Bioadhesive microspheres and their use as drug delivery and...

A - Human Necessities – 61 – K

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A61K 9/14 (2006.01) A61K 9/16 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) B01J 13/02 (2006.01) G01N 19/04 (2006.01) G01N 33/53 (2006.01)

Patent

CA 2134082

Bioadhesive polymers in the form of, or as a coating on, microcapsules containing drugs or bioactive substances which may serve for therapeutic, or diagnostic purposes in diseases of the gastrointestinal tract, are described. The polymeric microspheres all have a bioadhesive force of at least 11 mN/cm2 (110 N/m2). Techniques for the fabrication of bioadhesive microspheres, as well as a method for measuring bioadhesive forces between microspheres and selected segments of the gastrointestinal tract in vitro are also described. This quantitative method provides a means to establish a correlation between the chemical nature, the surface morphology and the dimensions of drug-loaded microspheres on one hand and bioadhesive forces on the other, allowing the screening of the most promising materials from a relatively large group of natural and synthetic polymers which, from theoretical consideration, should be used for making bioadhesive microspheres.

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