The kinetic mechanism for the preparation of silymarin from milk thistle seeds was studied during the microwave-assisted extraction （MAE） process. The results showed that the transfer rate of silymarin from milk thi...The kinetic mechanism for the preparation of silymarin from milk thistle seeds was studied during the microwave-assisted extraction （MAE） process. The results showed that the transfer rate of silymarin from milk thistle seeds increased with the microwave output power and temperature during MAE processing. The apparent extraction rate constant k （s-1） was 1.2028×10-2 , 1.2248×10-2 , and 1.2485×10-2 , and diffusion coefficient D （m2·s-1 ） was 4.21×10-10, 4.29×10-10 , and 4.37×10-10 at the microwave temperatures of 383, 393, and 403 K, respectively, in the silymarin MAE process. With the help of scanning electron microscopy （SEM）, the microstructures of the samples extracted by MAE were observed. The results revealed that the increased efficiency and rate of MAE of silymarin could be attributed mainly to the subsequent cell change resulting from superheating effects during MAE.展开更多
OBJECTIVE To fabricate Silymarin(SM) nanosuspensions(NSs) and evaluate their protective effect on stress-induced liver injury. METHODS SM nanosuspensions were tailored by combination of the anti-solvent precipitation ...OBJECTIVE To fabricate Silymarin(SM) nanosuspensions(NSs) and evaluate their protective effect on stress-induced liver injury. METHODS SM nanosuspensions were tailored by combination of the anti-solvent precipitation and high pressure homogenization(HPH); the formulations were optimized by central composite design. The pharmacokinetics and pharmacodynamics of SM-NSs were also performed.RESULTS In light of the quadratic mathematical equations derived from the Design of Expert Software,the optimal formulation of SM-NSs consisted of PVP 0.34% and F188 0.36%. The morphology of NSs was found to be spherical with a diameter of about 150 nm using transmission electron microscope(TEM)observation. The pharmacokinetics experiment demonstrated that oral administration of SM-NSs significantly increased its bioavailability compared to the coarse powder(Cmax: 9.03 ± 2.39 mg · L^(-1);AUMC_(0→∞):3757.35±227.19 mg·L^(-1)·h; AUC_(0→∞):171.84±26.61 mg·L^(-1)·h). In pharmacodynamics,it was found that restraint stress produced oxidative effects and increased serum AST and ALT levels in mice,both of which were significantly inhibited by SM and SM-NSs; in addition,administration of SM-NSs showed more effective prevention against acute liver injury than SM coarse suspensions(r^2=0.986,0.984,P<0.05). CONCLUSION The results suggest that fabricated SM-NSs exert potent hepatoprotective effects and attenuate restraint stress-induced liver injury. The study provides an effective approach to improving the property of SM,which can be used for treatment of liver diseases.展开更多
基金Supported by the National Natural Science Foundation of China(31071579)the Key Program of the Natural Science Foundation of Heilongjiang Province of China(ZD201013)the Key Project of Education Department of Heilongjiang Province of China(125212003)
文摘The kinetic mechanism for the preparation of silymarin from milk thistle seeds was studied during the microwave-assisted extraction （MAE） process. The results showed that the transfer rate of silymarin from milk thistle seeds increased with the microwave output power and temperature during MAE processing. The apparent extraction rate constant k （s-1） was 1.2028×10-2 , 1.2248×10-2 , and 1.2485×10-2 , and diffusion coefficient D （m2·s-1 ） was 4.21×10-10, 4.29×10-10 , and 4.37×10-10 at the microwave temperatures of 383, 393, and 403 K, respectively, in the silymarin MAE process. With the help of scanning electron microscopy （SEM）, the microstructures of the samples extracted by MAE were observed. The results revealed that the increased efficiency and rate of MAE of silymarin could be attributed mainly to the subsequent cell change resulting from superheating effects during MAE.
基金The project supported by Natural Science Foundation of Shandong Province(ZR2014HL103,ZR2016HM21,J13LM51)Taishan Medical University Foundation(2014GCC15)the Foundation of Overseas Distinguished Taishan Scholars of Shandong Province,China
文摘OBJECTIVE To fabricate Silymarin(SM) nanosuspensions(NSs) and evaluate their protective effect on stress-induced liver injury. METHODS SM nanosuspensions were tailored by combination of the anti-solvent precipitation and high pressure homogenization(HPH); the formulations were optimized by central composite design. The pharmacokinetics and pharmacodynamics of SM-NSs were also performed.RESULTS In light of the quadratic mathematical equations derived from the Design of Expert Software,the optimal formulation of SM-NSs consisted of PVP 0.34% and F188 0.36%. The morphology of NSs was found to be spherical with a diameter of about 150 nm using transmission electron microscope(TEM)observation. The pharmacokinetics experiment demonstrated that oral administration of SM-NSs significantly increased its bioavailability compared to the coarse powder(Cmax: 9.03 ± 2.39 mg · L^(-1);AUMC_(0→∞):3757.35±227.19 mg·L^(-1)·h; AUC_(0→∞):171.84±26.61 mg·L^(-1)·h). In pharmacodynamics,it was found that restraint stress produced oxidative effects and increased serum AST and ALT levels in mice,both of which were significantly inhibited by SM and SM-NSs; in addition,administration of SM-NSs showed more effective prevention against acute liver injury than SM coarse suspensions(r^2=0.986,0.984,P<0.05). CONCLUSION The results suggest that fabricated SM-NSs exert potent hepatoprotective effects and attenuate restraint stress-induced liver injury. The study provides an effective approach to improving the property of SM,which can be used for treatment of liver diseases.
