In order to solve the adhesion and the softening problems of traditional Chinese medicine extract during spray drying, a new method of adding dehumidified air into spray drying process was proposed, and the storage stability conditions of extract powder could be predicted. Kouyanqing extract was taken as model drug to investigate on the wet air (RH = 70%) and dry air conditions of spray drying. Under the dry air condition, the influence of the spray drying result with different air compression ratio and the spray-dried powder properties (extract powder recovery rate, adhesion percentage, water content, angle of repose, compression ratio, particle size and distribution) with 100, 110, 120, 130, 140 °C inlet temperature were studied. The hygroscopic investigation and Tg value with different moisture content of ideal powder were determined. The water activity-equilibrium moisture content (aw-EMC) and the equilibrium moisture content-Tg (EMC-Tg) relationships were fitted by GAB equation and Gordon-Taylor model respectively, and the state diagram of kouyanqing powder was obtained to guide the rational storage conditions. The study found that in the condition of dry air, the extract powder water content decreased with the increase of air compression ratio and the spray drying effect with air compression ratio of 100% was the best performance; in the condition of wet air, the extract powder with high water content and low yield, and the value were 4.26% and 16.73 °C, while, in the dry air condition the values were 2.43% and 24.86 °C with the same other instru- ment parameters. From the analysis of kouyanqing powder state diagram, in order to keep the stability, the critical water content of 3.42% and the critical water content of 0.188. As the water decreased Tg value of extract powder is the major problem of causing adhesion and softening during spray drying, it is meaningful to aid dehumidified air during the process.
Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Humidity ; Medicine, Chinese Traditional ; Plant Extracts ; chemistry ; Powders ; Temperature

Bipolar Disorder ; blood ; immunology ; metabolism ; Depressive Disorder ; blood ; immunology ; metabolism ; Humans ; Proteomics

OBJECTIVETo investigate the cough-relieving, analgesic and antibiotic effects of durian shell extract (DSE) in relieving cough and its analgesic and antibiotic effects.

METHODSThe effect of DSE in relieving cough was assessed in mice challenged with ammonia and SO(2) to induce coughing. The analgesic and antibiotic effects of DSE in mice were evaluated by hot plate test and twisting reaction induced by acetic acid, and by minimal inhibitory concentration (MIC) and disc-agar diffusion tests, respectively.

RESULTSCompared with the control group, the mice treated with 300 and 900 mg/kg DSE showed significantly prolonged latency with decreased number of coughing induced by ammonia and SO(2), and the effect was dose-dependent. DSE markedly prolonged the latency and decreased the twisting number of the mice induced by acetic acid without affecting the pain threshold in hot plate test. DSE produced no significant inhibitory effects against Staphylococcus aureus, Staphylococcus epidermidis, or E. coli, and showed a week inhibition against Bacillus aeruginosus.

CONCLUSIONDSE shows obvious effect in relieving cough and produces better analgesic effect against chemical factor-induced pain than against physical agent-induced pain sensation. DSE has a moderate inhibitory effect against Bacillus aeruginosus.

Analgesics ; pharmacology ; Animals ; Anti-Bacterial Agents ; pharmacology ; Antitussive Agents ; pharmacology ; Bombacaceae ; chemistry ; Male ; Mice ; Plant Extracts ; pharmacology ; Random Allocation

AIMTo identify the factors influencing diagnosis and treatment of chronic prostatitis (CP) among Chinese urologists.

METHODSA sample of 656 urologists from 29 provinces of China were asked to complete a questionnaire that explored attitudes towards CP as well as diagnosis and treatment patterns in the management of CP. Both univariate and multivariate logistic regression analysis schemes were used to determine the factors that influence the diagnosis and treatment of CP.

RESULTSA total of 656 questionnaires were given out. All were returned and 410 of those were included in the final univariate and multivariate analysis. Multivariate logistic regression analysis indicated that belief of bacterial infection in the etiology of CP (odds ratio [OR], 2.544; 95% confidence interval [CI], 1.650-3.923; P < 0.001) was the most significant factor influencing the routine performance of bacterial culture test. Using the same model, the type of hospital (OR, 2.799; 95% CI, 1.719-4.559; P < 0.001) and the routine use of the 4- or the 2-glass test (OR, 3.194; 95% CI, 2.069-4.931; P < 0.001) were determined to be significant factors influencing the use of the National Institutes of Health (NIH) new classification system. According to the same model, belief of bacterial infection in the etiology of CP (OR, 3.415; 95% CI, 2.024-5.762; P < 0.001) and the routine use of bacterial culture test (OR, 2.261; 95% CI, 1.364-3.749; P < 0.01) were important factors influencing the routine prescription of antibiotics.

CONCLUSIONOur findings suggest that attitudes towards CP, and the characteristics of individual urologists' practices may influence the diagnosis and treatment of CP among Chinese urologists.

Adult ; Aged ; Anti-Bacterial Agents ; therapeutic use ; China ; Chronic Disease ; Cross-Sectional Studies ; Health Knowledge, Attitudes, Practice ; Health Surveys ; Humans ; Logistic Models ; Male ; Middle Aged ; Multivariate Analysis ; Practice Patterns, Physicians' ; Prostatitis ; diagnosis ; drug therapy ; microbiology ; Surveys and Questionnaires

Objective To develop neutralizing monoclonal antibodies (MAbs) against H10N8 avian influenza virus hemagglutinin and to identify the binding sites. Methods MAbs against hemagglutinin of H10N8 avian influenza virus were developed by genetic engineering. Neutralizing MAbs were screened by microneutralization assay,and then tested by enzyme-linked immunosorbent assay and Western blot to identity the binding sites.The homology modeling process was performed using Discovery Studio 3.5 software,while the binding epitopes were analyzed by BioEdit software. Results One MAb that could neutralize the H10N8 pseudovirus was obtained and characterized. Analysis about epitopes suggested that the antibody could bind to the HA1 region of hemagglutinin,while the epitopes on antigen were conserved in H10 subtypes.Conclusions One neutralizing antibody was obtained by this research.The MAb may potentially be further developed as a pre-clinical candidate to treat avian influenza H10N8 virus infection.
Antibodies, Monoclonal ; immunology ; Antibodies, Neutralizing ; immunology ; Antibodies, Viral ; immunology ; Enzyme-Linked Immunosorbent Assay ; Epitopes ; immunology ; Hemagglutinin Glycoproteins, Influenza Virus ; immunology ; Influenza A Virus, H10N8 Subtype ; Neutralization Tests

Objective To provide data for the control and prevention of hepatitis B and HBV surface antigen(HBsAg)status among the appliances and practitioners working in the public service places.Methods 63 beauty parlors,barber shops and bathing centers selected under stratified randomization sampling method and 682 workers were investigated through questionnaire.HBsAg from the appliances of the public service places and employee was detected by RIA.Results Two main sanitizing modes that including alcohol cleaning(34.60%)and ultraviolet light disinfection(30.79%)were used.The rates of testing on HBsAg among the appliances were 2.13% at the public service places,and were 0.63%,2.67% and 3.70% in large-.medium-and small-sized appliances respectively.The rate of testing on HBsAg on large-,medium-and small-sized appliances were statistically different(χ2=6.68,P＜0.05).The positive rates of HBsAg on the appliances of beauty parlors,barbering shops and footbath inns were 2.97%,0.61% and 3.42% respectively.People working in different service sites had different rates of HBsAg:those who worked at the‘acne needle'and the forceps were 5.13% and 4.17%.The positive rate of HBsAg among the workers in the public service places was 7.13%.The rates of HBsAg among the workers in large-,medium-and small-sized public service places were 7.34%,8.33% and 2.94% respectively.The rates of HBsAg among the workers in beauty parlors,barbering shops,footbath inns and bathing centers were 9.01%,6.37%,4.35% and 7.29% respectively.HBsAg positive rates were different among the workers working at different service sites:13.33% at tattoo business.12.68% in pedicures workers and 8.03% in massagists.Conclusion It is important to improve the sanitizing management of the appliances used in the public service places and to improve the knowledge,attitude,as well as practice of vaccination on hepatitis B among those populations.

Objective To evaluate the prevalence and risk factors of metabolic syndrome among hepatitis C patients in Chinese Han population .Methods This was a multicenter ,cross-sectional study . A total of 997 Chinese Han patients with hepatitis C virus (HCV) infection were enrolled .Demographic data ,anthropometric data and clinical parameters related to metabolic syndrome were collected .Statistical analysis was performed by t-test (normal distribution) or Mann-Whitney U two-sample test (non-normal distribution) and χ test .Binary logistic regression analyses were used to determine the parameters significantly related to metabolic syndrome .Results Among the 997 patients ,170 (17 .1%) patients were diagnosed with metabolic syndrome .Binary logistic regression showed that genotype 2 (OR＝1 .594 ;95% CI :1 .045－2 .431 , P＝ 0 .030) ,older age (OR＝ 1 .040 ;95% CI :1 .022 －1 .058 , P＜ 0 .01) , overweight (OR＝3 .876 ;95% CI :2 .593－5 .792 ,P＜0 .01) ,fatty liver history (OR＝2 .106 ;95% CI : 1 .384－3 .204 ,P＝0 .001) ,homeostasis model assessment insulin (HOMA-IR) (OR＝1 .263 ;95% CI :1 .118－1 .427 , P＜0 .01) ,fasting insulin (OR＝0 .949 ;95% CI :0 .915 －0 .985 , P＝0 .006) ,lower serum albumin level (OR＝0 .957 ;95% CI :0 .915 －1 .000 , P＝0 .049) and higher γ-GT level (OR＝1 .004 ;95% CI :1 .000 －1 .008 , P＝ 0 .0041 ) were all significantly associated with the presence of metabolic syndrome .Conclusions Hepatitis C patients with genotype 2 ,older age ,overweight ,fatty liver history ,higher HOMA-IR ,lower fasting insulin level ,lower serum albumin level or higher γ-GT level should be screened for metabolic syndrome .

Objective To assess the efficacy and safety of 100 mg or 200 mg yimitasvir phosphate combined with sofosbuvir in patients with non-cirrhotic chronic hepatitis C virus ( HCV) genotype 1 infection who were treatment-na?ve or had a virologic failure to prior interferon-based treatment.Methods A multicenter, randomized, open-label, phase 2 clinical trial was conducted.The patients were randomly assigned to yimitasvir phosphate 100 mg+sofosbuvir 400 mg group (Group 100 mg) and yimitasvir phosphate 200 mg+sofosbuvir 400 mg group ( Group 200 mg) in a 1∶1 ratio with the stratified factors of " treatment-naive" or"treatment-experienced" for 12 weeks and followed up for 24 weeks after the end of treatment.During the clinical trial, HCV RNA was tested in all patients.Resistance of virus in patients who didn′t achieved sustained virological response (SVR) was monitored.Safety and tolerability were assessed by monitoring adverse events , physical examination , laboratory examination, electrocardiogram, and vital signs during the study.The primary end point was SVR12 after the end of therapy.Descriptive statistics were used for categorical variables and eight descriptive statistics were used for continuous variables.Descriptive statistics were used and summarized according to HCV genotypes and treatment groups.Safety data were presented using descriptive statistics and summarized according to treatment groups.Results A total of 174 subjects were screened from July 31, 2017 to September 26, 2018.One hundred and twenty-nine patients were successfully enrolled and received treatment , and 127 completed the study.There were 64 patients and 65 patients assigned to Group 100 mg and Group 200 mg, respectively.Among the 129 patients who underwent randomization and were treated , 18.6% were treatment-experienced and: 100%were HCV genotype 1b infection.The total SVR rate was 98.4%(127／129), with 98.4%(63／64, 95%confidence interval [CI]: 91.60%-99.96%) in the Group 100 mg, and 98.50%(64／65, 95%CI: 91.72%-99.96%) in the Group 200 mg.There was no significant difference between the two groups (χ2 ＝0.000 2, P＝0.989 2).The SVR rates in treatment-naive group and treatment-experienced group were 98.10%(95%CI: 93.29%-99.77%) and 100.00%(24／24, 95%CI: 85.75%-100.00%), respectively.Virological failure during treatment ( including breakthrough , rebound and poor efficacy) and relapse after treatment did not occur during the trial.By Sanger sequencing , 11.6%(15／129) patients had baseline NS5A Y93H／Y or Y93H resistance-associated substitutions ( RAS), 1.6%( 2／129) patients had baseline NS5A L31M RAS.No mutation was observed in NS5B S282 at baseline.There was no S282 mutation in HCV NS5B.A total of 100 (77.5%) subjects had adverse events.No adverse events ≥Grade 3 or severe adverse events related to the study treatment.No patient prematurely discontinued study treatment owing to an adverse event.No life-threatening adverse event was reported.Conclusion Twelve weeks of yimitasvir phosphate 100 mg or 200 mg combined with sofosbuvir 400 mg daily is a highly effective and safe regimen for patients without cirrhosis with HCV genotype 1b infection who had not been treated previously or had a virologic failure to prior interferon-based treatment.

The global COVID-19 coronavirus pandemic has infected over 109 million people, leading to over 2 million deaths up to date and still lacking of effective drugs for patient treatment. Here, we screened about 1.8 million small molecules against the main protease (M^pro) and papain like protease (PL^pro), two major proteases in severe acute respiratory syndrome-coronavirus 2 genome, and identified 1851M^pro inhibitors and 205 PL^pro inhibitors with low nmol/l activity of the best hits. Among these inhibitors, eight small molecules showed dual inhibition effects on both M^pro and PL^pro, exhibiting potential as better candidates for COVID-19 treatment. The best inhibitors of each protease were tested in antiviral assay, with over 40% of M^pro inhibitors and over 20% of PL^pro inhibitors showing high potency in viral inhibition with low cytotoxicity. The X-ray crystal structure of SARS-CoV-2 M^pro in complex with its potent inhibitor 4a was determined at 1.8 Å resolution. Together with docking assays, our results provide a comprehensive resource for future research on anti-SARS-CoV-2 drug development.
Humans ; Antiviral Agents/chemistry* ; COVID-19 ; COVID-19 Drug Treatment ; High-Throughput Screening Assays ; Molecular Docking Simulation ; Protease Inhibitors/chemistry* ; SARS-CoV-2/enzymology* ; Viral Nonstructural Proteins