ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF ERLOTINIB HYDROCHLORIDE BY SOLID DISPERSION TECHNIQUE WITH POLOXAMER 188: PREPARATION AND IN-VITRO EVALUATION

摘要

Solid dispersions (SDs) of Erlotinib hydrochloride (ETN) were prepared to enhance the solubility by solvent evaporation (SE) and Melting (MM) method using poloxamer 188 (PL 188) in the ratio of 1:1, 1:3 and 1:5 (w:w). The solubility of the drug was increased in a concentration-dependent manner of polymer and follow linearity order. The solid dispersion was characterized by Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The FTIR spectra revealed the drug was found compatible and did not show any interaction with polymer, PXRD spectra, and DSC thermographs showed a clear transformation of crystalline to an amorphous form of drug particles. In-vitro dissolution study was performed in dissolution medium i.e. 0.1N HCl (pH 1.2). Cumulative percent drug release from SDs prepared by the SE method was faster than from the pure drug, physical mixture (PM), and SDs prepared by the MM method. The maximum percent drug release (90.07 ± 0.78) was found with PL 188 in the ratio of 1:5 (w/w). Among the used techniques, the SE method demonstrating maximum increased in solubility as well as in-vitro drug release profile. Therefore, it is concluded that the use of the SE method is a promising approach to enhance the solubility and dissolution rate of ETN.