United States Patent:  6,004,996

Assignee:  Hoffman-La Roche Inc. (Nutley, NJ)

Filed:  January 6, 1998

Product containing tetrahydrolipstatin as the active ingredient and pharmaceutically acceptable excipients, characterized in that it is in the form of particles with a diameter of 0.25 to 2 mm; and pharmaceutical preparation s or compositions for oral administration containing the product.

SUMMARY OF THE INVENTION

In one of its aspects, the present invention relates to a product containing THL as active ingredient, stabilizers, pharmaceutically acceptable excipients, characterized in that it is in the form of particles with a diameter in the range of from about 0.25 mm to about 2 mm.

These particles are typically in the form of particles or pellets. The preferred pellet form requires the presence of microcrystalline cellulose. Preferably, the diameter of the pellets ranges from about 0.5 to about 1.5 mm.

Surprisingly, it was found that THL containing particles do not feature the sticking and picking phenomena and exhibit superior THL stability.

Claim 1 of 15 Claims

1. A pharmaceutical composition comprising a plurality of pellets having a diameter in the range of from about 0.25 mm to about 2 mm, and at most only a trace amount of pellets outside this range, each pellet comprising about 50% by weight tetrahydrolipstatin; polyvinylpyrrolidone; microcrystalline cellulose; and at least one pharmaceutically acceptable excipient.

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