Preparation and in vitro release rate of trichosanthes sustained-release pellets / 国际药学研究杂志

Objective: To prepare Trichosanthes sustained-release pellets and investigate its in vitro release. Methods: Trichosanthes sustained-release pellets were prepared by fluid-bed coating technique.The preparation process of its drug loading layer was optimized by orthogonal experiment with binder, solvent, drug loading and creeping speed of peristaltic pump as the factors of investigation and the yield as the investigation index. The optimum prescription and preparation of the pellets were optimized by single factor test with the content of coating material EC, the amount of poreforming agent PEG4000, the amount of talc powder, the coating weight and the curing time as the factors of investigation and the in vitro release as the investigation index. The in vitro release of the pellets was investigated by high performance liquid chromatography with 3, 29-Diphenyl of Trichosanthes Kirilowii Triol(3, 29-DK)as the detection index. Results: The optimum preparation technology of the drug loading layer was 5% binder, 60% ethanol, 35% drug loading and 0.3 r/min peristaltic velocity of fluid-bed peristaltic pump. The optimum preparation technology of sustained-release layer was 5% EC, 1.5% PEG 4000, 1.25% talc powder, 10% weight gain of coating and 6 h curing. Conclusion: The Tricho- santhes sustained-release pellets prepared in this study were released smoothly. Its production method was simple and easy for operation.

Screening and validation of antithrombotic effective components group from Trichosanthes extract / 药学学报

To screen the antithrombotic effective components group of Trichosanthes extract, and to verify its pharmacodynamics and analyze its mechanism, the HPLC fingerprint of Trichosanthes extract (0.09, 0.45, 0.9 g·kg-1) was established, and the pharmacodynamic indexes of antithrombosis in rats with aspirin (0.01 g·kg-1) as positive control group were determined (the animals used in this experiment were approved by the Medical Ethics Committee of Wannan Medical College). The antithrombotic spectrum-activity relationship of Trichosanthes extract was studied and the effective antithrombotic ingredients group was screened by grey relational analysis. The monomer compound mixed solution (0.006, 0.03, 0.06 g·kg-1) was prepared according to the content of each component in the active component group, and the pharmacodynamics and action mechanism were studied to verify the correctness of the spectrum-effect relationship. The correlation between the 22 components of Trichosanthes extract and antithrombotic efficacy was different and showed dose-effect relationship. Cytosine, uracil, guanine, hypoxanthine, xanthine, adenine, guanosine, and adenosine are the main antithrombotic components of Trichosanthes extract. The ratio of cytosine, uracil, guanine, hypoxanthine, xanthine, adenine, guanosine and adenosine was 3∶12∶10∶5∶2∶8∶13∶14. Compared with the model group, the thrombus dry weight of each effective components group could be effectively reduced (P<0.01 or P<0.05), but there was no significant difference between each effective components group and the Trichosanthes extract group. Compared with the model group, the TXB2 content in group (0.06 g·kg-1, 0.03 g·kg-1) could be effectively reduced (P<0.01 or P<0.05), and the content of 6-keto-PGF1α could be increased in each group (P<0.01), and the TXB2/6-keto-PGF1α tended to be normal and showed a dose-effect relationship. The effect was better than that in the Trichosanthes extract group (0.45 g·kg-1) (P<0.01). The effective ingredients group has a good antithrombotic effect, its mechanism is to inhibit platelet aggregation and improve vascular endothelial function.

Anti-platelet aggregation and anti-thrombotic mechanism of Trichosanthis Fructus combined with aspirin based on network pharmacology / 中国中药杂志

To explore the anti-platelet aggregation and anti-thrombotic mechanisms of Trichosanthis Fructus combined with aspirin based on network pharmacology and the validation of arteriovenous by pass model in rats. The databases of Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP),Drug Repositioning and Adverse Drug Reaction Chemical-Protein Interactome(DRAR-CPI),Universal Protein Resource(Uniprot) and the Database for Annotation,Visualization,and Integrated Discovery(DAVID) were used to predict protein targets and analyze biological pathway and signal pathway in the combination of Trichosanthis Fructus with aspirin. The effects of pretreatment with Trichosanthis Fructus pellets,aspirin pellets and their combination on thromboxane B2(TXB2),6-keto prostaglandin F1α(6-keto-PGF1α) and cyclic adenosine monophosphate(c AMP) in rat thrombotic model were studied. Through the study of network pharmacology,12 components of aspirin and Trichosanthis Fructus,including hydroxygenkwanin,quercetin and adenosine,were found to show the anti-platelet aggregation and anti-thrombosis mechanisms through9 common protein targets,such as SRC,RAC1,MAPK14,MAPK1,AKT1,and 14 common signaling pathways,such as VEGF signaling pathway. After the intervention with Trichosanthis Fructus pellets combined with aspirin pellets,the vascular endothslia growth factor(VEGF) signaling pathway can be activated to inhibit platelet aggregation and improve vascular endothelial function,and show the anti-platelet aggregation and anti-thrombosis mechanisms,which verify the results of the network pharmacology,and explain the anti-platelet aggregation and anti-thrombotic mechanisms of the combination of Trichosanthis Fructus pellets with aspirin pellets.