Extended release lipophilic indomethacin microspheres: formulation factors and mathematical equations fitted drug release rates.
Extended release liphophilic microspheres of indomethacin were prepared using cetostearyl alcohol (CsA), stearyl alcohol (SA) and cetyl alcohol (CA) in the various drug-lipid ratios. The release of indometacin was studied on the basis of USP criteria and the effects of drug-lipid ratio, the size of microspheres and carboxymethylcellulose sodium (CMC-Na) added as a hydrophilic polymer on the drug release were investigated. In vitro dissolution studies were performed using USP XXIII apparatus I at pH 6.2. Release profiles were evaluated according to first order, Higuchi square root of time and Hixson-Crowell cube root models. The best fit was found with the square root of time model (r2=0.991) for the microspheres (125-250 microm) prepared in 1:4:1 drug-lipid-copolymer ratio using stearyl alcohol. With a further regression analysis, an excellent equation (Release%=-10.721+42.549*square root of (t)-4.027*t) was developed for empirical drug estimation (r2=0.998).
Karasulu
Ercüment
E
Department of Biopharmaceutics and Pharmacokinetics, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey. karasulue@pharm.ege.edu.tr
Yeşim Karasulu
H
H
Ertan
Gökhan
G
Kirilmaz
Levent
L
Güneri
Tamer
T
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D007213:Indomethacin / Q000737:chemistry* / Q000493:pharmacokinetics*; D008863:Microspheres; D008962:Models, Theoretical
D003692:Delayed-Action Preparations; D007213:Indomethacin