CN1194688C - 石杉碱甲及其衍生物或其盐的注射用缓释微球及其制备方法 - Google Patents
石杉碱甲及其衍生物或其盐的注射用缓释微球及其制备方法 Download PDFInfo
- Publication number
- CN1194688C CN1194688C CNB011199520A CN01119952A CN1194688C CN 1194688 C CN1194688 C CN 1194688C CN B011199520 A CNB011199520 A CN B011199520A CN 01119952 A CN01119952 A CN 01119952A CN 1194688 C CN1194688 C CN 1194688C
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- CN
- China
- Prior art keywords
- acid
- huperzine
- spheres
- release micro
- microsphere
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- 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.)
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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
- A61K9/14—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
- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
样品编号 | 含药量μg/mg | pH值 | 取值方式 | 释 放 百 分 数 % | |||||||||||
0 | 1 | 2 | 4 | 6 | 8 | 10 | 12 | 14 | 16 | 18 | 20 | ||||
实施例2 | 18.5 | 4.0 | 当天 | 0 | 26.6 | 4.0 | 0 | 1.5 | 1.15 | 14.0 | 11.95 | 3.0 | 0 | 6.5 | |
累积 | 0 | 26.6 | 30.6 | 30.6 | 33.6 | 35.9 | 63.9 | 87.8 | 93.8 | 93.8 | 106.8 | 106.8 | |||
5.5 | 当天 | 0 | 28.0 | 2.0 | 0 | 1.5 | 1.7 | 29.5 | 16.4 | 1.0 | 0 | 0.5 | |||
累积 | 0 | 28.0 | 30.0 | 30 | 33 | 36.4 | 95.4 | 128.2 | 130.2 | 130.2 | 131.2 | 131.2 | |||
实施例3 | 18.3 | 4.0 | 当天 | 0 | 28.3 | 0.3 | 0.95 | 1.1 | 2.1 | 9.0 | 12.35 | 4.8 | 2.8 | 0.85 | 0.5 |
累积 | 0 | 28.3 | 28.6 | 30.5 | 32.7 | 36.9 | 54.9 | 79.6 | 89.2 | 94.8 | 96.5 | 97.5 | |||
5.5 | 当天 | 0 | 18.1 | 0.9 | 3.5 | 0.05 | 2.65 | 8.6 | 10.5 | 12.7 | 2.05 | 1.2 | 0.6 | ||
累积 | 0 | 18.1 | 19.0 | 26.0 | 26.1 | 31.4 | 48.6 | 69.6 | 95.0 | 99.1 | 101.5 | 102.7 | |||
实施例4 | 23.96 | 4.0 | 当天 | 0 | 33.8 | 2.1 | 1.3 | 2.5 | 3.0 | 5.95 | 11.65 | 5.05 | 1.2 | 0.45 | 0.35 |
累积 | 0 | 33.8 | 35.9 | 38.5 | 43.5 | 49.5 | 61.4 | 84.7 | 94.8 | 97.2 | 98.1 | 98.8 | |||
5.5 | 当天 | 0 | 31.7 | 1.7 | 1.95 | 1.3 | 2.35 | 17.65 | 4.2 | 5.75 | 1.15 | 0.55 | 0.2 | ||
累积 | 0 | 31.7 | 33.4 | 37.3 | 39.9 | 44.6 | 79.9 | 88.3 | 99.8 | 102.1 | 103.2 | 103.6 |
Claims (10)
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB011199520A CN1194688C (zh) | 2001-07-03 | 2001-07-03 | 石杉碱甲及其衍生物或其盐的注射用缓释微球及其制备方法 |
PCT/CN2002/000472 WO2003004024A1 (fr) | 2001-07-03 | 2002-07-03 | Microspheres injectables a liberation prolongee de composes d'huperzine a |
DE10297018T DE10297018B4 (de) | 2001-07-03 | 2002-07-03 | Depotmikrokügelchen für die Injektion von Huperzin-A-Verbindungen |
US10/482,631 US20040266813A1 (en) | 2001-07-03 | 2002-07-03 | Injectable sustained-release microspheres of huperzine a compoounds |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB011199520A CN1194688C (zh) | 2001-07-03 | 2001-07-03 | 石杉碱甲及其衍生物或其盐的注射用缓释微球及其制备方法 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1393220A CN1393220A (zh) | 2003-01-29 |
CN1194688C true CN1194688C (zh) | 2005-03-30 |
Family
ID=4663822
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB011199520A Expired - Fee Related CN1194688C (zh) | 2001-07-03 | 2001-07-03 | 石杉碱甲及其衍生物或其盐的注射用缓释微球及其制备方法 |
Country Status (4)
Country | Link |
---|---|
US (1) | US20040266813A1 (zh) |
CN (1) | CN1194688C (zh) |
DE (1) | DE10297018B4 (zh) |
WO (1) | WO2003004024A1 (zh) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100398093C (zh) * | 2003-03-14 | 2008-07-02 | 德比欧药物研究有限公司 | 皮下给药系统、其制备方法及其治疗胆碱能缺乏障碍的用途 |
EP1603532B1 (en) | 2003-03-14 | 2008-08-13 | Debio Recherche Pharmaceutique S.A. | Subcutaneous delivery system, process for the preparation of the same and use of the same for the treatment of cholinergic deficient disorders |
CN1795845B (zh) * | 2004-12-23 | 2010-10-13 | 李又欣 | 作为毒蕈碱受体拮抗剂的3,3-二苯基丙胺衍生物注射用缓释微球制剂 |
CN1883609B (zh) * | 2005-06-21 | 2010-12-01 | 天津天士力制药股份有限公司 | 一种含有桃仁的中药注射用微球及其制备方法 |
CN1965839B (zh) * | 2005-11-15 | 2010-11-10 | 上海医药工业研究院 | 非那雄胺及其类似物的注射用缓释微球、其制备方法及其应用 |
CN1981744B (zh) * | 2005-12-12 | 2011-09-07 | 上海医药工业研究院 | 石杉碱及其衍生物的注射用缓释微球的制备方法 |
CN101264058B (zh) * | 2007-03-13 | 2010-09-01 | 中国科学院上海药物研究所 | 石杉碱甲及其衍生物或其盐的缓释纳米粒、和它的制造方法 |
CN100528844C (zh) * | 2007-04-20 | 2009-08-19 | 中国科学院昆明植物研究所 | 石杉碱甲衍生物,其制备方法和其应用 |
CA2743600C (en) * | 2008-11-14 | 2016-11-08 | Ewha University-Industry Collaboration Foundation | Method for preparing microspheres and microspheres produced thereby |
WO2011132157A1 (en) * | 2010-04-22 | 2011-10-27 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Oral sustained release formulation of huperzine a |
CN101961318A (zh) * | 2010-09-17 | 2011-02-02 | 南昌大学 | 高乌甲素的注射用缓释微球及其制备方法 |
WO2013091283A1 (en) * | 2011-12-22 | 2013-06-27 | Shandong Luye Pharmaceutical Co., Ltd. | Pharmaceutical compositions of triptorelin microspheres |
CN103505413B (zh) * | 2012-06-28 | 2015-07-08 | 上海现代药物制剂工程研究中心有限公司 | 石杉碱甲微粒长效注射剂及其制备方法 |
WO2015043404A1 (zh) * | 2013-09-24 | 2015-04-02 | 万邦德制药集团股份有限公司 | (-)-石杉碱甲盐 |
CN105586304B (zh) * | 2014-11-18 | 2019-03-05 | 北京化工大学 | 一种生产乙醇酸基聚合物的重组菌及其应用 |
CN106511348B (zh) * | 2016-11-02 | 2019-04-19 | 中山大学 | 石杉碱甲骨架微粒、口崩片及其制备方法 |
CN107149595B (zh) * | 2017-05-10 | 2019-11-12 | 烟台大学 | 一种载有石杉碱甲明胶纳米粒微球的制备方法和用途 |
CN109662954B (zh) * | 2019-02-25 | 2021-07-06 | 福建中医药大学 | 石杉碱甲分子印迹水凝胶微球的制备方法 |
CN112402380A (zh) * | 2020-11-19 | 2021-02-26 | 上海应用技术大学 | 一种含石杉碱甲微胶囊的缓释微丸及其制备方法 |
CN113456640A (zh) * | 2021-08-26 | 2021-10-01 | 烟台大学 | 石杉碱甲在心肌缺血损伤预防中的应用 |
CN113476446A (zh) * | 2021-08-26 | 2021-10-08 | 烟台大学 | 石杉碱甲在急性肝损伤预防中的应用 |
CN114796132B (zh) * | 2022-05-13 | 2023-08-22 | 海南灵康制药有限公司 | 一种石杉碱甲冻干粉针剂及其制备方法 |
Family Cites Families (14)
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US4344431A (en) * | 1969-03-24 | 1982-08-17 | University Of Delaware | Polymeric article for dispensing drugs |
US3773919A (en) * | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
JPS63122620A (ja) * | 1986-11-12 | 1988-05-26 | Sanraku Inc | ポリ乳酸マイクロスフエア及びその製造方法 |
US5106979A (en) * | 1989-02-21 | 1992-04-21 | University Of Pittsburgh | Method for the synthesis of huperzine A and analogs thereof and compounds useful therein |
US5547960A (en) * | 1994-09-07 | 1996-08-20 | Mayo Foundation For Medical Education And Research | C-10 analogs of huperzine a |
CN1047732C (zh) * | 1995-04-10 | 1999-12-29 | 浙江省医学科学院 | 石杉碱透皮吸收贴片 |
US5759583A (en) * | 1995-08-30 | 1998-06-02 | Syntex (U.S.A.) Inc. | Sustained release poly (lactic/glycolic) matrices |
US5665428A (en) * | 1995-10-25 | 1997-09-09 | Macromed, Inc. | Preparation of peptide containing biodegradable microspheres by melt process |
SE9504537D0 (sv) * | 1995-12-19 | 1995-12-19 | Jan Hedner | Sätt att behandla och diagnosticera andningsstörningar under sömn och medel för utförande av sättet |
US6663899B2 (en) * | 1997-06-13 | 2003-12-16 | Genentech, Inc. | Controlled release microencapsulated NGF formulation |
CN1279065A (zh) * | 1999-07-06 | 2001-01-10 | 青岛科达生物工程有限公司 | 一种治疗记忆障碍和老年痴呆的药物组合物 |
AR023940A1 (es) * | 2000-05-03 | 2002-09-04 | Eriochem Sa | Procedimiento para la produccion de microcapsulas de liberacion prolongada de peptidos solubles en agua |
US6369052B1 (en) * | 2000-08-07 | 2002-04-09 | Georgetown University | Combination of huperzine and nicotinic compounds as a neuroprotective agent |
US6558702B2 (en) * | 2001-04-13 | 2003-05-06 | Alkermes Controlled Therapeutics, Inc. | Method of modifying the release profile of sustained release compositions |
-
2001
- 2001-07-03 CN CNB011199520A patent/CN1194688C/zh not_active Expired - Fee Related
-
2002
- 2002-07-03 WO PCT/CN2002/000472 patent/WO2003004024A1/zh not_active Application Discontinuation
- 2002-07-03 DE DE10297018T patent/DE10297018B4/de not_active Expired - Lifetime
- 2002-07-03 US US10/482,631 patent/US20040266813A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
WO2003004024A1 (fr) | 2003-01-16 |
CN1393220A (zh) | 2003-01-29 |
US20040266813A1 (en) | 2004-12-30 |
DE10297018B4 (de) | 2010-01-28 |
DE10297018T5 (de) | 2004-09-16 |
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GR01 | Patent grant | ||
C56 | Change in the name or address of the patentee |
Owner name: SHANDONG LUYE PHARMACEUTICAL CO., LTD. Free format text: FORMER NAME OR ADDRESS: SHANDONG GREEN LEAF PHARMACEUTICAL CO., LTD. |
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Address after: 264003, No. 9, Po Yuen Road, Laishan District, Shandong, Yantai Patentee after: Shandong Luye Pharma Co., Ltd. Address before: 264003, No. 9, Po Yuen Road, Laishan District, Shandong, Yantai Patentee before: Luye Pharmaceutical Co., Ltd., Shandong |
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