Echinococcus Species 0.000 claims 2
- CXEGAUYXQAKHKJ-FYOMLGFFSA-N Emamectin Chemical compound C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@H](C)[C@@H](NC)[C@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 CXEGAUYXQAKHKJ-FYOMLGFFSA-N 0.000 claims 2
- 239000005894 Emamectin Substances 0.000 claims 2
- WPNHOHPRXXCPRA-TVXIRPTOSA-N Eprinomectin Chemical compound O1[C@@H](C)[C@@H](NC(C)=O)[C@H](OC)C[C@@H]1O[C@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O3)C=C[C@H](C)[C@@H](C(C)C)O4)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C\C=C/[C@@H]2C)\C)O[C@H]1C WPNHOHPRXXCPRA-TVXIRPTOSA-N 0.000 claims 2
- 229960002418 Ivermectin Drugs 0.000 claims 2
- KXKVLQRXCPHEJC-UHFFFAOYSA-N Methyl acetate Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims 2
- YZBLFMPOMVTDJY-LSGXYNIPSA-N Moxidectin Chemical compound O1[C@H](C(\C)=C\C(C)C)[C@@H](C)C(=N/OC)/C[C@@]11O[C@H](C\C=C(C)\C[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 YZBLFMPOMVTDJY-LSGXYNIPSA-N 0.000 claims 2
- 229960004816 Moxidectin Drugs 0.000 claims 2
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 2
- PMDCZENCAXMSOU-UHFFFAOYSA-N N-ethylacetamide Chemical compound CCNC(C)=O PMDCZENCAXMSOU-UHFFFAOYSA-N 0.000 claims 2
- 229920000954 Polyglycolide Polymers 0.000 claims 2
- 241000206609 Porphyra Species 0.000 claims 2
- 210000002832 Shoulder Anatomy 0.000 claims 2
- 241000044136 Solenopotes Species 0.000 claims 2
- RNVYQYLELCKWAN-UHFFFAOYSA-N Solketal Chemical compound CC1(C)OCC(CO)O1 RNVYQYLELCKWAN-UHFFFAOYSA-N 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 2
- 241000607216 Toxascaris Species 0.000 claims 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N Triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 2
- 229960002622 Triacetin Drugs 0.000 claims 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 2
- 229960002346 eprinomectin Drugs 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 239000001087 glyceryl triacetate Substances 0.000 claims 2
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N iso-propanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N n-butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 2
- AMQJEAYHLZJPGS-UHFFFAOYSA-N n-pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 claims 2
- 229920000747 poly(lactic acid) polymer Polymers 0.000 claims 2
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims 2
- 229920001281 polyalkylene Polymers 0.000 claims 2
- 229920001610 polycaprolactone Polymers 0.000 claims 2
- 239000004632 polycaprolactone Substances 0.000 claims 2
- -1 polyesteramide Polymers 0.000 claims 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propanol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- MEJYDZQQVZJMPP-ULAWRXDQSA-N (3S,3aR,6R,6aR)-3,6-dimethoxy-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan Chemical compound CO[C@H]1CO[C@@H]2[C@H](OC)CO[C@@H]21 MEJYDZQQVZJMPP-ULAWRXDQSA-N 0.000 claims 1
- GUSTUIJJPMXTTI-UHFFFAOYSA-N 1-dodecylazepane Chemical compound CCCCCCCCCCCCN1CCCCCC1 GUSTUIJJPMXTTI-UHFFFAOYSA-N 0.000 claims 1
- NZJXADCEESMBPW-UHFFFAOYSA-N 1-methylsulfinyldecane Chemical compound CCCCCCCCCCS(C)=O NZJXADCEESMBPW-UHFFFAOYSA-N 0.000 claims 1
- XXJWXESWEXIICW-UHFFFAOYSA-N 2-(2-Ethoxyethoxy)ethanol Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims 1
- CUDYYMUUJHLCGZ-UHFFFAOYSA-N 2-(2-methoxypropoxy)propan-1-ol Chemical compound COC(C)COC(C)CO CUDYYMUUJHLCGZ-UHFFFAOYSA-N 0.000 claims 1
- AQIXEPGDORPWBJ-UHFFFAOYSA-N 3-Pentanol Chemical compound CCC(O)CC AQIXEPGDORPWBJ-UHFFFAOYSA-N 0.000 claims 1
- VIESAWGOYVNHLV-UHFFFAOYSA-M 3H-pyrrol-2-olate Chemical compound O=C1CC=C[N-]1 VIESAWGOYVNHLV-UHFFFAOYSA-M 0.000 claims 1
- VTDOEFXTVHCAAM-UHFFFAOYSA-N 4-methylpent-3-ene-1,2,3-triol Chemical compound CC(C)=C(O)C(O)CO VTDOEFXTVHCAAM-UHFFFAOYSA-N 0.000 claims 1
- 229950008167 Abamectin Drugs 0.000 claims 1
- 241000238876 Acari Species 0.000 claims 1
- 241000197196 Bullidae Species 0.000 claims 1
- 241000209507 Camellia Species 0.000 claims 1
- DJHJJVWPFGHIPH-OODMECLYSA-N Chitin Chemical compound O[C@@H]1C(NC(=O)C)[C@H](O)OC(CO)[C@H]1COC[C@H]1C(NC(C)=O)[C@@H](O)[C@H](COC[C@H]2C([C@@H](O)[C@H](O)C(CO)O2)NC(C)=O)C(CO)O1 DJHJJVWPFGHIPH-OODMECLYSA-N 0.000 claims 1
- 229920002101 Chitin Polymers 0.000 claims 1
- 229920001661 Chitosan Polymers 0.000 claims 1
- 241000254173 Coleoptera Species 0.000 claims 1
- 241000258922 Ctenocephalides Species 0.000 claims 1
- MMOXZBCLCQITDF-UHFFFAOYSA-N DEET Chemical compound CCN(CC)C(=O)C1=CC=CC(C)=C1 MMOXZBCLCQITDF-UHFFFAOYSA-N 0.000 claims 1
- QLFZZSKTJWDQOS-YDBLARSUSA-N Doramectin Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O3)C=C[C@H](C)[C@@H](C3CCCCC3)O4)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C QLFZZSKTJWDQOS-YDBLARSUSA-N 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 241001385463 Hepatica <moth> Species 0.000 claims 1
- 210000000554 Iris Anatomy 0.000 claims 1
- 229950000961 Latidectin Drugs 0.000 claims 1
- 210000004185 Liver Anatomy 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N Malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- 239000005918 Milbemectin Substances 0.000 claims 1
- BWCRYQGQPDBOAU-WZBVPYLGSA-N Milbemycin D Chemical compound C1C[C@H](C)[C@@H](C(C)C)O[C@@]21O[C@H](C\C=C(C)\C[C@@H](C)\C=C\C=C/1[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\1)O)C[C@H]4C2 BWCRYQGQPDBOAU-WZBVPYLGSA-N 0.000 claims 1
- CKVMAPHTVCTEMM-ALPQRHTBSA-N Milbemycin oxime Chemical compound O1[C@H](C)[C@@H](C)CC[C@@]11O[C@H](C\C=C(C)\C[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)C(=N/O)/[C@H]3OC\2)O)C[C@H]4C1.C1C[C@H](C)[C@@H](CC)O[C@@]21O[C@H](C\C=C(C)\C[C@@H](C)\C=C\C=C/1[C@]3([C@H](C(=O)O4)C=C(C)C(=N/O)/[C@H]3OC\1)O)C[C@H]4C2 CKVMAPHTVCTEMM-ALPQRHTBSA-N 0.000 claims 1
- 240000001307 Myosotis scorpioides Species 0.000 claims 1
- 241000244206 Nematoda Species 0.000 claims 1
- 241001674048 Phthiraptera Species 0.000 claims 1
- 239000004952 Polyamide Substances 0.000 claims 1
- 229920002732 Polyanhydride Polymers 0.000 claims 1
- 229920000604 Polyethylene Glycol 200 Polymers 0.000 claims 1
- 229920002556 Polyethylene Glycol 300 Polymers 0.000 claims 1
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 1
- 229920001710 Polyorthoester Polymers 0.000 claims 1
- 229960002245 Selamectin Drugs 0.000 claims 1
- 241000270708 Testudinidae Species 0.000 claims 1
- 241000244031 Toxocara Species 0.000 claims 1
- 241001467018 Typhis Species 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 150000001298 alcohols Chemical class 0.000 claims 1
- 150000001299 aldehydes Chemical class 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 230000003078 antioxidant Effects 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- RRZXIRBKKLTSOM-XPNPUAGNSA-N avermectin B1a Chemical compound C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 RRZXIRBKKLTSOM-XPNPUAGNSA-N 0.000 claims 1
- 235000018597 common camellia Nutrition 0.000 claims 1
- 229960003997 doramectin Drugs 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 150000002170 ethers Chemical class 0.000 claims 1
- 229940074076 glycerol formal Drugs 0.000 claims 1
- 201000008267 intestinal tuberculosis Diseases 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 239000003120 macrolide antibiotic agent Substances 0.000 claims 1
- 239000001630 malic acid Substances 0.000 claims 1
- 229940099690 malic acid Drugs 0.000 claims 1
- 235000011090 malic acid Nutrition 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- ZLBGSRMUSVULIE-GSMJGMFJSA-N milbemycin A3 Chemical compound O1[C@H](C)[C@@H](C)CC[C@@]11O[C@H](C\C=C(C)\C[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 ZLBGSRMUSVULIE-GSMJGMFJSA-N 0.000 claims 1
- 229940099245 milbemycin oxime Drugs 0.000 claims 1
- 235000006408 oxalic acid Nutrition 0.000 claims 1
- 229920002866 paraformaldehyde Polymers 0.000 claims 1
- 244000045947 parasites Species 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims 1
- 229920001308 poly(aminoacid) Polymers 0.000 claims 1
- 229920000141 poly(maleic anhydride) Polymers 0.000 claims 1
- 239000002745 poly(ortho ester) Substances 0.000 claims 1
- 229920002463 poly(p-dioxanone) polymer Polymers 0.000 claims 1
- 229920002627 poly(phosphazenes) Polymers 0.000 claims 1
- 229920002432 poly(vinyl methyl ether) polymer Polymers 0.000 claims 1
- 229920002647 polyamide Polymers 0.000 claims 1
- 239000011528 polyamide (building material) Substances 0.000 claims 1
- 229920000515 polycarbonate Polymers 0.000 claims 1
- 239000004417 polycarbonate Substances 0.000 claims 1
- 239000000622 polydioxanone Substances 0.000 claims 1
- 229920001855 polyketal Polymers 0.000 claims 1
- 229920002635 polyurethane Polymers 0.000 claims 1
- 239000004814 polyurethane Substances 0.000 claims 1
- AFJYYKSVHJGXSN-XHKIUTQPSA-N selamectin Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1C(/C)=C/C[C@@H](O[C@]2(O[C@@H]([C@@H](C)CC2)C2CCCCC2)C2)C[C@@H]2OC(=O)[C@@H]([C@]23O)C=C(C)C(=N/O)/[C@H]3OC\C2=C/C=C/[C@@H]1C AFJYYKSVHJGXSN-XHKIUTQPSA-N 0.000 claims 1
- 239000011877 solvent mixture Substances 0.000 claims 1
- 239000001384 succinic acid Substances 0.000 claims 1
- 229920001897 terpolymer Polymers 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
Claims (17)
- (a)治療上有効な量の少なくとも1つの生物活性剤;
(b)皮下揮発性溶媒又は皮下揮発性溶媒混合物;
(c)生物学的に許容可能なポリマー;
(d)必要に応じて、少なくとも1つの抗外部寄生虫性又は抗内部寄生虫性の点から許容可能な添加剤、賦形剤又はそれらの混合物;
(e)必要に応じて、抗酸化剤;
を含む、哺乳動物(但し、ヒトを除く)における外部寄生虫及び/又は内部寄生虫を駆除するための長期作用型注射用液体製剤。 - (a)生物活性剤が、アベルメクチン、ミルベマイシン、それらの誘導体及びそれらの混合物からなる群から選択されること;
(b)皮下揮発性溶媒が、アルコール、アルデヒド、ケトン、エーテル、エステル、アミド及びそれらの混合物からなる群から選択されること;
(c)生物学的に許容可能なポリマーが、ポリラクチド、ポリグリコリド、ポリカプロラクトン、ポリ無水物、ポリアミド、ポリウレタン、ポリエステルアミド、ポリオルソエステル、ポリジオキサノン、ポリアセタール、ポリケタール、ポリカーボネート、ポリオルソカーボネート、ポリホスファゼン、ポリヒドロキシ酪酸、ポリヒドロキシ吉草酸、ポリアルキレンシュウ酸、ポリアルキレンコハク酸、ポリ(リンゴ酸)、ポリ(アミノ酸)、ポリ(メチルビニルエーテル)、ポリ(無水マレイン酸)、キチン、キトサン、並びにそれらのコポリマー、ターポリマー、及び混合物からなる群から選択されること;
を特徴とする請求項1記載の製剤。 - (a)生物活性剤が、アバメクチン、ドラメクチン、エマメクチン、エプリノメクチン、イベルメクチン、ラチデクチン、レピメクチン、及びセラメクチン、ミルベメクチン、ミルベマイシンD、ミルベマイシンオキシムモキシデクチン並びにそれらの混合物からなる群から選択されること;
(b)皮下揮発性溶媒が、エタノール、1−プロパノール、2−プロパノール、1−ブタノール、2−ブタノール、1−ペンタノール、2−ペンタノール、3−ペンタノール、プロピレングリコール、PEG200、PEG300、PEG400、ジエチレングリコールエチルエーテル、イソプロピリデングリセロール、ジメチルイソソルビド、プロピレンカーボネート、グリセロール、アセトン、N−メチル−ピロリドン、N−ピロリドン、メチルエチルケトン(MEK)、ジメチルスルホキシド(DMSO)、1−ドデシルアザシクロヘプタン、ジプロピレングリコールメチルエーテル、酢酸メチル、酢酸エチル、乳酸エチル、ジメチルホルムアミド、N,N−ジエチル−m−トルアミド、ジメチルアセトアミド、エチルアセトアミド、テトラヒドロフラン、カプロラクタム、デシルメチルスルホキシド、トリアセチン、ソルケタール、プロピレンカーボネート、乳酸エチル及びそれらの混合物からなる群から選択されること;
(c)生物学的に許容可能なポリマーが、ポリラクチド、ポリカプロラクトン、ポリグリコリド及びそれらのコポリマーからなる群から選択されること;
を特徴とする請求項2記載の製剤。 - (a)生物活性剤が、エマメクチン、エプリノメクチン、イベルメクチン、モキシデクチン及びそれらの混合物からなる群から選択されること;
(b)皮下揮発性溶媒が、グリセロールホルマール、N−メチルピロリドン(NMP)、トリアセチン、ジメチルアセトアミド、エチルアセトアミド、酢酸エチル、ソルケタール、プロピレンカーボネート、乳酸エチル及びそれらの混合物からなる群から選択されること;
(c)生物学的に許容可能なポリマーが、ポリ(乳酸−コ−グリコール酸)コポリマー(PLGA)であること;
を特徴とする請求項3記載の製剤。 - 内部寄生虫を駆除するための請求項1記載の製剤であって、前記内部寄生虫が、アンキロストーマ属、Anecator属、回虫属、毛頭虫属、クーペリア属、ディロフィラリア属、ディクチオカウルス属、エキノコックス属、肝蛭属、捻転胃虫属、腸結節虫属、オステルタギア属、トキソカラ属、ストロンギロイデス属、トキサスカリス属、旋毛虫属、鞭虫属、毛様線虫属及びそれらの混合からなる群から選択される蠕虫であることを特徴とする請求項1〜4のいずれかに記載の製剤。
- 外部寄生虫を駆除するための請求項1記載の製剤であって、前記外部寄生虫が、クテノセファリデス属、コイタマダニ属、カクマダニ属、マダニ属、ウシマダニ属、キララマダニ属、イボマダニ属、ヒゼンダニ属、キュウセンヒゼンダニ属、ミミヒゼンダニ属、ショクヒヒゼンダニ属、ウシバエ属、ダマリニア属、ケモノホソジラミ属、ブタジラミ属、ソレノポテス属及びそれらの混合からなる群から選択されることを特徴とする請求項1〜5のいずれかに記載の製剤。
- 製剤が、少なくとも約4カ月〜約1年、少なくとも約4カ月〜約6カ月及び少なくとも約3カ月〜約5カ月からなる群から選択される期間にわたって治療効果を有することを特徴とする請求項1〜6のいずれかに記載の製剤。
- (i)生物学的に許容可能なポリマーを皮下揮発性溶媒に溶解させて溶液を形成するステップ;
(ii)治療上有効な量の生物活性剤を前記溶液に添加して製剤を形成するステップ;
を含む、請求項1記載の長期作用型注射用液体製剤の製造方法。 - 長期作用型注射用液体製剤が、約16〜約30、約18〜約24及び約24〜約30からなる群から選択されるゲージの注射針を目詰まりさせる粒子を含まないことを特徴とする、請求項8記載の方法。
- 治療上有効な量の請求項1記載の製剤を、それを必要とする哺乳動物(但し、ヒトを除く)に非経口投与することを特徴とする、哺乳動物(但し、ヒトを除く)における外部寄生虫及び/又は内部寄生虫を駆除する方法。
- 内部寄生虫が、アンキロストーマ属、Anecator属、回虫属、毛頭虫属、クーペリア属、ディロフィラリア属、ディクチオカウルス属、エキノコックス属、肝蛭属、捻転胃虫属、腸結節虫属、オステルタギア属、トキソカラ属、ストロンギロイデス属、トキサスカリス属、旋毛虫属、鞭虫属、毛様線虫属及びそれらの混合からなる群から選択されるアンテルミンスであることを特徴とする請求項10記載の方法。
- 外部寄生虫が、クテノセファリデス属、コイタマダニ属、カクマダニ属、マダニ属、ウシマダニ属、キララマダニ属、イボマダニ属、ヒゼンダニ属、キュウセンヒゼンダニ属、ミミヒゼンダニ属、ショクヒヒゼンダニ属、ウシバエ属、ダマリニア属、ケモノホソジラミ属、ブタジラミ属、ソレノポテス属及びそれらの混合からなる群から選択されることを特徴とする請求項10記載の方法。
- 哺乳動物(但し、ヒトを除く)への注射部位が、皮下であって、耳部;頸部中の両肩部間の耳根元;及び肩部からなる群から選択されることを特徴とする請求項10〜12のいずれかに記載の方法。
- 外部寄生虫及び/又は内部寄生虫の駆除が、少なくとも約4カ月〜約1年、少なくとも約4カ月〜約6カ月及び少なくとも約3カ月〜約5カ月からなる群から選択される期間にわたって治療効果を有することを特徴とする請求項10〜13のいずれかに記載の方法。
- 内部寄生虫が、オステルタギア属、捻転胃虫属及びそれらの混合からなる群から選択される蠕虫であって、請求項10記載の方法で投与されない場合、マクロライド系抗生物質にアンテルミンスが耐性を有することを特徴とする請求項10記載の方法。
- 第二の生物活性剤をさらに含むことを特徴とする請求項4記載の製剤。
- 第二の生物活性剤が、クロルスロンであることを特徴とする請求項16記載の製剤。
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-
2005
- 2005-08-19 US US11/207,980 patent/US8362086B2/en active Active
-
2006
- 2006-08-18 TR TR2019/02039T patent/TR201902039T4/tr unknown
- 2006-08-18 PT PT06801888T patent/PT1962794T/pt unknown
- 2006-08-18 HU HUE06801888A patent/HUE042225T2/hu unknown
- 2006-08-18 PL PL06801888T patent/PL1962794T3/pl unknown
- 2006-08-18 WO PCT/US2006/032407 patent/WO2007024719A2/en active Application Filing
- 2006-08-18 MX MX2008002345A patent/MX2008002345A/es active IP Right Grant
- 2006-08-18 SI SI200632314T patent/SI1962794T1/sl unknown
- 2006-08-18 EP EP18195458.7A patent/EP3479818A1/en not_active Withdrawn
- 2006-08-18 KR KR1020087006713A patent/KR101351644B1/ko active IP Right Grant
- 2006-08-18 EP EP06801888.6A patent/EP1962794B1/en active Active
- 2006-08-18 ES ES06801888T patent/ES2711233T3/es active Active
- 2006-08-18 DK DK06801888.6T patent/DK1962794T3/en active
- 2006-08-18 JP JP2008527182A patent/JP5132560B2/ja not_active Expired - Fee Related
- 2006-08-18 LT LTEP06801888.6T patent/LT1962794T/lt unknown
- 2006-08-18 CA CA2619601A patent/CA2619601C/en not_active Expired - Fee Related
- 2006-08-18 RS RS20190113A patent/RS58385B1/sr unknown
- 2006-08-18 CN CNA2006800388650A patent/CN101312710A/zh active Pending
- 2006-08-18 BR BRPI0615355A patent/BRPI0615355B8/pt active IP Right Grant
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