2. Effect of polymers on dissolution of nifedipine solid dispersion
Chinese Pharmaceutical Journal 2016;51(8):635-638
OBJECTIVE: To investigate the effect of copovidone (PVP/VA), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and hydroxypropylmethylcellulose (HPMC) on drug dispersion and in vitro dissolution of solid dispersion by using nifedipine as model drug. METHODS: Nifedipine solid dispersion was prepared by hotmelt extrusion (HME) technology, and the drug dispersion was evaluated by differential scanning calorimetry (DSC) and dissolution test. RESULTS: DSC analysis results showed that nifedipine was amorphous in all HME extruders. Drug release from solid dispersion prepared with HPMCAS reached 100% in 30 min, but was only 75% for PVP/VA solid dispersion. Adding 5% HPMC E5 to PVP/VA extruders before dissolution test could raise the drug release from 75% to 90%. CONCLUSION: HPMCAS or combination of PVP/VA and HPMC E5 are desirable polymers for nifedipine solid dispersion.
3. Preparation and in vitro evaluation of ciprofloxacin hydrochloride gastro-retentive tablets
Chinese Pharmaceutical Journal 2015;50(24):2135-2138
OBJECTIVE: To investigate the effect of polymers, including hydrophilic polymers and swelling aids, on floatability and dissolution of ciprofloxacin hydrochloride gastro-retentive tablets. METHODS: Hydroxypropyl methyl cellulose (HPMC), hydroxyethylcellulose (HEC) and hydroxypropylcellulose (HPC) were used as hydrophilic swelling excipients, and disintegrants crospovidone (PVPP XL and PVPP XL-10) or croscarmellose sodium (CCS) were used as swelling agents to facilitate the swelling/floating and drug release. Initial floating time and floating duration were tested to evaluate buoyance, and drug dissolution was tested to evaluate the controlled release. RESULTS: Using HPMC K250 and PVPP XL as excipients for ciprofloxacin hydrochloride gastro-retentive tablets could obtain products with rapid onset of floating, long floating durion and desirable drug release. CONCLUSION: Variety and amount of polymers have dramatic effects on buoyance and drug release of gastro-retentive tablets. HPMC K250 and PVPP XL are suitable excipients for ciprofloxacin hydrochloride gastro-retentive tablets.
4.Indomethacin for prevention of post-ERCP pancreatitis and hyperamylasemia
Tao LIN ; Yi ZHOU ; Jun WANG ; Ru YAO ; Li JIANG ; Rutang FANG ; Suli WANG ; Yan XIE
Chinese Journal of Digestive Endoscopy 2012;29(4):185-187
Objective To investigate the preventive effect of Indomethacin for post-ERCP pancreatitis and hyperamylasemia.Methods A total of 600 patients,who were undergoing ERCP,were randomly divided into 3 groups to receive anal Indomethacin (n=200),intravenous octreotide (n=200) or no special medication (n=200) before ERCP.The level of serum amylase before and 24h after ERCP were measured,and the rate of acute pancreatitis and hyperamylasemia after ERCP were assessed.Results Serum amylase levels before ERCP of all groups were normal.The mean serum amylase level of Indomethacin group (101.3±77.7 U/L) after ERCP was significantly lower than those of octreotide group ( 176.6±138.3 U/L,P =0.040 ]and control group (227.2±264.9 U/L,P=0.048),while there was no difference between octreotide group and control group ( P>0.05 ).The incidence of post-ERCP pancreatitis in Indomethacin group (2.5%) was significantly lower than that of control group (9.5%,P=0.003),while there was no difference between octreotide group (4.5%) and control group ( P=0.05 ).The incidence of hyperamylasemia after ERCP in Indomethacin group (5.5%) was significantly lower than that of control group ( 13.5%,P=0.006 ),while there was no difference between octreotide group (10.0%) and control group ( P>0.05 ).Conctusion Anal administration of Indomethacin before ERCP can effectively reduce the incidence of acute pancreatitis and hyperamylasemia after ERCP.
5.Effect of terpene penetration enhancer and its mechanisms on membrane fluidity and potential of HaCaT keratinocytes.
Yi LAN ; Jing-yan WANG ; Yan LIU ; Qing-guo RU ; Yi-fei WANG ; Jing-xin YU ; Qing WU
China Journal of Chinese Materia Medica 2015;40(4):643-648
The aim of this paper was to investigate the effect of terpene penetration enhancers on membrane fluidity and membrane potential using HaCaT keratinocytes, and study the potential mechanisms of these terpene compounds using as natural transdermal penetration enhancer. Six terpene compounds, namely menthol, limonene, 1,8-cineole, menthone, terpinen-4-ol and pulegone, were chosen in this study on account of their good penetration-enhancement activities. The cytotoxicity of these terpene compounds was measured using an MTT assay. The fluorescence recovery after photobleaching (FRAP) technique was employed to measure the change of membrane fluidity of HaCaT cells. The flow cytometer was used to study the alteration of membrane fluidity of HaCaT cells, and investigate the effect of terpene compounds on intracellular Ca2+. It was found that 6 terpene compounds possessed low cytotoxicity in comparison to the well-established and standard penetration enhancer azone. Those terpene compounds could significantly enhance HaCaT cells membrane fluidity and decrease HaCaT cells membrane potentials. Meanwhile, after treated with various terpene compounds, the Ca2(+)-ATPase activity and intracellular Ca2+ of HaCaT cells was decreased significantly. Terpene penetration enhancers perhaps changed the membrane fluidity and potentials of HaCaT cells by altering the Ca2+ balance of the cell inside and outside, resulting in the low skin permeability to increase the drug transdermal absorption.
Cell Line
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Drugs, Chinese Herbal
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pharmacokinetics
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Humans
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Keratinocytes
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drug effects
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metabolism
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Membrane Fluidity
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drug effects
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Skin Absorption
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drug effects
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Terpenes
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pharmacokinetics
6.Preparation and in vitro evaluation of doxorubicin-loaded magnetic iron oxide nanoparticles.
Song SHEN ; Lin WU ; Cheng-Run WANG ; Xue-Yong QI ; Yan-Ru GE ; Yi JIN
Acta Pharmaceutica Sinica 2013;48(12):1844-1849
PEG-modified magnetic Fe3O4 (Fe3O4-PEG) nanoparticles were sythesized using a solvothermal reaction and characterized with transmission electron microscopy (TEM) and thermo gravimetric analysis (TGA). The photothermal effect and photothermal destruction of cancer cells were evaluated. Then the doxorubicin loaded Fe3O4-PEG (DOX-Fe3O4-PEG) nanoparticles were prepared. The cytotoxicity and combined chemotherapy/photothermal therapy (PTT) effect were investigated. Uniform PEG coated Fe3O4 nanoparticles with particle size of 155 nm were obtained in the experiment. The loading and release of doxorubicin on Fe3O4-PEG were pH-dependent. The drug loading capacity in water was 21%. The results of MTT indicated a good biocompatiblity of Fe3O4-PEG nanoparticles and high cytotoxicity of DOX-Fe3O4-PEG. In combined therapy experiment, photothermal therapy demonstrated unambiguously enhanced chemotherapy efficacy. In conclusion, the obtained Fe3O4-PEG nanoparticles which exhibit good photothermal effect and drug loading capacity can be used for chemotherapy and photothermal therapy. The synergetic anti-tumor activity indicates the potential for the combined application of chemotherapy and photothermal therapy in cancer treatment.
Antibiotics, Antineoplastic
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administration & dosage
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pharmacology
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Cell Survival
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drug effects
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Doxorubicin
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administration & dosage
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pharmacology
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Drug Carriers
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Ferrosoferric Oxide
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chemistry
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Humans
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Hyperthermia, Induced
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MCF-7 Cells
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Magnetite Nanoparticles
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chemistry
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Particle Size
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Polyethylene Glycols
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chemistry
7.Clinical observation of porcelain and composite veneer in repairing dental fluorosis
Yu, SUN ; wei-li, XIE ; wen-ru, JIANG ; Yi-xin, BAI ; Han, WANG
Chinese Journal of Endemiology 2009;28(5):565-567
Objective To observe the clinical changes in resin and porcelain veneer in restoring dental fluorosis in order to provide a basis for the repair of dental fluorosis. Methods Fifty six severe dental fluorosis patients were divided into porcelain and resin teeth group in the department of Prosthetics, school of Stomatology, Harbin Medical University during 2005 to 2008. All 162 teeth of 25 patients in porcelain group were veneered with porcelain. 201 teeth of 31 patients in resin group were repaired with resin. To evaluat the clinic effect, the veneer surface color was detected by the Easyshade computer-aided colorimeter when the repair was completed and 18 months afterward. The edge of veneer adaptation, retention, secondary caries and abutment were examined after 18 months, and classified by color, shape, function and feeling. Results The color difference between the porcelain and resin teeth group was 0.27±0.20 and 0.21±0.15 when it was completed, and it was 0.28±0.21 and 0.77± 0.68 respectively after 18 months. The color difference value of the porcelain teeth group was lower when it was completed than 18 months later(t=-13.55, P<0.01). The color difference value of the resin teeth group was lower than the porcelain teeth group after 18 months(t=-12.60, P<0.01). The percentage of level A of veneer adaptation in the porcelain group[100%(162/162)] was higher than the resin group[91.04% (183/201), χ2=15.26, P< 0.01) after 18 months. The clinical effect was divided into three degrees of excellent, moderate or failed, into which the number of the teeth catergorized was 158, 4 and 0 in porcelain group, 148, 56 and 4 in resin group respectively. The clinical effect of the porcelain group was superior to the resin group(χ2=44.24, P<0.01). Conclusions The surface color of porcelain veneer last 16nger than the resin veneer, the adaptation and clinical effect is also superior to the resin veneer. But the long-term efficacy of two methods needs further study, especially of the resin veneer.
8.Influence of preschool children′s habits at home on the prevalence of caries in Huangpu District(Eastern Part)
Hong-xia QU ; Yi-jun WANG ; Ru-yu CHEN
Shanghai Journal of Preventive Medicine 2020;32(10):801-
Objective To provide supporting evidence to prevention and controlling of caries in preschool children in Huangpu District(Eastern Part), by studying the influence of their habits at home on the prevalence of caries. Methods The oral health of preschool children in Huangpu District was examined, and their habits at home were recorded through survey questionnaire, including sugary diet, tooth brushing, parents′ attitude for oral health. Results Sugary diet could affect the prevalence of caries.There was no association between dental caries and times of tooth brushing.Parents′ attitude for oral health is the risk factor for the children′s caries. Conclusion Because of the higher prevalence of caries in the children in our district, effective measures should be taken.In addition, policy should consider how to ensure that children with high-risk dental caries receive adequate prevention and early care.
9.Effects of Shen-wu Capsule on motor function and content of dopamine in striatum in Huntington model rats
Ru-yi ZHANG ; Lan ZHANG ; Lin LI ; Hui WANG ; Cuifei YE
Chinese Journal of Rehabilitation Theory and Practice 2002;8(9):513-515
ObjectiveTo investigate the role of mitochondrial dysfunction in neurodegenerative diseases and the pharmacological effects of Shen-wu Capsule.MethodsSD rats were divided into 6 groups with 10 rats each:model group was developed by peritoneal injection of 3-nitropropionic acid(3-NPA) 20mg/kg, once every another day. Haloferidoli was used as the positive drug (given to positive control group from 10μg/100g/day to 100μg/100g/day, during modeling). Low dose of Shen-wu Capsule is 0.45g/kg; middle dose of Shen-wu Capsule is 0.9g/kg; high dose of Shen-wu Capsule is 1.8g/kg (once a day for 25days). The rats in normal control group were peritoneally injected with saline and were fed with water.The open field test was used to test the space recognition ability and excitability of CNS of rats. The climbing test was used to test strength of muscles.The content of dopamine(DA) and it's metabolite dihydroxyphenylacetic acid (DOPAC),5-HT in stratium of all groups were detected by high performance liquid chromatograph (HPLC-ECD).ResultsThe 3-NPA model rats showed decrease of activity, rigidity and stagger just like clinical patients with Huntington's diseases. In open field test all indexes of 3-NPA model rats are decreased (P<0.05), while Shen-wu Capsule low dose and high dose can improve all the indexes. There is no difference in strength of muscles among all groups. The content of DA,DOPAC and 5-hydroxytryptamine (5-HT) were distinctly decreased in 3-NPA model rats(P<0.01); rats in three groups of Shen-wu Capsule and positive drug control groups showed increased content of these neurotransmitter(P<0.01). Conclusions Rats injected with 3-NPA can mimic the abnormal behaviors and changes of neurotransmitter in stratium of Huntington's patients, Shen-wu Capsule can ameliorate the behavior of model animals and improve the content of DA,DOPAC and 5-HT in stratium.
10.Mechanism study on preventive and curative effects of buyang huanwu decoction in Qi deficiency and blood stasis diseases based on network analysis.
Fan DING ; Qian-ru ZHANG ; Yuan-jia HU ; Yi-tao WANG
China Journal of Chinese Materia Medica 2014;39(22):4418-4425
In this study, researchers adopted the network analysis method to study Buyang Huanwu decoction at three levels, namely chemical ingredients, targets and diseases, and discovered the potential effect of Buyang Huanwu decoction in cancer treatment. Besides, they analyzed the "target-target" network of Buyang Huanwu decoction based on diseases, calculated four network indexes, namely node centrality, closeness centrality, betweenness centrality and eigenvector centrality for a comprehensive evaluation on the importance and significance of each target in the network. Afterwards, key targets of Buyang Huanwu decoction were excavated to obtain two important targets--COX-2 and PPAR-gamma, which may be important targets involved in the qi deficiency and blood stasis diseases. Meanwhile, the two targets were the basis to build the core network of "chemical component-target-disease" of Buyang Huanwu decoction, which provided reference for further studies on the effect of Buyang Huanwu decoction in treating qi deficiency and blood stasis diseases. According to the study, the network analysis method was helpful to excavate potential targets Buyang Huanwu decoction in treating qi deficiency and blood stasis diseases, and could provide methodological reference for revealing the mechanism of Buyang Huanwu decoction at multiple levels, with a guiding significance for interpreting mechanisms of traditional Chinese medicinal formulae and developing new drugs.
Drugs, Chinese Herbal
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pharmacology
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Hematologic Diseases
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drug therapy
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Medicine, Chinese Traditional
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Qi
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Yang Deficiency
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drug therapy
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Yin Deficiency
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drug therapy