A Pharmaceutical Study on Felodipine “Enhanced Dissolution Characteristics of Felodipine” Ahmed Abd-El Bary, Mohamed M. Nafady,Mahmoud E. Nasr Department.

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A Pharmaceutical Study on Felodipine “Enhanced Dissolution Characteristics of Felodipine” Ahmed Abd-El Bary, Mohamed M. Nafady,Mahmoud E. Nasr Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo, Egypt.

Aim of work Enhancement of aqueous solubility of felodipine with subsequent expected increase in drug bioavailability.The dissolution characteristics of felodipine were enhanced via preparation of its solid dispersions PVP K25, PVP K90, PEG 4000, PEG 6000, Mannitol, Soribitol, aerosil and Avicel in different ratios using various techniques(solvent evaporation method, fusion method,solvent deposition method and surface solid dispersion method).

Also felodipine subligual table ts were prepared by direct compression of powder of mixture I(felodipine with PVPK90, NaLS and aerosil) and mixture II(felodipine with PVPK90, NaLS and avicel) to give a rapid onset of action and to bypass the hepatic metabolism of the dug, which is the reason of its limited bioavailability.

Conclusion 1-Solid dispersions prepared with different techniques resulted in marked increase in the amount of drug dissolved, solid dispersions of felodipine prepared with PVPK90 and utilizing the solvent evaporation technique revealed the highest drug dissolution rate. The prepared felodipine sublingual tablet formulation complied with the pharmacopoeial standards. The percent of felodipine dissolved after 45 minutes from the prepared sublingual tablets according to mixture I was 87.87%.

2-The invitro permeation study of the selected felodipine sublingual tablet through pocine buccal mucosa showed that 4.5 mg felodipine was permeated after 30 minutes which indicates rapid permeation of the drug. Therefore, it would be possible to formulate felodipine sublingual tablets having fast onset of action.

Temperature Fig(1):DSC Thermogram of Felodipine Alone and its Solid Dispersion with PVPK90.

2Ө angle(deg) Fig(3):XRD of Felodipine Alone and its solid dispersion with PVPK90.