Effect of poloxamer on the dissolution of felodipine and preparation of controlled release matrix tablets containing felodipine.

Author(s): Lee KR, Kim EJ, Seo SW, Choi HK

Affiliation(s): BK21 Project Team, College of Pharmacy, Chosun University, Gwangju 501-759, Korea.

Publication date & source: 2008-08, Arch Pharm Res., 31(8):1023-8. Epub 2008 Sep 12.

Publication type:

The effects of poloxamer and HPMC on the dissolution rate of felodipine were investigated and a felodipine controlled release tablet was developed by increasing the water solubility of felodipine and using swelling polymer to control release rate. Milling of felodipine slightly increased the dissolution rate of felodipine when compared with physical mixture. XRD results indicated that felodipine remained in the crystalline form even after co-milling with poloxamer. Improved dissolution rates after co-milling with HPMC and poloxamer were due to both solubilization effect of polymer and milling. The effect of poloxamer on dissolution rate was more significant than that of HPMC. Based on increased solubility of felodipine in the presence of poloxamer, it was concluded that the improved dissolution rate of felodipine was mainly due to a high local concentration of poloxamer around felodipine. Controlled release felodipine tablets were prepared using poloxamer as a solubilizing agent and Carbopol as a controlled release matrix.