Objective Enzyme triggered multi unit colon targeting mini tablet of indomethacin were prepared,in order to improve the target treatment of colon disease.Methods Different proportion of enteric layer and chitosan layer were screened to optimize the prescription.The colon targeting mini tablets were prepared by direct compression method.The drug release properties were investigated in different release medium.Rats were used to investigate the distribution of tissue in vivo.The Beagle dogs were used to study the pharmacokinetics and bioavailability.Results The optimum chitosan layer prescription:coating liquid concentration was 2％,plasticizer three citric acid ethyl ester (TEC) was 15％,an anti sticking agent amount of talc was 30％,coating weight was 5％;Enteric layer prescription:coating liquid solid content was 20％,plasticizer content of TEC was 5％,anti sticking agent talc powder dosage was 40％,coating weight was 3％.The chitosan multi unit colon targeted preparation seldom released in rat stomach and small intestine,released slowly in colon.The pharmacokinetics parameters in Beagle dogs were:Cmax =(3.25 + 0.672) mg·L-1,tmax =(2.00 + 0.014) h,AUC(0.∞) =(10.2 +0.871) mg·L-1 ·h,MRT (0-∞) =(2.82 + 0.180) h,CL =(2.46 + 0.202) L·h-1 ·kg-1.The release time of mini tablets for colon targeted was significantly prolonged and preserved stable blood concentration.Conclusion The enzyme triggered multi unit colon targeting mini tablet of indomethacin showed good target to colon and sustained release effect,providing an important reference for the development of preparation of indomethacin for the treatment of colon disease.

Hepatitis B virus infection is a serious threat to human life and health. The approved anti-HBV drugs including interferons and nucleos(t)ide analogues have serious adverse effect, rebound phenomena after drug withdrawal, and drug resistance. And the cccDNA cannot be completely eliminated by both of them, which is the reason why a complete cure for hepatitis B cannot be achieved. Therefore, developing anti-HBV drugs directly targeting protein or nucleic acid of HBV remains a current public health priority. Based on the analysis of representative literature from the last decade, this article reviews recent developments in small molecule inhibitors directly targeting HBV from a medicinal chemistry perspective.

OBJECTIVETo observe the characteristics of the physiological uptake of uterus and ovaries on 18F-fluorodeoxyglucose positron emission tomography (FDG PET).

METHODSA total of 288 PET examinations performed in 247 women (164 with malignancies, 44 with benign diseases, and 39 without remarkable abnormality) were included for analysis, and clinical follow-ups were applied for at least 10 months to exclude pelvic diseases. The menstrual statuses, menstrual cycles, and related pelvic examinations with other modalities were inquired before each PET examination. PET scanning was performed from pelvis to neck with a Siemens ECAT EXACT HR + system. The uptake levels of uterus and ovaries were set as intense, moderate, and mild by comparing to liver uptake.

RESULTSIn 116 patients (131 examinations ) with regular menstruation, the endometrial uptake, usually in inverted cone shape surrounded by relatively low-uptake uterine wall, was observed with two peaks in the early menstrual flow phase and in the mid-cycle respectively; the ovarian uptake was more prominent in the mid-cycle, with the foci of uptake in ovoidal shape and located at the left and/or right side superior-posterior to the bladder. From the early menstrual flow phase to the late secretory phase of the menstrual cycles, the probabilities of mild uptake in both endometrium and ovaries were 7%, 86%, 80%, 58%, 20%, 40%, 64%, and 59%, respectively, indicating that the late menstrual flow phase and the early proliferative phase had the least probability of intense or moderate uptake. No intense uptake was observed in the 17 patients (19 examinations) presenting remarkably irregular menstrual cycle, 112 patients (136 studies) in menopause for 3 months to 39 years, and 2 patients without menstruation yet. Only one patient within 1 year of menopause and a 14-year-old girl expected to start menstruation showed mild to moderate uptake in the endometrium.

CONCLUSIONThe physiological endometrial and ovarian uptakes have specific shapes and positions on 18F-FDG PET images, which correlates well with the menstrual phases.

Adolescent ; Adult ; Female ; Fluorodeoxyglucose F18 ; pharmacokinetics ; Humans ; Menopause ; Menstrual Cycle ; Middle Aged ; Ovary ; diagnostic imaging ; metabolism ; Positron-Emission Tomography ; methods ; Uterus ; diagnostic imaging ; metabolism ; Young Adult

OBJECTIVETo observe the effects of interleukin-8 monoclonal antibody on smooth muscle cell proliferation and balloon inflation-induced abdominal aorta stenosis in rabbits.

METHODSThirty-six New Zealand white rabbits were randomly assigned to balloon inflation group (group A, n = 12), interleukin-8 monoclonal antibody pre-treated rabbits (2 mg/kg for 3 days before balloon inflation, group B, n = 12) and sham-operated control group (group C, n = 12). Peripheral blood was collected before experiment and at 4 h, 1, 3, 7, 14, and 28 days post balloon inflation or sham operation and the levels of IL-8 were measured by enzyme linked immunosorbent assay (ELISA). The ratio of positive and negative masculine cells in the high power microscopic field was determined in proliferating cell nuclear antigen (PCNA) stained slide. Histopathologic examination was performed in abdominal aorta and luminal area, intima and tunica media area were measured.

RESULTSPlasma interleukin-8 began to rise at 4 h and peaked at 1 day and remained increased up to 28 days after balloon inflation in rabbits of group A, plasma interleukin-8 level in group A was significantly higher than in group B and C at 4 h and thereafter post operation. The ratio of positive and negative masculine cells was significantly increased in group A compared to group C and was significantly lower in group B than in group A. Abdominal aorta stenosis, luminal area, intima and tunica media area were significantly reduced in group B than in group A. Correlation analysis indicated that there were positive relations between plasma IL-8 level and intima thickness, area of intima and tunica media, respectively (r = 0.894, 0.783, 0.801, 0.912, all P < 0.01).

CONCLUSIONSPlasma IL-8 level is increased in this abdominal aorta stenosis model and is positively correlated to the severity of abdominal aorta stenosis. IL-8 monoclonal antibody could significantly reduce abdominal aorta stenosis in this abdominal aorta stenosis model.

Animals ; Antibodies, Monoclonal ; pharmacology ; therapeutic use ; Aorta, Abdominal ; pathology ; Aortic Coarctation ; drug therapy ; pathology ; Cell Proliferation ; drug effects ; Interleukin-8 ; immunology ; Muscle, Smooth, Vascular ; cytology ; drug effects ; Myocytes, Smooth Muscle ; drug effects ; Rabbits

To study the acute Leukemia immunophenotype and its diagnosis value, three color direct immunofluorescece staining methods of flow cytometry and immunophenotype of antibody integration system were used for detection of 180 cases of acute leukemia. The results showed that patients with ALL expressed lymphocyte antigen, and 49.4% patients with ALL accompanied myeloid antigen; all patients with AML expressed myeloid antigen, and 43.2% patients with AML accompanied lymphocyte antigen. In conclusion, leukemia immunophenotyping by three-color direct immunofluore staining methods could define some particular types of leukemia with an important value in diagnosis, treatment and predicting prognosis of acute leukemia.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Antigens, CD ; analysis ; CD79 Antigens ; Child ; Child, Preschool ; Female ; Flow Cytometry ; methods ; Humans ; Immunophenotyping ; Infant ; Leukemia, Myeloid, Acute ; immunology ; Leukocyte Common Antigens ; analysis ; Male ; Middle Aged ; Precursor Cell Lymphoblastic Leukemia-Lymphoma ; immunology ; Receptors, Antigen, B-Cell ; analysis

OBJECTIVETo study the feasibility of magnetron sputtering Cr-Ti-Al-N complex coating as an interlayer on titanium to enhance the titanium-ceramic binding strength.

METHODSWith a three-point bending test according to ISO 9693, the binding strength of Duceratin (Degussa) to titanium substrate prepared with 4 different surface treatments (polishing, polishing and megnetron sputtering Cr, Ti, Al, and N complex coating, sandblasting, sandblasting and coating) was evaluated. Ti/porcelain interface and fractured Ti surface were examined using scanning electron microscopy with energy-dispersive spectrometry (EDS).

RESULTSThe binding strength of polished and coated titanium/Duceratin was significantly higher than polished titanium group (P<0.05). The binding strength of sandblasted and coated titanium/Duceratin did not differ significantly from that of sandblasted titanium group (P>0.05), and the strength in the two sandblasted titanium groups was significantly higher than that in polished and coated titanium group (P<0.05).

CONCLUSIONMegnetron sputtering Cr-Ti-Al-N complex on polished titanium can increase the titanium/porcelain binding strength. Megnetron sputtering coating is a promising Ti/porcelain interlayer.

Aluminum ; chemistry ; Ceramics ; chemistry ; Chromium ; chemistry ; Coated Materials, Biocompatible ; chemistry ; standards ; Dental Bonding ; Dental Porcelain ; chemistry ; Dental Stress Analysis ; methods ; Metal Ceramic Alloys ; chemistry ; standards ; Nitrogen ; chemistry ; Surface Properties ; Tensile Strength ; Titanium ; chemistry

OBJECTIVETo investigate the effects of the Chinese herbal medicine of Longbixiao (LBX) Capsule on the expressions of TGF-beta1 and Smoothelin in human prostatic stromal cells cultured in vitro.

METHODSBlood serum medicated with LBX was incubated with the stromal cells isolated from men with benign prostatic hyperplasia (BPH) and cultured in vitro. The mRNA expression levels of TGF-beta1 and Smoothelin were detected by real-time RT-PCR and other relevant techniques.

RESULTSIn the high and low concentration groups, the gene relative expressions of TGF-beta1 were (0.158 +/- 0.020) and (0.169 +/- 0.020) , while those of Smoothelin were (0.035 +/- 0.007) and (0.036 +/- 0.007) respectively, both significantly decreased in comparison with the control group(P < 0.01).

CONCLUSIONLBX reduces the mRNA expressions of TGF-beta1 and Smoothelin in human prostatic stromal cells and can be used in the treatment of BPH.

Animals ; Capsules ; Cells, Cultured ; Cytoskeletal Proteins ; genetics ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Gene Expression ; drug effects ; Humans ; Male ; Muscle Proteins ; genetics ; Prostatic Hyperplasia ; pathology ; Rabbits ; Reverse Transcriptase Polymerase Chain Reaction ; Serum ; chemistry ; Stromal Cells ; drug effects ; metabolism ; pathology ; Transforming Growth Factor beta1 ; genetics

OBJECTIVETo investigate the relationship between the -308G/A, -857C/T and -1031T/C of tumor necrosis factor alpha gene (TNF- alpha), -174G/C and -572C/G of interleukin-6 gene (IL-6) polymorphisms and schizophrenia.

METHODSGenomic DNA was isolated from the venous blood leukocytes of 346 unrelated patients with schizophrenia and 323 healthy unrelated individuals (control group). All of the polymorphisms were genotyped by PCR-restriction fragment length polymorphisms (PCR-RFLP). Genotype and allele frequencies were analyzed by SPSS13.0 software.

RESULTSThere were significant differences in both allele and genotype frequencies of -857C/T of TNF-alpha gene between the schizophrenia and control groups (P< 0.05). The allele T of -857C/T in schizophrenia group was significantly higher than that in control group (chi-square was 9.414, P=0.002, OR=1.511, 95%CI:1.160-1.969). In addition, there were significant differences in the positive and negative syndrome scale (PANSS) total score and negative symptoms between the patients with different -857C/T genotypes, and the negative symptom score of TT genotype was significantly higher than that of CC genotype (P<0.05).

CONCLUSIONThere is an association between -857C/T of TNF-alpha gene and schizophrenia, individuals with T allele of -857C/T are susceptible to schizophrenia, and there is an association between -857C/T and negative symptom score.

Adult ; Case-Control Studies ; Female ; Gene Frequency ; Genotype ; Humans ; Interleukin-6 ; genetics ; Male ; Phenotype ; Polymerase Chain Reaction ; Polymorphism, Genetic ; genetics ; Polymorphism, Restriction Fragment Length ; Promoter Regions, Genetic ; genetics ; Schizophrenia ; genetics ; Tumor Necrosis Factor-alpha ; genetics ; Young Adult

Objective To explore the feasibility of fabricating a self-powered and implantable stimulator . Methods Based on pyroelectric effect and high penetrability of infrared ray , an implantable stimulator was designed and fabricated .The electrical performance of stimulator was measured under infrared ray illumination .We conducted the animal experiments in vitro and in vivo to observe the response of gastrocnemius contraction under stimulation .Results The stimulator could output the electrical signal under the periodical infrared ray illumination .The output voltage and current were proportional to the intensity of infrared ray ,which could reach up to 1 .2 V . A real-time electrical stimulation of frog gastrocnemius was conducted and obvious contraction was observed .The tension values increased with the increase of infrared intensity .We further carried out the in vivo experiment with a frog in order to evaluate the performance of the stimulator after being implanted into the body . The gastrocnemius would also be made to contract even though the infrared intensity decayed when through the skin .Conclusion The proposed pyroelectric stimulator can be self-powered and controlled through near-infrared illumination .This study can provide some guidance for solving the problems of implantable power .

Forensic dentistry is an interdiscipline of forensic medicine and stomatology, which provides legal information by collecting, testing and assessing the dental evidence scientifically. In this review, the present application of forensic dentistry has been described, such as the estimation of age, sex, species, occupation and living habit, as well as the identification of individual, domestic violence or abuse, which aims to enrich and improve forensic dentistry for making it be more useful in forensic medicine even in juridical practice.
Age Determination by Teeth ; Forensic Anthropology ; Forensic Dentistry/methods* ; Forensic Medicine ; Humans ; Tooth