AIM:To optimize formulation of Xiao'er Magan Orally Disintegrating Tablet by central composite design-response surface methodology. METHODS:By two factors and five levels central composite design,independent variables were the proportion of optimized microcrystalline cellulose 50 and mannitol and the pressure,while disintegrating time and tensile strength were dependent variables. Binary linear and quadratic models were used to estimate the relationship between the dependent and the indepedent variables,and to delineate response surface method and overlay contour plots in order to select the optimal formulations. RESULTS:The binomial regression equation were TS =0. 096 88X1 + 0. 027 6X1X2(r = 0. 759),DT = 9. 845 4X1 -63. 196X2 + 40. 092 9X22 (r = 0. 838) which indicated the quantitative relationship between the factors and the evaluation indexes was characterized. The optimal formulation were the ratio of microcrystalline cellulose 50 and mannitol in the range of 0. 35 and 0. 6,and the pressure was in the range of 6 and 8 KN. CONCLUSION:The optimized formulation validation is close to the estimated value,indicating that the method has a good predictability and reliability.

Adolescent ; Adult ; Anti-Inflammatory Agents ; therapeutic use ; Diagnosis, Differential ; Dipyridamole ; therapeutic use ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Lupus Erythematosus, Systemic ; drug therapy ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Phytotherapy ; Prednisone ; therapeutic use ; Tripterygium ; chemistry

Objective To explore the effects of polymorphisms of Crohn's disease related NOD2 gene and human beta-defensin 2 (hBD-2) on transcription of hBD-2 gene and its mechanism. Methods HEK293T cells were transfected with hBD-2 gene and NOD2 eukaryotic expression plasmid, and were then stimulated with LPS, TNF-α, or BAY 11-7082 (antagonist of NF-κB), respectively. Transcriptional activity of hBD-2 was detected afterwards. Results LPS could suppress transcription of hBD-2 (P=0. 020), which was increased by TNF-α in a dose-dependent manner (P =0. 004). In the presence of LPS, there was sig-nificant difference in transcriptional activity of hBD-2 between wild-NOD2 transfected group and mutated NOD2 (P268S) transfected group (P=0. 008), but there was no significant difference between wild hBD-2 transfected group and mutated hBD-2 transfected group (P=0. 053). With the stimulation of TNF-α (5 ng/ml), there was a significant difference between mutated hBD-2 transfected group and wild hBD-2 transfected group (P=0. 006), but no significant difference between wild-NOD2 transfected and mutated NOD2 transfected group was defected (P = 0. 064). Pretreatment with BAY 11-7082 before TNF-α (5 ng/ml) significantly inhibited the transcriptional activity of hBD-2 (P < 0. 001). Conclusion The poly-morphism of NOD2 affects the innate expression of hBD-2, the polymorphism of site in hBD-2 promoter (-233) may lead to significant decline of the inducible expression of hBD-2, and NF-κB might be a key pathway that NOD2 protein mediates the expression of defensin.

Objective To investigate the association of two single nuclear peptides(SNPs)polymorphisms(rs11209026 and rs11805303)which lies in interleukin-23 receptor(IL23R)gene with susceptibility to inflammatory bowel disease(IBD).Methods The target SNPs were directly sequenced by polymerase chain reaction(PCR)and gene polymorphisms of 50 healthy and 81 patients with IBD (Crohn's disease in 41 patients and ulcerative colitis in 40 patients)were analyzed using chromassoftware.Results The geno-type frequency and allelic frequency of rs11209026 were 7.3%and 3.7%in patients with Crohn's disease respectively,15.0%and 7.5%in patients with ulcerative colitis respectively as well as 14.0%and 7.0%in normal population respectively(all P value＞0.05).The geno-type frequency and allelic frequency of rs11805303 were 22.0%and 52.4%in patients with Crohn's disease respectively,15.0% and 41.2% in patients with ulcerative colitis respectively as well as 34.0%and 59.0%in normal population respectively(all P value＞0.05).But in allelic frequency there was significant difference between ulcerative colitis patients and normal population(P=0.018).The polymorphisms of rs11805303 loci did not correlate with age,gender,disease duration.activity and site in patients with ulcerative colitis.Conclusions IL23R gene polymorphism is not associated with the susceptibility to Crohn's disease.rs11805303 allele may be related with susceptibility to ulcerative colitis.But no correlation was found between the SNP polymorphisms and the clinical characteristic of ulcerative colitis.

0.05).The adverse effect of treatment group was significantly less than control group(P

Objective To investigate the clinical characteristics and diagnostic main points of poliomyelitis-like syndrome(PS).Met-hods The clinical data of 15 children with PS were analyzed retrospectively including nervous system manifestation,results of lab andauxiliary examination,diagnosis and reason of misdiagnosis,treatment and progress.Results PS in all 15 children was characterized by mean age of onset(3.3 years),and forerunner infection(in 11 cases,73%)with acute upper respiratory infection of diarrhea 1-2 weeks pre-onset or during onset.All cases were acute flaccid paralysis,12 cases(80%) of which were only one limb.The positive outcome of serologic examination in PS consisted of 4 cases in coxsackie virus-IgM,1 case in EB virus-IgM,1 case in herpes simplex virus-IgM and 1 case in mycoplasma-IgM.All children showed the electromyologram changes in nerve damage.The muscle force of 4 cases increased one grade.Conclusions Children with PS are characterized by the age of onset under 5 years old,acute flaccid paralysis(mostly affected one limb),and the most pathogen being enterovirus.The electromyologram examination can help establish a definite diagnosis in PS.

Objective To explore the risk factors affecting prognosis of children with Tourette syndrome(TS).Methods The follow-up visits were conducted on the clinical data of 98 cases with TS(85 male,13 female;aged 4-16 years old)from 1997 to 2005 in Wuhan children's hospital.All cases were consistent with the diagnostic criteria of TS in the 4th edition of Diagnostic and Statistical Manual of Mental Disorders(DSM-Ⅳ).The investigations were performed by the investigators who received special training using the unified questionnaire with the methods of direct inquiry or by telephone.The factors included sex,age,severity of TS,the primary symptoms,family history,coexisting diseases,basic diseases,perinatal abnormity and family-social relations.The prognosis of TS and these factors were analyzed by linear regression and stepwise regression with SPSS 12.0 software.Results About 16 cases lost follow-up and the other 82 cases with follow-up(72 male and 10 female)received retrospective review.They were 14 to 25 years old with complete data,and 50 cases healed,32 cases not healed.Results from non-conditional simple variant Logistic regression showed that such cases were associated with the following factors:age,family history of TS,severity of TS,coexisting diseases,basic diseases and perinatal abnormity(Pa0.05).Out of 6 suspicious factors,there were coexisting diseases(OR=84.088,95%CI 10.850-651.682),severity of TS(OR=13.956,95% CI 2.412-80.762),and family history of TS(OR=27.127,95% CI 1.047-702.831)of risk factors.Conclusion The long-term prognosis of children with TS may be related with coexisting disease,severity of TS and family history respectively.

ObjectiveTo investigate the occurrence of new cretinism cases and the prevalence of endemic goiter in iodine deficiency disorders(IDD) high-risk areas of Fujian province,so as to put forward target prevention and control measures for these areas.Methods Twelve counties from Xiuyu,Xiangan,Pingtan,and Dongshan were chosen into the survey by simple random sampling,searching for new cretinism cases were carried out in children under 10 years old.Two schools were chosen in every county and the thyroid volume of forty children aged 8 - 10 were determined by B-ultrasonography methods and their urinary iodine(UI) was determined by As3--Ce4+catalytic spectrophotometry in each school.Twenty women of child-bearing age aged 18 - 40 were chosen for collecting edible salt and urine samples,and the salt iodine content was determined using self-quantitative kit and their UI was also determined by As3--Ce4+ catalytic spectrophotometry.Results In the 4 high-risk counties,no cretinism cases were found.The goiter rate of children aged 8 - 10 was 3.6％(37/1027),and that in Dongshan county was 5.4％(13/240),which was higher than the national standards for eliminating IDD( ＜ 5％).The median urinary iodine(MUI) of children aged 8 - 10 was 175.3 μg/L,and the MUI of women aged 18 -40 was 152.7 μg/L.The coverage rate of iodized salt was 82.7％(382/462).ConclusionsNew case or suspected new case of cretinism is not discovered in the high-risk areas of IDD of Fujian province,and median urinary iodine level of people is in the adequate range.

Organic anion transporting polypeptide 1B1 (OATP1B1) is an important liver-specific uptake transporter, which mediates transport of numerous endogenous substances and drugs from blood into hepatocytes. To identify and investigate potential modulators of OATP1B1 from natural products, the effect of 21 frequently used natural compounds and extracts on OATP1B1-mediated fluorescein methotrexate transport was studied by using Chinese hamster ovary cells stably expressing OATP1B1 (CHO-OATP1B1) in 96-well plates. This method could be used for the screening of large compound libraries. Our studies showed that some flavonoids (e.g., quercetin, quercitrin, rutin, chrysanthemum flavonoids and mulberrin) and triterpenoids (e.g., glycyrrhetinic acid and glycyrrhizic acid) were inhibitors of OATP1B1 with IC50 values less than 16 µmol · L(-1). The IC50 value of glycyrrhetinic acid on OATP1B1 was comparable to its blood concentration in clinics, indicating an OATPlB1-mediated drug-drug interaction could occur. Structure-activity relationship analysis showed that flavonoids had much higher inhibitory activity than their glycosides. Furthermore, the type and length of saccharides had a significant effect on their activity. In addition, we used OATP1B1 substrates fluvastatin and rosuvastatin as probe drugs to investigate the substrate-dependent effect of several natural compounds on the function of OATP1B1 in vitro. Our results demonstrated that the effect of these natural products on the function of OATPlB1 was substrate-dependent. In summary, this study would be conducive to predicting and avoiding potential OATP1B1-mediated drug-drug and drug-food interactions and thus provide the experimental basis and guidance for rational drug use.
Animals ; Biological Products ; CHO Cells ; Cricetulus ; Drug Interactions ; Fatty Acids, Monounsaturated ; pharmacology ; Flavonoids ; pharmacology ; Indoles ; pharmacology ; Inhibitory Concentration 50 ; Organic Anion Transporters ; genetics ; metabolism ; Rosuvastatin Calcium ; pharmacology ; Structure-Activity Relationship

Two Pseudomonas strains, K80 - B and K80 - A, can use hydrocarbon as carbon source by two different mechanisms. Different effects can be observed when they are applied to 69-8 oil of Dagan Oil Field. The strain K80-B producing both hydrocarbon pseudosolubilizing factor and hydrocarbon emulsifying factor can decrease the viscosity and solidifying point of the 69-8 oil 51.6% and 2℃ respectively. Whereas the other can only decrease 43.5% and 3℃ respectively. When the two strains are mixed, synergistic effect on crude oil is obvious.