Abstract
Liquisolid systems are an innovative dosage form used for enhancing dissolution rate and improving in vivo bioavailability of poorly soluble drugs. These formulations require specific evaluation methods for their quality assurance (e.g., evaluation of angle of slide, contact angle, or water absorption ratio). The presented study is focused on the preparation, modern in vitro testing, and evaluation of differences of liquisolid systems containing varying amounts of a drug in liquid state (polyethylene glycol 400 solution of rosuvastatin) in relation to an aluminometasilicate carrier (Neusilin US2). Liquisolid powders used for the formulation of final tablets were prepared using two different methods: simple blending and spraying of drug solution onto a carrier in fluid bed equipment. The obtained results imply that the amount of liquid phase in relation to carrier material had an effect on the hardness, friability, and disintegration of tablets, as well as their height. The use of spraying technique enhanced flow properties of the prepared mixtures, increased hardness values, decreased friability, and improved homogeneity of the final dosage form.
Highlights
Bioavailability of drugs after oral administration depends on several factors such as aqueous solubility, drug permeability, dissolution rate, first-pass and presystemic metabolism, and susceptibility to efflux mechanisms
The presented study is focused on the preparation, in vitro testing, and evaluation of differences of liquisolid systems containing varying amounts of liquid state drug in relation to aluminometasilicate carrier Neusilin US2
A liquisolid system can be prepared by incorporating a drug in liquid state onto a specific carrier and coating material while forming a dry, free-flowing, and readily compressible powdered blend
Summary
Bioavailability of drugs after oral administration depends on several factors such as aqueous solubility, drug permeability, dissolution rate, first-pass and presystemic metabolism, and susceptibility to efflux mechanisms. One of the most important and promising areas of the modern pharmaceutical technology is focused on modern approaches to the formulation and evaluation of solid dosage forms with enhanced bioavailability of poorly soluble drugs. These drugs represent up to 40% of commonly used active substances and almost 70% of newly synthesized molecules. The formulation of liquisolid systems (LSS) represents one of the most promising and innovative techniques for promoting dissolution rate and in vivo bioavailability of poorly soluble drugs
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