Background Vancomycin has been increasingly recommended for the management of endophthalmitis,but few research report has been published about the pharmacokinetics of intravitreal vancomycin up to now.It is necessary to have an exact method to measure the concentration of vancomyein in animal eyes after intravitreal injection.Objective This study was to observe and compare the phamacokinetical process of vancomycin in serum,vitreous and aqueous humor between normal and infected rabbit eyes.Methods Seventy-two healthy adult rabbits were randomly divided into normal group and infected group and 36 rabbits for each.The animal models of endophthalmitis were established by intravitreal inoculation of 2000 CFU/ml staphylococcus aureus in the right eyes of rabbits in the infected group.Once endophthalmitis developed,0.1 ml vancomycin ( 10 g/L) solution was injected into the vitreous of every rabbit.The peripheral blood,vitreous and aqueous humor samples were respectively collected in 4 rabbits for each group at 0.5,2,4,6,12,24,48,72 and 84 hours after injection for detection of vancomycin concentration by high performance liquid chromatography(HPLC-UV).3p97 software was used to create fit parameters of pharmacokinetics.This experiment followed the Regulations for the Administration of Affair Concerning Experimental Animals by State Science and Technology Commission (Version 1988).Results The accuracy of HPLC fitted the detecting request of biological specimen.The concentration-time data of vancomycin in normal rabbit aqueous humor and vitreous was subject to two-compartment model.The pharmacokinetic parameters were separately as following:Cmax was 50.16 mg/L and 751.42 mg/L,t1/2was 51.04 hours and 53.21 hours.The concentration-time data of vancomycin in infected rabbit aqueous humor and vitreous was subject to one-compartment model.The pharmacokinetic parameters were separately as following:Cmaxwas 24.94 mg/L and 687.66 mg/L,t1/2was 11.42 hours and 12.91 hours.The concentration of vancomycin in serum was much lower and almost undectable.The concentration of vancomycin in vitreous was gradually reduced as the prolong of time after injection in both normal group and infected group,but a obvious decline after increased level was scen in aqueous humor.Compared with normal group,the concentrations of vancomycin in both vitreous and aqueous humor were reduced at various time points(P＜0.05,P＜0.01 ).Conclusions HPLC is simple,highly sensitive and specific for the pharmacokinetic analysis of vancomycon.These results indicate that pharmacokinetic parameters of vancomycin alter in pathological condition,which is helpful for us to establish the better treatment guidelines for endophthalmitis.

ObjectiveTo study the effct of the early rehabilitation of acute stroke with acupunction added to rehabilitational training.Methods120 patients with acute stroke were divided into 2 growps with 60 cases each:the acupunction growp,in which the patients were acepted acupuncture added to rehabilitational training,and the control growp,in which the patients were acepted the rehabilitational training only.All the patients were evaluated with Clinical Nervous Functional Deficiency(CNFD),Fugl-Meyer Assessment(FMA) and Modified Barthel Index(MBI).Results The scales of CNFD,FMAanal Deficiency (CNFD),Fugl-Meyer Assess me that of the control growp.The rate of cure and significantly in the acupunction growp was 75%,while that of the control growp was 41.7%(P<0.01).Conclusions Acupunction compared with the rehabilitational training is effective on the with stroke.

Objective To explore the relationship between serum adiponectin concentration and hyperuricemia in Han people in Hunan.Methods Cluster random sampling method was used to carry out the survey during October to December 2008 in Changsha Health Checkup Center of the Second Xiangya Hospital.All subjects completed the questionnaires,physical examination,biochemical measurements,and the data were analyzed by t test,Pearson's correlation analysis and multiple linear regression analysis.Results The Age,WC,TG,SBP,DBP,SUA,BMI were significantly higher in hyperuricemia group compared with the normal uric acid group.The concentration of adiponectin in hyperuricemia group was significantly lower than that in the normal uric acid group (5.0±2.7 vs 6.8±4.2 μg/ml,t=3.961,P＜0.05).In the normal serum uric acid group,the serum adiponectin concentration in female was significantly higher than that in male (t=4.99,P＜0.05).Pearson's correlation analysis showed that serum adiponectin concentration was negatively correlated with the serum uric acid level,but the adiponectin level was not significantly correlated with Age and blood pressure.Stepwise analysis showed that the main factors that could affect the adiponectin level were SUA,gender and BMI (P＜0.05).Conclusion The decreasing of serum adiponectin concentration might be one of the mechanisms of hyperuricemia,therefore,detecting serum adiponectin concentration may provide the basis for the prevention and treatment of hyperuricemia.

Objective To explore the therapeutic effects of 660 nm red light on sciatic nerve injury in adult rats.Methods Forty-five adult,male rats were divided into a control group and treatment groups 1,2,3 and 4.Sciatic nerve injury was modeled by crushing the nerve.The treatment groups received irradiation with red light once daily for 21 consecutive days.The power density of red light and irradiation time varied among the groups.The latency and amplitude of compound muscle action potentials (CMAPs) and nerve conductive velocity were examined at different time points.The Sciatic Function Index (SFI) was used to evaluate walking function.Results After 21 days of red light therapy no statistically significant differences were observed between the control group and treatment groups 1 to 4 with regard to the latency or the amplitude of the CMAPs.There was a significant difference between the control group and treatment group 3 in terms of sciatic nerve conduction velocity.The average Sciatic Function Indexes of treatment groups 2,3 were significantly different from that of the control group.Conclusion Red light irradiation can promote recovery after sciatic nerve injury,at least in rats,thereby improving walking function.

Objective To explore the value of MRI-R2 * and to compare clinical effect of two iron chelators(deferasirox and deferoxamine) in iron-overloaded patients.Methods By completely randomized balanced design,24 iron-overloaded patients were randomly divided into 2 groups,which consisted of 12 patients treated with deferasirox and 12 patients treated with deferoxamine.The planned deferasirox dose was 40 mg· kg-1 · d-1,and the deferoxamine dose was no less than 50 mg · kg-1 · d-1 All patients underwent quantitative MRI at the time points of the primary screening,6 months and 12 months.Pair Wilcoxon rank sum test was used to compare the differences of liver R2 * values of the 2 groups at various time points respectively.Wilcoxon rank sum test was used to compare the differences of change rate of liver R2 * values between the two groups at the time point of 6 months,12 months,respectively.Results Deferasirox group's liver R2 * values of primary screening,6 months and 12 months were 1081,889 and 712 Hz,while deferoxamine group's liver R2 * values were 1042,838 and 488 Hz.There was no statistically significant difference between liver R2 * values of two groups at primary screening (Z =-0.029,P ＞ 0.05).The change rate of liver R2 * of deferasirox group at 12 month was-32％,while it was-58％ for the deferoxamine group,and there was statistically significant difference between the two groups (Z =-3.060,P ＜0.01).The change rate of serum ferritin of deferasirox group at 12 month was-15％,while it was -55％ for the deferoxamine group,and there was statistically significant difference between the two groups (Z =-2.945,P ＜ 0.01).Conclusion By using MRI-R2*,it suggest that both deferasirox and deferoxamine can effectively remove liver iron and deferoxamine is superior to deferasirox.

Objective To study the relationship between the MRI features and pathological types of intracranial meningiomas. Methods MRI findings of intracranial meningiomas in 63 cases proved by operation and pathology were analyzed retrospectively.Results Of 63 cases,62 cases were singular and one case was multiple lesions. The lesions were located in frontal,parietal and occipital regions nearby the convexity of the brain in 30 cases,in sellar region in 10,at sphenoidal crest in 8 , at olfactory sulcus in 5 and at other regions in 10. Isointense or slightly hypointense signal on T 1WI was found in 87.27% cases of meningiomas . On T 2WI, tumors had isointense or slightly hyperintense signal in 69.84%, obviously hyperintense signal in 19.05%,heterogenous texture signal in 7.94% and slightly low intense signal in 3.17%. Pathological type was included meningiomas meningothelial(n=29), meningiomas fibrous(n=11) , meningiomas psammomatous(n=8),angioblastic meningiomas (n=5) and meningiomas angiomatous(n=10). Conclusion It is great value in diagnosis of meningiomas with MRI. Meningiomas angiomatous show effecting of blood-vessel flowed empty with MR imaging.

Objective To assess the prevalence of metabolic syndrome (MS) and explore the associated risk factors with MS among 35 ～ 80 years elderly people in Changsha.Methods The survey used by cluster random sampling method (from October to December,2008 ) was carried out by the Physical Examination Center of the Second Xiangya Hospital,Changsha.All subjects aged from 35 to 80 years old had the questionnaires,physical examination,and biochemical measurements.MS was defined by IDF 2005.Results The prevalence of MS was 24.3％ among elderly people in Changsha.The prevalence of MS in male and female was 27.9％ and 19.3％,respectively; which in male was significantly higher than in females ( P ＜0.01).According to census of 2000 in Changsha,the age-adjusted rate of MS was 24.4％ among elderly people,27.8％ in male and 21.9％ in female,respectively.The metabolic abnormalities and the prevalence rate of MS were different in gender and age.Except the essential component of the central obesity in the 194 cases of MS patients,there are 80 cases include other two kinds of metabolic abnormalities,accounting for 41.2％,most of them with elevated blood pressure + sugar metabolism disorders; the most common three kinds of metabolic abnormalities of the 78 cases,accounting for 40.2％ of the people with MS,most of them with high TG + elevated blood pressure + sugar metabolism disorders; With 4 kinds of metabolic abnormalities of 36 patients,accounting for 18.6％ of the MS patients.Increasing age,male,overweight and (or) obesity,high LDL-C hematic disease,high uric acid hematic disease,diabetes were all the risk factors of the elderly people in Changsha city.Conclusions Elderly people in Changsha have a relatively high prevalence of MS,especially for male.The prevalence of MS is considerably high in Changsha,which may continue to rising with the social economic development and population aging.There is an urgent need to take actions to reduce the burden of MS.

A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.
Animals ; Antineoplastic Agents ; administration & dosage ; chemistry ; Cell Line, Tumor ; Deoxycholic Acid ; chemistry ; Drug Carriers ; chemistry ; Humans ; Male ; Mice ; Neoplasms ; drug therapy ; Phospholipids ; chemistry ; Solubility ; Triterpenes ; administration & dosage ; chemistry

OBJECTIVETo study the preparation of phenols gastric floating tablet.

METHODThe tablets which were prepared using Eudragit IV, HPMC(K4M), MCC101 and Octadecanol as excipients were evaluated by vitro floatation and releasing performance. The pressure of preparationg was also study to select the optimal preparation.

RESULTThe tablets were successfully prepared in which the drug, Eudragit IV, Octadecanol were 31% respectively,and MCC101 was 7%. And 3-4 kg was found to be the eligible pressure.

CONCLUSIONThe study was found to be effective in the process of phenols gastric floating tablet.

Drug Carriers ; Excipients ; chemistry ; Gastrointestinal Agents ; chemistry ; Phenols ; chemistry ; Polymethacrylic Acids ; chemistry ; Tablets ; Technology, Pharmaceutical ; methods

Simvastatin is a hypolipidemic drug that inhibits hydroxymethylglutaryl coenzyme A (HMGCoA) reductase to control elevated cholesterol,or hypercholesterolemia.Previous studies have shown that simvastatin may attenuate inflammation in ischemia-reperfusion injury and sepsis.Herein,we hypothesized that simvastatin may prevent rats from lipopolysaccharide (LPS)-induced septic shock.In our study,rats were divided into a saline group,an LPS group and an LPS plus simvastatin group.Male Sprague-Dawley (SD) rats were pretreated with simvastatin (1 mg/kg) for 30 min before the addition of LPS (8 mg/kg),with variations in left ventricular pressure recorded throughout.Ninety min after LPS injection,whole blood was collected from the inferior vena cava,and neutrophils were separated from the whole blood using separating medium.The neutrophils were then lysed for Western blotting to detect the levels of urokinase-type plasminogen activator (uPA) and plasminogen activator inhibitor-1 (PAI-1).In addition,mesentery microcirculations of inlet diameter,outlet diameter and blood flow rate were measured in all three groups.The results indicated that simvastatin significantly promoted heart systolic function and increased the level ofuPA while simultaneously inhibited the expression of PAI-1 as compared with LPS group.Moreover,simvastatin reversed the LPS-induced inhibition of mesentery microcirculation.Taken together,it was suggested that simvastatin can effectively protect the rats from LPS-induced septic shock.