Controlled release formulations of levodopa and uses thereof

摘要

602302 Disclosed is a controlled release oral solid formulation of levodopa comprising: a. a 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, and c. an immediate release component comprising levodopa and a decarboxylase inhibitor, wherein the carboxylic acid component of (b) is a distinct component and is coated with an enteric polymer; and wherein the controlled release component (a), the immediate release component (c) and the carboxylic acid component (b) comprise beads or granules; with the proviso that the controlled release oral solid formulation is not: a multiparticulate, controlled release oral solid formulation of levodopa comprising: d. a controlled release component comprising a core of levodopa and carbidopa which is coated with one or more enteric polymers; e. a carboxylic acid component which is coated with an enteric polymer; and f. an immediate release component comprising a mixture of levodopa and carbidopa, wherein the controlled release component (d) , the carboxylic acid component (e) and the immediate release component (f) are distinct, separable beads or granules; and wherein the carboxylic acid component (e) comprises a carboxylic acid that is not in (d) and (f). Further disclosed is a multiparticulate, controlled release oral solid formulation of levodopa comprising: a. a controlled release component comprising levodopa, carbidopa and one or more rate controlling excipients; b. an immediate release component comprising levodopa and carbidopa, and c. a carboxylic acid component comprising a carboxylic acid that is not levodopa or carbidopa and one or more rate controlling excipients, wherein the carboxylic acid component of (c) is a distinct component and is coated with an enteric polymer and wherein the controlled release component (a), the immediate release component (b) and the carboxylic acid component (c) comprise beads or granules; with the proviso that the controlled release oral solid formulation is not: a multiparticulate, controlled release oral solid formulation of levodopa comprising: d. a controlled release component comprising a core of levodopa and carbidopa which is coated with one or more enteric polymers; e. a carboxylic acid component which is coated with an enteric polymer; and f. an immediate release component comprising a mixture of levodopa and carbidopa, wherein the controlled release component (d), the carboxylic acid component (e) and the immediate release component (f) are distinct, separable beads or granules; and wherein the carboxylic acid component (e) comprises a carboxylic acid that is not in (d) and (f). Further disclosed is a controlled release oral solid formulation of levodopa comprising: a. a controlled release component comprising levodopa and a decarboxylase inhibitor, wherein the component is coated with a rate controlling excipient, b. a carboxylic acid component coated with a rate controlling excipient, and c. an immediate release component comprising levodopa and a decarboxylase inhibitor, wherein the carboxylic acid component of (b) is a distinct component and wherein the carboxylic acid component (b) comprises a carboxylic acid that is not in (a) and (c) ; with the proviso that the controlled release oral solid formulation is not: a multiparticulate, controlled release oral solid formulation of levodopa comprising: d. a controlled release component comprising a core of levodopa and carbidopa which is coated with one or more enteric polymers; e. a carboxylic acid component which is coated with one or more enteric polymers; and f. an immediate release component comprising a mixture of levodopa and carbidopa, wherein the controlled release component (d), the carboxylic acid component (e) and the immediate release component (f) are distinct, separable beads or granules; and wherein the carboxylic acid component (e) comprises a carboxylic acid that is not in (d) and (f).