Multicomponent determination of traditional Chinese medicine preparation yin-zhi-huang injection by LC-MS/MS for screening of its potential bioactive candidates using HepaRG cells.

Yin-zhi-huang (YZH) injection is an injectable multiherbal prescription derived from the ancient Chinese medicine formula of Yin-chen-hao-tang, which is widely used in the clinic for the treatment of jaundice and chronic liver diseases. To date, the systematic study of the components in this multiherbal prescription still lacks suitable analytical methods that are able to simultaneously detect a broad array of components at low concentrations. In this study, a new liquid chromatography-tandem mass spectrometry method using dynamic multiple reaction monitoring mode was developed to determine multiple peaks in traditional Chinese medicine preparation YZH injection. This simple, selective and sensitive method enabled the quantification of 22 components with standard materials with a lower limit of quantification of 1.46-12.5 ng/mL in cell lysates. This method was successfully applied to celluar uptake and binding investigation of components in YZH injection. The results indicated that this strategy might be a useful approach for rapidly screening of the potential bioactive candidates from YZH injection, and the discovered candidates could be used to investigate the pharmacodynamics in further studies.

Development of a LC-MS/MS method for simultaneous determination of metoprolol and its metabolites, α-hydroxymetoprolol and O-desmethylmetoprolol, in rat plasma: application to the herb-drug interaction study of metoprolol and breviscapine.

A simple, specific and sensitive LC-MS/MS method was developed and validated for the simultaneous determination of metoprolol (MET), α-hydroxymetoprolol (HMT) and O-desmethylmetoprolol (DMT) in rat plasma. The plasma samples were prepared by protein precipitation, then the separation of the analytes was performed on an Agilent HC-C18 column (4.6 × 250 mm, 5 µm) at a flow rate of 1.0 mL/min, and post-column splitting (1:4) was used to give optimal interface flow rates (0.2 mL/min) for MS detection; the total run time was 8.5 min. Mass spectrometric detection was achieved using a triple-quadrupole mass spectrometer equipped with an electrospray source interface in positive ionization mode. The method was fully validated in terms of selectivity, linearity, accuracy, precision, stability, matrix effect and recovery over a concentration range of 3.42-7000 ng/mL for MET, 2.05-4200 ng/mL for HMT and 1.95-4000 ng/mL for DMT. The analytical method was successfully applied to herb-drug interaction study of MET and breviscapine after administration of breviscapine (12.5 mg/kg) and MET (40 mg/kg). The results suggested that breviscapine have negligible effect on pharmacokinetics of MET in rats; the information may be beneficial for the application of breviscapine in combination with MET in clinical therapy.

[Improvement in blood glucose fluctuations of insulin-treated type 1 diabetic patients with additional use of acarbose and assessed by continuous blood glucose monitoring program].

OBJECTIVE: To investigate the effect of combined use of insulin and acarbose on glucose excursion in type 1 diabetic patients. METHODS: 120 cases were randomly divided into control group and observation group. The control group received preprandial ultra-short effect insulin and long-acting insulin before bedtime while the observation group received acarbose 50 mg added to the medicine taken by the control group. Continuous Glucose Monitoring System (CGMS) was used to watch the blood glucose fluctuations. Data related to blood glucose level, glucose excursions after meals and hypoglycemia at night were compared between patients in the two groups. RESULTS: The average blood glucose (9.37 ± 1.70) mmol/L, the largest amplitude of glycemic excursions (LAGE) (11.42 ± 2.73) mmol/L, hyperglycemia-area under curve 0.89 ± 0.54, mean amplitude of glycemic excursions (MAGE) (5.13 ± 2.23) mmol/L, M-value (18.93 ± 11.43) mmol/L and insulin dosage (42.11 ± 14.42) U/day of observation group were significantly lower than in the control group (P < 0.05). Glucose excursions after meals and the times (0.33 ± 0.50)/day, the maintenance time (43.75 ± 43.50)/min and low glycemic index (LBGI) (0.005 ± 0.002) mmol/L of hypoglycemia at night were also significantly lower than in the control group, with statistically significant (P < 0.05) differences. CONCLUSION: The blood glucose fluctuation was significantly improved, with the decrease of insulin dosage while both glucose excursions and hypoglycemia at night reduced in patients with type1 diabetes mellitus after the acarbose treatment.We suggested that this program deserve further observation.