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  • Effects of drug solubility ...
    Chakraborty, Santanu; Khandai, Madhusmruti; Sharma, Anuradha; Patra, Ch; Patro, V.; Sen, Kalyan

    Acta pharmaceutica (Zagreb, Croatia), 09/2009, Volume: 59, Issue: 3
    Journal Article

    The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release. Cilj rada bio je praćenje učinka topljivosti na kinetiku oslobađdanja vodotopljivog verapamil hidroklorida i netopljivog lijeka aceklofenaka iz matriksnih sustava na bazi hidrofilnog polimera. Matriksni sustavi pripravljeni su izravnom metodom kompresije. Uz ispitivanje uobičajenih fizikalnih svojstava, ispitivana je i dinamika primanja vode, te erozija, SEM i in vitro oslobađanje ljekovite tvari iz tableta. Primjenom eksponencijalne jednadžbe utvrđeno je da mehanizam oslobađanja topljivih lijekova slijedi anomalni ne-Fickov difuzijski transport, dok netopljivi lijekovi slijede kinetiku nultog reda. SEM ispitivanja pokazala su pore na površini matriksa ovisne o topljivosti ljekovite tvari. t-test ukazuje da količina oslobođenog lijeka značajno ovisi o njegovoj topljivosti. Topljivost lijeka ima značajan učinak na kinetiku i mehanizam oslobađanja.