柚皮素脂质体的制备及大鼠肺部给药药动学研究

目的制备柚皮素(naringenin)脂质体,研究其理化性质及经大鼠肺部给药后的体内药动学行为。方法采用薄膜分散法制备柚皮素脂质体,考察其形态、粒径、Zeta电位、载药量、包封率及渗漏率,透析袋测定脂质体在磷酸盐缓冲液中的释放,通过肺部滴注给药考察脂质体在大鼠体内的药动学行为。结果柚皮素脂质体外形圆整,平均粒径为(137.6±8.1)nm,Zeta电位为(-21.9±5)m V,包封率为(80.51±2.63)%,泄漏率低;24 h累积释放达70%以上,脂质体的体外释放符合Weibull方程;柚皮素原料药和脂质体的MRT分别为(14.650±0.242)h和(20.721±0.873)h,Cmax分别为(117.910±0.012),(722.477±0.025)ng/m L,AUC0-48分别为(928.431±0.137),(1 850.061±0.348)ng·h/m L。结论薄膜分散法成功制备了柚皮素脂质体;与原料药相比,柚皮素脂质体肺部给药后有明显的缓释作用,能提高药物的生物利用度。     

青蒿素类纳米脂质体在大鼠体内的药动学研究

目的制备水化后粒径较小(150 nm)且分布较窄的具有良好稳定性的青蒿素类冻干脂质体,考察其体外释药特性及其在大鼠体内药动学特征。方法采用薄膜分散法制备纳米脂质体,冷冻干燥工艺制成冻干脂质体,采用透析法测定其包封率和体外释放曲线,以紫外分光光度法测定青蒿素类药物的血药浓度,与以青蒿素原料药作对照,比较大鼠体内的药动学参数。结果实验数据经origin7.5软件处理提示:平均包封率为74.4%。双氢青蒿素脂质体前3 h释药曲线符合Higuchi方程:Q=17.213t1/2+17.821 1(r=0.994 55),青蒿琥脂脂质体前6 h原料药符合Higuchi方程:Q=17.63t1/2+16.09(r=0.990 31)。而二者原料药在30 min释放均超过60%。血药浓度-时间数据符合单室模型。结论薄膜法经超声分散所制脂质体包封率较高,体外有明显的延缓药物释放的性质。与原料药相比,大鼠灌胃给药青蒿琥酯脂质体后,具有较长的消除半衰期,纳米脂质体制剂组曲线下面积(AUC)是青蒿素组的3.89倍以上。     

柚皮素固体脂质纳米粒冻干粉的制备及其大鼠肺部给药药动学研究

目的制备柚皮素(NRG)固体脂质纳米粒冻干粉,考察其理化性质及经大鼠肺部给药后的体内药动学行为。方法采用乳化蒸发-低温固化法,以包封率、粒径为考察指标,正交试验优化其处方并考察其粒径、形态、电位及体外释放。以外观、色泽、再分散性为考察指标筛选最佳冻干保护剂,采用差式扫描量热(DSC)分析药物在纳米粒中的存在状态。通过肺部给药考察NRG固体脂质纳米粒和NRG原料药溶液在大鼠体内的药动学行为。结果 NRG固体脂质纳米粒外观呈球形,分布均匀,平均粒径为(97.69±2.84)nm,多分散系数(PDI)为0.207±0.010,Zeta电位为(-26.20±0.45)m V,包封率为(81.09±1.37)%,载药量为(8.30±0.04)%(n=3),5%甘露醇为冻干保护剂最好,药物以无定形状态分散在脂质载体中,体外溶出实验表明NRG固体脂质纳米粒与原料药相比具有明显的缓释作用。NRG原料药和纳米粒的Cmax分别为(163.00±23.05)、(269.00±35.34)ng/m L,t1/2分别为(5.13±0.23)、(18.93±7.90)h,AUC0-t分别为(929.32±190.28)、(3 390.23±533.68)ng·h/m L,MRT分别为(7.19±0.44)、(23.29±9.27)h。结论乳化蒸发-低温固化法制得的NRG固体脂质纳米粒,粒径小,包封率高,稳定性好,工艺简单。NRG固体脂质纳米粒肺部给药后有明显的缓释作用,能提高药物的生物利用度。     

洛莫司汀脂质体的制备及其在大鼠体内的药动学

 目的研究洛莫司汀(CCNU)脂质体的制备方法并考察用聚乙二醇单甲醚(2000)胆固醇琥珀酸酯(PEGCHS)修饰前后的2种脂质体静脉给药后在大鼠体内的药动学。方法用改良逆相蒸发法制备普通和PEGCHS修饰的CCNU脂质体,测定包封率和粒径,静脉注射给药后,以格列苯脲为内标,采用高效液相色谱法测定血液中的药物含量;并采用3P87药动学程序进行数据处理。结果制备的洛莫司汀脂质体包封率高(>80%),平均粒径50 nm左右;CCNU PBS溶液、CCNU脂质体和用PEGCHS修饰的CCNU脂质体的t_1/2α分别为0.061 8,0.093 1和0.153 1 h;t_1/2β分别为0.087 9,0.416 2和1.002 1 h;AUC分别为13.520 7,86.911 3和166.640 6 mg·h·L^-1。结论制备的CCNU脂质体包封率较高,粒径小;2种CCNU脂质体均可不同程度地增加CCNU的AUC,延长其在血液循环中的时间,并以用PEGCHS修饰的CCNU脂质体效果最好。     

重组水蛭素-2脂质体的制备及大鼠鼻腔给药药代动力学

目的：为了提高重组水蛭素-2(rHV2)鼻腔给药的生物利用度,研制rHV2脂质体并对其理化性质和大鼠经鼻给药后药代动力学特点进行研究。方法：以逆相蒸发法制备rHV2脂质体；通过研究rHV2脂质体的包封率、粒径、稳定性来考察其理化性质；将制备的rHV2脂质体鼻腔给予大鼠,用呈色肽法测定不同时间血浆中rHV2的浓度,通过3p87程序拟合药代动力学参数。结果：用该法制备的脂质体包封率约为76.95%,平均粒径为168.3 nm,分布在24～286 nm,相对峰宽±0.47,稳定性较好；药代动力学研究表明,rHV2脂质体较rHV2生理盐水溶液的鼻腔吸收明显增加。结论：将rHV2制备成脂质体可明显增加鼻腔给药的生物利用度。     

三七总皂苷脂质体的制备及其生理适应性的初步考察

目的:研究三七总皂苷(PNS)脂质体的制备方法并对其生理适应性进行初步考察.方法:以薄膜分散法制备PNS脂质体,采用析因设计确定最优处方;以蟾蜍上腭纤毛摆动频率和大鼠肺水肿指数以及肺组织病理改变作为指标考察PNS脂质体的生理适应性.结果:PNS脂质体为大单室脂质体(LUV),圆形或椭圆形,外形圆整光滑,形态分布均一.平均粒径为(1546.5±321.4)nm,符合肺部给药对制剂粒径的要求,包封率为(78.5±2.15)%;PNS脂质体应用于蟾蜍上腭黏膜后,黏膜纤毛摆动频率是PBS的92.14%,PNS脂质体组大鼠的肺水肿指数和肺组织病理改变均显著轻于PNS溶液组,接近PBS组.结论:PNS脂质体具有良好的生理适应性,具有良好的开发应用前景.     

姜黄素PLGA纳米粒的制备及其经鼻给药研究

目的:制备姜黄素聚乳酸羟基乙酸共聚物纳米粒(Cur-PLGA-NPs),鼻腔给药后考察其在大鼠体内的药动学行为并对其脑组织分布进行研究。方法:以PLGA为载体材料,采用改良的自乳化溶剂挥发法制备Cur-PLGA-NPs;透射电镜观察纳米粒的形态;激光粒度仪考察粒径;超速离心法测定其包封率及载药量;以姜黄素混悬液(Cur-Sol)为对照组,考察大鼠鼻腔给药Cur-PLGA-NPs的体内药动学过程,并测定其在大鼠脑组织的浓度。结果:纳米粒外观呈圆形或类圆形,平均粒径为(99.37±1.79)nm,包封率和载药量分别为(81.63±1.96)%和(4.55±0.15)%;体内药动学结果显示,Cur-Sol和Cur-PLGA-NPs的T1/2分别为(0.85±0.12)h和(1.72±0.44)h,AUC0-t分别为(224.59±22.44)μg·h·L~(-1)和(588.03±34.02)μg·h·L~(-1)。脑组织分布结果显示,Cur-Sol和Cur-PLGA-NPs的AUC0→t分别为(31.33±6.38)μg·h·g-1和(45.39±2.08)μg·h·g~(-1)。结论:Cur-PLGA-NPs经鼻腔给药后显著提高姜黄素体内和脑组织蓄积量并且延缓消除。     

紫杉素磁靶向脂质体的研制及其抗肿瘤作用的研究

 目的：制备紫杉素磁性脂质体，考察有关理化性质、在小鼠体内的分布及其抑瘤作用。方法：用逆相蒸发法制备紫杉素磁性脂质体，对其包封率、粒径和pH值等性质进行了研究，用高效液相色谱法测定了在兔体内的药动学参数，测定了其对小鼠EMT-6肿瘤的抑瘤率。结果：紫杉素磁性脂质体包封率为97.25%,平均粒径为526 nm, pH值为6.20。结论：制备得到的紫杉素磁性脂质体适宜于非胃肠道给药，且具有明显的抑瘤作用。     

延胡索乙素多囊脂质体的制备及其大鼠体内药代动力学分析

目的:制备延胡索乙素多囊脂质体,考察其体外释放情况和在大鼠体内的药代动力学特性。方法:采用HPLC测定延胡索乙素血药浓度,流动相甲醇-(KH2PO4-NaOH缓冲盐,pH 6.0)(45∶55),流速0.9 mL·min-1,检测波长280 nm。利用复乳法制备延胡索乙素多囊脂质体,考察其形状、粒径及体外释放特性,以延胡索乙素注射剂为参比制剂进行大鼠肌内注射的药动学研究。结果:延胡索乙素多囊脂质体粒径均一,80%分布在15.0~30.0μm,包封率88.47%,72 h体外累积释放率82.3%。延胡索乙素注射剂和多囊脂质体经肌内注射给药后,t1/2分别为(3.09±0.37),(33.97±4.78)h,Cmax分别为(289.05±30.37),(68.34±8.72)μg·L-1,Tmax分别为(0.93±0.15),(3.92±0.43)h,均存在显著性差异。结论:复乳法制备的延胡索乙素多囊脂质体的工艺可行且重复性好,在大鼠肌内注射后缓释效果良好。     

mPEG-DSPE修饰的紫杉醇脂质体的制备及其药动学研究

 目的采用甲氧基聚乙二醇磷脂酰乙醇胺(mPEG-DSPE)修饰紫杉醇脂质体,并考察其在大鼠体内的药动学行为。方法合成两亲线型聚合物mPEG-DSPE;采用薄膜分散法制备mPEG-DSPE修饰的紫杉醇脂质体;并用HPLC测定紫杉醇在大鼠体内的血药浓度。结果得到的紫杉醇脂质体粒径为(411.8±31.9)nm,包封率为(82.47±2.15)%。紫杉醇注射液和修饰后脂质体的t_1/2β分别为1.48和10.48h,后者AUC约为前者的3.13倍。结论mPEG-DSPE修饰的紫杉醇脂质体具有显著的长循环特性,并可提高其体内的利用度。     

微波消解-电感耦合等离子体质谱法测定脉络宁注射液中25种矿物质元素

目的建立微波消解-电感耦合等离子体质谱(ICP-MS)直接稀释测定脉络宁注射液中25种矿物质元素(Mg、Ca、Fe、Cu、Zn、Mn、Al、B、Ba、Co、Cr、K、Li、Mo、Na、Ni、P、Pb、Sr、Th、Ti、V、As、Cd和Hg)的方法。方法分别对微波消解条件和测试条件进行考察;样品经微波消解后,采用电感耦合质谱仪测定25种矿物质元素,并对测定方法学进行考察。结果确定最佳消解条件为3步缓慢升温:400 W 80℃升温10 min,保留5 min;600 W 120℃升温10 min,保留5 min;900 W 200℃升温20 min,保留20 min;25种矿物质元素在各自的线性范围内线性关系良好,r≥0.999 6,精密度、稳定性和重复性试验的RSD均符合定量分析要求;加标回收率为94.7%~106.1%,RSD在0.34%~2.79%。脉络宁注射液中检测出Mg、Ca、Fe、Cu、Zn、Mn、Al、B、Ba、Co、Cr、K、Li、Mo、Na、Ni、P、Pb、Sr、Th、Ti、V,未检出As、Cd和Hg。结论该方法简便、迅速、准确,适用于脉络宁注射液中25种矿物质元素的同时测定。     

Die Lateralität und Lateralitätsinstabilität in der Diagnostik und Therapie

The disturbance and instability of laterality are obstacles to diagnostics and therapy. Correction prior to starting therapy is required. They also predispose toward defined health problems and unspecific diseases. Numerous research activities provide evidence of the relevance of undisturbed laterality in diagnostics and therapy. Techniques of testing and therapeutic corrections will allow for optimized therapy success.     

Journal of Acupuncture and Tuina Science Instructions for Authors

The Journal of Acupuncture and Tuina Science, a journal with an international scope （IS SN 1672-3597, CN 31-1908/R, Bimonthly）, is embodied by ＇Springer Verlag＇ Database, Index Copernicus （IC） and Chinese Scientific and Technical Paper and Citations Data （CSTPCD）. You can search full text on http：//www, springerlink, com/content/1672 -3597.     

Yerba Mate or Paraguay Tea

正Beverages based on Ilex paraguariensis A.St.-Hil.are used in the south Brazil and other Latin American countries located at the so-called southern cone.It is known as chimarro or mate in south and southeast Brazil,tererêin     

Ethnopharmacologic study of chinese rhubarb

This paper deals with an interdisciplinary study covering historic, botanical, phytochemical, pharmacological and clinical aspects of rhubarb and related species, to lay stress on the correlation between plant phylogeny, chemical constituents and purgative activity.

It was found that the official rhubarbs were exclusively restricted in the Sect. Palmata e.g. Rheum palmatum R. palmatum var. tanguticum R. officinale; the following criteria may serve as their standard, viz., the presence of sennoside derivatives and rhein, the occurrence of the reduced form of rhein and aloe-emodin, the leaves with any kind of palmate incision. Comprehensive multivariate analyses showed that there is a very close relationship between the leaf incision, existence of sennosides or rhein and purgative activity.     

Wirksamkeit der Akupunktur bei der Therapie von idiopathischen Schmeckstörungen: Eine randomisierte Placebo-kontrollierte Studie

Background

At present, the state-of-the-art medication in treating idiopathic taste disorder (gustatory dysfunction) is zinc. If zinc medication was unsuccessful, not tolerated or if it is contraindicated the persons affected can hardly be helped.

Objectives

In a randomized placebo-controlled clinical trial an attempt was made to determine the efficacy of acupuncture.

Methods

The treatment group was treated with acupuncture needles, the placebo group with an inactive acupuncture-laser. Endpoints of the study were changes in the taste test, the quality of life and the severity of symptoms of depression (BDI) as well as mood changes (ZMS). Satisfaction with the success of the respective therapy was also evaluated. Data were collected before and after therapy and again for the treatment group 10 weeks after completion of the treatment period.

Findings

Treatment with real acupuncture showed a significant improvement in gustatory function as well as a significant improvement in psychological symptoms. Greater satisfaction with the treatment results was evident in the treatment group. The treatment results of acupuncture remained stable over a period of ten weeks after completion of the treatment.

Conclusion

Acupuncture was effective in the therapy of idiopathic taste disorders and therefore it is an effective alternative when zinc medication is not tolerated or unsuccessful. But it is also suitable as a therapy of first choice. Acupuncture can be considered as an extension of the therapeutic spectrum in the difficult treatment of taste disorders.     

Veränderungen der Herzratenvariabilität (HRV) während Low Level Lasernadelakupunktur: Placebokontrollierte Studie an 19 herzgesunden Probanden

Background

Experimental and clinical studies postulate a neurobiological mechanism of acupuncture by modulating central pain systems, neurohormones and -transmitters. It seems to be quite likely that the autonomic nervous system (ANS) plays an important mediating role in this neuromodulation.

Aim

In measuring heart rate variability (HRV), as a non-invasive approach to the ANS-function, the object of this study was to monitor probable acupuncture-induced changes of autonomic balance. The innovative technology of laser-needle acupuncture offers for the first time a stimulation method which fulfils the demands on a placebo-controlled acupuncture trial not requiring controversial sham acupuncture.

Method

19 healthy voluntary subjects underwent 3 treatments in randomized sequence, consisting of placebo-, 1-point- (PC 6) and simultaneous 3-point- (PC 6, LR 3, SI 3) laser-needle-stimulation over 20 minutes. Before, during and after placebo-/verum laser-needle acupuncture, HRV-data for normalized HF(high frequency)- and LF(low frequency)-Power (nHF, nLF) and their quotient nLF/nHF obtained by power spectrum analysis (FFT), were measured and analyzed statistically at 5 different time points (ANOVA repeated measures, p < 0,05).

Results

During both verum applications, the 1-point- (PC 6) as well as the simultaneous 3-point- (PC 6, LR 3, SI 3) laser-needle stimulation, significant changes of the ANS-activity were found in comparison to the placebo application. The most significant modification of HRV was an increase of nHF (p < 0,05 (PC 6), p < 0,0001 (PC 6, LR 3, SI 3)) as an expression of growing vagal activity during acupuncture.

Conclusion

Laser-needle acupuncture causes in 1-point-stimulation (PC 6) as well as in simultaneous 3-point-stimulation (PC 6, LR 3, SI 3) significant changes in HRV in comparison to placebo application. HRV-monitoring seems to be a suitable approach in exploration of acupuncture-induced changes of ANS and could possibly be established in combination with laser needle acupuncture as a standard for further scientific and clinical acupuncture investigations which are greatly needed.     

瑞香科五属植物中酚性聚合物的结构特征、分布及药理活性研究进展

瑞香科植物广泛分布于世界热带和温带地区,其中多种植物可供药用。在对该科植物的研究中发现,黄酮类、木脂素和香豆素等酚性化合物的低聚体为其重要的特征性成分,药理活性主要表现在抗肿瘤、抗炎、抗氧化、抗菌和抗病毒等方面。对已发现的酚性聚合体的化学结构、植物来源及药理活性进行综述,为瑞香科植物今后的研究和开发利用提供参考。     

HPLC法同时测定沉香化滞丸中11种成分

目的采用HPLC梯度洗脱法同时测定沉香化滞丸中沉香四醇、柚皮苷、橙皮苷、新橙皮苷、和厚朴酚、大黄素、厚朴酚、木香烃内酯、去氢木香内酯、大黄酚、大黄素甲醚11种成分。方法采用Thermo Syncronis C18色谱柱(250 mm×4.6 mm,5μm),流动相为水-乙腈,梯度洗脱:0～10 min,20%乙腈;10～20 min,20%～40%乙腈;20～24 min,40%乙腈;24～26 min,40%～52%乙腈;26～30 min,52%乙腈;30～31 min,52%～90%乙腈;31～35 min,90%乙腈;35～40 min,90%～100%乙腈;40～43min,100%乙腈;43～45min,100%～20%乙腈;检测波长215nm,体积流量1.0m L/min,柱温30℃,进样量20μL。结果各成分在43 min内分离良好,沉香四醇、柚皮苷、橙皮苷、新橙皮苷、和厚朴酚、大黄素、厚朴酚、木香烃内酯、去氢木香内酯、大黄酚、大黄素甲醚的线性范围分别为1.4～13.6、10.0～200.0、31.5～315.0、1.0～120.1、1.8～50.6、0.93～10.1、1.8～30.0、0.2～40.3、1.8～18.1、1.7～25.0、0.45～10.70μg/mL;样品中各成分的平均回收率均在98.90%～100.87%;11种成分精密度RSD在0.55%～1.54%;供试品溶液在30 h内稳定性良好,RSD在0.75%～1.94%;重复性RSD在0.39%～1.73%。6批次样品中沉香四醇、柚皮苷、橙皮苷、新橙皮苷、和厚朴酚、大黄素、厚朴酚、木香烃内酯、去氢木香内酯、大黄酚、大黄素甲醚质量分数分别为92.0～201.0、511.5～9 033.0、5 475.0～12 635.5、54.5～5 095.5、192.0～2 137.5、117.0～391.5、106.5～1 281.5、13.0～136.5、93.5～199.0、177.0～1 207.0、33.5～251.5μg/g。结论本方法准确、快速、简便,重复性好,精密度高,适用于沉香化滞丸中多种活性成分的定量分析。