Objective: To compare the pharmacokinetics and relative bioavailability of rapid oral disintegrating tablet of dimenhydrinate (RODTD) and those of market available tablet of dimenhydrinate (DMH). Methods: Eight healthy volunteers were evenly randomized into 2 groups, one group received RODTD (25 mg) and the other received available market tablet of dimenhydrinate (25 mg). The blood levels of DMH were determined by high performance liquid chromatography (HPLC) before and after drug administration in 2 groups. Chromatography conditions were: Nova-Pak C18 as chromatographic column, methanol triethylamine buffer (1 : 1),flow rate: 1.0 ml/min, detection wavelength: 225 nm, and room temperature. The pharmacokinetics and relative bioavailability of RODTD and market available tablets were investigated. Results: The standard curve of DMH in the blank plasma was linear within the range of 5-500 ng/ml, with the regression equation being C=0.004 4 A+4.745 and R2=0.996. The limit of detection was 2 ng/ml; the average recovery rate was (90.55±4.69)% and the RSD was 0.041%. The intra-day derivations of 3 different concentrations (low, middle, and high) of plasma were 9.27%, 4.93%, and 2.95%, respectively (n=5), and the inter-day derivations were 9.97%, 3.81%, and 3.06%, respectively (n=5). Blood samples (3 ml) were subjected to HPLC assay and significant difference was found between the 2 forms of DMH. The pharmacokinetic parameters of RODTD were: AUC=(602.04±113.82) ng • h • ml-1, Cmax=(95.86±21.28) ng • h • ml-1, and TPeak=(1.8±0.32) h; the pharmacokinetic parameters of market available tablets were: AUC=(342.73±84.96) ng • h • ml-1 Cmax=(46.34± 10.32) ng • ml-1, and TPeak=(2.65±0.24) h. Statistical analysis showed there was significant difference in the relative bioavailability of 2 forms of DMH(P<0.01). The relative bioavailability of RODTD to market tablet was 175.66%. Conclusion: The developed RODTD can obviously increase the relative bioavailability of DMH.

Eustachian Tube ; abnormalities ; surgery ; Humans ; Laser Therapy ; Male ; Middle Aged ; Prosthesis Implantation ; Stents ; Tympanoplasty

Objective To analyze the predictive factors of fever after percutaneous renal stone surgery,and to provide reference for clinical treatment.Methods A total of 147 patients underwent percutaneous nephrolithotomy in after operation was chosen in the Department of Urology in our hospital from January 2014 to January 2016.According to the existence of fever,patients were divided into fever (n =25,heating rate 17.0％) and control (n =122) groups.Preoperative information were collected,including age,gender,preoperative serum creatinine,stone size and shape,the involvement of calyceal number,water,urine culture results,operative time,blood loss,intraoperative perfusion volume,pyonephrosis,puncture channel length,hospitalization time and other information including intraoperative,postoperative information including fever,and postoperative renal fistula complications if there is information.SPSS 18.0 was used for statistical analysis.Results The fever group stone surface area,CT value affected calyx number,stone shape,stone properties,the involvement of calyceal number,degree of hydronephrosis,operative time,intraoperative blood loss,intraoperative perfusion,hospitalization time,and renal fistula complication rates were higher than the control group (P ＜ 0.05).There were no significant differences between two groups (P ＞0.05).The results of Logistic regression analysis found that the stone surface area (OR =5.19),stone,stone shape (OR =7.86) properties (OR =3.87),operation time (OR =5.68),intraoperative perfusion (OR =5.24),and renal fistula complications (OR =2.65) for the influence factors of fever.Conclusions The stone surface area is large,stone nature infection stones,stone shape for staghorn calculi,longer operation time,and intraoperative perfusion of large renal fistula complications were more prone to postoperative fever in postoperative.

Objective To analyze the distribution and antimicrobial resistance of pathogenic bacteria in urinary tract infection (UTI)so as to provide evidence for appropriate selection of antimicrobial agents in clinical practice. Methods From January 2001 to December 2008 in Shanghai Ruijin Hospital,4683 strains of pathogenic bacteria isolated from urine samples were detected by ATB system;drug susceptibility test was performed with disk diffusion method and pathogenic bacteria distribution and drug resistance was analyzed with WHO NET 5.3 software. Results Among 4683 strains of pathogenic bacteria,most was gramnegative bacilli,accounting for about 77.8%,of which predominant strain was Escherichia coli (68.7%,3217/4683).The predominant strain of gram-positive bacteria was Enterococcus faecalis,accounting for 10.0%(468/4683).Escherichia coli showed hish resistance rotes to ampicillin,piperacillin and compound snlfamethoxazole(SMZ-TMP),which were 76.6%,61.7%and 57.4%respectively,while a low resistance to imipenem,cefoperazone-sulbactam,piperacillin-tazobactam,Enterococcus faecalis showed high resistance rates to erythromycin,gentamicin and levofloxacin,which were 65.8%,43.2%and 31.1%respectively,and were most susceptive to vancomycin and teicoplanin, both with resistance rates of 0. The susceptibility rate of Enterobacteriaceae to imipenem was 100%. From 2006 to 2008, the detection rate of extend-spectrum β-lactamases ESBLs -producing Escherichia coil in outpatient increased year by year, from 28.7% to 43.3% (P＜0.05), whereas no significant change was found in inpatients. The detection rate of (ESBLs)-producing Escherichia coil in inpatients was significantly higher than that in outpatients (P＜0.05).The detection rate of ESBLs-producing Escherichia coil was 23.6%. The antimicrobial resistance rate in elderly patients was significantly higher than that in overall antimicrobial resistance rote (P＜0.05). Conclusions The predominant bacteria of UTI are still gram-negative bacteria, main of which is Escherichia col. Bacteria are resistant to a variety of antibiotics. Approximate selection of antibiotics in clinical practice should be made on the basis of susceptibility test results.

Animals ; Brain Edema ; prevention & control ; Brain Ischemia ; physiopathology ; Erythropoietin ; pharmacology ; Female ; Hippocampus ; metabolism ; pathology ; Male ; Nitric Oxide ; metabolism ; Protective Agents ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; prevention & control ; Superoxide Dismutase ; metabolism

Inosiplex is a compound formulation composed of inosine and p-acetaminobenzoic acid (PABA) salt of N,N-dimethylamino-2-propanol (DIP). This study was to investigate the clinical plasma pharmacokinetic properties of DIP and PABA after single and multiple oral doses of inosiplex tablets in healthy Chinese volunteers. The established LC/MS/MS method for plasma DIP determination had a linear range of 0.02-10 mg/mL, and the HPLC method for plasma PABA determination had a linear range of 0.05-40 mg/mL. Linear pharmacokinetic characteristics were found with single oral doses of 0.5, 1.0 and 2.0 g. No obvious accumulation effects were observed for DIP and PABA.

Objective To dynamically observe the changes of cytokines of splenocytes in mice immunized with recombinant bifidobacteria bifidum (Bb)- Eg95-EgA31 vaccine of Echinococcus grauulosus (Eg). Methods Balb/c mice were vaccinated by 5× 108 colony forming unit(CFU) orally and 5 × 105 CFU intranasally, respectively.Mice were killed on week 0,2,4,6,8,10, 12,14,16, 18 and 20 after immunization, respectively, and spleens were separated for cell culture with the stimulation of EgAg, concanavalin A (ConA) or lipopolysaccharide (LPS). The splenocyte supernatants were collected to determine the levels of interferonγ(IFN-γ), interleukin(IL)-12, tumor necrosis factor α(TNF-o) and IL-l0 using enzyme linked immunosorbent assay(ELISA) with MRS as control. Results In the oral immunization group, the levels of IFN-γ, IL-12, TNF-α and IL-10 showed a significant increase from week 2 to week 8, week 2 to week 8, week 4 and week 6 to week 10 after vaccination, respectively, and reached the highest level on week 4, week 2, week 4 and week 6 after vaccination, respectively;in EgAg stimulation group, the levels of IFN-γ, IL-12, TNF-α and IL-10 were (700.0 ± 115.5), (45.0 ± 5.8), (350.0 ± 57.7), (112.5 ± 14.4)ng/L, respectively, compared with week 0[(35.0 ± 5.8), (12.5 ± 2.9), (190.0 ± 11.6), (25.0 ± 5.8)ng/L, P ＜0.05 or ＜ 0.01] and MRS control group[(37.5 ± 5.0),(13.8 ± 2.5), (195.0 ± 5.8), (27.5 ± 2.9)ng/L, P＜ 0.05or ＜ 0.01]. In the intranasal immunization group, the levels of IFN-γ, IL-12, TNF-α and IL-10 showed an obvious increase from week 2 to week 8, week 2 to week 8, week 2 to week 6 and week 6 to week 16 after vaccination,respectively, and reached the highest level on week 2, week 2, week 4 and week 8 after vaccination, respectively;in EgAg stimulation group, the levels of IFN-γ, IL-12, TNF-α and IL-10 were (700.0 ± 115.5), (55.0 ± 5.8),(275.0 ± 28.9), (140.0 ± 11.6)ng/L, compared with week 0[(35.0 ± 5.8), (12.5 ± 2.9), (190.0 ± 11.6), (25.0 ±5.8)ng/L, P ＜ 0.05 or ＜ 0.01] and MRS control group[(37.5 ± 5.0), (13.8 ± 2.5), (195.0 ± 5.8), (27.5 ± 2.9)ng/L, P ＜ 0.05 or ＜ 0.01]. The cytokine levels in the groups with EgAg, ConA or LPS stimulus were significantly higher than those in the corresponding splenocytes suspension groups(P ＜ 0.05 or ＜ 0.01) , and the cytokine levels in the groups with ConA or LPS stimulus were obviously higher than those in the corresponding groups with EgAg stimulation(P ＜ 0.05 or ＜ 0.01). Conclusion The mixed Th1 and Th2 type response can be induced in mice immunized with the recombinant Bb-Eg95-EgA31 vaccine of Echinococcus granulosus in the early stage of immunization(2 to 6weeks).

Objective To construct and express the recombinant plasmid pET28α-Sj26GST-Sj32 of Schistosoma japonicum(Sj) in Escherichia coli BL21 (DE3). Methods Total RNA was extracted from Sj adult worms by ultrasound-breaking, Sj26GST and Sj32 antigen gene was respectively amplified by RT-PCR from the total RNA; Sj26GST-Sj32 fusion gene obtained with gene splicing by overlap extension(SOEing) was cloned into prokaryotic expression plasmid pET28α and transformed into Escherichia coli BL2 (DE3) to construct pET28α-Sj26GST-Sj32;BL21 (pET28α-Sj26GST-Sj32) was induced with isopropyl-β-D-thiogalactopyranosid (IPTG), and the expressed products were analyzed and identified by sodium dodecyl sulfate polyacrylamide gel electropheresis (SDS-PAGE)and Western blotting. Results The 1991 bp Sj26GST-Sj32 fusion gene was successfully amplified by gene SOEing and cloned into pET28α by restriction analysis and PCR identification, the recombinant plasmid pET28α-Sj26GST-Sj32 was successfully constructed; the relative molecular mass of the expressed recombinant protein was approximately 69 × 103 by SDS-PAGE, and the amount of the expressed protein was 25% of the total bacterial proteins; the fusion protein could be recognized by sera from rabbits infected with Sj by Western blotting.Conclusions The recombinant plasmid pET28α-Sj26GST-Sj32 is successfully constructed and highly expressed in Escherichia coli in fused form with His-tag, and the expressed fusion protein shows specific antigenicity.

Objective To construct and identify recombinant Bifutobacteria (rBb)-Eg95 vaccine of Echinococcus granulosus (Eg). Methods The total RNA was extracted from hydatid cyst protoscoleces shattered by ultrasound, Eg95 antigen encoding gene was obtained by reverse transcription-polymerase chain reaction(RT-PCR) from the template of total RNA using the primer designed according to the DNA sequence of Eg95, the gene was cloned into Escherichia coli-Bifutobacteria(E.coli-Bb) shuttle plasmid pGEX-1λT and transformed into E.coli BL2 (DE3) competent cell to construct recombinant plasmid pGEX-Eg95 using BamH Ⅰ and EcoR Ⅰ, the recombinant plasmid was identified by restriction endonuclease digestion, then was electroporated into Bb to construct rBb-Eg95 vaccine, the vaccine was identified by PCR. Results Four hundred and seventy-one bp Eg95 gene was amplified by RT-PCR, the products of restriction endonuclease digestion were the same as expected(471 bp Eg95 gene and 4947 bp pGEX-1λT), 471 bp Eg95 gene fragment was amplified by PCR from the template of pGEX-Eg95 extracted from rBb vaccine. Conclusion rBb-Eg95 vaccine of Eg is successfully constructed, which lays the theoretical foundation for exploitation and utilization of this vaccine.

Objective To construct and express the recombinant plasmid pET32α-Sj26GST of Schistosoma japonicum(sj)in Escherichia coli(E.coli)B121(DE3).Methods The total RNA was extracted from sj adult worms by ultrasound-breaking,Sj26GST antigen gene was amplified by RT-PCR from the total RNA,then cloned into prokaryotic expression plasmid pET32α(+) and transformed into E.coli B12(DE3)to construct pET32α-Sj26GST;BL21(pET32α-Sj26GST)WaS induced with isopropyl-β-D-thiogalactopyranosid(IPTG),and the expressed products were analyzed and identified by SDS-PAGE and Western blot.Results The 676 bp Sj26GST gene was successfully amplified by RT-PCR and cloned into pET32α(+)by restriction analysis and PCR identification,the recombinant plasmid pET32α-Sj26GST was successfully constructed;the relative molecular mass of the expressed recombinant protein was approximately 49×103 by SDS-PAGE,and the amount of the expressed protein was 24%of the total bacterial proteins;the fusion protein could be recognized by sera from rabbits infected with sj by Western blot.Conclusions The recombinant plasmid pET32α-Sj26GST is successfully constructed and highly expressed in E.coli in fused form with Trx-tag and His-tag,and the expressed fusion protein shows specific antigenicity.