Dextran esters, the preparation thereof and the use thereof for

Details Dextran esters, the preparation thereof and the use thereof for Dextran esters, the preparation thereof and the use thereof for

1996-03-11

1998-04-14

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514964, 536112, A61K 3172, C08B 3702

Patent

active

057391220

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to water-insoluble dextran esters, to a process for preparing them, to their use for coating and/or embedding pharmaceutical active ingredients or drug formulations, and to drugs containing an active ingredient coated by or embedded in a dextran ester.
Ancillary substances are becoming increasingly important in the development and formulation of modern drugs. Thus, it is not just a medicinal substance alone which is responsible for a specific effect but, on the contrary, the interplay with one or more added ancillary substances. Ancillary substances have particular importance for the timing and the site-specificity of release of the medicinal substance, as well as for absorption. On administration as oral drug forms to date the timing or site-specificity of release of the medicinal substance has been confined to the stomach and various regions of the small intestine by the choice of suitable coating materials. However, to date there are no suitable coating materials making it possible for the drug form to be transported unchanged and completely active as far as the colon in order to release the medicinal substance specifically there. A drug form of this type would be desirable, for example, for the local therapy of inflammatory disorders of the colonic mucosa such as Crohn's disease. In addition, it might be possible to describe new ways of treatment with peptide medicinal substances which, on oral administration, are digested by physiological or enzymatic effects of the gastric and small intestinal fluids and thus become inactive. The development of an oral peptide drug form will result in the advantage compared with other possible routes of administration, such as nasal, transdermal or pulmonary administration, that no other aids (eg. plasters, atomizers) are necessary. This leads to reduced costs of therapy and to increased compliance because the patient regards oral administration of medicinal substances as more natural and, moreover, can carry it out himself.
For specific release of medicinal substances in the human colon, the coating material must comply with a number of requirements: cleaved by bacterial enzymes in the colon. attack. physiologically tolerated.
There is a marked difference in the density of bacterial colonization between the small intestine (10.sup.4 organisms/ml) and the colon (10.sup.14 organisms/ml). It is therefore possible to utilize the enzymatic activity of some bacteria in the colonic flora for cleaving a film coating which is stable in the small intestine.
J. Chem. Soc. 74 (1952) 5016 discloses stearyldextrans. However, no information about the molecular weight or the degree of substitution (degree of esterification) is to be found therein. Accordingly, there is also no disclosure of how these parameters must be set for the substances to be broken down by colonic bacteria.
DE 40 06 521 A1 (and the corresponding European Patent Application 450 176 A1) describes sugar-containing polymers for coating and embedding the medicinal substances. These sugar-containing polymers are used for coating and/or embedding pharmaceutical active ingredients which can be administered orally, and have the effect that the active ingredients contained in the polymers are released only when the colon is reached. The polymers described in this publication have the disadvantage that they require complicated preparation and are crosslinked with polyisocyanates.
DE 41 36 324 A1 discloses dextran derivatives which have a molecular weight of up to 20,000 and are intended as absorbents for bile acids.
DE 41 31 292 A1 discloses galactomannan derivatives for coating or embedding drugs, the galactomannans being etherified or esterified. The preparation process and the purification of the etherified or esterified galactomannan derivatives is, however, complicated and elaborate.
It is an object of the present invention to provide ancillary substances for drugs which comply with the abovementioned requirements for materials which can be broken down in the colon, are derived from ea

REFERENCES:
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Kurthals et al., Acta Pham. Nord., vol. 1(4): 201-210 Abstract Only.
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Schacht et al., Polym. Prepr. (ACS, Div. Polym. Chem.), vol. 31(2): 717-718, (1990) Abstract Only.
Larsen et al., Pharm Res., vol. 6(12): 995-999, (1989) Abstract Only.
Larsen et al., Int. J. Pharm., vol. 51(3): 233-240, (1989) Abstract Only.

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