CN110548008A - 阿考替胺固体分散体及其组合物 - Google Patents
阿考替胺固体分散体及其组合物 Download PDFInfo
- Publication number
- CN110548008A CN110548008A CN201910408704.5A CN201910408704A CN110548008A CN 110548008 A CN110548008 A CN 110548008A CN 201910408704 A CN201910408704 A CN 201910408704A CN 110548008 A CN110548008 A CN 110548008A
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- Prior art keywords
- acotiamide
- solid dispersion
- composition
- taste
- polyethylene glycol
- Prior art date
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- 229950005462 acotiamide Drugs 0.000 title claims abstract description 151
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- 239000000230 xanthan gum Substances 0.000 claims description 24
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- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 23
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- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 1
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- 238000010521 absorption reaction Methods 0.000 description 1
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- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 description 1
- 229940022698 acetylcholinesterase Drugs 0.000 description 1
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- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 230000010100 anticoagulation Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000000305 astragalus gummifer gum Substances 0.000 description 1
- 235000019606 astringent taste Nutrition 0.000 description 1
- 235000019611 bitter taste sensations Nutrition 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 229960002303 citric acid monohydrate Drugs 0.000 description 1
- 230000015271 coagulation Effects 0.000 description 1
- 238000005345 coagulation Methods 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 238000005520 cutting process Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 238000007865 diluting Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 210000003194 forelimb Anatomy 0.000 description 1
- 235000019525 fullness Nutrition 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 230000030136 gastric emptying Effects 0.000 description 1
- 210000002599 gastric fundus Anatomy 0.000 description 1
- 230000030135 gastric motility Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000000665 guar gum Substances 0.000 description 1
- 235000010417 guar gum Nutrition 0.000 description 1
- 229960002154 guar gum Drugs 0.000 description 1
- 229960002897 heparin Drugs 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 description 1
- 238000009776 industrial production Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 238000010309 melting process Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- NPTDXIXCQCFGKC-UHFFFAOYSA-N n-[2-[di(propan-2-yl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide;trihydrate;hydrochloride Chemical compound O.O.O.Cl.C1=C(OC)C(OC)=CC(O)=C1C(=O)NC1=NC(C(=O)NCCN(C(C)C)C(C)C)=CS1 NPTDXIXCQCFGKC-UHFFFAOYSA-N 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 239000007935 oral tablet Substances 0.000 description 1
- 229940096978 oral tablet Drugs 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 230000000291 postprandial effect Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 235000019643 salty taste Nutrition 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000030812 sensory perception of bitter taste Effects 0.000 description 1
- 238000010008 shearing Methods 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- OKODKVMXHLUQSW-JITBQSAISA-M sodium;(e)-4-hydroxy-4-oxobut-2-enoate;octadecanoic acid Chemical compound [Na+].OC(=O)\C=C\C([O-])=O.CCCCCCCCCCCCCCCCCC(O)=O OKODKVMXHLUQSW-JITBQSAISA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
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- 230000009747 swallowing Effects 0.000 description 1
- 235000019605 sweet taste sensations Nutrition 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 210000001779 taste bud Anatomy 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
-
- 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
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- Health & Medical Sciences (AREA)
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- General Chemical & Material Sciences (AREA)
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- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇EPO | 100.00 |
合计 | 200.00 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇L100-55 | 200.00 |
泊洛沙姆P188 | 33.33 |
合计 | 333.33 |
组分 | 处方比例(%) |
盐酸阿考替胺 | 18.0 |
尤特奇L100-55 | 72.0 |
硬脂酸 | 10.0 |
合计 | 100.0 |
组分 | 单位剂量(mg) |
盐酸阿考替胺掩味颗粒 | 555.55 |
山梨醇 | 480.00 |
甘露醇 | 480.00 |
黄原胶 | 40.00 |
三氯蔗糖 | 5.00 |
橙子香精 | 10.00 |
合计 | 1570.55 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇EPO | 500.00 |
合计 | 600.00 |
组分 | 单位剂量(mg) |
盐酸阿考替胺掩味颗粒 | 600.00 |
山梨醇 | 480.00 |
甘露醇 | 480.00 |
黄原胶 | 40.00 |
三氯蔗糖 | 5.00 |
橙子香精 | 10.00 |
合计 | 1615.00 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇L100-55 | 1000.00 |
硬脂酸 | 122.22 |
合计 | 1222.22 |
组分 | 单位剂量(mg) |
盐酸阿考替胺掩味颗粒 | 1222.22 |
山梨醇 | 960.00 |
甘露醇 | 960.00 |
黄原胶 | 80.00 |
三氯蔗糖 | 10.00 |
橙子香精 | 20.00 |
合计 | 3252.22 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇EPO | 3000.00 |
合计 | 3100.00 |
组分 | 单位剂量(mg) |
盐酸阿考替胺掩味颗粒 | 3100.00 |
山梨醇 | 1920.00 |
甘露醇 | 1920.00 |
黄原胶 | 240.00 |
三氯蔗糖 | 30.00 |
橙子香精 | 20.00 |
合计 | 7230.00 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇EPO | 5000.00 |
合计 | 5100.00 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇L100-55 | 2000.00 |
泊洛沙姆P188 | 233.33 |
合计 | 2333.33 |
组分 | 处方比例(%) |
盐酸阿考替胺 | 10.0 |
蔗糖 | 73.5 |
一水柠檬酸 | 14.0 |
羟丙甲纤维素 | 1.0 |
阿斯巴甜 | 1.0 |
草莓香精 | 0.5 |
合计 | 100.0 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
尤特奇L100-55 | 50.00 |
硬脂酸 | 16.67 |
合计 | 166.67 |
组分 | 单位剂量(mg) |
盐酸阿考替胺掩味颗粒 | 166.67 |
山梨醇 | 480.00 |
甘露醇 | 480.00 |
黄原胶 | 40.00 |
三氯蔗糖 | 5.00 |
橙子香精 | 10.00 |
合计 | 1181.67 |
组分 | 单位剂量(mg) |
盐酸阿考替胺 | 100.00 |
HPMCAS-HG | 400.00 |
硬脂酸 | 55.55 |
合计 | 555.55 |
样品序号 | 对应实施例 |
1 | 对比实施例2 |
2 | 对比实施例1 |
3 | 盐酸阿考替胺原料药粉末 |
4 | 实施例7 |
5 | 实施例5 |
6 | 实施例2 |
7 | 实施例6 |
8 | 实施例4 |
9 | 实施例8 |
样品名称 | 参照品 | 距离(↓) |
2 | 3 | 367.19 |
1 | 3 | 574.30 |
6 | 3 | 651.20 |
5 | 3 | 845.03 |
9 | 3 | 883.99 |
8 | 3 | 1520.71 |
7 | 3 | 1642.33 |
4 | 3 | 2261.07 |
Claims (14)
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CN2018105577827 | 2018-06-01 |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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CN113350291A (zh) * | 2020-03-04 | 2021-09-07 | 广东东阳光药业有限公司 | 一种乙酰胆碱酯酶抑制剂的组合物及其制备方法 |
CN114522166A (zh) * | 2022-04-22 | 2022-05-24 | 北京剂泰医药科技有限公司 | 一种固体分散体组合物及其制备方法和应用 |
Citations (5)
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US20100055133A1 (en) * | 2008-08-12 | 2010-03-04 | Biovail Laboratories International (Barbados) S.R.L | Pharmaceutical compositions |
WO2014029953A1 (en) * | 2012-08-21 | 2014-02-27 | Cipla Limited | Hot melt extruded (hme) pharmaceutical composition of cinacalcet |
CN105232486A (zh) * | 2015-07-20 | 2016-01-13 | 广西大学 | 一种氟尼辛葡甲胺掩味口腔崩解制剂及其制备方法 |
CN105343009A (zh) * | 2015-11-09 | 2016-02-24 | 米克珐玛(苏州)生物医药有限公司 | 富马酸卢帕他定掩味干混悬剂 |
CN106511291A (zh) * | 2016-09-24 | 2017-03-22 | 济南康和医药科技有限公司 | 一种盐酸阿考替胺缓释片剂及其制备方法 |
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2019
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US20100055133A1 (en) * | 2008-08-12 | 2010-03-04 | Biovail Laboratories International (Barbados) S.R.L | Pharmaceutical compositions |
WO2014029953A1 (en) * | 2012-08-21 | 2014-02-27 | Cipla Limited | Hot melt extruded (hme) pharmaceutical composition of cinacalcet |
CN105232486A (zh) * | 2015-07-20 | 2016-01-13 | 广西大学 | 一种氟尼辛葡甲胺掩味口腔崩解制剂及其制备方法 |
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CN106511291A (zh) * | 2016-09-24 | 2017-03-22 | 济南康和医药科技有限公司 | 一种盐酸阿考替胺缓释片剂及其制备方法 |
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CN114522166A (zh) * | 2022-04-22 | 2022-05-24 | 北京剂泰医药科技有限公司 | 一种固体分散体组合物及其制备方法和应用 |
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