Abstract

Objective: The objective of the present work was to formulate the solid dispersions of simvastatin for enhancement of its aqueous solubility and dissolution rate.
 Methods: In the present study, solid dispersions of simvastatin were prepared by Kneading and Solvent evaporation methods. The polymeric carriers like Polyethylene glycol (PEG) 6000 and Polyvinyl Pyrrolidone (PVP) K30 were used in different ratios (ratio of drug: carrier was 1:1, 1:2) to formulate solid dispersions. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and evaluated for drug content, percentage yield, saturation solubility, in vitro dissolution studies. The best formula of the solid dispersion was selected according to the solubility and dissolution data.
 Results: The F7 formulation was found to be an optimized formulation containing PVP K30 in the ratio 1:1 prepared by solvent evaporation technique. The Drug content was found to be higher i.e. 94.89 in the F7 batch. The FT-IR spectra revealed that there was no interaction between drugs and carriers. DSC thermogram indicated entrapment of simvastatin in PVP K30 and the conversion of crystalline simvastatin into an amorphous form. The F7 formulation showed maximum drug release i.e. 98.60% in 60 min which is 2 times greater than pure drug making it an optimized formulation.
 Conclusion: The solubility of simvastatin was successfully enhanced through the solid dispersion technique. Solid dispersions prepared with solvent evaporation method were more soluble than solid dispersions prepared with kneading method with carrier PVP K30.

Highlights

  • Near about 35-40% of new chemical entities possess the problem of low aqueous solubility that affects drug absorption in the gastrointestinal tract (GIT) which leads to lower bioavailability, high inter and intrasubject variability, dose dumping chances, reduction in the effectiveness of the medication, and lastly, formulation development get collapsed [1]

  • The plot had a correlation coefficient (R2) of 0.996, a slope of 0.022, and a Cintercept of–0.012. These results indicated that there is a linear relationship between concentration (5–25 μg/ml) and absorbance, as shown in fig

  • The result showed that the solid dispersions prepared with the solvent evaporation method give a higher dissolution rate than the kneading method

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Summary

Introduction

Near about 35-40% of new chemical entities possess the problem of low aqueous solubility that affects drug absorption in the gastrointestinal tract (GIT) which leads to lower bioavailability, high inter and intrasubject variability, dose dumping chances, reduction in the effectiveness of the medication, and lastly, formulation development get collapsed [1]. In such cases, scientists look for better formulations that will improve solubility and dissolution and bioavailability get improved. The term dispersion means a hydrophobic drug is dispersed in an inert hydrophilic matrix [4]

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