Modified release preparations containing oxcarbazepine and derivatives thereof
Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
1. A controlled-release formulation comprising a homogeneous matrix comprising (a) oxcarbazepine, (b) a matrix-forming polymer selected from the group consisting of cellulosic polymers, alginates, gums, cross-linked polyacrylic acid, carageenan, polyvinyl pyrrolidone, polyethylene oxides, and polyvinyl alcohol, and (c) at least one agent that enhances the solubility of oxcarbazepine, and (d) at least one release promoting agent comprising an enteric polymer.
2. The formulation of claim 1 , wherein the formulation is effective in minimizing fluctuations between C min and C max of monohydroxy derivative of oxcarbazepine.
3. The formulation of claim 1 , wherein the amount of oxcarbazepine in the controlled release formulation is 600 mg.
4. The formulation of claim 1 , wherein the enteric polymer comprises a polymer having pH-dependent solubility.
5. The formulation of claim 1 , which can be administered once a day.
6. The formulation of claim 1 , wherein the at least one agent that enhances the solubility of oxcarbazepine is selected from the group consisting of surface active agents, complexing agents, cyclodextrins, pH modifying agents, and hydration promoting agents.