2005 Volume 65 Issue 1 Pages 55-59
Cefcapene pivoxil hydrochloride (CFPN-PI), an oral prodrug for cefcapene with a broad antibacterial spectrum, has a strong bitter taste. Hot-melt powder coating (HMPC) technique with hydrogenated castor oil (HCO) was applied to CFPN-PI fine granules for pediatric use in order to mask the bitterness of the drug. Preheating was essential to effective coating of HCO powder, because the material with a low melting point, which is contained in the core particles, acts as a binder in the HMPC process. EPMA showed the amount of CFPN-PI on the surface of the fine granules decreased by HMPC. The coated CFPN-PI fine granules had lower initial dissolution and, consequently, reduced bitterness, but a similar dissolution profile in JP 1st fluid, compared with the non-coated granules. As a result, the taste of the hot-melt powder coated CFPN-PI fine granules was significantly improved, and desirable for the pediatric formulations. The developed initial dissolution test, which was the method to predict the bitterness of the formulations easily, was useful for in-process controls.
