Controlled release formulations of levodopa and uses thereof

摘要

The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor.

主权项

1. A controlled release oral solid formulation of levodopa comprising:
a. a first controlled release component comprising levodopa, a decarboxylase inhibitor and one or more rate controlling excipients, b. a carboxylic acid component comprising a carboxylic acid that is not levodopa or the decarboxylase inhibitor and one or more rate controlling excipients, c. an immediate release component comprising levodopa and a decarboxylase inhibitor, and d. a second controlled release component comprising levodopa, a decarboxylase inhibitor and one or more rate controlling excipients, the second controlled release component (d) being in a separate bead or granule from (a) and having less levodopa and decarboxylase inhibitor than (a),wherein the carboxylic acid component of (b) is in a distinct component and is coated with an enteric polymer; and wherein the first controlled release component (a), the second release component (d), the immediate release component (c) and the carboxylic acid component (b) comprise beads or granules and wherein the first and second controlled release components release decarboxylase inhibitor and levodopa at different rates.