CN101103972A - 一种奥沙利铂脂质体葡萄糖制剂及其制备方法、应用 - Google Patents
一种奥沙利铂脂质体葡萄糖制剂及其制备方法、应用 Download PDFInfo
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- CN101103972A CN101103972A CNA2007100251300A CN200710025130A CN101103972A CN 101103972 A CN101103972 A CN 101103972A CN A2007100251300 A CNA2007100251300 A CN A2007100251300A CN 200710025130 A CN200710025130 A CN 200710025130A CN 101103972 A CN101103972 A CN 101103972A
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- liposome
- glucose
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- oxaliplatin
- oxaliplatinum
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- 239000002502 liposome Substances 0.000 title claims abstract description 77
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 title claims abstract description 54
- 239000008103 glucose Substances 0.000 title claims abstract description 54
- 238000002360 preparation method Methods 0.000 title claims abstract description 44
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims abstract description 67
- 229960001756 oxaliplatin Drugs 0.000 claims abstract description 67
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims abstract description 48
- 238000001035 drying Methods 0.000 claims abstract description 25
- 235000012000 cholesterol Nutrition 0.000 claims abstract description 24
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims abstract description 16
- 229920006395 saturated elastomer Polymers 0.000 claims abstract description 6
- 239000000243 solution Substances 0.000 claims description 35
- 238000005984 hydrogenation reaction Methods 0.000 claims description 15
- 238000012856 packing Methods 0.000 claims description 15
- 238000000859 sublimation Methods 0.000 claims description 15
- 230000008022 sublimation Effects 0.000 claims description 15
- 238000001914 filtration Methods 0.000 claims description 13
- 150000003904 phospholipids Chemical class 0.000 claims description 13
- 239000002245 particle Substances 0.000 claims description 10
- 238000003756 stirring Methods 0.000 claims description 10
- 238000002347 injection Methods 0.000 claims description 9
- 239000007924 injection Substances 0.000 claims description 9
- 239000012528 membrane Substances 0.000 claims description 9
- 239000000843 powder Substances 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- JGSARLDLIJGVTE-UHFFFAOYSA-N 3,3-dimethyl-7-oxo-6-[(2-phenylacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid Chemical compound O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-UHFFFAOYSA-N 0.000 claims description 5
- 206010013786 Dry skin Diseases 0.000 claims description 5
- 239000007864 aqueous solution Substances 0.000 claims description 5
- 210000000481 breast Anatomy 0.000 claims description 5
- 229940079593 drug Drugs 0.000 claims description 5
- 230000001804 emulsifying effect Effects 0.000 claims description 5
- 239000000706 filtrate Substances 0.000 claims description 5
- 238000004108 freeze drying Methods 0.000 claims description 5
- 238000010438 heat treatment Methods 0.000 claims description 5
- 238000009413 insulation Methods 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 5
- 239000012982 microporous membrane Substances 0.000 claims description 5
- 239000002105 nanoparticle Substances 0.000 claims description 5
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- 238000005303 weighing Methods 0.000 claims description 5
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- 229920001427 mPEG Polymers 0.000 claims description 3
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- 238000011275 oncology therapy Methods 0.000 claims description 2
- 238000000926 separation method Methods 0.000 claims description 2
- 238000000746 purification Methods 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 abstract description 3
- 239000000839 emulsion Substances 0.000 abstract description 3
- 238000001816 cooling Methods 0.000 abstract 1
- 150000003017 phosphorus Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
- 230000001093 anti-cancer Effects 0.000 description 10
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- 239000008280 blood Substances 0.000 description 8
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- 230000000694 effects Effects 0.000 description 5
- 230000001988 toxicity Effects 0.000 description 5
- 231100000419 toxicity Toxicity 0.000 description 5
- 210000003734 kidney Anatomy 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 206010065553 Bone marrow failure Diseases 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229960004316 cisplatin Drugs 0.000 description 3
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 3
- 238000010253 intravenous injection Methods 0.000 description 3
- 229940104914 oxaliplatin injection Drugs 0.000 description 3
- 206010051779 Bone marrow toxicity Diseases 0.000 description 2
- 230000000259 anti-tumor effect Effects 0.000 description 2
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- 230000007774 longterm Effects 0.000 description 2
- PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 1
- 101001105486 Homo sapiens Proteasome subunit alpha type-7 Proteins 0.000 description 1
- 241000699660 Mus musculus Species 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 102100021201 Proteasome subunit alpha type-7 Human genes 0.000 description 1
- 230000000118 anti-neoplastic effect Effects 0.000 description 1
- 229940034982 antineoplastic agent Drugs 0.000 description 1
- 229940041181 antineoplastic drug Drugs 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 201000008275 breast carcinoma Diseases 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000000105 evaporative light scattering detection Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000007710 freezing Methods 0.000 description 1
- 230000008014 freezing Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 238000011580 nude mouse model Methods 0.000 description 1
- 239000003186 pharmaceutical solution Substances 0.000 description 1
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- 238000004445 quantitative analysis Methods 0.000 description 1
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- 239000006228 supernatant Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000005199 ultracentrifugation Methods 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
Description
放置时间(月) | 0 | 3 |
性状pH值粒径(nm)Zeta电位(mV)含量(%)包封率(%)DSPE-PEG2000(mg/ml)CHOL(mg/ml)HSPC(mg/ml) | 类白色乳状液6.94129-7.34103.099.6214.7211.9049.21 | 类白色乳状液6.90130-7.8101.299.6413.9012.4949.47 |
组别 | 白鼠数量/性别 | 剂量(mg/Kg) | 抗癌结果(T/C%) |
5%葡萄糖对照空白脂质体对照奥沙利铂脂质体溶液奥沙利铂注射液 | 10/雌10/雌10/雌10/雌 | 0055 | 10099.542.581.2 |
Claims (8)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CNB2007100251300A CN100563646C (zh) | 2007-07-13 | 2007-07-13 | 一种奥沙利铂脂质体葡萄糖制剂的制备方法 |
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CNB2007100251300A CN100563646C (zh) | 2007-07-13 | 2007-07-13 | 一种奥沙利铂脂质体葡萄糖制剂的制备方法 |
Publications (2)
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CN101103972A true CN101103972A (zh) | 2008-01-16 |
CN100563646C CN100563646C (zh) | 2009-12-02 |
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CNB2007100251300A Active CN100563646C (zh) | 2007-07-13 | 2007-07-13 | 一种奥沙利铂脂质体葡萄糖制剂的制备方法 |
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Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2011047689A3 (en) * | 2009-10-23 | 2011-11-17 | Bio-Bedst Aps | Spla2 hydrolysable liposomes with improved storage stability |
CN102665689A (zh) * | 2009-09-21 | 2012-09-12 | Jw制药公司 | 奥沙利铂纳米颗粒及其制备方法 |
CN102697741A (zh) * | 2012-06-29 | 2012-10-03 | 海南灵康制药有限公司 | 一种奥沙利铂囊泡型磷脂凝胶注射剂 |
CN103181898A (zh) * | 2012-11-23 | 2013-07-03 | 杭州师范大学 | 一种奥沙利铂脂质体及其应用 |
CN105232460A (zh) * | 2015-09-24 | 2016-01-13 | 南京泛太化工医药研究所 | 一种奥沙利铂脂质体冻干粉针剂的制备和应用 |
CN105412025A (zh) * | 2015-12-31 | 2016-03-23 | 中国药科大学 | 一种奥沙利铂脂质体冻干粉针剂的制备方法 |
EA023757B1 (ru) * | 2012-12-24 | 2016-07-29 | Общество С Ограниченной Ответственностью "Технология Лекарств" | Способ получения липосомальной формы оксалиплатина |
CN106955271A (zh) * | 2016-01-08 | 2017-07-18 | 佛山英特医药科技有限公司 | 奥沙利铂聚集体及其制备方法 |
CN107998080A (zh) * | 2017-11-21 | 2018-05-08 | 东南大学 | 一种偶联抗体的主动靶向载药长循环脂质体及其制备方法 |
CN110507613A (zh) * | 2019-07-29 | 2019-11-29 | 苏州大学 | 一种脂质体制剂及其制备方法与应用 |
-
2007
- 2007-07-13 CN CNB2007100251300A patent/CN100563646C/zh active Active
Cited By (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102665689A (zh) * | 2009-09-21 | 2012-09-12 | Jw制药公司 | 奥沙利铂纳米颗粒及其制备方法 |
WO2011047689A3 (en) * | 2009-10-23 | 2011-11-17 | Bio-Bedst Aps | Spla2 hydrolysable liposomes with improved storage stability |
CN102639114A (zh) * | 2009-10-23 | 2012-08-15 | 拜奧贝德斯特有限责任公司 | 经改善贮藏稳定性的脂质体 |
CN102639114B (zh) * | 2009-10-23 | 2015-04-01 | 拜奧贝德斯特有限责任公司 | 经改善贮藏稳定性的脂质体 |
US9820941B2 (en) | 2009-10-23 | 2017-11-21 | Bio-Bedst Aps | SPLA2 hydrolysable liposomes with improved storage stability |
CN102697741A (zh) * | 2012-06-29 | 2012-10-03 | 海南灵康制药有限公司 | 一种奥沙利铂囊泡型磷脂凝胶注射剂 |
CN103181898A (zh) * | 2012-11-23 | 2013-07-03 | 杭州师范大学 | 一种奥沙利铂脂质体及其应用 |
CN103181898B (zh) * | 2012-11-23 | 2016-03-09 | 杭州师范大学 | 一种奥沙利铂脂质体及其应用 |
EA023757B1 (ru) * | 2012-12-24 | 2016-07-29 | Общество С Ограниченной Ответственностью "Технология Лекарств" | Способ получения липосомальной формы оксалиплатина |
CN105232460A (zh) * | 2015-09-24 | 2016-01-13 | 南京泛太化工医药研究所 | 一种奥沙利铂脂质体冻干粉针剂的制备和应用 |
CN105412025A (zh) * | 2015-12-31 | 2016-03-23 | 中国药科大学 | 一种奥沙利铂脂质体冻干粉针剂的制备方法 |
CN106955271A (zh) * | 2016-01-08 | 2017-07-18 | 佛山英特医药科技有限公司 | 奥沙利铂聚集体及其制备方法 |
CN107998080A (zh) * | 2017-11-21 | 2018-05-08 | 东南大学 | 一种偶联抗体的主动靶向载药长循环脂质体及其制备方法 |
CN110507613A (zh) * | 2019-07-29 | 2019-11-29 | 苏州大学 | 一种脂质体制剂及其制备方法与应用 |
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CN100563646C (zh) | 2009-12-02 |
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Owner name: JIANGSU AOSAIKANG PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: CHEN XIANGFENG Effective date: 20110324 Free format text: FORMER OWNER: CAI KEXIA |
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Effective date of registration: 20110324 Address after: 211112 Jiangsu Province, Nanjing City, Jiangning Science Park Road No. 699 Patentee after: Jiangsu Aosaikang Pharmaceutical Co., Ltd. Address before: 210017, room 44, 1-203 West Lake Street, Jianye District, Jiangsu, Nanjing, China Co-patentee before: Cai Kexia Patentee before: Chen Xiangfeng |
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Address after: 211112 Jiangsu Province, Nanjing City, Jiangning Science Park Road No. 699 Patentee after: Jiangsu Aosaikang Pharmaceutical Co., Ltd. Address before: 211112 Jiangsu Province, Nanjing City, Jiangning Science Park Road No. 699 Patentee before: Jiangsu Aosaikang Pharmaceutical Co., Ltd. |
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Address after: 211112 Jiangsu Province, Nanjing City, Jiangning Science Park Road No. 699 Patentee after: Jiangsu Aosaikang Pharmaceutical Co., Ltd. Address before: 211112 Jiangsu Province, Nanjing City, Jiangning Science Park Road No. 699 Patentee before: Jiangsu Aosaikang Pharmaceutical Co., Ltd. |
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