ES2218147T3 - Composiciones microesfericas inyectables a base de naltrexona y su utilizacion en la reduccion del consumo de heroina y alcohol. - Google Patents
Composiciones microesfericas inyectables a base de naltrexona y su utilizacion en la reduccion del consumo de heroina y alcohol.Info
- Publication number
- ES2218147T3 ES2218147T3 ES00921946T ES00921946T ES2218147T3 ES 2218147 T3 ES2218147 T3 ES 2218147T3 ES 00921946 T ES00921946 T ES 00921946T ES 00921946 T ES00921946 T ES 00921946T ES 2218147 T3 ES2218147 T3 ES 2218147T3
- Authority
- ES
- Spain
- Prior art keywords
- naltrexone
- microspheres
- composition
- poly
- lactide
- 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
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 title claims abstract description 108
- 229960003086 naltrexone Drugs 0.000 title claims abstract description 108
- 239000000203 mixture Substances 0.000 title claims abstract description 55
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 title claims abstract description 11
- 239000004005 microsphere Substances 0.000 claims abstract description 104
- 229920001244 Poly(D,L-lactide) Polymers 0.000 claims abstract description 24
- GVGLGOZIDCSQPN-PVHGPHFFSA-N Heroin Chemical compound O([C@H]1[C@H](C=C[C@H]23)OC(C)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4OC(C)=O GVGLGOZIDCSQPN-PVHGPHFFSA-N 0.000 claims abstract description 11
- 229960002069 diamorphine Drugs 0.000 claims abstract description 11
- 239000011159 matrix material Substances 0.000 claims abstract description 9
- 239000012458 free base Substances 0.000 claims abstract description 4
- 238000007918 intramuscular administration Methods 0.000 claims abstract description 3
- 241000124008 Mammalia Species 0.000 claims abstract 2
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 42
- 229920000642 polymer Polymers 0.000 claims description 36
- 239000003814 drug Substances 0.000 claims description 26
- 238000000034 method Methods 0.000 claims description 26
- 239000000243 solution Substances 0.000 claims description 24
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 20
- 238000009472 formulation Methods 0.000 claims description 19
- 238000002347 injection Methods 0.000 claims description 18
- 239000007924 injection Substances 0.000 claims description 18
- 238000000605 extraction Methods 0.000 claims description 12
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 10
- 201000009032 substance abuse Diseases 0.000 claims description 10
- 239000000839 emulsion Substances 0.000 claims description 9
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 8
- 238000002360 preparation method Methods 0.000 claims description 7
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 6
- 229930195725 Mannitol Natural products 0.000 claims description 6
- 239000000594 mannitol Substances 0.000 claims description 6
- 235000010355 mannitol Nutrition 0.000 claims description 6
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 5
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 5
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 5
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 3
- 229920000136 polysorbate Polymers 0.000 claims description 3
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 229950008882 polysorbate Drugs 0.000 claims description 2
- 239000012071 phase Substances 0.000 claims 3
- 239000008346 aqueous phase Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 229940079593 drug Drugs 0.000 description 25
- 230000008569 process Effects 0.000 description 14
- JLVNEHKORQFVQJ-PYIJOLGTSA-N 6alpha-Naltrexol Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@H]3O)CN2CC1CC1 JLVNEHKORQFVQJ-PYIJOLGTSA-N 0.000 description 11
- 241000282472 Canis lupus familiaris Species 0.000 description 11
- 238000011282 treatment Methods 0.000 description 11
- 239000006185 dispersion Substances 0.000 description 10
- 239000003981 vehicle Substances 0.000 description 10
- 239000000725 suspension Substances 0.000 description 7
- PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 description 6
- 229960002428 fentanyl Drugs 0.000 description 6
- 239000002207 metabolite Substances 0.000 description 6
- VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 description 6
- 238000003756 stirring Methods 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 230000036470 plasma concentration Effects 0.000 description 5
- 230000004044 response Effects 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- 208000007848 Alcoholism Diseases 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- 201000007930 alcohol dependence Diseases 0.000 description 4
- 238000004458 analytical method Methods 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 238000004108 freeze drying Methods 0.000 description 4
- UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 description 4
- 229960004127 naloxone Drugs 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- 239000006187 pill Substances 0.000 description 4
- 230000001954 sterilising effect Effects 0.000 description 4
- 238000004659 sterilization and disinfection Methods 0.000 description 4
- 231100000736 substance abuse Toxicity 0.000 description 4
- 208000011117 substance-related disease Diseases 0.000 description 4
- 239000000654 additive Substances 0.000 description 3
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 3
- 229910052782 aluminium Inorganic materials 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000000284 extract Substances 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 239000007972 injectable composition Substances 0.000 description 3
- 239000004810 polytetrafluoroethylene Substances 0.000 description 3
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 3
- 229910001220 stainless steel Inorganic materials 0.000 description 3
- 239000010935 stainless steel Substances 0.000 description 3
- 238000003860 storage Methods 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 230000036765 blood level Effects 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 229920001971 elastomer Polymers 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 239000011888 foil Substances 0.000 description 2
- 239000011521 glass Substances 0.000 description 2
- 231100000304 hepatotoxicity Toxicity 0.000 description 2
- 238000010255 intramuscular injection Methods 0.000 description 2
- 239000007927 intramuscular injection Substances 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 238000012423 maintenance Methods 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 239000011859 microparticle Substances 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
- 239000007764 o/w emulsion Substances 0.000 description 2
- 238000011002 quantification Methods 0.000 description 2
- 230000029058 respiratory gaseous exchange Effects 0.000 description 2
- 238000000638 solvent extraction Methods 0.000 description 2
- 230000006641 stabilisation Effects 0.000 description 2
- 238000011105 stabilization Methods 0.000 description 2
- 239000008223 sterile water Substances 0.000 description 2
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 206010063659 Aversion Diseases 0.000 description 1
- 241000282465 Canis Species 0.000 description 1
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 description 1
- 206010012335 Dependence Diseases 0.000 description 1
- 241001539473 Euphoria Species 0.000 description 1
- 206010015535 Euphoric mood Diseases 0.000 description 1
- 208000005176 Hepatitis C Diseases 0.000 description 1
- 206010019851 Hepatotoxicity Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 102000003840 Opioid Receptors Human genes 0.000 description 1
- 108090000137 Opioid Receptors Proteins 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 229910000831 Steel Inorganic materials 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 230000036626 alertness Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 238000010923 batch production Methods 0.000 description 1
- 238000006065 biodegradation reaction Methods 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 description 1
- 229960001736 buprenorphine Drugs 0.000 description 1
- 210000001217 buttock Anatomy 0.000 description 1
- 238000000237 capillary viscometry Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 229960002896 clonidine Drugs 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 229960003920 cocaine Drugs 0.000 description 1
- 238000004590 computer program Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 238000009223 counseling Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000003599 detergent Substances 0.000 description 1
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
- 238000000835 electrochemical detection Methods 0.000 description 1
- 230000002996 emotional effect Effects 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000013213 extrapolation Methods 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 231100000334 hepatotoxic Toxicity 0.000 description 1
- 230000003082 hepatotoxic effect Effects 0.000 description 1
- 230000007686 hepatotoxicity Effects 0.000 description 1
- 238000000265 homogenisation Methods 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 230000007803 itching Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 229960001797 methadone Drugs 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 239000004081 narcotic agent Substances 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 229940127240 opiate Drugs 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000002953 phosphate buffered saline Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920000747 poly(lactic acid) Polymers 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
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 238000011045 prefiltration Methods 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000001337 psychedelic effect Effects 0.000 description 1
- 210000001747 pupil Anatomy 0.000 description 1
- 230000001698 pyrogenic effect Effects 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000005057 refrigeration Methods 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000003252 repetitive effect Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000010959 steel Substances 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000003809 water extraction Methods 0.000 description 1
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
- A61K9/14—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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Inorganic Chemistry (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12847799P | 1999-04-09 | 1999-04-09 | |
| US128477P | 1999-04-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2218147T3 true ES2218147T3 (es) | 2004-11-16 |
Family
ID=22435553
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES00921946T Expired - Lifetime ES2218147T3 (es) | 1999-04-09 | 2000-04-08 | Composiciones microesfericas inyectables a base de naltrexona y su utilizacion en la reduccion del consumo de heroina y alcohol. |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US6306425B1 (enExample) |
| EP (1) | EP1171132B1 (enExample) |
| JP (2) | JP4995371B2 (enExample) |
| KR (1) | KR100621261B1 (enExample) |
| CN (1) | CN1210031C (enExample) |
| AT (1) | ATE262906T1 (enExample) |
| AU (1) | AU780852B2 (enExample) |
| BR (1) | BR0009639A (enExample) |
| CA (1) | CA2369302C (enExample) |
| CZ (1) | CZ20013636A3 (enExample) |
| DE (1) | DE60009477T2 (enExample) |
| DK (1) | DK1171132T3 (enExample) |
| EA (1) | EA004734B1 (enExample) |
| ES (1) | ES2218147T3 (enExample) |
| HK (1) | HK1047245B (enExample) |
| HU (1) | HUP0200838A3 (enExample) |
| IL (2) | IL145802A0 (enExample) |
| MX (1) | MXPA01010185A (enExample) |
| NO (1) | NO328647B1 (enExample) |
| NZ (1) | NZ515359A (enExample) |
| PL (1) | PL196930B1 (enExample) |
| PT (1) | PT1171132E (enExample) |
| TR (1) | TR200102880T2 (enExample) |
| UA (1) | UA79921C2 (enExample) |
| WO (1) | WO2000061147A1 (enExample) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6194006B1 (en) * | 1998-12-30 | 2001-02-27 | Alkermes Controlled Therapeutics Inc. Ii | Preparation of microparticles having a selected release profile |
| US6610317B2 (en) | 1999-05-27 | 2003-08-26 | Acusphere, Inc. | Porous paclitaxel matrices and methods of manufacture thereof |
| US7919119B2 (en) | 1999-05-27 | 2011-04-05 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
| AU2001223396A1 (en) * | 2000-02-01 | 2001-08-14 | Disetronic Licensing Ag | Container and device for administering a substance |
| US6264987B1 (en) * | 2000-05-19 | 2001-07-24 | Alkermes Controlled Therapeutics Inc. Ii | Method for preparing microparticles having a selected polymer molecular weight |
| US6495164B1 (en) * | 2000-05-25 | 2002-12-17 | Alkermes Controlled Therapeutics, Inc. I | Preparation of injectable suspensions having improved injectability |
| DE60223254T2 (de) | 2001-07-06 | 2008-08-14 | Penwest Pharmaceuticals Co. | Verzögert freisetzende formulierungen von oxymorphon |
| JP2005515966A (ja) | 2001-07-06 | 2005-06-02 | エンドー ファーマシューティカルズ， インコーポレイティド | 鎮痛薬としての使用のための６−ヒドロキシ−オキシモルホンの経口投与 |
| US8329216B2 (en) | 2001-07-06 | 2012-12-11 | Endo Pharmaceuticals Inc. | Oxymorphone controlled release formulations |
| US7094369B2 (en) | 2002-03-29 | 2006-08-22 | Scimed Life Systems, Inc. | Processes for manufacturing polymeric microspheres |
| US7462366B2 (en) | 2002-03-29 | 2008-12-09 | Boston Scientific Scimed, Inc. | Drug delivery particle |
| US7131997B2 (en) | 2002-03-29 | 2006-11-07 | Scimed Life Systems, Inc. | Tissue treatment |
| US7053134B2 (en) | 2002-04-04 | 2006-05-30 | Scimed Life Systems, Inc. | Forming a chemically cross-linked particle of a desired shape and diameter |
| US7157102B1 (en) | 2002-05-31 | 2007-01-02 | Biotek, Inc. | Multi-layered microcapsules and method of preparing same |
| US7041320B1 (en) | 2002-05-31 | 2006-05-09 | Biotek, Inc. | High drug loaded injectable microparticle compositions and methods of treating opioid drug dependence |
| US6972291B2 (en) * | 2002-07-02 | 2005-12-06 | Bernstein Richard K | Method for reducing food intake |
| US7842377B2 (en) * | 2003-08-08 | 2010-11-30 | Boston Scientific Scimed, Inc. | Porous polymeric particle comprising polyvinyl alcohol and having interior to surface porosity-gradient |
| US7449236B2 (en) | 2002-08-09 | 2008-11-11 | Boston Scientific Scimed, Inc. | Porous polymeric particle comprising polyvinyl alcohol and having interior to surface porosity-gradient |
| US20040109886A1 (en) * | 2002-08-27 | 2004-06-10 | Larry Rigby | Methods and apparatus for transdermal delivery of abusable drugs with a deterrent agent |
| US8012454B2 (en) | 2002-08-30 | 2011-09-06 | Boston Scientific Scimed, Inc. | Embolization |
| US7883490B2 (en) | 2002-10-23 | 2011-02-08 | Boston Scientific Scimed, Inc. | Mixing and delivery of therapeutic compositions |
| US7588825B2 (en) | 2002-10-23 | 2009-09-15 | Boston Scientific Scimed, Inc. | Embolic compositions |
| MXPA05009803A (es) * | 2003-03-13 | 2006-04-18 | Cheryl M Burgess | Metodos para administrar un material en un paciente para realce dermico. |
| EP1628664A4 (en) * | 2003-06-04 | 2008-11-05 | Alkermes Inc | POLYMORPHIC FORMS OF NALTREXONE |
| US6987111B2 (en) * | 2003-08-06 | 2006-01-17 | Alkermes Controlled Therapeutics, Ii | Aripiprazole, olanzapine and haloperidol pamoate salts |
| US20050031713A1 (en) * | 2003-08-06 | 2005-02-10 | Elliot Ehrich | Methods for administering active agents to CYP3A4 sensitive patients |
| US7976823B2 (en) | 2003-08-29 | 2011-07-12 | Boston Scientific Scimed, Inc. | Ferromagnetic particles and methods |
| EP1667659A1 (en) * | 2003-09-30 | 2006-06-14 | Acusphere, Inc. | Injectable, oral, or topical sustained release pharmaceutical formulations |
| US7901770B2 (en) | 2003-11-04 | 2011-03-08 | Boston Scientific Scimed, Inc. | Embolic compositions |
| LT2351555T (lt) * | 2004-02-23 | 2016-12-27 | Euro-Celtique S.A. | Piktnaudžiavimui atspari priemonė, skirta transderminiam opoido įvedimui |
| US7736671B2 (en) | 2004-03-02 | 2010-06-15 | Boston Scientific Scimed, Inc. | Embolization |
| US20050245461A1 (en) * | 2004-03-19 | 2005-11-03 | Elliot Ehrich | Methods for treating alcoholism |
| US8173176B2 (en) | 2004-03-30 | 2012-05-08 | Boston Scientific Scimed, Inc. | Embolization |
| US7919499B2 (en) | 2004-04-22 | 2011-04-05 | Alkermes, Inc. | Naltrexone long acting formulations and methods of use |
| US7311861B2 (en) | 2004-06-01 | 2007-12-25 | Boston Scientific Scimed, Inc. | Embolization |
| US7727555B2 (en) | 2005-03-02 | 2010-06-01 | Boston Scientific Scimed, Inc. | Particles |
| US7858183B2 (en) | 2005-03-02 | 2010-12-28 | Boston Scientific Scimed, Inc. | Particles |
| US7963287B2 (en) | 2005-04-28 | 2011-06-21 | Boston Scientific Scimed, Inc. | Tissue-treatment methods |
| CN1872063B (zh) * | 2005-06-03 | 2011-01-26 | 中国人民解放军军事医学科学院毒物药物研究所 | 纳美芬或其盐的长效注射用微球或组合物及其制备方法 |
| US9463426B2 (en) | 2005-06-24 | 2016-10-11 | Boston Scientific Scimed, Inc. | Methods and systems for coating particles |
| US7947368B2 (en) | 2005-12-21 | 2011-05-24 | Boston Scientific Scimed, Inc. | Block copolymer particles |
| US7501179B2 (en) | 2005-12-21 | 2009-03-10 | Boston Scientific Scimed, Inc. | Block copolymer particles |
| EP1810714A1 (de) * | 2006-01-19 | 2007-07-25 | Holger Lars Hermann | Verwendung einer Kombination von Heroin und Naloxon zur Drogensubstitution |
| RU2310449C1 (ru) * | 2006-05-17 | 2007-11-20 | Руслан Геннадьевич Нервалев | Способ лечения опиоидной и/или алкогольной зависимости |
| WO2009051824A2 (en) * | 2007-10-18 | 2009-04-23 | Aiko Biotechnology | Combination analgesic employing opioid and neutral antagonist |
| US8748448B2 (en) | 2007-10-18 | 2014-06-10 | Aiko Biotechnology | Combination analgesic employing opioid agonist and neutral antagonist |
| RU2010129907A (ru) | 2007-12-17 | 2012-01-27 | Лабофарм Инк. (CA) | Лекарственная форма с контролируемым высвобождением, предотвращающая неправильное употребление |
| US8486449B2 (en) | 2008-12-16 | 2013-07-16 | Paladin Labs Inc. | Misuse preventative, controlled release formulation |
| US20100196436A1 (en) * | 2009-01-30 | 2010-08-05 | Gooberman Lance L | Implants containing disulfiram and an anti-inflammatory agent |
| US8791093B2 (en) * | 2009-05-29 | 2014-07-29 | Lance L. Gooberman | Pharmaceutical delivery systems for treatment of substance abuse and other addictions |
| EP2544667B1 (en) * | 2010-03-09 | 2018-11-14 | Alkermes Pharma Ireland Limited | Alcohol resistant enteric pharmaceutical compositions |
| RU2476209C1 (ru) * | 2012-02-29 | 2013-02-27 | Станислав Анатольевич Кедик | Имплантируемое лекарственное средство на основе налтрексона для лечения пациентов, зависимых от алкоголя или опиатов |
| WO2015020240A1 (ko) | 2013-08-06 | 2015-02-12 | 동국제약 주식회사 | 엔테카비어 미립구 및 이를 포함하는 비경구투여용 약제학적 조성물 |
| WO2016013993A1 (en) * | 2014-07-25 | 2016-01-28 | Imuneks Farma Llac Sanayi Ve Ticaret A.Ş. | Stable preservative free ophthalmic formulations of opioid antagonists |
| WO2020080806A1 (en) | 2018-10-15 | 2020-04-23 | Chong Kun Dang Pharmaceutical Corp. | Injectable long-acting naltrexone microparticle compositions |
| GR1009871B (el) * | 2019-07-30 | 2020-11-12 | Φαρματεν Α.Β.Ε.Ε. | Φαρμακευτικο σκευασμα που περιλαμβανει μικροσφαιριδια ναλτρεξονης και μεθοδος παρασκευης αυτου |
| US20210059943A1 (en) * | 2019-09-04 | 2021-03-04 | Buffalo Pacific LLC | Systems and methods addressing multiple aspects to provide a comprehensive recovery program for addictions, chronic conditions and diseases |
| CA3208374A1 (en) * | 2021-03-09 | 2022-09-15 | Ju Hee Kim | Sustained formulation for prevention or treatment of autoimmune disease containing naltrexone and method using same |
| CA3236690A1 (en) * | 2021-11-18 | 2023-05-25 | Ju Hee Kim | Sustained-release injectable composition containing naltrexone and method for preparing same |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3887699A (en) | 1969-03-24 | 1975-06-03 | Seymour Yolles | Biodegradable polymeric article for dispensing drugs |
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4568559A (en) | 1984-02-06 | 1986-02-04 | Biotek, Inc. | Composite core coated microparticles and process of preparing same |
| US4623588A (en) | 1984-02-06 | 1986-11-18 | Biotek, Inc. | Controlled release composite core coated microparticles |
| US4981696A (en) | 1986-12-22 | 1991-01-01 | E. I. Du Pont De Nemours And Company | Polylactide compositions |
| DE3710175A1 (de) | 1987-02-12 | 1988-08-25 | Hoechst Ag | Mehrteilige implantierbare arzneizubereitung mit langzeitwirkung |
| FR2618674B1 (fr) | 1987-07-30 | 1990-06-15 | Ire Celltarg Sa | Microparticules comportant un polymere biodegradable controlant la liberation d'un principe actif antimalarique, compositions pharmaceutiques en comprenant et procede de preparation |
| US4897268A (en) | 1987-08-03 | 1990-01-30 | Southern Research Institute | Drug delivery system and method of making the same |
| DE3734223A1 (de) * | 1987-10-09 | 1989-04-20 | Boehringer Ingelheim Kg | Implantierbares, biologisch abbaubares wirkstofffreigabesystem |
| JP2670680B2 (ja) | 1988-02-24 | 1997-10-29 | 株式会社ビーエムジー | 生理活性物質含有ポリ乳酸系微小球およびその製造法 |
| US4902515A (en) | 1988-04-28 | 1990-02-20 | E. I. Dupont De Nemours And Company | Polylactide compositions |
| DE69024953T3 (de) | 1989-05-04 | 2005-01-27 | Southern Research Institute, Birmingham | Einkapselungsverfahren |
| US5486362A (en) * | 1991-05-07 | 1996-01-23 | Dynagen, Inc. | Controlled, sustained release delivery system for treating drug dependency |
| AU2605592A (en) | 1991-10-15 | 1993-04-22 | Atrix Laboratories, Inc. | Polymeric compositions useful as controlled release implants |
| US5736152A (en) * | 1995-10-27 | 1998-04-07 | Atrix Laboratories, Inc. | Non-polymeric sustained release delivery system |
| AU7582498A (en) * | 1997-05-20 | 1998-12-11 | Yale University | Substance dependence treatment using opiate antagonists and serotonin compounds |
| JPH11269094A (ja) * | 1998-01-16 | 1999-10-05 | Takeda Chem Ind Ltd | 徐放性組成物、その製造法および用途 |
-
2000
- 2000-04-07 US US09/545,064 patent/US6306425B1/en not_active Expired - Fee Related
- 2000-04-08 HK HK02108954.5A patent/HK1047245B/zh not_active IP Right Cessation
- 2000-04-08 HU HU0200838A patent/HUP0200838A3/hu unknown
- 2000-04-08 TR TR2001/02880T patent/TR200102880T2/xx unknown
- 2000-04-08 DK DK00921946T patent/DK1171132T3/da active
- 2000-04-08 MX MXPA01010185A patent/MXPA01010185A/es active IP Right Grant
- 2000-04-08 JP JP2000610480A patent/JP4995371B2/ja not_active Expired - Fee Related
- 2000-04-08 ES ES00921946T patent/ES2218147T3/es not_active Expired - Lifetime
- 2000-04-08 PL PL350548A patent/PL196930B1/pl unknown
- 2000-04-08 EA EA200101062A patent/EA004734B1/ru active IP Right Revival
- 2000-04-08 CA CA002369302A patent/CA2369302C/en not_active Expired - Fee Related
- 2000-04-08 KR KR1020017012866A patent/KR100621261B1/ko not_active Expired - Fee Related
- 2000-04-08 PT PT00921946T patent/PT1171132E/pt unknown
- 2000-04-08 AT AT00921946T patent/ATE262906T1/de not_active IP Right Cessation
- 2000-04-08 DE DE60009477T patent/DE60009477T2/de not_active Expired - Lifetime
- 2000-04-08 AU AU42203/00A patent/AU780852B2/en not_active Ceased
- 2000-04-08 IL IL14580200A patent/IL145802A0/xx active IP Right Grant
- 2000-04-08 EP EP00921946A patent/EP1171132B1/en not_active Expired - Lifetime
- 2000-04-08 WO PCT/US2000/009438 patent/WO2000061147A1/en not_active Ceased
- 2000-04-08 CN CNB008085684A patent/CN1210031C/zh not_active Expired - Fee Related
- 2000-04-08 NZ NZ515359A patent/NZ515359A/xx unknown
- 2000-04-08 BR BR0009639-3A patent/BR0009639A/pt not_active Application Discontinuation
- 2000-04-08 CZ CZ20013636A patent/CZ20013636A3/cs unknown
- 2000-08-04 UA UA2001117615A patent/UA79921C2/uk unknown
-
2001
- 2001-10-05 IL IL145802A patent/IL145802A/en unknown
- 2001-10-08 NO NO20014896A patent/NO328647B1/no not_active IP Right Cessation
-
2009
- 2009-11-02 JP JP2009252183A patent/JP2010031036A/ja active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2218147T3 (es) | Composiciones microesfericas inyectables a base de naltrexona y su utilizacion en la reduccion del consumo de heroina y alcohol. | |
| ES2647614T3 (es) | Composiciones biodegradables de liberación de fármaco | |
| Lasky et al. | A prospective study of omeprazole suspension to prevent clinically significant gastrointestinal bleeding from stress ulcers in mechanically ventilated trauma patients | |
| ES2314089T3 (es) | Composiciones liquidas administradas por via oral que comprenden guaifenesina y un copolimero de bloques de polioxialquileno. | |
| ES2665999T3 (es) | Dispositivo polimérico implantable para la liberación sostenida de buprenorfina | |
| PENDER et al. | Toxicity with dextromethorphan-containing preparations: a literature review and report of two additional cases | |
| US20080292710A1 (en) | Liquid Dosage Forms Of Acid Labile Drugs | |
| CA2490145C (en) | Use of a fast dissolving tablet of a proton pump inhibitor (ppi) to produce a liquid formulation for the treatment of gastrointestinal disorders | |
| Wang et al. | Bulleyaconitine A isolated from aconitum plant displays long-acting local anesthetic properties in vitro and in vivo | |
| CA2490147C (en) | Liquid dosage forms of non-enterically coated proton pump inhibitors | |
| CN1938040A (zh) | 缩宫素控释制剂及其应用方法 | |
| Rameesa et al. | Orodispersible tablet: a patient friendly dosage form (a review) | |
| RU2661617C1 (ru) | Суппозитории нефопама для лечения острого и хронического болевого синдрома на гидрофильной эмульсионной основе и способ их получения | |
| ES2236183T3 (es) | Reduccion de las recaidas en el uso de las drogas. | |
| Söderberg et al. | In-vitro release of bupivacaine from injectable lipid formulations investigated by a single drop technique—relation to duration of action in-vivo | |
| Vilas et al. | A Review on Floating Microsphere | |
| Al-Hammami et al. | Effects of excipients on the bioavailability of sodium salicylate from orally administered, oily suspensions | |
| WO2025078964A1 (en) | An oral liquid formulation of methocarbamol | |
| Aly | 4 THISli | |
| Manojlovikj et al. | PP-009 Implementing appropriate compounded paediatric chloral hydrate rectal dosage form |