Encapsulation of ketoprofen and ketoprofen lysinate by prilling for controlled drug release.
In this paper, ketoprofen and ketoprofen lysinate were used as model drugs in order to investigate release profiles of poorly soluble and very soluble drug from sodium alginate beads manufactured by prilling. The effect of polymer concentration, viscosity, and drug/polymer ratio on bead micromeritics and drug release rate was studied. Ketoprofen and ketoprofen lysinate loaded alginate beads were obtained in a very narrow dimensional range when the Cross model was used to set prilling operative conditions. Size distribution of alginate beads in the hydrated state was strongly dependent on viscosity of drug/polymer solutions and frequency of the vibration. The release kinetics of the drugs showed that drug release rate was related with alginate concentration and solubility of the drug. Alginate solutions with concentration higher than 0.50% (w/w) were suitable to prepare ketoprofen gastro-resistant formulation, while for ketoprofen lysinate alginate, concentration should be increased to 1.50% (w/w) in order to retain the drug in gastric environment. Differential scanning calorimetry thermograms and Fourier transform infrared analyses of drug-loaded alginate beads indicated complex chemical interactions between carboxyl groups of the drug and polymer matrix in drug-loaded beads that contribute to the differences in release profile between ketoprofen and ketoprofen lysinate. Total release of the drugs in intestinal medium was dependent on the solubility of the drug and was achieved between 4 and 6 h.
Department of Pharmaceutical Sciences, University of Salerno, 84084, Fisciano, SA, Italy. pdelgaudio@unisa.it
Pasquale
P
Del Gaudio
Paola
P
Russo
Maria
M
Rosaria Lauro
Paolo
P
Colombo
Rita P
RP
Aquino
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D007660:Ketoprofen / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000737:chemistry; D008239:Lysine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; C029946:ketoprofen lysine; D007660:Ketoprofen; D008239:Lysine