Human protein tyrosine kinases play an essential role in carcinogenesis and have been recognized as promising drug targets. By the end of 2012, eight small molecule tyrosine kinase inhibitors (TKIs) have been approved by State Food and Drug Administration of China for cancer treatment. In this paper, the pharmacokinetic characteristics (absorption, distribution, metabolism and excretion) and drug-drug interactions of the approved TKIs are reviewed. Overall, these TKIs reach their peak plasma concentrations relatively fast; are extensively distributed and highly protein bound (> 90%); are primarily metabolized by CYP3A4; most are heavily influenced by CYP3A4 inhibitors or inducers except for sorafenib; are mainly excreted with feces and only a minor fraction is eliminated with the urine; and are substrate of the efflux transporters ABCB1 (P-gp) and ABCG2 (BCRP). Additionally, many of the TKIs can inhibit some CYP450 enzymes, UGT enzymes, and transporters. Gefitinib, erlotinib, dasatinib, and sunitinib are metabolized to form reactive metabolites capable of covalently binding to biomolecules.

Objective To observe the clinical efficacy of rigid gaspermeable contact lens (RGPCL) for correcting keratoconus and analyze the predictors for the base curve of RGPCL.Methods Data of 86 patients (143 eyes) with keratoconus fitted with RGPCL were retrospectively analyzed.All eyes were divided into the mild (n =18 eyes),moderate (n =73 eyes),advanced (n =34 eyes) and severe group (n =18 eyes).After evaluating the lens fitting,best corrected visual acuity of eyes wearing spectacle lenses and RGPCL among the 4 groups was statistically compared.And the correlation between the fitting guidance index and HL-K RGPCL base curve in each group was analyzed according to keratometry.Results All patients wearing RGPCL gained significantly better corrected vision in the mild (t =-3.336,P =0.004),moderate (t =-11.213,P ＜0.001),advanced (t =-13.959,P ＜0.001) and severe groups(t =-11.047,P ＜0.001) than those with spectacles.Equivalent spherical degree of spectacle lenses was lower than the diopter of HL-K RGPCL in the moderate (P =0.043) and severe group (P =0.006).The mean base curve of RGPCL was (50.52 ±5.64) diopter,and it was correlated with corneal curvature parameters.In mild group,the RGPCL base curve was correlated with the steep keratometry (P ＜ 0.001).The average K and relative steep K of 0.2 mm (Rm-0.2) were highly correlated with RGPCL base curve in moderate group (r =0.798,P ＜ 0.001;r =0.798,P ＜ 0.001),in advanced group (r =0.745,P ＜ 0.001;r =0.745,P ＜ 0.001) and in severe group (r =0.616,P =0.007;r =0.617,P =0.006).Conclusion Patients with keratoconus wearing HL-K RGPCL can obtain ideal corrected vision.Determination of RGPCL base curve by adjusting the corresponding indicators is conducive to improving the long-term wearing safety of the lens and enhancing the efficiency of lens fitting.

Obiective: To compare the tissue biocompatibility of domestically manufactured NiTi alloy before and after thermal surface oxidation under 3 different temperatures. Methods: Domestically manufactured NiTi alloy was oxidized in air (group A) and subjected to 30 min heat treatment at 400°C (group B),500°C, (group C),and 600°C (group D) to form different protective oxide surface layers in presence of argon (607.95 kPa). Wire samples from A, B, C and D groups were subcutaneously implanted in guinea pigs. Guinea pigs received 317L stainless steel transplantation(group E) and sham-operation group (F) were taken as control. The order of inflammatory cell infiltration and tissue hyperplasia around implanted materials were observed 1, 2, 4, and 8 weeks after implantation. Results: The peak time of inflammatory cell infiltration and fibrous hyperplasia were at the first and fourth week after implantation. The inflammatory cell infiltration and fibrous hyperplasia were both slight and all met the GB/T 16886. 6-1997 in vivo implantation standard. The order of inflammatory cell infiltration and thickness of capsule walls from low to high was F

Objective To evaluate the effect of a bioartificial liver (BAL) system for treatment of acute liver failure (ALF) in canines and its relationship to serum endotoxin. Methods ALF was induced by end-side portocaval shunt combined with common bile duct ligation and transection. Ten ALF canines were distributed to BAL group (n=5), or to a control group (n=5). Each BAL circulation lasted 5h. Serum endotoxin, alanine aminotransferase (ALT) and total bilirubin (TB) before establishment of ALF model, pre-circulation and post-circulation were determined. Results Serum endotoxin level was 0.284 EU/ml, 0.526 EU/ml and 0.416 EU/ml before establishment of ALF model, and pre-circulation and post-circulation in BAL group, respectively. The serum endotoxin level in BAL group increased pre-circulation (P

In this paper, the application of 霤/OS-II, one of the real-time oper ation systems (RTOS), to ECG tele-monitoring system based on mobile communicatio n is introduced. The system is composed of monitoring terminals and a monitoring center. The terminals have functions such as ECG data acquisition and storage, real-time data analysis, keyboard input, LCD display, system monitor and automat ic transmission of abnormal ECG data to the monitoring center through mobile com munication network. Because these functions are not executed simultaneously, mul ti-task management is adopted instead of single task management. In Rabbit2000 m ain controller, 霤/OS-II is applied to multi-task management.

Adenoma, Pleomorphic ; Adult ; Female ; Humans ; Nose Neoplasms

The hypothesis that tumor comes from stem cells has been demonstrated in various human tumors.Cancer is not only a genetic disease but also a stem cell disease. It is a key to regeneration, mutations and recurrence of tumors that gene mutations affect stem cells, and then stem cells mutate to cancer stem cells. In an effort to review the evidence that liver cancer stem cells exist, two fundamental questions must be addressed. First, do hepatocellular carcinomas(HCC)arise from liver stem cells? Second, do HCCs contain cells that possess properties of cancer stem cells?More recently, there is a hypothesis that HCC arise from maturation arrest of liver stem cells. Analysis of the cells in HCC supports the presence of cells with stem-cell properties(ie, immortality, transplantability, and resistance to therapy). However, definitive markers for these putative cancer stem cells have not yet been found and a liver cancer stem cell has not been isolated.

Objective To investigate the clinical significance of dynamic change of serum IL‐17A/IL‐23 in131 I treatment of Graves hyperthyroidism by dynamically detecting the serum IL‐23/Th17 axis related factor levels before and after 131 I treatment of Graves hyperthyroidism .Methods 30 untreated inpatients with Graves disease(GD) in our hospital were selected as the T0 group , those treated by 1- ,3- ,6-month 131 I treatment were taken as the group T1 ,T3 and T6 .Contemporeneous 30 individuals under‐going healthy physical examination were selected as the normal control (NC) group .The various groups had no statistical differences in the aspects of the age ,gender and disease course ,and had the comparability (P>0 .05) .Serum concentration of IL‐17A and IL‐23 was measured by the enzyme‐linked immunosorbent assay (ELISA) technique .FT3 ,FT4 and TSH were detected by combing with clinic .Results The levels of serum IL‐17A and IL‐23 before131I treatment were significantly higher than those in the NC group(P<0 .05);with the treatment proceeding ,which at ,1 ,3 ,6 months were gradually decreased ,the differences were statistically signifi‐cant but(P<0 .05);after 6 -month 131 I treatment in the GD patients ,the effects of IL‐17A and IL‐23 double negative in the T6 group were better than those of single negative ,and better than those of double positive ,the differences were statistically (Fisher value=13 .273 ,P<0 .05) .Conclusion Dynamically monitoring the serum IL‐23/Th17 axis related factor levels has the significance for guiding treatment ,judging the curative effect and predicting recurrence .

Objective To study the anatomical character of compartment syndrome of foot after calcaneal intra-articaular by experimental model. MethodSix intact human cadaver lower extremities were used to produce calcaneal intra-articular fracture models, fracture patterns of the model were observed with radiographical technique, and anatomical study was proceeded to observe the fractures and their effects on soft tissues and compartments in foot.ResultAll specimens were sustained calcaneal intra-articular fractures successfully, 4 were joint depression fracture in x-ray, 2 were tongue type; 3 were Sander Ⅱ type and others were Sander Ⅲ type in CT. the primary fracture line coursed from anterolateral to posteromedial, and from anterosuperior to posteroinferior. It damaged all the soft tissue arosed from fractures medially and laterally, included adductor hallucis,quadratus plantae, flexor digitorum brevis and abductor digiti minimi as well.ConclusionFrom anatomical view, soft tissues of many compartments in foot rather than of simple compartmen are injuried when calcaneal intra-articular fractures occur, decompressive fasciotomies should be performed in all compartments involved. The present experimental protocol is useful to reproduce calcaneal intra-articular fractures.

Objective:To observe the ratio of the syndrome of deficiency in origin to the syndrome of excess in superficiality in chronic renal failure(CRF)and co-existent states,and to analyze the relationship between TCM syndrome types and related biochemical indexes.Methods:TCM syndrome differentiation was carried out and related biochemical indexes were determined in 146 cases of CRF.The data were compared and analyzed with single factor analysis of variance between groups.Results:(1)Deficiency of both qi and yin of spleen and kidney was the most frequently-appeared type in the deficiency syndrome,and damp-heat syndrome was the most frequently-appeared type in the excess syndrome;(2)Serum creatinine(SCr)and blood uria nitrogen(BUN)in the patient of damp-turbid syndrome in the excess syndrome were significantly higher than those in the patient of damp-heat and blood stasis syndrome;(3)Fibrin in the patient of blood stasis was significantly higher than that in damp-heat syndrome and damp-turbid syndrome.Conclusion:Generation and development of CRF are closely related with dampness syndrome,usually marked by syndrome of damp-turbid,damp-heat,blood stasis,damp-stagnation,and was mainly related with abnormal renal function and hemorheologic indexes in the biochemical indexes.