Bioequivalence of rosuvastatin calcium tablets in Chinese healthy subjects / 中国临床药理学与治疗学

AIM: To study the bioequivalence of rosuvastatin calcium tablets produced by two different manufacturers on a fasting and postprandial basis in Chinese healthy subjects. METHODS: A single-center, randomized, balanced, open, two-sequence, two-cycle, double-crossover, and single-dose trial design was used in this study. Each of the fasting group and the postprandial group was enrolled in 52 healthy subjects. Fasting/postprandial oral rosuvastatin calcium tablets 10 mg test preparation or reference preparation, the validated LC-MS/MS method was used to determine the concentration of rosuvastatin calcium tablets in plasma, and the pharmacokinetic parameters were calculated. Human bioequivalence and safety evaluation of two rosuvastatin calcium tablets were evaluated. RESULTS: The t

Preparation and Quality Evaluation of Formononetin Inclusion Compound Liposome / 中国药房

OBJECTIVE: To prepare Formononetin (FMN) inclusion compound liposome and evaluate its quality. METHODS: FMN inclusion compound liposome was prepared by film dispersion method. The morphology, particle size, Zeta potential, encapsulation efficiency and in vitro release properties were studied. RESULTS: The particle size, Zeta potential and encapsulation efficiency of prepared FMN inclusion compound liposome were (255. 34 ± 12. 87) nm, (25. 32 ± 3. 51) mV, (81. 63 ± 0. 79)％, respectively (n=3). The 24 h accumulative release rate of prepared FMN inclusion compound liposome was 56. 12％. CONCLUSIONS: FMN inclusion compound liposome with good sustained-release effect is prepared successfully and in line with related quality standard.

Pharmacokinetics of nicotine in blood and brain using microdialysis and stable labelled isotope / 中国中药杂志

<p><b>OBJECTIVE</b>Using the stable isotopes as the internal standard of microdialysis technology to establish a new method to study the whole and local brain dynamics of nicotine percutaneous preparations.</p><p><b>METHOD</b>Using th healthy rats as experimental animals, administrating nicotine in abdominal transdermal way, then sample in the blood and brain simultaneously by microdialysis which use deuterium nicotine (DL-nicotine) as internal standard. Detecting the samples by LC-MS/MS method.</p><p><b>RESULT</b>The configuration process in blood and brain both conforms to 2 compartments model, t1/2 is 29.38 min, t1/2beta is 208.51 min, AUC(0-infinity) is 152 127.10 microg x min x L(-1) in the blood t1/2 is 86.64 min, t1/2beta is 386.00 min, AUC(0-infinity) is 152 820.90 microg x min x L(-1) in the brain.</p><p><b>CONCLUSION</b>Dl-nicotine can be used as internal standard of nicotine to correcte the recovery; Stable isotopes internal standard microdialysis technology can be used for studing the whole and the local pharmacokinetic of nicotine and also provide new ideas and methods to studing the process of new drug delivery system.</p>

Effect of sodium aescinate on oxidative stress and pulmonary function during acute exacerbation of chronic obstructive pulmonary disease / 中国综合临床

Objective To investigate the effects of sodium aescinate(SA)on oxidative stress and pulmonary function during acute exacerbation of chronic obstructive pulmonary disease(COPD).Methods One hundred and twenty patients with COPD were randomly divided into two groups:the control group(n =60) and the treatment group(n =60).All patients were treated with routine anti-infection,oxygen inhalation,relieving phlegm and anti-asthma The treatment group took SA in addition to the routine beteropathy.The changes of serum SOD,MDA,GSH-Px,T-AOC,pulmonary functions and 6 minute walk distance(6MWD) were detected before and after two-week treatment in patients of the two groups to compare with 60 healthy subjects.Results The total effective rate in the treatment group was 91.67％,while 76.67％ in the control group.The difference was statistically significant(x2 =5.065,P ＜0.05).Serum MDA level in both groups were comparatively higher than the healthy controls(9.25±1.55) μmol/L vs.(9.74±1.50) μmol/L vs.(2.06±0.29) μmol/L,P ＜0.001),while the levels of SOD,GSH-Px and T-AOC were lower than the healthy controls[SOD:(91.14±9.54) kU/L vs.(90.61±8.01) kU/L vs.(116.63±6.57) kU/L; GSH-Px:(139.38±36.56) U vs.(137.57±34.19) U/L vs.(189.34±35.54) U/L; T-AOC:(6.48±1.15) kU/L vs.(6.39±1.13) kU/L vs.(13.34±1.23)kU/L;P < 0.001].After treatment,all indexes of the two groups were obviously ameliorated in comparison with before treatment(P ＜ 0.001),but the level of MDA[(4.56±1.39) μmol/L]in the treatment group decreased more greatly than in the control groups(P ＜ 0.001).The levels of SOD[(103.85±7.07) kU/L],GSH-Px[(169.65±34.51) U/L],T-AOC[(10.52±1.09) KU/L],forced expiratory volume in 1 second/forced vital capacity(FEV1/FVC)[(60.49±6.11)％],FEVI％[(76.62±6.35)％]and 6MWD [(394.83±10.11)m]increased considerably more than those in the control group(P ＜ 0.001).Conclusion Oxidative stress might be involved in the course of acute exacerbation of COPD.Sodium aeseinate can improve the pulmonary functions by ameliorating the oxidative stress during acute exacerbation in patients with COPD.

Study of pharmacokinetics of nicotine in local brain by using microdialysis and stable labeled isotope / 药学学报

The paper is to report the study of pharmacokinetics of transdermal administered nicotine in the brain of freely moving rat by using microdialysis with stable labeled isotope as internal standard. The pharmacokinetic behavior of nicotine in Sprague Dawley rat brain was investigated after intranasal administration (3.75 mg). Brain fluid samples were collected by intracerebral microdialysis with DL-nicotine as internal standard. Concentrations of nicotine and DL-nicotine in the sample were measured by HPLC-MS/MS. Main pharmacokinetic parameters were calculated and analyzed by Das 2.0 pharmacokinetic software. The recovery of nicotine and the delivery of DL-nicotine were the same. The fate of absorption and distribution was two compartment model and the values of t1/2alpha was 170.31 min, t1/2beta was 263.30 min and the AUC(0-infinity) was 2.75 x 10(5) microg x L(-1) min separately. DL-nicotine can be used to calibrate the recovery of nicotine, and the new method of stable isotope microdialysis can be used to study the pharmacokinetics of freely moving rat. It will make sense for the treatment of addiction of tobacco and provide a new thought for the research of pharmacokinetics-pharmacodynamic combination.

Study on in vitro microdialysis recovery of Shuanghuanglian / 中国中药杂志

<p><b>OBJECTIVE</b>To explore the feasibility of microdialysis techniqiue to be used in pharmacokinetic study of Chinese medicine, taking Shuanghuanglian as a model drug.</p><p><b>METHOD</b>The samples were obtained by retrodialysis, determined by HPLC gradient elution to calculate the in vitro recovery rate (RR) of specific components. To study the difference of RR of a certain component in different dialysis mediums, and the effect of flow rates and concentration on RR.</p><p><b>RESULT</b>Along with the increase of number of substances in the dialysis medium, the RR of specific components reduced. But the RR was independent of the concentration of the component in the dialysis medium. The RR reduced with the increasing flow rate in the same dialysis medium.</p><p><b>CONCLUSION</b>The microdialysis technique can be used in pharmacokinetics study of Chinese medicine.</p>

Serum Pharmacochemistry and Pharmarcokinetics Study of Naoxuening Injection / 中药新药与临床药理

Objective To study the serum pharmacochemistry and pharmacokinetics of Naoxuening Injection(NXI).Methods Based on the established HPLC fingerprint of NXI,analysis and comparison were carried out among the HPLC profiles of NXI,blank plasma and human serum samples obtained after intravenous administration of NXI.and the main compounds were identified and then the pharmacokinetics of the main compounds were studied.Results Three compounds were i- dentified from the serum after intravenous administration of NXI.Two were the compounds containing in NXI,which were named after geniposide and paeonol,respectively.The other one was identified as metabolic product.The concentration- time curve of geniposide in blood accorded with one-compartment model of pharmacokinetics,and 70 % of geniposie was cleared from the kidney.The concentration-time curve of paenol in blood accorded with two - compartment model of pharmacoki- netics,and 0.04 % of geniposie was cleared from the kidney.Conclusion The compounds contained in the blood and their metabolites are the effective constituents,and the further serum pharmacochemical research will be beneficial to the pharmacol- ogy and the therapeutic mechanism of of NXI.