CN114681459A - 伊布替尼药物组合物、其制备方法及应用 - Google Patents
伊布替尼药物组合物、其制备方法及应用 Download PDFInfo
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- CN114681459A CN114681459A CN202111557994.3A CN202111557994A CN114681459A CN 114681459 A CN114681459 A CN 114681459A CN 202111557994 A CN202111557994 A CN 202111557994A CN 114681459 A CN114681459 A CN 114681459A
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- ibrutinib
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 76
- 238000002360 preparation method Methods 0.000 title abstract description 19
- 239000002177 L01XE27 - Ibrutinib Substances 0.000 claims abstract description 99
- XYFPWWZEPKGCCK-GOSISDBHSA-N ibrutinib Chemical compound C1=2C(N)=NC=NC=2N([C@H]2CN(CCC2)C(=O)C=C)N=C1C(C=C1)=CC=C1OC1=CC=CC=C1 XYFPWWZEPKGCCK-GOSISDBHSA-N 0.000 claims abstract description 99
- 229960001507 ibrutinib Drugs 0.000 claims abstract description 99
- 239000007957 coemulsifier Substances 0.000 claims abstract description 18
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 18
- 239000003814 drug Substances 0.000 claims description 21
- GHHURQMJLARIDK-UHFFFAOYSA-N 2-hydroxypropyl octanoate Chemical group CCCCCCCC(=O)OCC(C)O GHHURQMJLARIDK-UHFFFAOYSA-N 0.000 claims description 18
- 229920001213 Polysorbate 20 Polymers 0.000 claims description 18
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical group CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims description 18
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 claims description 18
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 18
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 18
- 239000004530 micro-emulsion Substances 0.000 claims description 14
- 229940079593 drug Drugs 0.000 claims description 12
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 claims description 4
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 claims description 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 210000003719 b-lymphocyte Anatomy 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 229920000136 polysorbate Polymers 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 2
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 201000003444 follicular lymphoma Diseases 0.000 claims description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 2
- 229920000053 polysorbate 80 Polymers 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000004973 liquid crystal related substance Substances 0.000 claims 1
- 239000000463 material Substances 0.000 claims 1
- 238000004090 dissolution Methods 0.000 abstract description 5
- 238000003860 storage Methods 0.000 abstract description 5
- 238000010579 first pass effect Methods 0.000 abstract description 3
- 230000002440 hepatic effect Effects 0.000 abstract description 3
- 238000009776 industrial production Methods 0.000 abstract description 2
- 239000000203 mixture Substances 0.000 description 10
- 239000002245 particle Substances 0.000 description 6
- 238000009210 therapy by ultrasound Methods 0.000 description 5
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 description 4
- 239000008187 granular material Substances 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- 238000005303 weighing Methods 0.000 description 4
- 239000002775 capsule Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 210000002751 lymph Anatomy 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- MKYBYDHXWVHEJW-UHFFFAOYSA-N N-[1-oxo-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propan-2-yl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(C(C)NC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 MKYBYDHXWVHEJW-UHFFFAOYSA-N 0.000 description 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 210000003240 portal vein Anatomy 0.000 description 1
- 230000002250 progressing effect Effects 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 230000002992 thymic effect Effects 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Dispersion Chemistry (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
成分 | 重量(mg/粒) | 占比(重量%) |
伊布替尼 | 100 | 9.09 |
丙二醇单辛酸酯 | 229.5 | 20.86 |
吐温20 | 536.4 | 48.75 |
二乙二醇单乙基醚 | 234.3 | 21.30 |
成分 | 重量(mg/粒) | 占比(重量%) |
伊布替尼 | 100 | 9.09 |
丙二醇单辛酸酯 | 370.7 | 33.70 |
吐温20 | 438.0 | 39.82 |
二乙二醇单乙基醚 | 191.3 | 17.39 |
成分 | 重量(mg/粒) | 占比(重量%) |
伊布替尼 | 100 | 9.17 |
丙二醇单辛酸酯 | 297.1 | 27.25 |
吐温20 | 462.2 | 42.39 |
二乙二醇单乙基醚 | 231.1 | 21.19 |
成分 | 重量(mg/粒) | 占比(重量%) |
伊布替尼 | 100 | 9.07 |
丙二醇单辛酸酯 | 200.1 | 18.16 |
吐温20 | 601.5 | 54.58 |
二乙二醇单乙基醚 | 200.5 | 18.19 |
项目 | 实施例1 | 实施例2 | 实施例3 | 实施例4 |
粒径(nm) | 237.02 | 285.73 | 400.68 | 81.61 |
Claims (10)
Applications Claiming Priority (2)
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CN2020116032224 | 2020-12-29 | ||
CN202011603222 | 2020-12-29 |
Publications (2)
Publication Number | Publication Date |
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CN114681459A true CN114681459A (zh) | 2022-07-01 |
CN114681459B CN114681459B (zh) | 2024-02-27 |
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Application Number | Title | Priority Date | Filing Date |
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CN202111557994.3A Active CN114681459B (zh) | 2020-12-29 | 2021-12-20 | 伊布替尼药物组合物、其制备方法及应用 |
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Country | Link |
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CN (1) | CN114681459B (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115192522A (zh) * | 2022-08-24 | 2022-10-18 | 烟台慧暄医药科技有限公司 | 一种含有伊布替尼的组合物及其制备方法和应用 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104039325A (zh) * | 2011-10-19 | 2014-09-10 | 药品循环公司 | 布鲁顿酪氨酸激酶(btk)抑制剂的用途 |
CN113440481A (zh) * | 2021-08-13 | 2021-09-28 | 湖南慧泽生物医药科技有限公司 | 伊布替尼的自微乳组合物 |
-
2021
- 2021-12-20 CN CN202111557994.3A patent/CN114681459B/zh active Active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104039325A (zh) * | 2011-10-19 | 2014-09-10 | 药品循环公司 | 布鲁顿酪氨酸激酶(btk)抑制剂的用途 |
CN113440481A (zh) * | 2021-08-13 | 2021-09-28 | 湖南慧泽生物医药科技有限公司 | 伊布替尼的自微乳组合物 |
Non-Patent Citations (1)
Title |
---|
冯年平等主编: "《中药经皮给药与功效性化妆品》", 中国医药科技出版社, pages: 334 - 174 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115192522A (zh) * | 2022-08-24 | 2022-10-18 | 烟台慧暄医药科技有限公司 | 一种含有伊布替尼的组合物及其制备方法和应用 |
CN115192522B (zh) * | 2022-08-24 | 2024-05-28 | 烟台慧暄医药科技有限公司 | 一种含有伊布替尼的组合物及其制备方法和应用 |
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CN114681459B (zh) | 2024-02-27 |
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Address after: 201203 Building 1, Lane 647, Songtao Road, Zhangjiang High Tech Park, Pudong New Area, Shanghai Applicant after: Shanghai Yunshengyan neoplasm Technology Co.,Ltd. Applicant after: Shanghai bozhiyan new drug research Co.,Ltd. Address before: 201203 Building 1, Lane 647, Songtao Road, Zhangjiang High Tech Park, Pudong New Area, Shanghai Applicant before: SHANGHAI BOCIMED PHARMACEUTICAL Co.,Ltd. Applicant before: Shanghai bozhiyan new drug research Co.,Ltd. |
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Effective date of registration: 20230516 Address after: 201203 Building 1, Lane 647, Songtao Road, Zhangjiang High Tech Park, Pudong New Area, Shanghai Applicant after: Shanghai Yunshengyan neoplasm Technology Co.,Ltd. Address before: 201203 Building 1, Lane 647, Songtao Road, Zhangjiang High Tech Park, Pudong New Area, Shanghai Applicant before: Shanghai Yunshengyan neoplasm Technology Co.,Ltd. Applicant before: Shanghai bozhiyan new drug research Co.,Ltd. |
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