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.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.
7.Profiling on the Invention Patents of Uncaria rhynchophylla in China
Xiaoyu GAO ; Ru DING ; Ping YI ; Daoping WANG ; Tengbing HE ; Changhu LIN
World Science and Technology-Modernization of Traditional Chinese Medicine 2017;19(1):178-183
U.rhynchophylla is an important herb in Chinese medical treasure with the functions of calming endogenous wind and arresting convulsion,clearing away heat and calming the liver,for the treatments of hypertension,epilepsy and convulsion,crying with fear in children.This paper retrieved and collated 3,304 items of application information in the invention patents over uncaria before July,2016.Data of the basic sciences were collected from Chinese Science Citation Database (CSCD) and those of situation analysis of patents from Patent Online Analysis System of Chinese Academy of Sciences.Year,region,patented technology,patentee and key technology were involved and analyzed in the system for profound investigation of the current situation and developing trend of invention patent application over uncaria.It was found that trace elements and chemical composition beneficial to human health were receiving favors from the market with rapt attention focusing on patent applications.However,there were still major limitations in the application and the patent quality needed improving.In conclusion,further development and the utilization of uncaria presented promising prospects.
9.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
10.Acupuncture for premature ovarian failure: a prospective cohort study.
Fei WANG ; Yi-Gong FANG ; Ying-Ru CHEN ; Yan BAI ; Xue WU ; Bao-Yan LIU
Chinese Acupuncture & Moxibustion 2014;34(7):653-656
OBJECTIVETo explore the clinical efficacy and action mechanism of acupuncture for premature ovarian failure (POF).
METHODSAccording to prospective cohort study design, 30 cases were included. Based on theory of regulating Chong and Conception Vessels as well as soothing the liver and calming the nerves, acupuncture at Guanyuan (CV 4), Dahe (KI 12), Taixi (KI 3), Taichong (LR 3), Baihui (GV 20) was applied, three times per week and 3 months were considered as one session. Totally two sessions were performed. The menstruation condition, estradiol (E2), follicle-stimulating hormone (FSH) and scores of the clinical perimenopausal symptoms were taken as treatment outcomes.
RESULTSThe total effective rate was 86.7% (26/30) and the cured rate was 16.7% (5/30). The recovery rate of menstruation was 16.7% (5/30) and the regain rate of menstruation was 56.7% (17/30). After the treatment, the level of E2 was significantly increased from (45.41 +/- 18. 09) pmol/L to (59.07 +/- 24.21) pmol/L (P < 0.05), and the score of perimenopausal symptoms was obviously reduced from 14.28 +/- 8. 30 to 4.04 +/- 3.28 (P < 0.01). However, no statistical differences could be seen in FSH before and after treatment (P > 0.05).
CONCLUSIONAcupuncture has certain effect on improving menstruation and perimenopausal symptoms in POF patients, which is likely to he related with increasing the level of E2.
Acupuncture Therapy ; Adolescent ; Estradiol ; metabolism ; Female ; Humans ; Luteinizing Hormone ; metabolism ; Primary Ovarian Insufficiency ; metabolism ; therapy ; Prospective Studies ; Young Adult