1.Study of the Intestinal Absorption Mechanism of Galangin in Rats
Junlin HU ; Tao YANG ; Kaiyong HE
Herald of Medicine 2015;(5):612-616
Objective To investigate the absorption characteristics of galangin in various intestinal segments. Methods Single-pass intestinal perfusion was employed in rats, and the mass quality was used to correct the volume;Galangin in rat intestinal perfusion was determined by HPLC to investigate the effects of intestinal segments, drug concentration and P-glycoprotein ( P-gp) inhibitor on drug’ s absorption. Results Galangin could be absorbed in the whole intestine, and its Ka values in the segments of duodenum, jejunum, ileum and colon were (5. 12±1. 14)í10-2,(2. 23±1. 02)í10-2,(4. 61± 0. 75)í 10-2 and(2. 68 ± 0. 70)í10-2 ·min-1 ,respectively. Meanwhile, the values of the Ka in the segment of ileum were not affected by the drug concentration and P-gp inhibitor. Conclusion The galangin is well absorbed in rats intestinal segments. The absorption procedure is mainly controlled by passive diffusion but unaffected by P-gp efflux protein.
2.Cytotoxicity of Ibuprofen Raw Material and its Part of Impurities
Yang WANG ; Kaiyong HE ; Jiate SHEN ; Yating YANG
China Pharmacist 2017;20(4):769-771
Objective:To evaluate the cytotoxicity of ibuprofen and its 6 kinds of impurities.Methods:Different concentrations of ibuprofen and the impurities were used to act on mouse fibroblasts (L929) for 72 h,and the cytotoxicity was observed under a microscope.Results:In ibuprofen raw material,the cytotoxicity of impurity B was the weakest with slight toxicity,the cytotoxicity of impurity N,D,J and V was moderate,and that of impurity E was severe.Conclusion:At the same concentration,the toxicity of impurity E is the strongest,and its content in ibuprofen preparations should be strictly controlled.
3.Pharmacological Study on Chaigeshubiao Granules
Yating YANG ; Xiaojun LYU ; Suwen ZHOU ; Wangping PAN ; Kaiyong HE
Herald of Medicine 2016;(2):137-140
Objective To study the antipyretic,anti-inflammatory and analgesic effects of Chaigeshubiao granules. Methods Animals were randomly divided into 6 groups:blank control group,indomethacin group,Fengreganmao granules group and the high, the medium and the low dosage groups of Chaigeshubiao granules ( 26, 13, 6. 5 g . kg-1 ) . Each group was administered via intragastric administration once a day for 5 days.Rat model suffering from fever by dried yeast,relieving fever of Chaigeshubiao granules was investigated;Rats with toe swelling by 1% carrageenin and mice with ear swelling by dimethylbenzene were applied to observe anti-inflammatory effects of Chaigeshubiao granules were observed;The pain models induced by 0. 6%acetic acid and the hot-plate tests in mice were used to observe the analgesic effects of Chaigeshubiao granules. Results Compared with negative control group,Chaigeshubiao granules in high dosage could obviously decrease the temperature of rat with fever induced by dried yeast 0.5 h later,and the medium dosage group decreased 4-6 h later. Moreover,Chaigeshubiao granules in high dosage could inhibit inflammatory reaction of rat with toe swelling caused by albumen at 1 h,2 h,3 h,when the medium dosage group inhibited at 2 h,3 h,4 h. The inhibition ratio of the mice with ear swelling induced by dimethylbenzene was 58.2%, 52.0% and 53.9%,respectively at the high,medium and low dose groups. And the inhibition ratio of retortion of mice by 0.6%acetic acid was 50.5%,68.8%,58.1%,respectively, at the high,medium and low dose groups. In addition,the high,medium and low dose groups reduced the pain reaction latency of mice in the hot-plate tests. Conclusion Chaigeshubiao granules have antipyretic,anti-inflammatory and analgesic actions.
4.Anti-inflammation,Analgesia and Ulcer Healing Promotion of Zhenbing Koukuining Tablets
Shan WU ; Kaiyong HE ; Wangping PAN ; Yating YANG ; Rui ZOU
China Pharmacist 2015;(4):565-567
Objective:To investigate the anti-inflammation,analgesia and ulcer healing promotion of Zhenbing Koukuining tab-lets. Methods:The anti-inflammatin,analgesia and ulcer healing promotion of the preparation was respectively observed in the croton oil-induced auricular edema in mice,acetic acid-induced writhing in mice and acetic acid-induced oral ulcer in golden hamsters. Re-sults:The tablets could obviously alleviate the auricular edema(P<0. 01)and reduce the writhing times in mice(P<0. 05),and nar-row the oral ulcer(P<0. 01 or P<0. 05)and inhibit the inflammation reaction in golden hamsters. Conclusion:Zhenbing Koukuining tablets have anti-inflammatory,analgesia and ulcer healing promotion effects.
5.Determination of Copper Ion in Rabbit with Implantation of Copper Intrauterine Device
Xiaoling XU ; Kaiyong HE ; Wangping PAN ; Xiaojun LYU ; Yuanhua HU
Herald of Medicine 2017;36(6):614-616
Objective To develop a method for determination of serumal copper ion in rabbit with implantation of copper intrauterine device.Methods At different time points after implantation,the serumal copper ion concentrations were determined by microwave digestion-inductively coupled plasma mass spectrometry(ICP-MS) using scandium(Sc) and indium(In) as internal standards to compensate sample matrix effects,and the pharmacokinetics parameters were calculated in order to reflect copper ion release and metabolic rule.Results The serumal copper ion concentrations were kept at a low and stable level.The recoveries were in the range of 98.7%-113.3%,with the relative standard deviations of less than 5.0%.Conclusion The analytical method is simple,fast,and can be used for the determination of serumal copper ion in rabbit.
6.Investigation on the depressor substance tests method of coenzyme complex for injection
ZHANG Ju ; LÜ ; Xiaojun ; ZHOU Daqing ; SHEN Jiate ; HE Kaiyong
Drug Standards of China 2024;25(1):072-075
Objective: To observe the acute hypotensive effect of compound coenzyme for injection on cats,and to establish a method for examination of depressor substance.
Methods: Ten batches of compound coenzyme for injection and histamine depressor substance were compared by cat blood pressure method to determine the limit value of depressor substance test method. According to the limit value, 22 batches of samples were tested for depressor substance.
Results: The limit of compound coenzyme for injection was 3 IU·kg-1 (calculated by coenzyme A). Two batches of 22 batches of compound coenzyme for injection did not meet the requirements.
Conclusion: The method of compound coenzyme for injection is feasible according to the proposed limit value. It is suggested that the quality standard of compound coenzyme for injection should be added with the examination of depressor substance.
7.Prevention against and treatment of doxorubicin-induced acute cardiotoxicity by dexrazoxane and schisandrin B.
Kaiyong HU ; Yong YANG ; Lihua HE ; Duowei WANG ; Zhirong JIA ; Shuran LI ; Wei TIAN ; Jie MAO ; Xianjing LI ; Wei ZHANG
Acta Pharmaceutica Sinica 2014;49(7):1007-12
In this study, it is to compare the effectiveness of prevention against and treatment of doxorubicin (DOX) induced cardiotoxicity by dexrazoxane and schisandrin B (Sch B) in rats. Sprague-Dawley (SD) rats were randomly divided into the following 6 groups: normal saline group, DOX group, DOX+DEX group, DOX+Sch B (80 mg x kg(-1)) group, DOX+Sch B (40 mg x kg(-1)) group and DOX+Sch B (20 mg x kg(-1)) group. The results showed that Sch B could combat the increase of myocardial enzymes in peripheral blood, decrease of the enzyme activity of myocardial tissue antioxidant enzymes and disorders of systolic and diastolic function of heart in rats intravenously injected with doxorubicin (15 mg x kg(-1)). Sch B was better than DEX in protecting rat against DOX-induced the symptoms. Sch B could protect rat against DOX-induced acute cardiomyopathy and has clinical potential applications.
8.Establishment and Validation of Caco-2 Cell in Vitro Absorption Model
Xiaojun LYU ; Yidan CAO ; Kaiyong HE
Herald of Medicine 2018;37(11):1311-1315
Objective To establish and validate the Caco-2 cell in vitro absorption model,so as to play a foundation for next study of drug absorption and transport. Methods Caco-2 cells were cultured on the polycarbonate membrane inserts fixed in the 24-well transwell transport chamber with three types cell density of low,medium and high concentration (5×104,1×105,2× 105·mL-1) respectively.After being cultured for 3,6,9,12,15,18,21 d,the integrity of monolayer were assessed and compared by the cell morphology,growth characters and transepithelial electrical resistance (TEER),aiming to determine the inoculum density and culture time.Then the permeability and polarity were validated by the apical-to-basolateral amount of Lucifer Yellow across cell monolayer,the alkaline phosphatase activity in the apical side (AP),the basolateral side (BL) and intracellular activity. Results The cells of low,medium and high concentration group had fusion into a integrate cell monolayer and the maximum absorbance after being cultured for 15,12,9 d respectively.However,conglobated and dead cells were observed at the later growth stage in the medium and high concentration group and the TEER of cell monolayer were smaller than the low concentration group,which could reach 300 Ω·cm2after cultured 15 d and keep a relatively stable value, then cells were cultured with 5×104·mL-1cell density for 21 d.The Lucifer Yellow apparent permeability coefficient (Papp) was 3.57×10-7 cm·s-1which was lower than 5. 0×10-7cm·s-1according to provision. And the intracellular alkaline phosphates’ activity increased,AP/BL increased by 5 times in day 21. Conclusion The integrity,permeability and polarity of the established Caco-2 cell model in our laboratory was validated,and it can be used as an in vitro model similar with small intestinal epithelium for absorption and transport studies.
9.Immunotoxicity of absorbable silk fibroin biofilm on rats
Xiaoling XU ; Wangping PAN ; Xiaojun LÜ ; Ju ZHANG ; Yuanhua HU ; Kaiyong HE
Chinese Journal of Tissue Engineering Research 2019;23(14):2190-2195
BACKGROUND: Silk fibroin, the main component of silk fibroin biofilm, is a natural protein, but it is still a heterologous protein to the body. Its immunogenicity/toxicity is an important factor in determining the development prospects. OBJECTIVE: To evaluate the toxicity of absorbable silk fibroin biofilm and its degradation products on the rat immune system by muscle implantation experiments in rats. METHODS: Ten Wistar rats from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd. were implanted with a long strip of 1 mm× 10 mm in the right gluteal muscle to observe the implant absorption and determine the implantation cycle. Seventy-two Wistar rats were assigned into control and experimental groups (n=36/group, 18 in either sexes) . A long strip of 1 mm×10 mm was implanted into the rat right gluteal muscle in the experimental group, and the control group received no implantation. Some of the rats were taken for histological examination and calculate the organ/weight ratio, at 26 weeks postoperatively. The spleen lymphocyte proliferation ability, NK cell activity, cell classification of T lymphocytes, and levels of interleukin 2 and tumor necrosis factor α were detected. Another part of the animals was taken for macrophage phagocytosis of erythrocytes cell capacity and antibody producing cell count. RESULTS AND CONCLUSION: (1) Silk fibroin biofilm was completely absorbed after implanted into the rat muscle for 26 weeks. (2) In female or male Wistar rats, the immune organs in the experimental group showed no significant changes in the appearance, weight and histological examination. There were no significant differences in the hematological indexes (hemoglobin, red blood cell count, hematocrit, blood platelet count and white blood cell count and classification) , spleen lymphocyte proliferation, NK cell activity, the ratio of T lymphocytes and their subpopulations, and the levels of interleukin 2 and tumor necrosis factor α had no significant differences between two groups (P> 0.05) . (3) In female or male Wistar rats, the macrophage phagocytosis of chicken erythrocytes cell capacity and antibody producing cell count showed no significant differences between two groups (P> 0.05) . (4) These results indicate that silk fibroin biofilm causes no immunosuppression or immunostimulation on immune organs, immune cells and immune molecules (cytokines) of rats.
10.Genotoxicity of Sanqi Liver-protecting Capsules
Yang WANG ; Kaiyong HE ; Jiate SHEN ; Yan WANG ; Xiaojun LV
China Pharmacist 2017;20(10):1749-1752
Objective:To study the acute toxicity and genotoxicity of Sanqi liver-protecting capsules to evaluate the toxicological safety. Methods:The mouse acute oral toxicity test, Ames test, micronucleus test of mouse bone marrow and mouse sperm shape ab-normality test were carried out for Sanqi liver-protecting capsules. Results:The mouse acute oral maximum tolerance dose ( MTD) of Sanqi liver-protecting capsules was above 20 g·kg-1 in the mouse acute oral toxicity test, which showed a non-toxic substance. The results of Ames test, micronucleus test of mouse bone marrow and mouse sperm shape abnormality test were negative in all the groups. Conclusion:Under the above experimental conditions,the genotoxicity of Sanqi liver-protecting capsules is not found out, therefore, the capsules are classified as a non-toxic drug.