Improved dissolution behavior of lipophilic drugs by solid dispersions: the production process as starting point for formulation considerations

Abstract

Solid dispersions can be successfully prepared by simple fusion, hot melt extrusion, spray drying, freeze drying and supercritical fluid precipitation. Hot melt extrusion, spray drying and freeze drying are processes that can be applied for large scale production. The simple fusion method is not very suitable for large scale production, but is particularly suitable for screening formulations. The most recent method to produce sold dispersions is supercritical fluid precipitation. The process conditions of this method need extensive investigation, in particular in relationship with the selection of the type of carrier and/or solvent. Both processes and formulation aspects strongly affect the characteristics of solid dispersion products. Furthermore, application of crystalline solid dispersions is gaining increasing interest because they are thermodynamically more stable than amorphous solid dispersions.

Peningkatan Laju Disolusi Dispersi Padat Amorf Genistein dengan PVP K-30

“…Kemudian larutan diuapkan dalam oven vakum pada suhu 40-50 °C sampai kering yang rendah kelarutan dalam air. Istilah sistem dispersi padat didefinisikan sebagai dispersi satu atau lebih senyawa obat dalam pembawa atau matriks inert dalam keadaan padat yang dibuat dengan metode pelarutan, pelelehan atau gabungan keduanya [4,5,6,7]. dan massa yang terbentuk digerus dan dilewatkan melalui ayakan mesh 70.…”

Extruded Soluplus/SIM as an oral delivery system: characterization, interactions,in vitroandin vivoevaluations

“…Converting crystalline drugs into their amorphous counterparts is an efficient way to improve the dissolution rate and solubility of poorly water-soluble drugs, especially for biopharmaceutics classification system (BCS) Class II compounds (Srinarong, 2011).…”

“…But the amorphous state is easy to decompose and also tend to go back to the natural crystalline one, which is called physicochemical instability (Ambike, 2005). HME technique is well-known to be an efficient way to enhance the dissolution (Srinarong et al, 2011). It is a continuous, simple and efficient process not requiring a solvent, aimed at preparing a molecular dispersion or glass solution of the drug in a matrix (Dexia, 2013).…”

Polymeric formulations for drug release prepared by hot melt extrusion: application and characterization

“…Further, HME technology has been widely applied to increase dissolution rate and thereby the bioavailability of poorly water-soluble drugs after oral administration by dispersing the drug in a matrix of a highly water-soluble polymer [77]. These so-called solid dispersions are two or more component systems in which the drug is molecularly dispersed or dispersed as nanoparticles in the crystalline or amorphous state in a hydrophilic carrier [78,79]. Suitable polymeric carries are PVP, PVP-VA, PEG, HPC, HPMC, polymethacrylate derivatives and a polyvinyl caprolactam-polyvinyl acetate-PEG graft copolymer (Soluplus 1 ).…”