CN110997666A - N-甲酰基帕博西尼及其制备方法和用途以及帕博西尼制剂及其质量控制方法 - Google Patents
N-甲酰基帕博西尼及其制备方法和用途以及帕博西尼制剂及其质量控制方法 Download PDFInfo
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- CN110997666A CN110997666A CN201780093736.XA CN201780093736A CN110997666A CN 110997666 A CN110997666 A CN 110997666A CN 201780093736 A CN201780093736 A CN 201780093736A CN 110997666 A CN110997666 A CN 110997666A
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- palbociclib
- formate
- acid
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- chloroformate
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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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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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
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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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
一种帕博西尼固体制剂中的降解杂质N‑甲酰基帕博西尼、其制备方法,及其在帕博西尼固体制剂处方研究、杂质检测中的应用。还提供了一种稳定化的帕博西尼固体制剂及其制备方法。N‑甲酰基帕博西尼制备方法,产物收率可达50%以上,纯度可达90%以上,其具有工艺简单,产物纯度高、生产周期较短、适合实验室快速制备及能大规模制备等优点。获得的帕博西尼固体制剂其稳定性提高,在60℃,75%相对湿度条件下放置10天后,帕博西尼固体制剂中N‑甲酰基帕博西尼杂质也未见增长。
Description
PCT国内申请,说明书已公开。
Claims (14)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (1)
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PCT/CN2017/102219 WO2019056163A1 (zh) | 2017-09-19 | 2017-09-19 | N-甲酰基帕博西尼及其制备方法和用途以及帕博西尼制剂及其质量控制方法 |
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CN110997666A true CN110997666A (zh) | 2020-04-10 |
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CN201780093736.XA Pending CN110997666A (zh) | 2017-09-19 | 2017-09-19 | N-甲酰基帕博西尼及其制备方法和用途以及帕博西尼制剂及其质量控制方法 |
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CN (1) | CN110997666A (zh) |
WO (1) | WO2019056163A1 (zh) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN112274493A (zh) * | 2020-11-18 | 2021-01-29 | 石药集团中奇制药技术(石家庄)有限公司 | 一种哌柏西利胶囊的制备方法 |
US11464779B2 (en) | 2016-03-29 | 2022-10-11 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
US11471418B2 (en) | 2020-09-29 | 2022-10-18 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical compositions of amorphous solid dispersions and methods of preparation thereof |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN112961152B (zh) * | 2020-02-26 | 2021-11-12 | 北京新康哌森医药科技有限公司 | 一种帕布昔利布杂质的合成方法 |
CN111362938A (zh) * | 2020-04-14 | 2020-07-03 | 北京鑫开元医药科技有限公司 | 一种帕布昔利布杂质、其制备方法及用途 |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105418603A (zh) * | 2015-11-17 | 2016-03-23 | 重庆莱美药业股份有限公司 | 一种高纯度帕布昔利布及其反应中间体的制备方法 |
CN105748435A (zh) * | 2016-04-21 | 2016-07-13 | 石家庄海瑞药物科技有限公司 | 一种帕布昔利布药物组合物及其制备方法 |
CN106667952A (zh) * | 2016-12-12 | 2017-05-17 | 河南润弘制药股份有限公司 | 一种帕布昔利布药物组合物及其制备方法 |
CN107666914A (zh) * | 2015-06-04 | 2018-02-06 | 辉瑞公司 | 帕博西尼的固体剂型 |
CN111239299A (zh) * | 2020-03-30 | 2020-06-05 | 重庆三圣实业股份有限公司 | 一种分离测定帕博西尼及其杂质的方法 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105616419A (zh) * | 2014-11-07 | 2016-06-01 | 江苏豪森药业集团有限公司 | 含有细胞周期蛋白抑制剂固体分散体的药物组合物及其制备方法 |
CN106474129A (zh) * | 2015-09-01 | 2017-03-08 | 上海方楠生物科技有限公司 | 一种帕博西林或其药学上可接受的盐与药用辅料的组合物及其制备方法 |
CN105213322A (zh) * | 2015-10-30 | 2016-01-06 | 南京正大天晴制药有限公司 | 一种干法制粒工艺制备的药物组合物 |
CN106924210A (zh) * | 2015-12-29 | 2017-07-07 | 北京新领先医药科技发展有限公司 | 一种含有帕布昔利布的胶囊剂及其制备方法 |
CN105816437B (zh) * | 2016-03-29 | 2018-08-03 | 深圳市药欣生物科技有限公司 | 一种帕布昔利布的药物制剂及其制备方法 |
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2017
- 2017-09-19 WO PCT/CN2017/102219 patent/WO2019056163A1/zh active Application Filing
- 2017-09-19 CN CN201780093736.XA patent/CN110997666A/zh active Pending
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107666914A (zh) * | 2015-06-04 | 2018-02-06 | 辉瑞公司 | 帕博西尼的固体剂型 |
CN105418603A (zh) * | 2015-11-17 | 2016-03-23 | 重庆莱美药业股份有限公司 | 一种高纯度帕布昔利布及其反应中间体的制备方法 |
CN105748435A (zh) * | 2016-04-21 | 2016-07-13 | 石家庄海瑞药物科技有限公司 | 一种帕布昔利布药物组合物及其制备方法 |
CN106667952A (zh) * | 2016-12-12 | 2017-05-17 | 河南润弘制药股份有限公司 | 一种帕布昔利布药物组合物及其制备方法 |
CN111239299A (zh) * | 2020-03-30 | 2020-06-05 | 重庆三圣实业股份有限公司 | 一种分离测定帕博西尼及其杂质的方法 |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11464779B2 (en) | 2016-03-29 | 2022-10-11 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
US11471418B2 (en) | 2020-09-29 | 2022-10-18 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical compositions of amorphous solid dispersions and methods of preparation thereof |
CN112274493A (zh) * | 2020-11-18 | 2021-01-29 | 石药集团中奇制药技术(石家庄)有限公司 | 一种哌柏西利胶囊的制备方法 |
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WO2019056163A1 (zh) | 2019-03-28 |
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