Ulcer prevention method using a melt-spun hydrogel

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Matrices

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Details

424485, 424487, 424499, 424500, 424501, 514925, A61K 910, A61K 914

Patent

active

056227175

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to ulcer treatments. In particular, the present invention relates to the use of dosage forms containing anti-ulcer agents dispersed in a soluble matrix.
Sucralfate is a therapeutic compound useful for treatment of various gastrointestinal disorders. Sucralfate accelerates the healing of gastric and duodenal ulcers and also finds use as a symptomatic treatment for disturbances such as dyspepsia and reflux.
Sucralfate displays its action in the acid medium of the digestive tract where it lines ulcerated mucous membranes of the stomach and duodenum with a protective coating. The preferential binding affinity of sucralfate for ulcerated areas of mucous membrane results in increased protection and accelerated healing of ulcers as well as regeneration of the mucous membrane.
Although sucralfate is usually taken orally in the form of tablets, other dosage forms are known. For example, U.S. Pat. No. 4,885,281 discloses an aqueous suspension containing sucralfate, xanthum gum and a "peptiser". Peptisers such as salts of inorganic or organic acids are added to ensure that the xanthan gum does not separate out of the suspension by gel formation.
Belgium Patent No. 900,605 discloses a composition of sucralfate and a nonsteroidal anti-inflammatory product. The compositions were prepared for administering to mammalian test specimens by suspending the active substances in an aqueous medium containing 0.5% sodium CMC (carboxymethylcellulose).
The preparation of melt-spun medicament-containing products is known. For example, commonly-assigned U.S. Pat. No. 4,855,326, which is incorporated by reference herein, discloses combining a medicament with a melt-spinnable carrier agent, preferably a mixture of sucrose and lactose, and then melt-spinning the mixture to form a spun product.
Similarly, commonly-assigned U.S. Pat. No. 4,997,856, also incorporated by reference herein, discloses melt spun, compacted dispersible systems containing a medicament, saccharide and an oleaginous substance such as a food oil.
In keeping with the foregoing, improvements are continuously being sought using high shear and/or heat processing to enhance the delivery of medicaments. In the case of anti-ulcer medicaments such as sucralfate, an investigation is being conducted to improve the protective and therapeutic action of the medicament on ulcerated areas of mucous membranes.
It is an object of the present invention to provide an improved method of treatment using medicaments spun in a matrix carrier.
It is a further object of the present invention to provide improved methods and compositions for preventing and treating ulcerated mucosa.
Other and further objects will become apparent to the artisan in view of the present disclosure, and the scope of the present application is not to be limited by the objects set forth above.


SUMMARY OF THE INVENTION

The present invention includes anti-ulcer compositions formed by having a medicament dispersed in a soluble matrix. The soluble matrix is formed by subjecting the feedstock to physical and/or chemical changes associated with flash flow processing, such as by melt-spinning the medicament with a mixture of a carrier material and a hydrogel. The anti-ulcer compositions can either be placed directly on the ulcer-bearing tissue/mucosa or may be dispersed in a liquid before contacting the affected tissue.
The medicament included in the composition of the present invention is preferably sucralfate. Alternatively, H.sub.2 -blocking agents such as cimetidine and the like or omeprazole may also be included.
The carrier materials included in the mixture are a saccharide-based and preferably materials such as maltodextrin, maltooligosaccharides or polydextrdse. The hydrogel is selected from materials such as xanthan gum, guar gum and carrageenan. In a preferred embodiment, the melt spinning mixture also includes an oleaginous substance such as a vegetable oil. A method of preparing such anti-ulcer compositions is also disclosed.
The composition of the present invention can also inc

REFERENCES:
patent: 3686000 (1972-08-01), Lawrence
patent: 3762846 (1973-10-01), Chivers
patent: 4855326 (1989-08-01), Fuisz
patent: 4885281 (1989-12-01), Hanstein et al.

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