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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 develop a method of quantitative analysis of multi-components by single marker (QAMS) for six active ingredients in Gualoupi injection. Methods: An HPLC method was used with a Waters Sunfire ODS C18column (250 mm×4. 6mm, 2. 5 μm), the mobile phase was methanol(A)-0. 2% glacial acetic acid solution(B) with gradient elution, the flow rate was 1. 0 ml· min-1,the detection wavelength was 254 nm,the column temperature was 30℃ and the injection volume was 20 μl. Using 3, 29-dibenzoyl rarounitriol as a reference, the relative correction factors among karounidiol, vanillic acid, adenosine, quercitrin and cynaro-side were detected by QAMS and their contents were calculated, and the results were compared with those of the external standard method. Results: The differences were not statistically significant between the calculated values of karounidiol, vanillic acid, adeno-sine, quercitrin and cynaroside and those measured by the external standard method (P>0. 05). Conclusion: QAMS can be used for the determination of 6 effective components in Gualoupi injection, and the result is accurate, simple and effective.
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Objective To establish the HPLC multi-index quantitative fingerprints of Xiao’er Xiaoji Zhike Oral Liquid (XXZOL), and to provide methods and technical support for improving its quality standard. Methods Using an Agilent Zorbax SB-C18 (250 mm × 4.6 mm, 5.0 μm) column, acetonitrile-0.4% glacial acetic acid mobile phase system, gradient elution, flow rate of 0.6 mL/min, column temperature 25 ℃, detection wavelength 254 nm; The HPLC-ESI-Q-TOF/MS technique was used to identify the chemical constituents (peak 1-synephrine, peak 13-chlorogenic acid, peak 16-quercetin-3-O-β-D-glucose-7-O-β-D-gentiobioside, peak 22-hyperoside, peak 24-forsythoside A, peak 26-naringin, peak 27-hesperidin, peak 29-neohesperidin, peak 33-phillyrin, peak 37-3,29-dibenzoyl rarounitriol) in the XXZOL, and the content of the main components was determined by HPLC-DAD. The HPLC fingerprint was established on the basis of multi-batch analysis. Results The fingerprints of the 10 batches of samples were established, and the similarities of them were above 0.9, which were 0.999 3, 0.999 6, 0.999 2, 0.999 2, 0.999 4, 0.999 3, 0.999 4, 0.999 5, 0.999 1, and 0.999 7, respectively. XXZOL has 38 common peaks, 32 of them was identified, six of them was unknown; the contents of the 10 chemical constituents were 2 542.42, 158.61, 147.02, 34.35, 432.42, 1 813.01, 1 339.70, 2 580.71, 175.32, and 1 615.17 μg/mL. Conclusion The establishment of multi-index analysis by HPLC and fingerprints of XXZOL provides a scientific basis for improving its quality standards.
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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.
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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.
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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.