Class II drugs; a dissolution / bioavailability challenge: Flutamide-loaded spray dried lactose for dissolution control

Flutamide (FL) is the only presently recommended drug for monotherapy of benign prostatic hypertrophy. Five FL-loaded powdered formulations were prepared by spray drying. Aerosil was used with PEG 400 or PEG 6000 to improve powder flow and FL dissolution, respectively. Differential Scanning Calorimetry (DSC) studies revealed no interactions as evidenced by the persisting FL peak at 113oC. SEM pictures showed changes in powder morphology with F3 and F5 giving spongy-appearing particles with intra-particle channels. Wettability of the formulations was strongly increased as evidenced by the fast water rise through the powder bed (1.5- 44 min) compared with native FL (> 3 hr). The powders were tested for their angle of repose, Carr’s index and Hausner’s ratio. The results showed improved flow compared to both native FL and lactose. The best angle of repose (27.4o ) was seen with F3. This formulation also showed "fair" compressibility index and Hausner's ratio of 16.7 and 12.0, respectively. Compressed into tablets, all formulations showed significant improvement of FL release (p < 0.05)compared to commercial tablets. The highest drug release was seen with F3 showing 37% of FL released after 120 minutes compared with 11% FL released from commercial tablet after the same interval.

Author(s): Wael M. Samy

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