参肽茶多酚胶囊配方优化研究

目的确定参肽茶多酚胶囊辅料的最佳配方用量。方法以淀粉、胶态二氧化硅、硬脂酸镁为考察因素,每个因素取3个水平,用L9（34）正交表安排试验,以粉体流动性为考察指标,进行正交试验。结果每1 000粒参肽茶多酚胶囊配方中添加淀粉130 g、胶态二氧化硅3 g、硬脂酸镁3 g时,粉体流动性最好。结论本研究配方合理,适于放大生产。     

银屑胶囊中白藜芦醇含量测定

目的：建立银屑胶裳中白藜芦醇的含量测定方法。方法：采用高效液相色谱法测定银屑胶囊中白藜芦醇的含量。结果：测定结果灵敏可靠,回收率在95．72％～99．92％,RSD为1．55％。结论：本方法可作为制剂质量控制方法。     

Systemic and cerebral exposure to and pharmacokinetics of flavonols and terpene lactones after dosing standardized Ginkgo biloba leaf extracts to rats via different routes of administration

BACKGROUND AND PURPOSE

Flavonols and terpene lactones are putatively responsible for the properties of Ginkgo biloba leaf extracts that relate to prevention and treatment of cardiovascular disease and cerebral insufficiency. Here, we characterized rat systemic and cerebral exposure to these ginkgo compounds after dosing, as well as the compounds’ pharmacokinetics.

EXPERIMENTAL APPROACH

Rats received single or multiple doses of ShuXueNing injection (prepared from GBE50 for intravenous administration) or GBE50 (a standardized extract of G. biloba leaves for oral administration). Brain delivery of the ginkgo compounds was assessed with microdialysis. Various rat samples were analysed using liquid chromatography/mass spectrometry.

KEY RESULTS

Slow terminal elimination features of the flavonols counterbalanced the influence of poor oral bioavailability on their systemic exposure levels, which also resulted in significant accumulation of the compounds in plasma during the subchronic treatment with ShuXueNing injection and GBE50. Unlike the flavonols, the terpene lactones had poor enterohepatic circulation due to their rapid renal excretion and unknown metabolism. The flavonol glycosides occurred as major forms in plasma after dosing with ShuXueNing injection, while the flavonol aglycone conjugates were predominant in plasma after dosing with GBE50. Cerebral exposure was negligible for the flavonols and low for the terpene lactones.

CONCLUSION AND IMPLICATIONS

Unlike the significant systemic exposure levels, the levels of cerebral exposure to the flavonols and terpene lactones are low. The elimination kinetic differences between the two classes of ginkgo compounds influence their relative systemic exposure levels. The information gained is relevant to linking ginkgo administration to the medicinal effects.     

银杏叶注射液治疗冠心病不稳定型心绞痛疗效观察

目的:观察银杏叶注射液治疗冠心病不稳定型心绞痛的疗效及安全性。方法:将60例冠心病不稳定型心绞痛患者随机分为两组各30例,治疗组应用银杏叶注射液,对照组除不用银杏叶注射液外,其余治疗同治疗组。结果:治疗组显效19例,有效9例,有效率93.3%;对照组显效12例,有效10例,有效率73.3%。两组有效率比较差异有统计学意义(χ2=4.32,P<0.05)。结论:银杏叶注射液治疗冠心病不稳定型心绞痛疗效显著。     

麻仁软胶囊对便秘的疗效及其安全性考察

目的 观察麻仁软胶囊对便秘的疗效和对结肠黏膜的影响。方法 结肠慢传输型及混合型便秘的门诊患者208例随机分为治疗组及对照组。治疗组患者每日口服麻仁软胶囊1次,每次2粒,连续服用10个月;对照组患者每日口服番泻叶5 g（沸水100 mL浸泡后顿服）1次,连续服用10个月。根据排便次数和胃肠传输实验（GITT）判断治愈率、总显效率（治愈率＋显效率）、总有效率（总显效率＋有效率）。依据腹胀、腹痛等判断不良反应。治疗10个月后肠镜观察结肠黏膜黑变情况。结果 治疗组的治愈率略低于对照组,总显效率、总有效率与对照组无显著差异,治疗组患者服药后10个月后镜检未发现结肠黑变,而对照组26.9%患者结肠黑变。结论 低剂量麻仁软胶囊治疗便秘有效,并具有较高安全性。     

桂枝茯苓胶囊化学成分研究（IV）

目的 对桂枝茯苓胶囊内容物石油醚和醋酸乙酯萃取部分的化学成分进行研究。方法 采用硅胶柱色谱葡聚糖凝胶及制备型高效液相色谱进行分离纯化,利用NMR及MS等谱学方法鉴定化合物的结构。结果 从石油醚萃取部分得到8个化合物,分别鉴定为香豆素（1）、7-羟基香豆素（2）、肉桂醇（3）、麦角甾醇（4）、麦角甾-4, 6, 8(14), 22-四烯-3-酮（5）、β-香树脂醇乙酸酯（6）、菜油甾醇（7）、α-香树脂醇乙酸酯（8）;从醋酸乙酯萃取部分得到13个化合物,分别鉴定为芹菜素（9）、山柰酚（10）、槲皮素（11）、山柰酚3-O-葡萄糖苷（12）、儿茶素（13）、表儿茶素（14）、丁香酸（15）、金丝桃苷（16）、正二十碳酸（17）、丁香脂素（18）、牡丹皮苷A（19）、牡丹皮苷C（20）、没食子酰芍药苷（21）。结论 所有化合物均为首次从该复方中分离得到。     

In Vitro Bactericidal Activity of Jinghua Weikang Capsule (荆花胃康胶丸) and Its Individual Herb Chenopodium Ambrosioides L. against Antibiotic-Resistant Helicobacter Pylor

Objective:To investigate the bactericidal effects of Jinghua Weikang Capsule(荆花胃良胶丸and its major component Chenopodium ambrosioides L.on antibiotic-resistant Helicobacter pylori.Methods: Four clinical antibiotic-resistant H.pylori strains were isolated and incubated in liquid medium containing Jinghua Weikang Capsule or Chenopodium ambrosioides L By means of time-kill curve method,the average colony counts and bactericidal rate were calculated at time points of 0,4,8 and 24 h after the incubation and the time-kill curves were charted.Results:Both Jinghua Weikang Capsule and Chenopodium ambrosioides L at a concentration of 0.64 g/L showed obvious bactericidal effect against antibiotic-resistant H.pylori after 4 h of incubation.Conclusion:Jinghua Weikang Capsule and Chenopodium ambrosioides L.are considered to be active against antibiotic-resistant H.pylori in vitro.     

抗骨疏不同提取物大鼠模型骨质疏松症的作用及其潜在机制

Objective： To investigate the preventive effects and possible underlying mechanism of different extracts of Kanggushu （抗骨疏） on osteoporosis in ovariectomized rats. Methods： One hundred and sixty- five female SD rats were divided into 11 groups： control, sham, model, Xianling Gubao Capsule （仙灵骨葆胶囊）, nilestriol, Kanggushu aqueous extract high-, medium-, and low-dose and suet extract high-, medium-, and low-dose groups. The osteoporosis model was made by ovariectomizing the rats. The latter 8 groups were administered intragastricly with Xianling Gubao Capsule, nilestriol, Kanggushu aqueous extract and suet extract for 12 weeks, respectively, while the other 3 groups were administered orally saline. The whole body bone mineral density, bone mineral content, organ coefficient of uterus, serum estradiol and alkaline phosphatase contents, blood calcium, phosphorus, interleukin 6 and bone Gla-protein levels after treatment were monitored. Additionally, three-point bending test of femur, HE staining, and scanning electron microscope were performed to explore the pharmacodynamics and underlying mechanisms. Results： In comparison with ovariectomized rats of model group, Kanggushu aqueous extract high-dose resulted in an increased bone mineral density, bone mineral content and organ coefficient of uterus, improved estradiol level, and improved maximum load and structural stiffness （P〈0.05 or P〈0.01）. Two-dimensional and thrae-dimensional trabecular structure was also observed under HE staining and scanning electron microscopy, and the number and thickness of trabecular bone in Kanggushu aqueous extract high-dose group was significantly increased compared to the model group, while the lipid droplets in bone marrow cavity were significantly less. However, there were no significant differences in blood calcium, total serum alkaline phosphatase and bone Gla protein among different treatment groups. Overall, the osteoprotective effects of Kanggushu aqueous extract were comparable to those of nilestriol and were significantly more effective than those of Xianling Gubao Capsule. Conclusion： The preventive effects of Kanggushu aqueous extract might be partly due to the increased estradiol level, accelerated restoration of bone trabecular reticulate structure, and accordingly increased bone mineral density in osteoporosis rats.     

Effects of Jinmaitong Capsule (筋脉通胶囊) on Ciliary Neurotrophic Factor in Sciatic Nerves of Diabetes Mellitus Rats

Objective:To study the effects of the Chinese medicine Jinmaitong Capsule(筋脉通胶囊,JMT) on the pathomorphology of sciatic nerves,ciliary neurotrophic factor(CNTF),and the mRNA expressions of CNTF in rats with streptozotocin-induced diabetes mellitus(STZ-DM).Methods:The animal model was established by one time intraperitoneal injection of streptozotocin.The rats were simply divided by random into 5 groups including model group,low-dose JMT group(JL),medium-dose JMT group(JM),high-dose JMT group(JH) and neurotropin group.For each of the above 5 groups,a group of 10 normal Wistar rats matched in body weight,age and gender were set as normal group.Intragastric administrations were started after the animal model established.The JL group were administered with five times the JMT dose recommended for a human adult;the JM group were administered with ten times the JMT dose recommended for a human adult;the JH group were administered with twenty times the JMT dose recommended for a human adult.The neurotropin group was administered with ten times the neurotropin dose recommended for a human adult.All rats were given intragastric administration for 16 weeks and then killed.In the 4th,8th,12th,16th week,body weight and blood glucose level were detected before and after the intervention.The morphologic changes of the sciatic nerves were observed by optical microscope and transmission electron microscope.The CNTFmRNA expressions were detected by real-time fluorescent quantitative polymerase chain protein,and the CNTF protein expressions were detected by immunohistochemical method.Results:The blood glucose levels of the STZ-DM rats were much higher than normal group(P<0.01),and there was no apparent difference between any treatment groups and the model group(P>0.05).Before and after the intervention in the 4th, 8th,12th,16th week,there were no significant differences in the body weight among all the groups(P>0.05). The sciatic nerves of STZ-DM rats might have pathomorphological changes in axons,myelin sheaths,and interstitium.The levels of CNTF and CNTF-mRNA expressions in the STZ-DM rats were both significantly decreased(P<0.01).The sciatic nerves of STZ-DM rats might have pathomorphological changes in axons, myelin sheaths,and interstitium.Conclusion:JMT could improve the pathomorphology of sciatic nerves by increasing CNTF’s and CNTF-mRNA expressions in sciatic nerve tissues,and promote the repair and regeneration of damaged nerve fibers.     

珍枣胶囊对老年阴虚火旺失眠患者5-HT、DA含量的影响

目的 通过观察珍枣胶囊治疗老年阴虚火旺型失眠患者中医临床症状的变化以及血浆5-羟色胺(5-HT)、多巴胺(DA)含量的改变,评价其临床疗效,并探究其作用机制。方法 将60例符合失眠诊断标准以及阴虚火旺证中医辨证标准的原发性失眠患者,按照随机分组、单盲以及平行对照的方式,分为治疗组和对照组各30例。治疗组患者睡前0.5 h服用珍枣胶囊,每日1次、5粒/次,对照组患者睡前0.5 h服用舒眠胶囊,每日1次、5粒/次。各组均连续服药4周为1个疗程,每7天复诊1次。观察时间为1个疗程。观测治疗前后血浆5-HT和DA水平的变化;并对2组患者的临床疗效以及中医证候疗效进行评定。结果 2组老年阴虚火旺型失眠患者改善失眠的临床疗效相当,P>0.05;但在改善中医证候疗效方面,治疗组改善更明显,与对照组比较,P<0.05。2组患者治疗前后相比,5-HT水平皆提高且DA含量皆降低,治疗组调节幅度优于对照组,P<0.05。结论 珍枣胶囊改善了老年阴虚火旺型失眠患者的中医临床症状,临床疗效显著;其治疗机理可能与提高5-HT水平以及降低DA含量有关。