CN1897975B - 口服给药的水溶性药物纳米颗粒组合物及其制备方法 - Google Patents
口服给药的水溶性药物纳米颗粒组合物及其制备方法 Download PDFInfo
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- CN1897975B CN1897975B CN2004800386637A CN200480038663A CN1897975B CN 1897975 B CN1897975 B CN 1897975B CN 2004800386637 A CN2004800386637 A CN 2004800386637A CN 200480038663 A CN200480038663 A CN 200480038663A CN 1897975 B CN1897975 B CN 1897975B
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- water soluble
- soluble drug
- lipid
- sodium
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- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61K9/08—Solutions
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- 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
- A61K9/51—Nanocapsules; Nanoparticles
- A61K9/5107—Excipients; Inactive ingredients
- A61K9/513—Organic macromolecular compounds; Dendrimers
- A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
-
- 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
- A61K9/51—Nanocapsules; Nanoparticles
- A61K9/5192—Processes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
Abstract
Description
胰岛素:多库酯钠的摩尔比 | 上清液中残余反应物 |
1∶31∶61∶9 | 20.7%0%0% |
冷冻干燥条件 | 冻干前(nm) | 冻干后(nm) | 冻干前后粒径的增加率 | |
条件1 | 室温,48小时 | 68.1 | 339.8 | 5.0 |
条件2 | 0℃:12小时→0℃:8小时→5℃:24小时 | 82.5 | 188.5 | 2.3 |
条件3 | -25℃:24小时→0℃:24小时 | 118.1 | 196.4 | 1.7 |
甘露醇 | -25℃,6小时→20℃,6小时 | |
粒径 | 冻干前后粒径的增加率 | |
0.5% | 394.1nm | 3.4 |
1% | 335.1nm | 2.8 |
2% | 321.6nm | 2.7 |
4% | 217.3nm | 1.8 |
5% | 196.4nm | 1.7 |
药物包载率(%) | |
实施例1 | 99.8 |
实施例1a | 95.7 |
实施例2 | 98.7 |
实施例3 | 97.2 |
实施例4 | 90.3 |
实施例5 | 91.3 |
实施例6 | 90.5 |
实施例7 | 92.0 |
比较实施例1 | 72.4 |
比较实施例2 | 64.8 |
比较实施例3 | 70.7 |
比较实施例4 | 92.6 |
比较实施例5 | 40.8 |
胰岛素剩余量(%) | ||||
0小时 | 1小时 | 3小时 | 5小时 | |
实施例1 | 100.0 | 95.8 | 93.6 | 91.6 |
实施例1a | 100.0 | 100.0 | 97.5 | 93.5 |
实施例3 | 100.0 | 100.0 | 97.5 | 93.5 |
实施例4 | 100.0 | 99.1 | 96.8 | 93.4 |
实施例5 | 100.0 | 92.7 | 92.0 | 91.3 |
比较实施例1 | 100.0 | 9.1 | 0.8 | 0 |
比较实施例2 | 100.0 | 87.5 | 82.6 | 82.1 |
比较实施例3 | 100.0 | 91.6 | 69.2 | 57.2 |
比较实施例4 | 100.0 | 51.2 | 14.9 | 14.5 |
Claims (19)
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020030096641 | 2003-12-24 | ||
KR10-2003-0096641 | 2003-12-24 | ||
KR1020030096641A KR100638041B1 (ko) | 2003-12-24 | 2003-12-24 | 수용성 약물의 경구투여용 나노입자 조성물 및 그의제조방법 |
PCT/KR2004/003448 WO2005061004A1 (en) | 2003-12-24 | 2004-12-24 | Nanoparticle compositions of water-soluble drugs for oral administration and preparation methods thereof |
Publications (2)
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CN1897975A CN1897975A (zh) | 2007-01-17 |
CN1897975B true CN1897975B (zh) | 2010-12-01 |
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CN2004800386637A Expired - Fee Related CN1897975B (zh) | 2003-12-24 | 2004-12-24 | 口服给药的水溶性药物纳米颗粒组合物及其制备方法 |
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US (1) | US7674767B2 (zh) |
EP (1) | EP1696961A4 (zh) |
JP (1) | JP4814107B2 (zh) |
KR (1) | KR100638041B1 (zh) |
CN (1) | CN1897975B (zh) |
AU (1) | AU2004305395B2 (zh) |
CA (1) | CA2549383C (zh) |
HK (1) | HK1096295A1 (zh) |
NZ (1) | NZ548086A (zh) |
WO (1) | WO2005061004A1 (zh) |
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AU2004305395A1 (en) | 2005-07-07 |
KR20050065014A (ko) | 2005-06-29 |
US20070154559A1 (en) | 2007-07-05 |
JP4814107B2 (ja) | 2011-11-16 |
US7674767B2 (en) | 2010-03-09 |
CN1897975A (zh) | 2007-01-17 |
JP2007517023A (ja) | 2007-06-28 |
WO2005061004A1 (en) | 2005-07-07 |
CA2549383A1 (en) | 2005-07-07 |
CA2549383C (en) | 2010-08-31 |
EP1696961A4 (en) | 2010-09-01 |
NZ548086A (en) | 2008-03-28 |
AU2004305395B2 (en) | 2008-05-22 |
KR100638041B1 (ko) | 2006-10-23 |
EP1696961A1 (en) | 2006-09-06 |
HK1096295A1 (en) | 2007-06-01 |
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