In vitro and in vivo evaluation of ofloxacin sustained release pellets.
Being a sustained release dosage form, pellets allow ofloxacin to exhibit improved release and absorption profiles. In this paper, the centrifugal granulation method was employed to prepare ofloxacin pellets. Then the pellets were subjected to a coating process with methacrylic acid copolymers to produce sustained release characteristics. The pellets with different coatings were investigated by release tests in vitro. Finally, pellets with the best coating suspension were subjected to a multiple doses pharmacokinetic study in beagle dogs. The in vitro release profiles showed that pellets coated with Eudragit NE30D and Eudragit L30D55, at a ratio of 1:8 (w/w) and a coating level of 8% with diethyl phthalate (DEP) as plasticizer equivalent to 10% of solid material in the coating suspension were suitable for sustained release. In the bioavailability study, the principal pharmacokinetic parameters showed there were differences between the sustained release pellets and the conventional ofloxacin capsules. The relative bioavailability of ofloxacin sustained release pellets compared with conventional ofloxacin capsules was 116.35+/-33.31%. All the statistics indicate that the preparation has a sustained release effect with many advantages over conventional preparations.
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Yue
Y
Cui
Yu
Y
Zhang
Xing
X
Tang
D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D003627:Data Interpretation, Statistical; D003692:Delayed-Action Preparations; D004285:Dogs; D005079:Excipients; D006207:Half-Life; D006863:Hydrogen-Ion Concentration; D008689:Methacrylates; D015242:Ofloxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D009997:Osmotic Pressure; D011109:Polymethacrylic Acids; D011208:Powders; D012995:Solubility; D013608:Tablets, Enteric-Coated
D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D008689:Methacrylates; D011109:Polymethacrylic Acids; D011208:Powders; D013608:Tablets, Enteric-Coated; C008384:methacrylic acid; C038300:methylmethacrylate-methacrylic acid copolymer; D015242:Ofloxacin