Light and electron microscopic studies on rat arterial lesions induced by experimental arterial contraction

Summary Experimental contraction was produced in the rat mesenteric arteries and the arterial segments were studied morphologically. When the rat mesenteric artery was exposed in physiological saline solution at 37° C and 2–3 mg of methoxamine hydrochloride (10 mg/ml) was dripped onto it, intense contraction was observed for about 30 min but elevation in blood pressure was slight. During the contraction, numerous vacuoles were seen in the medial smooth muscle cells of the arterial segments, and these vacuoles were shown electron microscopically to have double unit membranes, indicating that they were formed by herniation of a part of the adjacent smooth muscle cell body. In the arteries 1–6 h after the end of the contraction, cellular, nuclear and vacuolar membranes and myofilaments of the medial muscle cells were partially lost. 12–24 h after the contraction the arteries exhibited necrosis and desquamation of endothelial cells and platelet adhesion. In the media, smooth muscle cells were completely deprived of cell membranes, myofilaments, nuclei, intracytoplasmic organelles other than mitochondria, and vacuolar membranes. The cytoplasm was filled with fine granular and granulo-vesicular material, and fibrin insudation was observed in these severely damaged cells. Arterial contraction may be an important factor in the induction of arterial lesions.     

Detection of radiolabelled bone marrow cells bearing surface ace immunoglobulins by combined autoradiography and immunoperoxidase

A method is described for the simultaneous detection of radiolabelled bone marrow cells bearing surface immunoglobulins by combined autoradiography and immunoperoxidase. Bone marrow cells from normal CBA mice prelabelled in vivo with ¹²⁵IUDR or exposed in vitro to [³H]thymidine were incubated with rabbit anti-mouse immunoglobulins under capping conditions, washed, cytocentrifuged and treated with methanol and hydrogen peroxide to destroy endogenous peroxidase. Cells were then covered with peroxidase-conjugated goat anti-rabbit immunoglobulins, washed, treated with diaminobenzidine a and hydrogen peroxide and finally covered with autoradiographic stripping film and exposed for different times. Peroxidase-positive cells were typically capped and those radiolabelled had autoradiographic silver grains overlying the nucleus.     

Outcomes and complications of naftopidil versus tamsulosin for elderly men with lower urinary tract symptoms secondary to benign prostatic hyperplasia: A systematic review and meta-analysis

We conducted a systematic review and meta-analysis to assess the outcomes and complications of naftopidil in treating elderly men with lower urinary tract symptoms secondary to benign prostatic hyperplasia and compared them with those administered with tamsulosin. A literature review was performed to identify the available randomised controlled trials concerning the comparison between naftopidil and tamsulosin for men with LUTS/BPH. We searched the following databases: the Cochrane Library Database, PubMed, Embase and Web of Science. Eleven publications involving 1,114 men (557 in the naf group and 557 in the tam group) were pooled in our analysis. We found no significant differences in the total IPSS, IPSS storage score, IPSS voiding score, quality of life index, peak urinary flow rate, average flow rate and post-void residual volumes. We assessed cardiovascular and sexual adverse events, acute urinary retention, surgical intervention, withdrawals due to any reason and withdrawals due to adverse events. The incidence of adverse events was similar among patients in naf and tam groups. In conclusion, naftopidil shared comparable efficacy and similar incidence of adverse events with tamsulosin and appears to be a promising agent for and alternative to tam. However, more prospective trials with high quality and long-term treatment duration are needed to verify this observation.     

基于熵权法评价干燥方法对经典名方华盖散基准样品质量属性的影响

目的 优选经典名方华盖散基准样品的干燥方法。方法 采用真空干燥、真空带式干燥、喷雾干燥、冷冻干燥方法制备华盖散基准样品,应用扫描电子显微镜、差式扫描量热分析、HPLC等方法测定基准样品的质量属性,以得粉率、玻璃化转变温度及成分含量转移率等为评价指标,运用熵权法对各指标赋予权重进行综合评价。结果 喷雾干燥基准样品粒子呈类球形、粒径最小,冷冻干燥基准样品不规则、蓬松、溶化性好。指标成分盐酸麻黄总碱、苦杏仁苷、橙皮苷、甘草苷、甘草酸转移率分别为85.66%～104.78%、90.81%～104.16%、91.42%～94.86%、83.98%～94.69%、87.85%～94.45%,指纹图谱相似度均大于0.9。结论 经综合评价得出冷冻干燥方法最佳,3批验证工艺重复性、可行性较好,为经典名方基准样品质量属性研究提供了理论依据和实践价值。     

基于网络药理学和16SrDNA测序的当归六黄汤合煎与单煎治疗阴虚甲亢作用的差异研究

目的 探讨当归六黄汤的抗阴虚甲亢作用,阐释传统汤剂合煎和单煎的差异。方法 运用网络药理学方法,筛选当归六黄汤的主要活性成分和治疗阴虚甲亢疾病的相关靶点,并对交集靶点进行蛋白质-蛋白质相互作用（protein-protein interaction,PPI）网络分析、基因本体（gene ontology,GO）功能和京都基因与基因组百科全书（Kyoto encyclopedia of genes and genomes,KEGG）通路富集分析,构建药材-成分-靶点-通路网络;进一步进行实验验证,构建阴虚甲亢大鼠模型,评价当归六黄汤合煎和单煎对阴虚甲亢大鼠体质量、粪便含水率及相关血清学指标的影响;利用16S rDNA测序技术,揭示合煎和单煎对大鼠肠道微生物群落多样性的影响。结果 筛选获得当归六黄汤方中102个活性成分,检索出与阴虚甲亢有关靶点116个。富集分析获得871条GO条目和158条KEGG相关条目（P<0.05）,其中生物过程（biological process,BP）675条、细胞组分（cellular component,CC）77条、分子功能（molecular fu...     

经典名方甘草泻心汤基准样品的量值传递研究

目的 建立经典名方甘草泻心汤（Gancao Xiexin Decoction,GXD）基准样品的HPLC图谱及指标性成分含量测定方法,研究GXD基准样品量值传递规律。方法 制备15批GXD基准样品,建立特征图谱并选用《中药色谱指纹图谱相似度评价》软件进行相似度评价,明确特征峰并对其进行归属。测定指标性成分甘草苷、甘草酸、黄芩苷、盐酸小檗碱、表小檗碱、黄连碱、巴马汀的含量,计算指标成分转移率,分析指标成分在饮片-基准样品中量值传递的规律。结果 15批GXD基准样品指纹图谱相似度均大于0.90,共指认22个共有峰,甘草5个、黄芩5个、甘草和黄芩共有3个、黄连6个、黄芩和黄连共有2个、干姜1个;各指标成分从药材-饮片平均转移率分别为98.69%、98.13%、96.94%、94.59%、91.76%、88.08%、94.16%;饮片-基准样品平均转移率为49.08%、42.24%、28.34%、26.72%、29.32%、33.62%、47.93%。结论 特征图谱与多指标成分含量测定方法相结合,对GXD药材-饮片-基准样品的量值传递过程进行分析研究,为经典名方GXD制剂开发提供参考。     

盐酸二甲双胍缓释片在健康受试者餐后条件下的生物等效性研究

评价盐酸二甲双胍缓释片受试制剂和参比制剂在健康受试者餐后单次给药条件下的生物等效性和安全性。试验采用单中心、随机、开放、单剂量、两周期、两序列、双交叉设计,32例健康受试者在餐后状态下单次服用受试制剂或参比制剂0.5 g,在给药前(0 h)至给药后1、3、4、4.5、5、5.5、6、7、8、9、10、12、15、24、36和48 h采集静脉血4 mL,检测血浆样本中二甲双胍的浓度,用Win Nonlin 7.0软件计算药代动力学参数,当受试制剂与参比制剂的c_max、AUC_0-t、AUC_0-∞几何均值比的90%置信区间均在80.00%～125.00%等效区间内,证明两制剂生物等效。有1例受试者因不良事件脱落。受试制剂和参比制剂的主要药代动力学参数：c_max为(0.68±0.14)和(0.65±0.11) mg/L,AUC_0-t为(7.33±1.65)和(7.00±1.89) h·mg/L,AUC_0-∞为(7.39±1.67)和(7.06±1.91) h·mg...     

国产盐酸西替利嗪片的人体药代动力学及相对生物利用度

目的 :研究国产盐酸西替利嗪片的人体药代动力学和相对生物利用度。 方法 :选择 8名男性健康志愿者 ,采用反相高效液相色谱法 ,以紫外 2 2 9nm为检测波长 ,测定了单剂量 (10 mg)口服国产盐酸西替利嗪片和进口盐酸西替利嗪片在人体内的西替利嗪浓度。 结果 :盐酸西替利嗪的体内动态过程呈一级吸收的二房室开放模型 ,国产片和进口片的 cmax分别为(316 .71± 39.6 6 )和 (314.80± 31.79) ng/ ml,tmax分别为 (0 .72± 0 .0 9)和 (0 .72± 0 .0 9) h,t1 /2β分别为 (10 .71± 3.0 6 )和(9.95± 2 .41) h,AU C0～∞ 分别为 (2 72 8.5 2± 35 6 .0 6 )和 (2 75 3.0 1± 36 0 .33) ng· h/ ml。结论 :国产盐酸西替利嗪片剂的相对生物利用度为 (99.5 0± 8.89) % ;选择 cmax和 AU C0～∞ 进行三因素方差分析与双单侧 t检验 ,结果表明国产片和进口片两种制剂具有生物等效性。     

盐酸氨溴索缓释胶囊的三维释放特性及其体内外相关性的 …

目的：评价自制盐酸氨溴索（Ａｍｂ）缓释胶囊的体外质量,并研究人体内吸刷与体外释放的相关性。方法：采用转法考察转速对释放度的影响。常温留样和加速实验观察制剂稳定性,并进行ＰＨ时间的三维释放实验和健康人体内单剂量生物利用度实验,计算累积释药分数并根据Ｗａｇｎｅｒ－Ｎｅｌｓｏｎ法计算体内药物吸收分数,经回归显示相关性。结果：Ａｍｂ缓释胶囊释药受介质ＰＨ影响较小,且不受转速的影响。制剂贮存３个月,质量稳定     

盐酸维拉帕米脉冲控释片人体内的药代动力学及生物利用度研究

目的：比较盐酸维拉帕米脉冲释放片与其片芯在人体的药代动力学特征及生物利用度。方法：采用拉丁方设计,将志愿者８人随机分为３组,交叉口服Ⅲ,Ⅳ型脉冲片和片芯,以片芯为对照制剂,考察体内脉冲控释效果。结果：Ⅲ型脉冲片在体内的时滞为４ｈ,而ｃｍａｘ,ＡＵＣ等与片芯无明显差异,达到设计要求。结论：该研究制备的脉冲释放制剂为防治心血管疾病的凌晨发作提供了一个良好的剂型选择。