Effect of the structure of ginsenosides on the in vivo fate of their liposomes

To utilize the multiple functions and give full play of ginsenosides, a variety of ginsenosides with different structures were prepared into liposomes and evaluated for their effect on the stability, pharmacokinetics and tumor targeting capability of liposomes. The results showed that the position and number of glycosyl groups of ginsenosides have significant effect on the in vitro and in vivo properties of their liposomes. The pharmacokinetics of ginsenosides liposomes indicated that the C-3 su...     

新抗肿瘤药铂(Ⅱ),(Ⅳ)配合物的合成

The synthesis of sixteen new analogs of cis-platinum (CDDP) and seven known Pt analogs, as well as the antitumor activity of seven Pt analogs against solid sarcoma 180 are reported. The new congeners consist of Pt (Ⅱ) and Pt (Ⅳ) complexes containing primary amine ligands (eg· NH3, en, pren) with variable anionic ligands such as malonate and 2-substituted malonates. In the experimental antitumor activity tests, 7 new platinum complexes were given on days 1～7, 24 hours after implanted with 10⁶ cells of solid sarcoma 180 tumor and producedT/C (treated/control) value between 15～35% with less toxicity than the parent cisplatinum. The experimental data indicate that it is favorable to introduce certain hydrophilic groups into the platinum complexes, in the view of increasing their aqueous solubility and lowering their toxicity while retaining their effectiveness.     

Injections of muscimol into the median raphe nucleus produce hippocampal theta rhythm in the urethane anesthetized rat

It has previously been shown that serotonergic [5-hydroxytryptamine (5-HT)] neurons of the median raphe nucleus (MR) are critically involved in the control of the hippocampal electroencephalogram (EEG). Activation of MR 5-HT neurons desynchronizes the hippocampal EEG, whereas inhibition of MR 5-HT activity produces hippocampal theta rhythm. The MR contains an intrinsic population of gamma-aminobutyric acid (GABA) containing neurons that synapse on 5-HT cells of the MR. The present study examined the effects on the hippocampal EEG of injections of the GABA_A agonist muscimol hydrobromide into the MR. Low doses of muscimol (0.5 μg) produced hippocampal theta rhythm at a mean latency of 6.81 min and for a mean duration of 23.6 min. Higher doses (1.0 μg and 3.0 μg, respectively) produced theta at mean latencies of 2.24 min and 3.2 min and for mean durations of 31.84 min and 24.88 min. Injections of muscimol into regions adjacent to the MR generated theta at significantly longer latencies or were without effect. The present results indicate that MR injections of muscimol produce theta by inhibiting the activity of MR 5-HT neurons. It is concluded that MR GABAergic systems, via their influence on MR 5-HT cells, serve an important role in the control of the hippocampal EEG.     

Proceedings of Symposium on the Tenth Anniversary of Foundation of CJP/JCP Club (10th CJP-99)

U. S. has the most sophisticated and advanced medical technol ogy in the world, but it has a serious problem in making the delivery of the technology and services to its population. In fact, U. S. is the only developed country that does not have a universal, comprehensive health care insurance for its people on earth. Today, more than 40 million (or 15％) Americans are uniusured and another 29 million Americans are under insured. There is an inequality in the distribution of quality care services between social classes. There are a lot of frauds, corruption, and forgeries in both public and private insurance programs. The worst of all is the run-away, skyrocketing health care cost that has caused various earth-shaking changes in the U. S. health insurance system in particular and the U. S. health care system in general.     

Improvement of memory in mice and increase of hippocampal excitability in rats by ginsenoside Rg1′s metabolites ginsenoside Rh1 and protopanaxatriol

The aim of present study is to observe the effect of ginsenoside Rg1′s metabolites(primary metabolit ginsenoside Rh1 and end metabolite protopanaxatriol) on learning and memory function.we employed the step through test and electrophysiological study to investigate the effects of Rh1 and Ppt on learning and memory as well as hippocampal excitability.The behavioral study showed that both ginsenoside Rh1 and Ppt significantly ameliorated memory-impaired model induced by scopolamine in mice.Consistently,electrophysiological work revealed that Rh1 and Ppt as well as their precursor Rg1 all increased hippocampal excitability in the dentate gyrus of anesthetized rats.The metabolism of Rg1 in cerebrospinal fluid was detected by HPLC-MS,indicating that Rg1 could not convert into Rh1 or Ppt.These results demonstrated that both Rh1 and Ppt have similar effect on improving memory and hippocampal excitability,suggesting that the role of ginsenoside’s sugar moeties in biological activities is not as necessary as traditionally considered.     

Multi-dimensional visualization for the morphology of lubricant stearic acid particles and their distribution in tablets

The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insights to the relationship of the morphology and spatial distribution of stearic acid(SA) with the lubrication efficiency, as well as the resulting tablet property. Unmodified SA particles as flat sheet-like particles were firstly reprocessed by emulsification in hot water to obtain the reprocessed SA particles with spherical morphology. The three-dimensional(3 D) information of SA particles in tablets was detected by a quantitative and non-invasive 3 D structure elucidation technique, namely, synchrotron radiation X-ray micro-computed tomography(SR-μCT). SA particles in glipizide tablets prepared by using unmodified SA(GUT), reprocessed SA(GRT), as well as reference listed drug(RLD) of glipizide tablets were analyzed by SR-μCT. The results showed that the reprocessed SA with better flowability contributed to similarity of breaking forces between that of GRT and RLD. SA particles in GRT were very similar to those in RLD with uniform morphology and particle size, while SA particles in GUT were not evenly distributed. These findings not only demonstrated the feasibility of SR-μCT as a new method in revealing the morphology and spatial distribution of excipient in drug delivery system, but also deepened insights of solid dosage form design into a new scale by powder engineering.     

Human brain acctylcholincstcrasc showed similarity in continuous antigcnic determinants with electric organ acctylcholincstcrasc

<正> Acctylcholincsterasc (AChE, EC 3.1.1.7) was purified from human embryonic brain by affinitychromatography. The reduced and alkylated AChE was hydrolyzed by TPCK-trypsin and the hydrolysate wasscparated by reversed-phase HPLC. The profile of RP-HPLC separation showed about 60 peaks. The eluentswere collected into 22 peak-groups and their antigenic activities were assayed by ELISA with use of the rabbit     

再谈痔瘘围手术期的镇痛治疗

For the sake of probing into perioperative analgesic therapies of hemorrhoids and fistulas, 80 patients with hemorrhoids or fistulas were randomly divided into two groups:the applied group (40 cases) and the controlled group (40 cases).The combines perioperative analgesia was used in the applied group and the conventional analgesia in the controlled group. The analgesic conditions of the two groups were prospectively evaluated and clinically observed. The result showed that the analgesic effect in the former was much better than that in the latter (P≤0.O1). It is concluded that the combined perioperative analgesic therapy should be used in the treatment of hemorrhoids and fistulas。     

The Synthesis of Some 17-（2＇-Oxazolyl）-androsta-5,16-diene Deriva-tives as 17α-Hydroxylase／C17,20 -Lyase Inhibitors

Several 4‘- and 5‘-substituted 17-(2‘-oxazolyl)-androsta-5,16-diene derivatives were designed and synthesized as inhibitors of 17α-hydroxylase/C17,20 -Lyase (P45017α) for the treatment of prostatic cancer, the results of the preliminary pharmacological screening showed that compound 6c, i.e. 17-(2‘-oxazoly)-androsta-5,16-diene-3-ol was a strong inhibitor, comparable with that of the reference compound VN-85. The introduction ofmethyl or phenyl group at the 4‘ or 5‘ position of oxazole ring decreased the activity. The in vitro activities of 3- acetate 5a-c and 8 were lower than their 3-ol counterparts 6a-c and 9 as expected. The further pharmacological study of 6c is in progress.     

冠状血管内皮激素受体单一或选择性激活的功能性意义(英文)

The purpose of this review is to present evidence that the lumen of the coronary vascular endothelium is an important site of hormonal action. This review is based on work performed for the last eight years in our laboratories. To demonstrate that selective and exclusive activation or blockade of coronary luminal hormonal receptors is feasible, we have covalently bound to microbeads or large size dextrans (2000 kDa) several hormones or their receptor blockers. These large molecular complexes when administered intravascularly because of their size, remain confined to the blood vessel lumen. The cardiac effects of these large size complexes are identical to those induced by their small size counterparts. The hormones we have used are; adenosine, acetylcholine, bradykinin, substance P, testosterone, and vasopressin. Furthermore, we have also determined the endothelial mediators responsible for the cardiac effects of these hormones. These findings demonstrate that intravascular hormone receptors are indeed     

子宫中隔切除术后预防粘连方法探讨

目的 探讨子宫中隔并不孕患者宫腔镜术后不同处理方法预防宫腔粘连的效果.方法 55例子宫中隔并不孕患者行腹腔镜监护下宫腔镜子宫中隔切除术(TCRS),术后针对不同患者采用不同术后处理措施,包括宫腔放置与不放IUD,是否进行人工周期治疗,部分患者术后使用GnRH-a类药物治疗术后第1、3个月行宫腔镜检查随访,宫内放置IUD的患者;于术后第3个月取环.结果 54例患者术后进行宫腔镜检查随访,其中40例分别于术后第1、3个月完成了术后2次宫腔镜检查,另14例只完成一次检查.宫腔术后放环与否对术后宫腔形态影响无差异(P>0.05),术后使用人工周期治疗患者较未使用者子宫内膜厚,此两者术后第3个月宫腔镜检查发现宫底创面均已有内膜覆盖.使用GnRH-a类药物患者术后官腔形态满意.结论 TCRS术后宫腔放置IUD无助于预防术后粘连的发生;术后人工周期治疗应更个体化并有针对性的使用GnRH-a类药物治疗.术后及时进行宫腔镜检查随访可防止术后宫底新粘连的形成.     

欧洲药典适用性认证介绍

目的介绍欧洲药典适用性认证程序,为国内药品监管机构和原料药生产企业提供信息,促进我国原料药生产企业的国际化。方法通过查阅调研欧盟相关药品法规和与EDQM同行面对面的交流,详细了解欧洲药典适用性认证的组织机构和具体程序。结果与结论欧洲药典适用性认证程序在对原料药的质量控制有重要作用,加强了药典的监管力度,进一步保证了原料药的质量、安全性和有效性。     

住院患者精神用药情况调查分析

目的：了解目前住院精神患者的药物使用情况。方法：采用一日法调查西安市精神卫生中心403例住院精神患者诊断和治疗情况，并与上海市精神卫生中心2004年调查结果相比较。结果：①传统精神药物使用显著减少，新型精神药物使用占据首位；②抗精神病药物使用趋向小剂量化；③本组联用丙戊酸盐类药物显著增多；④我院精神药物使用情况与上海精神卫生中心比较有显著差异。结论：近年来精神药物使用情况已发生了显著变化，与新型精神药物疗效好，副作用少，患者依从性高有关。     

不同方法治疗慢性宫颈炎的疗效分析

目的慢性宫颈炎是妇科最常见的疾病之一,可引起盆腔脏器炎症,并且与宫颈癌的发生关系密切。本文诣在探讨不同方法在慢性宫颈炎中的疗效。方法回顾性分析新乡市中心医院收治的210例宫颈炎患者,采用药物保妇康栓、聚焦超声治疗及宫腔镜下宫颈电切术的临床效果进行统计分析。结果宫颈电切术治疗有效率为97.9%,明显高于另外两组,差异有统计学意义。结论宫腔镜下宫颈电切术治愈慢性宫颈炎,并且切除宫颈移行带,减少宫颈癌发生。     

槲皮素代谢产物定性检出条件研究

目的:研究给予大鼠槲皮素后血浆中代谢产物的定性检出条件。方法:给予大鼠槲皮素单体(100mg.kg-1)后腹腔静脉取血,血浆样品经2mol.L-1盐酸(甲醇-水溶液)水解,采用高效液相色谱法对血浆样品中代谢产物进行定性分析。结果:大鼠给药后3h内取血、血浆样品经盐酸水解处理4h,可稳定检测槲皮素和异鼠李素,样品在—20℃条件下贮存稳定。结论:血浆样品采集时间、盐酸水解时间及贮存方式等不同均可影响代谢产物的有效检出。     

片剂溶出度影响因素分析

目的:考察片剂溶出度的影响因素,提高片剂溶出度,从而提高产品质量。方法:通过实验,研究各种参数对片剂溶出度的影响,选择出最佳工艺条件,如改进处方、控制颗粒硬度和大小、控制压力等工艺参数,用于指导大型生产,提高片剂溶出度。结论:崩解剂及润滑剂的用量对片剂溶出度影响较大,颗粒的硬度及大小、粘合剂的温度,压片压力对片剂的溶出度亦有影响;片剂直径大小对片剂溶出度影响不大。     

甲泼尼龙佐治毛细支气管炎疗效观察

目的探讨甲泼尼龙与布地奈德治疗毛细支气管炎的疗效。方法将182例毛细支气管炎患儿随机分成三组,三组均采用综合治疗,A组62例用甲泼尼龙静脉滴注,B组60例雾化吸入布地奈德,C组60例用静滴氢化可的松,观察三组喘憋、哮鸣音消失和住院时间。结果A组喘憋、哮鸣音消失时间及住院时间均比B,C组缩短（P〈0.05）。结论甲泼尼龙静滴治疗毛细支气管炎有效、安全、方便,明显加快治愈过程,优于布地奈德与氢化可的松。     

新疆维吾尔自治区基层医院平均住院日调查分析

目的 通过对新疆维吾尔自治区14个县乡级医疗机构住院患者平均住院日及影响因素进行分析,为县乡级医疗机构进一步提高医疗管理质量提供依据.方法 将2009-2010年1504例县乡级医院住院患者平均住院天数,按性别、年龄、院别、付费方式、疾病分类进行描述性统计和秩和检验分析.结果 不同性别间及院别间平均住院日差异均有统计学意义(均P＜0.05),男性平均住院日为10.39 d,女性为8.69d,乡级医院为9.27d,县级医院为9.50 d.不同年龄间平均住院日差异有统计学意义(P＜0.05),小于15岁组、15 ～24岁组、25～44岁组、45 ～65岁组、大干65岁组平均住院日分别为8.10 d、7.66d、8.83 d、10.26 d和11.33 d.自费患者平均住院日为8.39 d,新农合组为9.10 d,商业保险组10.17 d,社会基本医疗保险患者则为11.08 d.不同疾病分类间平均住院日差异明显,妊娠类平均住院日最短,为6.73 d,而肿瘤患者则为14.26 d.结论 不同性别、不同年龄段、不同疾病分类及不同付费方式间平均住院日存在差异,县级医疗机构和乡级医疗机构住院患者平均住院日也存在差异.     

住院患者抗菌药物不合理使用分析

目的了解该院住院患者不合理使用抗菌药物情况。方法随机抽取2009年住院使用抗菌药物病历544份。依据《抗菌药物临床使用原则》等相关规定进行评价,统计、分析抗菌药物不合理使用现象。结果该院住院患者抗菌药物不合理使用率为31.8%,不合理现象主要表现有选药不当、高起点用药、用法用量不当等。结论该院住院患者抗菌药物不合理使用现象严重,医院应采取措施加强监管,促进抗菌药物合理使用。     

对天津市北辰医院医务人员药品不良反应认知度调查分析

药品不良反应(ADR)监测工作是对上市药品安全性的再评价,是公众安全合理用药的保障,是药品监督管理工作的重要组成部分。本中心对天津市北辰医院103名医务人员进行了药品不良反应相关知识认知度调查,并对调查结果进行统计分析,为相关部门的药品监管工作提供依据和参考。