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 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.

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.

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.

Glycyrrhiza uralensis Fisch. ex DC is widely used in traditional Chinese medicine (TCM). Among its various active components, glycyrrhizic acid is believed to be the marker component. Squalene synthase (SQS) and beta-amyrin synthase (beta-AS) are key enzymes in the biosynthetic pathway of glycyrrhizic acid in G uralensis. To reveal the effects of co-expression of SQS1 and beta-AS genes on this pathway, 7 yeast expression vectors harboring different SQS1 variants and beta-AS were constructed and expressed in Saccharomyces cerevisiae as fusion proteins. TLC and GC-MS results showed that co-expression of SQS1 and beta-AS enhanced the accumulation of beta-amyrin. The effects of SQS12 were more obvious than the other two SQS1 variants. This study is significant for further investigations concerned with exploring the biosynthesis of glycyrrhizic acid in vitro and strengthening the efficacy of G. uralensis by means of increasing the content of glycyrrhizic acid.

Animals ; Chicory ; Fibronectins ; metabolism ; Insulin-Like Growth Factor Binding Proteins ; metabolism ; Liver ; drug effects ; metabolism ; Liver Cirrhosis, Experimental ; metabolism ; Male ; Plant Extracts ; pharmacology ; Rats ; Rats, Wistar ; Smad3 Protein ; metabolism ; Transforming Growth Factor beta1 ; metabolism

Glycyrrhiza uralensis Fisch. ex DC is widely used in traditional Chinese medicine (TCM). Among its various active components, glycyrrhizic acid is believed to be the marker component. Squalene synthase (SQS) and beta-amyrin synthase (beta-AS) are key enzymes in the biosynthetic pathway of glycyrrhizic acid in G uralensis. To reveal the effects of co-expression of SQS1 and beta-AS genes on this pathway, 7 yeast expression vectors harboring different SQS1 variants and beta-AS were constructed and expressed in Saccharomyces cerevisiae as fusion proteins. TLC and GC-MS results showed that co-expression of SQS1 and beta-AS enhanced the accumulation of beta-amyrin. The effects of SQS12 were more obvious than the other two SQS1 variants. This study is significant for further investigations concerned with exploring the biosynthesis of glycyrrhizic acid in vitro and strengthening the efficacy of G. uralensis by means of increasing the content of glycyrrhizic acid.
Farnesyl-Diphosphate Farnesyltransferase ; genetics ; metabolism ; Glycyrrhiza uralensis ; genetics ; Intramolecular Transferases ; metabolism ; Oleanolic Acid ; analogs & derivatives ; metabolism ; Plant Proteins ; genetics ; Recombinant Proteins ; metabolism ; Saccharomyces cerevisiae ; metabolism

OBJECTIVETo study the acting mechanism of endothelial cell line ECV304 in regulating angiogenesis induced by Xuefu Zhuyu Decoction (XFZY).

METHODSThe angiogenesis effect of XFZY-contained serum (XFZY-CS) was confirmed by observing its impact on proliferation, cell cycle, migration of ECV304 and on vascular neogenesis in vitro. Then the effect of XFZY on various angiogenesis controlling factors was analyzed with gene chip microarray technique.

RESULTSTreatment of XFZY-CS in 2.5% concentration for 48 h showed evident actions of enhancing ECV304 activity, increasing cell numbers of S phase, inducing cell migration and promoting the in vitro angiogenesis. Meanwhile, expressions of four angiogenesis controlling genes were up-regulated and 10 were down-regulated.

CONCLUSIONThe angiogenesis mechanism of ECV304 induced by XFZY is complex, it shows a multi-pathway and multi-target feature.

Angiogenesis Inducing Agents ; Animals ; Cell Line ; Drugs, Chinese Herbal ; pharmacology ; Endothelial Cells ; drug effects ; Female ; Gene Expression Regulation ; drug effects ; Male ; Neovascularization, Physiologic ; drug effects ; Rats ; Rats, Sprague-Dawley