FI111909B - Förfarande för framställning av kompositioner för inhalering - Google Patents
Förfarande för framställning av kompositioner för inhalering Download PDFInfo
- Publication number
- FI111909B FI111909B FI956228A FI956228A FI111909B FI 111909 B FI111909 B FI 111909B FI 956228 A FI956228 A FI 956228A FI 956228 A FI956228 A FI 956228A FI 111909 B FI111909 B FI 111909B
- Authority
- FI
- Finland
- Prior art keywords
- polypeptide
- hormone
- powder
- process according
- enhancer
- Prior art date
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- WDFRNBJHDMUMBL-FUXQPCDDSA-M sodium;(4r)-4-[(3r,5s,7s,8r,9s,10s,13r,14s,17r)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]pentanoate Chemical compound [Na+].C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)CC1 WDFRNBJHDMUMBL-FUXQPCDDSA-M 0.000 description 1
- IWQPOPSAISBUAH-VOVMJQHHSA-M sodium;2-[[(2z)-2-[(3r,4s,5s,8s,9s,10s,11r,13r,14s,16s)-16-acetyl-3,11-dihydroxy-4,8,10,14-tetramethyl-2,3,4,5,6,7,9,11,12,13,15,16-dodecahydro-1h-cyclopenta[a]phenanthren-17-ylidene]-6-methylheptanoyl]amino]ethanesulfonate Chemical compound [Na+].C1C[C@@H](O)[C@@H](C)[C@@H]2CC[C@]3(C)[C@@]4(C)C[C@H](C(C)=O)/C(=C(C(=O)NCCS([O-])(=O)=O)/CCCC(C)C)[C@@H]4C[C@@H](O)[C@H]3[C@]21C IWQPOPSAISBUAH-VOVMJQHHSA-M 0.000 description 1
- XBYKLNAHPCSCOD-UHFFFAOYSA-M sodium;2-hydroxy-5-methoxybenzoate Chemical compound [Na+].COC1=CC=C(O)C(C([O-])=O)=C1 XBYKLNAHPCSCOD-UHFFFAOYSA-M 0.000 description 1
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- WBWWGRHZICKQGZ-HZAMXZRMSA-N taurocholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS(O)(=O)=O)C)[C@@]2(C)[C@@H](O)C1 WBWWGRHZICKQGZ-HZAMXZRMSA-N 0.000 description 1
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- 210000005166 vasculature Anatomy 0.000 description 1
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Classifications
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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
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/27—Growth hormone [GH], i.e. somatotropin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K9/145—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 compounds
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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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Zoology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Compositions Of Macromolecular Compounds (AREA)
- Biological Depolymerization Polymers (AREA)
Claims (15)
1. Förfarande för framställning av en farmaceutisk komposi-’·* * tion i form av ett torrt pulver lämplig för intagning genom inhalering frän en torrpulversinhalator tili den nedre and- • · I • *,·’ ningsvägen, kännetecknat av att 25 a) man ästadkommer en lösning, i vilken (a) en farmaceutiskt : aktiv polypeptid och (b) en förstärkarförening, som ökar ·,,,· absorptionen av polypeptiden i organismen i den nedre and- ningsvägen hos en patient, är lösta; avlägsnar lösningsmedlet ,·, ; frän nämnda lösning för att erhälla ett torrt fast ämne inne- 30 hällande nämnda polypeptid och nämnda förstärkarförening; och 111909' 27 pulveriserar nämnda torra fasta ämne för att ästadkomma ett pulver; eller b) torrblandar (a) en farmaceutiskt aktiv polypeptid och (b) en förstärkarförening som ökar absorptionen av polypeptiden i 5 den nedre andningsvägen hos en patient; och mikroniserar den erhallna blandningen; eller c) ästadkommer en första mikroniserad beredning innehällande farmaceutiskt aktiv polypeptid och en andra mikroniserad beredning innehällande en förstärkarförening som ökar absorp- 10 tionen av polypeptiden i lungan hos en patient; och blandar nämnda första och andra mikroniserade beredningar; varvid nämnda farmaceutiskt aktiva polypeptid och förstärkar-föreningen är aktiva föreningar; nämnda förstärkarförening är ett gallsalt, ett gallsaltsderivat, en alkylglykosid, ett 15 fettsyresalt, ett cyklodextrin eller derivat därav, eller en fosfolipid med en kedja; och varvid minst 50 % av de aktiva föreningarnas totala massa bestär av primära partiklar med en diameter som är mindre än eller lika med ca 10 mikroner, vilka primära partiklar eventuellt agglomererats. 20
2. Förfarande enligt patentkrav 1, kännetecknat av att det ; under förfarandet tillförs ett farmaceutiskt acceptabelt tillsatsämne sä, att den resulterande kompositionen innehäl-' ler antingen: .7. (a) partiklar som har en diameter av mindre än ca 10 mikron, 25 sä att minst 50 % av det resulterande pulvret bestär av even- y-' tuellt agglomererade primära partiklar som har en diameter av mindre än ca 10 mikron; : (b) grova partiklar, sä att en ordnad blandning bildas mellan ,···, de aktiva föreningarna och nämnda tillsatsämne. 30
3. Förfarande enligt patentkrav 1 eller 2, kännetecknad av : att nämnda polypeptid är ett polypeptidhormon. 111909 28
4. Förfarande enligt patentkrav 3, kannetecknad av att nämnda hormon är vasopressin, en vasopressinanalog, desmopressin, glukagon, kortikotropin (ACTH), gonadotropin (lu-teiniserande hormon eller LHRH), kalcitonin, C-peptid av 5 insulin, paratyroidhormon (PTH), humant tillväxthormon (hGH), tillväxthormon (HG), tillväxthormonfrisättande hormon (GHRH), oxitocin, kortikotropinfrisättande hormon (CRH), somatosta-tinanaloger, gonadotropinagonistanalog (GnRHa), förmaksnat-riumuretisk peptid (hANP), tyroxinfrisättande hormon (TRHrh), 10 follikelstimulerande hormon (FSH) eller prolaktin.
5. Förfarande enligt patentkrav 1, kannetecknad av att nämnda polypeptid är en tillväxtfaktor, interleukin, poly-peptidvaccin, enzym, endorfin, glykoprotein, lipoprotein eller polypeptid inbegripen i blodkoagulationskaskaden. 15
6. Förfarande enligt patentkrav 1, kannetecknad av att nämnda polypeptid har en molekylvikt av mindre än 30 kD.
7. Förfarande enligt patentkrav 1, kannetecknad av att nämnda polypeptid har en molekylvikt av mindre än 20 kD.
. . 8. Förfarande enligt patentkrav 1, kännetecknad av att ; *, 20 nämnda polypeptid har en molekylvikt av mindre än 10 kD.
9. Förfarande enligt patentkrav 1, kannetecknat av att nämnda förstärkarförening är ett fettsyresalt.
10. Förfarande enligt patentkrav 1, kannetecknat av att '·’ * nämnda fettsyra har 10-14 kolatomer. •'*'. 25
11. Förfarande enligt patentkrav 1, kännetecknat av att ,···, nämnda fettsyra är kaprinsyra.
; : : 12. Förfarande enligt patentkrav 1, kännetecknat av att nämnda fettsyresalt är natriumkaprat. i t
:,*·* 13. Förfarande enligt patentkrav 2, kännetecknat av att 30 nämnda tillsatsämne är valt bland mono-, di- och polysacka-rider, sockeralkoholer och andra polyoler. 29 11190ί
14. Förfarande enligt patentkrav 2, kannetecknat av att nämnda tillsatsämne är ett icke-reducerande socker.
15. Förfarande enligt patentkrav 2, kännetecknat av att nämnda tillsatsämne är raffinos, melezitos, laktitol, 5 maltitol, trehalos, sackaros, mannitol eller stärkelse. » » i
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE9302198 | 1993-06-24 | ||
SE9302198A SE9302198D0 (sv) | 1993-06-24 | 1993-06-24 | Powder preparation for inhalation |
SE9400371A SE9400371L (sv) | 1994-02-04 | 1994-02-04 | Kompositioner för inhalation |
SE9400371 | 1994-02-04 | ||
PCT/SE1994/000634 WO1995000128A1 (en) | 1993-06-24 | 1994-06-23 | Compositions for inhalation |
SE9400634 | 1994-06-23 |
Publications (3)
Publication Number | Publication Date |
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FI956228A0 FI956228A0 (sv) | 1995-12-22 |
FI956228A FI956228A (sv) | 1995-12-22 |
FI111909B true FI111909B (sv) | 2003-10-15 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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FI956228A FI111909B (sv) | 1993-06-24 | 1995-12-22 | Förfarande för framställning av kompositioner för inhalering |
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US (1) | US5952008A (sv) |
EP (1) | EP0706383B1 (sv) |
JP (2) | JPH09500621A (sv) |
KR (1) | KR100372674B1 (sv) |
CN (1) | CN1116030C (sv) |
AT (1) | ATE206046T1 (sv) |
AU (1) | AU692781B2 (sv) |
BR (1) | BR9406908A (sv) |
CA (1) | CA2166109C (sv) |
CZ (1) | CZ287656B6 (sv) |
DE (1) | DE69428442T2 (sv) |
DK (1) | DK0706383T3 (sv) |
EE (1) | EE03222B1 (sv) |
EG (1) | EG21484A (sv) |
ES (1) | ES2162865T3 (sv) |
FI (1) | FI111909B (sv) |
HK (1) | HK1009587A1 (sv) |
HU (1) | HU226474B1 (sv) |
IL (1) | IL110085A (sv) |
IS (1) | IS1796B (sv) |
MX (1) | MX9404762A (sv) |
MY (1) | MY114125A (sv) |
NO (1) | NO313080B1 (sv) |
NZ (1) | NZ268138A (sv) |
PL (1) | PL178261B1 (sv) |
PT (1) | PT706383E (sv) |
SA (1) | SA94150060B1 (sv) |
SK (1) | SK283253B6 (sv) |
UA (1) | UA48111C2 (sv) |
WO (1) | WO1995000128A1 (sv) |
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1994
- 1994-06-21 IS IS4179A patent/IS1796B/is unknown
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- 1994-06-22 IL IL11008594A patent/IL110085A/en not_active IP Right Cessation
- 1994-06-22 MY MYPI94001613A patent/MY114125A/en unknown
- 1994-06-23 EP EP94919961A patent/EP0706383B1/en not_active Expired - Lifetime
- 1994-06-23 DE DE69428442T patent/DE69428442T2/de not_active Expired - Lifetime
- 1994-06-23 CN CN94192867A patent/CN1116030C/zh not_active Expired - Fee Related
- 1994-06-23 CZ CZ19953393A patent/CZ287656B6/cs not_active IP Right Cessation
- 1994-06-23 PL PL94312210A patent/PL178261B1/pl not_active IP Right Cessation
- 1994-06-23 KR KR1019950705905A patent/KR100372674B1/ko not_active IP Right Cessation
- 1994-06-23 SK SK1602-95A patent/SK283253B6/sk not_active IP Right Cessation
- 1994-06-23 CA CA002166109A patent/CA2166109C/en not_active Expired - Fee Related
- 1994-06-23 AT AT94919961T patent/ATE206046T1/de active
- 1994-06-23 MX MX9404762A patent/MX9404762A/es not_active IP Right Cessation
- 1994-06-23 DK DK94919961T patent/DK0706383T3/da active
- 1994-06-23 HU HU9503660A patent/HU226474B1/hu not_active IP Right Cessation
- 1994-06-23 AU AU70902/94A patent/AU692781B2/en not_active Ceased
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- 1994-06-23 WO PCT/SE1994/000634 patent/WO1995000128A1/en active IP Right Grant
- 1994-06-23 JP JP7502737A patent/JPH09500621A/ja not_active Withdrawn
- 1994-06-23 UA UA95125418A patent/UA48111C2/uk unknown
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- 1994-06-23 BR BR9406908A patent/BR9406908A/pt not_active Application Discontinuation
- 1994-06-23 PT PT94919961T patent/PT706383E/pt unknown
- 1994-07-05 SA SA94150060A patent/SA94150060B1/ar unknown
- 1994-11-23 EE EE9400457A patent/EE03222B1/xx not_active IP Right Cessation
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1995
- 1995-12-21 NO NO19955227A patent/NO313080B1/no not_active IP Right Cessation
- 1995-12-22 FI FI956228A patent/FI111909B/sv not_active IP Right Cessation
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1997
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1998
- 1998-09-01 HK HK98110333A patent/HK1009587A1/xx not_active IP Right Cessation
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2005
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