SUMMARY:

Pregabalin is currently marketed in the US and EU as Lyrica in the form of capsules ranging from 25 to 300 mg for the management of neuropathic pain, fibromyalgia, postherpetic neuralgia and adjunctive therapy for adult patients with partial onset seizures.

A pregabalin 20 mg/mL oral solution formulation has been developed. The formulation is a clear, colorless solution. A sweetening agent (sucralose) and flavor (artificial strawberry) aid in masking the bitter taste of pregabalin.  The solution is buffered to approximately pH 6.1 with 30 mM phosphate buffer. The solution includes an antimicrobial preservative system consisting of methylparaben and propylparaben. 

The pregabalin oral solution composition is shown in Table 1. All excipient amounts are based on a batch size of 3600 liters. The formulation contains 20 mg/mL pregabalin. The formulation’s targeted pH is 6.1 (target range 5.8 to 6.3). The solution will be packaged in a 16 fl. ounce white HDPE Modern Round bottle with a child-resistant screw cap. All excipients meet global compendial requirements.

Table 1. Composition of Pregabalin 20 mg/mL Oral Solution

^a All components meet global compendia.

^b NOTE: x denotes an insignificant number.

^c N/A = Not Applicable

MANUFACTURING PROCESS

Overview

Pregabalin active pharmaceutical ingredient is synthesized according to United States Patent Application 2009-0042262A1 The proposed process for manufacture of the pregabalin oral solution is shown in the  flow chart in F...