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.Effects of Cadmium on Rat Sperm Motility Evaluated With Computer Assisted Sperm Analysis
LI-CHUN XU ; SHU-YI WANG ; XIAO-FANG YANG ; XIN-RU WANG
Biomedical and Environmental Sciences 2001;14(4):312-317
Objective To study effects of cadmium on rat sperm motility evaluated with computer assisted sperm analysis. Methods Different doses of cadmium chloride (0.2,0.4,0.8mg Cd/kg BW) were administrated ip to adult male Sprague-Dawley rats. Control animals received the same volume of 0.9% NaCl solution. After 7 days, the rats were sacrificed with their testes removed. A part of one testis was used for testicular sperm head counts and daily sperm production observation. The motility of spermatozoa obtained from cauda epididymides using the “diffusion”method was measured by computer assisted sperm analysis(CASA). Results The sperm head counts and daily sperm production decreased significantly in the high dose group. The motility of spermatozoa in the middle dose group was reduced significantly. No motile sperm was found in the high dose group. The results suggest that germinal epithelium was impaired irreversibly in a short time to produce toxic effects on spermatogenesis at high cadmium doses. Conclusion Cadmium may reduce sperm motility at a dose far below the dose affecting sperm production at this time point. The motility of sperm is an early and sensitive endpoint for the assessment of cadmium toxicity on male reproduction.
6.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
8.Overwhelming Th17 cells compared to insufficient CD4+ regulatory T cells in rheumatoid arthritis
Tian WANG ; Yi ZHAO ; Xu LIU ; Xia LIU ; Ru LI ; Limin REN ; Hua YE ; Zhanguo LI
Chinese Journal of Rheumatology 2009;13(7):439-442
Objective To identify interleukin (IL)-17-producing T cells and Foxp3 positive CD4 positive T ceils from patients with rheumatoid arthritis (RA), and investigate their cytokine levels as well as their correlations. Methods Flow cytometry was used to analyze the subsets of T cells in peripheral blood from 39 RA patients and 40 healthy donors. IL-17, IL-6, IL-23 and transforming growth factor (TGF)-beta levels in sera of these subjects were tested by ELISA. Results IL-17+CD4+ T cells increased significantly and IL-17, IL-6 and IL-23 elevated markedly in peripheral blood of RA patients compared to healthy donors (P< 0.01 ). However,Foxp3+CD4+T cells decreased evidently (P<0.01) and TGF-beta did not increase in RA pati-ents when compared to healthy donors (P>0.05). Conclusion This study suggests that Th17 cells predomin-ance coupled with relatively insufficient CD4+ regulatory T cells in RA is mainly caused by alterations of rela-ted cytokines.
9.Serum Uric Acid and Prehypertension
Tao CHEN ; Wei LI ; Bo HU ; Yang WANG ; Xiao-Ru CHENG ; Xuan JIA ; Yi SUN ;
Chinese Journal of Hypertension 2006;0(08):-
Background Previous experimental and clinical studies have proved that elevated serum uric acid increased risk for developing hypertension.Whereas,there are a paucity of information on the relationship between serum uric acid and prehypertension.Objective The purpose of this research is to evaluate the association between the serum uric acid and prehypertension.Method A cohort of seven thousand eight hundred thirty-nine subjects without hypertension and other cardiovascular diseases were recruited from a cross sectional study in urban and rural place in 9 provinces during 2005-2006.Based on serum uric acid(324 ?mol/L for overall population,366 ?mol/L for male,285 ?mol/L for female),people were categorized into quartiles.The odds ratio for prehypertension was calculat ed with the lowest quartile as the reference.Results The prevalence of prehypertension increased with increasing uric acid in total population(P324 ?mol/L)to lowest quartile 1(
10.Practice in experimental teaching reform of molecular biology course for postgraduates
Xia LI ; Jing ZHANG ; Qinhao WANG ; Yi RU ; Jian ZHANG ; Libo YAO
Chinese Journal of Medical Education Research 2014;13(12):1260-1263
Molecular biology experiment is an important course for postgraduates in medical university.Through updating and optimizing what to teach(emphasizing study design,setting up comprehensive experiment and updating practical techniques),improving teaching mode(paying attention to experimental preparation,teacher qualification and postgraduates' capability training) and perfecting evaluation approaches(combining the experiment report with experimental summary and regular grades with experimental practice),good results have been obtained.