BACKGROUND: Anti-tuberculous chemotherapy is the main method for treating bone and joint tuberculosis. However, systemic administration hardly maintains the effective drug concentration in the focus area, and the therapeutic efficacy is unsatisfactory. OBJECTIVE: To prepare a chitosan-gelatin/poly(lactic-co-glycolic acid) combined with drug-loaded hydrogel, which can release anti-tuberculosis drugs in situ for a long time and promote osteogenesis. METHODS: Isoniazid, a hydrophilic anti-tuberculosis drug, and a hydrophobic stromal cell derived factor-1 were loaded into poly(lactic-co-glycolic acid) by double emulsion method to prepare drug-loaded poly(lactic acid co-glycolic acid) microspheres, which were then mixed into chitosan gelatin/poly(lactic acid co-glycolic acid) combined with drug-loaded hydrogel. The ability of drug delivery and anti-tuberculosis of poly(lactic acid co-glycolic acid) microspheres and chitosan gelatin/poly(lactic acid co-glycolic acid) combined with drug-loaded hydrogels in vitro were tested. MC3T3-E1 cells were inoculated on the surface of microspheres and hydrogel respectively. The biocompatibility was detected by cell counting kit-8 assay. The osteogenetic activity was detected by alkaline phosphatase activity. RESULTS AND CONCLUSION: (1) The burst release of isoniazid in the microspheres was about 23.3% in 1 hour, 42.6% in 2 days, and then it entered the sustained-release stage in the later 25 days. The burst release of stromal cell derived factor was about 19.8% in 1 hour, 44.7% in 2 days, and then it entered the sustained-release stage in the next 25 days. The release of isoniazid and stromal cell-derived factor in the combined drug-loaded hydrogel was 8.3% and 8.5% in the first hour, respectively. The cumulative release rates on the second day were 15.2% and 17.6%, respectively, which were much lower than that of poly(lactic acid co-glycolic acid) microspheres. (2) After 4 weeks in vitro, the antibacterial diameter of the combined drug-loaded hydrogel was much larger than that of the drug-loaded microspheres, and the antibacterial rate was higher than that of the drug-loaded microspheres (P < 0.05). (3) The combined drug-loaded hydrogel and the drug-loaded microspheres had good cytocompatibility and cell viability was about 100%. (4) After 5 and 10 days of culture, there was no significant difference in the activity of alkaline phosphatase on the surface of drug-loaded hydrogel and drug-loaded microspheres. (5) These results show that the in situ chitosan-gelatin/poly(lactic acid co-glycolic acid) combined with drug-loaded hydrogel can be used for treating tuberculosis and other bone and joint infections.

Objective A headspace-solid phase microextraction-gas chromatography-mass spectrometry method (HS-SPME-GC-MS) was adopted for analyzing the volatile components of different parts of Clausena lansium in Hainan Province. Methods Five different fibers were investigated and optimized. Other five experimental parameters such as volume of water, extraction temperature, equilibrium time, extraction time, and salt concentration had been evaluated and optimized by means of the orthogonal design with L16(45) table. Finally, the volatile components of C. lansium leaves, pericarps, and seeds in Hainan were analyzed and identified by GC-MS combined with retention index (RI). Results The optimum extraction conditions were as follows: a 50/30 μm DVB/CAR/PDMS fiber, 10 mg sample powders, 2.0 mL water, 0.2 g NaCl, extraction temperature 80 ℃, equilibrium time 30 min, extraction time 60 min. A total of 83 chemical components were identified from leaves, 96 from pericarps, and 106 from seeds, representing the relative contents of 95.24%, 92.15%, and 95.92% of the total composition. The highest contents were sesquiterpenes in all of the parts, but there were obviously different both in components and contents. Conclusion The HS-SPME-GC-MS method is rapid and sensitive, with a small sample size, without any organic solvents. GC-MS combined with RI has improved the accuracy of analysis and identification. The results may provide experimental basis for further exploitation of C. lansium in Hainan. This method can be used to perform enrichment analysis of the components with high-boiling point and micro-components, which can comprehensively and scientifically characterize and evaluate the quality of Chinese materia medica.

OBJECTIVE: To investigate the taste-masking effect of montelukast sodium orally disintegrating tablets using electronic tongue technology and human sensory evaluation and determine the optimum formulation. METHODS: Orally disintegrating tablets were prepared with five different concentrations of flavoring agents or without flavoring agent.The tastes of those tablets were determined by electronic tongue, and principal component analysis and linear discriminant analysis were used to evaluate differences of different formulations. The taste-masking effect of the tablets was investigated combined with electronic tongue analysis and sensory evaluation of subjects. RESULTS: The taste of orally disintegrating tablet was the best when the total amount of flavoring agent was 1.6 mg, and the ratio of sweetening agent to aromatic agent was 5∶3. CONCLUSION: The combination of electronic tongue and human sensory assess can evaluate the taste-masking effect of orally disintegrating tablets and provide the basis for determining the optimum formulation.

OBJECTIVE: To prepare montelukast sodium orally disintegrating tablets and investigate the bioequivalence in Beagle dogs. METHODS: The orally disintegrating tablets were prepared by direct compression method,and the optimal formulation was screened by orthogonal test.HPLC-fluorescence method was developed for determination of montelukast sodium plasma concentration in Beagle dogs. RESULTS: The optimized formulation(1 000 tablets) was montelukast sodium 10.4 g, microcrystalline cellulose 60 g, cross linked povidone 30 g, mannitol 15 g, magnesium stearate 2 g, aerosil 1 g, aspartame 1 g, flavor 0.6 g. CONCLUSION: Montelukast sodium orally disintegrating tablets made of the optimized formulation could disintegrate rapidly. Relatively bioavailability of montelukast sodium orally disintegrating tablets is 90.7%.

BACKGROUND:Thoracolumbar fracture becomes more in the clinic. The fixation manner of thoracolumbar fracture is controversial. Injured vertebra pedicle screw fixation or traditional cross-segment pedicle screw fixation are controversial and lack the support of evidence-based medicine. OBJECTIVE: To evaluate the outcomes of injured vertebra pedicle screw and cross-segment pedicle screw fixation for thoracolumbar fractures. METHODS: According to Cochrane system evaluation, the folowing databases were retrieved: National Library of Medicine database, China National Knowledge Infrastructure, Wanfang database and VIP database. Conference proceedings were searched by hand. The retrieval time ranged from 2005 to March 2015. Randomized controled trials were colected. Meta-analysis was performed by using Cochrane Colaboration Revman 4.2. RESULTS AND CONCLUSION: By screening, a total of 14 clinical controled trials were selected, including 956 patients. Meta-analysis results showed that postoperative Cobb angle was improved significantly in the vertebral pedicle screw group than in the cross-segment pedicle screw fixation group (OR=-2.72, 95%CI:-3.08--2.35,P < 0.01). Correction rate of the vertebral height was higher in the vertebral pedicle screw group than in the cross-segment pedicle screw fixation group (OR=7.45, 95%CI:6.94-7.97,P < 0.01). The failure rate was lower in the vertebral pedicle screw group than in the cross-segment pedicle screw fixation group (OR=0.12, 95%CI: 0.05- 0.27,P < 0.01). Results verify that postoperative Cobb angle improved significantly after the injured vertebrae pedicle screw and cross-segment pedicle screw fixation for thoracolumbar fractures. The height was obviously corrected and fewer complications were caused such as implant failure. The fixation effect was good.

BACKGROUND: Magnetic resonance imaging (MRI) plays an increasingly important role in the diagnosis of osteoporosis. As a new method of image analysis, radiomics has potential clinical significance in the diagnosis of osteoporosis. OBJECTIVE: To explore the diagnostic value of osteoporosis based on lumbar MRI imaging model. METHODS: Fifty female patients who underwent both lumbar-spine MRI and dual-energy X-ray absorptiometry in Outpatient Department of First Hospital of Hebei Medical University from February 2017 to October 2018 at the age of 40-84 years were enrolled in this study. Dual-energy X-ray absorptiometry showed 28 osteoporosis patients, and 22 normal bone mineral density. In the sagittal plane T1WI and T2WI images of lumbar MRI, five consecutive layers in the middle of L2-4 vertebral body were selected for image segmentation; radiomics features were extracted; diagnostic models were constructed. Combined with clinical risk factors, the clinical-radiomics model was constructed. The area under the receiver operating characteristic curve was used to assess the model performance. The experiment was approved by the Ethics Committee of First Hospital of Hebei Medical University. RESULTS AND CONCLUSION: (1) The 396 × 3 features were extracted from T1WI, T2WI and combined sequences respectively in 50 subjects. After feature dimensionality reduction, four features of T1WI sequence, six features of T2WI sequence and four features of T1WI and T2WI combined sequence were screened out respectively. After diagnostic model establishment, the areas under the receiver operating characteristic curve of T1WI and T2WI models were 0. 810 and 0. 820, respectively. The area under the receiver operating characteristic curve of combined T1WI+T2WI model was 0. 937, which was higher than that of a independent sequence. (2) Combining the T1WI + T 2WI radiomics features with clinical data, the diagnostic model suitable for female combined with clinical factors was constructed, and the area under the receiver operating characteristic curve of clinical-radiomics model was 0. 960. (3) The results showed that the radiomics features based on routine lumbar MRI can distinguish osteoporosis from normal bone mass, and the clinical-radiomics diagnosis model based on clinical and radiomics features can improve the diagnostic efficiency, which is valuable for diagnosis of osteoporosis.

Objective To investigate the effects of finasteride on microvascular density and vascular endothelial growth factor (VEGF) expression in glomeruli of streptozotocin-induced diabetic mice. Methods Diabetes was induced in mice with a single intraperitoneal injection of streptozotocin in a dose of 150mg/kg, and they were randomly divided into 4 groups (7 each): diabetic model group and 3 treatment groups (treated with 0.1, 1, 10mg/kg of finasteride, respectively). Seven normal mice served as control group. Animals in finasteride treatment groups were intragastrically administered with finasteride 0.1, 1 and 10mg/kg once daily for 4 weeks, respectively, and those in control and diabetic model group were given the same volume of normal saline at the same time. The kidney sections from all mice were stained with hematoxylin and eosin (HE) for the pathological study, and immunohistochemistry methods were performed to detect the microvascular density, and VEGF expression in glomeruli. Results Compared with control group, the glomerular area and volume, microvascular density and VEGF index were significantly increased in diabetic model and finasteride treated groups (P<0.05). However, the glomerular area and volume, microvessel density and VEGF index were significantly decreased in 10mg/kg finasteride treated group compared with that in diabetic model group (P<0.05). Conclusion Finasteride can inhibit the VEGF expression and decrease the glomerular microvascular density in diabetic mice.

OBJECTIVE: To investigate the cardioprotective effect of astragaloside IV on the mitochondrial pathway, and to explore its possible mechanism.

Palbocicril, the first cyclin-dependent kinases 4 and 6 inhibitors, is a crucial milestone in the development history of antineoplastic drugs. It combined with aromatase inhibitor or fulvestrant as first-line, second-line or post-line therapy has good efficacy and safety for hormone receptor-positive, human epidermal growth factor receptor-2 negative locally advanced or metastatic breast cancer, which has a good application prospect. This article summarizes the clinical trials and safety studies related to palbociclib.

Calcium Channels, L-Type ; genetics ; metabolism ; Esophageal Achalasia ; genetics ; metabolism ; Esophagus ; metabolism ; Humans ; Nitric Oxide Synthase ; metabolism ; Nitric Oxide Synthase Type I ; genetics ; metabolism ; RNA, Messenger ; metabolism ; Real-Time Polymerase Chain Reaction ; Receptors, Calcium-Sensing ; genetics ; metabolism