United States Patent:   6,086,920

Assignee:  Fuisz Technologies Ltd. (Chantilly, VA)

Filed:  August 12, 1998

Microspheres which disintegrate quickly in water are composed of bio-affecting agent(s), disintegrant(s) and spheronization aid(s). The microspheres, which may have taste-masking coatings, are useful in making comestible units, such as pharmaceutical dosage forms.

SUMMARY OF THE INVENTION

The invention relates to novel particles, comestible units containing them, and processes for making each of these.

The particles are preferably microspheres which give 100% aqueous dissolution of bio-affecting agents therein, in 30 minutes or less. The particles are thermoformed from compositions containing bio-affecting agent(s), disintegrants, and spheronization aid(s). Lubricant(s) may also be included.

One would expect that, during thermoforming, the disintegrant would become coated, or encapsulated, with one or more of the other ingredients in the microspheres. Surprisingly, no such coating takes place. The microspheres made herein are water sensitive, so that, when hydrated, water readily interacts with their surfaces, resulting in rapid rupture into fragments, from which the bio-affecting agents therein are dissolved quickly.

In dissolution tests on disclosed embodiments, drug-containing masses made using compositions of the invention readily fragmented in water to yield smaller particles which enhanced dissolution of the bio-affecting agent(s) therein, i.e., complete solution in 30 minutes or less. The faster dissolution of the agent(s) in these microspheres should lead to more rapid absorption.

Claim 1 of 14 Claims

1. Disintegratable microspheres giving 100% aqueous dissolution in less than 30 minutes made from a composition comprising:

(a) about 50% to about 90% of at least one bio-affecting agent;

(b) about 2% to about 40% of at least one disintegrant; and

(c) about 5% to about 15% by weight of at least one spheronization aid.

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