OBJECTIVE: To study the preparation technology of tamsulosion hydrochloride sustained-release capsules and investigate the release degree in vitro. METHODS: The pellets containing tamsulosin hydrochloride were prepeared in the fluid-bed using bottom gush medicine. Then, it was coated with ethylcellulose aqueous dispersion (surelease), and in the following procedures, water-based acrylic resin enteric system (Acryl-EZE®) was used as coating material, hydroxypropylmethylcellulose E6 (HPMCE6) was considered as porous agent by fluid-bed. Based on the release degree in vitro, prescription influence factors were evaluated, as well as drug releases curve was compared, according to the single factor experiment. RESULTS: The preparation technology referred in our research was available to make tamsulosin hydrochloride sustained-release capsules, and drug release curve of self-made sustained-release capsules was similar to the commercial one. Additionally, the products reproducibility of intra-batch and inter-batch was excellent. CONCLUSION: The tamsulosin hydrochloride sustained-release capsules prepared in this study exhibited ideal sustained-release characteristics in vitro. The formulation is reasonable and feasible. It is suitable for industrial production.

The methyl group plays an important role in the rational drug design. Introducing methyl into small molecules has become an important strategy of lead compound optimization. The application of methyl in drug design is reviewed in this paper. Methyl can modulate the physicochemical, pharmacodynamic, and pharmacokinetic properties by ortho effect, inductive effect, and conformational effect. It also improves the metabolic stability as a soft metabolic point. In addition, introducing methyl into drug molecules can also be applied as a strategy in new uses of old drugs and generate me-too drugs.
Drug Design ; Hydrophobic and Hydrophilic Interactions ; Lipid Metabolism ; Methylation ; Pharmaceutical Preparations ; chemical synthesis ; chemistry ; metabolism ; Solubility ; Stereoisomerism ; Structure-Activity Relationship

Objective To find out the iodine nutritional status of children in Xiamen island, and to provide the scientific basis for iodine supplimentation. Methods On March 2010, thyroids of all children aged 6to 12, from primary school on the Xiaodeng island of Xiamen were examined by palpation, urinary iodine, iodine content of salt athome and IQ level were tested, and were collected 20 households, iodine content of drinking water was tested randomly. Results IQ testing and thyroid palpation were carried out among a total of 156 children, the goiter rate of children was 1.28% (2/156), the mean IQ was 110; 154 urine samples were taken, the median urinary iodine was 219.1 μg/L; a total of 153 salt samples were tested, and the qualified rate of iodized salt was 87.58%(134/153), and the mean iodine content in the tap water was 4.52 μg/L Conclusions Iodine nutritional status of the island residents is better, and there are no such problems as excessive iodine.

OBJECTIVETo critically evaluate the currently available randomized clinical trials regarding the effectiveness of acupuncture in palliative care for cancer patients, hence, to provide sufficient evidences for the widespread use of acupuncture in cancer treatment.

METHODSTwo independent reviewers extracted data from all of the randomized clinical trials (RCTs) that assessed the efficacy of acupuncture in palliative care for cancer patients. Seven databases were searched from their respective inception to December 2010. All eligible trials identified were evaluated by two independent reviewers using the Jadad scale, and data from the articles were validated and extracted.

RESULTSIn total, 33 RCTs met the inclusion criteria. The effects of acupuncture on different cancer-related aspects were shown, including chemotherapy or radiotherapy-induced side effects (13/33, 39.4%), cancer pain (6/33, 18.2%), post-operative urinary retention (4/33, 12.1%), quality of life (2/33, 6.1%), vasomotor syndrome (2/33, 6.1%), post-operative gastrointestinal dysfunction (2/33, 6.1%), prevention of prolonged postoperative ileus (2/33, 6.1%), joint symptoms (1/33, 3.0%), and immunomodulation (1/33, 3.0%).

CONCLUSIONSThe result of our systematic review suggested that the effectiveness of acupuncture in palliative care for cancer patients is promising, especially in reducing chemotherapy or radiotherapyinduced side effects and cancer pain. Acupuncture may be an appropriate adjunctive treatment for palliative care.

Acupuncture Therapy ; adverse effects ; Drug Therapy ; Humans ; Neoplasms ; surgery ; therapy ; Palliative Care ; Postoperative Complications ; etiology ; therapy ; Quality of Life ; Radiotherapy ; adverse effects ; Randomized Controlled Trials as Topic ; Treatment Outcome

Objective To investigate the current conditions of water iodine,childrens'iodine nutrition and residents'edible circumstance of iodized salt in the villages with high iodine in drinking water and the adjacent three villages in Xiamen city of Fujian province.Methods Four natural villages of Qianbian,Donglian,Dazhong and Dongshan of Xiangan county were chosen as survey spots in 2008.In each village,one running water sample and all well water samples were collected to obtain the benchmark for each location.All children aged 7-13 year in the four villages underwent thyroid palpation and were selected to measure the urine iodine and the salt iodine.The water iodine and urine iodine were determined by As3+-Ce4+ catalytic spectrophotometry digestion,salt iodine was determined by direct titration.Results In four investigated villages,iodine of four running water samples were all 1.5μg/L.The range of 237 well water iodine samples was from 0.1 μg/L to 506.0 μg/L.There were 18.6% (44/237)specimens in which the well water iodine less than 10 μg/L,73.4%(174/237)between 10 μg/L and 150 μg/L and 8%(19/237)more than 150μg/L.The median of urinary iodine was 153.3 μg/L in 79 urine samples,which was 114%(9/79)more than 200μg/L and less than 300μg/L,12.7%(10/79)equal or more than 300 μg/L and less than 500μg/L,7.6%(6/79)equal or more than 500μg/L and less than 800 μg/L in all samples.Seventy-nine students were examined by palpation and the total goiter rate of children measured was 11.4% (9/79).Seventy-one samples of iodine salt were detected and the coverage rate of iodized salt was 77.5%(55/71).Conclusions The well water iodine contents have a wide distribution in the investigated villages.We should enhance the community awareness by educating them on the damage of iodine excess and iodine deficiency.

OBJECTIVETo evaluate the diagnostic value of liver fibrosis markers and ultrasonic examination for determining compensated liver cirrhosis in patients with chronic hepatitis B, and screen applicable non-invasive diagnostic marker for compensated liver cirrhosis.

METHODSSerum hyaluronic acid (HA), Type III procollagen (PCIII), laminin (LN) and Type IV collagen (CIV) were measured from 350 patients with chronic hepatitis B, who were also detected with liver biopsy and ultrasonography. To determine the cut-off value of every serum liver fibrosis marker for diagnosing compensated liver cirrhosis, data was analysed with clinical epidemiology methods. Then evaluated and compared all the markers.

RESULTS85 out of 350 patients were diagnosed as compensated liver cirrhosis by liver biopsy, and 81 had liver cirrhosis images by ultrasonic examination. HA achieved the biggest area under the ROC curve. The cut-off values with best sensitivity and accuracy of HA, PCIII, LN and CIV were 154.35 microg/L, 198.44 microg/L, 137.58 microg/L and 100.80 microg/L respectively. The related diagnostic sensitivities of HA, PCIII, LN and CIV were 82.4%, 63.5%, 57.3% and 70.6%, specificities were 79.3%, 54.0%, 56.8%, 68.3%, and accuracies were 80.0%, 56.3%, 56.9%, 68.9%, respectively. Parallel tests could increase the diagnostic sensitivity, but decreased specificity and accuracy accordingly. Compared with other non-invasive diagnostic methods, HA was the best marker (mu > or =1.814, P<0.05). The level of HA at 119.17 microg/L was suitable for determining compensated cirrhosis, with a 87.1% sensitivity, 67.6% specificity, 72.3% accuracy, 46.25% positive predictive value and 94.7% negative predictive value.

CONCLUSIONAmong the non-invasive serum diagnostic markers for liver fibrosis and ultrasonic examination for cirrhosis image, HA is the best marker for diagnosing compensated liver cirrhosis.

Adolescent ; Adult ; Biomarkers ; blood ; Child ; Collagen Type IV ; blood ; Female ; Hepatitis B, Chronic ; complications ; Humans ; Hyaluronic Acid ; blood ; Laminin ; blood ; Liver Cirrhosis ; diagnosis ; etiology ; Male ; Middle Aged ; Procollagen ; blood

Objective To determine the relationship between abnormal blood glucose and lipid levels and body mass index in patients with chronic respiratory diseases. Methods This research was conducted in Urumqi baseline survey population from "Xinjiang multi-ethnic cohort study" in which patients with chronic bronchitis, emphysema and chronic obstructive pulmonary disease (COPD) were screened.The patients were defined as angular, normal, overweight, obesity groups according to body mass index (BMI), and were compared with blood levels of lipid and glucose, and rate of abnormal metabolism. Results A total of 6 046 subjects were included in the 2018 Urumqi cohort study, including 545 patients with chronic respiratory diseases.The prevalence of chronic respiratory diseases in different age groups and at different physical activity levels was different, and the prevalence of emaciation group was significantly higher than that of the other three groups.However, there were no statistically significant differences among people with different genders, nationalities, educational levels and whether they smoked or not.There were statistically significant differences in fasting glucose, serum cholesterol (TC) and serum high-density lipoprotein (HDL) levels among respiratory patients with different BMI (P < 0.05).The detection rates of hyperglycemia, high TG and low HDL increased with the increase of BMI.The result of multi-factor analysis showed that blood glucose, TG and HDL were the influencing factors of BMI. Conclusion Increase of body mass index in patients with chronic respiratory diseases is associated with abnormal glucose and lipid metabolism, which is not significantly different from that in patients with non-respiratory diseases.However, the body mass index and nutritional status of patients with long-term diseases should be closely monitored, and timely intervention measures should be taken to delay the disease process.

Objective To assess the neointimal coverage after the implantation of various drug eluting stents (DES) by optical coherence tomography ( OCT). Methods The study comprised of 62 patients implanted DES for ( 15. 3 ± 5.7 ) months. Patients were divided into three groups according to the type of implanted stent: Cypher group ( patient = 26, stent = 57 ), Endeavor group ( patient = 17, stent = 23 )and Firebird group (patient = 19, stent = 32). OCT images of the stent were analyzed by software equipped by Light Lab system. Intimal thickness of 64 μm, 168 μm and 366 μm represents 10%, 25% and 50%lumen area loss, respectively. Neointimal coverage was thin with intimal thickness≤64 μm, satisfactory with intimal thickness between 65 μm and 366 μm and hyperplaisa and restenosis with intimal thickness ＞ 366μm. Results The percent of complete neointimal coverage was similar among groups ( P ＞ 0. 05 ). The thickness of neointimal coverage in Cypher and Endeavor and Firebird group was (178.7 ± 11.9)μm,(228.7 ± 17. 1 ) μm and ( 170. 3 ± 13.3 ) μm, respectively( all P ＜ 0. 05 ). The symmetry of Cypher stent was better than Firebird stent, and the symmetry of Firebird stent was better than Endeavoe stent. Conclusion There was significant difference on neointimal coverage after various types of DES implantation, and OCT can be used to evaluate the symmetry of neointimal coverage post implantation of various DES.

OBJECTIVETo investigate the biocompatibility of polyurethane-BaFe(12)O(19) magnetic composite microsphere as a new endovascular embolization material.

METHODSThe biocompatibility of BaFe(12)O(19) particle was evaluated in vitro using Ames test, cell toxicity test, acute and subacute systemic toxicity test, hemolysis test, bleeding time and clotting time test and blood clotting function assay.

RESULTSAmes test showed that the MR values of this particle leaching solution were all less than 2 without mutagenicity. Cell toxicity test showed that leaching solution at different concentrations had grade I toxicity on L929 cells. Acute and subacute systemic toxicity test showed that the experimental animals had good general condition without obvious pathological abnormality. The hemolysis rate of experimental group was 2.43%, which met the ISO standard (no more than 5%). The bleeding time and clotting time in mice were comparable between the experimental group and control group (P>0.05). There were no significant differences in blood clotting function between experimental group and control group (P>0.05).

CONCLUSIONThe material has no obvious toxicity or mutagenicity, and does not cause hemolysis or hemopexis or affect the bleeding time and clotting time. Polyurethane-BaFe(12)O( 19) particle possesses satisfactory biocompatibility.

Animals ; Barium Compounds ; chemistry ; toxicity ; Biocompatible Materials ; Cell Line, Tumor ; Embolization, Therapeutic ; instrumentation ; Ferric Compounds ; chemistry ; toxicity ; Microspheres ; Polyurethanes ; chemistry ; toxicity ; Toxicity Tests

OBJECTIVETo explore the categories of drugs causing hepatotoxicity and analyze the clinical and histological features of the corresponding drug-induced liver injury (DILI), in order to gain insights into potential diagnostic factors for DILI.

METHODSA total of 138 DILI patients treated at our hospital from April 2008 to April 2010 were retrospectively analyzed. The responsible drug for each DILI case was recorded. The Roussel Uclaf Causality Assessment Method (RUCAM) had been used to diagnose DILI. Only cases that had scored as highly probable or probable (more than or equal to 6 points by RUCAM) were included in this study. The patients' general condition, clinical manifestations, and serum biochemical and immunological parameters were assessed. Sixty-six of the patients underwent liver biopsy, and were assessed for liver pathological changes. Clinical and laboratory test data were collected and used to classify the total 138 cases as hepatocellular injury, cholestatic, or mixed hepatocellular-cholestatic types.

RESULTSWithin our patient population, the leading cause of DILI was Chinese herb medicine, accounting for 53.62% of cases. Antibiotics were implicated in 7.97% of cases, and dietary supplement in 6.52% of cases. Correlation between the clinical features and histological injury pattern was stronger at the time of biopsy (more than or equal to 3 days after laboratory results) (kappa = 0.63, P less than 0.05) than at the onset of DILI (kappa = 0.25, P less than 0.05). All modified hepatic activity index (HAI) necroinflammatory scores and fibrosis scores were more severe in the cholestatic and mixed injury types than in the hepatocellular injury type (P less than 0.01 and P less than 0.05, respectively).

CONCLUSIONChinese herbal medicine, dietary supplements and antibiotics were the main causes of DILI in our patient population. The clinical and histological features correlated well, especially at later stages of DILI. The degree of inflammation and fibrosis was significantly higher in cholestatic and mixed hepatocellular-cholestatic injury types than in the hepatocellular injury type. Assessment of both clinical and pathological features may represent a more accurate diagnostic method for DILI.

Adolescent ; Adult ; Aged ; Aged, 80 and over ; Anti-Bacterial Agents ; adverse effects ; Anti-Infective Agents ; adverse effects ; Chemical and Drug Induced Liver Injury ; pathology ; Drugs, Chinese Herbal ; adverse effects ; Female ; Humans ; Liver ; pathology ; Male ; Middle Aged ; Young Adult