Dizajniranje i evaluacija oralnih raspadajućih tableta dekstrometorfan hidrobromida s maskiranim okusom

The present study is aimed to develop dextromethorphan hydrobromide (DXM) oral disintegrating tablets (ODT) with acceptable palatability to help patients of all age group. The bitter taste of the drug was masked by binding the drug to ion exchange resin. The effect of particle size of resin on drug loading was studied. In vitro and in vivo disintegration time and in vitro drug release studies were performed. Drug loading increased significantly with a decrease in the particle size of the resin. DSC and XRPD studies reveal that the molecular state of the drug changed from crystalline to amorphous form. The dissolution efficiency calulated for optimized ODT and conventional directly compressed tablet were almost comparable, indicating free dissociation of the drug from the resinate. The bitter taste of DXM can be masked by binding with ion exchange resin and the resinate can be successfully formulated into oral disintegrating tablets.Cilj rada bio je pripraviti raspadajuće tablete dekstrometorfan hidrobromida (DXM) za oralnu primjenu (ODT) prihvatljivog okusa s namjerom da se pomogne pacijentima svih dobnih skupina. Gorki okus ljekovite tvari maskiran je vezanjem lijeka na ionsko-izmjenjivačku smolu. Proučavan je utjecaj veličine čestica smole na količinu ljekovite tvari koja se može na nju vezati, vrijeme raspadanja in vitro i in vivo, te oslobađanje lijeka in vitro. Količina vezanog lijeka značajno se povećava sa smanjenjem veličine čestica smole. DSC i XRPD studije pokazuju da prilikom vezanja kristalinični oblik lijeka prelazi u amorfni. Oslobađanje ljekovite tvari izračunato za optimizirane ODT i izravno komprimirane tablete vrlo je slično, što ukazuje na slobodno oslobađanje lijeka iz smole. Gorki okus DXM može se maskirati vezanjem ljekovite tvari na ionsko-izmjenjivačku smolu iz koje se mogu pripraviti raspadajuće tablete za oralnu primjenu

In vitro transcutaneous permeation of acyclovir sodium from HPMC gels: role of chemical permeation enhancers

The main objective of the present study is to improve the permeation of acyclovir sodium (ACV) across stratum corneum (SC) from HPMC gel formulations. We have also investigated the role of chemical permeation enhancers like dimethyl sulfoxide, ethanol, limonene and sodium taurodeoxycholate on the transcutaneous permeation of ACV from HPMC gels. The optimized formulations were characterized and subjected to in vitro permeation study using excised rat abdominal skin. The histological examination of the skin was studied to understand the mechanisms involved in the permeation of ACV across skin. The cumulative amount of ACV permeated and the increase in permeation parameters (Jss, Kp and ER) were significantly higher for gel formulations compared to marketed formulation. A 2 to 4 fold increase in enhancement ratio clearly indicates the potential of formulating ACV into a gel.Colegio de Farmacéuticos de la Provincia de Buenos Aire