CN103251929A - 包含奥曲肽和两种或更多种聚丙交酯-共-乙交酯聚合物的缓释制剂 - Google Patents
包含奥曲肽和两种或更多种聚丙交酯-共-乙交酯聚合物的缓释制剂 Download PDFInfo
- Publication number
- CN103251929A CN103251929A CN2013101523825A CN201310152382A CN103251929A CN 103251929 A CN103251929 A CN 103251929A CN 2013101523825 A CN2013101523825 A CN 2013101523825A CN 201310152382 A CN201310152382 A CN 201310152382A CN 103251929 A CN103251929 A CN 103251929A
- Authority
- CN
- China
- Prior art keywords
- pharmaceutical composition
- microgranule
- plga
- octreotide
- solvent
- 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.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 33
- 229920000642 polymer Polymers 0.000 title claims abstract description 33
- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 title claims abstract description 22
- 108010016076 Octreotide Proteins 0.000 title claims abstract description 22
- 229960002700 octreotide Drugs 0.000 title claims abstract description 22
- 238000009472 formulation Methods 0.000 title claims abstract description 16
- 238000013268 sustained release Methods 0.000 title claims abstract description 5
- 239000012730 sustained-release form Substances 0.000 title claims abstract description 5
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims abstract description 35
- 150000003839 salts Chemical class 0.000 claims abstract description 15
- 239000004531 microgranule Substances 0.000 claims description 61
- 239000008194 pharmaceutical composition Substances 0.000 claims description 37
- 239000003814 drug Substances 0.000 claims description 30
- 238000002360 preparation method Methods 0.000 claims description 21
- 238000000034 method Methods 0.000 claims description 18
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 8
- 229930195725 Mannitol Natural products 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 102000055135 Vasoactive Intestinal Peptide Human genes 0.000 claims description 8
- 108010003205 Vasoactive Intestinal Peptide Proteins 0.000 claims description 8
- 239000007943 implant Substances 0.000 claims description 8
- VBUWHHLIZKOSMS-RIWXPGAOSA-N invicorp Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 VBUWHHLIZKOSMS-RIWXPGAOSA-N 0.000 claims description 8
- 239000000594 mannitol Substances 0.000 claims description 8
- 235000010355 mannitol Nutrition 0.000 claims description 8
- 238000011282 treatment Methods 0.000 claims description 8
- 239000002904 solvent Substances 0.000 claims description 7
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims description 6
- 238000004090 dissolution Methods 0.000 claims description 6
- 238000011010 flushing procedure Methods 0.000 claims description 6
- 239000000178 monomer Substances 0.000 claims description 6
- 239000002245 particle Substances 0.000 claims description 6
- 229920002959 polymer blend Polymers 0.000 claims description 6
- 239000000839 emulsion Substances 0.000 claims description 5
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 claims description 5
- 206010012735 Diarrhoea Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 208000002458 carcinoid tumor Diseases 0.000 claims description 4
- 230000001804 emulsifying effect Effects 0.000 claims description 4
- 230000007774 longterm Effects 0.000 claims description 4
- 239000003791 organic solvent mixture Substances 0.000 claims description 4
- 238000005406 washing Methods 0.000 claims description 4
- 229940071643 prefilled syringe Drugs 0.000 claims description 3
- 238000000935 solvent evaporation Methods 0.000 claims description 3
- 238000000638 solvent extraction Methods 0.000 claims description 3
- 239000003381 stabilizer Substances 0.000 claims description 3
- 230000001954 sterilising effect Effects 0.000 claims description 3
- 238000004659 sterilization and disinfection Methods 0.000 claims description 3
- 208000034189 Sclerosis Diseases 0.000 claims description 2
- 239000003708 ampul Substances 0.000 claims description 2
- 238000012423 maintenance Methods 0.000 claims description 2
- 238000011418 maintenance treatment Methods 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 12
- 229940079593 drug Drugs 0.000 description 12
- 239000000725 suspension Substances 0.000 description 11
- 239000000243 solution Substances 0.000 description 10
- 150000002148 esters Chemical class 0.000 description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
- 239000002253 acid Substances 0.000 description 6
- 230000037058 blood plasma level Effects 0.000 description 6
- 230000003578 releasing effect Effects 0.000 description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 5
- 238000011068 loading method Methods 0.000 description 5
- 239000011734 sodium Substances 0.000 description 5
- 239000007787 solid Substances 0.000 description 5
- 239000004372 Polyvinyl alcohol Substances 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 4
- 238000004108 freeze drying Methods 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- -1 oxygen ethylene-oxypropylene Chemical group 0.000 description 4
- 229920001983 poloxamer Polymers 0.000 description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 description 4
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 4
- BYEAHWXPCBROCE-UHFFFAOYSA-N 1,1,1,3,3,3-hexafluoropropan-2-ol Chemical compound FC(F)(F)C(O)C(F)(F)F BYEAHWXPCBROCE-UHFFFAOYSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 229920001214 Polysorbate 60 Polymers 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000008367 deionised water Substances 0.000 description 3
- 229910021641 deionized water Inorganic materials 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 239000011521 glass Substances 0.000 description 3
- 239000008103 glucose Substances 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 229920000136 polysorbate Polymers 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- KFWJVABDRRDUHY-XJQYZYIXSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1.C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 KFWJVABDRRDUHY-XJQYZYIXSA-N 0.000 description 2
- GHCZTIFQWKKGSB-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;phosphoric acid Chemical compound OP(O)(O)=O.OC(=O)CC(O)(C(O)=O)CC(O)=O GHCZTIFQWKKGSB-UHFFFAOYSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 2
- 102000007327 Protamines Human genes 0.000 description 2
- 108010007568 Protamines Proteins 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N 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 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 2
- 239000003513 alkali Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 239000008121 dextrose Substances 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 238000001914 filtration Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 229940071826 hydroxyethyl cellulose Drugs 0.000 description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000011859 microparticle Substances 0.000 description 2
- 230000002572 peristaltic effect Effects 0.000 description 2
- RLLPVAHGXHCWKJ-UHFFFAOYSA-N permethrin Chemical compound CC1(C)C(C=C(Cl)Cl)C1C(=O)OCC1=CC=CC(OC=2C=CC=CC=2)=C1 RLLPVAHGXHCWKJ-UHFFFAOYSA-N 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 229960000502 poloxamer Drugs 0.000 description 2
- 229920000747 poly(lactic acid) Polymers 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 229940048914 protamine Drugs 0.000 description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 150000005846 sugar alcohols Polymers 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 229920002449 FKM Polymers 0.000 description 1
- 206010016825 Flushing Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 241000206672 Gelidium Species 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 108010039918 Polylysine Proteins 0.000 description 1
- 229920001219 Polysorbate 40 Polymers 0.000 description 1
- 229920002642 Polysorbate 65 Polymers 0.000 description 1
- 229920002651 Polysorbate 85 Polymers 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- FMRLDPWIRHBCCC-UHFFFAOYSA-L Zinc carbonate Chemical compound [Zn+2].[O-]C([O-])=O FMRLDPWIRHBCCC-UHFFFAOYSA-L 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 150000001412 amines Chemical group 0.000 description 1
- 239000008365 aqueous carrier Substances 0.000 description 1
- 239000008135 aqueous vehicle Substances 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 229920002988 biodegradable polymer Polymers 0.000 description 1
- 239000004621 biodegradable polymer Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000000337 buffer salt Substances 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- UGMCXQCYOVCMTB-UHFFFAOYSA-K dihydroxy(stearato)aluminium Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[Al](O)O UGMCXQCYOVCMTB-UHFFFAOYSA-K 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 125000004185 ester group Chemical group 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 150000008282 halocarbons Chemical class 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 229940102213 injectable suspension Drugs 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 229910017053 inorganic salt Inorganic materials 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 108010059642 isinglass Proteins 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 239000006193 liquid solution Substances 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 1
- 239000000347 magnesium hydroxide Substances 0.000 description 1
- 229910001862 magnesium hydroxide Inorganic materials 0.000 description 1
- 238000003760 magnetic stirring Methods 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 229910052627 muscovite Inorganic materials 0.000 description 1
- 229920005615 natural polymer Polymers 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical group C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 description 1
- 239000013618 particulate matter Substances 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 229920000656 polylysine Polymers 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 1
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 239000001816 polyoxyethylene sorbitan tristearate Substances 0.000 description 1
- 235000010988 polyoxyethylene sorbitan tristearate Nutrition 0.000 description 1
- 229940101027 polysorbate 40 Drugs 0.000 description 1
- 229940113124 polysorbate 60 Drugs 0.000 description 1
- 229940099511 polysorbate 65 Drugs 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229940113171 polysorbate 85 Drugs 0.000 description 1
- 229920002689 polyvinyl acetate Polymers 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 239000007974 sodium acetate buffer Substances 0.000 description 1
- 239000006104 solid solution Substances 0.000 description 1
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical class C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 230000003068 static effect Effects 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000011667 zinc carbonate Substances 0.000 description 1
- 235000004416 zinc carbonate Nutrition 0.000 description 1
- 229910000010 zinc carbonate Inorganic materials 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/31—Somatostatins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5015—Organic compounds, e.g. fats, sugars
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5089—Processes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
- A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Zoology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Inorganic Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
- Polyesters Or Polycarbonates (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0526247A GB0526247D0 (en) | 2005-12-22 | 2005-12-22 | Organic compounds |
| GB0526247.2 | 2005-12-22 | ||
| EP06119086 | 2006-08-17 | ||
| EP06119086.4 | 2006-08-17 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2006800487961A Division CN101346130A (zh) | 2005-12-22 | 2006-12-20 | 包含奥曲肽和两种或更多种聚丙交酯-共-乙交酯聚合物的缓释制剂 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103251929A true CN103251929A (zh) | 2013-08-21 |
Family
ID=37772904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013101523825A Pending CN103251929A (zh) | 2005-12-22 | 2006-12-20 | 包含奥曲肽和两种或更多种聚丙交酯-共-乙交酯聚合物的缓释制剂 |
Country Status (22)
| Country | Link |
|---|---|
| US (7) | US20090004283A1 (enExample) |
| EP (3) | EP2359809B1 (enExample) |
| JP (4) | JP2009520727A (enExample) |
| KR (5) | KR20130024987A (enExample) |
| CN (1) | CN103251929A (enExample) |
| AR (1) | AR058591A1 (enExample) |
| AU (1) | AU2006328950B2 (enExample) |
| BR (2) | BR122019027412B8 (enExample) |
| CA (1) | CA2631811C (enExample) |
| CL (1) | CL2018003398A1 (enExample) |
| EC (1) | ECSP088560A (enExample) |
| ES (2) | ES2755032T3 (enExample) |
| IL (1) | IL191842A0 (enExample) |
| IN (1) | IN2015DN03936A (enExample) |
| MA (1) | MA30064B1 (enExample) |
| NO (1) | NO20082988L (enExample) |
| PE (1) | PE20071139A1 (enExample) |
| PL (2) | PL2359809T3 (enExample) |
| PT (2) | PT1968549E (enExample) |
| RU (1) | RU2464972C2 (enExample) |
| TW (2) | TWI469788B (enExample) |
| WO (1) | WO2007071395A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111214643A (zh) * | 2020-03-11 | 2020-06-02 | 苏州善湾生物医药科技有限公司 | 一种基于皮下凝胶缓释的奥曲肽组合物、制备方法及应用 |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2611020T3 (es) | 2007-06-06 | 2017-05-04 | Debiopharm Research & Manufacturing Sa | Composición farmacéutica de liberación lenta hecha de micropartículas |
| US8470360B2 (en) * | 2008-04-18 | 2013-06-25 | Warsaw Orthopedic, Inc. | Drug depots having different release profiles for reducing, preventing or treating pain and inflammation |
| ES2324009B1 (es) * | 2007-11-23 | 2010-05-21 | Gp Pharm S.A. | Composicion farmaceutica de liberacion sostenida de somatostatina o un analogo suyo. |
| WO2009095450A1 (en) * | 2008-01-30 | 2009-08-06 | Novartis Ag | Sustained release formulation comprising octreotide and three linear polylactide-co-glycolide polymers |
| AU2013201877B2 (en) * | 2008-01-30 | 2015-01-29 | Novartis Ag | Sustained release formulation comprising octreotide and three linear polylactide-co-glycolide polymers |
| ES2629131T3 (es) * | 2008-09-17 | 2017-08-07 | Chiasma Inc. | Composiciones farmacéuticas y métodos de suministro relacionados. |
| AU2015201581B2 (en) * | 2008-09-17 | 2017-03-09 | Amryt Endo, Inc. | Pharmaceutical Compositions and Related Methods of Delivery |
| US20100151033A1 (en) * | 2008-12-15 | 2010-06-17 | Novartis Ag | Octreotide depot formulation with constantly high exposure levels |
| JP2012515791A (ja) * | 2009-01-23 | 2012-07-12 | サーモディクス ファーマシューティカルズ， インコーポレイテッド | ポリマー混成物由来の放出制御システム |
| US20120022137A1 (en) * | 2010-07-21 | 2012-01-26 | Rivers Hongwen M | METHOD OF CONTROLLING INITIAL DRUG RELEASE OF siRNA FROM SUSTAINED-RELEASE IMPLANTS |
| GB201016436D0 (en) | 2010-09-30 | 2010-11-17 | Q Chip Ltd | Method of making solid beads |
| GB201016433D0 (en) | 2010-09-30 | 2010-11-17 | Q Chip Ltd | Apparatus and method for making solid beads |
| WO2012083026A1 (en) * | 2010-12-15 | 2012-06-21 | Evonik Degussa Corporation | Branched polyol polyesters, blends and pharmaceutical formulations comprising same |
| CN104127385B (zh) * | 2011-04-25 | 2017-08-04 | 山东绿叶制药有限公司 | 利培酮缓释微球组合物 |
| CN102488619B (zh) * | 2011-12-05 | 2014-08-06 | 上海交通大学 | 连续生产艾塞那肽微球的装置及控制微球释放速度的方法 |
| WO2016084849A1 (ja) * | 2014-11-25 | 2016-06-02 | Cbc株式会社 | ヤヌス微粒子及びその製造方法 |
| RS66942B1 (sr) | 2015-02-03 | 2025-07-31 | Amryt Endo Inc | Lečenje akromegalije oralnim oktreotidom |
| WO2016208685A1 (ja) * | 2015-06-26 | 2016-12-29 | オリンパス株式会社 | 内視鏡電源供給システム |
| US12396951B2 (en) * | 2016-12-27 | 2025-08-26 | Upexmed Co. Ltd. | Prevention of local tumor recurrence following surgery using sustainedand/or delayed release of medicaments contained in micro-particles |
| KR102142026B1 (ko) * | 2017-05-31 | 2020-08-06 | 주식회사 대웅제약 | 방출제어가 용이한 서방성 약물 미립자의 제조방법 |
| MX2022002980A (es) | 2019-09-16 | 2022-04-06 | Amgen Inc | Metodo para la esterilizacion externa de un dispositivo de suministro de farmacos. |
| KR20220163417A (ko) * | 2020-05-08 | 2022-12-09 | 엠. 테크닉 가부시키가이샤 | 주제가 균일하게 분산된 마이크로스피어 및 그것을 함유하는 서방성 제제 |
| JP6810502B1 (ja) * | 2020-05-08 | 2021-01-06 | エム・テクニック株式会社 | 生理活性物質が均一に分散されたマイクロスフェアー及びそれを含有する徐放性製剤 |
| KR20220163418A (ko) * | 2020-05-08 | 2022-12-09 | 엠. 테크닉 가부시키가이샤 | 생리 활성 물질이 균일하게 분산된 마이크로스피어 및 그것을 함유하는 서방성 제제 |
| US11141457B1 (en) | 2020-12-28 | 2021-10-12 | Amryt Endo, Inc. | Oral octreotide therapy and contraceptive methods |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) * | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| ATE2512T1 (de) * | 1979-11-27 | 1983-03-15 | Sandoz Ag | Polypeptide, verfahren zu ihrer herstellung, pharmazeutische zusammensetzungen, die diese polypeptide enthalten, und ihre verwendung. |
| US4675189A (en) * | 1980-11-18 | 1987-06-23 | Syntex (U.S.A.) Inc. | Microencapsulation of water soluble active polypeptides |
| US4897268A (en) * | 1987-08-03 | 1990-01-30 | Southern Research Institute | Drug delivery system and method of making the same |
| PH30995A (en) * | 1989-07-07 | 1997-12-23 | Novartis Inc | Sustained release formulations of water soluble peptides. |
| US5538739A (en) * | 1989-07-07 | 1996-07-23 | Sandoz Ltd. | Sustained release formulations of water soluble peptides |
| HU221294B1 (en) * | 1989-07-07 | 2002-09-28 | Novartis Ag | Process for producing retarde compositions containing the active ingredient in a polymeric carrier |
| MY107937A (en) * | 1990-02-13 | 1996-06-29 | Takeda Chemical Industries Ltd | Prolonged release microcapsules. |
| CH683149A5 (fr) | 1991-07-22 | 1994-01-31 | Debio Rech Pharma Sa | Procédé pour la préparation de microsphères en matériau polymère biodégradable. |
| WO1993015722A1 (en) * | 1992-02-07 | 1993-08-19 | Syntex (Usa) Inc. | Controlled delivery of pharmaceuticals from preformed porous microparticles |
| KR100260632B1 (ko) * | 1992-12-28 | 2000-07-01 | 성재갑 | 이식형 소마토트로핀 조성물 |
| US5603960A (en) * | 1993-05-25 | 1997-02-18 | O'hagan; Derek T. | Preparation of microparticles and method of immunization |
| US5417982A (en) * | 1994-02-17 | 1995-05-23 | Modi; Pankaj | Controlled release of drugs or hormones in biodegradable polymer microspheres |
| US6447796B1 (en) * | 1994-05-16 | 2002-09-10 | The United States Of America As Represented By The Secretary Of The Army | Sustained release hydrophobic bioactive PLGA microspheres |
| KR20000057693A (ko) * | 1996-12-20 | 2000-09-25 | 다케다 야쿠힌 고교 가부시키가이샤 | 지효성 제제의 제조 방법 |
| AR012448A1 (es) * | 1997-04-18 | 2000-10-18 | Ipsen Pharma Biotech | Composicion en forma de microcapsulas o de implantes que comprende un excipiente biodegradable, polimero o co-polimero, o una mezcla de talesexcipientes, y una sustancia activa o una mezcla de sustancias activas, procedimiento para la preparacion de una sustancia soluble en agua de elevada |
| WO1998055101A1 (fr) * | 1997-06-04 | 1998-12-10 | Debio Recherche Pharmaceutique S.A. | Implants pour la liberation controlee de principes pharmaceutiquement actifs et procede pour leur fabrication |
| ES2169980B1 (es) * | 1999-12-17 | 2003-11-01 | Lipotec Sa | Microcapsulas para la liberacion prolongada de farmacos. |
| KR100392501B1 (ko) * | 2000-06-28 | 2003-07-22 | 동국제약 주식회사 | 다중 에멀젼법에 의한 서방출성 미립구의 제조방법 |
| EP1344520B1 (en) * | 2002-03-15 | 2007-10-03 | Alrise Biosystems GmbH | Microparticles and method for their production |
| CN1713890A (zh) * | 2002-11-06 | 2005-12-28 | 阿尔萨公司 | 控释储库制剂 |
| US20040097419A1 (en) * | 2002-11-19 | 2004-05-20 | Holger Petersen | Organic compounds |
| KR100466637B1 (ko) * | 2003-06-26 | 2005-01-13 | 주식회사 펩트론 | 서방성 미립구의 혼합 제형을 연속한 단일 공정으로제조하는 방법 |
| CA2819769C (en) * | 2003-07-18 | 2016-06-28 | Oakwood Laboratories, L.L.C. | Prevention of molecular weight reduction of the polymer, impurity formation and gelling in polymer compositions |
| WO2005009357A2 (en) * | 2003-07-23 | 2005-02-03 | Pr Pharmaceuticals, Inc. | Controlled release compositions |
| MY158342A (en) * | 2003-11-14 | 2016-09-30 | Novartis Ag | Pharmaceutical composition |
| US7964219B2 (en) * | 2004-08-12 | 2011-06-21 | Qps, Llc | Pharmaceutical compositions for controlled release delivery of biologically active compounds |
-
2006
- 2006-12-20 WO PCT/EP2006/012313 patent/WO2007071395A1/en not_active Ceased
- 2006-12-20 AU AU2006328950A patent/AU2006328950B2/en active Active
- 2006-12-20 IN IN3936DEN2015 patent/IN2015DN03936A/en unknown
- 2006-12-20 KR KR1020137004518A patent/KR20130024987A/ko not_active Ceased
- 2006-12-20 CN CN2013101523825A patent/CN103251929A/zh active Pending
- 2006-12-20 KR KR1020147031146A patent/KR20140133968A/ko not_active Ceased
- 2006-12-20 PT PT68410596T patent/PT1968549E/pt unknown
- 2006-12-20 PL PL10175382T patent/PL2359809T3/pl unknown
- 2006-12-20 RU RU2008129626/15A patent/RU2464972C2/ru active
- 2006-12-20 PE PE2006001665A patent/PE20071139A1/es not_active Application Discontinuation
- 2006-12-20 JP JP2008546248A patent/JP2009520727A/ja active Pending
- 2006-12-20 BR BR122019027412A patent/BR122019027412B8/pt active IP Right Grant
- 2006-12-20 PL PL06841059T patent/PL1968549T3/pl unknown
- 2006-12-20 AR ARP060105668A patent/AR058591A1/es unknown
- 2006-12-20 KR KR1020137004517A patent/KR101458728B1/ko active Active
- 2006-12-20 US US12/158,345 patent/US20090004283A1/en not_active Abandoned
- 2006-12-20 EP EP10175382.0A patent/EP2359809B1/en active Active
- 2006-12-20 KR KR1020137004520A patent/KR20130024988A/ko not_active Ceased
- 2006-12-20 EP EP19188892.4A patent/EP3603623A1/en not_active Withdrawn
- 2006-12-20 EP EP06841059.6A patent/EP1968549B1/en active Active
- 2006-12-20 CA CA2631811A patent/CA2631811C/en active Active
- 2006-12-20 ES ES10175382T patent/ES2755032T3/es active Active
- 2006-12-20 BR BRPI0620063A patent/BRPI0620063B8/pt active IP Right Grant
- 2006-12-20 PT PT101753820T patent/PT2359809T/pt unknown
- 2006-12-20 ES ES06841059.6T patent/ES2492641T3/es active Active
- 2006-12-20 KR KR1020087014985A patent/KR101245919B1/ko active Active
- 2006-12-21 TW TW95148218A patent/TWI469788B/zh active
- 2006-12-21 TW TW103107772A patent/TWI468172B/zh active
-
2008
- 2008-05-29 IL IL191842A patent/IL191842A0/en unknown
- 2008-06-18 MA MA31048A patent/MA30064B1/fr unknown
- 2008-06-19 EC EC2008008560A patent/ECSP088560A/es unknown
- 2008-07-02 NO NO20082988A patent/NO20082988L/no not_active Application Discontinuation
-
2013
- 2013-04-25 JP JP2013092845A patent/JP6239851B2/ja active Active
-
2014
- 2014-10-08 JP JP2014207464A patent/JP6178772B2/ja active Active
- 2014-10-16 US US14/516,016 patent/US20150037420A1/en not_active Abandoned
-
2015
- 2015-12-22 US US14/977,801 patent/US20160120935A1/en not_active Abandoned
-
2016
- 2016-06-09 JP JP2016115579A patent/JP2016216467A/ja not_active Withdrawn
-
2018
- 2018-01-17 US US15/873,473 patent/US20180140662A1/en not_active Abandoned
- 2018-11-29 CL CL2018003398A patent/CL2018003398A1/es unknown
-
2020
- 2020-03-10 US US16/813,864 patent/US20200206306A1/en not_active Abandoned
-
2022
- 2022-06-07 US US17/834,014 patent/US20220296675A1/en not_active Abandoned
-
2024
- 2024-11-22 US US18/956,119 patent/US20250082718A1/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111214643A (zh) * | 2020-03-11 | 2020-06-02 | 苏州善湾生物医药科技有限公司 | 一种基于皮下凝胶缓释的奥曲肽组合物、制备方法及应用 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103251929A (zh) | 包含奥曲肽和两种或更多种聚丙交酯-共-乙交酯聚合物的缓释制剂 | |
| CN105233251A (zh) | 有恒定高暴露水平的奥曲肽贮库制剂 | |
| CN101917969A (zh) | 包含奥曲肽和三种线形聚丙交酯-共-乙交酯聚合物的缓释制剂 | |
| CN101511341A (zh) | 芳香酶抑制剂的缓释制剂 | |
| CN101346130A (zh) | 包含奥曲肽和两种或更多种聚丙交酯-共-乙交酯聚合物的缓释制剂 | |
| AU2013201877B2 (en) | Sustained release formulation comprising octreotide and three linear polylactide-co-glycolide polymers |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination |