Effect of diosgenin on mTOR/FASN/HIF-1α/VEGFA expression in rats with non-alcoholic fatty liver disease / 中国中药杂志

The present study aimed to investigate the effect of diosgenin on mammalian target of rapamycin(mTOR), fatty acid synthase(FASN), hypoxia inducible factor-1α(HIF-1α), and vascular endothelial growth factor A(VEGFA) expression in liver tissues of rats with non-alcoholic fatty liver disease(NAFLD) and explore the mechanism of diosgenin on lipogenesis and inflammation in NAFLD. Forty male SD rats were divided into a normal group(n=8) fed on the normal diet and an experimental group(n=32) fed on the high-fat diet(HFD) for the induction of the NAFLD model. After modeling, the rats in the experimental group were randomly divided into an HFD group, a low-dose diosgenin group(150 mg·kg~(-1)·d~(-1)), a high-dose diosgenin group(300 mg·kg~(-1)·d~(-1)), and a simvastatin group(4 mg·kg~(-1)·d~(-1)), with eight rats in each group. The drugs were continuously given by gavage for eight weeks. The levels of triglyceride(TG), total cholesterol(TC), low-density lipoprotein cholesterol(LDL-C), alanine transaminase(ALT), and aspartate transaminase(AST) in the serum were detected by the biochemical method. The content of TG and TC in the liver was detected by the enzyme method. Enzyme-linked immunosorbent assay(ELISA) was used to measure interleukin 1β(IL-1β) and tumor necrosis factor α(TNF-α) in the serum. Lipid accumulation in the liver was detected by oil red O staining. Pathological changes of liver tissues were detected by hematoxylin-eosin(HE) staining. The mRNA and protein expression levels of mTOR, FASN, HIF-1α, and VEGFA in the liver of rats were detected by real-time fluorescence-based quantitative polymerase chain reaction(PCR) and Western blot, respectively. Compared with the normal group, the HFD group showed elevated body weight and levels of TG, TC, LDL-C, ALT, AST, IL-1β, and TNF-α(P<0.01), increased lipid accumulation in the liver(P<0.01), obvious liver steatosis, up-regulated mRNA expression levels of mTOR, FASN, HIF-1α, and VEGFA(P<0.01), and increased protein expression levels of p-mTOR, FASN, HIF-1α, and VEGFA(P<0.01). Compared with the HFD group, the groups with drug treatment showed lowered body weight and levels of TG, TC, LDL-C, ALT, AST, IL-1β, and TNF-α(P<0.05, P<0.01), reduced lipid accumulation in the liver(P<0.01), improved liver steatosis, decreased mRNA expression levels of mTOR, FASN, HIF-1α, and VEGFA(P<0.05, P<0.01), and declining protein expression levels of p-mTOR, FASN, HIF-1α, and VEGFA(P<0.01). The therapeutic effect of the high-dose diosgenin group was superior to that of the low-dose diosgenin group and the simvastatin group. Diosgenin may reduce liver lipid synthesis and inflammation and potentiate by down-regulating the mTOR, FASN, HIF-1α, and VEGFA expression, playing an active role in preventing and treating NAFLD.

Mechanism of Baihe Dihuangtang in Treatment of Depression with Yin Deficiency and Internal Heat / 中国实验方剂学杂志

ObjectiveTo establish a traditional Chinese medicine （TCM） syndrome model with yin deficiency and internal heat， discuss the rationality of model evaluation， and analyze differentially expressed genes in multiple dimensions to explore the molecular mechanism-signaling pathways as well as key targets of Baihe Dihuangtang （BHDH） in treating depression with Yin deficiency and internal heat. MethodForty male SD rats were randomly divided into a blank control group，a model group，a fluoxetine group （positive drug），a BHDH group， and a Zhibai Dihuangtang group （positive drug for Yin deficiency and internal heat）. The depression model with Yin deficiency and internal heat was induced by chronic unpredictable mild stress （CUMS）combined with Chinese herbal drugs with warm and heat nature. The model established was comprehensively evaluated by the detection of the basic condition， behavioral performance， and biochemical indicators of rats in each group. The differentially expressed genes were screened out by mRNA sequencing and underwent Gene Ontology（GO） and Kyoto Encyclopedia of Genes and Genomes（KEGG） pathway enrichment analyses. The protein-protein interaction （PPI） network was plotted and key genes were analyzed to explore the underlying mechanism of BHDH in treating depression with Yin deficiency and internal heat. ResultThe comparison of basic conditions， behavioral assays， energy metabolism， endocrine hormones， cytokines， and neurotransmitters showed that the model was properly induced. BHDH could significantly improve depression with Yin deficiency and internal heat by regulating the pathways related to the nervous system， endocrine system， and inflammatory and immune system. The key genes of the PPI network were Fos， Epha8， Npy2r， Htr2c， and Nr4a1. ConclusionUnder the guidance of TCM theories of treatment based on syndrome differentiation and etiology and pathogenesis，this study established a depression model with yin deficiency and internal heat in animals and evaluation system in accordance with the symptoms and signs of emotional diseases， and further confirmed the scientificity of the modeling method and the underlying mechanism of BHDH in interfering with depression with Yin deficiency and internal heat based on the results of mRNA sequencing.

lncRNA HOTAIR knockdown suppresses gastric cancer cell biological activities.

The aim of this study was to characterize the involvement of long noncoding RNA HOTAIR in gastric cancer development. Measurement of HOTAIR and miRNA-206 expression by in situ hybridization (ISH) and analyzed for the correlation between HOTAIR and miRNA-206 in gastric cancer tissues. To evaluate the effects of HOTAIR in gastric cancer, MTT assay, flow cytometry, transwell, and wound healing assays were applied. To explain the mechanism behind HOTAIR's involvement, the expression of proteins related to it was also measured by Western blotting. Finally, correlations among related factors were determined by a luciferase target experiment. HOTAIR expression significantly increased, and miRNA-206 expression significantly decreased in cancer tissues (p < .01 and p < .001, respectively); HOTAIR knockdown suppressed cell viability, increased cell apoptosis by maintaining cells in the G1 phase, and inhibited cell invasion and migration by regulating miRNA-206 expression (p < .01 or p < .001). Meanwhile, with HOTAIR knockdown, CCND1 and CCND2 protein expressions were significantly suppressed, whereas miRNA-206 expression increased (p < .01 or p < .001). HOTAIR was shown to target miRNA-206 and miRNA-206 targeted CCND1 and CCND2. HOTAIR knockdown had antitumor effects by suppressing CCND1 and CCND2 expression by stimulating miRNA-206 in gastric cancer in vitro study.

Advances in the application of motor imagery based brain computer interface systems for brain function activation and neural network remodeling in patients with paralysis after stroke / 中华神经科杂志

Motor imagery (MI) and its related brain computer interface (BCI) technologies have been used for speech and movement disorders in patients with spinal cord injury, stroke, multiple sclerosis, etc. Current studies have shown that BCI can activate brain function in stroke patients with enhanced frequency, longer duration and more stable electroencephalogram signals. Imaging results showed a significant increase in functional connectivity between the two hemispheres and within the affected hemispheres. In this paper, MI-BCI for stroke patients with brain function activation and neural network remodeling were reviewed, the research progress on mechanisms of the technology was summarized, to provide reference for the application of the technology in clinical and future research.

Clinical application of supraclavicular fasciocutaneous island flap in the repair of tracheal defects / 中华耳鼻咽喉头颈外科杂志

Objective: To explore the clinical application of supraclavicular fasciocutaneous island flap (SIF) in the repair of tracheal defect. Methods: From May 2016 to March 2021, the clinical data of 10 patients (8 males,2 females,aged 27-73 years old) were retrospectively analyzed who underwent repair surgery with SIF for trachea defects after resection of cervical or thoracic tumors, including 2 cases of laryngotracheal adenoid cystic carcinoma, 2 cases of laryngeal carcinoma, 3 cases of esophageal carcinoma, 2 cases of thyroid carcinoma and one case of parathyroid carcinoma. All of the primary tumors were at T4. The outcomes of 10 cases with tracheal defect repaired by SIF were evaluated. Results: The areas of the SIF were (3-7) cm × (6-10) cm, the thicknesses of the flaps were 8-11 mm, and the lengths of the pedicles were 10-15 cm. The blood supply of the SIF came from the transverse carotid artery. The skin defects of the donor areas of the shoulders were directly closed. After 1-60 months of follow-up, all the flaps survived. The flaps, tracheas as well as shoulder wounds healed well. Conclusion: The SIF is suitable for the repair of tracheal defects. It has perfect thickness compatible with the trachea. The technique is simple and microsurgical technique is not needed, with a good application prospect.

Seasonal characteristics and time series analysis of hepatitis E in Shanghai from 2005 to 2019 / 上海预防医学

Objective:To analyze the seasonal characteristics and incidence trend of hepatitis E from 2005 to 2019 in Shanghai， and provide references for the prevention and treatment of hepatitis E. Methods:The seasonal characteristics of hepatitis E in Shanghai from 2005 to 2019 were analyzed by circular distribution method. The incidence trend of hepatitis E was analyzed by ARIMA （autoregressive moving average model）. Results:The peak period of hepatitis E in Shanghai from 2005 to 2019 was from November 17 to June 9， and the peak day was on February 27. The time series shows that the optimal model is SARIMA（0，1，1）×（0，1，1）12， Akaike information criterion（AIC） and Schwartz Bayesian information criterion （SBC） are 1 243.799 and 1 250.035 respectively， and the residual is white noise sequence. The mean absolute percentage error（MAPE）between the predicted value， and the actual value of this model is 20.253%. The forecast shows a slight decrease in the number of cases of hepatitis E in 2020-2021 compared with 2019， but it is still at a high level. Conclusion:The incidence of hepatitis E in Shanghai shows a solid seasonal characteristic. Health education and prevention/control measures should be conducted well before the epidemic peak. Based on the short-term prediction， the incidence of hepatitis E would still be high. Effective prevention and control strategies should be developed， and active measures should be taken.

Early efficacy evaluation of the treatment of complex proximal humeral fractures in the elderly with reverse shoulder arthroplasty / 中华骨科杂志

Objective@#To evaluate the short-term efficacy of one-stage reverse shoulder arthroplasty in the treatment of complex proximal humeral fractures in the elderly.@*Methods@#Data of 43 elderly patients with complex proximal humeral fractures who were treated by reverse shoulder arthroplasty from July 2017 to January 2019 were retrospectively analyzed. There were 12 males and 31 females with an average age of 72 years (range, 66-78 years). All fractures were fresh and close which caused by trauma. The average time from injury to operation was 8.0 days (range, 6-11 days). According to Neer classification, 21 cases (48.8%, 21/43) were three-part fractures, 22 cases (51.2%, 22/43) four-part fractures. Visual analogue scale (VAS), Neer shoulder replacement evaluation system and Constant-Murley score were used to evaluate the postoperative results.@*Results@#All operations were successfully completed. The average operation time was 141.3 minutes (range, 120-170 minutes. The mean blood loss was 407 ml (range, 250-700 ml) and intraoperative blood transfusion was 446.5 ml (range, 400-800 ml). All patients were followed up for 10.9 months (range, 6 to 16 months). All patients were discharged within 7 days after operation, and no wounds related complications occurred. The bigger and lesser tuberosities of all patients healed completely within 8 weeks. At the latest follow-up, no loosening or dislocation of prosthesis occurred, and the forward elevation was 133.0° (range, 100°-165°); external rotation was 29.5° (range, 20°-35°); internal rotation was 46.7° (range, 30°-60°). VAS score was 0.8 (range, 0-3). The Neer score was 87 (range, 73-98), with 20 cases (46.5%, 20/43) excellent, 16 cases (37.2%, 16/43) good, and 7 cases (16.3%, 7/43) fair. Constant-Murley score was 88.7 (range, 70-98). A 71-year-old patient had symptoms of axillary nerve injury after operation and recovered completely 6 weeks after the operation, which did not affect the functional rehabilitation exercise or the stability of the prosthesis. During the follow-up, no other complications such as infection, acromial stress fracture and scapular notching were found in all patients.@*Conclusion@#The short-term effect of one-stage reverse shoulder arthroplasty for the treatment of complex proximal humeral fractures in the elderly is satisfactory.

Early efficacy evaluation of the treatment of complex proximal humeral fractures in the elderly with reverse shoulder arthroplasty / 中华骨科杂志

Objective To evaluate the short-term efficacy of one-stage reverse shoulder arthroplasty in the treatment of complex proximal humeral fractures in the elderly.Methods Data of 43 elderly patients with complex proximal humeral fractures who were treated by reverse shoulder arthroplasty from July 2017 to January 2019 were retrospectively analyzed.There were 12 males and 31 females with an average age of 72 years (range,66-78 years).All fractures were fresh and close which caused by trauma.The average time from injury to operation was 8.0 days (range,6-11 days).According to Neer classification,21 cases (48.8％,21/43) were three-part fractures,22 cases (51.2％,22/43) four-part fractures.Visual analogue scale (VAS),Neer shoulder replacement evaluation system and Constant-Murley score were used to evaluate the postoperative results.Results All operations were successfully completed.The average operation time was 141.3 minutes (range,120-170 minutes.The mean blood loss was 407 ml (range,250-700 ml) and intraoperative blood transfusion was 446.5 ml (range,400-800 ml).All patients were followed up for 10.9 months (range,6 to 16 months).All patients were discharged within 7 days after operation,and no wounds related complications occurred.The bigger and lesser tuberosities of all patients healed completely within 8 weeks.At the latest followup,no loosening or dislocation of prosthesis occurred,and the forward elevation was 133.0° (range,100°-165°);external rotation was 29.5° (range,20°-35°);internal rotation was 46.7° (range,30°-60°).VAS score was 0.8 (range,0-3).The Neer score was 87 (range,73-98),with 20 cases (46.5％,20/43) excellent,16 cases (37.2％,16/43) good,and 7 cases (16.3％,7/43) fair.Constant-Murley score was 88.7 (range,70-98).A 71-year-old patient had symptoms of axillary nerve injury after operation and recovered completely 6 weeks after the operation,which did not affect the functional rehabilitation exercise or the stability of the prosthesis.During the follow-up,no other complications such as infection,acromial stress fracture and scapular notching were found in all patients.Conclusion The short-term effect of one-stage reverse shoulder arthroplasty for the treatment of complex proximal humeral fractures in the elderly is satisfactory.

Effect of pre-treatments on biological methane potential of dewatered sewage sludge under dry anaerobic digestion.

The aim of the study is to enhance hydrolysis of dewatered sewage sludge to tackle the problem of low biological methane potential (BMP) and low efficiency of dry anaerobic digestion. Different pre-treatment i.e. physical (ultrasonication), chemical (acid, ozone) and combined (ultrasonication-ozone) methods were investigated and evaluated in terms of BMP and biodegradation. Ultrasonic pre-treatment had the best result among the single technologies, the BMP increased by 104.7%, while total solid (TS), volatile solid (VS) and chemical oxygen demand (COD) reduction were improved by 30.1%, 36.9% and 33.9%, respectively, over control. Combined pre-treatment (ultrasonication-ozone) showed more significant enhancement than single methods as evidenced by 138.2% higher BMP and 53.7%, 63.7% and 57.3% more reduction in TS, VS, COD, respectively, over control. The BMP increment positively correlated either with energy input, concentration or dose of pre-treatment applied. Among the tested methods, the physical pre-treatments out-compete chemical ones. Ultrasonic combined with ozone pre-treatment technology has good energy and economic feasibility.

(3R)-5,6,7-trihydroxy-3-isopropyl-3-methylisochroman-1-one ameliorates retinal degeneration in Pde6brd10 mice.

As a severe photoreceptor-degenerative disease, retinitis pigmentosa (RP) is currently incurable and eventually leads to partial or complete blindness. (3R)-5,6,7-trihydroxy-3-isopropyl-3-methylisochroman-1-one (TIM) is a novel antioxidant isolated from the plant of Alpinia katsumadai Hayata, with protective effects on photoreceptor cells against lipoteichoic acid-induced damage through inhibiting oxidative stress. The present study was to further demonstrate whether TIM could ameliorate retinal degeneration of Pde6brd10 (rd10) mice, a mouse model of RP. rd10 mice were treated with TIM by intraperitoneal injection daily from postnatal Day 10 (P10) to P26. Retinal function was tested by electroretinography. Histology was evaluated by toluidine blue staining and TUNEL assay. Oxidative stress markers were measured by ELISA. Immunohistochemistry, real-time PCR, and western blotting were applied to explore the protective mechanism. Results showed TIM significantly improved the retinal function and decreased photoreceptor cell apoptosis in rd10 mice through reducing oxidative stress. For the first time, this study demonstrated the protective effects of TIM against retinal degeneration in rd10 mice, providing scientific rationale to use TIM treating the RP.

MRI Features and Site-specific Factors of Ischemic Changes in White Matter: A Retrospective Study / 华中科技大学学报（医学）（英德文版）

Brain magnetic resonance imaging (MRI) of the elderly often reveals white matter changes (WMCs) with substantial variability across individuals.Our study was designed to explore MRI features and site-specific factors of ischemic WMCs.Clinical data of consecutive patients diagnosed with ischemic cerebral vascular disease who had undergone brain MRI were collected and analyzed.Multi-logistic regression analysis comparing patients with mild versus severe WMCs was performed to detect independent associations.Analyses of variance (ANOVAs) were used to detect regionally specific differences in lesions.We found that lesion distribution differed significantly across five cerebral areas,with lesions being predominant in the frontal lobe and parieto-occipital area.To explore WMCs risk factors,after adjusting for gender,diabetes mellitus,and hypertension,only age (P＜0.01),creatinine (P=0.01),alkaline phosphatase (ALP) (P=0.01) and low-density lipoprotein cholesterol (LDL-C) (P=0.03) were found to be independently associated with severe WMCs.Age (P＜0.001) was strongly associated with WMCs in the frontal lobe while hypertension was independently related to lesions in the basal ganglia (P=0.048) or infratentorial area (P=0.016).In conclusion,MRI of WMCs showed that ischemic WMCs occurred mostly in the frontal lobe and parieto-occipital area.The infratentorial area was least affected by WMCs.Typically,age-related WMCs were observed in the frontal lobes,while hypertension-related WMCs tended to occur in the basal ganglia and infratentorial area.

MRI Features and Site-specific Factors of Ischemic Changes in White Matter: A Retrospective Study / 华中科技大学学报（医学）（英德文版）

Brain magnetic resonance imaging (MRI) of the elderly often reveals white matter changes (WMCs) with substantial variability across individuals.Our study was designed to explore MRI features and site-specific factors of ischemic WMCs.Clinical data of consecutive patients diagnosed with ischemic cerebral vascular disease who had undergone brain MRI were collected and analyzed.Multi-logistic regression analysis comparing patients with mild versus severe WMCs was performed to detect independent associations.Analyses of variance (ANOVAs) were used to detect regionally specific differences in lesions.We found that lesion distribution differed significantly across five cerebral areas,with lesions being predominant in the frontal lobe and parieto-occipital area.To explore WMCs risk factors,after adjusting for gender,diabetes mellitus,and hypertension,only age (P＜0.01),creatinine (P=0.01),alkaline phosphatase (ALP) (P=0.01) and low-density lipoprotein cholesterol (LDL-C) (P=0.03) were found to be independently associated with severe WMCs.Age (P＜0.001) was strongly associated with WMCs in the frontal lobe while hypertension was independently related to lesions in the basal ganglia (P=0.048) or infratentorial area (P=0.016).In conclusion,MRI of WMCs showed that ischemic WMCs occurred mostly in the frontal lobe and parieto-occipital area.The infratentorial area was least affected by WMCs.Typically,age-related WMCs were observed in the frontal lobes,while hypertension-related WMCs tended to occur in the basal ganglia and infratentorial area.

Insights into Initial Demyelinating Episodes of Central Nervous System during Puerperium / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Inflammatory demyelinating disease of central nervous system (CNS) is an inflammatory disease characterized by a high childbearing female predominance. Labor-related alterations for postpartum demyelinating attacks are not entirely clear. This study aimed to summarize clinical features of female patients of reproductive age with initial CNS inflammatory demyelinating attacks during puerperium.</p><p><b>METHODS</b>Fourteen female patients with initial demyelinating events during puerperium between January 2013 and December 2016 were retrospectively studied. Records of clinical features, neuroimaging, serum antibodies, cerebrospinal fluid (CSF) findings, annualized relapse rate (ARR), and treatment were analyzed.</p><p><b>RESULTS</b>Among 14 patients, 5 patients were diagnosed with multiple sclerosis (MS), four as neuromyelitis optica (NMO), two as longitudinal extensive transverse myelitis, two as clinical isolated syndrome (CIS), and one as acute brainstem syndrome. All the 14 puerperal female patients presented with more than one manifestation of hemiplegia, paraplegia, uroschesis, visual loss or dysarthria, and with mild to moderate abnormalities of CSF. Attacks occurred during the first trimester postpartum and cesarean section was the main delivery way (n = 10). Median Expanded Disability Status Scale (EDSS) scores were 5.0 (range: 2.0-9.0) at the onset and 2.5 (range: 0-7.0) at the end of follow-ups. Patients with MS and CIS had a significantly lower EDSS scores than patients with NMO spectrum disorders (P < 0.05). Median ARR was 0.46 (range: 0-1.16); all patients had a low ARR (0.49 ± 0.34, 95% confidence interval: 0.29-0.69) with standardized treatments.</p><p><b>CONCLUSION</b>Labor-related alterations in the mother's immune system might result in newly-onset demyelinating diseases of central nervous system.</p>

Effects of Prior Antiplatelet Therapy on the Prognosis of Primary Intracerebral Hemorrhage: A Meta-analysis / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Antiplatelet therapy (APT) was prevalently being used in the prevention of vascular disease, but the influence of prior APT on the prognosis of patients with intracerebral hemorrhage (ICH) remains controversial. This meta-analysis was to explore the effects of prior APT on the prognosis of patients with primary ICH.</p><p><b>METHODS</b>PubMed and Embase were searched to identify the eligible studies. The studies comparing the mortality of ICH patients with or without prior APT were included. The quality of these studies was evaluated by the Newcastle-Ottawa quality assessment scale. The adjusted or unadjusted odds ratio (OR) for mortality between ICH patients with and without prior APT were pooled with 95% confidence interval (95% CI) as the effect of this meta-analysis.</p><p><b>RESULTS</b>Twenty-two studies fulfilled the inclusion criteria and exhibited high qualities. The pooled OR was 1.37 (95% CI: 1.13-1.66, P = 0.001) for univariate analysis and 1.41 (95% CI: 1.05-1.90, P = 0.024) for multivariate analysis. The meta-regression indicated that for each 1-day increase in the time of assessment, the adjusted OR for the mortality of APT patients decreased by 0.0049 (95% CI: 0.0006-0.0091, P = 0.026) as compared to non-APT patients.</p><p><b>CONCLUSION</b>Prior APT was associated with high mortality in patients with ICH that might be attributed primarily to its strong effect on early time.</p>

Primary exploration of key influential factors recognization method of Tanreqing injection / 中国中药杂志

To recognize the key influential factors during the liquid preparation process of Tanreqing injection, the near infrared(NIR) spectra of the raw materials and the operating parameters of 24 batches of physical manufacturing were recorded as independent variables, and the total soluble solids contents and the light inspection acceptance rate of the final products were collected as dependent variables. The calibration models were developed using the partial least-square regression (PLSR) method, and the correlation coefficients between the independent variables and the dependent variables were calculated. For the quantitative models, the correlation coefficients for the calibration and inner cross validation of total soluble solids contents and the light inspection acceptance rate reached 0.911 9, 0.724 2 and 0.873 8, 0.795 9, respectively. Using the correlation coefficients diagrams, several key influence factors were preliminarily determined, and the physical significance were analyzed combined with production experience. This work demonstrated that NIR spectroscopy with PLSR algorithm could be used for the key influential factors recognization during the liquid preparation process of Tanreqing injection and can be popularized to solve similar problems..

Study on the Pharmacokinetics and Absolute Bioavailability of Anti-inflammatory Compound HB0314 in Rats in vivo / 中国药房

OBJECTIVE:To establish the detection method for anti-inflammatory compound HB0314 in plasma of rats,and study on its pharmacokinetic characteristics in rats in vivo. METHODS:UPLC-MS/MS was performed on the column of Waters Ac-quity UPLCTM BEH C18 with mobile phase of 0.1% formic acid aqueous solution(A)-methanol(B)by gradient elution(0-2 min, 70%-90% B) at flow rate of 0.25 mL/min,column temperature was 30 ℃,and injection volume was 5 μL. Electrospray ion source was used,capillary voltage was 3 kV,ion source temperature was 150 ℃,desolvation gas temperature was 450 ℃,desol-vent air flow volume was 600 L/h,cone air flow volume was 45 L/h,and the inner standard was tetrahydropalmatine. 12 rats were randomly divided into iv group and ig group,6 in each group. Rats were intravenously injected and intragastrically administrated HB0314 solution 5,10 mg/kg. Sample blood 0.4 mL were taken from the jugular vein blood before administration and after 5,15, 30,60,120,240,360,480,600,720,1440 min of administration to determine the HB0314 plasma concentration. DAS 2.0 software was used to calculate the pharmacokinetic parameters and absolute bioavailability. RESULTS:The linear range of HB0314 was 1-1000 ng/mL(r=0.9955),and the lower limit of quantification was 1 ng/mL. RSDs of extra-day and daytime precision,sta-bility were not higher than 8.45%(n=5);recovery were 68.21%-90.29%(RSD≤11.20%,n=5),and matrix effects were 82.63%-106.90%(RSD≤6.75%,n=5). After intravenous injection and intragastric administration,AUC0-24 h were (270.267 ± 21.164), (252.755 ± 26.169)μg·h/L (n=6);t1/2z were (8.722 ± 2.266),(11.877 ± 4.517) h (n=6);and absolute bioavailability was 56.79%. CONCLUSIONS:The method is rapid,simple,and can be used for the determination of HB0314 content in plasma of rats. HB0314 shows high oral absolute bioavailability in rats in vivo,indicating that post-dosage form design may be considered as oral anti-inflammatory drugs.

Study on Preparation of Anti-tumor Drug H6 Polymeric Micelles and Their in vitro Anti-tumor Effects / 中国药房

OBJECTIVE:To prepare anti-tumor drug H6(lactone compound)polymeric micelles,and to investigate its in vitro anti-tumor effects. METHODS:Using mPEG2000-PCL4000 as carrier,H6/mPEG2000-PCL4000 micelles were prepared. Using particle size, PDI and 48 h whether to produce precipitation as indexes,feeding ratio,H6 concentration,volume ratio of organic solvent were screened. The encapsulation efficiency and drug-loading amount of micelle were all detected. MTT assay was used to detect the tox-icity of micelles and H6 solution to human non-small cell lung cancer cell A549 and human lung cancer cell H460. RESULTS:The screened formulation was as follows as feeding ratio of 1∶25,H6 concentration of 2 mg/mL,the ratio of ethanol to chloroform of 1∶1(V/V). The parameters of prepared H6/mPEG2000-PCL4000 micelles were as follows as particle size of(40.74±0.116 3)nm,PDI of(0.101±0.006),encapsulation efficiency of(94.87±0.016 3)%,drug-loading amount of(7.07±0.001 5)%(n=3). IC50 of mi-celles and H6 solution to A549 cell were 15.62 and 12.57 nmol/L;IC50 of micelles and H6 solution to H460 cell were 27.68 and 15.19 nmol/L. CONCLUSIONS:H6/mPEG2000-PCL4000 micelles are prepared successfully and show in vitro anti-tumor effects.

Evaluation of the safety of metallic elements in borosilicate glass controlled injection bottle by ICP-MS / 药物评价研究

Objective Determination of extractable components in medium/low borosilicate glass controlled injection bottles under 5 different extraction conditions,assess the risk of drug safety by the amount of migration.Methods Determination of 24 elements in extraction solution by ICP-MS.Result Establish the standard curves of 24 elements,and the detection limit and quantitative limit were determined.The determination of the elements in the 5 extraction solutions was completed and their safety was evaluated.Conclusion Medium/low borosilicate glass injection bottle for packing freeze-dried products of Tianjin Tasly Pride Pharmaceutical Co.,Ltd.,the daily intake of Li、V、Cr、Fe、Co、Ni、Cu、Zn、As、Cd、Sb、Ba、Hg、Pb was lower than permitted daily exposure,the amount of migration does not pose a risk to drugs,therefore,the injection quality is not affected.

Study on the Pharmacokinetics and Absolute Bioavailability of Anti-inflammatory Compound HB0314 in Rats in vivo / 中国药房

OBJECTIVE:To establish the detection method for anti-inflammatory compound HB0314 in plasma of rats,and study on its pharmacokinetic characteristics in rats in vivo. METHODS:UPLC-MS/MS was performed on the column of Waters Ac-quity UPLCTM BEH C18 with mobile phase of 0.1% formic acid aqueous solution(A)-methanol(B)by gradient elution(0-2 min, 70%-90% B) at flow rate of 0.25 mL/min,column temperature was 30 ℃,and injection volume was 5 μL. Electrospray ion source was used,capillary voltage was 3 kV,ion source temperature was 150 ℃,desolvation gas temperature was 450 ℃,desol-vent air flow volume was 600 L/h,cone air flow volume was 45 L/h,and the inner standard was tetrahydropalmatine. 12 rats were randomly divided into iv group and ig group,6 in each group. Rats were intravenously injected and intragastrically administrated HB0314 solution 5,10 mg/kg. Sample blood 0.4 mL were taken from the jugular vein blood before administration and after 5,15, 30,60,120,240,360,480,600,720,1440 min of administration to determine the HB0314 plasma concentration. DAS 2.0 software was used to calculate the pharmacokinetic parameters and absolute bioavailability. RESULTS:The linear range of HB0314 was 1-1000 ng/mL(r=0.9955),and the lower limit of quantification was 1 ng/mL. RSDs of extra-day and daytime precision,sta-bility were not higher than 8.45%(n=5);recovery were 68.21%-90.29%(RSD≤11.20%,n=5),and matrix effects were 82.63%-106.90%(RSD≤6.75%,n=5). After intravenous injection and intragastric administration,AUC0-24 h were (270.267 ± 21.164), (252.755 ± 26.169)μg·h/L (n=6);t1/2z were (8.722 ± 2.266),(11.877 ± 4.517) h (n=6);and absolute bioavailability was 56.79%. CONCLUSIONS:The method is rapid,simple,and can be used for the determination of HB0314 content in plasma of rats. HB0314 shows high oral absolute bioavailability in rats in vivo,indicating that post-dosage form design may be considered as oral anti-inflammatory drugs.