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1.
目的:建立HPLC—MS/MS法测定人体血浆中甲磺酸多沙唑嗪浓度的方法。方法:以KromasilC_18(4.6mm×250mm,5μm)为色谱柱,流动相为乙腈:20mM乙酸胺(含0.3%甲酸)水溶液(55:45),流速为0.30mL·min-1,柱温为25℃,进样器温度为4℃,进样量为10μL,内标物为吡格列酮。结果:甲磺酸多沙唑嗪在血浆浓度0.3~100ng/mL范围内线性良好,定量下限为0.3ng/mL,日内RSD≤6.0%,日间RSD≤6.3%,回收率为96.58%~100.16%。结论:该法灵敏,检测结果准确,适用于甲磺酸多沙唑嗪片的人体生物等效性研究。  相似文献   
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The current study was carried out with an attempt to separate similarly structured title drugs by liquid chromatography. Spectrophotometric techniques were generally insufficient under these conditions because of the spectral overlapping of drugs with similar functional groups. The pharmaceutical drugs prazosin, terazosin, and doxazosin contain the same parent quinazoline nucleus, thus making it especially difficult to separate the former two drugs because of their very similar structures. A simple and sensitive method for the routine determination of these drugs in pharmaceutical formulations was attempted. We found that the mobile phase consisting of A: ACN–diethylamine (0.05 ml), B: methanol, and C: 10 mM Ammonium acetate separated these drugs effectively. Separations were carried out on a new Kromasil C18 column (250 × 4.6 mm, 5.0 μm) at 254 nm wavelength. The calibration curve was found to be linear in the range of 2–500 μg/ml. The stated method was then validated in terms of specificity, linearity, precision, and accuracy. Additionally, the proposed method reduced the duration of the analysis.  相似文献   
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OBJECTIVES:To evaluate predictors of the response to doxazosin, a selective alpha-adrenoceptor antagonist, when used for the treatment of lower urinary tract symptoms in men with Parkinson''s disease.METHODS:In a prospective study, 33 consecutive men (mean age 59.2±7.0 years) with Parkinson''s disease and lower urinary tract symptoms were evaluated. Neurological dysfunction was assessed with the Unified Parkinson''s Disease Rating Scale. Urological assessment was performed at baseline and after 12 weeks of treatment with 4 mg/day of extended-release doxazosin, including symptom evaluation with the International Continence Society male short-form questionnaire, an assessment of the impact of lower urinary tract symptoms on quality of life and urodynamics. Clinical and urodynamic predictors of response were specifically evaluated.RESULTS:Compared with the score at baseline, the total International Continence Society male short-form score was reduced after doxazosin administration, from 17.4±7.5 to 11.1±6.9 (p<0.001). The impact of lower urinary tract symptoms on quality of life was also significantly reduced, from 1.8±1.1 to 1.0±1.0 (p<0.001) and the maximum urinary flow varied from 9.3±4.4 to 11.2±4.6 ml/s (p = 0.025). The severity of neurological impairment was the only predictor of the clinical response. Additionally, patients with a Unified Parkinson''s Disease Rating Scale score lower than 70 had a significantly higher chance of clinical improvement with doxazosin treatment than those with higher Unified Parkinson''s Disease Rating Scale scores did (RR = 3.10, 95% CI = [1.15 to 5.37], p = 0.011).CONCLUSIONS:Doxazosin resulted in the improvement of lower urinary tract symptoms and the maximum flow rate and was well tolerated in men with Parkinson''s disease. The response to treatment is dependent on the severity of neurological disability.  相似文献   
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Summary The effect of doxazosin, an a,-adrenoceptor blocking drug, on blood pressure, sensitivity to insulin and serum lipids has been evaluated in 14 hypertensive, non-insulin dependent diabetic patients. The dose was titrated individually upwards from 1 mg until the diastolic blood pressure was below 90 mm Hg, side-effects precluded further dosage increase or the maximum daily dose of 16 mg was achieved.After 12 weeks of treatment (mean doxazosin dose 5.6 ± 5.1 mg daily), the supine and standing diastolic blood pressure of the patients had declined by about 7 mmHg, whereas their systolic blood pressure and heart rate were not significantly changed. The metabolic clearance rate of glucose increased from 2.35 to 3.37 ml - min–1 - kg–1 during treatment, suggesting improved sensitivity to insulin. Fasting plasma glucose was 11.9 mmol·1–1 before and 10.9 mmol·l–1 after doxazosin therapy (NS). Serum electrolytes and lipids did not change significantly but serum uric acid decreased from 305 to 281 mol · 1–1 Doxazosin may be a useful alternative for the treatment of hypertension in NIDDM patients.  相似文献   
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目的 将甲磺酸多沙唑嗪控释片与酚苄应用于在嗜铬细胞瘤患者的术前准备,比较两者对围术期血压的控制效果.方法 1978-2006年上交通大学医学院附属瑞金医院40例左侧肾上腺嗜铬细胞瘤患者,根据术前的药物准备情况分为3组:组1,手术前未使用a受体阻滞剂进行术前准备;组2,酚苄明20~40 mg/d,分2~3次口服,平均服用天数为(25.1±2.4)d;组3,甲磺酸多沙唑嗪控释片4~8 mg/d顿服,平均服用天数为(10.6±3.9)d.连续挠动脉内监测血压,记录5个时间点的收缩压.分别为手术麻醉诱导前、麻醉后、探查肿瘤时、肿瘤切除后和手术结束时.结果 麻醉前,3组间收缩压的差异有统计学意义(P<0.01).组2最低,组3次之,组1最高.麻醉后,3组收缩压都有下降,还是以组2最低,组1次之,组3最高,3组间差异有统计学意义(P<0.01).探查肿瘤时,三组收缩压均升高,依然是组2最低,组3次之,组1最高,3组间差异有统计学意义(P<0.001),但是组2与组3间差异无统计学意义(P>0.05).肿瘤切除后,3三组收缩压均下降,组l与组2的差异无统计学意义(P>0.05),但是与组3的差异均有统计学意义(P值均<0.01).手术结束时,3组收缩压的差异无统计学意义(P>0.05).组2、3的最高与最低血压差小于组1(P值均<0.01),组3显著小于组2(P<0.01).结论 在左肾上腺嗜铬细胞瘤手术中,术前服用甲磺酸多沙唑嗪控释片可更好地控制术中收缩压的波动,而酚苄明对术前收缩压的控制更佳.  相似文献   
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多沙唑嗪的多晶型研究   总被引:4,自引:0,他引:4  
多沙唑嗪是一种抗高血压药物,本文通过选用不同的溶剂对其进行多晶型的制备,并利用差热分析法、红外分光光度法、X-射线粉末衍射法等确证其至少存在三种晶型。此外,还利用差热分析法研究比较了它们的固体稳定性。  相似文献   
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非那雄胺与多沙唑嗪联用对鼠前列腺增生模型的影响   总被引:1,自引:0,他引:1  
目的:探讨非那雄胺与多沙唑嗪联用对鼠前列腺增生模型的影响。方法:将34只雄性W istar大鼠,随机分为模型组(28只)、假手术组(6只)。造模成功后将24只模型鼠随机分为非那雄胺与多沙唑嗪联用、非那雄胺、多沙唑嗪组、阴性对照组,继续予皮下注射丙酸睾酮4mg/d.kg造模,连续4周;假手术组继续予皮下注射等量橄榄油4周。各组实验鼠分别于注射4周后处死,取出前列腺,光镜下观察其形态学变化,计算各实验组前列腺指数(PI)。免疫组化检测bax、fas、bcl-2蛋白表达情况。结果:与阴性对照组相比,给药4周后非那雄胺与多沙唑嗪联用、非那雄胺组PI、bcl-2表达下降(P<0.05),bax、fas表达增加(P<0.05)。结论:两种药物联用显著地降低了鼠前列腺增生的进展,有望成为临床治疗前列腺增生的新方法。  相似文献   
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目的观察多沙唑嗪治疗轻、中度原发性高血压的疗效,探讨多沙唑嗪对血浆内皮素(ET)和降钙素基因相关肽(CGRP)的影响。方法采用随机、对照、双盲法,将轻、中度原发性高血压48例分为两组各24例,治疗组和对照组分别给予多沙唑嗪和特拉唑嗪,均为2mg,po,qd,共治疗8周。结果治疗组和对照组降血压有效率分别为835%,783%,差异无显著性(P>005)。治疗组总胆固醇亦明显下降(P<005)。两组治疗后ET浓度下降、CGRP水平升高。结论多沙唑嗪为一安全有效的降血压药物,在降血压的同时有降血脂作用;多沙唑嗪的降血压作用可能部分与其拮抗ET、升高CGRP的浓度有关。  相似文献   
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α1-Adrenoceptors mediate contraction of iris dilator smooth muscle and hence pupil dilatation. We compared the ability of i.v. bolus injections of alfuzosin, doxazosin, naftopidil, prazosin, tamsulosin and terazosin to antagonise phenylephrine-induced mydriasis relative to their potency for inhibiting phenylephrine-induced elevations of intraurethral pressure (IUP) in rabbits. Moreover, we compared the ability of these drugs to induce miosis in conscious rabbits in the absence of phenylephrine. All antagonists inhibited the effects of phenylephrine on pupil size and IUP, and the ratio of the respective ED50 values was close to unity in all cases. The doses required to induce statistically significant miosis in the absence of phenylephrine were 30- to 100-fold higher than those inhibiting phenylephrine-induced mydriasis for all antagonists, except for naftopidil. Moreover, the miotic effects of all α1-adrenoceptor antagonists were fully reversible within 8 h. We conclude that alfuzosin, doxazosin, naftopidil, prazosin, tamsulosin and terazosin inhibit phenylephrine-induced mydriasis in the same dose range as they inhibit elevations in IUP. Higher doses of all antagonists are required to induce miosis in the absence of an exogenous agonist, and such miosis is always reversible within hours.  相似文献   
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