ABSTRACTObjectiveTo investigate the pharmacokinetics of flupirtine maleate in Chinese Korean and Han healthy volunteers. MethodsTen Chinese Korean and 10 Han volunteers （the ratio of male:female at 1：1) were enrolled in this study. Each subject received a single oral dose （100 mg) of flupirtine maleate respectively. Blood samples were determined by HPLCfluorescence method and the pharmacokinetic parameters were calculated by Das Ver 2.0 software. ResultsThe main pharmacokinetic parameters of Chinese Korean and Han were as follows: t1/2 （7.72±0.85) and （8.85±2.15) h；tmax （2.35±2.06) and （1.70±0.79) h；Cmax（1 012.73±376.16) and （1 078.09±296.74) μg·L－1；AUC036 （8 552.69±1 773.64) and （8 406.24±1 622.5) μg·L－1·h；AUC0∞ （8 914.96±1 890.04) and （8 971.71±1 996.53) μg·L－1·h，respectively. ConclusionThe pharmacokinetic parameters obtained from our study showed no significant difference between Chinaese Korean and Han （P＞0.05).
ABSTRACTObjectiveTo observe the protective effects of Lcarnitine （LCN) preconditioning on rat hearts with cold preservation in St.Thomas No.2 solution ex vivo.MethodsIsolated rat heart Langendorff model was established.Twentyfour male SpragueDawley rats were randomly divided into three groups （8 rats in each group): Sham group，the hearts were not arrested；I/R group and LCN preconditioning group，in which the rats were intraperitoneally injected with distilled water or LCN for 5 days respectively，and then the hearts were preserved in St.Thomas No.2 solution ex vivo for 4 h.The recovery of myocardial function，heart resuscitation time，malonyldialdehyde （MDA) and wet weight in myocardium were analyzed.ResultsAfter the hearts were preserved for 4 h，there were no differences in the heart resuscitation time between I/R group and LCN preconditioning group［（71.24±10.48) s vs.（69.42±9.49) s］，but LCN preconditioning group showed a better recovery of myocardial function，a lower release of MDA［（2.71±0.39) nmol·mg－1 vs.（3.57±0.47) nmol·mg－1］ （P＜0.05)，and the less wet weight in myocardium［（69.27±6.52)% vs.（79.42±5.93)%］ （P＜0.05) than that in I/R group.ConclusionLCN preconditioning exerts myocardial protective effects on the hypothermic preservative rat hearts ex vivo.
ABSTRACTObjectiveTo study the efficacy and toxicity of concurrent chemotherapy［nedaplatin （NDP) and cisplatin （DDP)］ and radiotherapy in the treatment of localadvanced head and neck squamous carcinoma. MethodsA total of 52 patients with localadvanced head and neck squamous carcinoma were randomized into NDP group （n＝26) and the DDP group （n＝26). The two groups of patients received five courses of chemotherapy during their radiotherapy. Chemotherapy regimens were as follows: NDP 40 mg·（m2）－1 once a week and DDP 40 mg·（m2）－1 once a week. Radiotherapy was as follow: all patients received intensity modulated radiation therapy （IMRT). The doses of radiation on primary tumor and lymphatic gland were (72－74) Gy/33f and (66－70) Gy/33f，respectively. The prophylactic dose of neck was (50－56) Gy/28f.ResultsThe effective rate of NDP and DDP was 92.3% and 88.5%，respectively （P＞0.05). Vomiting rate was significantly lower in NDP group （65.4%) than DDP group （92.3%) （P＜0.05). There was no significant difference between the two groups in the incidence of leukopenia （73.1% vs. 88.5%) and reaction rate of hemoglopenia （65.4% vs. 73.1%). There was a significantly higher incidence rate of thrombocytopenia in NDP group （92.3%) than in DDP group （50.0%) （P＜0.05). ConclusionThere is no significant difference between NDP and DDP regimens，and the NDP group has a lower digestive reaction rate than DDP group. The main adverse reaction of NDP regimens is myelosuppression，especially thrombocytopenia.
ABSTRACTObjectiveTo observe the effect of bailing capsule in combination with irbesartan on treating patients with proteinuria after renal transplantation. MethodsA total of 56 patients were randomized into 2 groups: control group （n＝26) and treatment group （n＝30). In the control group，the patients were treated with irbesartan 150 mg daily；the patients in the treatment group were administered with bailing capsule 1.0 g，three times a day. Six months later，amount of 24 h proteinuria，blood routine，urine routine and renal function （blood urine nitrogen，creatinine) were detected，and the ultrasonography examination of the renal allograft was carried out. The side effects of the drugs were documented. ResultsIn the control group，the total effective rate of the control group and the treatment group was 84.6% and 93.3%，respectively （P＜0.05). After 6 months，the amounts of 24 h proteinuria in both groups were decreased significantly （P＜0.05)；the amount of 24 h proteinuria was decreased more significantly in the treatment group than in the control group （P＜0.05). No apparent side effect was observed. ConclusionBailing capsule in combination with irbesartan could reduce the proteinuria of patients with renal allograft，with better result than single use of irbesartan，without significant side effect.
ABSTRACTObjectiveTo prepare and optimize the formulation of flupritine maleate orally disintegrating tablets. MethodsThe formulation was optimized with an orthogonal design according to disintegrating time in vitro and dissolution. Filter paper test was designed to evaluate disintegration time of tablets. The disintegration time of the orally disintegrating tablets in vitro was compared with the disintegration time in mouth and that detected by the common method.ResultsThe taste of tablets were desirable. The tablets were disintegrated within 34 s in mouth，31 s by the filter paper test and 8.5 s by the common method. ConclusionThe formulation of flupritine maleate orally disintegrating tablets was reasonable. The design can closely estimate the disintegration time of orally disintegrating tablets.
ABSTRACTObjectiveTo prepare fanjiao ointment and to study its release behavior in vitro.MethodsThe release behavior in vitro of fanjiao ointment was tested by bag filter with anhydrous dextrose as a blank control，bletillae rhizome polysaccharide as an index，sodium chloride as a delivery mediator，0.2% anthronesulfuric acid as stain. ResultsThe cumulative release rate of fanjiao ointment within 4 h was 61.8%，the drug release rate after 4 h was 38.2%，and the cumulative release rate within 48 h was 97.8%.ConclusionThe method to study the release of fanjiao ointment is convenient，stable and reliable.
ABSTRACTObjectiveTo establish a high performance liquid chromatography （HPLC) method for quantitative determination of fluticasone propionate in percutaneous solution，and investigate the ability of percutaneous penetration of fluticasone propionate cream.MethodsHypersil ODS C18 column （250 mm×4.6 mm，5 μm) was used. Mobile phase was as follows: methanol1.15 g·L－1 ammonium dihydrogen phosphate （adjusted to pH 3.5)acetonitrile （55：35：15 in volume). The column temperature was set at 55 ℃. The flow rate was 1.0 mL·min－1. The detection wavelength was 240 nm. Improved Franz type diffusion cells were used in vitro permeation studies and excised minipig’s skins in vitro were used as a transdermal barrier. The concentration of fluticasone propionate in the receptor solution was determined by HPLC to investigate its cumulative permeation quantities at different time points respectively，which were compared with those of the commercial cream. ResultsThe regression equation of penciclovir was linear in the range of 0.050 2－1.003 0 μg·mL－1 （A＝47 709.364 7×C＋300.774 4，r＝0.999 8). The average recovery was 99.58%. A good linear relationship existed between the cumulative penetration quantities and the time. There was no significant difference in the skin permeation quantities between the selfmade cream and commercial cream. ConclusionThe method was simple，rapid，and accurate. It is a better method to evaluate the characteristics of permeation for fluticasone propionate.
ABSTRACTObjectiveTo establish an HPLC method for determination of verticinone and cholic acid in verticinonecholic acid salt. MethodsThe separation was performed on a C18 column （250 mm×4.6 mm，5 μm). The mobile phase was methanol : ammonium acetate （0.1 mol·L－1) : triethylamine : ethanoic acid （78：22：0.2：0.03). The flow rate was 1 mL·min－1. The gas flow rate of ELSD was 2 mL·min－1 and the temperature of drift tube was 72.1 ℃. ResultsThe linear ranges of verticinone and cholic acid were 50.4－151.1 μg·mL－1 （r＝0.999 6，n＝5) and 50.5－151.4 μg·mL－1 （r＝0.999 9，n＝5) respectively. The average recoveries of the two components were 99.37% （RSD＝0.63%，n＝9) and 99.17% （RSD＝0.62%，n＝9) respectively. ConclusionThe method is simple and reliable for the quality control of verticinone and cholicacid salt.
ABSTRACTObjectiveTo establish a high performance liquid chromatography method for the determination of psoralen and isopsoralen in fructus psoraleae microemulsion. MethodsThe assay was performed on a Kromasil C18 column using methanol0.6% acetic acid （50:50) as mobile phase and the detection wavelength was 246 nm. ResultsThe liner calibration curve of psoralen was obtained in a range of 4.24－50.88 μg·mL－1 with an average recovery of 99.3% （RSD＝1.51%). The liner calibration curve of isopsoralen was obtained in the range of 4.48－53.76 μg·mL－1 with an average recovery of 98.6% （RSD＝1.65%). ConclusionThe method is simple and reproducible. It can be used for the determination of psoralen and isopsoralen in fructus psoraleae microemulsion.
ABSTRACTObjectiveTo establish a quantitative method for detecting 16 amino acids in cordyceps mycelium powder. MethodsThe sample was hydrolyzed for 24 h at 110 ℃，and derived with phenyl isothiocyanate （PITC)，with norleucine serving as an internal standard. High performance liquid chromatography （HPLC) was performed on a Agela Venusil XBP C18 （150 mm×4.6 mm，5 μm) column with gradient elution of 0.1 mol·L－1 acetic acidsodium acetate buffer solution （pH 6.5)acetonitrile （95：5) （A) and acetonitrilewater （4：1) （B) at a flow rate of 1.0 mL·min－1，detected at 254 nm. ResultsSixteen amino acids had a good linearity in the range of 1.81－7.50 μg·mL－1 （r＝0.998 3－1.000 0). The average recoveries were 95.3%–104.1%，except His 92.9 %，Met 90.6%，and RSD less than 2.0%，except His 2.8% and Met 3.3%.ConclusionThe method is sensitive and accurate with high repeatability and stability，and is helpful for the determination of amino acids in cordyceps mycelium powder.
ABSTRACTObjectiveTo approach the clinic characteristics of epileptic seizure related with antibiotics. MethodsThe patients having epileptic seizure related with antibiotics in Weipu Wanfang and Zhongguo Zhiwang databases were retrieved and their clinical characteristics were approached. Results①Totally 238 patients were retrieved. One hundred and thirty cases of epileptic seizure was related with quinolinones，80 with betalactam，8 with macrolide，7 with aminoglycoside，5 with clindamycin and 8 with nitramisole. One hundred and ninetyfive patients were injected intravenously and 43 cases were orally administered. One hundred and ninetyseven patients had grand mal，12 minor seizure，13 myoclonus，and 16 patial seizures. One hundred and fiftyseven patients developed seizures 2－4 days after the administration. In 162 patients，duration of epileptic seizure was 10－30 min. In 210 patients，seizures were controlled after drug withdrawal and antiepileptic treatment.ConclusionQuinolinones and betalactam are prone to inducing epileptic seizure. So those patients with central nervous system diseases should avoid using such antibiotics and the dose should be decreased when used in those with renal insufficiency. More patients administered medication through vein developed seizures than those administered per os. So，we should choose to take medicine per os as far as possible. Grand mal is the main style of epileptic seizure related with antibiotics. Most of epileptic seizure happened 2－4 days after giving antibiotics. Most of epileptic seizure can be controlled after withdrawal and antiepileptic treatment in 10－30 min.
