ABSTRACT
OBJECTIVE@#To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS).@*METHODS@#Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software.@*RESULTS@#LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05).@*CONCLUSIONS@#Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.
Subject(s)
Animals , Male , Rats , Chromatography, High Pressure Liquid , Delayed-Action Preparations , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , TrichosanthesABSTRACT
OBJECTIVE@#To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS).@*METHODS@#Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software.@*RESULTS@#LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05).@*CONCLUSIONS@#Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.
Subject(s)
Animals , Male , Rats , Area Under Curve , Benzoates , Pharmacokinetics , Chromatography, Liquid , Delayed-Action Preparations , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , Trichosanthes , ChemistryABSTRACT
The TNF-α signaling pathway is a valuable target in the therapy of autoimmune diseases.TNF-α binds to two different receptors and exerts anti-inflammatory and anti-rheumatic effects.The drugs of anti-TNF-α are widely used in rheumatoid arthritis, such as infliximab, adalimumab etc.These TNF blockers have become invaluable tools to reduce damages induced by inflammation and allow recovery of the affected tissues.Unfortunately, this therapy has some drawbacks, such as increasing the risk of infection, malignancy and the incidence rate of new auto-immune diseases.Some of these effects are caused by the unwanted abrogation of beneficial TNF signaling.Therefore, elective antagonism of TNFR is an important approach to alleviate the side effects of TNF-α antibody.The medications specifically targeting the TNFR might have better applicability and safety.In this article, research progresses of TNF-α and its receptors in the therapy of rheumatoid arthritis were reviewed.
ABSTRACT
Research on the inflammatory bowel disease(IBD) is a hot topic in the field of digestive system disease.IBD mainly consists of ulcerative colitis(UC) and Crohn′s disease(CD).The pathogenesis of IBD has not been fully understood.So far, there is no specific medication for IBD.A number of novel medicines and preparations have emerged with the research progress on the pathogenesis of IBD.The research status on IBD drug therapy is briefly reviewed in this paper.