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1.
Chinese Journal of Industrial Hygiene and Occupational Diseases ; (12): 354-358, 2022.
Article in Chinese | WPRIM | ID: wpr-935809

ABSTRACT

Objective: To understand the incidence of pneumoconiosis in Ningbo city from 1967 to 2019, and to analyze the distribution characteristics and change trend of pneumoconiosis. Methods: In February 2021, the data of pneumoconiosis patients in Ningbo city from 1967 to 2019 were sorted out. The data from 1967 to 1987 were from historical case files of Zhejiang Center for Disease Control and Prevention, the data from 1988 to 2005 were from the historical case files of Ningbo Center for Disease Control and Prevention, and the data from 2006 to 2019 were from the pneumoconiosis report card in China Disease Prevention and Control Information System; Followed up and supplement relevant information, including basic information, basic information of employers and information related to pneumoconiosis diagnosis, and comprehensively analyze the composition and development trend, population characteristics and industry characteristics of pneumoconiosis. Results: From 1967 to 2019, a total of 1715 cases of pneumoconiosis were reported in Ningbo City, including 1254 cases of stageⅠpneumoconiosis, 258 cases of stageⅡpneumoconiosis, 172 cases of stage Ⅲpneumoconiosis. 1202 cases of silicosis (70.09%) , 296 cases of asbestosis (17.26%) , 40 cases of welder's pneumoconiosis (2.33%) , 32 cases of graphite pneumoconiosis (1.87%) were reported. There were 1296 male cases (75.57%) and 419 female cases (24.43%) were reported. Silicosis (91.15%, 1102/1209) and welder's pneumoconiosis (100.00%, 40/40) were the most common pneumoconiosis in males, while asbestosis (90.24%, 268/297) and graphite pneumoconiosis (87.50%, 28/32) were the most common pneumoconiosis in females. The average age was (49.71±10.90) years old and the average length of service was (10.98±6.96) years. The top three reported pneumoconiosis cases were construction industry (336 cases, 19.59%) , ferrous metal smelting and rolling industry (317 cases, 18.48%) and non-metallic mineral products industry (315 cases, 18.37%) . The top three reported pneumoconiosis cases were 414 cases (24.14%) in Ninghai County, 294 cases (17.14%) in Yuyao City and 272 cases (15.86%) in Yinzhou District. Conclusion: With the development of industries in Ningbo City, government departments should strengthen supervision and management of enterprises involving silica dust and welding fume to curb the high incidence of pneumoconiosis.


Subject(s)
Adult , Female , Humans , Male , Middle Aged , Asbestosis , China/epidemiology , Graphite , Incidence , Pneumoconiosis/epidemiology , Pulmonary Fibrosis , Silicosis/epidemiology
2.
Journal of Preventive Medicine ; (12): 1003-1008, 2017.
Article in Chinese | WPRIM | ID: wpr-792664

ABSTRACT

Objective To compare the applicability of different occupational health risk assessment methods in small furniture manufacturing industry. Methods American EPA inhalation risk model, Singapore semi-quantitative risk assessment model of occupational exposure to chemical substances and Australian Occupational Health and Safety Risk Assessment model, were used to assess the occupational health risk in a small furniture manufacturing industry from a city of Zhejiang Province. Results The results of American EPA model showed that the workers who exposed to benzene and formaldehyde had low risk of carcinogens, and who exposed to benzene and xylene had very high risk of non-carcinogens. According to Singapore semi-quantitative risk assessment model, there were low and medium health risk caused by toluene and xylene, and high risk caused by wood dust in preparation and polishing jobs. Similar to the results of other models, Australia qualitative risk assessment model showed that there were medium health risk caused by toluene and xylene, and high risk caused by benzene, wood dust and noise. All of the three methods could found the key risk control point in furniture manufacturing industry. The risk ratios of the three methods were higher than the toxic work classification ratio (P<0.01), and the risk ratio of EPA model were higher than the results of Singapore model and Australia model (P<0.05) . Conclusion All of the three methods can be applied to assess the occupational health risk in furniture manufacturing industry, and the combined application of multiple risk assessment methods can be used as one of the risk assessment strategies.

3.
Chinese Pharmaceutical Journal ; (24): 849-857, 2014.
Article in Chinese | WPRIM | ID: wpr-859725

ABSTRACT

OBJECTIVE: To study deformation behaviors of directly compressed materials using induction tableting machine. METHODS: Eighteen types of materials, which were widely used in tablet production, were selected and compressed. Their deformation behaviors and compactability were investigated by applying classic methods involving compression models, mechanical energy and elastic stretch. RESULTS: Cellulose and copovidone with lower Py and E were ranked in high TS interval; starches with lower Py, high FES and Esp, and larger E values than cellulose, were ranked in inferior TS interval; polyols and lactose materials resembling cellulose powders in appearance of Esp and Py, were of higher E values than that of the latter and mostly ranked in intermediate interval; mineral materials with highest Py and E were ranked in inferior TS interval. CONCLUSION: Copovidone and cellulose derivatives display good plastic deformation and compactability whereas Ac-Di-Sol SD711 mainly deform elastically; starch derivatives primarily undergo plastic deformation during compaction but with high FES and relatively poor compactability; polyols and lactose materials exhibit brittle characteristics during loading and the former consolidating better; mineral materials show great resistance to break and deform and have relatively high elastic recovery.

4.
Acta Pharmaceutica Sinica ; (12): 1475-1483, 2013.
Article in Chinese | WPRIM | ID: wpr-298055

ABSTRACT

The present work is to investigate the correlation between physical properties and deformation behaviors of tablet excipients, and rank them according to their plastic performances during compaction. The excipients selected were compacted using Korsch XP1 after measuring their physical properties where the compression parameters for evaluating deformation behaviors were Heckle equation, compression work and elastic stretch in die. The correlations between compaction descriptors and physical parameters were analyzed by canonical correlation analysis, and factor analysis was simultaneously employed to synthetically assess deformation behaviors for all our samples. The canonical variables show that true density (Pa) correlated negatively with plastic coefficient (PL) and positively with yield pressure (YP); compression degree (Cp) correlated negatively with fast elastic stretch (FES) as well as YP and positively with PL. When factor scores were used in combination with original data, the plasticity of our samples was sorted and ranked as high (-0.56 < F' < 0.21), intermediate (-0.16 < F' < 0.36), or low (0.38 < F' < 0.84), which are in accord with plasticity rankings previously reported in literature. This study indicates factor analysis can be an approach to evaluate deformation behaviors of pharmaceutical powders.


Subject(s)
Chemistry, Pharmaceutical , Methods , Compressive Strength , Elasticity , Excipients , Chemistry , Factor Analysis, Statistical , Particle Size , Pharmaceutical Preparations , Chemistry , Powders , Chemistry , Pressure , Tablets
5.
Chinese Pharmaceutical Journal ; (24): 116-122, 2013.
Article in Chinese | WPRIM | ID: wpr-860500

ABSTRACT

OBJECTIVE: To study correlation between physical properties and compressibility and compactablility of Microcrystalline cellulose. METHODS: After determining the physical properties such as particle size distribution, moisture capacity, angle of repose, bulk density, tapped density, the powder was tableted by the Korsch XP1 at the same filling height, and data derived from heckle model, plasticity constant, cumulative elastic recovery, tensile strength and it's changes with time were evaluated. RESULTS: The physical properties of microcrystalline cellulose had great effect on its compactablility as well as cumulative elastic recovery out of die, but not on compressibility. And pressure applied correlated closely with changes of tensile strength in storage, which was intensified by the influence of water in powder on the particle size. CONCLUSION: Microcrystalline cellulose shows excellent compressibility, however, particle size reduction is able to decrease the compactability. Since the water in powder can increase particle size by changing internal structure of particles and plays a prerequisite role in lubrication and adherence, the variation of water content may weaken the compatability of microcrystalline cellulose and worsen the mechanical strength stability of tablets in storage.

6.
Chinese Journal of Gastrointestinal Surgery ; (12): 918-921, 2012.
Article in Chinese | WPRIM | ID: wpr-312386

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate the learning process of video-assisted minimally invasive esophagectomy (MIE).</p><p><b>METHODS</b>One hundred consecutive patients with thoracic esophageal carcinoma were treated by a same team of surgeons, and were divided into 3 groups in chronological order. The former two groups both consisted of 25 patients with thoracoscopy plus laparotomy. The remaining 50 patients were enrolled in the third group with thoracoscopy plus laparoscopy. Clinicopathological data including operative time, blood loss, protection of normal structures, complications, length of ICU stay, postoperative stay, and lymph nodes harvest, were collected and compared between groups.</p><p><b>RESULTS</b>Procedures were accomplished successfully in 96 patients. Only 4 cases were converted to open thoracotomy and none to laparotomy. The median operative time was 310 min and blood loss was 200 ml. The median number of lymph node harvest was 22. The overall complication rate was 50%. Comparison of first two groups revealed that significant differences existed in the preservation rate of arch of azygos vein (P=0.010), bronchial vessels (P=0.038), and exposure rate of thoracic part of left recurrent laryngeal nerve( P=0.048). Comparison of the former and latter 50 patients revealed that significant differences existed in thoracic operative time (P<0.001), blood loss (P=0.025), preservation rate of arch of azygos vein (P=0.001) and bronchial vessels (P<0.001), the number of lymph node harvest in thoracoscopy (P=0.022) and in left recurrent laryngeal nerve chain (P<0.001), and exposure rate of initiate part of left recurrent laryngeal nerve (P=0.002).</p><p><b>CONCLUSION</b>The learning curve of MIE is long and beginners should proceed step by step.</p>


Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Esophageal Neoplasms , General Surgery , Esophagectomy , Methods , Learning Curve , Retrospective Studies , Thoracoscopy , Methods , Video-Assisted Surgery , Methods
7.
Chinese Journal of Industrial Hygiene and Occupational Diseases ; (12): 883-887, 2012.
Article in Chinese | WPRIM | ID: wpr-242744

ABSTRACT

<p><b>OBJECTIVE</b>Using the stable HSPA1A (HSP70-1) promoter-driven luciferase reporter HepG2 cells (HepG2/HSPA1A cells) to assess the overall toxicity of coke oven emissions.</p><p><b>METHODS</b>The stable HepG2/HSPA1A cells were treated with different concentrations of coke oven emissions (COEs) collected from the top, side, and bottom of a coke oven battery for 24 h. After the treatments, luciferase activity, cell viability, malondialdehyde (MDA) concentration, Olive tail moment, and micronuclei frequency were determined, respectively.</p><p><b>RESULTS</b>The bottom COEs induced significant increases (P < 0.01) in relative luciferase activity up to 1.4 times the control level at 0.15 µg/L. The low dose of side COEs (0.02 µg/L) led to a significant increase (P < 0.01) in relative luciferase activity that progressively increased to 2.1 times the control level at 65.4 µg/L. The top COEs produced a strong dose-dependent induction of relative luciferase activity up to over 5 times the control level at the highest concentration tested (202 µg/L). In HepG2/HSPA1A cells treated with the bottom COEs, relative luciferase activity was positively correlated with MDA concentration (r = 0.404, P < 0.05). For the three COEs samples, positive correlations were observed between relative luciferase activity and Olive tail moment and micronuclei frequency.</p><p><b>CONCLUSION</b>The relative luciferase activity in HepG2/HSPA1A cells can sensitively reflect the overall toxicity of COEs. The stable HepG2/HSPA1A cells can be used for rapid screening of the overall toxicity of complex air pollutants in the workplace.</p>


Subject(s)
Humans , Coke , Toxicity , Genes, Reporter , HSP70 Heat-Shock Proteins , Genetics , Hep G2 Cells , Luciferases , Genetics , Malondialdehyde , Micronuclei, Chromosome-Defective , Occupational Exposure , Promoter Regions, Genetic , Toxicity Tests
8.
Chinese Journal of Industrial Hygiene and Occupational Diseases ; (12): 888-892, 2012.
Article in Chinese | WPRIM | ID: wpr-242743

ABSTRACT

<p><b>OBJECTIVE</b>To explore the effects of smoking on urinary 10 metabolites of polycyclic aromatic hydrocarbons (PAHs) in the coke oven workers.</p><p><b>METHODS</b>Occupational health examination was performed on 1401 coke oven workers in one coking plant, their urine were collected respectively. The concentrations of the ten monohydroxy polycyclic aromatic hydrocarbons in urine were detected by gas chromatography/mass spectrometry. The 1401 workers were divided into four groups, namely control, adjunct workplaces, bottom and side, top group according to their workplaces and the different concentrations of PAHs in the environment. The concentrations of the ten monohydroxy polycyclic aromatic hydrocarbons between smokers and nonsmokers in each workplace group were compared using analysis of covariance, respectively.</p><p><b>RESULTS</b>The levels of concentrations of the sixteen polycyclic aromatic hydrocarbons we detected at control were significantly higher than those at other areas (P < 0.05). Comparing the ten monohydroxy polycyclic aromatic hydrocarbons levels between smokers and nonsmokers, the levels of 1-hydroxynaphthalene and 2-hydroxynaphthalene among smokers were higher than nonsmokers with statistically significance in control, adjunct workplaces, bottom and side and top groups (P < 0.05). However, the levels of 1-hydroxypyrene had no statistically significant differences between the four areas.</p><p><b>CONCLUSION</b>Urinary 1-hydroxynaphthalene and 2-hydroxynaphthalene may be used as biomarkers for the impact of smoking on monohydroxy polycyclic aromatic hydrocarbons in the coke oven workers.</p>


Subject(s)
Humans , Male , Air Pollutants, Occupational , Urine , Biomarkers , Urine , Coke , Naphthols , Urine , Occupational Exposure , Polycyclic Aromatic Hydrocarbons , Urine , Pyrenes , Urine , Smoking , Urine
9.
Chinese Journal of Industrial Hygiene and Occupational Diseases ; (12): 898-901, 2012.
Article in Chinese | WPRIM | ID: wpr-242741

ABSTRACT

<p><b>OBJECTIVE</b>To explore the characteristics of particulate matter pollution in coke oven plant, so as to provide scientific data for establishing occupational exposure limits for coke oven emissions.</p><p><b>METHODS</b>Concentrations of CO, SO₂, BSM, BTEX (concentrations of benzene, toluene and xylene were determined in this study), PM₁₀, PM₂.₅, 16 selected PAHs in PM₁₀ and PM₂.₅ were determined in the work environment of a coke oven plant in Wuhan. The work environment was divided into the adjunct area, the bottom of, the side of and the top of coke oven.</p><p><b>RESULTS</b>The concentrations of CO, SO₂, BSM, BETX, PM₁₀, PM₂.₅, PAHs in PM₁₀ and PM₂.₅ were significantly related to working environmental categories, respectively, and were increasing as the adjunct area < bottom < side < top (P (trend) < 0.05). PM₁₀ was statistically significantly correlated with CO, SO₂, benzene, BTEX and BSM (0.705, 0.823, 0.664, 0.624 and 0.734, respectively). PM₂.₅ was statistically significantly correlated with CO, SO₂, benzene, BTEX and BSM (0.635, 0.916, 0. 680, 0.553 and 0.726, respectively). BSM was statistically significantly correlated with benzene (0.689). The ratios of PM₂.₅ to PM₁₀ between different work environments were not significantly different in one-way ANOVA (P > 0.05). The distribution of aromatic rings and the concentrations of total benzo[a] pyrene equivalents in PM₁₀ and PM₂.₅ were not statistically different between work environments.</p><p><b>CONCLUSION</b>The concentrations of particulate matter was related with other contents of coke oven emissions in coke work environment, and the contents and types of PAHs in PM₁₀ and PM₂.₅ were similar.</p>


Subject(s)
Air Pollutants, Occupational , Benzene , Benzo(a)pyrene , Coke , Occupational Exposure , Particulate Matter , Polycyclic Aromatic Hydrocarbons , Toluene , Workplace , Xylenes
10.
Chinese Journal of Industrial Hygiene and Occupational Diseases ; (12): 17-20, 2012.
Article in Chinese | WPRIM | ID: wpr-273557

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effects of occupational exposure to formaldehyde on the micronuclei frequencies in peripheral blood lymphocytes of workers.</p><p><b>METHODS</b>Two hundred thirty six plywood workers were divided into 3 exposure groups (low, middle and high) according to internal exposure biomarker (formaldehyde human serum albumin conjugate, FA-HSA), which was detected by ELISA. The concentrations of formaldehyde (FA) in air of two workshops were measure using the high performance liquid chromatography. Cytokinesis-block micronucleus (CBMN) test was used to detect the micronuclei frequencies of peripheral blood lymphocyte in 236 workers.</p><p><b>RESULTS</b>The average concentrations of FA in the low and high exposure workshops were 0.58 +/- 0.20 and 1.48 +/- 0.61 mg/m3, respectively, there was significant difference (P < 0.01). The average concentrations of serum FA-HAS of workers in two workshops were 69.22 +/- 15.37 and 136.29 +/- 89.49 pg/ml, respectively, there was significant difference (P < 0.01). The results of CBMN test showed that the micronucleus frequencies in low, middle and high exposure groups were 1.94 +/- 1.72, 2.10 +/- 1.92 and 2.10 +/- 1.70 per thousand, respectively, there were no significant differences between groups. However, the micronucleus frequencies in accumulative low, middle and high exposure groups were 1.36 +/- 1.36, 2.31 +/- 1.81 and 2.49 +/- 1.92 per thousand, respectively, there were significant differences between different accumulative exposure groups (P < 0.01). The results of correlation analysis indicated that there was a positive correlation between accumulative exposure levels and micronucleus frequencies (r(s) = 0.321, P < 0.01). The accumulative exposure doses may be a risk factor for high micronucleus frequencies in workers exposed to FA (P(trend) = 0.002).</p><p><b>CONCLUSION</b>FA-HSA levels can serve as an internal exposure biomarker for assessing the exposure level of workers exposed to FA. Accumulative formaldehyde exposure resulted in an increase of micronuclei frequencies of peripheral blood lymphocyte in plywood workers.</p>


Subject(s)
Adult , Humans , Asian People , Biomarkers , Blood , Formaldehyde , Blood , Lymphocytes , Cell Biology , Micronucleus Tests , Occupational Exposure , Respiratory Hypersensitivity , Blood
11.
Acta Pharmaceutica Sinica ; (12): 1231-1236, 2012.
Article in Chinese | WPRIM | ID: wpr-274672

ABSTRACT

The main methods of characterizing the flowability of pharmaceutical powders include repose angle method, HR method, Carr's index method, Jenike flow function method, fractal dimension method, and mass flow rate method, etc. Regarding powders with different flowabilities as the research subject, comprehensive features of pharmaceutical materials were investigated and characterized. The multivariate analysis method was employed to evaluate and analyze flowability values of the tested pharmaceutical materials. Comparing with the method of the mass flow rate, it was feasible to use multivariate analysis method to evaluate the flowability of powders. Simultaneously, the flowability of pharmaceutical materials could be ranked and definitely quantified, and critical values be determined according to the actual production, which has promoted the previous methods dependent only on the single parameter, i.e. repose angle and compression degree methods. A relatively objective standard method of evaluating flowability of powders is formed.


Subject(s)
Multivariate Analysis , Particle Size , Powders , Chemistry , Principal Component Analysis , Technology, Pharmaceutical , Methods
12.
Chinese Journal of Gastrointestinal Surgery ; (12): 875-878, 2011.
Article in Chinese | WPRIM | ID: wpr-321217

ABSTRACT

<p><b>OBJECTIVE</b>To explore long-term effect of the treatment of refractory benign esophageal strictures with a novel retrievable fully covered stent made of nitinol alloy.</p><p><b>METHODS</b>From November 2009 to May 2011, the stents were placed in 8 patients with refractory benign esophageal strictures in the Department of Thoracic Surgery at the Cancer Center of Sun Yat-sen University. Esophago-gastro-duodenoscopy and barium swallow examinations were performed respectively on the 1st, 7th, 30th, 60th day after implantations of the stents and 1,2,3,6 months or even longer after removal of the stents in order to assess the long-term effect on the improvement of dysphagia and the development of complications.</p><p><b>RESULTS</b>The stents were successful deployed in all the patients. The dysphagia scores were improved instantly and significantly as compared to the preoperative scores(P<0.05). Seven patients had long-term improvement of dysphagia. The dwelling time of all the stents ranged from 4 to 60 weeks, with a median of 16.8 weeks. Six patients had their stent removed after a dwelling time of 4 to 18 weeks(median 9.7 weeks). The follow-up period was 1.5-9 months (median 6.1 months). The improvement of dysphagia was also significant during follow-up after removal of the stents(P<0.05). At the most recent follow up, two patients still had the stent in place. The first one has already been followed up for 15 months and was still on regular diet. The other one experienced improvement of dysphagia score up to two months after placement, but downgraded to 3 by the third month. Relapse of stenosis occurred in 1 patient, migration in 2 patients, and tissue hyperplasia in 3 patients, of whom 2 developed inward growth of granulation tissue due to the rupture of the covering membrane.</p><p><b>CONCLUSIONS</b>The new retrievable fully covered stent made of nitinol alloy significantly improves the swallowing function of patients with intractable benign esophageal strictures after implantation and after removal of the stents, with low incidence of long-term restenosis. However, the high rate of migrations and the poor quality of the covering membrane further implies that the design of the new stent still needs to be improved.</p>


Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Alloys , Esophageal Stenosis , General Surgery , Prosthesis Implantation , Methods , Stents , Treatment Outcome
13.
Chinese Journal of Oncology ; (12): 263-265, 2008.
Article in Chinese | WPRIM | ID: wpr-348117

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the feasibility of regional lymph nodes targetting with enrichment of radioactive 99mTc-polyphase liposome of 5-fluorouracil (99mTc-FL, FL).</p><p><b>METHODS</b>18 rabbits were randomly divided into 3 groups, 6 rabbits per group. All rabbits were injected hypodermally with of 99mTc-FL in the right and left big toe webs, 18.5 MBq each side. The post-injection interval was 3 h in group 1, 6 h in group 2, and 8 h in group 3. The radioactivity was examined in the resected local lymph nodes, non-draining lymph nodes, liver, spleen, kidney, heart, lung, intestines, and in blood and urine.</p><p><b>RESULTS</b>The radioactive isotope uptake percentage (%) was 2.32 +/- 0.75 in group 1, 5.37 +/- 1.73 in group 2, 8.61 +/- 1.89 in group 3. The radioactive isotope uptake percentage (%) per gram in local lymph nodes was significantly different between each two groups among the 3 groups (P < 0.05). The ratios of x of regional lymph nodes/non-draining lymph nodes, regional lymph nodes/blood, regional lymph nodes/urine, regional lymph nodes/liver, regional lymph nodes/spleen, regional lymph nodes/kidney, regional lymph nodes/heart, regional lymph nodes/lung, regional lymph nodes/intestine in group 1 were 232.00, 16.57, 23.20, 29.00, 19.33, 25.78, 46.40, 46.40 and 25.78, respectively. The ratios in group 2 were 89.50, 41.31, 18.52, 67.13, 41.31, 25.57, 134.25, 59.67 and 59.67, respectively. The ratios in group 3 were 86.10, 61.50, 16.56, 53.81, 57.40, 10.01, 107.63, 107.63 and 86.10, respectively. The differences of radioactive isotope uptake percentage were statistically significant (P < 0.01) between regional lymph nodes and other organs, i. e. non-draining lymph nodes, blood, urine, liver, spleen, kidney, heart, lung and intestine per gram in each group.</p><p><b>CONCLUSION</b>The radioactive 99mTc-FL may slowly flow into regional lymphatic chains rather than directly enter blood circulation. So 99mTc-FL can be highly accumulated in the local lymph nodes. This regional lymph nodes targetting with enrichment of radioactive 99mTc-FL evidently indicates the feasibility of regional lymph system chemotherapy for pulmonary malignancies.</p>


Subject(s)
Animals , Female , Male , Rabbits , Fluorouracil , Pharmacokinetics , Heart , Diagnostic Imaging , Intestines , Diagnostic Imaging , Kidney , Diagnostic Imaging , Liposomes , Liver , Diagnostic Imaging , Lung , Diagnostic Imaging , Lymph Nodes , Diagnostic Imaging , Organotechnetium Compounds , Pharmacokinetics , Radionuclide Imaging , Random Allocation , Spleen , Diagnostic Imaging
14.
Acta Pharmaceutica Sinica ; (12): 50-53, 2002.
Article in Chinese | WPRIM | ID: wpr-343402

ABSTRACT

<p><b>AIM</b>To establish a high-performance capillary electrophoresis (HPCE) chiral separation method for d-securinine and l-securinine, and use this method to investigate the stereoselective metabolism process of d- and l-securinine in Wistar rats.</p><p><b>METHODS</b>The electrophoretic condition and parameters were investigated and the optimized conditions were as following: the electrophoretic medium was 40 mmol.L-1 Tris-H3PO4 buffer (pH adjusted to 6.0 with H3PO4) containing 32 mmol.L-1 HP-beta-CD as chiral selector. Determination was carried out with a UV detector at 254 nm. The separations were performed at 16 degrees C with a positive voltage of 15 kV. Samples were injected into the capillary by pressure for 6 s. The biological samples (urine, bile, plasma and feces) of rats were alkalized and extracted with ethyl acetate.</p><p><b>RESULTS</b>The experimental results showed that the concentration of HP-beta-CD, the concentration of the running buffer and the pH value of the buffer were the main important factors which effected the resolution. d-Securinine and l-securinine were separated at baseline level under the determination conditions. The determination was not interfered by endogenous components and metabolites. After i.p. administration, the rats excreted more d-securinine than l-securinine through bile, urine and feces. The metabolism process in rats was stereoselective.</p><p><b>CONCLUSION</b>This method is simple, reliable and suitable for studying the stereoselective metabolism of securinine in rats.</p>


Subject(s)
Animals , Male , Rats , Alkaloids , Chemistry , Metabolism , Urine , Azepines , Chemistry , Metabolism , Urine , Bile , Metabolism , Electrophoresis, Capillary , Methods , Euphorbiaceae , Chemistry , Heterocyclic Compounds, 4 or More Rings , Chemistry , Metabolism , Urine , Heterocyclic Compounds, Bridged-Ring , Lactones , Chemistry , Metabolism , Urine , Molecular Structure , Piperidines , Chemistry , Metabolism , Urine , Plants, Medicinal , Chemistry , Rats, Wistar , Stereoisomerism
15.
Acta Pharmaceutica Sinica ; (12): 288-293, 2002.
Article in Chinese | WPRIM | ID: wpr-274825

ABSTRACT

<p><b>AIM</b>To study the in vitro and in vivo metabolism of (-)-securinine.</p><p><b>METHODS</b>The metabolic transformation of (-)-securinine was studied by using phenobarbital-induced rat liver microsomal incubate containing the NADPH-generating system in vitro and the constitution of the system was optimized. A reversed phase HPLC method was established to analyze the parent drug and its metabolites. The major metabolites were isolated and purified by liquid-liquid extraction, preparative TLC and HPLC, and their structures were elucidated as 6-hydroxyl securinine, 6-carbonyl securinine, 5 beta-hydroxyl securinine and 5 alpha-hydroxyl securinine by 1HNMR, 13CNMR and MS spectral analysis. An HPLC method was developed to analyze securinine and its metabolites in biofluids (bile, urine) of rat. The bile, urine and their enzymatic hydrolyzed samples of the rat i.p. administrated with (-)-securinine were determined by using this method.</p><p><b>RESULTS</b>Four main metabolites of (-)-securinine in rat hepatic microsome incubation were obtained and their structures were elucidated. Metabolites from in vitro study were confirmed in biofluids (bile, urine) which were collected from rats given securinine i.p. It was suggested that 6-hydroxyl securinine was excreted in conjugated form as well by analyzing enzymatic hydrolyzed bile.</p><p><b>CONCLUSION</b>The main metabolic pathway of (-)-securinine in vitro and in vivo is basically elucidated.</p>


Subject(s)
Animals , Male , Rats , Alkaloids , Metabolism , Urine , Azepines , Metabolism , Urine , Bile , Metabolism , Euphorbiaceae , Chemistry , Heterocyclic Compounds, 4 or More Rings , Metabolism , Urine , Heterocyclic Compounds, Bridged-Ring , In Vitro Techniques , Lactones , Metabolism , Urine , Microsomes, Liver , Metabolism , Piperidines , Metabolism , Urine , Plants, Medicinal , Chemistry , Rats, Wistar , Stereoisomerism
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