Simultaneous determination of four components of Shuganning Injection in rat plasma by UPLC-MS/MS and its application to a pharmacokinetic study / 中国中药杂志

This study aims to reveal the pharmacokinetics of Shuganning Injection in normal rats. In this experiment,ultra-high performance liquid chromatography-electrospray-tandem mass spectrometry( UPLC-ESI-MS/MS) was used to establish an analytical method for simultaneous determination of chlorogenic acid,gardenioside,oroxylin A and baicalin in rat plasma. Then,the non-compartmental model( NCA) in Phoenix WinN onL in 6. 4 software was used to fit pharmacokinetic parameters. The methodological validation showed that the linear relationship of the components in rat plasma samples were good( r>0. 995). The recovery rate and matrix effect of plasma samples with low,middle and high concentration were 79. 14%-101. 4%. The intra-day and inter-day precision,accuracy and stability meet the requirements of biological sample analysis. The half-life( t1/2) of chlorogenic acid,gardenioside,oroxylin A did not change significantly and the area under blood concentration-time curve( AUC0-t) is proportional to the dose,which suggested that three components showed a linear kinetic characteristics,but baicalin showed nonlinear kinetic characteristics. Moreover,the retention time of each component in rats was short. The established UPLC-MS/MS quantitative analysis method is rapid,sensitive and accurate,which can be used for the determination of chlorogenic acid,gardenioside,oroxylin A and baicalin in rat plasma and pharmacokinetic study of Shuganning Injection.

The Economic Evaluation of Three Kinds of Angiotensin Ⅱ Receptor Blockers in Stroke and Myocardial Infarction Prevention among Hypertension Patients Using Markov Model / 中国药学杂志

OBJECTIVE:To investigate the long-term economic consequences of candesartan cilexetilirbesartan and telmisartan in preventing stroke and myocardial infarction (MI) among hypertension patients using Markov model, to offer the reference for hypertension intervention. METHODS:A Markov state transition model was built based on the natural history of hypertension from the societal perspective to estimate the expected health care costs and the quality adjusted life years. Meanwhile, the incremental cost-effectiveness ratio was obtained. One year cycle length and 20 years horizon were adopted. The 5% yearly discount rate was applied to both health care costs and QALYs. One-way sensitivity analysis, second-order Monte-Carlo and probabilistic sensitivity analysis were performed. RESULTS:Candesartan cilexetil was at an absolute disadvantage because of the highest cost and the lowest effect in the baseline analysis. The incremental cost-effectiveness ratio for irbesartan versus telmisartan was 5 799.67 yuan/QALY. The sensitivity analysis was consistent with the baseline results. CONCLUSION:Irbesartan shows significant economic advantage at the threshold of 49 992 yuan/QALY compared with telmisartan. And candesartan cilexetil is with less economical.

Synthesis and animal imaging of 99mTc-hydrazinonicotinamide-folate as a new folate receptor-targeted tumor imaging agent / 中国医学科学院学报

<p><b>OBJECTIVE</b>The synthesis, biodistribution, and animal imaging of 99mTc- hydrazinonicotinamide-folate (99mTc-HYNIC-Folate) were studied as a folate receptor-targeted tumor imaging agent.</p><p><b>METHODS</b>HYNIC-Folate was synthesized by a muti-step reaction and radiolabeled with 99mTc using tricine and trisodium phenylphosphine-3, 3', 3"-trisulfonate (TPPTS) as coligands. The radiochemical purity and stability of 99mTc HYNIC-Folate was measured. The biodistributions of 99mTc-HYNIC-Folate in normal mice and tumor-bearing mice were detected. Whole-body gamma imaging was performed using an athymic mouse tumor xenograft model.</p><p><b>RESULTS</b>The ligand HYNIC-Folate was successfully synthesized and characterized by hydrogen nuclear magnetic resonance (1HNMR) and mass spectrometry (MS). The radiochemical purity of 99mTc-HYNIC-Folate was 96% under optimal conditions. Data from gamma scintigraphy and the biodistribution in tumor-bearing mice showed that 99mTc-HYNIC-Folate predominantly accumulated in tumor, its uptake rate per gram tissue alpham was 5. 620+/- 0. 753. The uptakes of 99mTc-HYNIC-Folate in the other non-target tissues were very low, except it was high in the kidneys ( am was 41. 959 +/-6. 759) .</p><p><b>CONCLUSION</b>99mTc-HYNIC-Folate has the potential to be used as a noninvasive radiodiagnostic imaging agent for the detection of folate receptor-positive human cancers.</p>