JP2013527213A5 - - Google Patents
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- JP2013527213A5 JP2013527213A5 JP2013512880A JP2013512880A JP2013527213A5 JP 2013527213 A5 JP2013527213 A5 JP 2013527213A5 JP 2013512880 A JP2013512880 A JP 2013512880A JP 2013512880 A JP2013512880 A JP 2013512880A JP 2013527213 A5 JP2013527213 A5 JP 2013527213A5
- Authority
- JP
- Japan
- Prior art keywords
- risperidone
- drug
- days
- polymer
- release
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000000203 mixture Substances 0.000 claims description 273
- 229920000642 polymer Polymers 0.000 claims description 175
- 229940079593 drug Drugs 0.000 claims description 171
- 239000003814 drug Substances 0.000 claims description 171
- 229960001534 risperidone Drugs 0.000 claims description 171
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims description 154
- 239000002904 solvent Substances 0.000 claims description 81
- 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 claims description 62
- 229960002428 fentanyl Drugs 0.000 claims description 62
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 51
- 229960003881 letrozole Drugs 0.000 claims description 51
- 238000000034 method Methods 0.000 claims description 48
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims description 40
- 229960005017 olanzapine Drugs 0.000 claims description 39
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 36
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 32
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 26
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical group CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 25
- 239000002207 metabolite Substances 0.000 claims description 23
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- 239000004310 lactic acid Substances 0.000 claims description 17
- 235000014655 lactic acid Nutrition 0.000 claims description 17
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- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 description 18
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- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 description 12
- 239000011159 matrix material Substances 0.000 description 12
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- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 8
- 239000011859 microparticle Substances 0.000 description 8
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- 238000013268 sustained release Methods 0.000 description 7
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- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
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- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 4
- 241000282472 Canis lupus familiaris Species 0.000 description 4
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 4
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 229960003616 bemiparin Drugs 0.000 description 4
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 4
- 239000012530 fluid Substances 0.000 description 4
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- 239000000047 product Substances 0.000 description 4
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- 238000000870 ultraviolet spectroscopy Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 239000004621 biodegradable polymer Substances 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 210000001124 body fluid Anatomy 0.000 description 3
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- 230000005923 long-lasting effect Effects 0.000 description 3
- 239000011777 magnesium Substances 0.000 description 3
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 3
- 239000000347 magnesium hydroxide Substances 0.000 description 3
- 229910001862 magnesium hydroxide Inorganic materials 0.000 description 3
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- 229940004157 risperidone 25 mg Drugs 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 2
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- 239000000164 antipsychotic agent Substances 0.000 description 2
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- 229960004323 rivastigmine tartrate Drugs 0.000 description 2
- 230000009469 supplementation Effects 0.000 description 2
- YONPGGFAJWQGJC-UHFFFAOYSA-K titanium(iii) chloride Chemical compound Cl[Ti](Cl)Cl YONPGGFAJWQGJC-UHFFFAOYSA-K 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
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- 238000012371 Aseptic Filling Methods 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 208000005888 Periodontal Pocket Diseases 0.000 description 1
- 229920001244 Poly(D,L-lactide) Polymers 0.000 description 1
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- 229910052783 alkali metal Inorganic materials 0.000 description 1
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- 229940035676 analgesics Drugs 0.000 description 1
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- 239000003242 anti bacterial agent Substances 0.000 description 1
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- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
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- 229940088597 hormone Drugs 0.000 description 1
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- 238000002513 implantation Methods 0.000 description 1
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- 229940080131 olanzapine 10 mg Drugs 0.000 description 1
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Images
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10382153.4 | 2010-05-31 | ||
| EP10382153.4A EP2394663B1 (en) | 2010-05-31 | 2010-05-31 | Compositions for injectable in-situ biodegradable implants |
| PCT/EP2011/059001 WO2011151356A2 (en) | 2010-05-31 | 2011-05-31 | Methods for the preparation of injectable depot compositions |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013527213A JP2013527213A (ja) | 2013-06-27 |
| JP2013527213A5 true JP2013527213A5 (https=) | 2014-09-11 |
| JP5923493B2 JP5923493B2 (ja) | 2016-05-24 |
Family
ID=43301929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013512880A Active JP5923493B2 (ja) | 2010-05-31 | 2011-05-31 | 注射可能なデポー組成物の調製方法 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US10058504B2 (https=) |
| EP (2) | EP2394663B1 (https=) |
| JP (1) | JP5923493B2 (https=) |
| CN (1) | CN102933234A (https=) |
| BR (1) | BR112012030707A2 (https=) |
| CA (1) | CA2800641C (https=) |
| CY (1) | CY1124783T1 (https=) |
| DK (1) | DK2582395T3 (https=) |
| EA (1) | EA024211B1 (https=) |
| ES (2) | ES2897976T3 (https=) |
| FI (1) | FI2582395T3 (https=) |
| HR (2) | HRP20211853T1 (https=) |
| HU (3) | HUE057236T2 (https=) |
| LT (2) | LT2394663T (https=) |
| MX (1) | MX346167B (https=) |
| PL (2) | PL2394663T3 (https=) |
| PT (2) | PT2394663T (https=) |
| RS (2) | RS64451B1 (https=) |
| SI (2) | SI2394663T1 (https=) |
| SM (2) | SMT202100679T1 (https=) |
| WO (1) | WO2011151356A2 (https=) |
| ZA (1) | ZA201209394B (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| EP2152315B1 (en) | 2007-05-25 | 2016-01-06 | Indivior UK Limited | Sustained delivery formulations of risperidone compounds |
| US10285936B2 (en) | 2010-05-31 | 2019-05-14 | Laboratorios Farmacéuticos Rovi, S.A. | Injectable composition with aromatase inhibitor |
| US10335366B2 (en) | 2010-05-31 | 2019-07-02 | Laboratorios Farmacéuticos Rovi, S.A. | Risperidone or paliperidone implant formulation |
| ES2390439B1 (es) * | 2012-08-03 | 2013-09-27 | Laboratorios Farmacéuticos Rovi, S.A. | Composición inyectable |
| EP2529757B1 (en) * | 2011-05-31 | 2014-01-08 | Laboratorios Farmaceuticos Rovi, S.A. | Paliperidone implant formulation |
| US10350159B2 (en) | 2010-05-31 | 2019-07-16 | Laboratories Farmacéuticos Rovi, S.A. | Paliperidone implant formulation |
| US10881605B2 (en) | 2010-05-31 | 2021-01-05 | Laboratorios Farmaceuticos Rovi, S.A. | Methods for the preparation of injectable depot compositions |
| PT2394663T (pt) | 2010-05-31 | 2021-11-26 | Farm Rovi Lab Sa | Composições para implantes biodegradáveis injectáveis |
| US10463607B2 (en) | 2010-05-31 | 2019-11-05 | Laboratorios Farmaceutics Rofi S.A. | Antipsychotic Injectable Depot Composition |
| LT2394664T (lt) | 2010-05-31 | 2016-09-26 | Laboratorios Farmaceuticos Rovi, S.A. | Antipsichozinė injekcinė depozitinė kompozicija |
| GB2481017B (en) | 2010-06-08 | 2015-01-07 | Rb Pharmaceuticals Ltd | Microparticle buprenorphine suspension |
| US9272044B2 (en) | 2010-06-08 | 2016-03-01 | Indivior Uk Limited | Injectable flowable composition buprenorphine |
| LT2529756T (lt) * | 2011-05-31 | 2021-07-26 | Laboratorios Farmaceuticos Rovi, S.A. | Risperidono ir (arba) paliperidono implantų kompozicija |
| US8935726B2 (en) | 2012-05-11 | 2015-01-13 | Comcast Cable Communications, Llc | Generation of dynamic content interfaces |
| US20140308352A1 (en) | 2013-03-11 | 2014-10-16 | Zogenix Inc. | Compositions and methods involving polymer, solvent, and high viscosity liquid carrier material |
| HK1220628A1 (zh) | 2013-03-11 | 2017-05-12 | Durect Corporation | 包含高粘度液体载体的可注射控制释放组合物 |
| GB201404139D0 (en) | 2014-03-10 | 2014-04-23 | Rb Pharmaceuticals Ltd | Sustained release buprenorphine solution formulations |
| CA2998504C (en) | 2015-09-21 | 2023-06-20 | Teva Pharmaceuticals International Gmbh | Sustained release olanzapine formulations |
| CN107811967B (zh) * | 2016-09-09 | 2021-08-24 | 中国疾病预防控制中心寄生虫病预防控制所(国家热带病研究中心) | 抗寄生虫药物原位固化缓释注射剂及其制备方法 |
| CN109890365A (zh) * | 2016-09-23 | 2019-06-14 | 戴尔普尔有限公司 | 小分子治疗剂化合物的组合物 |
| WO2018070940A1 (en) * | 2016-10-14 | 2018-04-19 | Nanyang Technological University | An injectable composition for localized controlled and sustained delivery system |
| JP7101694B2 (ja) | 2016-11-16 | 2022-07-15 | ペルシカ ファーマシューティカルズ リミテッド | 腰痛のための抗生物質製剤 |
| WO2018172850A1 (en) | 2017-03-20 | 2018-09-27 | Teva Pharmaceuticals International Gmbh | Sustained release olanzapine formulaitons |
| EP3709970B1 (en) * | 2017-11-16 | 2025-05-14 | Persica Pharmaceuticals Ltd. | Linezolid formulations |
| PE20210047A1 (es) | 2018-06-12 | 2021-01-08 | Farm Rovi Lab Sa | Composicion inyectable |
| US20240100012A1 (en) | 2021-01-18 | 2024-03-28 | Mark Hasleton | Pharmaceutical dosage form |
| CA3227324A1 (en) | 2021-07-06 | 2023-01-12 | Mark Hasleton | Treatment of serotonin reuptake inhibitor withdrawal syndrome |
| US12594236B2 (en) | 2021-07-16 | 2026-04-07 | Laboratorios Farmaceuticos Rovi, S.A. | Method of treating acute exacerbation of schizophrenia with long-acting injectable depot composition |
| US12318387B2 (en) | 2021-07-16 | 2025-06-03 | Laboratorios Farmaceuticos Rovi, S.A. | Method of treating acute exacerbation of schizophrenia with long-acting injectable depot composition |
| TW202313047A (zh) | 2021-09-21 | 2023-04-01 | 西班牙商禾霏藥品實驗室有限公司 | 抗精神病可注射儲積型組合物 |
| AU2023281232A1 (en) | 2022-05-18 | 2024-10-24 | Laboratorios Farmacéuticos Rovi, S.A. | Prolonged-release injectable compositions for use in treatment with risperidone together with cyp2d6 enzyme inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| BE758156R (fr) | 1970-05-13 | 1971-04-28 | Ethicon Inc | Element de suture absorbable et sa |
| US4389330A (en) | 1980-10-06 | 1983-06-21 | Stolle Research And Development Corporation | Microencapsulation process |
| US4902506A (en) * | 1983-07-05 | 1990-02-20 | The University Of Rochester | Immunogenic conjugates |
| US4530840A (en) | 1982-07-29 | 1985-07-23 | The Stolle Research And Development Corporation | Injectable, long-acting microparticle formulation for the delivery of anti-inflammatory agents |
| US4523591A (en) | 1982-10-22 | 1985-06-18 | Kaplan Donald S | Polymers for injection molding of absorbable surgical devices |
| US4938763B1 (en) | 1988-10-03 | 1995-07-04 | Atrix Lab Inc | Biodegradable in-situ forming implants and method of producing the same |
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