Spironolactone release from liquisolid formulations prepared with Capryol™ 90, Solutol® HS-15 and Kollicoat® SR 30 D as non-volatile liquid vehicles

Eur J Pharm Biopharm. 2013 Feb;83(2):203-23. doi: 10.1016/j.ejpb.2012.08.004. Epub 2012 Aug 30.

Abstract

The purpose of the study is to enhance dissolution of spironolactone as a model hydrophobic drug through application of liquisolid technology. Spironolactone is prepared as liquisolid formulations, and its dissolution property is evaluated and compared to that of conventional spironolactone tablets and pure spironolactone. Three non-volatile liquid vehicles were used in the design of spironolactone liquisolid formulations, Capryol™ 90, Synperonic® PE/L61 in combination with Solutol® HS-15 at a ratio of 1:1, and Kollicoat® SR 30 D. Spironolactone liquisolid formulations were tested according to British Pharmacopoeia (BP) quality control tests. Furthermore, the prepared liquisolid powder formulations were evaluated via differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) and scanning electron microscopy. Also, liquisolid formulations were subjected to testing of storage stability at high relative humidity. The results indicated that most of liquisolid tablets met the BP requirements. Dissolution results indicate that release of spironolactone was significantly increased (P<0.05) through liquisolid formulations, compared to pure drug. Liquisolid powder formulations formulated from a combination of Synperonic® PE/L61-Solutol® HS-15 showed highest dissolution. DSC thermograms from liquisolid formulations revealed that drug endothermic peak was disappeared after processing. Dissolution, DSC and FT-IR data after storage demonstrated that there were no significant changes in the formulations after storage. In conclusion, the liquid vehicles used within spironolactone liquisolid formulations enhanced drug dissolution rate.

Keywords: Capryol™ 90; Kollicoat® SR 30 D; Solutol® HS 15; Spironolactone liquisolid tablets; Synperonic® PE/L61.

MeSH terms

  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Excipients / chemistry
  • Humidity
  • Hydrophobic and Hydrophilic Interactions
  • Polyethylene Glycols / chemistry*
  • Polyvinyls / chemistry*
  • Powders / chemistry
  • Solubility
  • Spironolactone / chemistry*
  • Stearic Acids / chemistry*
  • Tablets / chemistry

Substances

  • Drug Carriers
  • Excipients
  • Polyvinyls
  • Powders
  • Stearic Acids
  • Tablets
  • Spironolactone
  • polyvinyl acetate
  • Polyethylene Glycols
  • Solutol HS 15