Objective:The pharmacokinetics and relative bioavailability of Jiaotai pill self-microemulsion were evaluated by investigating the blood concentration of Berberine,Coptisine,Palmatine and Jatrorrhizine in insomnia rat...Objective:The pharmacokinetics and relative bioavailability of Jiaotai pill self-microemulsion were evaluated by investigating the blood concentration of Berberine,Coptisine,Palmatine and Jatrorrhizine in insomnia rats.Methods:Insomnia rat model was established by intraperitoneal injection of p-chlorophenylalanine(PCPA).The model rats were given Jiaotai pill self-microemulsion and Jiaotai pill suspension.The contents of Berberine,Coptisine,Palmatine and Jatrorrhizine in plasma at different times after administration were determined by UPLC-MS/MS,and calculate pharmacokinetic parameters.Results:Under the set chromatographic conditions,the linear relationship of the four components was good,and the precision,accuracy and stability meet the requirements of biological samples.After intragastric administration of Jiaotai pill self-microemulsion,The C_(max) of Berberine,Coptisine,Palmatine and Jatrorrhizine were(412.68±28.45),(68.65±3.92),(34.06±3.13),(40.60±1.22)ng/mL,and AUC_(0-∞)were(672.70±72.55),(146.04±25.01),(71.49±18.67),(72.25±9.54)ng·mL^(-1)·h^(-1),respectively.Compared with Jiaotai pill suspension,the Cmax,AUC_(0-t) and AUC_(0-∞)of the four components in insomnia rats were significantly increased(P<0.01).Conclusion:Jiaotai pill self-microemulsionl can promote the absorption of effective components in insomnia rats and improve its bioavailability.展开更多
Objective： To study the mechanism of inhibition of SMMC-7721 liver cancer cells by quercetin self-nanoemulsifying drug delivery system （Q-SNEDDS） in vitro. Methods： The inhibitory effect of Q-SNEDDS on hepatoma ce...Objective： To study the mechanism of inhibition of SMMC-7721 liver cancer cells by quercetin self-nanoemulsifying drug delivery system （Q-SNEDDS） in vitro. Methods： The inhibitory effect of Q-SNEDDS on hepatoma cells was detected by MTT assay. The effect of Q-SNEDDS on apoptosis of hepatoma cells was detected by flow cytometry. The changes of Q-SNEDDS after hepatoma cells were observed by fluorescence microscopy. The effect of Q-SNEDDS on the expression of signal tra_nsduction and activator of transcription 3 （STAT3） and a_nti-apoptotic factor （survivin） protein in hepatoma cells was examined by Immunohistochemistry. Results： Q-SNEDDS significantly inhibited the proliferation of hepatoma cells in a concentration-dependent manner. After 24 h of Q-SNEDDS treatment, the total apoptosis rate was 25.8%; STAT3 and survivin protein expression was down-regulated in the Q-SNEDDS group. Conclusion： Q-SNEDDS may play a role in inducing apoptosis by inhibiting the expression of STAT3 and survivin proteins.展开更多
Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of H...Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion(SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve(AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension(P <0.01).The absorption rate constant(K_a) and the apparent permeability coefficient(P_(app)) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of K_a and P_(app) of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration(C_(max)) of the blocking model were significantly lower than those of the control model(P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.展开更多
基金Scientific Research Project of Heilongjiang Provincial Health Commission(No.2018-482)Excellent Discipline Team Project of Jiamusi University(No.JDXKTD-2019005)。
文摘Objective:The pharmacokinetics and relative bioavailability of Jiaotai pill self-microemulsion were evaluated by investigating the blood concentration of Berberine,Coptisine,Palmatine and Jatrorrhizine in insomnia rats.Methods:Insomnia rat model was established by intraperitoneal injection of p-chlorophenylalanine(PCPA).The model rats were given Jiaotai pill self-microemulsion and Jiaotai pill suspension.The contents of Berberine,Coptisine,Palmatine and Jatrorrhizine in plasma at different times after administration were determined by UPLC-MS/MS,and calculate pharmacokinetic parameters.Results:Under the set chromatographic conditions,the linear relationship of the four components was good,and the precision,accuracy and stability meet the requirements of biological samples.After intragastric administration of Jiaotai pill self-microemulsion,The C_(max) of Berberine,Coptisine,Palmatine and Jatrorrhizine were(412.68±28.45),(68.65±3.92),(34.06±3.13),(40.60±1.22)ng/mL,and AUC_(0-∞)were(672.70±72.55),(146.04±25.01),(71.49±18.67),(72.25±9.54)ng·mL^(-1)·h^(-1),respectively.Compared with Jiaotai pill suspension,the Cmax,AUC_(0-t) and AUC_(0-∞)of the four components in insomnia rats were significantly increased(P<0.01).Conclusion:Jiaotai pill self-microemulsionl can promote the absorption of effective components in insomnia rats and improve its bioavailability.
文摘Objective： To study the mechanism of inhibition of SMMC-7721 liver cancer cells by quercetin self-nanoemulsifying drug delivery system （Q-SNEDDS） in vitro. Methods： The inhibitory effect of Q-SNEDDS on hepatoma cells was detected by MTT assay. The effect of Q-SNEDDS on apoptosis of hepatoma cells was detected by flow cytometry. The changes of Q-SNEDDS after hepatoma cells were observed by fluorescence microscopy. The effect of Q-SNEDDS on the expression of signal tra_nsduction and activator of transcription 3 （STAT3） and a_nti-apoptotic factor （survivin） protein in hepatoma cells was examined by Immunohistochemistry. Results： Q-SNEDDS significantly inhibited the proliferation of hepatoma cells in a concentration-dependent manner. After 24 h of Q-SNEDDS treatment, the total apoptosis rate was 25.8%; STAT3 and survivin protein expression was down-regulated in the Q-SNEDDS group. Conclusion： Q-SNEDDS may play a role in inducing apoptosis by inhibiting the expression of STAT3 and survivin proteins.
基金supported by the National Natural Science Foundation of China(Grant Nos.8127410081573615)+2 种基金Natural Science Foundation of Anhui Province of China(Grant No.1408085QH189)Key Project for the Excellent Higher Education of Anhui Province of China(Grant No.2013SQRL019ZD)Research Project for the Science and Technology of Bozhou city of China(Grant No.BK2015005)
文摘Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion(SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve(AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension(P <0.01).The absorption rate constant(K_a) and the apparent permeability coefficient(P_(app)) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of K_a and P_(app) of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration(C_(max)) of the blocking model were significantly lower than those of the control model(P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.
