In Vitro Dissolution And In Vivo Pharmacokinetic Evaluation Of Panax Notoginseng Powder With Different Particle Sizes

Objective:To study the effect of different particle sizes on the dissolution and bioavailability of effective substances in Panax notoginseng powder?PNP?.Methods:The surface morphology,thermal characteristics and rheological properties of PNP were characterized by scanning electron microscope,polarized light microscope,DSC,and rheometer.The in vitro release properties and different particle sizes of PNP were investigated using water and artificial gastric juice as release media.In vitro release performance of PNP after warm soaking in water at different temperatures?30,40,50 and 100??,the effects of particle size and water infiltration temperature on the pharmacokinetic behavior were investigated.The acute toxicity of PNP with different particle sizes was investigated by the maximum dose method.Results:1.Six kinds of PNP with a particle size ranging from 59.89 to 213.93?m were prepared.The appearance of the powder was a gray-yellow powder.As the particle size decreased,the color changed from dark to light.Scanning electron microscopy results showed that when the particle size was reduced to 90?m,agglomeration began to occur;polarized light results showed that as the particle size decreased,the contained starch particles were more easily exposed;DSC results showed that the PNP began to gelatinize.The temperature is between 40 and 50?,regardless of particle size.Rheological studies show that the viscoelasticity of PNP changes after water infiltration at different temperatures,and the viscosity of each powder reaches a maximum at 100?.2.Dissolution experiments of PNP treated with different particle diameters and different temperatures in water and artificial gastric juice as dissolution media found that within the particle size range of 213.93 to 59.89?m,the amount of PNS dissolution in powder1 was higher than other powders,the PNS dissolution amount of PNP at 40?water temperature was higher than that of PNP at other water temperatures.3.Pharmacokinetics of blood in rats showed that the AUC_0-Tof three saponins in powder 4?90.38±8.28?m?group was significantly higher than other powder groups.The bioavailability of panax notoginsenoside R₁and ginsenoside Rg₁contained in PNP at a water temperature of 40?was higher than other temperatures.After the PNP infiltrated at 50?,the bioavailability of the contained ginsenoside Rb₁was the highest.The integrated pharmacokinetic results showed that the bioavailability of PNP under the infiltration of powder 4 and 40?was the highest.4.The maximum tolerated dose of PNP is 42.72 g/kg and different particle sizes of PNP has no acute toxicity effect on mice.Conclusion:The PNP in the particle size range of 213.93 to 59.89?m is not the smaller the particle size and the higher the dissolution amount with dissolution rate with bioavailability of saponin components.The particle size of 213.93?m was the highest in dissolution rate and dissolution rate,and 90.38?m had the highest bioavailability after intragastric administration.