Original Article

Physicochemical Characterization and Dissolution Properties of Cinnarizine Solid Dispersions

  • Bahar Selen KALAVA
  • Müzeyyen DEMIREL
  • Yasemin YAZAN

Received Date: 25.08.2004 Accepted Date: 30.05.2005 Turk J Pharm Sci 2005;2(2):51-62

Abstract Bioavailability of acalcium antagonist cinnarizine, known to have a low aqueous solubility, islow or variable. Enhancement of the dissolution behavior of such a drug material can improve its oral bioavailability. For the improvement of the dissolution rate, solid dispersions were prepared by fusion method dur to the complete dispersion ability of the active ingredient. Two different lipid carriers were used of which one has a gastric solubility and the other does not. The dispersions prepared were filled into cellulose hard capsules. In vitro dissolution rates of the formulations prepared were compared to pure cinnarizine and a commercially available tablet. active material/lipid ratio was found to be effective on the dissolution rates. Dissolution rates of cinnarizine from the solid dispersions prepared using a lipid with gastric solubility were increased when compared to pure cinnarizine while sustained with the other lipid. As a conclusion of the study, it was determined that the dissolution rate of cinnarizine could be enhanced or sustained by using dsfferent carriers with different ratios. Özet Sudaki çözünürlügü düsük olarak bilinen kalsiyum antagonisti sinnarizinin biyoyararlanimi degisken veya düsüktür. Bu özellikleri bir ilaç materyalinin çözünme davranisinin iyilestirilmesi, etkin maddenin biyoyararlanimi gelistirebilir. Çözünme hizinin arttirilmasi için, kati dispersiyonlar, etkin maddenin dispersiyonyeteneginin tam oldugu eritme yöntemiyle hazirlanmistir. Çalismada gastrointestinal sivida çözünebilen ve çözünmeyen iki farkli tasiyici kullanilmistir. Hazirlanan dispersiyonlar sert selüloz kapsüllere doldurulmustur. Formülasyonlarin in vitro çözünme hizlari, saf sinnarizin ve bir piyasa tabletiyle karsilastirilmistir. Etkin Madde I lipit oraninin çözünme hizi üzerinde etkili olabilecegi bulunmustur. Saf sinnarizin ile hazirlanan kati dispersiyonlarin çözünme hizlari karsilastirildiginda, mide sivisinda çözünen lipit kullanildiginda özellik artarken, diger lipitle geciktirilmistir. Çalismanin sonucu olarak, sinnarizin`in çözünme hizinin farkli tasiyicilar ve farkli oranlar kullanilarak, arttirilabilecegi veya kontrol edilebilecegi saptanmistir.

Keywords: Cinnarizine, Solid Dispersion, Fusin Method, Dissolution Rate, In Vitro Dissolution