CN102036654A - 稳定的非典型抗精神病制剂 - Google Patents
稳定的非典型抗精神病制剂 Download PDFInfo
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- CN102036654A CN102036654A CN2008801290042A CN200880129004A CN102036654A CN 102036654 A CN102036654 A CN 102036654A CN 2008801290042 A CN2008801290042 A CN 2008801290042A CN 200880129004 A CN200880129004 A CN 200880129004A CN 102036654 A CN102036654 A CN 102036654A
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- controlled release
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- atypical antipsychotic
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- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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- A—HUMAN NECESSITIES
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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Abstract
Description
材料 | 优选 | 最优选 |
非典型抗精神病药物 | 0.5-75% | 1-50% |
有机酸 | 5-75% | 20-60% |
填充剂 | 5-70% | 10-65% |
助流剂 | 0-5% | 0.1-3% |
润滑剂 | 0-5% | 0.1-3% |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0332 | 0.0336 | 0.0334 |
1周 | 0.0301 | 0.0312 | 0.0307 |
2周 | 0.0350 | 0.0382 | 0.0366 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 低于检出限 | 低于检出限 | 低于检出限 |
1周 | 0.0183 | 0.0179 | 0.0181 |
2周 | 0.0300 | 0.0312 | 0.0306 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0682 | 0.0695 | 0.0689 |
1周 | 0.0721 | 0.0716 | 0.0719 |
2周 | 0.0807 | 0.0798 | 0.0803 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.102 | 0.104 | 0.103 |
1周 | 0.120 | 0.120 | 0.120 |
2周 | 0.146 | 0.149 | 0.148 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0158 | 0.0167 | 0.0163 |
1周 | 0.0119 | 0.0127 | 0.0123 |
2周 | 0.0137 | 0.0157 | 0.0147 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0322 | 0.0328 | 0.0325 |
1周 | 0.0309 | 0.0309 | 0.0309 |
2周 | 0.0330 | 0.0337 | 0.0334 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0708 | 0.0698 | 0.0703 |
1周 | 0.0698 | 0.0697 | 0.0698 |
2周 | 0.0726 | 0.0721 | 0.0724 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.119 | 0.119 | 0.119 |
1周 | 0.113 | 0.114 | 0.114 |
2周 | 0.119 | 0.121 | 0.120 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0100 | 0.0097 | 0.0099 |
1周 | 17.3115 | 20.668 | 18.9898 |
2周 | 17.4295 | 19.3841 | 18.4068 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 低于检出限 | 低于检出限 | 低于检出限 |
1周 | 8.2142 | 10.794 | 9.5041 |
2周 | 14.1043 | 18.4762 | 16.2903 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0323 | 0.0324 | 0.0324 |
1周 | 0.0136 | 0.0136 | 0.0136 |
2周 | 0.0161 | 0.0502 | 0.0332 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | —— | —— | —— |
1周 | 0.0340 | 0.0757 | 0.0549 |
2周 | 0.0837 | 0.2570 | 0.1704 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | —— | —— | —— |
1周 | 0.2615 | 0.3827 | 0.3221 |
2周 | 0.3943 | 0.7645 | 0.5794 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0702 | 0.0692 | 0.0697 |
1周 | 0.0566 | 0.0538 | 0.0552 |
2周 | 0.0533 | 0.0583 | 0.0559 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.112 | 0.112 | 0.112 |
1周 | 25.891 | 31.987 | 28.939 |
2周 | 32.081 | 38.990 | 35.5355 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0357 | 0.0327 | 0.0342 |
1周 | 0.0295 | 0.0318 | 0.0307 |
2周 | 0.0351 | 0.0361 | 0.0356 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0700 | 0.0688 | 0.0694 |
1周 | 0.0699 | 0.0687 | 0.0693 |
2周 | 0.0725 | 0.0739 | 0.0732 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.106 | 0.101 | 0.104 |
1周 | 0.100 | 0.100 | 0.100 |
2周 | 0.108 | 0.110 | 0.109 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0137 | 0.0146 | 0.0142 |
1周 | 0.0363 | 0.0374 | 0.0369 |
2周 | 0.1813 | 0.1947 | 0.1880 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0345 | 0.0341 | 0.0343 |
1周 | 0.9724 | 1.0025 | 0.9875 |
2周 | 2.9422 | 3.1656 | 3.0539 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | —— | —— | —— |
1周 | 0.0422 | 0.0424 | 0.0423 |
2周 | 0.1856 | 0.1953 | 0.1905 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0700 | 0.0705 | 0.0703 |
1周 | 0.0688 | 0.0696 | 0.0692 |
2周 | 0.0701 | 0.0705 | 0.0703 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.118 | 0.119 | 0.1185 |
1周 | 1.120 | 1.151 | 1.136 |
2周 | 3.379 | 3.625 | 3.502 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0137 | 0.0136 | 0.0137 |
1周 | 0.1411 | 0.1536 | 0.1474 |
2周 | 0.3128 | 0.3628 | 0.3378 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 低于检出限 | 低于检出限 | 低于检出限 |
1周 | 0.5761 | 0.6746 | 0.6254 |
2周 | 1.2091 | 1.4720 | 1.3406 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 低于检出限 | 低于检出限 | 低于检出限 |
1周 | 低于检出限 | 低于检出限 | 低于检出限 |
2周 | 0.0633 | 0.0508 | 0.0571 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0347 | 0.0332 | 0.0340 |
1周 | 0.3403 | 0.3977 | 0.3690 |
2周 | 0.8782 | 1.0318 | 0.9550 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 低于检出限 | 低于检出限 | 低于检出限 |
1周 | 68.9090 | 73.5815 | 71.2453 |
2周 | 76.6554 | 79.3466 | 78.001 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0694 | 0.0700 | 0.0697 |
1周 | 0.0420 | 0.0363 | 0.0392 |
2周 | 0.0394 | 0.0343 | 0.0369 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.118 | 0.117 | 0.118 |
1周 | 70.008 | 74.844 | 72.426 |
2周 | 79.158 | 82.298 | 80.728 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0142 | 0.0147 | 0.0145 |
1周 | 0.762 | 0.832 | 0.797 |
2周 | 1.7530 | 1.5296 | 1.6413 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 低于检出限 | 低于检出限 | 低于检出限 |
1周 | 4.971 | 5.591 | 5.281 |
2周 | 9.6604 | 8.6327 | 9.1466 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0335 | 0.0336 | 0.0336 |
1周 | 29.6478 | 34.3748 | 32.0113 |
2周 | 41.9445 | 38.6429 | 40.2937 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | |||
1周 | 1.2120 | 1.4466 | 1.3293 |
2周 | 2.4228 | 2.3229 | 2.3729 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0686 | 0.0696 | 0.0691 |
1周 | 0.0590 | 0.0556 | 0.0573 |
2周 | 0.0921 | 0.0930 | 0.0926 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.117 | 0.117 | 0.117 |
1周 | 36.652 | 42.299 | 39.476 |
2周 | 55.873 | 51.221 | 53.547 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0357 | 0.0377 | 0.0367 |
1周 | 0.0363 | 0.0374 | 0.0369 |
2周 | 0.0352 | 0.0375 | 0.0364 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.0705 | 0.0696 | 0.0701 |
1周 | 0.0700 | 0.0713 | 0.0707 |
2周 | 0.0719 | 0.0729 | 0.0724 |
时间点 | 样品1 | 样品2 | 平均值 |
最初 | 0.106 | 0.107 | 0.107 |
1周 | 0.106 | 0.109 | 0.108 |
2周 | 0.107 | 0.110 | 0.109 |
成分 | %w/w | Mg/片 |
半富马酸喹硫平 | 41.09 | 230.26 |
琥珀酸 | 28.93 | 162.11 |
乳糖醇 | 2.68 | 15.01 |
LUBRITAB | 7.39 | 41.43 |
胶体二氧化硅 | 0.41 | 2.31 |
硬脂酸镁 | 0.82 | 4.61 |
滑石 | 0.82 | 4.61 |
活性片剂小计 | 82.15 | 460.33 |
乳糖 | 14.10 | 79.0 |
LUBRITAB | 3.57 | 20.0 |
滑石 | 0.18 | 1.0 |
安慰层小计 | 17.85 | 100.0 |
总计 | 100.0 | 560.33 |
成分 | %w/w | Mg/片 |
半富马酸喹硫平 | 41.3 | 230.26 |
琥珀酸 | 29.0 | 162 |
乳糖醇 | 2.7 | 15 |
LUBRITAB | 7.4 | 41.4 |
硬脂酸镁 | 0.8 | 4.6 |
滑石 | 0.8 | 4.6 |
活性片剂小计 | 82.1 | 457.86 |
乳糖 | 14.2 | 79.0 |
LUBRITAB | 3.6 | 20.0 |
滑石 | 0.2 | 1.0 |
安慰层小计 | 17.9 | 100.0 |
总计 | 100.0 | 557.9 |
成分 | Mg/片(实施例8) | Mg/片(实施例9) |
半富马酸喹硫平 | 230.26 | 230.26 |
琥珀酸 | 162 | 162 |
乳糖醇 | 15 | 15 |
胶体二氧化硅 | 2.3 | - |
硬脂酸镁 | 4.6 | 4.6 |
滑石 | 4.6 | 4.6 |
活性片剂小计 | 418.76 | 416.46 |
乳糖 | 79.2 | 79.2 |
滑石 | 0.8 | 0.8 |
安慰层小计 | 80 | 80 |
总计 | 498.8 | 496.5 |
成分 | Mg/片(实施例8) | Mg/片(实施例9) |
半富马酸喹硫平 | 230.26 | 230.26 |
富马酸 | 162 | 162 |
乳糖醇 | 15 | 15 |
胶体二氧化硅 | 2.3 | - |
硬脂酸镁 | 4.6 | 4.6 |
滑石 | 4.6 | 4.6 |
活性片剂小计 | 418.76 | 416.46 |
乳糖 | 79.2 | 79.2 |
滑石 | 0.8 | 0.8 |
安慰层小计 | 80 | 80 |
总计 | 498.8 | 496.5 |
Claims (24)
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US8327008P | 2008-07-24 | 2008-07-24 | |
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PCT/US2008/075333 WO2010011232A1 (en) | 2008-07-24 | 2008-09-05 | Stabilized atypical antipsychotic formulation |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105310980A (zh) * | 2015-10-09 | 2016-02-10 | 北京万全德众医药生物技术有限公司 | 帕利哌酮缓释混悬口服液及其制备方法 |
CN107469087A (zh) * | 2017-09-10 | 2017-12-15 | 孙永丽 | 用于治疗精神病的制剂 |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102036654B (zh) | 2008-07-24 | 2014-05-14 | 湖南洞庭药业股份有限公司 | 稳定的非典型抗精神病制剂 |
US9271939B2 (en) | 2010-03-15 | 2016-03-01 | Inventia Healthcare Private Limited | Stabilized prolonged release pharmaceutical composition comprising atypical antipsychotic |
CN101940561A (zh) * | 2010-09-14 | 2011-01-12 | 浙江华海药业股份有限公司 | 喹硫平片及其制备方法 |
CN102614140B (zh) * | 2011-01-26 | 2015-11-25 | 浙江九洲药物科技有限公司 | 伊潘立酮口崩片及其制备方法 |
DE102011115690A1 (de) * | 2011-10-11 | 2013-04-11 | Acino Pharma Ag | Quetiapin enthaltende Formulierungen |
WO2013100879A1 (en) * | 2011-12-27 | 2013-07-04 | Mahmut Bilgic | Pharmaceutical compositions comprising quetiapine |
WO2013114400A2 (en) * | 2012-01-20 | 2013-08-08 | Rubicon Research Private Limited | Compressed pharmaceutical compositions of atypical antipsychotics |
CN104487071B (zh) * | 2012-07-26 | 2017-06-13 | 久光制药株式会社 | 贴附剂 |
WO2014027974A1 (en) * | 2012-08-17 | 2014-02-20 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Orally disintegrating formulation of paliperidone |
CA2885941A1 (en) * | 2012-09-28 | 2014-04-03 | Delpor, Inc. | Device and method for sustained release of antipsychotic medications |
JP6392355B2 (ja) | 2013-09-13 | 2018-09-19 | アール.ピー.シェーラー テクノロジーズ、エルエルシー | ペレット包含錠剤 |
GR1008842B (el) * | 2015-08-06 | 2016-09-05 | Φαρματεν Ανωνυμος Βιομηχανικη Και Εμπορικη Εταιρεια Φαρμακευτικων Ιατρικων Και Καλλυντικων Προϊοντων | Φαρμακευτικο σκευασμα περιεχον εναν ατυπο αντιψυχωσιμο παραγοντα και μεθοδος για την παρασκευη αυτου |
WO2017025930A1 (en) | 2015-08-12 | 2017-02-16 | Ftf Pharma Private Limited | Oral solution of aripiprazole |
US20210346374A1 (en) * | 2016-10-03 | 2021-11-11 | Suven Life Sciences Limited | Pharmaceutical compositions of 5-ht6 receptor antagonist |
CA3047451A1 (en) | 2016-12-20 | 2018-06-28 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine |
JP7149287B2 (ja) | 2016-12-20 | 2022-10-06 | エルテーエス ローマン テラピー-ジステーメ アーゲー | アセナピンおよびポリシロキサンまたはポリイソブチレンを含有する経皮治療システム |
US9993486B1 (en) | 2017-06-19 | 2018-06-12 | Tlc Therapeutics, Llc | Oral quetiapine suspension formulations with extended shelf life and enhanced bioavailability |
EP3644973B1 (en) | 2017-06-26 | 2021-03-24 | LTS LOHMANN Therapie-Systeme AG | Transdermal therapeutic system containing asenapine and silicone acrylic hybrid polymer |
AU2019291060B2 (en) | 2018-06-20 | 2024-09-05 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine |
Family Cites Families (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3845770A (en) * | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
US3916899A (en) * | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
US4034758A (en) * | 1975-09-08 | 1977-07-12 | Alza Corporation | Osmotic therapeutic system for administering medicament |
US4036228A (en) * | 1975-09-11 | 1977-07-19 | Alza Corporation | Osmotic dispenser with gas generating means |
US4077407A (en) * | 1975-11-24 | 1978-03-07 | Alza Corporation | Osmotic devices having composite walls |
US4008719A (en) * | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
US4612008A (en) * | 1983-05-11 | 1986-09-16 | Alza Corporation | Osmotic device with dual thermodynamic activity |
US4783337A (en) * | 1983-05-11 | 1988-11-08 | Alza Corporation | Osmotic system comprising plurality of members for dispensing drug |
US5002776A (en) * | 1983-12-22 | 1991-03-26 | Elan Corporation, Plc | Controlled absorption diltiazem formulations |
KR890000387B1 (ko) * | 1984-09-24 | 1989-03-16 | 디 엎존 캄파니 | 2-(피리딜알켄술 피닐)벤즈 이미드아졸류의 n-치환 유도체의 제조방법 |
US4663147A (en) * | 1985-09-03 | 1987-05-05 | International Minerals & Chemical Corp. | Disc-like sustained release formulation |
GB8607684D0 (en) * | 1986-03-27 | 1986-04-30 | Ici America Inc | Thiazepine compounds |
GB2189698A (en) * | 1986-04-30 | 1987-11-04 | Haessle Ab | Coated omeprazole tablets |
US4984240A (en) * | 1988-12-22 | 1991-01-08 | Codex Corporation | Distributed switching architecture for communication module redundancy |
US5071607A (en) * | 1990-01-31 | 1991-12-10 | Alza Corporatino | Method and apparatus for forming a hole in a drug dispensing device |
US5229382A (en) * | 1990-04-25 | 1993-07-20 | Lilly Industries Limited | 2-methyl-thieno-benzodiazepine |
US5312819A (en) * | 1990-08-20 | 1994-05-17 | Sandoz Ltd. | Pharmaceutical compositions comprising clozapine and a radical scavenger |
US5627178A (en) * | 1991-04-23 | 1997-05-06 | Lilly Industries Limited | 2-methyl-thieno-benzodiazepine |
US5288505A (en) * | 1991-06-26 | 1994-02-22 | Galephar P.R., Inc., Ltd. | Extended release form of diltiazem |
US5314697A (en) * | 1992-10-23 | 1994-05-24 | Schering Corporation | Stable extended release oral dosage composition comprising loratadine and pseudoephedrine |
US5654005A (en) * | 1995-06-07 | 1997-08-05 | Andrx Pharmaceuticals, Inc. | Controlled release formulation having a preformed passageway |
US5948437A (en) * | 1996-05-23 | 1999-09-07 | Zeneca Limited | Pharmaceutical compositions using thiazepine |
AU720366B2 (en) * | 1996-09-23 | 2000-06-01 | Eli Lilly And Company | Olanzapine dihydrate D |
US6099859A (en) * | 1998-03-20 | 2000-08-08 | Andrx Pharmaceuticals, Inc. | Controlled release oral tablet having a unitary core |
GB9921933D0 (en) * | 1999-09-17 | 1999-11-17 | Univ Gent | Solid shaped articles comprising biologically active substances and a method for their production |
HUP0500795A3 (en) * | 2001-07-04 | 2008-04-28 | Sun Pharmaceutical Ind Ltd | Gastric retention controlled drug delivery system |
WO2005041935A1 (en) | 2003-10-21 | 2005-05-12 | Alpharma, Inc. | Pharmaceutical formulations containing quetiapine |
WO2006088305A1 (en) | 2005-02-15 | 2006-08-24 | Chong Kun Dang Pharmaceutical Corp. | Gastric-retentive controlled release mono-matrix tablet |
US20070104778A1 (en) * | 2005-11-07 | 2007-05-10 | Hongxia Zeng | Controlled-release emulsion compositions |
WO2007090091A2 (en) | 2006-01-27 | 2007-08-09 | Eurand, Inc. | Drug delivery systems comprising weakly basic drugs and organic acids |
US20080081069A1 (en) * | 2006-09-28 | 2008-04-03 | Lupin Limited | Novel controlled release formulations of divalproex sodium |
PT103884A (pt) | 2006-11-17 | 2008-05-19 | Astrazeneca Ab | Composições de libertação prolongada e métodos para a sua preparação |
WO2008110337A2 (en) * | 2007-03-09 | 2008-09-18 | Synthon B.V. | Pharmaceutical composition of quetiapine fumarate |
US20090004281A1 (en) * | 2007-06-26 | 2009-01-01 | Biovail Laboratories International S.R.L. | Multiparticulate osmotic delivery system |
US8632805B2 (en) * | 2008-06-20 | 2014-01-21 | Mutual Pharmaceutical Company, Inc. | Controlled-release formulations, method of manufacture, and use thereof |
CN102036654B (zh) | 2008-07-24 | 2014-05-14 | 湖南洞庭药业股份有限公司 | 稳定的非典型抗精神病制剂 |
-
2008
- 2008-09-05 CN CN200880129004.2A patent/CN102036654B/zh not_active Expired - Fee Related
- 2008-09-05 WO PCT/US2008/075333 patent/WO2010011232A1/en active Application Filing
- 2008-09-05 AU AU2008359725A patent/AU2008359725A1/en not_active Abandoned
- 2008-09-05 NZ NZ588311A patent/NZ588311A/xx not_active IP Right Cessation
- 2008-09-05 CA CA2724533A patent/CA2724533C/en active Active
- 2008-09-05 US US12/205,356 patent/US8173637B2/en active Active
- 2008-09-05 EP EP08799205A patent/EP2299983A4/en not_active Withdrawn
-
2010
- 2010-10-07 ZA ZA2010/07156A patent/ZA201007156B/en unknown
-
2011
- 2011-03-28 US US13/073,873 patent/US8003637B2/en active Active
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105310980A (zh) * | 2015-10-09 | 2016-02-10 | 北京万全德众医药生物技术有限公司 | 帕利哌酮缓释混悬口服液及其制备方法 |
CN107469087A (zh) * | 2017-09-10 | 2017-12-15 | 孙永丽 | 用于治疗精神病的制剂 |
Also Published As
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NZ588311A (en) | 2012-08-31 |
ZA201007156B (en) | 2011-06-29 |
CA2724533A1 (en) | 2010-01-28 |
US8003637B2 (en) | 2011-08-23 |
US20100022511A1 (en) | 2010-01-28 |
AU2008359725A1 (en) | 2010-01-28 |
US8173637B2 (en) | 2012-05-08 |
US20110165238A1 (en) | 2011-07-07 |
EP2299983A1 (en) | 2011-03-30 |
CA2724533C (en) | 2014-07-29 |
WO2010011232A1 (en) | 2010-01-28 |
EP2299983A4 (en) | 2012-10-10 |
CN102036654B (zh) | 2014-05-14 |
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