复方血栓通滴丸的薄层色谱鉴别和含量测定

目的制订复方血栓通滴丸的鉴别和含量测定的质量标准。方法薄层色谱法。结果供试品薄层色谱鉴别的斑点清晰，重现性好，阴性对照无干扰；三七主要成分人参Rg1和人参Rn1的含量测定色谱在540nm波长处有最大吸收，浓度与吸收度呈线性关系，平均回收率分别为99、29％和99．66％，RSD分别为1．0％和0．6％（n=6）。结论该准确可靠、操作简便，可作为复方血栓通滴丸有效的质量控制方法。     

三七固体分散体滴丸制备工艺及质量研究

目的：确定三七滴丸的处方和制备工艺,并对其质量进行初步考察。方法：采用正交验进行三七滴丸的处方设计和工艺优化。利用薄层色谱(TLC)进行定性鉴别。以人参皂苷Rg1、人参皂苷Rb1为标准,运用双波长薄层扫描法对人参皂苷Rg1和人参皂苷Rb1进行含量测定。结果：三七总皂苷——PEG6000——硬脂酸——吐温-80为15：31：1：3组成处方,滴丸甲醇提取液在λs=510nm,λr=700nm,经外标二点法扫描测定,得三七皂苷的含量。结论：所得滴丸在溶散时限、丸重差异上均符合药典标准。双薄层扫描法含量测定简便、准确。     

HPLC测定复方丹参片中三七总皂苷的含量

目的建立复方丹参片中三七有效成分的含量测定方法。方法采用HPLC法测定本品中三七中人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1的含量。结果人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1线性范围分别依次为0.850～8.524、0.922～9.013、0.377～3.317μg;平均回收率分别为101.1%、101.2%、103.2%,RSD分别为1.5%、1.6%、1.8%。结论本方法简便可靠,结果稳定,可用于丹心舒胶囊中三七的有效成分的含量测定。     

HPLC 法同时测定复方血栓通胶囊中5种皂苷类成分

目的：建立 HPLC 法同时测定复方血栓通胶囊中人参皂苷 Rg1、Re、Rb1、Rd 和三七皂苷 R1含量的方法。方法采用YMC －Pack Pro C18柱（250 mm ×4．6 mm,5μm）,以乙腈为流动相 A,水为流动相 B 进行梯度洗脱,检测波长为203 nm,流速为1．0 mL·min －1,柱温为35℃。结果测得三七皂苷 R1在50．10～501．00 ng、人参皂苷 Rg1在151．02～1510．20 ng、人参皂苷Re 在32．01～302．10 ng、人参皂苷 Rb1在102．23～1022．30 ng、人参皂苷 Rd 在16．32～163．20 ng 范围内线性关系良好（r ＝0．9999）;精密度、稳定性、重复性 RSD 均小于3％;平均加样收回率在95％～105％之间。结论该法简便、准确、重复性好,可用于复方血栓通胶囊的质量控制。     

HPLC测定中药水煎液中人参皂苷Rg1、Rb1和三七皂苷R1的含量

目的：建立中药水煎液中人参皂苷Rg1、Rb1和三七皂苷R1的含量测定方法.方法：采用高效液相色谱法测定三七及复方丹参滴丸水煎液中有效成分含量.结果：三七及复方丹参滴丸水煎液中人参皂苷Rg1、Rb1及三七皂苷R13种成分均达到良好分离,在测定范围内线性良好,回收率在99.2%～100.4%之间.结论：所建立的定量方法简便可行、重复性好,可用于含三七皂苷类成分的中药制剂的质量控制.     

高效液相色谱法测定复方血栓通胶囊中三七总皂苷的含量

目的建立复方血栓通胶囊中三七皂苷R1和人参皂苷Rg1、Rb1含量测定的HPLC法。方法采用Venusil-XBP-C18色谱柱(250 mm×4.6 mm,5μm),以乙腈(A)和水(B)为流动相梯度洗脱,流动相梯度0～12 min为A∶B=20∶80(V/V),12～16 min为A∶B=(20～36)∶(80～64)(V/V)。流速1.0 mL.min-1,柱温30℃,检测波长203 nm。结果三七皂苷R1、人参皂苷Rg1、人参皂苷Rb1线性范围分别为0.39～8.57μg、1.43～32.96μg、1.72～41.53μg,平均加样回收率分别为(99.50±1.26)%、(99.40±1.31)%、(100.10±1.53)%,RSD分别为1.14%、1.07%、0.91%。结论该方法操作简便、结果准确可靠、灵敏度高,重复性好,能有效控制复方血栓通胶囊的质量。     

高效液相色谱法测定复方丹参片与滴丸中7种活性成分含量

目的：建立高效液相色谱( HPLC)法同时测定复方丹参片和复方丹参滴丸中7种活性成分含量的方法。方法采用Zorbax C18色谱柱,以乙腈-0.1％磷酸溶液为流动相,梯度洗脱,流速1 mL·min-1,检测波长为203,270和281 nm。结果7种成分峰面积与浓度的线性关系良好;加样回收率在95.1％~100.4％;滴丸样品中丹参酮ⅡA未能检出。结论建立了两类复方丹参制剂中同时测定丹参素、原儿茶醛、三七皂苷R1、人参皂苷Rg1、丹酚酸B、人参皂苷Rb1和丹参酮ⅡA含量的方法,精密度高,重复性好,可用于两类复方丹参制剂的质量控制;复方丹参片中丹参酮ⅡA含量明显高于滴丸。     

复方三七胶囊的工艺制备及临床疗效观察

目的探讨复方三七胶囊的工艺制备及相关的临床疗效观察。方法将中药三七、肉桂按照一定的比例,粉碎成细粉后,用胶囊分装机器进行填充,制备成复方三七胶囊,采用精密仪器测定复方三七胶囊中有效成分人参皂苷Rb1和人参皂苷Rg1的含量,同时选择自愿接受治疗的患者66例,设立观察组与对照组,分别观察其临床治疗效果。结果制备的复方三七胶囊中人参皂苷Rb1、人参皂苷Rg1含量测定的回收率分别为99.84%(RSD=1.24%)、101.20%(RSD=1.15%),通过两组观察,观察组与对照组的临床有效率分别为97.22%(35/36)、76.67%(23/30)。结论复方三七胶囊制备工艺简单,临床上在散瘀、温经通脉以及消肿止痛等方面的疗效肯定,质量稳定。     

血塞通滴丸的含量测定研究

目的建立血塞通滴丸的鉴别、含量测定方法。方法采用TLC法鉴别血塞通滴丸中的人参皂苷Rb1、Rg1和三七皂苷R1;采用HPLC法测定本品三七皂苷R1的含量。结果TLC鉴别方法简便、准确;三七皂苷R1在0.51-4.08μg呈良好的线性关系,人参皂苷Rb1在3.75-30.00μg呈良好的线性关系。相对标准偏差（RSD）小于1%。重现性试验其相对标准偏差（RSD）小于1%。三七皂苷R1的平均回收率为100.5%,相对标准偏差（RSD）为1.74%;人参皂苷Rg1的平均回收率为99.00%,相对标准偏差（RSD）为1.63%;人参皂苷Rb1的平均回收率为98.78%,相对标准偏差（RSD）为1.97%。结论所建的TLC鉴别方法准确、特异性强、无干扰;HPLC含量测定方法简单、分离度高,完全能够控制本品质量。     

RP-HPLC同时测定复方三七制剂中的人参皂苷Rg1、Rb1

目的 建立复方三七制剂中人参皂苷Rg1、Rb1含量测定的方法.方法 采用RP-HPLC法,色谱柱为Phenomenex C18(250 mm x4.6 mm,5 μm);流速1.0 ml·min-1;检测波长203 nm;柱温30℃;流动相为乙腈-水(梯度洗脱).结果 人参皂苷Rg1的线性范围为0.2124～2.1240 μg(r=0.9999),平均回收率为100.24%,RSD=1.14%(n=9);人参皂苷Rb1的线性范围为0.2108～2.1080μg(r=0.9999),平均回收率为99.71%,RSD=0.79%(n=9).结论 所建方法简便、准确,重复性好,可同时测定复方三七制剂中人参皂苷Rg1和人参皂苷Rb1的含量.     

三七总皂苷肠溶微囊的药代动力学及体内外相关性

目的:考察三七总皂苷(panax notoginseng saponins,PNS)肠溶微囊在Beagle犬体内的释药行为及其体内外相关性研究。方法:采用双周期交叉试验设计,6只健康Beagle犬口服市售血栓通胶囊或自制PNS肠溶微囊(胶囊型)后,用HPLC法测定血药浓度,计算两制剂的药代动力学参数,进行生物利用度比较,并对体外累积释放度和体内累积吸收百分率进行线性回归。结果:自制PNS肠溶微囊对市售血栓通胶囊的相对生物利用度为三七皂苷R1(R1)313.63%,人参皂苷Rb1(Rb1)314.35%,人参皂苷Rg1(Rg1)202.03%,上述3成分在体内的平均滞留时间均延长,R1,Rb1和Rg1的体内外相关系数分别为0.866 4,0.958 0和0.719 2。结论:自制PNS肠溶微囊与市售血栓通胶囊相比生物利用度更高,Rb1体内外相关性较好,可用一定的体外释放条件进行体内行为的预测,R1和Rg1体内外相关性较差。     

Protective effect of fermented Red ginseng on a transient focal ischemic rats

Red ginseng and fermented red ginseng were prepared, and their composition of ginsenosides and antiischemic effect were investigated. When ginseng was steamed at 98-100 degrees C for 4 h and dried for 5 h at 60 degrees C, and extracted with alcohol, its main components were ginsenoside Rg3> ginsenoside Rb1 > ginsenoside Rb2. When the ginseng was suspended in water and fermented for 5 days by previously cultured Bifidobacterium H-1 and freeze-dried (fermented red ginseng), its main components were compound K > ginsenoside Rg3 > or = ginsenoside Rh2. Orally administered red ginseng extract did not protect ischemia-reperfusion brain injury. However, fermented red ginseng significantly protected ischemica-reperfusion brain injury. These results suggest that ginsenoside Rh2 and compound K, which was found to be at a higher content in fermented red ginseng than red ginseng, may improve ischemic brain injury.     

HPLC指纹图谱法测定不同粉碎度野山花旗参粉末中人参皂苷含量

目的：建立高效液相色谱法（HPLC）指纹图谱法,测定野山花旗参100目、200目、1000目粉三种粉末中人参皂苷Re、Rb1、Rg1的总含量,通过指纹图谱相似度比较,考察粉碎对野山花旗参中人参皂苷的影响。方法：采用梯度洗脱、HPLC测定三种粒径粉末的HPLC指纹图谱,计算主要药效成分人参皂苷Re、Rb1、Rg1的含量,并进行比较,通过“中药色谱指纹图谱相似度评价系统”评价三个样品的相似度。结果：野山花旗参100目、200目、1000目粉的主要有效成分人参皂苷Re、Rb1、Rg1的总含量均大于3.96%,三种粉末的指纹图谱重叠率高,共有峰的相对保留时间吻合,与生成的对照指纹图谱相似度分别为0.946,0.979,0.970。结论：野山花旗参100目、200目与1000目粉的HPLC指纹图谱相似度大于0.946,化学成分的种类没有变化,主要有效成分人参皂苷Re、Rb1、Rg1的总含量基本相等,野山花旗参超微粉碎成1000目粉,化学成分保持不变。     

Comparison of the pharmacological effects of Panax ginseng and Panax quinquefolium

Medical application of Panax ginseng was first found in "Shen-Nong Herbal Classic"around 200 AD Panax quinquefolium was first introduced in "Essential of Materia Medica" in 1694 in China. The most important bioactive components contained in P ginseng and P quinquefolium are ginseng saponins (GS). The contents of ginsenoside Rb1, Re, and Rd in P quinquefolium are higher than they are in P ginseng. In P ginseng, the contents of Rg1,Rb2, and Rc are higher than they are in P quinquefolium. P ginseng had a higher ratio of Rg1: Rb1, and which was lower in P quinquefolium. After steaming for several hours, the total GS will decrease. However, some ginsenosides (Rg2, 20R-Rg2, Rg3, Rh1 and Rh2) increase, while others (Rb1, Rb2, Rb3, Rc, Rd, Re, and Rg1) decrease. However, variation, especially in P quinquefolium, is high. P ginseng and P quinquefolium are general tonics and adaptogens. Rg1 and Rb1 enhance central nervous system (CNS) activities, but the effect of the latter is weaker. Thus, for the higher contents of Rg1, P ginseng is a stimulant, whereas the Rb1 contents of P quinquefolium are mainly calming to the CNS. Re, Rg1, panaxan A and B from P ginseng are good for diabetes. Re and Rg1 enhance angiogenesis, whereas Rb1, Rg3 and Rh2 inhibit it. Rh2, an antitumor agent, can be obtained from Rb1 by steaming. The content of Re in P quinquefolium are higher than in P ginseng by 3-4 times. The vasorelax, antioxidant, antihyperlipidemic, and angiogenic effects of Re are reported. Thus, for the CNS "hot," wound healing and hypoglycemic effects, P ginseng is better than P quinquefolium. For anticancer effects, P quinquefolium is better.     

三七总皂苷肠溶胶囊在比格犬体内的药代动力学

目的探讨三七总皂苷(PNS)肠溶胶囊在比格犬体内的药代动力学。方法比格犬采用随机交叉给药方案,口服PNS肠溶胶囊86.2 mg·kg-1或血栓通胶囊111.8 mg·kg-1后,用反相高效液相色谱法同时测定犬血浆中三七皂苷R1、人参皂苷Rg1和Rb1的血药浓度,采用3P97药动学软件计算药动学参数和基于曲线下面积(AUC0-∞)自定义权重系数整合血药浓度后的药动学参数。结果与参比制剂血栓通比较,受试制剂PNS R1、Rg1、Rb1的达峰时间延长:R10.18±0.09 vs(0.16±0.06)h,Rg12.03±0.76 vs(1.74±0.27)h,Rb1 0.76±0.39 vs(0.74±0.17)h;吸收延迟时间延长:R1 0.96±0.16 vs(0.50±0.11)h,Rg10.87±0.05 vs(0.02±0.01)h,Rb10.92±0.12 vs(0.44±0.07)h,3种成分及其整合后PNS的相对生物利用度分别为248.41%,107.19%,152.94%和155.31%。整合后,血栓通胶囊和PNS肠溶胶囊的主要药动学参数分别为:AUC0→t39.17±3.89 vs(46.91±3.86)mg.L-1.h,Lag时间0.45±0.18 vs(0.92±0.13)h,tmax0.74±0.17 vs(0.77±0.13)h,Cl(3.84±0.24 vs 1.84±0.97 L.kg-1.h-1)。结论本实验制备的PNS肠溶胶囊能提高PNS的口服生物利用度。     

Simultaneous quantification of 14 ginsenosides in Panax ginseng C.A. Meyer (Korean red ginseng) by HPLC-ELSD and its application to quality control

A new method of high-performance liquid chromatography coupled with evaporative light scattering detection (HPLC-ELSD) was developed for the simultaneous quantification of 14 major ginsenosides, which are the marker compounds of Panax ginseng C.A. Meyer (Korean red ginseng). Various types of ginseng samples were extracted, and the amounts of the 14 ginsenosides (Rg1, Re, Rf, Rh1, Rg2, Rb1, Rc, Rb2, Rb3, Rd, Rg3, Rk1, Rg5, and Rh2) were determined by reverse-phase HPLC-ELSD using digoxin as an internal standard. The mobile phase consisted of a programmed gradient of aqueous acetonitrile. Calibration curves for each ginsenoside were determined for the quantification. The method was validated for linearity, precision, accuracy, limit of detection, and limit of quantification. This quantification method was applied to several finished ginseng products including white ginseng, red ginseng powder, and red ginseng concentrate. The amounts of the 14 ginsenosides in the various ginseng samples could be analyzed simultaneously. This validated HPLC method is expected to provide a new basis for the quality assessment of ginseng products.     

Anxiolytic-like effects of ginsenosides on the elevated plus-maze model in mice

In a previous study, we reported that ginseng extract has anxiolytic-like effects in the elevated plus-maze model and that the ginseng saponin fraction plays an important role. This experiment was performed to investigate the anxiolytic-like effects of ginsenosides Rb1, Rg1, Rg3-R, and Rg3-S, and the Rg5 and Rk mixture isolated from the ginseng saponin fraction in the elevated plus-maze. Furthermore, the anxiolytic-effects of Rb1, Rg1, Rg3-R, Rg3-S, and the Rg5 and Rk mixture were compared with those of a well-known active anxiolytic drug (diazepam). The oral administration of ginsenoside Rb1 significantly increased the number of open arm entries and the time spent on the open arm compared with those in the vehicle-treated group. Ginsenoside Rg1 and the Rg5 and Rk mixture also significantly increased the number of open arm entries and the time spent on the open arm. However, ginsenosides Rg3-R and Rg3-S did not increase the number of open arm entries or the time spent on the open arm. On the other hand, ginsenoside Rb1 and the Rg5 and Rk mixture decreased locomotor activity in a manner similar to diazepam. These data indicate that ginsenosides Rb1, Rg1, and the Rg5 and Rk mixture have anxiolytic-like effects, but ginsenosides Rg3-R and Rg3-S do not in this model. We provide evidence that some ginsenosides may be useful for the treatment of anxiety.     

疾病以及配伍对人参皂苷在大鼠体内的药动学影响

目的 建立SD大鼠血浆中人参皂苷Rb1、Rb2和Rg1的HPLC分析方法,对比分析配伍白术挥发油前后,人参皂苷在慢性萎缩性胃炎模型大鼠体内药动学特征。方法 SD大鼠分为4组,其中单用正常组和单用模型组均给药人参总皂苷292 mg·kg^-1,配伍正常组和配伍模型组均给药人参总皂苷292 mg·kg^-1和白术挥发油0.1 mL·kg^-1。于给药前和给药后不同时间点进行眼眶取血,采用HPLC测定各成分的血药浓度,并采用Winnolin 6.3软件计算其药动学参数。结果 与单用正常大鼠比较,单用模型组大鼠体内人参皂苷Rb1的C_max和AUC值降低,T_max、T_1/2以及MRT增加,人参皂苷Rb2和Rg1则呈现出AUC增加的变化;而配伍正常组大鼠体内人参皂苷Rb1、Rb2和Rg1的C_max和AUC值均增加,T_max、T_1/2以及MRT值均缩短。与单用模型组大鼠比较,配伍模型组大鼠体内人参皂苷Rb1和Rg1的C_max和AUC值均增加,T_max、T_1/2以及MRT值均降低。结论 在相同给药剂量下,疾病状态机体对人参皂苷的吸收和代谢呈现缓慢趋势,而配伍后能促进皂苷成分在体内的吸收,同时加快代谢消除,为人参的临床用药提供参考依据。     

Preparation and In Vitro and In Vivo Evaluation Of Panax Notoginseng Saponins-loaded Nanoparticles Coated with Trimethyl Chitosan Derivatives

In this study, novel Panax notoginseng saponins (PNS)-loaded nanoparticles coated with the Trimethyl chitosan (TMC) derivatives TMC-VB₁₂ and TMC-Cys (PPTT-NPs) were developed to improve the oral absorption of the constituents. PPTT-NPs were prepared by the double emulsion method and showed different encapsulation effects on the major components, including Rg1, Rb1, and R1, in PNS. In vivo, the absorption rate constant and apparent absorption coefficient of PPTT-NPs were higher than PNS solution. These findings preliminarily proved that PPTT-NPs can promote intestinal absorption to a certain extent. The pharmacokinetic results indicated that the blood concentration and the area under the curve of Rg1 and Rb1 in the PPTT-NPs were higher than Xueshuantong capsules. The cell viability of PPTT-NPs was above 90% within 25-150 μg/mL. PPTT-NPs promoted the cellular uptake of PNS by receptor-mediated endocytosis. In summary, NPs coated with TMC-VB₁₂ and TMC-Cys can be used as promising drug delivery systems.