The effect of superdisintegrants on the properties and dissolution profiles of liquisolid tablets containing rosuvastatin

Pharm Dev Technol. 2017 Mar;22(2):138-147. doi: 10.3109/10837450.2015.1089900. Epub 2015 Sep 24.

Abstract

Context: The preparation of liquisolid systems (LSS) represents a promising method for enhancing a dissolution rate and bioavailability of poorly soluble drugs. The release of the drug from LSS tablets is affected by many factors, including the disintegration time.

Objective: The evaluation of differences among LSS containing varying amounts and types of commercially used superdisintegrants (Kollidon® CL-F, Vivasol® and Explotab®).

Materials and methods: LSS were prepared by spraying rosuvastatin solution onto Neusilin® US2 and further processing into tablets. Varying amounts of superdisintegrants were used and the differences among LSS were evaluated. The multiple scatter plot method was used to visualize the relationships within the obtained data.

Results and discussion: All disintegrants do not showed negative effect on the flow properties of powder blends. The type and concentration of superdisintegrant had an impact on the disintegration time and dissolution profiles of tablets. Tablets with Explotab® showed the longest disintegration time and the smallest amount of released drug. Fastest disintegration and dissolution rate were observed in tablets containing Kollidon® CL-F (≥2.5% w/w). Also tablets with Vivasol® (2.5-4.0% w/w) showed fast disintegration and complete drug release.

Conclusion: Kollidon® CL-F and Vivasol® in concentration ≥2.5% are suitable superdisintegrants for LSS with enhanced release of drug.

Keywords: Data visualization; disintegration time; dissolution profile; liquisolid systems; superdisintegrant.

MeSH terms

  • Aluminum Compounds / chemistry*
  • Anticholesteremic Agents / administration & dosage*
  • Anticholesteremic Agents / chemistry
  • Drug Compounding
  • Drug Liberation
  • Magnesium Compounds / chemistry*
  • Pharmaceutic Aids / chemistry*
  • Povidone / chemistry*
  • Rosuvastatin Calcium / administration & dosage*
  • Rosuvastatin Calcium / chemistry
  • Silicates / chemistry*
  • Solubility
  • Starch / analogs & derivatives*
  • Starch / chemistry
  • Tablets / chemistry

Substances

  • Aluminum Compounds
  • Anticholesteremic Agents
  • Magnesium Compounds
  • Pharmaceutic Aids
  • Silicates
  • Tablets
  • aluminum magnesium silicate
  • Rosuvastatin Calcium
  • Starch
  • sodium starch glycolate
  • Povidone