Razvoj i vrednovanje lako topljivih tableta kompleksa meloksikama s β-ciklodekstrinom pripravljenih izravnom kompresijom

The aim of this study was to prepare fast-dissolving tablets of meloxicam after its complexation with β-cyclodextrin (β-CD) and to investigate the effect of using different superdisintegrants on the disintegration and release of meloxicam from the tablets. A complex of meloxicam with β-CD was prepared by spray drying and then compressed in the form of tablets utilizing the direct compression technique. Three superdisintegrants were employed at various levels sodium starch glycolate, croscarmellose sodium, and crospovidone. Co-spray dried micro-crystalline cellulose and mannitol (Avicel HFE-102) were used as diluents in the tablets. Prior to compression, the pre-compression parameters showed satisfactory flow properties. Post-compression parameters showed that all tablet formulations had acceptable mechanical properties. Wetting and disintegration times were prolonged by increasing the level of sodium starch glycolate in the tablets. This was attributed to the formation of a viscous gel layer around the tablets by sodium starch glycolate whereas this effect was not observed with croscarmellose sodium and crospovidone. Dissolution studies showed fast release of meloxicam except in tablets containing a high level of sodium starch glycolate. Complexation of meloxicam with β-CD significantly improved the solubility of the drug and improved the mechanical properties of tablets produced by direct compression.Cilj rada bio je priprava lako topljivih tableta kompleksa meloksikama s β-ciklodekstrinom (β-CD) te ispitati utjecaj različitih superdezintegratora na raspadljivost tableta i oslobađanje meloksikama. Kompleks meloksikama s β-CD pripravljen je metodom sušenja sprejem, a komprimiran je u tablete metodom izravne kompresije. U pripravi tableta korištene su tri različite količine triju superdezintegratora: natrijev škrobni glikolat, natrijeva sol kroskarmeloze i krospovidon, dok su mikrokristalinična celuloza i manitol (Avicel HFE-102) upotrijebljeni kao punila. Predkompresijski parametri ukazivali su na zadovoljavajuću tečnost. Postkompresijski parametri pokazali su da sve tablete imaju prihvatljiva mehanička svojstva. Vlaženje i vrijeme raspadanja bilo je produljeno kada se povećao udio natrijevog škrobnog glikolata u tabletama. To je pripisano stvaranju viskoznog sloja gela oko tableta, što nije primijećeno u pripravi tableta s natrijevom soli kroskarmeloze i krospovidonom. Oslobađanje meloksikama bilo je brzo iz svih tableta, osim iz tableta s visokim udjelom natrijeve soli škrobnog glikolata. Kompleksiranje meloksikama s β-CD značajno je povećalo topljivost lijeka i poboljšalo mehanička svojstva tableta

Enhancement and modification of etoposide release from crospovidone particles loaded with oil-surfactant blends

A novel solid formulation for oral delivery of pH-sensitive, scarce& water-soluble etoposide has been designed, characterized, and tested in vitro. The pulpose of this study was to assess the perfomance of the new dosage forms, in comparison to marketed, liquid-filled capsules. The solid formulation was developed by grinding the drug with a cross-linked polymeric carrier (crospovidone) under controlled prqcess conditions (mechano-physical drug activation), and subsequently incorporating selected oil/surfactant (oh) blends into the polymer particles. Physicochemical characterization (thermal analysis, drug dissolution kinetics, drug o/w partition studies) provided information on drugpolymer interaction at the solid state, and on the formulation peqormance in vitro, resulting in the enhancement and modification of the etoposide solubilization process. DSC thermograms showed the amorphous or nanocrystalline state of etoposide within the carrier, as indicated by the shifting of DSC peaks (AT > -1O'C). Solubility kinetics of etoposide in oversaturation conditions were strongly affected by the chemical nature of the vehicle used: short-chain triglycerides afforded drug concentrations well above 600 pg ml-I for more than 3 hr, versus a drug equilibrium solubility of approximately 150 pg ml-'. Drug dissolution curves under sink conditions were superimposable to those of liquid-jilled capsules available on the market (Vepesid@5 0, Bristol-Myers Squibb), yielding 100% drug release in 10 min. The oil phase/water partition coeficient of etoposide (P) was af fected by the surfactant concentration. The biphasic trend observed in P values suggested a dual mechanism in drug release from polymeric particles: the presence of oily vehicles and suqactants in the formulation could create, upon release, a favorable environment to sustain etoposide dissolution, .slowing down drug reprecipitation. Such solid formulation could be considered equivalent, in vitro, to the current marketed produc