CN1074923C - 微囊密封的3-哌啶基取代的1,2-苯并异唑类和1,2-苯并异噻唑类 - Google Patents
微囊密封的3-哌啶基取代的1,2-苯并异唑类和1,2-苯并异噻唑类 Download PDFInfo
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- CN1074923C CN1074923C CN94194190A CN94194190A CN1074923C CN 1074923 C CN1074923 C CN 1074923C CN 94194190 A CN94194190 A CN 94194190A CN 94194190 A CN94194190 A CN 94194190A CN 1074923 C CN1074923 C CN 1074923C
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- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
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- 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
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- 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
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- 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
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Chemical & Material Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
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- Organic Chemistry (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Medicinal Preparation (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
表1:在给狗进行肌肉注射一种含有约2.5mg/kg剂量抗精神病的risperdone的微粒后,在一段连续的时间间隔内对阿朴吗啡引发的呕吐有无拮抗作用:有(+);无(-) | |||||
项目 | Prodex 2 | Prodex 3 | Prodex 4A | Prodex 4B | Prodex 4C |
狗重(kg) | 14.2 11.5 9 8 | 12.9 12.4 13.4 | 10.0 12.3 9.2 | 9.7 8.6 10.6 | 13.2 16.4 16.2 |
体积(ml/狗) | 0.5’ 0.5’ 0.5’ | 0.5’ 0.5’ 0.5’ | 0.5’ 0.5’ 0.5’ | 0.5’ 0.5’ 0.5’ | 0.5’ 0.5’ 0.5’ |
剂量(mg/kg) | 2.5 2.5 2.8 | 2.5 2.5 2.5 | 2.5 2.3 2.6 | 2.5 2.5 2.6 | 2.4 2.4 2.5 |
时间经过 | im im im | im im im | im im im | im im im | im im im |
1h | + + - | + + + | + + + | - + + | + + + |
5h | + + + | + + + | + + + | + - + | + + + |
1d | + + + | + + + | + + + | + + + | + + + |
4d | - - + | + - + | + + - | - - + | + + + |
7d | - - - | - + + | - - - | - - + | + + + |
11d | - - - | + + + | + + - | - - + | + + + |
14d | - | + + + | + + + | - + + | + + + |
18d | + + + | + + + | + + + | + + + | |
21d | + + + | + + + | + + + | + + + | |
25d | + + + | + + + | + + + | + + + | + + + |
29d | + + + | + + + | + + + | + + + | + + + |
32d | + + + | + + + | + + + | + + + | + + + |
35d | + + + | + + + | + + + | + + + | + + + |
表1:在给狗进行肌肉注射一种含有约2.5mg/kg剂量抗精神病的risperdone的微粒后,在一段连续的时间间隔内对阿朴吗啡引发的呕吐有无拮抗作用:有(+);无(-) | |||||
39d | - + + | + - + | + + - | - - - | + + + |
42d | - - - | + - + | + - - | - - - | + + - |
46d | - - - | + - - | - - - | - - - | + + - |
49d | 停止 | - - - | - - - | 停止 | + + - |
53d | 停止 | 停止 | - + - | ||
56d | - - - | ||||
停止 | |||||
3注射体积:0.5ml/狗;微粒的浓度根据狗的体重选择 |
Claims (14)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US15440393A | 1993-11-19 | 1993-11-19 | |
US08/154,403 | 1993-11-19 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1137756A CN1137756A (zh) | 1996-12-11 |
CN1074923C true CN1074923C (zh) | 2001-11-21 |
Family
ID=22551225
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN94194190A Expired - Lifetime CN1074923C (zh) | 1993-11-19 | 1994-11-11 | 微囊密封的3-哌啶基取代的1,2-苯并异唑类和1,2-苯并异噻唑类 |
Country Status (30)
Country | Link |
---|---|
US (11) | US5688801A (zh) |
EP (1) | EP0729357B1 (zh) |
JP (1) | JP3645906B2 (zh) |
KR (1) | KR100354270B1 (zh) |
CN (1) | CN1074923C (zh) |
AT (1) | ATE288270T1 (zh) |
AU (1) | AU694147B2 (zh) |
BG (1) | BG63246B1 (zh) |
CL (1) | CL2004001182A1 (zh) |
CZ (1) | CZ293764B6 (zh) |
DE (1) | DE69434258T2 (zh) |
DK (1) | DK0729357T3 (zh) |
ES (1) | ES2236700T3 (zh) |
FI (1) | FI117122B (zh) |
HK (1) | HK1010694A1 (zh) |
HU (1) | HU219487B (zh) |
IL (1) | IL111647A (zh) |
MX (1) | MX9408969A (zh) |
MY (1) | MY113298A (zh) |
NO (1) | NO309226B1 (zh) |
NZ (1) | NZ276088A (zh) |
PL (1) | PL314481A1 (zh) |
PT (1) | PT729357E (zh) |
RO (1) | RO119224B1 (zh) |
RU (1) | RU2178695C2 (zh) |
SG (1) | SG47445A1 (zh) |
SI (1) | SI0729357T1 (zh) |
SK (1) | SK282231B6 (zh) |
WO (1) | WO1995013814A1 (zh) |
ZA (1) | ZA949191B (zh) |
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- 1994-11-11 JP JP51420695A patent/JP3645906B2/ja not_active Expired - Lifetime
- 1994-11-11 WO PCT/EP1994/003754 patent/WO1995013814A1/en active IP Right Grant
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Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4389330A (en) * | 1980-10-06 | 1983-06-21 | Stolle Research And Development Corporation | Microencapsulation process |
EP0368388A2 (en) * | 1988-11-07 | 1990-05-16 | Janssen Pharmaceutica N.V. | 3-Piperidinyl-1,2-benzisoxazoles |
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