Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-t...Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-tumor drug, the aim of this study was to obtain a solid dispersion form Garcinia Glycosides by using solvent-melt method so that improve the solubility and dissolution rate. The solid dispersion was characterized by High Performance Liquid Chromatography (HPLC), infrared spectroscopy and evaluated the intestinal absorption of the drug by rat in situ single pass intestinal perfusion. The results showed the increase of solubility, dissolution velocity and absorption compared to other forms. This indicated that solid dispersion could greatly improve the relative bioavailability of Garcinia Glycosides in vivo.展开更多
AIM: To investigate the absorption characteristics of the total alkaloids from Mahoniae Caulis(TAMC) through the administration of monterpene absorption enhancers or protein inhibitors. METHOD: The absorption behavior...AIM: To investigate the absorption characteristics of the total alkaloids from Mahoniae Caulis(TAMC) through the administration of monterpene absorption enhancers or protein inhibitors. METHOD: The absorption behavior was investigated in an in situ single-pass intestinal perfusion(SPIP) assay in rats. RESULTS: The intestinal absorption of TAMC was much more than that of a single compound or a mixture of compounds(jatrorrhizine, palmatine, and berberine). Promotion of absorption by the bicyclic monoterpenoids(borneol or camphor) was higher than by the monocyclic monoterpenes(menthol or menthone), and promotion by compounds with a hydroxyl group(borneol or menthol) was higher than those with a carbonyl group(camphor or menthone). The apparent permeability coefficient(Papp) of TAMC was increased to 1.8-fold by verapamil, while it was reduced to one half by thiamine. The absorption rate constant(Ka) and Papp of TAMC were unchanged by probenecid and pantoprazole. CONCLUSION: The intestinal absorption characteristics of TAMC might be passive transport, and the intestinum tenue was the best absorptive site. In addition, TAMC might be likely a substrate of P-glycoprotein(P-gp) and organic cation transporters(OCT), rather than multidrug resistance protein(MRP) and breast cancer resistance protein(BCRP). Compared with a single compound and a mixture of compounds, TAMC was able to be absorbed in the blood circulation effectively.展开更多
目的:研究不同电荷自乳化递药系统对细梗香草皂苷B(CAPB)小肠吸收的影响。方法:分别制备CAPB的正电荷自乳化递药系统(PO-SEDDS)与负电荷自乳化递药系统(NE-SEDDS),评价其乳粒粒径、Zeta电位和自乳化时间,采用大鼠在体单向肠灌流模型考察...目的:研究不同电荷自乳化递药系统对细梗香草皂苷B(CAPB)小肠吸收的影响。方法:分别制备CAPB的正电荷自乳化递药系统(PO-SEDDS)与负电荷自乳化递药系统(NE-SEDDS),评价其乳粒粒径、Zeta电位和自乳化时间,采用大鼠在体单向肠灌流模型考察CAPB以及两种自乳化递药系统的有效肠渗透速率Peff。结果:CAPB-PO-SEDDS与CAPB-NE-SEDDS的乳粒粒径、Zeta电位和自乳化时间分别为在57.14±6.11 nm vs 56.80±4.72 nm,16.77±4.59 m V vs-3.52±0.31 m V,23±12.1 s vs 27±10.6 s,CAPB在p H=6.55的肠灌流液中能保持稳定,CAPB-PO-SEDDS的Peff为3.73±0.62×105 cm/s,显著高于CAPB-NE-SEDDS(Peff=2.72±0.42×105 cm/s)以及CAPB溶液(Peff=1.08±0.72×105 cm/s)。结论:正电荷自乳化递药系统与负电荷自乳化递药系统以及药物溶液相比,即能保持自乳化性能,又能明显促进CAPB的小肠吸收。展开更多
文摘Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-tumor drug, the aim of this study was to obtain a solid dispersion form Garcinia Glycosides by using solvent-melt method so that improve the solubility and dissolution rate. The solid dispersion was characterized by High Performance Liquid Chromatography (HPLC), infrared spectroscopy and evaluated the intestinal absorption of the drug by rat in situ single pass intestinal perfusion. The results showed the increase of solubility, dissolution velocity and absorption compared to other forms. This indicated that solid dispersion could greatly improve the relative bioavailability of Garcinia Glycosides in vivo.
基金supported by China Pharmaceutical University Training Programs of Innovation for Undergraduates(No.02640390)
文摘AIM: To investigate the absorption characteristics of the total alkaloids from Mahoniae Caulis(TAMC) through the administration of monterpene absorption enhancers or protein inhibitors. METHOD: The absorption behavior was investigated in an in situ single-pass intestinal perfusion(SPIP) assay in rats. RESULTS: The intestinal absorption of TAMC was much more than that of a single compound or a mixture of compounds(jatrorrhizine, palmatine, and berberine). Promotion of absorption by the bicyclic monoterpenoids(borneol or camphor) was higher than by the monocyclic monoterpenes(menthol or menthone), and promotion by compounds with a hydroxyl group(borneol or menthol) was higher than those with a carbonyl group(camphor or menthone). The apparent permeability coefficient(Papp) of TAMC was increased to 1.8-fold by verapamil, while it was reduced to one half by thiamine. The absorption rate constant(Ka) and Papp of TAMC were unchanged by probenecid and pantoprazole. CONCLUSION: The intestinal absorption characteristics of TAMC might be passive transport, and the intestinum tenue was the best absorptive site. In addition, TAMC might be likely a substrate of P-glycoprotein(P-gp) and organic cation transporters(OCT), rather than multidrug resistance protein(MRP) and breast cancer resistance protein(BCRP). Compared with a single compound and a mixture of compounds, TAMC was able to be absorbed in the blood circulation effectively.
文摘目的:研究不同电荷自乳化递药系统对细梗香草皂苷B(CAPB)小肠吸收的影响。方法:分别制备CAPB的正电荷自乳化递药系统(PO-SEDDS)与负电荷自乳化递药系统(NE-SEDDS),评价其乳粒粒径、Zeta电位和自乳化时间,采用大鼠在体单向肠灌流模型考察CAPB以及两种自乳化递药系统的有效肠渗透速率Peff。结果:CAPB-PO-SEDDS与CAPB-NE-SEDDS的乳粒粒径、Zeta电位和自乳化时间分别为在57.14±6.11 nm vs 56.80±4.72 nm,16.77±4.59 m V vs-3.52±0.31 m V,23±12.1 s vs 27±10.6 s,CAPB在p H=6.55的肠灌流液中能保持稳定,CAPB-PO-SEDDS的Peff为3.73±0.62×105 cm/s,显著高于CAPB-NE-SEDDS(Peff=2.72±0.42×105 cm/s)以及CAPB溶液(Peff=1.08±0.72×105 cm/s)。结论:正电荷自乳化递药系统与负电荷自乳化递药系统以及药物溶液相比,即能保持自乳化性能,又能明显促进CAPB的小肠吸收。
