ES2664818T3 - Micelas - Google Patents
Micelas Download PDFInfo
- Publication number
- ES2664818T3 ES2664818T3 ES12154683.2T ES12154683T ES2664818T3 ES 2664818 T3 ES2664818 T3 ES 2664818T3 ES 12154683 T ES12154683 T ES 12154683T ES 2664818 T3 ES2664818 T3 ES 2664818T3
- Authority
- ES
- Spain
- Prior art keywords
- micelles
- aqueous solution
- hydrodynamic diameter
- solution
- compound
- 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.)
- Expired - Lifetime
Links
- 239000000693 micelle Substances 0.000 title claims abstract description 100
- 150000001875 compounds Chemical class 0.000 claims abstract description 73
- 159000000000 sodium salts Chemical class 0.000 claims abstract description 25
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 19
- 238000004108 freeze drying Methods 0.000 claims abstract description 6
- 239000007864 aqueous solution Substances 0.000 claims description 75
- 239000000243 solution Substances 0.000 claims description 39
- 230000007935 neutral effect Effects 0.000 claims description 34
- 238000000034 method Methods 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 31
- 239000002253 acid Substances 0.000 claims description 22
- 229910021645 metal ion Inorganic materials 0.000 claims description 20
- 239000012670 alkaline solution Substances 0.000 claims description 17
- 238000002360 preparation method Methods 0.000 claims description 14
- -1 basic metal salt Chemical class 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 9
- 239000007853 buffer solution Substances 0.000 claims description 7
- 229910052728 basic metal Inorganic materials 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- 239000000725 suspension Substances 0.000 claims description 6
- 239000007900 aqueous suspension Substances 0.000 claims description 5
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 3
- 239000008176 lyophilized powder Substances 0.000 claims description 3
- 231100000252 nontoxic Toxicity 0.000 claims description 3
- 230000003000 nontoxic effect Effects 0.000 claims description 3
- 230000002378 acidificating effect Effects 0.000 description 30
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 21
- 239000000825 pharmaceutical preparation Substances 0.000 description 19
- 229940127557 pharmaceutical product Drugs 0.000 description 18
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 15
- 239000011734 sodium Substances 0.000 description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- 125000000217 alkyl group Chemical group 0.000 description 9
- 239000000872 buffer Substances 0.000 description 9
- 229910052751 metal Inorganic materials 0.000 description 8
- 239000002184 metal Substances 0.000 description 8
- 230000008859 change Effects 0.000 description 7
- 238000009472 formulation Methods 0.000 description 7
- 239000011780 sodium chloride Substances 0.000 description 7
- 238000003860 storage Methods 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 239000002158 endotoxin Substances 0.000 description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 6
- 229920006008 lipopolysaccharide Polymers 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 5
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 4
- 230000002776 aggregation Effects 0.000 description 4
- 238000004220 aggregation Methods 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 238000001802 infusion Methods 0.000 description 4
- 238000002347 injection Methods 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 239000008055 phosphate buffer solution Substances 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid group Chemical class S(O)(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 4
- 241000894006 Bacteria Species 0.000 description 3
- 208000037487 Endotoxemia Diseases 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- 206010040047 Sepsis Diseases 0.000 description 3
- 239000003929 acidic solution Substances 0.000 description 3
- 150000007513 acids Chemical class 0.000 description 3
- 239000007859 condensation product Substances 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- 238000009792 diffusion process Methods 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 3
- 230000003993 interaction Effects 0.000 description 3
- 238000001990 intravenous administration Methods 0.000 description 3
- GZQKNULLWNGMCW-PWQABINMSA-N lipid A (E. coli) Chemical class O1[C@H](CO)[C@@H](OP(O)(O)=O)[C@H](OC(=O)C[C@@H](CCCCCCCCCCC)OC(=O)CCCCCCCCCCCCC)[C@@H](NC(=O)C[C@@H](CCCCCCCCCCC)OC(=O)CCCCCCCCCCC)[C@@H]1OC[C@@H]1[C@@H](O)[C@H](OC(=O)C[C@H](O)CCCCCCCCCCC)[C@@H](NC(=O)C[C@H](O)CCCCCCCCCCC)[C@@H](OP(O)(O)=O)O1 GZQKNULLWNGMCW-PWQABINMSA-N 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 235000011007 phosphoric acid Nutrition 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 239000000375 suspending agent Substances 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 2
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 description 2
- 206010040070 Septic Shock Diseases 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 2
- 238000000149 argon plasma sintering Methods 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 239000002270 dispersing agent Substances 0.000 description 2
- 235000011167 hydrochloric acid Nutrition 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 2
- 230000002209 hydrophobic effect Effects 0.000 description 2
- 238000001361 intraarterial administration Methods 0.000 description 2
- 238000010253 intravenous injection Methods 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 239000000178 monomer Substances 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 239000000346 nonvolatile oil Substances 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 150000003016 phosphoric acids Chemical class 0.000 description 2
- 238000005057 refrigeration Methods 0.000 description 2
- 239000008174 sterile solution Substances 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 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 description 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 description 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- 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
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- 208000009304 Acute Kidney Injury Diseases 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
- 102000014914 Carrier Proteins Human genes 0.000 description 1
- 108010078791 Carrier Proteins Proteins 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
- 206010014824 Endotoxic shock Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 1
- 239000005642 Oleic acid Substances 0.000 description 1
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 1
- 206010037660 Pyrexia Diseases 0.000 description 1
- 208000033626 Renal failure acute Diseases 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 1
- 239000007983 Tris buffer Chemical class 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 235000011054 acetic acid Nutrition 0.000 description 1
- 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 1
- 150000001243 acetic acids Chemical class 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000011149 active material Substances 0.000 description 1
- 201000011040 acute kidney failure Diseases 0.000 description 1
- 208000012998 acute renal failure Diseases 0.000 description 1
- 125000004423 acyloxy group Chemical group 0.000 description 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 125000001931 aliphatic group Chemical group 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 125000002947 alkylene group Chemical group 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 239000003637 basic solution Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 150000004653 carbonic acids Chemical class 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 239000007979 citrate buffer Substances 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid group Chemical class C(CC(O)(C(=O)O)CC(=O)O)(=O)O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
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- 239000006185 dispersion Substances 0.000 description 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000002587 enol group Chemical group 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 150000002367 halogens Chemical group 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 150000004679 hydroxides Chemical class 0.000 description 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 230000036543 hypotension Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 150000004668 long chain fatty acids Chemical group 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
- 238000007726 management method Methods 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 230000035800 maturation Effects 0.000 description 1
- 229960003194 meglumine Drugs 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 231100000344 non-irritating Toxicity 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 125000000962 organic group Chemical group 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N p-hydroxybenzoic acid propyl ester Natural products CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 150000003003 phosphines Chemical class 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 238000005381 potential energy Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000008085 renal dysfunction Effects 0.000 description 1
- 230000036303 septic shock Effects 0.000 description 1
- 208000013223 septicemia Diseases 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
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- 238000007920 subcutaneous administration Methods 0.000 description 1
- 150000003455 sulfinic acids Chemical class 0.000 description 1
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- 229940095064 tartrate Drugs 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 230000005945 translocation Effects 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
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Classifications
-
- 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
- A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7024—Esters of saccharides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- 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
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Dispersion Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Biophysics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18376800P | 2000-02-18 | 2000-02-18 | |
| US183768P | 2000-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2664818T3 true ES2664818T3 (es) | 2018-04-23 |
Family
ID=22674206
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12154683.2T Expired - Lifetime ES2664818T3 (es) | 2000-02-18 | 2001-02-20 | Micelas |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US6906042B2 (enExample) |
| EP (2) | EP2452684B1 (enExample) |
| JP (2) | JP4959085B2 (enExample) |
| KR (1) | KR100841813B1 (enExample) |
| AU (2) | AU2001238507C9 (enExample) |
| CA (1) | CA2400371C (enExample) |
| ES (1) | ES2664818T3 (enExample) |
| HK (1) | HK1052872A1 (enExample) |
| IL (2) | IL151314A0 (enExample) |
| WO (1) | WO2001060382A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030130212A1 (en) * | 1999-01-14 | 2003-07-10 | Rossignol Daniel P. | Administration of an anti-endotoxin drug by intravenous infusion |
| AU2001238507C9 (en) * | 2000-02-18 | 2005-07-07 | Eisai R&D Management Co., Ltd. | Micelles |
| JP4366081B2 (ja) * | 2001-05-22 | 2009-11-18 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 高度に精製されたアンチエンドトキシン化合物 |
| US7727974B2 (en) | 2001-08-10 | 2010-06-01 | Eisai R & D Management Co., Ltd. | Methods of reducing the severity of mucositis |
| WO2003013440A2 (en) * | 2001-08-10 | 2003-02-20 | Eisai Co., Ltd. | Treatment and prevention of heat shock protein-associated diseases and conditions |
| WO2003082303A1 (en) * | 2002-03-29 | 2003-10-09 | Wisconsin Alumni Research Foundation | Polymeric micelle formulations of hydrophobic compounds and methods |
| WO2004034992A2 (en) * | 2002-10-15 | 2004-04-29 | Wisconsin Alumni Research Foundation | Encapsulation and deaggregation of polyene antibiotics using poly(ethylene glycol)-phospholipid micelles |
| CA2536283A1 (en) * | 2003-08-20 | 2005-03-03 | Ajinomoto Co., Inc. | Pharmaceutical preparations having an improved solubility |
| ATE446581T1 (de) * | 2004-03-12 | 2009-11-15 | Trinity College Dublin | Magnetoresistives medium |
| WO2007026675A1 (ja) * | 2005-08-31 | 2007-03-08 | Eisai R & D Management Co., Ltd. | リピッドａ類縁体の製造方法 |
| US20070249572A1 (en) * | 2005-12-20 | 2007-10-25 | Verus Pharmaceuticals, Inc. | Systems and methods for the delivery of corticosteroids |
| US20070178049A1 (en) * | 2005-12-20 | 2007-08-02 | Verus Pharmaceuticals, Inc. | Systems and methods for the delivery of corticosteroids having an enhanced pharmacokinetic profile |
| US20070197486A1 (en) * | 2005-12-20 | 2007-08-23 | Verus Pharmaceuticals, Inc. | Methods and systems for the delivery of corticosteroids |
| US20070160542A1 (en) * | 2005-12-20 | 2007-07-12 | Verus Pharmaceuticals, Inc. | Methods and systems for the delivery of corticosteroids having an enhanced pharmacokinetic profile |
| US20070185066A1 (en) * | 2005-12-20 | 2007-08-09 | Verus Pharmaceuticals, Inc. | Systems and methods for the delivery of corticosteroids |
| JP2009526619A (ja) * | 2006-02-15 | 2009-07-23 | ティカ レーケメデル アーベー | 質量減量を伴うコルチコステロイドの滅菌 |
| BR112014024139A8 (pt) | 2012-03-28 | 2018-01-16 | Univ Maryland | administração de eritoran ou sais farmaceuticamente aceitáveis do mesmo para tratar infecções de ortomixovírus |
| WO2018053073A1 (en) | 2016-09-16 | 2018-03-22 | Eisai R&D Management Co., Ltd. | Method of use of eritoran as a tlr4 antagonist for treatment of ebola and marburg disease |
| BR112021010717A2 (pt) | 2018-12-17 | 2021-08-31 | Eisai R&D Management Co., Ltd. | Formulação que compreende lipossomas |
| US11198831B2 (en) | 2019-01-31 | 2021-12-14 | Kvi Llc | Lubricant for a device |
| WO2021207218A1 (en) | 2020-04-06 | 2021-10-14 | Eisai R&D Management Co., Ltd. | Treatment of nidovirales infection with eritoran |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5530113A (en) | 1991-10-11 | 1996-06-25 | Eisai Co., Ltd. | Anti-endotoxin compounds |
| US6417172B1 (en) | 1995-06-05 | 2002-07-09 | Eisai Co., Ltd. | Prevention and treatment of pulmonary bacterial infection or symptomatic pulmonary exposure to endotoxin by inhalation of antiendotoxin drugs |
| US5681824A (en) | 1995-06-05 | 1997-10-28 | Eisai Co., Ltd. | Substituted liposaccharides useful in the treatment and prevention of endotoxemia |
| AU7254396A (en) * | 1995-09-29 | 1997-04-17 | Eisai Research Institute | Method for treating alcoholic liver disease |
| JP4326030B2 (ja) * | 1996-07-03 | 2009-09-02 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | リピッドａ類縁体含有注射用製剤及びその製造方法 |
| US6235724B1 (en) * | 1996-07-03 | 2001-05-22 | Eisai Co., Ltd. | Injections containing lipid a analogues and process for the preparation thereof |
| US6495532B1 (en) | 1997-03-19 | 2002-12-17 | Sky High, Llc | Compositions containing lysophosphotidic acids which inhibit apoptosis and uses thereof |
| JP2002501540A (ja) | 1997-05-23 | 2002-01-15 | エーザイ株式会社 | 製薬製剤を調製するための方法 |
| US6437006B1 (en) | 1999-09-27 | 2002-08-20 | American Cyanamid Company | Pharmaceutical carrier formulation |
| EP1250141A4 (en) | 2000-01-14 | 2007-05-16 | Eisai Co Ltd | Prevention and treatment of endotoxemia and related complications in the field of surgery |
| AU2001238507C9 (en) | 2000-02-18 | 2005-07-07 | Eisai R&D Management Co., Ltd. | Micelles |
| US6861512B2 (en) | 2000-03-01 | 2005-03-01 | Eisai Co., Ltd. | Separation of olefinic isomers |
| US20030105033A1 (en) | 2000-06-09 | 2003-06-05 | Rossignol Daniel P. | Administration of an anti-endotoxin drug by bolus or intermittent intravenous infusion |
| JP4179881B2 (ja) | 2000-12-06 | 2008-11-12 | エーザイ株式会社 | 凍結乾燥ケークの抵抗を測定するためのシステム及び方法 |
| WO2002089743A2 (en) | 2001-05-09 | 2002-11-14 | The Regents Of The University Of Michigan | Use of compositions for treating rosacea |
| US7727974B2 (en) | 2001-08-10 | 2010-06-01 | Eisai R & D Management Co., Ltd. | Methods of reducing the severity of mucositis |
| AU2004218358A1 (en) | 2003-03-05 | 2004-09-16 | Eisai R&D Management Co., Ltd. | Compositions and methods for preventing and treating endotoxin-related diseases and conditions |
-
2001
- 2001-02-20 AU AU2001238507A patent/AU2001238507C9/en not_active Expired
- 2001-02-20 IL IL15131401A patent/IL151314A0/xx active IP Right Grant
- 2001-02-20 WO PCT/US2001/005297 patent/WO2001060382A1/en not_active Ceased
- 2001-02-20 EP EP12154683.2A patent/EP2452684B1/en not_active Expired - Lifetime
- 2001-02-20 ES ES12154683.2T patent/ES2664818T3/es not_active Expired - Lifetime
- 2001-02-20 JP JP2001559478A patent/JP4959085B2/ja not_active Expired - Lifetime
- 2001-02-20 AU AU3850701A patent/AU3850701A/xx active Pending
- 2001-02-20 US US10/204,227 patent/US6906042B2/en not_active Expired - Lifetime
- 2001-02-20 HK HK03105085.2A patent/HK1052872A1/zh unknown
- 2001-02-20 CA CA002400371A patent/CA2400371C/en not_active Expired - Lifetime
- 2001-02-20 EP EP01910952.9A patent/EP1274443B1/en not_active Expired - Lifetime
- 2001-02-20 KR KR1020027010810A patent/KR100841813B1/ko not_active Expired - Lifetime
-
2002
- 2002-08-18 IL IL151314A patent/IL151314A/en unknown
-
2005
- 2005-04-15 US US11/106,654 patent/US7390793B2/en not_active Expired - Lifetime
-
2008
- 2008-06-19 US US12/142,608 patent/US7989432B2/en not_active Expired - Fee Related
-
2012
- 2012-02-09 JP JP2012025659A patent/JP2012116860A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2001238507B2 (en) | 2004-04-22 |
| AU2001238507C1 (en) | 2005-02-24 |
| WO2001060382A1 (en) | 2001-08-23 |
| JP2012116860A (ja) | 2012-06-21 |
| EP2452684B1 (en) | 2018-01-24 |
| US6906042B2 (en) | 2005-06-14 |
| IL151314A (en) | 2007-06-03 |
| CA2400371A1 (en) | 2001-08-23 |
| HK1052872A1 (zh) | 2003-10-03 |
| US7989432B2 (en) | 2011-08-02 |
| EP1274443B1 (en) | 2017-05-10 |
| KR100841813B1 (ko) | 2008-06-26 |
| US20030216331A1 (en) | 2003-11-20 |
| KR20030011774A (ko) | 2003-02-11 |
| JP2003522797A (ja) | 2003-07-29 |
| AU2001238507C9 (en) | 2005-07-07 |
| US20050181039A1 (en) | 2005-08-18 |
| EP2452684A3 (en) | 2012-10-03 |
| US7390793B2 (en) | 2008-06-24 |
| JP4959085B2 (ja) | 2012-06-20 |
| AU3850701A (en) | 2001-08-27 |
| EP2452684A2 (en) | 2012-05-16 |
| EP1274443A1 (en) | 2003-01-15 |
| IL151314A0 (en) | 2003-04-10 |
| US20090136564A1 (en) | 2009-05-28 |
| EP1274443A4 (en) | 2008-12-31 |
| CA2400371C (en) | 2009-12-08 |
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