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1.
Article in Chinese | WPRIM | ID: wpr-828940

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 , Chromatography, High Pressure Liquid , Delayed-Action Preparations , Male , Rats , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , Trichosanthes
2.
Article in Chinese | WPRIM | ID: wpr-845558

ABSTRACT

Objective To study the in situ intestinal absorption behaviors of 3, 29- dibenzoyl- karounitriol (DK) in Gualou- Xiebai (GX) extract in rats. Methods A rat in situ single-pass perfusion model was used and the concentrations of the perfusate were determined by HPLC-PDAD to investigate the intestinal absorption site and mechanism. Results The main absorption site of DK in GX extract was jejunum, ileum and colon, and the absorption had no significant difference in the three different segments of rat intestine (P>0.05), but was significantly higher than that in duodenum (P0.05). Conclusion DK in GX extract could be absorbed in whole intestinal segment, with the best intestinal absorption site of jejunum, ileum and colon. Its absorbing mechanism may be related to passive diffusion.

3.
Article in Chinese | WPRIM | ID: wpr-492724

ABSTRACT

Objective To study the in situ intestinal absorption behaviors of 3,29-dibenzoyl-karounitriol(DK)in Gualou-Xiebai(GX)extract in rats. Methods A rat in situ single-pass perfusion model was used and the concentrations of the perfusate were determined by HPLC-PDAD to investigate the intestinal absorption site and mechanism. Results The main absorption site of DK in GX extract was jejunum,ileum and colon,and the absorption had no significant difference in the three different segments of rat intes?tine(P>0.05),but was significantly higher than that in duodenum(P0.05). Conclusion DK in GX extract could be absorbed in whole intestinal segment,with the best intestinal absorption site of jejunum,ileum and colon. Its absorbing mechanism may be related to passive diffusion.

4.
Article in Chinese | WPRIM | ID: wpr-573049

ABSTRACT

shell of ST. Conclusion ST and stir-baked ST are better slices of prepared ST, the results are in an accordance with the status of ST in clinical application.

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