A new approach for preparing a controlled release ketoprofen tablets by using beeswax.
Solid lipid ketoprofen micropellets (SLKM) at different drug/beeswax ratios [(1:1) and (1:2)] were prepared by emulsion congealing technique and then compressed into tablets. Ketoprofen in solid state was incorporated into the melted beeswax at 90 degrees C and the mixture was emulsified in the hot aqueous Tween 80 solution by stirring at a constant rate. The SLKM were obtained by cooling the coarse emulsion down to room temperature and filtering. Drug entrapment efficiency and particle size analysis by laser diffractometry (LD) were determined, and existence of a drug-lipid interaction was investigated by differential scanning calorimetry (DSC) on the SLKM, before being compressed into the tablets by direct compression method. Finally, in vitro release studies were performed and the release kinetics of the waxy tablets were calculated. A commercial ketoprofen retard tablet (reference: Profenid Retard 200 mg) was also examined to compare the release properties. While the data obtained from DSC were indicating absence of drug-lipid interaction in the SLKM, it was determined that 28.62% (+/-2.08), 38.60% (+/-1.91) and 47.00% (+/-1.82) of ketoprofen was released from the tablets containing (1:2) and (1:1) SLKM and Profenid Retard 200 mg in pH 7.4 phosphate buffer solution after 8 h, respectively.
Uner
Melike
M
Faculty of Pharmacy, Department of Pharmaceutical Technology, Istanbul University, Beyazit, 34119 Istanbul, Turkey. melikeuner@yahoo.com
Gönüllü
Umit
U
Yener
Gülgün
G
Altinkurt
Turan
T
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000493:pharmacokinetics*; D004655:Emulsions; D006207:Half-Life; D007660:Ketoprofen / Q000097:blood / Q000493:pharmacokinetics*; D010316:Particle Size; D013607:Tablets; D014885:Waxes
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004655:Emulsions; D013607:Tablets; D014885:Waxes; C038228:beeswax; D007660:Ketoprofen