Abstract
The activity of pharmaceutical substances crucially depends on the bioavailability of the substances. The bioavailability of drugs in body and their rate of dissolution in the biological fluids are increased if the particle size is decreased. In the present paper, the Gas Anti-Solvent (GAS) method was used to lower the size of rosuvastatin particles. The effects of temperature (313–338 K), pressure (105–180 bar) and initial solute concentration (20–60 mg/ml) were evaluated by Response Surface Methodology (RSM). The optimum initial solute concentration, temperature and pressure were found to be 20 mg/ml, 313 K and 180 bar, respectively which resulted in the minimum particle size. Furthermore, the particles were characterized by Differential Scanning Calorimetry (DSC), Dynamic Light Scattering (DLS), Fourier Transform Infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and X-Ray Diffraction (XRD). The analyses showed that the rosuvastatin particles (60.3 nm) precipitated by GAS process become significantly smaller than the initial particles (45.8 µm).
Highlights
In the pharmaceutics, the insolubility or weak solubility of many drugs in the biological media results in the limited bioavailability, and at the low doses, the therapeutic response is poor [1]
The analyses showed that the rosuvastatin particles (60.3 nm) precipitated by Gas Anti-Solvent (GAS) process become significantly smaller than the initial particles (45.8 μm)
Mean size of rosuvastatin calcium (ROSCa) particles was reduced from 45.8 μm to 60.3 nm using the GAS method
Summary
The insolubility or weak solubility of many drugs in the biological media results in the limited bioavailability, and at the low doses, the therapeutic response is poor [1]. It has been estimated that more than 60 % of pharmaceutical drugs have poor water solubility. A major challenge in the pharmaceutics is that the drugs are weakly soluble in water. The weak solubility of a drug may lead to the low dissolution characteristics which may bring about limited bioavailability as well as reduced therapeutic efficacy [2]. The size of drug particle is a limiting factor contributing to the low bioavailability of the compounds with the weak solubility. The dissolution rate of drugs can be improved using the micronization method to resolve the above problems
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
