CN105456228B - 一种包载阿瑞吡坦纳米晶体脂质微囊及其制备方法 - Google Patents
一种包载阿瑞吡坦纳米晶体脂质微囊及其制备方法 Download PDFInfo
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- CN105456228B CN105456228B CN201510928963.2A CN201510928963A CN105456228B CN 105456228 B CN105456228 B CN 105456228B CN 201510928963 A CN201510928963 A CN 201510928963A CN 105456228 B CN105456228 B CN 105456228B
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- aprepitant
- nanocrystal
- lipid microcapsule
- lipid
- microcapsule
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- ATALOFNDEOCMKK-OITMNORJSA-N aprepitant Chemical compound O([C@@H]([C@@H]1C=2C=CC(F)=CC=2)O[C@H](C)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)CCN1CC1=NNC(=O)N1 ATALOFNDEOCMKK-OITMNORJSA-N 0.000 title claims abstract description 98
- 229960001372 aprepitant Drugs 0.000 title claims abstract description 98
- 239000002159 nanocrystal Substances 0.000 title claims abstract description 75
- 150000002632 lipids Chemical class 0.000 title claims abstract description 42
- 239000003094 microcapsule Substances 0.000 title claims abstract description 41
- 238000002360 preparation method Methods 0.000 title abstract description 13
- 238000000034 method Methods 0.000 claims abstract description 11
- 238000001035 drying Methods 0.000 claims abstract description 7
- 239000007791 liquid phase Substances 0.000 claims abstract description 7
- 238000002156 mixing Methods 0.000 claims abstract description 6
- 230000001804 emulsifying effect Effects 0.000 claims abstract description 5
- 239000000725 suspension Substances 0.000 claims description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 10
- 239000003381 stabilizer Substances 0.000 claims description 10
- 235000010445 lecithin Nutrition 0.000 claims description 8
- 239000000787 lecithin Substances 0.000 claims description 8
- 239000002245 particle Substances 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 6
- 229920002554 vinyl polymer Polymers 0.000 claims description 6
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 5
- 238000004108 freeze drying Methods 0.000 claims description 5
- 229920000578 graft copolymer Polymers 0.000 claims description 5
- 238000000227 grinding Methods 0.000 claims description 5
- 229940067606 lecithin Drugs 0.000 claims description 5
- 150000003904 phospholipids Chemical class 0.000 claims description 5
- 229920001983 poloxamer Polymers 0.000 claims description 5
- 150000003233 pyrroles Chemical class 0.000 claims description 5
- 238000001694 spray drying Methods 0.000 claims description 5
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
- 229960003943 hypromellose Drugs 0.000 claims description 4
- 229940083466 soybean lecithin Drugs 0.000 claims description 4
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 3
- 239000003960 organic solvent Substances 0.000 claims description 3
- 229960000502 poloxamer Drugs 0.000 claims description 3
- 150000002576 ketones Chemical class 0.000 claims 2
- 229920006316 polyvinylpyrrolidine Polymers 0.000 claims 2
- 230000000857 drug effect Effects 0.000 abstract description 3
- 230000002496 gastric effect Effects 0.000 abstract description 2
- 238000011031 large-scale manufacturing process Methods 0.000 abstract description 2
- 238000004519 manufacturing process Methods 0.000 abstract description 2
- 210000004877 mucosa Anatomy 0.000 abstract description 2
- 238000005498 polishing Methods 0.000 abstract description 2
- 238000010521 absorption reaction Methods 0.000 description 8
- 239000003814 drug Substances 0.000 description 8
- 239000000843 powder Substances 0.000 description 7
- 239000007788 liquid Substances 0.000 description 6
- 239000006070 nanosuspension Substances 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 5
- 239000008367 deionised water Substances 0.000 description 5
- 229910021641 deionized water Inorganic materials 0.000 description 5
- 238000004945 emulsification Methods 0.000 description 5
- 239000000243 solution Substances 0.000 description 4
- 235000010469 Glycine max Nutrition 0.000 description 3
- 244000068988 Glycine max Species 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
- 210000000577 adipose tissue Anatomy 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 235000015097 nutrients Nutrition 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 description 2
- 206010002091 Anaesthesia Diseases 0.000 description 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 1
- 102000002322 Egg Proteins Human genes 0.000 description 1
- 108010000912 Egg Proteins Proteins 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 description 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 229960001138 acetylsalicylic acid Drugs 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 230000036760 body temperature Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 229940121657 clinical drug Drugs 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000002242 deionisation method Methods 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000002183 duodenal effect Effects 0.000 description 1
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 238000011010 flushing procedure Methods 0.000 description 1
- 210000003736 gastrointestinal content Anatomy 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 210000003405 ileum Anatomy 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000007709 nanocrystallization Methods 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- 210000004681 ovum Anatomy 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- QGMRQYFBGABWDR-UHFFFAOYSA-N sodium;5-ethyl-5-pentan-2-yl-1,3-diazinane-2,4,6-trione Chemical compound [Na+].CCCC(C)C1(CC)C(=O)NC(=O)NC1=O QGMRQYFBGABWDR-UHFFFAOYSA-N 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000002627 tracheal intubation Methods 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Classifications
-
- 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
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5015—Organic compounds, e.g. fats, sugars
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
Claims (4)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CN201510928963.2A CN105456228B (zh) | 2014-12-24 | 2015-12-11 | 一种包载阿瑞吡坦纳米晶体脂质微囊及其制备方法 |
Applications Claiming Priority (3)
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CN201410814246 | 2014-12-24 | ||
CN2014108142462 | 2014-12-24 | ||
CN201510928963.2A CN105456228B (zh) | 2014-12-24 | 2015-12-11 | 一种包载阿瑞吡坦纳米晶体脂质微囊及其制备方法 |
Publications (2)
Publication Number | Publication Date |
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CN105456228A CN105456228A (zh) | 2016-04-06 |
CN105456228B true CN105456228B (zh) | 2018-06-05 |
Family
ID=55594696
Family Applications (1)
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CN201510928963.2A Active CN105456228B (zh) | 2014-12-24 | 2015-12-11 | 一种包载阿瑞吡坦纳米晶体脂质微囊及其制备方法 |
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CN (1) | CN105456228B (zh) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ITUB20161016A1 (it) * | 2016-02-24 | 2017-08-24 | Emenem Srl | Composizioni farmaceutiche o cosmetiche comprendenti un polimero e un promotore di assorbimento per il rilascio controllato di principi attivi |
CN107375238B (zh) * | 2016-05-16 | 2022-04-01 | 刘东飞 | 一种超高载药纳米粒子及其制备方法 |
CN108653236A (zh) * | 2017-03-31 | 2018-10-16 | 复旦大学 | 一种生物膜包载药物纳米晶体的制备方法及其用途 |
US11260028B2 (en) | 2017-06-26 | 2022-03-01 | Fordoz Pharma Corp. | Nanosome formulations of aprepitant and methods and applications thereof |
CN108030924B (zh) * | 2017-12-29 | 2021-01-05 | 成都百裕制药股份有限公司 | 一种高稳定性阿瑞匹坦组合物的制备方法 |
CN110478316A (zh) * | 2019-02-27 | 2019-11-22 | 江西中医药大学 | 一种阿瑞吡坦纳米结晶混悬剂及其制备方法和应用 |
CN112007012A (zh) * | 2019-05-31 | 2020-12-01 | 广州北斗生物科技有限公司 | 一种类外泌体结构的脂质微囊制备方法 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007147160A2 (en) * | 2006-06-16 | 2007-12-21 | Dr. Reddy's Laboratories Ltd. | Aprepitant compositions |
CN102920681A (zh) * | 2012-10-30 | 2013-02-13 | 浙江工业大学 | 一种以卵磷脂为载体的杨梅黄酮脂质微囊及其制备方法 |
-
2015
- 2015-12-11 CN CN201510928963.2A patent/CN105456228B/zh active Active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007147160A2 (en) * | 2006-06-16 | 2007-12-21 | Dr. Reddy's Laboratories Ltd. | Aprepitant compositions |
CN102920681A (zh) * | 2012-10-30 | 2013-02-13 | 浙江工业大学 | 一种以卵磷脂为载体的杨梅黄酮脂质微囊及其制备方法 |
Non-Patent Citations (1)
Title |
---|
纳米效应对难溶性药物阿瑞匹坦体内外性质的影响;张晓燕,等;《中国药学杂志》;20140731;第49卷(第14期);第1227-1228、1230页 * |
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Publication number | Publication date |
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CN105456228A (zh) | 2016-04-06 |
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CB03 | Change of inventor or designer information |
Inventor after: Dang Mingan Inventor after: Pan Na Inventor after: Chen Shuiku Inventor after: Liang Qian Inventor after: Luo Feng Inventor after: Liu Jinxia Inventor after: Yue Xiaohui Inventor after: Zhu Songlin Inventor after: Xiao Yan Inventor after: Meng Qingle Inventor after: Wang Yan Inventor after: Zhao Yongxing Inventor after: Cui Hao Inventor after: Chen Yongqiang Inventor after: Fang Shuixia Inventor before: Zhu Songlin Inventor before: Liang Qian Inventor before: Luo Feng Inventor before: Liu Jinxia Inventor before: Yue Xiaohui Inventor before: Xiao Yan Inventor before: Meng Qingle Inventor before: Zhao Yongxing Inventor before: Cui Hao Inventor before: Chen Yongqiang Inventor before: Fang Shuixia Inventor before: Pan Na Inventor before: Chen Shuiku |
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Effective date of registration: 20190801 Granted publication date: 20180605 |
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