14种氨基酸纸层析系统的最佳选取

本文基于信息论的基本原理,应用shannon方程,采用数值分类—信息量选取法、系统差值—信息量分类法以及类平均—信息量分类法,对14种氨基酸的15种纸层析系统进行了分类,从中选取了最佳系统组合,并结合实验的实际情况进行了分析,结果表明经三种方法选取后的最佳系统组合都能比较满意地解决问题。同时还对达三种分类法进行了初步评价。     

22种氨基酸的纸层析溶剂系统最佳组合选取方法的研究

本文利用“逐步组合法”在TRS-80微型电子计算机上对22种氨基酸的纸层析溶剂系统的最佳组合作出了成功的选取,共选出三组最佳溶剂系统组合,它们的系统号码分别为:7,4,2,1;7,9,4,2;21,17,4,2,其中每一组均能在任意两供试药物的Rf×100的差值大于或等于10的情况下达到该22种氨基酸的完全分离。本文也用“数值分类—信息量选取法”选取系统最佳组合,但未能获得成功的结果。     

22种氨基酸的纸层析溶剂系统最佳组合选取方法的研究

本文利用“逐步组合法”在TRS-80微型电子计算机上对22种氨基酸的纸层析溶剂系统的最佳组合作出了成功的选取,共选出三组最佳溶剂系统组合,它们的系统号码分别为:7,4,2,1;7,9,4,2;21,17,4,2,其中每一组均能在任意两供试药物的Rf×100的差值大于或等于10的情况下达到该22种氨基酸的完全分离。本文也用“数值分类—信息量选取法”选取系统最佳组合,但未能获得成功的结果。     

纸层析和薄层层析溶剂系统的最佳组合选取法

本文为电子计算机辅助纸层析和薄层层析溶剂系统最佳组合的选取提供了一种算法。针对供试药物和系统数目的多少提出了两种方法:逐步组合法和择优组合法。通过TRs-80微型电子计算机对26种食用染料和22种磺胺类药物的计算,取得满意结果,不仅克服了数值分类信息量选取法和系统差值信息量分类法的某些缺点,而且还能给出众多的、甚至所有可能的各种系统的最佳组合方案。此法也适于人工手算进行选取。     

纸层析和薄层层析溶剂系统的最佳组合选取法

本文为电子计算机辅助纸层析和薄层层析溶剂系统最佳组合的选取提供了一种算法。针对供试药物和系统数目的多少提出了两种方法:逐步组合法和择优组合法。通过TRs-80微型电子计算机对26种食用染料和22种磺胺类药物的计算,取得满意结果,不仅克服了数值分类信息量选取法和系统差值信息量分类法的某些缺点,而且还能给出众多的、甚至所有可能的各种系统的最佳组合方案。此法也适于人工手算进行选取。     

基于不同分类法对医院药库管理应用效果的应用研究

目的:探讨ABC分类法和排序分析法应用于医院药库管理工作的效果,提高药库工作效率.方法:2014年1～6月应用排序分析法管理我院药库应用HIS系统,2014年6～12月应用HIS系统,运用ABC分类法管理我院药库,比较两种分类法的应用效果.结果:ABC分类法在药库人员满意率、病人投诉率两方面显著优于排序分析法(P＜0.05);ABC分类法在月平均库存金额、库存周转天数两方面显著差于排序分析法(P＜0.05).结论:排序分析法整体效果更佳,但是由于应用难度较大,ABC分类法简洁、易于掌握,可作为医院药库管理的最佳方式.     

逐步组合法用于选取13种巴比妥类药物的最佳层析系统

薄层层析和纸层析法迄今在药物分析中仍占有重要地位,这方面的研究也较多。其中对供试物提供了很多溶剂系统,在众多的系统中,选取最佳系统和系统组合使供试物最大限度地得到分离、鉴别的方法,除国内外已提出的数值分类选取法(NT-I)、系统差值信息量     

信息量法评价川芎提取效果

目的对不同提取条件下川芎色谱指纹图谱的信息量进行比较,论证信息量评价方法的可行性.方法通过3种不同提取方法和不同溶剂分别对川芎进行提取.借助HPLC-DAD联用色谱进行检测.引入信息量理论量化指纹图谱.结果确定了川芎的最佳提取条件:用60%乙醇作为提取溶剂进行超声波提取.结论用信息量方法对川芎提取效果进行评价是可行的.     

ABC分类法在门诊西药房库存管理中的应用与实践

目的 观察ABC分类法在门诊西药房库存管理中的应用效果.方法 广东省人民医院门诊西药房从2020年6月在门诊西药房库存管理中采取ABC分类法进行管理,检索2020年1—5月(ABC分类法库存管理开展前)、2020年6—10月(ABC分类法库存管理开展后)两个阶段内医院药库管理系统中门诊西药房药品出入库数据,比较两个阶段...     

基于不同分类法对社区医院药库管理应用效果的研究

目的：分析经验管理法、ABC分类法和排序分析法在社区医院药库管理中的应用效果,寻找一种最适合社区医院药库管理的方法。方法：利用我院2013年6～12月使用经验管理法,2014年1～6月使用ABC分类法以及2014年6～12月使用排序分析法管理药库的数据,对应用效果进行满意度调查,对药库库存数据进行统计分析。结果：采用ABC分类法和排序分析法,可以使得药品供应状况改善,药品周转加快,药品覆盖改善,医生和病人的满意率提高。但药库管理人员对经验管理法的满意度最高;ABC分类法和排序分析法可以明显改善药库库存指标,使缺药率显著下降。结论：在社区医院的药品库存中,排序分析法可以使采购计划科学合理,保证医院药品的供应,库存量明显下降,加快药品周转,药库得到有效管理;但综合考虑社区医院人力的实际情况,推荐ABC分类法作为社区医院库存管理的最佳选择。     

不同粒径神经毒素-Ⅰ纳米粒大鼠鼻腔给药脑药动学研究

目的制备不同粒径甲基化聚乙二醇(methylated-polyethyleneglycol,Me-PEG)修饰的神经毒素-Ⅰ(neurotoxin,NT-Ⅰ)聚乳酸(polylactic acid,PLA)纳米粒(NT-Ⅰ-MePEG-PLA-NP,NT-Ⅰ-NP),并考察不同粒径NT-Ⅰ-NP大鼠鼻腔给药后脑药动学特征。方法以聚乙二醇单甲醚聚乳酸共聚物(MePEG-PLA)为纳米材料,采用复乳-溶剂挥发法制备NT-Ⅰ-NP。以尾静脉注射NT-Ⅰ-NP为对照组,4组不同粒径NT-Ⅰ-NP大鼠鼻腔给药,运用脑微透析取样技术分析NT-Ⅰ在大鼠中脑导水管周围灰质(periaqueductal gray,PAG)部位浓度的经时变化。结果不同粒径的NT-Ⅰ-NP呈圆形或类圆形,大小均匀。大鼠鼻腔给药后小于100nm的NT-Ⅰ-NP的AUC(0-t)分别是100～200、200～300和大于300nm NT-Ⅰ-NP的1.22、1.34、1.60倍(P<0.05),表明粒径小于100nm时NT-Ⅰ在脑靶部位的浓度明显高于其他粒径的纳米粒。结论纳米粒的粒径对NT-Ⅰ的脑内递送有着较为明显的影响,粒径小于100nm的NT-Ⅰ-NP可以明显增加NT-Ⅰ的脑内浓度,这一结果为研究适宜粒径的NP用于蛋白多肽类大分子药物入脑奠定了基础。     

血浆溶血磷脂酸和癌抗原125检测在卵巢癌早期诊断中的价值

目的探讨血浆溶血磷脂酸（LPA）和CA-125检测在卵巢癌早期诊断中的价值。方法选取2005年10月至2008年2月收治的卵巢癌患者50例为卵巢癌组,同时选取同期卵巢良性肿瘤患者44例（卵巢良性病组）,以及50例健康妇女作为健康对照组,全部病例均于术前采血且经病理诊断证实,分别检测各组血浆LPA和CA-125。结果血浆LPA水平在卵巢癌组中的均值及阳性率明显高于卵巢良性病组和健康对照组（P〈0．05）,血浆CA-125在卵巢癌组中的均值和阳性率与卵巢良性病组相比较差异无统计学意义（P〉0．05）,但两组均高于健康对照组（P〈0．05）;血浆LPA检测特异度明显高于血浆CA．125检测,早期卵巢癌的诊断中,两者联合检测的灵敏度为85．7％,优于单项检测（P〈0．01）;Ⅱ-Ⅳ期卵巢癌患者血浆LPA及CA-125阳性率及水平较Ⅰ期高（P〈0．01）;CA-125阳性率在卵巢癌各病理类型间比较差异有统计学意义（P〈0．05）。结论LPA是卵巢上皮性癌的诊断尤其是早期诊断的敏感生物学标记物,联合检测CA-125可提高卵巢癌的早期诊断率。     

乳腺癌患者CA-15-3、CEA临床应用价值探讨

目的探讨CA-15-3、CEA在乳腺癌患者中的应用价值。方法应用电化学发光技术对62例乳腺癌患者、22例乳腺良性疾病患者及20例正常对照者血清CA-15-3、CEA水平进行了检测并比较。结果CA-15-3、CEA水平在乳腺癌Ⅰ、Ⅱ、Ⅲ期与乳腺良性疾病组及正常对照组无显著性差异(P>0.05),但在乳腺癌临床分期中有逐渐升高趋势,在Ⅳ期乳腺癌中表达明显增高(P<0.05;P<0.01),在远处转移患者表达明显高于单纯淋巴结转移患者,有淋巴结转移患者表达明显高于无淋巴结转移患者(P均<0.01),在不同组织来源乳腺癌患者中表达无明显差异(P>0.05)。结论CA-15-3、CEA并非乳腺癌早期诊断的理想标志物,但其表达与肿瘤临床分期、淋巴结转移及远处转移密切相关,在预测乳腺癌转移、复发及监测疗效、判断预后等方面具有重要临床应用价值,在乳腺癌中表达无组织细胞特异性。     

Antihypertensive effect of a novel calcium antagonist, SD-3211, in experimental hypertensive rats.

The antihypertensive effect of SD-3211, a structurally novel type of nondihydropyridine calcium antagonist, was assessed using several types of experimental hypertensive rats. Oral administration of SD-3211 (10, 20, and 30 mg/kg) to conscious spontaneously hypertensive rats (SHR), deoxycorticosterone acetate-salt hypertensive rats (DHR) and 2-kidney, 1-clip renal hypertensive rats (RHR) resulted in a dose-dependent decrease in systolic blood pressure (SBP). The hypotensive effect of SD-3211 in these hypertensive rats was more pronounced than in normotensive rats (NR). The potencies of SD-3211 for the hypotensive effect in the hypertensive rats and NR were 5-7 times greater than that of diltiazem but 2-3 times less than that of nicardipine. Furthermore, SD-3211 showed longer-lasting hypotensive action than diltiazem and nicardipine, at the respective equihypotensive dose. During the course of hypotension, SD-3211 did not exert any influence on heart rate (HR) in any type of hypertensive rats or NR, in contrast to the appearance of tachycardia with nicardipine in SHR, DHR, and NR and of bradycardia with diltiazem in DHR. At doses of 10 and 30 mg/kg, the hypotensive doses, SD-3211 elicited a dose-dependent natriuresis but no kaliuresis in SHR. In the chronic study using SHR, SD-3211 at 10 mg/kg/day showed an antihypertensive effect during an administration period of 12 consecutive weeks. These results allow us to conclude that SD-3211 has a potent and long-lasting hypotensive action with little cardiac effect.     

Enhancement of mite allergen-induced eosinophil infiltration in the murine airway and local cytokine/chemokine expression by Asian sand dust

Data on the effects of sand dust toward allergic asthma produced by indoor allergens, such as house dust mites, are not currently available. This study was undertaken to clarify the role of Asian sand dust on mite allergen, Dermatophagoides farinae (D. farinae)-induced eosinophilic inflammation in the murine lung, using sand dusts from the Maowusu Desert (Inner Mongolia) (SD-1) and the Tengger Desert (China) (SD-2). ICR mice were intratracheally administered saline; SD-1 alone; SD-2 alone; D. farinae alone; D. farinae + SD-1; and D. farinae + SD-2, 4 times at 2-wk intervals. The two sand dusts enhanced infiltration of eosinophil in the airway, along with goblet-cell proliferation related to D. farinae. The degree of eosinophil infiltration induced with SD-2 was greater than with SD-1. The SD-1, which contained higher amounts of beta-glucan, increased the expression of interferon (IFN)-gamma in bronchoalveolar lavage fluids (BALF) with or without D. farinae, but SD-2 did not. Synergistically or cumulatively elevated levels of interleukin (IL)-5, eotaxin, and monocyte chemotactic protein in BALF related to D. farinae were higher with D. farinae + SD-2 than with D. farinae + SD-1. These results suggest that increased cytokine and chemokines in BALF play an important role in the enhancement of eosinophil infiltration in the airway induced by D. farinae + sand dusts. The reduced eosinophil infiltration in the SD-1-treated mice could be due to suppression of Th-2 cytokine and eotaxin via interferon-gamma induced by microbial materials, such as beta-glucan.     

Electrophysiological properties of SD-3211, a novel putative Ca2+ antagonist, in isolated guinea pig and rabbit hearts.

The cardiac effects of SD-3211, a novel non-dihydropyridine type of Ca2+ antagonist, were examined in isolated guinea pig and rabbit hearts using an electrophysiological technique. SD-3211 (10(-6)-10(-5) M) shortened the action potential duration of guinea pig papillary muscles in a concentration-dependent manner without affecting the resting potential or the maximum upstroke velocity (Vmax). The Vmax of slow responses induced by high extracellular K+ and isoproterenol was inhibited by SD-3211 at concentrations of greater than 10(-6) M. Elevation of extracellular Ca2+ by 2 mM reversed this inhibited response. The inhibitory effect of SD-3211 on the slow response was enhanced as the stimulation frequency was increased. In Langendorff-perfused rabbit hearts electrically driven at 2.0 Hz, SD-3211 (10(-8)-10(-6) M) produced a concentration-dependent prolongation of the atrium-His bundle conduction time (A-H interval) as well as a reduction in the developed tension of ventricular muscle, whereas SD-3211 did not affect the His bundle-ventricular conduction time (H-V interval) significantly. The potency of SD-3211 in A-H prolongation was greater than those of diltiazem and bepridil, but weaker than those of nicardipine, nifedipine, and verapamil. The effect of SD-3211 on the A-H interval was more pronounced at higher stimulation frequencies. SD-3211 was intermediate between nicardipine and verapamil in its intensity of frequency-dependent effects on the A-H interval. These results suggest that SD-3211 has a preferential and frequency-dependent inhibitory action on cardiac slow Ca2+ channels.     

Tissue selectivity of the novel calcium antagonist sesamodil fumarate in isolated smooth muscles and cardiac muscles

The effects of the novel Ca2+ antagonist sesamodil fumarate (JAN), (+)-3,4-dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-[(3,4- methylenedioxy)phenoxy]ethyl]amino]propoxy]phenyl]-4-methyl-3-oxo-2H- 1,4-benzothiazine hydrogen fumarate (SD-3211), on isolated smooth muscles and cardiac muscles were investigated and compared with those of diltiazem, verapamil, nifedipine and nicardipine. Ca2+ antagonistic activity of SD-3211 (pA2 = 8.42) was more potent than that of diltiazem and verapamil, but less potent than that of nifedipine and nicardipine in isolated pig coronary artery. The inhibition of Ca2(+)-induced contraction by SD-3211 was not reversed by drug washout, whereas that by diltiazem was easily reversed by drug washout. SD-3211 produced a concentration-dependent relaxation (EC50 = 5.7 x 10(-8) mol/l) of KCl-contracted pig coronary artery. The order of potency of the various compounds correlated with their respective Ca2+ antagonistic activities. SD-3211 antagonized KCl-induced contraction, but not that induced by A23187, in the rabbit aorta. On the other hand, negative inotropic and chronotropic effects of SD-3211 on the guinea pig right atria approximated those of diltiazem and verapamil. These results suggest that SD-3211 exerts a potent and long-lasting Ca2+ antagonistic effect on isolated arteries, possessing pharmacological properties diverse from those of known Ca2+ antagonists with respect to tissue selectivity, i.e., it is more vasoselective than diltiazem and verapamil, and more cardioselective than nifedipine and nicardipine.     

ANTI-ISCHAEMIC AND VASOSPASMOLYTIC EFFECTS OF A NOVEL Ca2+ CHANNEL BLOCKER, SD-3211, IN VITRO

1. The present study was undertaken to determine the vasospasmolytic activity of a novel non-dihydropyridine type of Ca2+ channel blocker, SD-3211, in isolated canine coronary arteries and its ability to reduce myocardial ischaemic damage in isolated perfused rabbit hearts. 2. The vasospasmolytic effect of SD-3211 was investigated using 3,4-diaminopyridine-induced rhythmic contraction, in comparison with its enantiomer (SD-3212), nicardipine and diltiazem. SD-3211 was shown to reduce the peak tension and increase the contraction frequency. The order of potency for the relaxation of the peak tension was as follows: nicardipine greater than SD-3211 greater than diltiazem greater than SD-3212 and being compatible with that for the relaxant effects of these compounds on KCl-induced contraction in the same specimen. 3. Furthermore, the effect of SD-3211 on myocardial damage due to global ischaemia for 60 min followed by 60 min of reperfusion was examined. SD-3211 at a concentration of 2 X 10(-8) mol/L was given for 40 min before and again for 60 min after the ischaemia. SD-3211 attenuated the increase in leakage of creatine phosphokinase from the hearts and the decrease in pH of perfusate during reperfusion, while concomitantly providing a significant improvement in the post-ischaemic recovery of developed tension. 4. These results suggest that SD-3211 has properties to reduce coronary vasospasm and to provide protection against ischaemic damage, both of which may have beneficial actions in the treatment of ischaemic heart disease.     

Analgesic and other pharmacological activities of an enkephalin analogue,syndyphalin (SD)-25

The pharmacological actions of Tyr-D-Met(O)-Gly-MePheol (syndyphalin (SD)-25) were compared with those of morphine after systematic administration. The analgesic potency of SD-25 was about 4 times that of morphine when administered s.c. to rats. SD-25 did not exhibit any narcotic antagonist activity. Subcutaneous administration of SD-25 produced a dose-dependent suppression of morphine withdrawal signs in morphine-dependent rats, typical morphine-like jumping in the mouse jumping test, and an increase in spontaneous locomotor activity in mice. These activities were 2–5 times those of morphine. In the anaesthetized dog, intravenous administration of SD-25 produced a 100–1000 times stronger increase in the amplitude of contractions of the jejunum than did morphine, a weaker depression in respiration than morphine, and a slight increase in blood pressure. These effects were reversed by naloxone. These results indicate that SD-25 possesses potent central nervous system actions closely similar to those of morphine, but its effect on blood pressure and respiration was weaker than that of morphine.     

Hippocampal distribution of acetylcholine, muscarinic receptors and cyclic GMP

The regional distribution of acetylcholine (ACh), guanosine 3′,5′-monophosphate (cyclic GMP), ACh fractional rate constant, ACh turnover rate and [³H]-quinuclidinyl benzilate (QNB) binding were measured in various regions of the rat hippocampus. In coronal sections of the hippocampus, concentrations of both ACh and cyclic GMP were found to be the highest in sections at the amygdaloid end. Within subsectional areas of coronal sections of the hippocampus (CA-1, CA-3, and dentate gyrus). the cyclic GMP content and the affinity of [³H]-QNB specific binding sites were the highest in the CA-3 and dentate gyrus regions, while the density of [³H]-QNB specific binding was the highest in the CA-1 area. In contrast, the ACh turnover rate was higher in the CA-3 area than in dentate gyrus or CA-1 area. This study demonstrates that an increase of ACh utilization, [³H]-QNB binding sites and cyclic GMP content appears to occur in some specific areas of the hippocampus. These findings suggest that the dissection described in the present experiments is useful in the study of cholinergic regulation of cyclic GMP content of some regions of the hippocampus.