3.Preparation of Clopidogrel Bisulfate Tablets and Optimization of the Formulation and Technology
Xia SUN ; Xue WANG ; Qingming GUO ; Wei XIAO
China Pharmacy 2015;26(31):4429-4432
OBJECTIVE:To prepare Clopidogrel bisulfate tablets,and to optimize its formulation and technology. METHODS:The single factor test and compatibility test were used to optimize the fillers,disintegrating agents,adhesive,lubricants and prepa-ration technology;using sticking situation and disintegration time as indexes,the orthogonal test was used to optimize the amount of disintegrating agents [low substituted hydroxypropyl cellulose(L-HPC)],lubricants(hydrogenated vegetable oil and PEG6000), and the optimal technology was validated. The dissolution of prepared tablet and imported tablet(Plavix)in water,pH 2.0 hydro-chlorate buffer,pH 4.5 phosphate buffer(PBS)and pH 6.8 PBS were investigated,and influential factor test was conducted. RE-SULTS:Clopidogrel bisulfate tablets were prepared with dry granulating. The optimal formulation (1 000 tablets) was as follows as clopidogrel bisulfate 97.8 g,mannitol 84 g,amylum pregelatinisatum 36 g,L-HPC 8 g,hydrogenated vegetable oil 8 g, PEG6000 6 g;no tablet compressing sticking situation was found in prepared tablets and it owned medium disintegration time;ac-cumulative dissolution curves of prepared tablets in 4 kinds of medium were similar to those of Plavix;there were no significant dif-ference in results of influential factor test between prepared tablet and Plavix. CONCLUSIONS:Clopidogrel bisulfate tablets are prepared successfully,and the formulation is reasonable,practical,stable and controllable in quality.
5.Experimental study on the effect of different moxibustion durations on rats with rheumatoid arthritis
Xinyu WU ; Yang WANG ; Zhiling SUN ; Xue QIN ; Jiang ZHAO ; Xiao XU ; Yongyi ZHANG ; Lian XUE
Journal of Acupuncture and Tuina Science 2017;15(3):177-183
Objective: To observe the effect of different moxibustion durations on rats with rheumatoid arthritis (RA) and to evaluate the relationship between moxibustion amount and moxibustion efficacy.Methods: Eight rats were randomly selected as a normal group from the 40 male Sprague-Dawley (SD) rats, and the other 32 rats were used to establish typeⅡ collagen-induced RA models. After successful modeling, the 32 rats were randomly divided into a model group, a moxibustion for 20 min group, a moxibustion for 40 min group and a moxibustion for 60 min group, with 8 rats in each group. Rats in the normal group did not receive modeling and moxibustion intervention; rats in the model group did not receive moxibustion after modeling; rats in the moxibustion for 20 min group, the moxibustion for 40 min group and the moxibustion for 60 min group were treated with moxibustion at Shenshu (BL 23) and Zusanli (ST 36) for 20 min, 40 min and 60 min, respectively. Six days were a course of treatment, with a total of 3-course treatments and a 1-day rest between the courses of treatment. After treatment, the serum levels of interleukin (IL)-1β and tumor necrosis factor (TNF)-α, arthritis index (AI) scores, toe volumes and pathological score of synovitis were evaluated in the rats.Results: Compared with the normal group, the serum IL-1β and TNF-α levels, and the toe volumes in the model group were increased, and the differences were statistically significant (P<0.01), before the treatment. Compared with the model group, the serum IL-1β and TNF-α levels, toe volumes and arthritis index (AI) scores were significantly decreased in the moxibustion for 20 min group, the moxibustion for 40 min group and the moxibustion for 60 min group (P<0.05 orP<0.01 ). Compared with the moxibustion for 20 min group and the moxibustion for 60 min group, serum IL-1β and TNF-α levels, toe volumes and AI scores were decreased more significantly in moxibustion for 40 min group, and the differences were statistically significant (P<0.05 orP<0.01). There were no significant differences in serum IL-1β and TNF-α levels, AI scores and toe volumes between the moxibustion for 20 min group and the moxibustion for 60 min group (allP>0.05). The synovial histopathological improvement was the most obvious in the moxibustion for 40 min group, when the synovial histopathological changes were compared among the moxibustion for 20 min group, moxibustion for 40 min group and moxibustion for 60 min group.Conclusion: The therapeutic efficacy of moxibustion for 40 min in RA rats was more significant than that of moxibustion for 20 min and moxibustion for 60 min, indicating that the duration of moxibustion is the main factor affecting its therapeutic efficacy.
6.Phytoestrogens in application prospect of treatment of myocardial ischemia/reperfusion injury.
Guang LI ; Xiao-yan XING ; Mei-shuang ZHANG ; Jin-jin SHI ; Xue-hong DENG ; Gui-bo SUN ; Xiao-bo SUN
China Journal of Chinese Materia Medica 2015;40(16):3132-3136
Reperfusion is the most effective treatment for acute myocardial infarction, markedly reducing mortality and morbidity. Reperfusion however induces necrotic and apoptotic damages to cardiomyocytes, that were viable prior to reperfusion, a process called myocardial ischemia/reperfusion injury(MI/RI). Over the past 30 years, hundreds of experimental interventions (both pharmacologic and nonpharmacologic) have been reported to protect the ischemic myocardium in experimental animals; however, with the exception of early reperfusion, none has been translated into clinical practice. The population-based survey assessed men have about twice the total incidence of morbidity and mortality of women, and the sex gap in morbidity tends to diminish after age 45 years. So hormone replacement therapy (HRT) is given to treat the MI/RI, and lots of studies shows that the side effect is greater for estrogen, compared with phyestrogen. In this article, we review the important pathogenesis of myocardial ischemia reperfusion injury, the prevention and limitations of HRT. And we highlight the mechanism of phyestrogens treatment the MI/RI in experiment. The aim is to provide the theoretically new way of develop the safe and effective products for the researchers.
Animals
;
Humans
;
Myocardial Ischemia
;
drug therapy
;
Myocardial Reperfusion Injury
;
drug therapy
;
Phytoestrogens
;
administration & dosage
;
Plant Extracts
;
administration & dosage
7.A comparative study of the effect of low-frequency electroacupuncture on blood lipids between men and women with simple obesity
kang Xiao XU ; Fei GAO ; li Li WANG ; qiu Zhong WU ; lei Yu LIANG ; xue Xiao SUN ; yi Xiao DU ; hong Xiao ZHOU ; hong Li SUN
Journal of Acupuncture and Tuina Science 2017;15(6):415-419
Objective: To observe the difference of the effect of low-frequency electroacupuncture (EA) on blood lipids between male and female patients with simple obesity due to damp induced by spleen deficiency. Methods: Eighty patients with simple obesity were recruited, including 37 males and 43 females, to receive low-frequency EA by selecting Yinlingquan (SP 10), Sanyinjiao (SP 6), Zusanli (ST 36), Fenglong (ST 40), Quchi (LI 11), Tianshu (ST 25), Zhongwan (CV 12), Shuifen (CV 9), Qihai (CV 6) and Guanyuan (CV 4), with needles retained for 30 min. The treatment was given once a day, 10 sessions as a treatment course, for 2 courses in total. The contents of body fat percentage (F%), total cholesterol (TC), triglyceride (TG), high-density lipoprotein (HDL), low-density lipoprotein (LDL), blood glucose (Glu) and adiponectin (ADPN) in serum were observed to see the changes, and the two groups were compared and analyzed. Results: After the treatment, F%, and serum contents of TC, TG, LDL, Glu and ADPN dropped significantly in the two groups (P<0.05 or P<0.01) and the serum content of HDL increased significantly in male group (P<0.05). The decrease of F% in female group was more significant than that in male group (P<0.01); the decrease of ADPN in male group was more significant than that in female group (P<0.05). Conclusion: EA can regulate the disordered blood lipids in male and female patients with simple obesity, with certain differences between genders. The decrease of subcutaneous fat content is more significant in females than that in males, while the decrease of ADPN is more significant in males.
8.Studies on the cell growth, differentiation and terpene lactone accumulation in Ginkgo biloba cell suspension cultures.
Chinese Journal of Biotechnology 2004;20(3):445-449
To provide supports for Ginkgo biloba cell engineering for production of Terpene lactones (Ginkgolides and bilobalide), the cell suspension were established from calli induced from zygote embryos and stems of 30-day-old seedlings respectively. The relationship between cell growth, differentiation and the terpene lactone accumulation in these suspension cultures were investigated. HPLC determination indicated that, the ginkgolide B was found in the embryo derived cell suspension cultures at 0.044% of cell dry weight, and this result was the first time reported in this study. The accumulation of terpene lactone in the suspension cultures derived from both the embryo and seedling stems are effected by the level of the cell differentiation. The ginkgolide B was only found in small cell aggregates in the size smaller than 2mm, and the highest level of ginkgolide B was accumulated in cell aggregates in the size smaller than 1mm; however, the cell aggregates in the size bigger than 3mm could only produced bilobalide and ginkgolide A. In the same size aggregates of the suspension cultures the terpene lactone accumulation is strongly effected by the source of the explant. When the size of cell aggregates was in less than 1mm, the concentration of bilobalide, ginkgolide A and B in the cell suspension cultures derived from the embryos was 2, 1.4 and 0.56-fold, respectively, higher than that of cell cultures derived from seedling stems.
Bilobalides
;
analysis
;
Cell Differentiation
;
physiology
;
Cell Proliferation
;
Culture Techniques
;
methods
;
Ginkgo biloba
;
growth & development
;
metabolism
;
Ginkgolides
;
analysis
;
Lactones
;
analysis
9.Effects of Citalopram on frontal cortical neurons' bax mRNA bcl-2 mRNA expression and cell apoptosis of rat after stress.
Ai-yue YU ; Xiao-hong SUN ; Xue-hong LIU ; Jin ZHOU ; Lan WANG
Chinese Journal of Applied Physiology 2015;31(5):455-461
OBJECTIVETo study the effects of Citalopram on the mRNA expression of bax and bel-2 in frontal cortical neurons and on cell apoptosis of rats after stress.
METHODSTwenty-four healthy male SD rats were randomly divided into three groups (n = 8). The control group did no receive any treatment, the stress group was subject to stress and given normal saline and experimental group was given Citalopram irrigation stomach after stress. Rats were forced to swim to establish chronic stress model (15 min/d, 4 weeks), bax, bcl-2 mRNA expression were tested by in situ hybridization technique (ISH), TUNEL assay was used to determine cell apoptosis, Nikon image analysis software were used to measure the number of positive cells in each index.
RESULTSCompared with the control group, the stress group showed a larger number of bax mRNA expressing cells( P < 0.01), a smaller number of bcl-2 mRNA expressing cells (P < 0.01), and the staining intensity of positive cells was significantly reduced( P < 0.01). Compared with the stress group, the experiment group showed more reduced number of bax mRNA positive cells( P < 0.01) and significantly increased bcl-2 mRNA positive cells( P < 0.05), a small amount of positive cells were found, compared with that in the stress group, nuclear condensation in the experimental group was reduced significantly and the staining was obviously weaker( P < 0.01).
CONCLUSIONCitalopram significantly antagonizes bax mRNA and potentiatesbcl-2 mRNA protein expression and inhibits apoptosis of rat prefrontal cortical neurons caused by chronic stress, which might be one possible mechanism of Citalopram for prevention and treatment of psychosis caused by chronic stress.
Animals ; Apoptosis ; Citalopram ; pharmacology ; Male ; Neurons ; drug effects ; metabolism ; Prefrontal Cortex ; cytology ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; RNA, Messenger ; Rats ; Rats, Sprague-Dawley ; Stress, Physiological ; bcl-2-Associated X Protein ; metabolism
10.Circulatory sleep apnea: Preliminary report of clinical observation on sleep apnea in patients with chronic heart failure.
Si-xin XIE ; Xing-guo SUN ; Fu-rong WANG ; Xiao-yue TAN ; Xue-mei ZHANG
Chinese Journal of Applied Physiology 2015;31(4):329-331
OBJECTIVEThe aim of this study is to investigate the occurrence and mechanism of Cheyne-Stokes breathing pattern in patients with heart failure.
METHODSFifty-six patients who performed polusomnography sleep testing at National Center of Cardiovascular Diseases Fuwai Hospital from March to May in 2015. We divided them into chronic heart failure (CHF) group and non-CHF group.
RESULTSThe occurrences of sleep apnea in two groups were high. In CHF group (n = 11) , there were 10 patients with apnea hypopnea index (AHI) > 5; and their AHI was 23.93 ±14.63. In non-CHF group (n = 45), there were 33 patients whose AHI > 5; and their AHI was 16.20 ± 18.76. The ratio of center sleep apnea to all gross sleep apnea ratio in CHF group was higher than that in non-CHF group (80.21% ± 30.55% vs 27.16% ± 35.71%, P < 0.01 ).
CONCLUSIONBased upon the new theory of holistic integrative physiology and medicine, we explain the mechanism of circulatory dysfunction induce the oscillation breathing in patients with CHF. The sleep apnea and C-S respiration in CHF should be called circulatory sleep apnea, rather than central sleep apnea.
Cheyne-Stokes Respiration ; Chronic Disease ; Heart Failure ; physiopathology ; Humans ; Polysomnography ; Sleep Apnea Syndromes ; physiopathology ; Sleep Apnea, Central