Comparison of the Pharmacokinetics of An Oral Extended-Release Capsule Formulation of Carbidopa-Levodopa (IPX066), with Immediate-Release Carbidopa-Levodopa (Sinemet®), Sustained-Release Carbidopa-Levodopa (Sinemet® CR), and Carbidopa-Levodopa-Entacapone (Stalevo®).

Data from healthy subjects on extended release carbidopa-levodopa (IPX066) - aims to provide better control of motor symptoms and less fluctuations

J Clin Pharmacol. 2015 Apr 8. doi: 10.1002/jcph.514. [Epub ahead of print]

Hsu A, Yao HM, Gupta S, Modi NB.

IPX066 (ER CD-LD) is an oral extended-release capsule formulation of carbidopa (CD) and levodopa (LD). The single-dose pharmacokinetics of ER CD-LD (as 2 capsules, total dose 97.5 mg-390 mg CD-LD) versus immediate-release (IR) CD-LD (25 mg-100 mg), sustained release (CR) CD-LD (25 mg-100 mg), and CD-LD-entacapone (25 mg-100 mg-200 mg) was evaluated in healthy subjects. Following IR dosing, LD reached peak concentrations (Cmax ) at 1 hour; LD concentrations then decreased rapidly and were less than 10% of peak by 5 hours. With CR CD-LD and CD-LD-entacapone, LD Cmax occurred at 1.5 hours and concentrations were less than 10% of peak by 6.3 and 7.5 hours, respectively. The initial increase in LD concentration was similar between ER CD-LD and IR CD-LD, and faster than for CR CD-LD and CD-LD-entacapone. LD concentrations from ER CD-LD were sustained for approximately 5 hours and did not decrease to 10% of peak until 10.1 hours. Dose-normalized LD Cmax values for ER CD-LD were significantly lower (P <0.05) than for the other CD-LD products. Bioavailability of LD from ER CD-LD was 83.5%, 78.3%, and 58.8% relative to IR CD-LD, CR CD-LD, and CD-LD-entacapone, respectively.