摘要：Ahn To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved liquid-liquid extraction, separation on a CN column and ultraviolet detection at 310 ran with granisetron as an internal standard. pharmacokinetics and bioequivalence of ondansetron in orally disintegrating tablets by direct compression and conventional 8 mg tablets were evaluated and compared in 20 healthy human male volunteers after a single oral dose in a randomized cross-over study. Results The limit of quantification was 0.25 ng· mL^-1. The recovery was about 85 % or over for ondan setron and about 90% for internal standard. Linearity was good within the concentration range of 0.5 - 50 ng·mL^-1 with r^2 ranging from 0.997 1 to 0.999 9. Intra- and inter-assay coefficients of variation ranged from 1.78% to 2.38% and 3.88% -5.19%, respectively. Accuracies for spiked concentrations of 2.0, 10.0, and 30.0 ng·mL^-1 were 104.7% ±4.4%, 102.2% ± 1.1%, and99.51% ±2.34%, respectively. Pharmacokinetic parameters of AUCo-t, AUCo-∞ , Cmax, Tmax, and T1/2 were 230.2 ± 78.0 ng·h·L^-1 , 265.2± 101.5 ng·h·mL^-1, 35.67 ± 8.94 ng·mL^-l, 1.51 ±0.79 h, and 5.00± 1.41 h for orally disintegrating tablets, respectively. The analysis of variance did not show any significant difference between orally disintegrating tablets and conventional tablets, and 90% confidence intervals fell within the acceptable range for bioequivalence. Conclusion High resolution HPLC method has been set up and applied in pharmacokinetic evaluation of ondansetron in orally disintegrating tablets.

摘要：pH-sensitive smart polymeric nanocarriers have been under development in the field ofbiomedicine due to permeabilization the physiological barriers readily to address the limitation of conventional chemotherapeutics delivery systems of low intracellular transport and targeting *** traditional polymers kept stable under physiological neutral or acidic conditions,pH-sensitive polymeric nanocarriers underwent rapid degradation with a labile group in tumor acidic environment(around 5.0-6.0),allowing these biomaterials to achieve controlled drug release,drug pharmacokinetics improvement and antitumor biotherapeutic molecules efficiency enhancement compared with traditional *** review mainly concentrated on properties of pH-sensitive polymers for biomedical purposes to construct the smart drug delivery system based on acid liable linkers which were categorized into pH-sensitive polymeric prodrugs composed of antitumor drugs(doxorubicin and paclitaxel)bounded to the polymer via acid liable linkers and pH-sensitive copolymeric nanocarriers prepared by block copolymers containing polymer blocks linked with acid-cleavable ***,advanced platforms in biomedicine for special biotherapeutic molecules delivery were reviewed in the ***,several acid-sensitive linkages were reviewed to study the mechanism of the controlled pH-responsive drug delivery,such as hydrazone,acetal,cis-aconityl linker and β-thioether ester,as well as improvement of drug pharmacokinetics.

摘要：It was recently revealed that Rhynchophylline （Rhy）, an important constituent of Uncaria rhynchophylla, possessed antihypertensive and neuroprotective effects. However, no information about the pharmacoldnetics of Rhy in a herbivorous species such as rabbit is available. Allometric scaling is valuable in designing human pharmacokinetic parameters from preclinical species. To investigate the characteristics of Rhy in vivo, a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry （UPLC-MS/MS） method was developed and validated for the measurement of Rhy concentrations in rabbit plasma. The method was linear over the concentration range of 0.01-10.24 μg/mL. Intra-day and inter-day precision and accuracy were less than 8.0%. The recoveries were in the range of 94.17%-103.32%. Matrix effects （ME） were minor. After oral administration of Rhy at 20, 40 and 80 mg/kg, the mean elimination half-life （h/E） for these doses were 1.19, 1.49 and 1.37 h in rabbits, respectively. There was a proportionate increase in the maximum concentration （Cmax） and the area under the blood concentration-time curve （AUC∞） for three doses. The developed method was suitable for the study on pharmacokinetics of Rhy after oral administration and it may provide a valuable basis for clinical application of such a bioactive compound of herbal medicines.

摘要：This review is intended to help clinicians design drug regimens for special populations of critically ill patients with extremes of body size, habitus and composition that make drug choice or dosing particularly challenging due to the lack of high-level evidence on which to make wellinformed clinical decisions. The data sources included a literature search of MEDLINE and EMBASE with reviews of reference lists of retrieved articles. Abstracts of original research investigations and review papers were reviewed for their relevance to drug choice or dosing in the following special critically ill populations: patients with more severeforms of bodyweight or height, patients with amputations or missing limbs, pregnant patients, and patients undergoing extracorporeal membrane oxygenation or plasma exchange. Relevant papers were retrieved and evaluated, and their associated reference lists were reviewed for citations that may have been missed through the electronic search strategy. Relevant original research investigations and review papers that could be used to formulate general principles for drug choice or dosing in special populations of critically ill patients were extracted. Randomized studies with clinically relevant endpoints were not available for performing quantitative analyses. Critically ill patients with changes in body size, habitus and composition require special consideration when designing medication regimens, but there is a paucity of literature on which to make drug-specific, high-level evidencebased recommendations. Based on the evidence that is available, general recommendations are provided for drug choice or dosing in special critically ill populations.

摘要：Artemisinin（ART） is a widely used active drug for malaria, including severe and cerebral malaria. However, its therapeutic efficacy is affected by its lower bioavailability. In the present study, nanostructured lipid carriers（NLCs） were proposed as carrier of ART to improve pharmacokinetic properties of the drug. ART-NLC was prepared by high-pressure homogenization based on orthogonal design. The particle size, zeta potential, encapsulation efficiency（EE） and percentage of drug loading（DL） of ART-NLC were（53.06±2.11） nm,（–28.7±3.59） m V, 73.9%±0.5% and 11.23%±0.37%, respectively. ART-NLC showed the sustained release characteristics and scarcely the hemolysis effect on human red blood cells. The pharmacokinetics of ART-NLC for rats after tail intravenous injection（i.v） or intraperitoneal injection（i.p） were investigated by liquid chromatography-tandem mass spectroscopy（LC-MS/MS）. And ART solution was designed as control preparation. For rats of i.v groups, the AUC0–∞（（707.45±145.65） ng·h/m L） of ART-NLC were significantly bigger than that of ART（（368.98±139.58） ng·h/m L）. The MRT（（3.38±0.46） h） of ART-NLC was longer than that of ART（（1.39±0.61） h）. And similar results were observed for rats of i.p groups. The AUC0–∞（（1233.06±235.57） ng·h/m L） and MRT（（4.97±0.69） h） of ART-NLC were both bigger than those of ART, which were（871.17±234.03） ng·h/m L） and（1.75±0.31） h）, respectively. Compared with ART, ART-NLC showed a significant increase in AUC0–∞（P〈0.05） and MRT（P〈0.001） for both i.p and tail i.v administrations.

摘要：Aim To prepare a self-emulsifying microemulsion of 9-nitrocamptothecin （9-NC ME） for intravenous injection and investi- gation of its pharmacokinetic profiles in normal SD rats. Methods 9-NC ME was optimized in terms of droplet size and lack of drug precipitation following aqueous dilution using a pseudo-ternary phase diagram. Physicochemical properties of 9-NC ME were evaluated. 9-NC ME was intravenously administered via tail vein in healthy rats. Results A stable microemulsion was formulated consisted of soybean oil as oil phase, EPC/Tween-80 as emulsifier, and anhydrous ethanol as co-emulsifier. The droplets of the microemulsion were spherical shape with mean diameter of 38.3 ± 4.0 nm after 1：20 dilution with 5% glucose injection. The pharmacokinetic parameters of 9-NC ME after intravenous administration in rats were t1/2 of 0.97 ± 0.14 h, A UC0-8 of 372.77 ±49.62 ng·h·mL^-1 and MRT of 1.40 ± 0.21 h which were 1.4-fold, 1.65-fold, and 1.4-fold more than those of 9-NC solution （P〈0.01）. Conclusion The results suggested that 9-NC ME was a promising drug delivery system and it was expected to provide a novel 9-NC injection for cancer patients.

摘要：Aim To establish a HPLC method for the determination of bicalutamide plasma concentration and to evaluate the bioequivalence of bicalutamide capsules （test） and tablets （reference）. Methods A single oral dose of 50 mg bicalutamide capsules or tablets were given to 48 Chinese healthy volunteers in a one period parallel design test. Bicalutamide in plasma was analyzed using a XB-C18 column with a mobile phase of acetonitrile-water （60：40, V/V） and the dectection wavelength of 272 nm and it is pharmacokinetic parameters were calculated and evaluated using DAS2.0. Results The linear range of bicalutamide was 10 - 1200 ng·mL^-1. The main pharmacokinetic parameters of the test and reference were as the followings, t1/2 （138.36 ± 32.03） and （146.12 ± 27.04） h, Tmax （17.17 ± 4.65） and （16.92 ± 4.85） h, Cmax（910.83 ± 130.49） and （868.71 ± 115.35） ng·mL^-1 AUC0-672（172437.08 ± 3986.07） and （176842.34 ± 35733.85） ng·mL^-1·h, and AUC0-∞ （179456.55 ± 43127.65） and （185270.39 ± 39688.63） ng·mL^-1·h, respectively. The two-one side t-test analysis showed that the confidence intervals of Crux, A UC0-672 and A UC0-∞ were （98.9% - 100.7%）, （98.8% - 100.6%） and （99.7% - 101.7%）, respectively. Conclusion The relative bioavailability of bicalutamide capsules was 97.51%. The bioequivalence was demonstrated by the two-one side t-test

摘要：Aim To develop a sensitive and accurate HPLC method for the determination of fleroxacin in human plasma, and study its pharmacokinetics in healthy subjects. Methods The analytes were isolated fi＇om plasma by simple protein precipitation with methanol, separated on a Diamonsil C18 column by isocratic elution with the mobile phase consisted of 1% triethylamine at pH 4.8 （adjusted with phosphoric acid） and acetonitrile （80/20, V/V） at a flow rate of 1.0 ***^-1 and analyzed by fluorescence detector with an excitation at 290 nm and emission 458 nm. The pharmacokinetic study of fleroxacin was performed according to a double period crossover design. Results The weighted （1/x） calibration curve was linear over the plasma concentration range of 0.025 - 8.00 μ***^-1 The inter- and intra-day precisions （RSD/%） were no more than 5.16%, and the method accuracies and extraction recoveries at three concentrations ranged firom 99.1% to 100.9%, and 86.7% to 92.0%, respectively. Following oral administration at a dose of 400 mg fleroxacin, the main pharmacokinetic parameters for test and reference capsules were Cmax5.08 ± 0.78 and 5.38 ± 1.40 μ***^-1, tmax 1.72 ±0.79 and 1.82 ± 0.78 h, t1/2 11.68 ± 1.27 and 11.38 ± 1.51 h^-1, AUC0-∞ 78.44 ± 11.44 and 76.53 ± 13.24 μ***^-1.h, respectively. Conclusion The method is sensitive and accurate, and suitable for human pharmacokinetic study of fleroxacin.