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1.
The aim of this study was to evaluate the ability of two non-toxic skin penetration enhancers, N-methylpyrrolidone (NMP) and a positively charged phospholipid mixture (PS), to increase in vitro corneal permeation of timolol maleate (TM) and acyclovir (AC) in comparison with two corneal absorption promoters, polyethylene glycol octadecyl ether (Brij 78) and sodium taurocholate (TA). In vitro experiments were performed on corneas from albino rabbits which were mounted in a perfusion apparatus. The concentrations of the enhancers being tested were: Brij 78 1%, PS 1%, TA 1%, NMP 5%, NMP 10%. The safety of the enhancers being tested was assessed in vitro by determining their effects on corneal hydration and in vivo by means of a modified Draize test. Calculating the amount of drug permeated at different time points (90 and 180 min) we observed that TA, PS and NMP 5% significantly increased the cumulative amount of AC permeated after 90 min but only PS was effective after 180 min. TA, Brij 78 and PS were able to increase significantly the amount of TM permeated after 90 min but after 180 min only Brij 78 retained its effect. TA, Brij 78 and NMP 10% significantly increased the percent hydration levels (% HL) compared to the control while PS and NMP 5% did not affect % HL. The results of in vivo ocular tolerability studies showed that the enhancers which caused an in vitro increase of % HL produced in vivo conjunctival and/or corneal damages. The results of this study suggest that PS could be regarded as a potential corneal enhancer to increase the intraocular bioavailability of AC and TM.  相似文献   

2.
The effect of taurine (TA) on acute paraquat (PQ) intoxication was investigated in rats. Treatment with TA was begun 10 min after rats received a s. c. injection of PQ 40 mg/kg. Saline (0.9%) or 5% TA solution were infused i.v. for 5-6 min (short-interval infusion study). One hour after TA infusion, PQ concentration in the blood was increased and that in the urine was lowered, as compared with those in the saline-infused group. Significant increases of the PQ concentration was observed in kidney at 3 hours after TA administration. Excreted urine volume was significantly higher in the TA group during the time-period of 0-1 and 0-5 hours after the 5% TA administration compared with that of the saline group. However, there were no significant differences in total urinary PQ excretion between the two groups. Saline or 2.5% and 5% TA was infused continuously during the time-period of 0-1, 0-3 or 0-5 hours (long-interval infusion study). A marked increase in PQ concentration in blood and a reduction of PQ concentration in kidney were noticed during the time-period of 1-5 hours after the 5%TA infusion. Urinary excretion was remarkably accelerated by 5% TA infusion and the total urine volume increased to 20 times during the time-period 0-1 hour and 1.7 times during the time-period of 3-5 hours as compared with the saline control. In addition, urinary volume during the time-period of 0-5 hours almost reached that of 5% TA volume which infused to animals. The mortality rate of the groups that received either single or double short-time infusion of 5% TA was 100%. Thus, these results suggest that a long continuous infusion of 5% TA increased urine output and inhibits of PQ accumulation in renal tissue despite a rise in blood PQ concentration.  相似文献   

3.
OBJECTIVE To investigate the effect of Nigella sativa L.as gastric protective on indomethacin-induced rats.METHODS the design of this research is randomized post test control group design.The rats were randomly divided into 5 groups which 5 rats in each.Rats were fasted for 8h before treatment.The first group was a control group(only gave aquadest as vehicle orally).The second group was subjected to induced with indomethacin 30mg·kg-1.The rest groups were subjected to induced by indomethacin and methanolic extract of Nigella sativa L.200,300 and 400mg·kg-1 every 8h for 24 h,respectively,for third,fourth and fifth group.Rats were sacrificed after anesthetized with ketamine and gastric were washed before observed.Macroscopic observation based on a score of lesion and microscopic observation on gastric based by histological HE staining.Whole data were analysis of an ANOVA statistical program.RESULTS The administration of Nigella sativa L.significantly decreased gastric ulcer macroscopically starting at dose 100,200 and 300mg·kg-1(P<0.05).Microscopic observation showed significant decreasing at dose 200 and 300mg·kg-1(P<0.05).Interestingly,there was no significant different between control and dose 300mg·kg-1.Negative correlation between lesion and doses were-0.919,-0.953 for macroscopic and microscopic lesion respectively.It means there was strong correlation between dose and lesion,higher dose lesser lesion.The mechanism of gastric protective of NigellasativaL.may caused by the bioactive compound such as thymoquinone which known as antiinflammation and antioxidant.CONCLUSION Methanolic extract of Nigella sativa L.decreased peptic ulcer both macroscopic and microscopic conditions on indomethacin-induced rats.  相似文献   

4.
目的比较国产和进口肺表面活性物质(Pulmonary surfactant,PS)治疗早产儿呼吸窘迫综合征(Respirory distress syndrome,RDS)的临床疗效及安全性。方法将2009年5月-2010年10月出生的RPD早产儿107例分为3组。A组(42例)患儿应用国产PS和机械通气治疗,B组(37例)患儿应用进口PS和机械通气治疗,C组(28例)患儿单纯应用机械通气治疗。结果①应用国产或进口PS均可迅速改善RDS患儿临床症状(P<0.05)。②三组患儿血气值比较差异无统计学意义(P>0.05)。③用药后1~24 h,A、B组机械通气参数PIP值明显低于C组(P<0.05)。④用药后2~6 h,A组机械通气参数FiO2明显低于C组。⑤应用PS后2~6 h,A、B组胸片显示,肺部病变明显好转。⑥三组机械通气时间、住院时间、并发症和结局等比较,差异无统计学意义(P>0.05)。⑦A、B组重复用药情况差异无统计学意义(P>0.05)。结论国产与进口肺表面活性物质治疗早产儿RDS同样安全有效,操作时应用进口PS更加方便快捷。  相似文献   

5.
The mutagenic (MUT) and chromosome-damaging (CHR) activities of 22 potential antimalarial drugs (5-nitroisoquinoline derivatives) were evaluated by the Salmonella test and the cytokinesis-blocked micronucleus assay (CBMN). The Salmonella mutagenicity test was performed with and without metabolic activation (S9 mix) in S. typhimurium strains TA100 and YG1042 (an overproducing nitroreductase and O-acetyltransferase TA100 strain). The CBMN was carried out on human lymphocytes without metabolic activation. Four concentrations were tested: 1, 10, 100 and 1000 ng/ml. MUT was expressed as minimal mutagenic concentrations (MMC, microM) and CHR was expressed as minimal chromosome-damaging concentrations (MCDC, nM) to compare both activities. All the 5-nitroisoquinoline compounds were mutagenic in TA100. MMC ranged from 0.1 to 52.9 microM in TA100. A statistically significant decrease in MMC was observed in YG1042 (8 x 10(-3) to 3.5 microM), implicating reduction of the nitro group. Modulation of MUT by S9 mix was not significant in TA100 and YG1042. CHR was detected in 13 products for at least one concentration. Among the chromosome-damaging compounds, the MCDC ranged from 2.9 x 10(-3) to 3.6 nM. No relationship was found between MUT and CHR, suggesting two distinct pathways of DNA damage.  相似文献   

6.
目的探讨中药制剂赤苷脉通注射液的致突变性。方法采用鼠伤寒沙门氏组氨酸营养缺陷型菌株回复突变实验(Ames实验)、中国仓鼠肺成纤维细胞(CHL)染色体畸变实验和小鼠骨髓微核实验来检测赤苷脉通注射液的致突变作用。结果 Ames实验中,赤苷脉通注射液在312.5~5 000μg.皿-1剂量范围内,无论加或不加S9,鼠伤寒沙门氏菌组氨酸缺陷型TA97,TA98,TA100,TA102和TA1535 5株菌的回复突变菌落数均未出现剂量依赖性的增加;染色体畸变实验中,非活化条件或代谢活化条件下,药物质量浓度为1 200,600和300μg.mL-1时,细胞的染色体畸变率均未出现剂量依赖性增加;微核实验中,在1 150,575和287.5mg.kg-1剂量组中均未见骨髓中含微核的嗜多染红细胞数增加。结论在该实验室条件下,Ames实验、CHL细胞染色体畸变实验和小鼠骨髓微核实验结果均为阴性,即中药制剂赤苷脉通注射液无潜在的遗传毒性。  相似文献   

7.
目的 研究心肺运动试验(CPET)相关指标在心肌缺血患者诊断中的价值。方法 52例胸痛患者患者分别行CPET、99Tcm-MIBI心肌灌注显像检查及心脏彩色多普勒超声检查。根据心肌灌注显像检查结果分为心肌缺血组(30例)及非缺血组(22例)。比较2组患者的CPET相关指标如每千克体重峰摄氧量( VO2 peak/kg)、峰摄氧最(VO2 peak)、峰氧脉搏(VO2 peak/HR)、最大呼吸频率、氧斜率、呼吸储备、最大心率、心率储备和无氧阈、无氧阈时氧气通气当最、无氧阈时二氧化碳通气当量、无氧阈时氧脉搏以及心脏彩色多普勒超声检查二尖瓣口血流舒张早期峰值速度(E)与舒张晚期峰值速度(A)的比值(E/A值)和左心室射血分数(LVEF)。结果 2组患者之间年龄、性别、BMI、E/A值及EF值差异均无统计学意义。心肌缺血组与非缺血组比较、VO2 peak/kg[(27±6) ml/(kg·min)比(33±7)ml/(kg·min),P<0.01],vO2 peak[(1.5±0.5) L/min比(2.1±0.5) L/min,P<0.01]、VO2 peak/HR[(10.7±2.6) ml/次比(14.1±3.0)ml/次,P<0.01]、最大心率[(143±15)次/min比(154±17)次/min,P<0.05]和无氧阈[(16.4±3.0)ml/(kg·min)比(20.6±5.0)ml/(kg·min),P<0.01]、无氧阈时氧脉搏[(9.0±1.8)ml/次比(11.3±2.3) ml/次,P<0.01]均明显为低,差异具有统计学意义。结论 采用心肺运动试验检测心肌缺血患者的VO2 peak/kg、VO2 peak、VO2 peak/HR、无氧阚和无氧阈时氧脉搏等指标对早期发现心肌缺血具有一定价值。  相似文献   

8.
目的 探讨油松花粉的遗传毒性,为其应用提供安全性毒理学评价依据.方法 用鼠伤寒沙门细菌营养缺陷型突变株TA97(a)、TA 98、TA 100和TA 102,采用平皿掺入法进行Ames实验,将实验分为加和不加代谢激活系统S9 2组平行实验.受实物设5个剂量组(0.008、0.040、0.200、1.000、5.000 mg/皿).应用小鼠骨髓嗜多染红细胞微核实验,检测小鼠骨髓嗜多染红细胞微核率;利用小鼠精子畸形实验,观察不同浓度的油松花粉致小鼠精子畸形的数目.结果 在Ames实验中,油松花粉各剂量组引起的回变菌落数未超过对照组自发回变菌落数的1倍以上;小鼠骨髓嗜多染红细胞微核实验显示,油松花粉3个剂量组的微核发生率均在正常范围内,与阴性对照组比较差异无显著性(P>0.05),与阳性对照组比较差异显著(P<0.05);小鼠精子畸形实验显示,油松花粉3个剂量组的精子畸形率均在正常范围内,与阴性对照组比较差异无显著性(P>0.05),与阳性对照组比较差异显著(P<0.05).结论 油松花粉对所实菌株、小鼠体细胞及生殖细胞无诱变性.  相似文献   

9.
The safety of intravitreally injected triamcinolone acetonide suspension (TA) was evaluated in rabbits. Each animal received 0.1 ml (1) balanced salt solution (BSS) vehicle, (2) formulation vehicle, (3) 4% TA (4-mg dose), (4) 16% TrAc (16-mg dose) or (5) 25% TA (25-mg dose) as a single intravitreal injection into the right eye. The left eyes served as untreated controls. All animals were observed for 1 month following treatment. In-life evaluations included clinical signs, body weights, slit-lamp biomicroscopic and indirect ophthalmoscopic examinations, intraocular pressure and corneal thickness measurements, and electroretinograms (ERGs). Ocular tissues were harvested following a 1-month post-treatment observation period, fixed, processed, and evaluated by light microscopy. No significant or treatment-related clinical signs were observed for any animals during the study. The opaque white test article was clearly visible in the eye for all TrAc-treated groups, and remained so throughout the study. No statistically significant differences in mean body weights were present between the control and treatment groups, though changes in body weight varied. Corneal thickness was slightly reduced for some treated groups. Intraocular pressures were not statistically significantly different from controls for any treatment group. No significant changes in ERG were evident between treatment groups or from baseline readings. Microscopically, basophilic material (presumed to be drug) was seen in the vitreous of all or most treated eyes, with accumulations in the vitreous or in clumps adjacent to the retinal surface. No pathological changes were observed in the retina or other ocular structures. Triamcinolone acetonide suspension was safe and well tolerated following intravitreal injection in New Zealand white rabbits.  相似文献   

10.
Several novel dopamine (DA) agonists (SKF 38393, 3-PPP, TL-99) have been reported to induce rotational behavior (RB) in rats unilaterally denervated of the nigro-striatal pathway by 6-hydroxydopamine. Other reports have indicated no RB, however, and these drugs do not cause other behavioral manifestations of postsynaptic DA agonism. In the present experiments, two groups of 6-hydroxydopamine-denervated rats were distinguished by their relative responsiveness to apomorphine-induced RB. A highly sensitive group showed maximal RB in response to doses as low as 0.03 mg/kg, while a less sensitive group exhibited comparable RB only in response to 15- to 20-fold higher doses. The high sensitivity group exhibited RB in response to SKF 38393, 3-PPP and pergolide, but the low sensitivity group did not show appreciable RB after these drugs, even at doses 50 to 100-fold higher. Haloperidol markedly attenuated apomorphine-induced RB in the low sensitivity subgroup, but only reduced by approximately one-half the number of turns induced by apomorphine or SKF 38393 in the high sensitivity group. The atypical antipsychotics, clozapine and RMI 81582, and the muscle relaxant, methocarbamol, reduced RB in all groups, but only at doses that caused performance impairment in a rotorod test. These results appear to reflect qualitative differences in responsiveness to different DA agonists. Behavioral preselection of 6-hydroxydopamine-denervated animals is necessary to achieve consistent pharmacological results with the 6-hydroxydopamine RB model.  相似文献   

11.
目的探讨E838对γ射线照射小鼠骨髓细胞染色体损伤的防护作用。方法将615小鼠,随机分为对照组、辐射对照组、E838组、炔雌三醇(EE3)组。E838组和EE3组分别腹腔注射E838和EE3,另两组给予等体积茶油,第3次给药24 h后进行剂量为1.5 Gy的137Csγ射线全身照射,观察其骨髓细胞染色体畸变率。结果 E838组、EE3组骨髓细胞染色体畸变与辐射对照组比较差异有统计学意义(P<0.01),E838组畸变细胞与EE3组比较差异有统计学意义(P<0.05)。结论 E838可降低辐射诱发的骨髓细胞染色畸变细胞数,对骨髓细胞染色体具有一定的辐射防护作用。  相似文献   

12.
Methyl tert-butyl ether (MTBE) is a synthetic compound that is used as a technological solution to problems created by air pollution from vehicle emissions. An important source of MTBE in the environment is leakage from underground storage tanks at gasoline stations or accidents during gasoline transport. The aim of this study was to evaluate the risk of MTBE leakage for the environment using the Microtox (Vibrio fischeri) toxicity test, Lactuca sativa seed germination test, and Ames bacterial mutagenicity test with Salmonella typhimurium his(-) strains TA98, TA100, YG1041, and YG1042, using both standard plate and preincubation protocols. The result of Microtox expressed as EC(50) was 33 mg (MTBE)/L. The effect of all tested MTBE concentration (0.05, 0.50, and 1.00% v/v) on Lactuca sativa roots elongation was negative and proved its toxicity. The highest tested concentration of MTBE that could be tested in Ames test was 3 mg (MTBE)/plate, because of cytotoxicity. No mutagenic response was observed at this or lower concentrations in any of the four strains used.  相似文献   

13.
建立一种快速灵敏的大鼠体内延胡索乙素 (tetrahydropalmatine,TET) 血药浓度的HPLC-FLD检测方法;并研究白芷香豆素 (coumarin,Cou) 和挥发油 (volatile oil,VO) 两种提取物与延胡索总碱 (TA) 配伍对TET在大鼠体内药代动力学的影响。血浆经正己烷-异丙醇 (95∶5) 沉淀蛋白,HPLC-FLD检测,结果血浆中TET的线性范围为2.096~167.68 μg·L−1;定量限2.096 μg·L−1;方法准确度94.0%~100.0%,提取回收率72.0%~81.5%,日内日间精密度均小于7.0%;大鼠灌胃TA、TA-VO、TA-Cou、TA-VO-Cou后,TET在大鼠体内药代动力学行为均为二室开放模型,与TA组相比,配伍VO或(和) Cou后TET的AUC0−t、AUC0−∞、MRT0−t、MRT0−∞等药代动力学参数有显著差异。建立的大鼠血浆中TET的测定方法具有灵敏、准确、专属性强等特点;Cou、VO与TA配伍,能显著延长TET在大鼠体内滞留时间,减缓体内的消除,提高其生物利用度。  相似文献   

14.
肌等压区排牙法全口义齿对面部肌肌电的影响   总被引:1,自引:0,他引:1  
目的比较肌等压区排牙法全口义齿(ND)和传统全口义齿(CD)修复后无牙颌者面部肌肌电活动的变化差异.方法选择10例牙槽嵴严重萎缩低平的无牙颌患者.记录其分别戴用ND和CD1个月、3个月时颞肌前束(TA)、嚼肌(MM)、二腹肌前腹(DA)和口轮匝肌(UOO、LOO)在下颌姿势位、ICP紧咬、咀嚼运动和吞咽运动时的肌电活动。根据记录阶段分为ND1个月组、ND3个月组、CD1个月组和CD3个月组.采用配对t检验分析ND1个月-CD1个月组、ND3个月-CD3个月组之间相应指标的差异.结果①下颌姿势位:受试肌肌电活动各组间无显著差异;②ICP紧咬双侧TA肌电活动ND3个月组>CD3个月组(左侧P<0.01、右侧P<0.05);③咀嚼运动:右侧咀嚼花生米时,右侧颞肌前束、右侧嚼肌肌电幅值ND3个月组大于CD3个月组(P<0.05),左侧咀嚼花生米时,右侧颞肌前束肌电幅值ND1个月组大于CD1个月组(P<0.05),右侧嚼肌肌电幅值ND3个月组大于CD3个月组(P<0.05)④吞咽运动:右侧TA、下唇口轮匝肌肌电活动CD3个月组相似文献   

15.
Male rats were exposed to 17-ethinylestradiol (EE2) in their drinking water either at concentrations of 1–1000 ng/mL (1 ppb to 1 ppm) for 3 weeks immediately after weaning from post-natal day 22 (PND 22) to PND 43 or at a concentration of 10 ng/mL from PND 5 onwards. Although given temporarily between PND 22 and PND 43, the 0.1 and 1 ppm doses of EE2 were found to significantly affect the ponderal growth of the animals. No male was found to be sterile neither in both exposed groups nor in control groups. Nevertheless, the males exposed to 10 ng/mL EE2 in drinking water from PND 5 onwards conceived a significantly higher proportion (25%) of small litters (one to five pups) than control males (0–3%). When exposed to 1 μg/mL EE2 but only from PND 22 to PND 43, the males produced an intermediate proportion (15%) of small litters in their progeny but this might be consecutive to the observed retardation in weight gain.  相似文献   

16.
Although potassium sorbate (PS), ascorbic acid and ferric or ferrous salts (Fe-salts) are used widely in combination as food additives, the strong reactivity of PS and oxidative potency of ascorbic acid in the presence of Fe-salts might form toxic compounds in food during its deposit and distribution. In the present paper, the reaction mixture of PS, ascorbic acid and Fe-salts was evaluated for mutagenicity and DNA-damaging activity by means of the Ames test and rec-assay. Effective lethality was observed in the rec-assay. No mutagenicity was induced in either Salmonella typhimurium strains TA98 (with or without S-9 mix) or TA100 (with S-9 mix). In contrast, a dose-dependent mutagenic effect was obtained when applied to strain TA100 without S-9 mix. The mutagenic activity became stronger increasing with the reaction period. Furthermore, the reaction products obtained in a nitrogen atmosphere did not show any mutagenic and DNA-damaging activity. PS, ascorbic acid and Fe-salts were inactive when they were used separately. Omission of one component from the mixture of PS, ascorbic acid and Fe-salt turned the reaction system inactive. These results demonstrate that ascorbic acid and Fe-salt oxidized PS and the oxidative products caused mutagenicity and DNA-damaging activity.  相似文献   

17.
糖尿病视网膜病变与尿微量白蛋白的关系   总被引:2,自引:0,他引:2  
目的 研究糖尿病视网膜病变(DR)与尿微量白蛋白及相关因素的关系。方法 选择131例糖尿病(DM)患者(A组)及40例正常对照者(B组),A组又分为Aa组(眼底正常)、Ab1组(非增殖期DR)、Ab2组(增殖前期DR)、Ab3组(增殖期DR),检测各组的尿微量白蛋白/尿肌酐指数(IMA/UCR)。结果 IMA/UCR平均值:Aa组〉B组;Ab1组〉Aa组;Ab2组〉Ab1组;Ab3组〉Ab2组。差异均有显著性(P〈0.05)。多元线性回归与相关分析显示,糖尿病视网膜病变程度与IMA/UCR、糖化血红蛋白以及糖尿病病程具有直接的相关性。结论 DR与尿微量白蛋白紧密相关,尿微量白蛋白是能反映DR程度的指标之一。  相似文献   

18.
The effects of prenatal rubratoxin-B (RB) exposure on 8 behavioral parameters in JCL:ICR mice were assessed. Pregnant mice were injected intraperitoneally with 0.1 or 0.2 mg/kg/day of RB dissolved in propylene glycol water solution on days 7-9 (Group A) or 10-12 (Group B) of gestation. Controls received the vehicle similarly on days 7-12 of gestation. Before weaning, the offspring of both sexes were examined to test their the surface righting reflex (5 days of age), cliff avoidance response (6 days), negative geotaxis response (7 days), and swimming development (8, 10, and 12 days). After weaning, male animals were examined using the rotarod test (6 weeks of age), the open-field test (7 weeks), the shuttle-box-avoidance-learning test (9 weeks), and the water E-maze test (10 weeks). The preweanling offspring in the 0.2 mg/kg-B group showed significantly lower success rates and longer response times than controls in the cliff-avoidance response. In swimming development, the offspring in the 0.2 mg/kg B group had significantly lower scores than controls for swimming angle at 10 and 12 days of age. The avoidance learning of the mice in all RB-exposed A and B groups was significantly poorer than that of controls. These results indicate that prenatal exposure to RB produced a delay of early response development and impaired learning ability in the offspring of mice exposed to RB during middle pregnancy.  相似文献   

19.
目的 分析运动负荷试验对胸部手术患者心肺储备功能分析的意义。方法 对 5 6例胸部手术患者手术前后进行阶段踏车运动负荷试验 ,分析其心肺功能的变化。结果 与术前相比术后由于运动氧分压低下者增多 ,在单侧肺切除组氧分压全部低下 ,被认为与肺组织切除量有关。在运动终点上 ,由于呼吸症状而终止运动的例数增多 ,其中氧分压低下者亦增多。与其他原因终止运动的患者相比 ,术前第 1秒未用力呼气量 (FEV 1)低下 ,术后肺一氧化碳弥散功能 (DL co)低下提示术前由于通气功能障碍所致 ,而术后由于换气功能障碍所致。作为需氧运动能力的厌氧代谢阈值与术式无关 ,而主动最大氧气摄入量与肺切除量有关。结论 在运动负荷试验中因呼吸系统症状而停止运动的患者增多。主要是由于肺换气功能障碍导致的低氧血症所致 ,评价胸部手术患者心肺储备功能不仅要测定厌氧代谢阈值 ,主动最大氧气摄入量也非常重要。呼出气体及血气分析也有一定价值  相似文献   

20.
This report dealt with the effects of dimercaprol (BAL) and thiotic acid (TA), antidotes against arsenical, on the distribution and the excretion of 74As in several organs of the rat. Each organ was removed and served for quantitative analysis of 74As five days after subcutaneous injection of Na374AsO3 5 microCi/100 g. Administration of BAL or TA was performed intraperitoneally with a single administration or five consecutive administrations for five days before animals were sacrificed. 74As content in each organ of the rat decreased to a greater extent in the five consecutive administration group of BAL or TA than in the non-treated or single administration groups. Moreover, the excretion of 74As in a digestive tract increased more remarkably in the five consecutive administration group than in the non-treated or single administration groups. There were no differences in the excretion or the content of 74As in each organ between the single administration group and the non-treated group.  相似文献   

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