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1. WO2012130193 - NON-COVALENT SOLUBLE COMPLEXES OF TERIPARATIDE WITH POLYSACCHARIDES AND A DOSAGE FORM OF TERIPARATIDE FOR ORAL ADMINISTRATION

Publication Number WO/2012/130193
Publication Date 04.10.2012
International Application No. PCT/CZ2012/000025
International Filing Date 16.03.2012
IPC
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
08
Solutions
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
36
Polysaccharides; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17
from animals; from humans
22
Hormones
29
Parathyroid hormone (parathormone); Parathyroid hormone-related peptides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
48
the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
16
Agglomerates; Granulates; Microbeadlets
A61K 9/08 (2006.01)
A61K 47/36 (2006.01)
A61K 9/00 (2006.01)
A61K 38/29 (2006.01)
A61K 47/48 (2006.01)
A61K 9/14 (2006.01)
CPC
A61K 47/36
A61K 47/61
A61K 9/0019
A61K 9/08
A61K 9/146
A61K 9/1652
Applicants
  • ZENTIVA, K.S. [CZ/CZ]; U Kabelovny 130 102 37 Praha 10, CZ (AllExceptUS)
  • ANTOSOVA, Zuzana [CZ/CZ]; CZ (UsOnly)
  • JUNKOVA Petra [CZ/CZ]; CZ (UsOnly)
  • PETKOVA, Galina [BG/BG]; BG (UsOnly)
  • RICHTEROVA Klara [CZ/CZ]; CZ (UsOnly)
  • REZANKA, Pavel [CZ/CZ]; CZ (UsOnly)
  • MACKOVA, Martina [CZ/CZ]; CZ (UsOnly)
  • FLIEGER, Miroslav [CZ/CZ]; CZ (UsOnly)
  • KRAL, Vladimir [CZ/CZ]; CZ (UsOnly)
Inventors
  • ANTOSOVA, Zuzana; CZ
  • JUNKOVA Petra; CZ
  • PETKOVA, Galina; BG
  • RICHTEROVA Klara; CZ
  • REZANKA, Pavel; CZ
  • MACKOVA, Martina; CZ
  • FLIEGER, Miroslav; CZ
  • KRAL, Vladimir; CZ
Agents
  • JIROTKOVA, Ivana; Rott, Ruzicka & Guttmann P.O. Box 44 120 00 Praha 2, CZ
Priority Data
PV 2011-18031.03.2011CZ
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) NON-COVALENT SOLUBLE COMPLEXES OF TERIPARATIDE WITH POLYSACCHARIDES AND A DOSAGE FORM OF TERIPARATIDE FOR ORAL ADMINISTRATION
(FR) COMPLEXES SOLUBLES NON COVALENTS DE TÉRIPARATIDE CONTENANT DES POLYSACCHARIDES ET FORME PHARMACEUTIQUE DE TÉRIPARATIDE POUR ADMINISTRATION ORALE
Abstract
(EN)
The present invention relates to stabilization of teriparatide for oral administration by forming of water-soluble complexes with soluble polysaccharides, e.g. β-glucan, chitosan, alginic acid, or their salts. Orally administered peptide medicaments such as teriparatide exhibit very low biological availability, which is mainly caused by rapid degradation in the digestive tract by proteolytic enzymes, as well as low efficiency of transport through the intestinal wall to the blood circulation. It is an advantage of the pharmaceutical composition according to the invention that teriparatide in the complex form is protected from being digested by proteases, the complex not preventing absorption of teriparatide from the gastrointestinal tract to the blood at the same time.
(FR)
L'invention concerne la stabilisation de tériparatide pour l'administration orale par formation de complexes hydrosolubles contenant des polysaccharides solubles, par ex. ß-glucane, chitosane, acide alginique ou leurs sels. Des médicaments peptidiques à administration orale tels que le tériparatide ont une disponibilité biologique très faible notamment en raison d'une dégradation rapide dans le tube digestif par des enzymes protéolytiques, ainsi que d'une efficacité de transport faible à travers la paroi intestinale, vers le sang. De manière avantageuse, le tériparatide sous forme de complexe est protégé contre la digestion par les protéases, le complexe n'empêchant pas l'absorption du tériparatide du tractus gastro-intestinal vers le sang.
Also published as
PL413855
PLP.413855
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