The improvement of dissolution is a better way for improving the oral absorption of lacidipine (LCDP) because it is a BCS II class drug. The purpose of this study is to improve the oral bioavailability of LCDP by applying nanosuspension technology. LCDP nanosuspensions were prepared by a hybrid method of microprecipitation and high pressure homogenization. The effects of the production parameters (shearing rates and time, the stabilizers and their concentrations, homogenization pressures and cycles) were investigated to optimize the preparation process. The in vitro characterizations (X-ray powder diffraction, differential scanning calorimetry, scanning electron microscopy and dissolution) were carried out and the oral pharmacokinetic study was performed in beagle dogs. LCDP was transformed to amorphous state in the preparation process, and the mean particle size was about 714.0 ± 12.7 nm. The dissolution rate of LCDP nanosuspensions was faster than that of physical mixtures, but slower than Lacipil® (the commercial tablet). For in vivo pharmacokinetics, the key pharmacokinetic parameters (Cmax and AUC 0-∞) of the nanosuspensions were statistically higher than that of both commercial tablet and physical mixtures.

 

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