BACKGROUND:The faults or defects in pharmaceutical dosage form designed for carbamazepine may lead to irregular drug absorption, great individual differences between the pharmacokinetics, narrow therapeutic concentration range, and the therapeutic drug monitoring for this drug. OBJECTIVE:To prepare a magnetic/pH double sensitive hydrogel beads carrying carbamazepine and to evaluate its properties. METHODS:Using chitosan, alginate and Fe3O4 nanoparticle as carrier materials, the magnetic/pH double sensitive hydrogel beads carrying anti-epileptic carbamazepine were prepared, and the composition and preparation technology were optimized by orthogonal test of L9(34). The surface morphology and structure of the hydrogel beads were characterized by scanning electron microscopy and Fourier transform infrared spectroscopy respectively. Also, the superparamagnetism, swel ing and release in vitro of hydrogel beads were determined. RESULTS AND CONCLUSION:The optimized preparation technology were described as:0.5%(w/v) chitosan, 1.5%(w/v) alginate, 2.0%(w/v) calcium chloride, and 1:2 ratio for magnetic versus carrier materials. The hydrogel beads under the optimal preparation conditions showed a round shape and smooth surface, and average encapsulation efficiency, loading efficiency and hydrogel beads diameter were 94.36%, 25.05%and 1-2 mm respectively. The hydrogel beads appeared to have superparamagnetism, the swel ing degrees were associated with pH value of medium, and the sequential release amount of carbamazepine from the hydrogel beads in simulated gastric fluid was 22.77%for 2 hours. Then, the beads were moved to the simulated intestinal fluid, and this value approached 91.63%for 24 hours. Experimental findings indicate that, the composition and preparation technology of magnetic/pH double sensitive hydrogel beads carrying carbamazepine was rational and feasible, and hydrogel beads show obvious pH sensitivity and magnetic sensitivety. The control ed-release effect of hydrogel beads in vitro is also good.

AIM: To find out whether traditional Chinese medicine Angelicae Sinensis has direct suppressive effect on schistosome egg-induced granulomatous response. METHODS: The lung model of granuloma response was established by injecting living eggs of Schistosoma japonicum into the tail veins of eggs-sensitized mice then the preparation of Angelicae Sinensis were given intraperitoneally once a day for ten days. In vitro model of granulomatous reaction was set up by incubating dry schistosome eggs together with those splenocytes isolated from schistosome infected-mice or from the mice with pulmonary granuloma formation. Different doses of the preparation was, in the need of experiment, added to culture fluid. The sizes of granulomas formed surrounding single egg in lungs or the intensity of in vitro granulomatous responses were measured and observed. RESULTS: The average diameter of pulmonary granulomas in administered group was significantly smaller than that of the control ( P

Objective:To observe the effect of chitosan on tumor. Methods: Experiments of antitumor in vitro and in vivo were adopted in tumor-bearing mice. Results: Experiment in vitro demonstrated that chitosan had some killing effects on S 180、EAC and H 22 tumor cells, but it did not have directly killing effect on human body liver cancer. Experiment demonstrated that rate of inhibitory tumor was 66.0% or so, and it markedly increased thymus and spleen weights of tumor-bearing mice (TBM), and markedly inhanced the transformation rate of lymphocytes, it had markedly protective effect on thymus and spleen weights and different antagonisfic effect on the decrease in WBC、 neutrophil cell and loss of body weight induced from 5-Fu. Conclusion: Chitosan had more intensive antitumous effect and immunologic function of tumor-bearing mice and antagonisfic effect on bone marrow and immunologic inhibition induced from 5-Fu.

Objective To investigate the effect of wogonin on ethology and its possible mechanisms in chronic cerebral ischemia in rats.Methods Rats were randomly divided into a sham operation group,a wogonin intervention group,and a phosphate buffered solution (PBS) control group.A rat model of chronic cerebral ischemia was induced by the two-vessel occlusion method.Six weeks after modeling,the rats in the wogonin intervention group and the PBS control group were intragastric administrated with wogonin (50 μmol/L,10 ml/kg,once a day) and PBS with equal volume for 14 days.Morris water maze test was used to evaluate the spatial learning and memory function.Laser confocal three-dimensional vascular imaging was used to detect the vascular proliferation of ischemic brain tissue.5-Bromo-2-deoxyuridine (BrdU)immunochemical staining was used to detect the cell proliferation in ischemic brain tissue.Transmission electron microscope was used to observe the morphological changes of neural cells in cerebral ischernic region.Results The Morris water maze (n =8) showed that the trains of escape latency from the second to the fifth day in the wogonin intervention group were 43.45 ± 8.64 s,37.12 ± 1.31 s,34.75 ± 5.36 s,and 24.36 ± 5.43 s,respectively.They were significantly shorter than 51.69 ± 5.32 s,43.65 ± 9.21 s,50.19 ± 10.31 s,and 53.65 ± 7.15 s in the PBS control group (all P ＜ 0.05).The first quadrant swimming time of the wogonin intervention group was significantly longer than that of the PBS control group (26.16 ±3.29 s vs.14.38 ±2.16 s; P＜0.01).Laser confocal three-dimensional vascular imaging (n=4) showed that the capillary inner diameter in cerebral ischemia region of the wogonin intervention group was reduced significantly compared to the PBS control group (3.02 ±0.21 μm vs.3.35 ±0.18 μm; P ＜0.05),vascular density was increased significantly (205.80 ± 12.70/0.002 mm3vs.158.42 ± 10.92/0.002 mm3; P＜0.01),and total microvascular area was increased significantly (83 389 ± 4 026 μm2/0.002 mm3 vs.73 349 ±3 986 μm2/0.002 mm3; P＜0.01).Immunohistochemical staining (n =6) showed that the number of BrdU positive cells in the ischemic brain tissue of the wogonin intervention group was increased significantly compared to the PBS control group (24.62 ±3.25/HPF vs.9.87 ±2.89/HPF; P＜0.01).The observation of transmission electron microscope showed that the inflammatory edema in the intercellular spaces of the wogonin intervention group was significantly reduced compare to the PBS control group.Conclusions Wogonin can significantly improve the spatial learning and memory ability of chronic cerebral ischemia in rats,and its possible mechanisms may include the promotion of proliferation and angiogenesis in ischemic region and angiogenesis,and reduce inflammatory response.

Objective To investigate the correlations of serum adipocyte fatty acid-binding protein (AFABP),adiponectin (APN) and A-FABP/APN ratio with acute ischemic stroke (AIS) and its subtypes.Methods The consecutive patients with AIS (AIS group) of having complete data admitted within 24 hours of onset were enrolled,and at the same time,the healthy subjects of age,sex and body mass index matched with the AIS group were selected as a control group.The demographic characteristics and general clinical data of the AIS group and control group were collected.The serum A-FABP and APN levels were detected by enzymelinked immunosorbent assay.The patients in the AIS group were further divided into large artery atherosclerosis (LAA),small artery occlusion,(SAO),cardioembolism (CE),and stroke of other determined etiology (SOE) according to the TOAST classification criteria.Multivariable logistic regression analysis was used to investigate the relationship between all factors and AIS and its subtypes.Spearman correlation analysis was used to analyze the correlations of the A-FABP and APN levels and the NIHSS scores.Results The serum A-FABP level (P =0.017) and A-FABP/APN ratio (P =0.002) in the AIS group were significantly higher than those in the control group,and the serum APN level was significantly lower than that in the control group (P =0.011).Multivariate logistic regression analysis showed that the increased serum A-FABP level (odds ratio [OR] 1.48,95％ confidence interval [CI] 1.07-1.93; P =0.009) and the A-FABP/APN ratio (OR 1.59,95％ CI 1.10-2.34; P =0.002) as well as the decreased APN level (OR 0.36,95％ CI 0.14-0.65; P =0.011) were independently associated with AIS.And the A-FABP/APN ratio was better than the correlation of both separately.The serum A-FABP level and A-FABP/APN ratio in the LAA,SAO and CE groups were significantly higher than those in other subtype groups (all P ＜0.05),and the APN level was significantly lower than that in other subtype groups (P ＜0.05).Multivariate logistic regression analysis showed that the increased serum A-FABP level and A-FABP/APN ratio as well as the decreased APN level were independently associated with LAA,SAO and CE,and the A-FABP/APN ratio was better than the correlation of both separately.The baseline NIHSS score was positively correlated with the serum A-FABP level (r =0.236,P =0.019),it was negatively correlated with the serum APN level (r =0.307,P =0.002),and the correlation of the serum AFABP/APN ratio was higher than that of A-FABP or APN (r =0.326,P =0.001).Conclusions The increased serum A-FABP level and the decreased APN level may serve as the new risk factors for AIS,especially LAA,SAO and CE subtypes,and they can reflect the severity of AIS.

Carcinoma ; pathology ; Carcinoma, Papillary ; Humans ; Thyroid Neoplasms ; pathology

Aim To determine the plasma protein binding rate of five components of Eucommia ulmoides extract. Methods The equilibrium dialysis method was used to study the plasma protein binding rate. The plasma samples were extracted by protein precipitation with methanol. With the use of puerarin as the internal standard, UPLC-MS/MS was carried out to determine the concentration of the five compounds in and out of the dialysis membrane. Results The average plasma protein binding rates of five compounds on the area of the concentration which was determinate were as fol-lows, respectively: geniposidic acid was ( 25. 77 ± 2. 68 )%, protocatechuic acid was ( 57. 54 ± 3. 79)%, chlorogenic acid was (53. 91 ± 3. 00)%, pinoresinol diglucoside was (24. 15 ± 4. 92)%, and pinoresinol singleglucoside was (49. 78 ± 3. 61)%. Conclusions The results show that the binding percentage of geniposidic acid and pinoresinol diglucoside is relatively low, but the binding rate of the others with rat plasma protein is moderate.

Objective To analyze epidemiological and clinical characteristics of chronic hepatitis C (CHC) patients. Methods The clinical data of 323 CHC patients were collected. The transmission modes, clinical manifestations and virological features were recorded. The liver histological change was also analyzed in 39 cases whose liver biopsy samples were available. The comparison between two groups was performed by t test. Results Among the 323 CHC patients, 135 cases (41. 8%) had history of blood or blood products transfusion. Sixty-seven cases (20. 7%) had undergone surgery and trauma operation. Nineteen cases (5. 9%) had history of Chinese medicine acupuncture. Eighteen cases (5.6%) had undergone hemodialysis. Two patients (0.6%) were infected through vertical transmission. Twenty-one cases (6. 5%) had history of intravenous drug use and two cases (0. 6%) had history of unsafe sexual contact. The possible transmission routes for the other 78 cases (24.1%)were unknown. Fourteen patients (4. 3%) were co-infected with hepatitis B virus (HBV). The major prevalent genotypes were hepatitis C virus ( HCV) genotype lb and 2a, which were 145 cases (65. 3%) and 21 cases (9. 5%) respectively. HCV viral loads were as high as 1 × 105 IU/mL in 74 cases (26. 1%) and 1× 106 IU/mL in 103 cases (36. 4%). Twenty-three patients (7.1%) developed obvious clinical manifestations. Among 39 patients undergoing liver biopsy, 14 cases (35. 9%) had hepatic inflammation activity index (HAI)≥4, six cases (15. 4%) had fibrosis stage (F) ≥3, four cases (10. 3%) had HAI≥4 and F≥3. Conclusions The most common HCV transmission modes are blood transfusion and use of blood products. However, surgery and trauma operation should be paid more attention. Besides blood transfusion, the transmission modes of intravenous drug injection, hemodialysis and traditional Chinese medicine acupuncture are increasing. The major HCV genotypes are lb and 2a. The viral loads of most patients are relatively high. Most patients infected with HCV don't show any obvious hepatitis symptoms and physical signs. However, the liver biopsy results from 39 patients suggest that most patients develop liver histological changes.

Objective To determine the distribution and antibiotic resistance of hospital - associated pneu-monia(HAP) in senile patient,and the high risk factors of HAP,pathogenic bacterium and prognosis,so as to instruct the clinic prevention and treatment. Methods Patients with age over 60 years old,who were diagnosed of HAP with confirmed pathogens. Pathogens were identified, then the antibiotic resistance was determined by Kirty-Baucer disk dif-fusion assay. High risk factors of HAP, pathogenic bacterium and prognosis were analyzed by Logistic regression analy-sis. Results The first 10th pathogens of HAP patients were pseudomonas aeruginosa( 16.1% ),staphylococcus au-reus( 14.6% ) ,klebsiella pneumonia( 10.2% ), escherichia coil (8.8%) ,staphylococcus hemolyticus (7.3%). MR-SA accounted for 90% in staphylococcus aureus. The drug resistance of pseudomonas aeruginosa to imipenem was 29.5%. The high risk factors of HAP were acute brain accident, hypoalbuminemia, tracheal intubation or mechanical ventilation, rennal failure,COPD, gastric tube, anaemia,liver disfunction,long length of stay ( all P < 0.05 ). The mor-tality of senile HAP was 29.2%. Conclusion There are high antibiotic resistance and high mortality of HAP in se-nile patients. Measures should be taken to modify the risk factors.

Aim To evaluate the inhibitive and induc-tive effects of Polygonum capitatum water extract on main cytochrome P450 isoforms in human and liver mi-crosomes of mouse in vitro for predicting the herb-drug interactions in clinical application. Methods The in vitro inhibitory effect was evaluated by incubating Po-lygonum capitatum water extract with the probe sub-strates of main phase I metabolic enzymes in human liver microsomes, including CYP1A2, CYP2E1, CYP2C9,CYP2C19 and CYP3A4. Mice were adminis-tered with Polygonum capitatum water extract at dosage of 0 . 58 g · kg-1 and 1 . 16 g · kg-1 by gastric lavage for successive 7 days and 14 days, then the cocktail-LC-MS/MS method was applied to assess the inductive effect of main CYP450 isoforms in mouse liver micro-somes. Results The IC50 values of Polygonum capita-tum water extract on main CYP450 isoforms in human liver microsomes were from 849 . 6 mg · L-1 to 2 287 mg·L-1 . Compared with the blank control group, the activites of CYP2C9 and CYP3A4 in 1. 16 g·kg-1 7 d group were about 49 . 9 % and 21. 1 % higher ( P <0. 01, P < 0. 05 ) respectively, the activities of CYP2C9 and CYP3A4 in 0. 58 g·kg-1 7 d group were 27. 6 % and 15. 5 % higher ( P <0. 01 , P <0. 05 ) respectively, the activities of CYP2C9 and CYP3A4 in 1. 16 g·kg-1 14 d group were 67. 5 % and 32. 1 %higher (P<0. 01) respectively, while the activities of CYP1 A2 , CYP2 E1 and CYP2 C19 were not increased significantly in Polygonum capitatum treatment group. Conclusions Polygonum capitatum water extract do not show the inhibitory effect on main CYP450 in hu-man liver microsomes. There is induction on CYP2C9 and CYP3 A4 in mouse liver microsomes by Polygonum capitatum water extract.