Abstract：OBJECTIVE To prepare notoginsenoside R1 (R1) phospholipid complex (R1-PC) under optimized conditions and conduct its quality evaluation, which belongs to class Ⅲ of biopharmaceuticals classification system (BCS) and has high water solubility, low permeability, and poor oral bioavailability, in order to improve its intestinal absorption. METHODS The phospholipid complex was prepared by solvent volatilization method. Taking the drug-lipid complex rate as the index, the reaction solvent, drug-lipid ratio and other influencing factors were optimized by single factor test. R1-PC was characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD) and differential calorimetric scanning (DCS). At the same time, the oil-water partition coefficient, intestinal absorption rate and stability were also investigated. RESULTS Under the conditions of using tetrahydrofuran as solvent, R1-lecithin (molar ratio) of 1∶2, R1 concentration of 10 mg ·mL-1, reaction temperature at 40 ℃, and reaction time for 2 h, the recombination rate of R1-PC could reach 99.00%. SEM, XRD and DCS all verified the formation of R1-PC. The oil-water partition coefficient was 3.6 (in water) and 4.1 (in pH 6.8 buffer) times higher than that of R1, and the cumulative absorption of colon in vitro was significantly higher than that of crude drug (P<0.001). It was stable under the condition of high temperature and humidity, but unstable under strong light, and it was also stable at room temperature for 3 months. CONCLUSION The established preparation process of R1-PC is simple and feasible, with high recombination rate, significantly improved intestinal absorption and good stability, so it is suitable for industrial production.
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