CN102772380B - 固体药物剂型 - Google Patents
固体药物剂型 Download PDFInfo
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- CN102772380B CN102772380B CN201210259721.5A CN201210259721A CN102772380B CN 102772380 B CN102772380 B CN 102772380B CN 201210259721 A CN201210259721 A CN 201210259721A CN 102772380 B CN102772380 B CN 102772380B
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- amino
- methyl
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- carbonyl
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Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- 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
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
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- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61K9/20—Pills, tablets, discs, rods
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- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/650178 | 2003-08-28 | ||
| US10/650,178 US20050048112A1 (en) | 2003-08-28 | 2003-08-28 | Solid pharmaceutical dosage form |
| CN200480024748XA CN1901884B (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200480024748XA Division CN1901884B (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
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| CN200480024748XA Ceased CN1901884B (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
| CN201210259721.5A Ceased CN102772380B (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
| CN201510531654.1A Pending CN105106104A (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
| CN2012102597395A Pending CN102764244A (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
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| CN200480024748XA Ceased CN1901884B (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
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| CN2012102597395A Pending CN102764244A (zh) | 2003-08-28 | 2004-08-23 | 固体药物剂型 |
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| CR (3) | CR8256A (und) |
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| UA (1) | UA85564C2 (und) |
| WO (1) | WO2005039551A2 (und) |
| ZA (3) | ZA200801362B (und) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1175205B1 (en) * | 1999-11-12 | 2006-06-14 | Abbott Laboratories | Solid dispersion comprising ritonavir, fenofibrate or griseofulvin |
| US8025899B2 (en) * | 2003-08-28 | 2011-09-27 | Abbott Laboratories | Solid pharmaceutical dosage form |
| US20050048112A1 (en) | 2003-08-28 | 2005-03-03 | Jorg Breitenbach | Solid pharmaceutical dosage form |
| US8377952B2 (en) * | 2003-08-28 | 2013-02-19 | Abbott Laboratories | Solid pharmaceutical dosage formulation |
| AU2012202831B2 (en) * | 2005-02-23 | 2015-01-22 | Abbvie Inc. | A solid pharmaceutical dosage formulation |
| KR20070025070A (ko) * | 2005-08-31 | 2007-03-08 | 주식회사 대웅제약 | 시부트라민 및 계면활성제를 함유하는 고체분산체 및 그의제조방법 |
| AP2008004533A0 (en) * | 2005-12-14 | 2008-08-31 | Cipla Ltd | Pharmaceutical combination |
| WO2007068615A2 (en) * | 2005-12-14 | 2007-06-21 | F. Hoffmann-La Roche Ag | Hcv prodrug formulation |
| US20090136570A1 (en) * | 2006-01-20 | 2009-05-28 | Bhagwant Rege | Taste-Masked Tablets and Granules |
| EP1832281A1 (en) * | 2006-03-10 | 2007-09-12 | Abbott GmbH & Co. KG | Process for producing a solid dispersion of an active ingredient |
| EP1880715A1 (en) * | 2006-07-19 | 2008-01-23 | Abbott GmbH & Co. KG | Pharmaceutically acceptable solubilizing composition and pharmaceutical dosage form containing same |
| PE20080422A1 (es) * | 2006-08-10 | 2008-04-28 | Cipla Ltd | Composicion solida antirretroviral de administracion oral |
| CA2669938C (en) * | 2006-11-15 | 2016-01-05 | Abbott Laboratories | Solid pharmaceutical dosage formulations |
| DK2487166T3 (en) | 2007-02-23 | 2017-02-20 | Gilead Sciences Inc | Modulators of the pharmacokinetic properties of therapeutics |
| PA8809601A1 (es) * | 2007-12-24 | 2009-07-23 | Cipla Ltd | Combinación anti-retroviral |
| TWI583405B (zh) * | 2008-02-28 | 2017-05-21 | 艾伯維有限公司 | 錠劑及其製備 |
| WO2009153654A1 (en) * | 2008-06-17 | 2009-12-23 | Aurobindo Pharma Limited | Solid dosage forms of antiretrovirals |
| MY160340A (en) * | 2008-10-07 | 2017-02-28 | Astrazeneca Uk Ltd | Pharmaceutical formulation 514 |
| EP2391350A1 (en) | 2008-12-18 | 2011-12-07 | Ranbaxy Laboratories Limited | Atazanavir formulations |
| TW201043269A (en) * | 2009-04-14 | 2010-12-16 | Bristol Myers Squibb Co | Bioavailable compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| TWI471321B (zh) | 2009-06-08 | 2015-02-01 | Abbott Gmbh & Co Kg | Ｂｃｌ－２族群抑制劑之口服醫藥劑型 |
| WO2011013110A1 (en) | 2009-07-31 | 2011-02-03 | Ranbaxy Laboratories Limited | Unit dosage forms of hiv protease inhibitors |
| US20110034489A1 (en) | 2009-07-31 | 2011-02-10 | Ranbaxy Laboratories Limited | Solid dosage forms of hiv protease inhibitors |
| UA113500C2 (xx) | 2010-10-29 | 2017-02-10 | Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб | |
| EP2683378A4 (en) * | 2011-03-07 | 2014-09-03 | Hetero Research Foundation | AMORPHOUS FORM OF A MIXTURE OF LOPINAVIR AND RITONAVIR |
| WO2012164575A2 (en) | 2011-05-27 | 2012-12-06 | Hetero Research Foundation | Amorphous ritonavir co-precipitated |
| EP2744481A4 (en) * | 2011-08-16 | 2015-07-01 | Merck Sharp & Dohme | USE OF INORGANIC MATRIX AND COMBINATIONS OF ORGANIC POLYMERS FOR THE PREPARATION OF STABLE AMORPHOUS DISPERSIONS |
| EP2564832A1 (en) | 2011-08-29 | 2013-03-06 | Hexal AG | Solid dosage form of HIV protease inhibitors |
| KR101794032B1 (ko) * | 2011-09-21 | 2017-11-07 | (주)바이오시네틱스 | 나노입자 제조방법 |
| WO2013131645A1 (en) | 2012-03-07 | 2013-09-12 | Ratiopharm Gmbh | Dosage form comprising non-crystalline lopinavir and crystalline ritonavir |
| EP2822554B1 (en) | 2012-03-07 | 2016-05-18 | ratiopharm GmbH | Dosage form comprising lopinavir and ritonavir |
| CN103655571B (zh) * | 2012-09-11 | 2016-04-20 | 上海星泰医药科技有限公司 | 一种洛匹那韦和利托那韦复方高均匀度纳米共分散体及其制备方法 |
| US9744240B2 (en) | 2012-09-27 | 2017-08-29 | Basf Se | Storage-stable dust-free homogeneous particulate formulation comprising at least one water-soluble vitamin E-derivative and at least one hydrophilic polymer |
| CN104684545B (zh) | 2012-09-27 | 2018-04-03 | 巴斯夫欧洲公司 | 包含至少一种水溶性维生素e衍生物和至少一种亲水聚合物的储存稳定的无粉尘均质颗粒状配制剂 |
| CN104661652B (zh) | 2012-09-27 | 2018-08-28 | 巴斯夫欧洲公司 | 包含至少一种水溶性维生素e衍生物和至少一种亲水聚合物的储存稳定的无粉尘均质颗粒状配制剂 |
| US9789063B2 (en) | 2012-09-27 | 2017-10-17 | Basf Se | Storage-stable dust-free homogeneous particulate formulation |
| RU2505286C1 (ru) | 2012-12-29 | 2014-01-27 | Открытое Акционерное Общество "Фармасинтез" | Фармацевтическая композиция для лечения вич-инфекции, способ ее получения и способ лечения |
| RU2543322C1 (ru) * | 2013-09-19 | 2015-02-27 | Открытое Акционерное Общество "Фармасинтез" | Фармацевтическая композиция для лечения вич-инфекции, способ ее получения и способ лечения |
| RU2619840C1 (ru) * | 2016-09-21 | 2017-05-18 | Общество с ограниченной ответственностью "Изварино Фарма" | Фармацевтическая композиция для лечения ВИЧ-инфекции |
| RU2659693C1 (ru) * | 2017-06-30 | 2018-07-03 | Общество с ограниченной ответственностью "Изварино Фарма" | Фармацевтическая композиция, обладающая активностью против ВИЧ-инфекции |
| US20190038754A1 (en) * | 2017-08-07 | 2019-02-07 | SE Tylose, USA, Inc. | Pharmaceutical composition in solid extruded form |
| US20190269662A1 (en) * | 2018-03-02 | 2019-09-05 | The University Of Liverpool | Solid compositions of actives, processes for preparing same and uses of such solid compositions |
| CN108186578A (zh) * | 2018-03-27 | 2018-06-22 | 聊城大学 | 一种利托那韦固体分散体的制备方法 |
| EP3569225A1 (en) | 2018-05-18 | 2019-11-20 | Pharmaceutical Oriented Services Ltd | Solid dispersion containing ritonavir |
| TWI799599B (zh) * | 2019-06-06 | 2023-04-21 | 華納國際生物科技股份有限公司 | 醫藥或保健品自乳化固體分散組成物 |
| CN114146061B (zh) * | 2020-09-07 | 2023-06-30 | 歌礼生物科技（杭州）有限公司 | 包含固体分散体的蛋白酶抑制剂增效组合物及其制备方法 |
| CN113318076B (zh) * | 2021-06-02 | 2022-09-23 | 聊城大学 | 一种兼具增溶及抑晶效果的利托那韦固体分散体及其制备方法 |
| CN114557967B (zh) * | 2022-03-17 | 2023-06-02 | 乐普制药科技有限公司 | 一种利托那韦固体分散体的制备方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001034119A2 (en) * | 1999-11-12 | 2001-05-17 | Abbott Laboratories | Inhibitors of crystallization in a solid dispersion |
| WO2004032903A2 (de) * | 2002-10-09 | 2004-04-22 | Abbott Gmbh & Co. Kg | Herstellung von festen dosierungsformen unter verwendung eines vernetzten nicht-thermoplastischen trägers |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2525108B1 (fr) | 1982-04-19 | 1989-05-12 | Elan Corp Ltd | Medicaments a haut degre de solubilite et procede pour leur obtention |
| DE3830353A1 (de) | 1988-09-07 | 1990-03-15 | Basf Ag | Verfahren zur kontinuierlichen herstellung von festen pharmazeutischen formen |
| US5354866A (en) * | 1989-05-23 | 1994-10-11 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5552558A (en) * | 1989-05-23 | 1996-09-03 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5542206A (en) | 1994-10-11 | 1996-08-06 | Lisch; Albert | Lure and tackle stacking container |
| US5914332A (en) * | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US6232333B1 (en) * | 1996-11-21 | 2001-05-15 | Abbott Laboratories | Pharmaceutical composition |
| US6027747A (en) * | 1997-11-11 | 2000-02-22 | Terracol; Didier | Process for the production of dry pharmaceutical forms and the thus obtained pharmaceutical compositions |
| DE19841244A1 (de) * | 1998-09-09 | 2000-03-16 | Knoll Ag | Verfahren und Vorrichtung zum Herstellen von Tabletten |
| DE60039379D1 (de) | 1999-02-10 | 2008-08-21 | Pfizer Prod Inc | Pharmazeutische feste Dispersionen |
| US20030104048A1 (en) * | 1999-02-26 | 2003-06-05 | Lipocine, Inc. | Pharmaceutical dosage forms for highly hydrophilic materials |
| DE19913606A1 (de) | 1999-03-25 | 2000-09-28 | Basf Ag | Pulverförmige Solubilisationshilfsstoffe für feste pharmazeutische Darreichungsformen |
| DE19913692A1 (de) | 1999-03-25 | 2000-09-28 | Basf Ag | Mechanisch stabile pharmazeutische Darreichungsformen, enthaltend flüssige oder halbfeste oberflächenaktive Substanzen |
| PL197671B1 (pl) | 1999-06-04 | 2008-04-30 | Abbott Lab | Kompozycja farmaceutyczna zawierająca ritonavir |
| JP4815085B2 (ja) | 1999-11-12 | 2011-11-16 | アボット・ラボラトリーズ | 固体分散体医薬製剤 |
| MXPA03011922A (es) | 2001-06-22 | 2004-03-26 | Pfizer Prod Inc | Composiciones farmaceuticas que contienen un dispersion solida de un farmaco ligeramente soluble en una matriz y plimero mejorador de solubilidad. |
| WO2003063833A1 (en) * | 2002-02-01 | 2003-08-07 | Pfizer Products Inc. | Pharmaceutical compositions of amorphous dispersions of drugs and lipophilic microphase-forming materials |
| DE10213242A1 (de) * | 2002-03-25 | 2003-10-16 | Abbott Gmbh & Co Kg | Testsystem zur Evaluierung der Kompatibilität biologisch aktiver Substanzen mit Copolymeren |
| US20050048112A1 (en) | 2003-08-28 | 2005-03-03 | Jorg Breitenbach | Solid pharmaceutical dosage form |
| US8377952B2 (en) | 2003-08-28 | 2013-02-19 | Abbott Laboratories | Solid pharmaceutical dosage formulation |
| CA2669938C (en) | 2006-11-15 | 2016-01-05 | Abbott Laboratories | Solid pharmaceutical dosage formulations |
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2003
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001034119A2 (en) * | 1999-11-12 | 2001-05-17 | Abbott Laboratories | Inhibitors of crystallization in a solid dispersion |
| WO2004032903A2 (de) * | 2002-10-09 | 2004-04-22 | Abbott Gmbh & Co. Kg | Herstellung von festen dosierungsformen unter verwendung eines vernetzten nicht-thermoplastischen trägers |
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| CN102772380B (zh) | 固体药物剂型 | |
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