Experimental Design for Determination of Effects of Superdisintegrant Combinations on Liquisolid System Properties

J Pharm Sci. 2017 Mar;106(3):817-825. doi: 10.1016/j.xphs.2016.11.002. Epub 2016 Dec 5.

Abstract

The preparation of liquisolid systems presents a promising and innovative possibility for enhancing dissolution profiles and improving the bioavailability of poorly soluble drugs. This study aims to evaluate the differences in the properties of liquisolid systems containing combinations of 3 commercially used superdisintegrants (sodium starch glycolate, crospovidone, and croscarmellose sodium). Multiple regression models and contour plots were used to study how the amount and the type of superdisintegrant used affected the quality parameters of liquisolid tablets. The results revealed that an increased amount of crospovidone in the mixture improves disintegration and wetting time and enhances drug release from the prepared liquisolid tablets. Moreover, it was observed that a binary blend of crospovidone and sodium starch glycolate improved tablet disintegration. Considering the obtained results, it could be stated that crospovidone showed the best properties to be used as superdisintegrant for the preparation of liquisolid systems containing rosuvastatin.

Keywords: Biopharmaceutics Classification System; dissolution rate; excipients; multivariate analysis; solid dosage form; solid state; solubility; sorption; tableting; wetting.

MeSH terms

  • Carboxymethylcellulose Sodium / chemical synthesis*
  • Carboxymethylcellulose Sodium / pharmacokinetics
  • Chemistry, Pharmaceutical / methods*
  • Dosage Forms
  • Drug Liberation
  • Excipients / chemical synthesis
  • Excipients / pharmacokinetics
  • Pharmaceutic Aids / chemical synthesis
  • Pharmaceutic Aids / pharmacokinetics
  • Povidone / chemical synthesis*
  • Povidone / metabolism
  • Research Design
  • Solubility
  • Starch / analogs & derivatives*
  • Starch / chemical synthesis
  • Starch / pharmacokinetics

Substances

  • Dosage Forms
  • Excipients
  • Pharmaceutic Aids
  • Starch
  • sodium starch glycolate
  • Povidone
  • Carboxymethylcellulose Sodium