AIM: To investigate the effectiveness of dosing technology and excipient application on solid drug's moisture-proof property and to provide a method improving the solid drug's moisture-proof property. METHODS: Based on the analysis of the moisture absorbing process and the absorbing mechanics,a new concept "active moisture absorbance site"(AMAS) was defined and mathematic model was constituted.Two constants as: initial AMAS concentration C_0,moisture resistance coemcient K,were proposed to indicate the drugs moisture-proof ability. The CI WU JIA extracts and SHUANG HUANG LIAN extracts were used to conduct experiments, which were designed to investigate the improvement of the drug's moisture resistance ability when varying the AMAS's concentration and/or its space distribution. RESULTS: Reducing the amount of moisture absorbance excipients in each dosage of solid drug can lower the drug's moisture absorbance ability,and applying a thin film coating material outside the drug can also slow the drug's moisture absorbance rate. CONCLUSION: The proposed mathematic model is useful for finding a way to improve the drug's moisture resistance;experimental data shows that the drug's moisture-proof property would be improved by reducing the amount of moisture absorbance excipient in each dosage and improving the moisture distribution resistance through a certain dosing technology,such as film coating technology.

Objective To explore the molecular and cell signal transduction mechanism of Astragalus mongholicus polysaccharides (ASP) on macrophage. Methods After stimulating RAW264.7, the change in value of NF-κB was determined by Western blot. The induction of NO and secretion of TNF-α by ASP in macrophage was observed with or without inhibitor of NF-κB using Griess method. Moreover, protein levels of TNF-α secreted by macrophage were investigated with ELISA in respond to ASP. Results 4 h after stimulation by 100 μg/ml ASP, the concentration of NF-κB in nucleus increased significantly, peaked at 6 h. 16 h after stimulation by 100 μg/ml ASP, the activity of iNOS[(23.54±2.41) U/mg protein; P<0.01], producton of NO [(18.9±1.5)μmol/L, P<0.01] and level of TNF-α[(81.2±16.7)pg/ml, P<0.0l] in macrophage were improved markedly. Blocking NF-κB with inhibitor results in decreased levels of NO and TNF-α. Conclusion The results suggest that NF-κB play an important role in induction of NO and TNF-α by ASP in macrophage.

On the basis of the investigation of the pathogenesis of cervical spondylotic radiculopathy, this paper studies the mechanisms of spinal micro-adjustment manipulations in recovering and improving cervical dynamic and stationary balance from the perspective of biomechanics.

Objective To determine the median effective target plasma concentration (Cp50) of remifentainil inhibiting body movement evoked by puncture during brachial plexus block in pediatric patients.Methods Pediatric patients of both sexes,aged 5-12 yr,who grown normally,scheduled for elective forearm or hand surgery,were enrolled in this study.Children were premedicated with oral midazolam 0.2 mg/kg at 30 min before anesthesia.The initial target Cp of remifentainil was 5.0 ng/ml.The target Cp was determined by up-and-down sequential method.Each time Cp increased/decreased by 20％ in the next patient depending on the response of the previous patient to puncture.The ratio between the two successive concentrations was 1.2.The puncture was performed after the target effect-site and plasma concentrations were balanced.Body movement was defined as puncture-induced movement of truncus,limbs and/or head and neck.The Cp50 and 95 ％ confidence interval of remifentainil were calculated by Dixon method.Results Cp50 of remifentainil inhibiting body movement evoked by puncture during brachial plexus block was 3.9 ng/ml,and 95 ％ confidence interval was 3.6-4.2 ng/ml.Conclusion Cp50 of remifentainil inhibiting body movement evoked by puncture during brachial plexus block is 3.9 ng/ml in pediatric patients.

AIM: To establish a model of subtotal nephrectomy (SNx) and investigate the changes of apoptosis and apoptosis-related genes (Bax, bcl-2, caspase-3, caspase-8 and caspase-9) in the rat remnant kidney. METHODS: Remnant kidneys were produced in adult male SD rats by 5/6 nephrectomy. The renal function and histopathological changes were evaluated at 1, 2, 4, 8, 12, 16, 26 and 40 weeks after operation. The tissues of remnant kidneys were collected to detect apoptosis cells by in situ end-labeling of cleaved DNA (TUNEL) and proliferating cells by determining the proliferating cell nuclear antigen (PCNA). The expression of Bax, bcl-2, caspase-3, caspase-8 and caspase-9 was measured by RT-PCR and Western blotting. The proteins were detected by immunohistochemistry staining. The relation between apoptosis, proliferation, glomerulosclerosis and renal interstitial fibrosis was also observed. RESULTS: The results showed the renal pathological dynamic changes in 5/6 nephrectomy remnant kidneys were tubule-interstitial inflammation and fibrosis, as well as glomerulosclerosis. There were transient increases in both proliferating and apoptotic processes in glomerulus, tubules and interstitium. Apoptosis was increased and most of apoptotic cells were detected in tubular epithelial cells and interstitial area. The mRNA and protein expression of Bax, caspase-3, caspase-8 and caspase-9 were increased in all course, and peaked at week 4 and 40 in the SNX rats. The successive changes of these parameters were parallel to the level of focal inflammation in interstitium. Glomerulosclerosis index was related with focal inflammation cells and 24 hours urine protein (r=0.788, 0.822; P

To investigate the role and mechanisms of apoptosis and apoptosis signaling pathway in 5/6 nephrectomy rat model (SN(x)), the mRNA and protein levels of caspase-3, -8, -9 and apoptosis were detected by in situ end labeling (TUNEL), immunohistochemistry, RT-PCR, Western-blotting 1, 2, 4, 8, 12, 16, 26 and 40 weeks after 5/6 nephrectomy rat model was made respectively. The rats in the model group developed glomerular sclerosis and renal interstitial fibrosis. The number of the apoptototic cells in glomeruli, renal tubule and renal interstitium was remarkably higher in the model group than that in the control group (P < 0.05, P < 0.01). Changes of mRNA and protein level of caspase-3, -8, -9 had the same tendency and was up-regulated wavily in the rat model compared with the control group (P < 0.05). Peaks in model appeared on the 4th and the 40th week respectively. The growth amplitude of caspase-9 was remarkably higher than that of caspase-8. It is concluded that the development of 5/6 nephrectomy rat model was correlated with the apoptosis of glomeruli, renal tubule and renal interstitium. Both of death receptor and mitochondria signaling pathways are involved in the process and the latter might play a primary role.

Abstract? AlM: To evaluate macular thickness and macular volume changes in people with diabetes mellitus but no significant decrease of visual acuity.?METHODS:A total of 87 eyes were collected in diabetic group. According to the international stage of diabetic retinopathy, these cases were divided into two subgroups:DR0 stage 54 eyes and DR1 stage 33 eyes. All the cases were received optical coherence tomography (OCT) scan in macular area;the scanning model is 512× 128; recording macular average thickness and macular volume, and compared with healthy subjects.? RESULTS: Macular average thickness and macular volume were higher in DR1 group than those in DR0 stage and control group, and differences were having statistical significance. But DR0 group and control group differences of the two indexes were not statistically significant.? CONCLUSlON: With the aggravation of diabetic retinopathy, the macular thickness tends to be thicken. Although without obvious visual loss, there have been slight morphological changes. Using OCT scan can find fundus changes earlier in patients with diabetes mellitus, and provide clinical basis for both early diagnosis and treatment.

Objective To study the effect of behavioral therapy combined with Paroxetine in the treatment of overactive bladder accompanied by depression and anxiety.Methods Over the past two years,a total of 69 cases of patients with overactive bladder accompanied by depression and anxiety were diagnosed by outpatient,they were divided into experimental group (n=33)and control group(n=36).The experimental group were given behavior therapy and Paroxetine in the treatment of anxiety,depression,while the control group were given behavior therapy.Then the overactive bladder symptom score(OABSS),urgency score,SDS,SAS score before and after treatment of the two groups of patients were statistically analyzed.Results (1)The OABSS score ((3.30± 1.01) vs (7.51 ± 0.69)),urgency score((2.60±0.51) vs (3.93±0.69)),SDS score((43.1±6.2) vs (66.4±4.7)) and SAS score ((41.9±0.6) vs (61.4±3.9)) decreased after treatment of the experimental group.There were statistically significant compared with before treatment(t=17.8773,8.9045,17.2039,16.0273,all P＜0.01).(2) The OABSS score,urgency score decreased after treatment of the control group.There were statistically significant compared with before treatment (t=6.1926,6.3483;both P＜0.01).SDS,SAS score before and after treatment of the control group were not statistically significant (t=1.3105,0.5852,bothP＞0.05) (3) The OABSS score,urgency score,of the experimental group were more depressed than the control group,which were statistically significant (t =3.3830,3.6391,both P＜0.01).Conclusion For overactive bladder patients with anxiety and depression,behavioral therapy combined with Paroxetine is better than behavioral therapy alone.

OBJECTIVESTo investigate the changes of nuclear factor (NF)-kappaB activation in lung tissues and expression of cytokines in homogenate from lung tissues in infant rabbits with mechanical ventilation (MV) caused lung injury.

METHODSForty-five general grade healthy infant rabbits were randomly divided into 3 groups: (1) CONTROL: with no MV (NMV, n = 9); (2): Conventional MV (CMV, n = 9): V(T) = 8 ml/kg; (3): MV with large tidal volume (V(T)) (LMV, n = 9), V(T) = 24 ml/kg. NF-kappaB activity in nuclear protein from lung tissues was measured with electrophoretic mobility shift assay (EMSA); quantity of IkappaBalpha in cellular plasma from lung tissues was analyzed with Western blotting method; TNF-alpha and IL-8 mRNA and their concentrations in homogenate were measured from lung tissues with RT-PCR and ELISA, respectively.

RESULTSAt all time points NF-kappaB activity was higher in LMV than that in CMV and NMV groups (P < 0.01). Quantity of IkappaBalpha decreased progressively in LMV with time (P < 0.01) as compared to CMV and NMV. The expressions of TNF-alpha and IL-8 and their protein quantity in lung tissues significantly increased in LMV after ventilation compared to that in CMV and NMV (P < 0.01). The expression level of TNF-alpha reached its peak at 4 hrs and IL-8 at 6 hrs after ventilation then TNF-alpha decreased significantly at 6 hrs after ventilation. Pathological examination of the lung tissues showed that as MV extended over the time in LMV, alveolar structures were severely destroyed and large number of WBC infiltrated in both alveolar sacs and pulmonary interstitia with RBC leakage. However, there was less lung injury in CMV and no obvious injury in NMV.

CONCLUSIONSIkappaBalpha degradation and NF-kappaB activation were involved in modulating the expression of pro-inflammatory cytokines in lung tissues during the occurrence of lung injury caused by injuring MV.

Animals ; Animals, Newborn ; Blotting, Western ; Disease Models, Animal ; Electrophoretic Mobility Shift Assay ; Enzyme-Linked Immunosorbent Assay ; Interleukin-8 ; genetics ; metabolism ; Lung ; metabolism ; NF-kappa B ; metabolism ; RNA, Messenger ; metabolism ; Rabbits ; Random Allocation ; Reverse Transcriptase Polymerase Chain Reaction ; Tidal Volume ; Tumor Necrosis Factor-alpha ; genetics ; metabolism ; Ventilator-Induced Lung Injury ; metabolism

The high and continuing soaring incidence of diabetes may become a huge obstacle to China's development. The antidiabetic drug development is one way to solve the problem. Animal model is a powerful tool for drug development. This paper compares and analyzes the three kinds of animal models for antidiabetic drug development in replicating principle, methods and characteristic, then summarized the application in the research of traditional Chinese medicine. At the same time, the analysis of the market, application and clinical advantages of hypoglycemic medicine from traditional Chinese medicine, is given in this paper, based on the literature analysis. From the point of the clinic advantage embodiment and new drug development, this paper will provide advisory and assistance support for the anti-diabetic fighting with traditional Chinese medicine.
Animals ; China ; Diabetes Mellitus ; drug therapy ; Disease Models, Animal ; Drug Discovery ; Humans ; Hypoglycemic Agents ; Medicine, Chinese Traditional