腹膜透析液添加葛根素对氧化应激状态的影响

目的:观察在腹膜透析(PD)液中添加葛根素对PD患者腹腔局部及全身氧化应激状态的影响。方法:38例终末期肾病连续性非卧床腹膜透析(CAPD)治疗患者,随机分为实验组和对照组,每组19例。实验组在PD液中添加葛根素注射液(50mg/2 L),对照组PD液中不加药,均行标准CAPD治疗,每次2 L,4次/d,观察16 d。比较两组患者用药前后血清及透出液氧化应激指标:谷胱甘肽(GSH)、总超氧化物岐化酶(T-SOD)、丙二醛(MDA)以及透析充分性指标的变化。结果:用药后实验组患者血清及透出液GSH、T-SOD均较用药前显著升高(P<0.05),透出液MDA在用药后显著降低(P<0.05),患者血清清蛋白、总肌酐清除率(Ccr)、尿素氮清除指数(K t/V)、每天超滤量无明显变化。结论:在PD液中短期应用葛根素,可改善患者腹腔局部及全身的氧化应激状态。     

葛根素联合西比灵治疗颈性眩晕40例临床分析

目的:总结葛根素联合西比灵治疗颈性眩晕的疗效。方法:对40例颈性眩晕患者应用葛根素注射液静滴联合西比灵口服治疗,与40例应用西比灵口服进行对比观察,对二组病人的临床疗效进行比较。结果:葛根素联合西比灵治疗组总有效率97.5%,西比灵治疗组总有效率82.5%,两组临床疗效对比有统计学意义(P<0.05)。结论:葛根素联合西比灵治疗颈性眩晕,临床疗效比应用西比灵明显提高,且未见明显不良反应。     

薄层扫描法测定通脉口服液中葛根素含量

采用薄层扫描法测定了通脉口服液中葛根素的含量,平均加样回收率为９７．１３％（ｎ＝６）,ＲＳＤ＝２．６５％,方法简便,专属性强,灵敏度高,重现性好。     

葛根素注射液上市后产品质量比较

目的：对国内4个厂家葛根素注射液的质量进行考察,为控制产品质量提供科学依据。方法：采用RP-HPLC法,紫外检测器(λ=250 nm)测定葛根素含量,色谱柱为Luna 5μm C18 150 mm×4.6 mm,流动相为甲醇-水(28：72),葛根素在0.01～0.13 mg/ml内线形良好(γ=0.9992,n=6),RSD为1.60％(n=6)。结果：4种产品在含量和色泽方面存在差异。结论：为保证葛根素注射液的质量和疗效,进一步提高产品质量并且规范质量标准势在必行。     

HPLC法测定蓝芪降糖胶囊中葛根素的含量

为控制蓝芪降糖胶囊的质量建立葛根素的ＨＰＬＣ方法。方法：色谱条件为：ＯＤＳ柱,以甲醇－０．０２ｍｏｌ／Ｌ磷酸二氢钾（２５．７５）为流动相,流速０．８ｍｌ／ｍｉｎ,。检测波长为２５０ｎｍ。结果平均回收率９９．７４％,ＲＳＤ＝１．４４％。结论：此方法简便,灵敏,准确,重复性好,其它组分对测定无干扰,可用于该制剂的质量评价和质量控制。     

Effects of particle size on the pharmacokinetics of puerarin nanocrystals and microcrystals after oral administration to rat

Puerarin, which is extracted from traditional Chinese medicine, is widely used in clinic in China and mainly used as a therapeutic agent to cardiovascular diseases. Owing to its poor water solubility and adverse drug reactions caused by cosolvents after intravenous administration, the development of oral formulation is urgently needed. Nowadays, nanocrystals technique has become a preferred way to develop oral dosage form. In this study, we used high pressure homogenization (HPH) to prepare puerarin nanocrystals and microcrystals with different sizes ranged from 525.8 nm to 1875.6 nm and investigated the influence of particle size on pharmacokinetics. The nanocrystals and microcrystals prepared were characterized using DLS, DSC, XRD and SEM, and we found that the crystalline state of puerarin was changed during the preparation process and the drug was dispersed into HPMC. In the pharmacokinetic study, we observed an increasing of C_max and AUC and a decreasing of CL/F with the decreasing of particle size. The AUC of the puerarin nanocrystals (525.8 nm) was 7.6-fold of that of raw puerarin suspension, with an absolute bioavailability of 21.44%. From the above results, we can conclude that nanocrystal technique is an efficient technology to improve the oral bioavailability of puerarin.     

葛根素治疗急性脑梗死68例临床疗效研究

目的分析研究葛根素注射液治疗急性脑梗死的临床疗效及安全性。方法将68例急性脑梗死患者随机分为治疗组和对照组各34例。对照组采用脱水、护脑、改善微循环等治疗,治疗组在对照组用药的基础上联合应用葛根素250 mL静脉滴注,10 d为1个疗程,治疗前和治疗第10天进行血液流变学和纤维蛋白单体聚合功能的检测,并观察两组临床疗效及不良反应。结果治疗组治疗前后血液流变学和纤维蛋白单体聚合功能显著改善(P<0.05),治疗组总有效率为91.17%,对照组总有效率为76.47%,两组比较差异有统计学意义(P<0.05);两组均未发现明显的不良反应。结论葛根素可通过改善血液流变学和纤维蛋白单体聚合功能发挥治疗急性脑梗死的作用,且疗效显著,无明显的不良反应,值得临床推广应用。     

Analysis of the mechanisms underlying the endothelium-dependent antivasoconstriction of puerarin in rat aorta

Puerarin, a major isoflavonoid compound from the Chinese herb, Ge-gen (Pueraria lobata), has effective treatment on myocardial and cerebral ischemia, glaucoma and sudden deafness in clinical setting in China. Our present work showed that puerarin (50, 150, 450 μM) concentration-dependently inhibited phenylephrine or KCl-induced contraction only in endothelium-intact rat aortic rings. In Ca²⁺-free solution, the antivasoconstriction of puerarin on phenylephrine was totally deprived. N ^G-nitro-l-arginine methyl ester, 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one, indomethacin and the three K⁺ channel blockers, glibenclamide, tetraethylammonium and Ba²⁺ displayed significant inhibitory effects on the antivasoconstriction of puerarin. 8-bromo-cGMP significantly strengthened the action of puerarin. Puerarin (10–160 μM) concentration-dependently induced the NO production in the rat aortic cells. These findings suggested that the antivasoconstriction elicited by puerarin is endothelium-dependent. NO/NO–cGMP pathway, PGI₂ and the opening of K⁺ channels sensitive to glibenclamide, tetraethylammonium, and Ba²⁺, which might be triggered by the extracellular Ca²⁺ influx in the endothelium, appear to contribute to the antivasoconstriction of puerarin.     

葛根中葛根素的高效液相色谱分析

目的 测定不同产地葛根中葛根素的含量。方法 用HPLC法测定，以MeOH—H2O-HAc-（25：75：0，5）为流动相，250nm为检测波长。结果葛根素在0．026—1．95μg与峰面积呈良好线性关系（r=0．9998），平均回收率为97．3％，RSD为1．35％（n=5）。结论 该法简单、快速、准确，适用于葛根中葛根素含量的测定。     

葛根素对糖尿病大鼠视网膜组织中细胞间黏附分子-1表达的影响及意义

目的观察葛根素对糖尿病大鼠视网膜细胞间黏分子-1（ICAM-1）表达的影响。方法利用链脲佐菌素腹腔注射法建立糖尿病大鼠模型,将实验用Wistar大鼠随机分为正常对照组、葛根素治疗组和糖尿病组,治疗12周。观察治疗期间及治疗后各组大鼠的一般情况、尿糖、血糖、血NO及血SOD值,HE染色及免疫组化染色法观察大鼠视网膜形态及ICAM-1表达的不同。结果和正常对照组相比,造模组大鼠血糖均升高,血SOD和血NO值降低（P〈0.05）。葛根素能改善大鼠基本情况,降低血糖（P〈0.05）,升高血SOD及血NO值（P〈0.05）,并减少视网膜组织细胞间ICAM-1表达,其差异有统计学意义。结论葛根素对糖尿病大鼠视网膜组织间ICAM-1的表达具有抑制作用,从而对高血糖引起的视网膜损伤有一定的保护作用。