Eurand America, Inc.

Sambasiva Rao Ghanta

Robert Edmon Guisinger

Marie Jean Bettman

This disclosure is directed to preparation of individual taste-masked, high bioavailability, high payload, microcapsules by microencapsulation of water-insoluble NSAID drug materials in the substantial absence of microcapsule agglomerates. These taste-masked microcapsules contain a high payload, e.g., about 83+ wt. % of said NSAID drug material having high bioavailability and can then be formulated into chewable tablets and liquid aqueous suspensions for medicinal use. Both cellulose acetate phthalate and gelatin are the microencapsulating polymer wall material. Control of pH, controlled addition of a Hofmeister (lyotropic) salt, microencapsulation of the water-insoluble NSAID medicament with a liquid phase of both cellulose acetate phthalate and gelatin microencapsulating material and the subsequent insolubilization of said liquid encapsulating material after it is wrapped around the medicament core with dilute acid are important process parameters to achieving the proper individual microcapsules to obtain highly bioavailability taste-masked, water-insoluble NSAID drug materials, esp., naproxen and ibuprofen, by microencapsulation alone.

Procedure for encapsulating ibuprofen

This disclosure is directed to preparation of individual taste-masked, high bioavailability, high payload, microcapsules by microencapsulation of water-insoluble NSAID drug materials in the substantial absence of microcapsule agglomerates. These taste-masked microcapsules contain a high payload, e.g., about 83+wt. % of said NSAID drug material having high bioavailability and can then be formulated into chewable tablets and liquid aqueous suspensions for medicinal use. Both cellulose acetate phthalate and gelatin are the microencapsulating polymer wall material. Control of pH, controlled addition of a Hofmeister (lyotropic) salt, microencapsulation of the water-insoluble NSAID medicament with a liquid phase of both cellulose acetate phthalate and gelatin microencapsulating material and the subsequent insolubilization of said liquid encapsulating material after it is wrapped around the medicament core with dilute acid are important process parameters to achieving the proper individual microcapsules to obtain highly bioavailability taste-masked, water-insoluble NSAID drug materials, esp., naproxen and ibuprofen, by microencapsulation alone.

An improvement in the process of coacervation of chlorpheniramine maleate is provided whereby a predetermined amount of chlorpheniramine maleate charged to the process is maintained in the microcapsules by pre-saturating the coacervation medium with chlorpheniramine maleate.

Growing community of inventors

Centerville, OH, United States of America

Sambasiva Rao Ghanta