Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1994-09-16
1997-11-18
Kight, John
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 59, 536 2, 536104, 536106, 536112, 536114, 5361231, 53612312, A61K 31715, C08B 3706, C08B 3702, C08B 3700
Patent
active
056887760
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
The invention relates to polysaccharides cross-linked with bifunctional crosslinkers, to a process for their preparation, to their use for coating and embedding drugs and to drugs coated and embedded using them.
The oral dosage form is a preferred administration of drugs. Drugs which do not act until the large intestine, eg. those employed for chronic inflammations of the large intestine or Crohn's disease, and drugs which are normally broken down or digested under physiological conditions in the stomach or in the small intestine or must be protected in order for them to reach the large intestine unchanged. Examples of medicinal substances which are broken down or digested in the small intestine include peptide medicinal substances.
There is therefore a need for a film coating and an embedding material by which, on oral administration, the administered active substance is protected on transport through the body as far as the large intestine and is then released there. Peptide medicinal substances could thus be protected, on oral use, from decomposition by gastric fluid as well as from decomposition by peptidases. Since the peptidase activity in the large intestine is only very low but the absorption of peptides takes place in the large intestine, this would be an acceptable way to administer peptide medicinal substances.
Owing to the natural physiological pH gradient between saliva and stomach on the one hand, and stomach and small intestine on the other hand, it is now possible without special difficulties to develop drug forms which release their active substances specifically in the stomach or in the small intestine. This is achieved by embedding or coating drugs with ancillary substances which are soluble or resistant at the appropriate pH values.
Since, however, there is only little difference between the pH values on passing from the small intestine into the large intestine, for targeting the large intestine it is necessary to look for other utilizable physiological differences which can be used to achieve small-intestine resistance and large-intestine degradability. The successful development of novel small-intestine resistant but large-intestine degradable ancillary substances has not to date succeeded in opening up possibilities to be implemented for targeting the large intestine.
DE 40 06 521 A1 (and European Patent Application 450 176 A1 which corresponds to it) describes sugar-containing polymers for coating and embedding medicinal substances. These sugar-containing polymers are used to coat and/or embed pharmaceutical active substances which can be administered orally and result in the active substances which are contained in the polymers not being released until the large intestine. The polymers described in this publication have the disadvantage that they need complicated preparations and are crosslinked with polyisocyanates.
Numerous review articles recently have referred to the possibilities of absorption in the large intestine (M. L. G. Gardner (1988): Gastrointestinal absorption of intact proteins, Ann. Rev. Nutr. 8, 329-350; P. Gruber, M. A. Longer and J. R. Robinson (1987): Some Biological issues in oral controlled drug delivery, Adv. Drug Deliv. Rev. 1, 1-18; T. T. Karrarly (1989): Gastrointestinal absorption of drugs, Crit. Rev. 6 (1), 39-86).
Studies on administrations of medicinal substances into the large intestine have also been published and refer to the suitability of this region not only as target organ for topically active medicinal substances but also absolutely as absorption site. Thus, P. R. Bieck (1987, Arzneistoffresorptionen aus dem menschlichen Dickdarm--neue Erkermtnisse, Acta Pharm. Technol. 33 (3), 109-114) describes how several medicinal substances introduced into the large intestine via tubes or by means of controlled release HF capsules, including the .beta.-receptor blockers oxprenolol and metoprolol as well as isosorbide 5-mononitrate, are absorbed virtually just as well as from the small intestine.
The present invention is based on the object of p
REFERENCES:
patent: 3615794 (1971-10-01), Nimerick
patent: 4143007 (1979-03-01), DeMartino
patent: 4960876 (1990-10-01), Molteni et al.
Chemical Abstracts, vol. 106, No. 1, abstract 106:5355m (1987).
Am. Quim, Ser. C, vol. 82, No. 1 (1986), Spain, pp. 37-45.
Polymer Preprints, vol. 30, No. 1, 1989, U.S.A., pp. 480-481.
Bauer Kurt Heinz
Betzing Juergen
BASF - Aktiengesellschaft
Kight John
White Everett
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