国产硫酸奈替米星注射液的药动学研究

采用微生物法对８名健康受试者单剂静脉滴注和肌注１００ｍｇ硫酸奈替米星注射液进行药动学研究，测定了给药后不同时间的血、尿药浓度，并经计算机程序计算药动学参数。结果显示：单剂静滴和肌注后的药动学符合二室开放模型，静滴药动学方程式为：Ｃ＝１０．８１２２ｅ－３．６７１４ｔ＋４．８８３１ｅ－０．２２０５ｔ；肌注药动学方程式为：Ｃ＝９．６８６８ｅ－１．４９１８ｔ＋５．４７５４ｅ－０．２０８６ｔ－１０．９７７０ｅ－３．７２５９ｔ。Ｔ１／２α分别为０．７４７８和０．４１２１ｈ，Ｔ１／２β分别为３．２３０８和２．８７４０ｈ，峰浓度分别为１３．１１和７．６０μｇ／ｍｌ，肌注后达峰时间为０．４８ｈ，总清除率分别为３．２２和３．２６（Ｌ／ｈ），２４ｈ肾排出率分别为５９．０６％和６８．５７％。给药后６ｈ内血药浓度及２４ｈ内尿药浓度＞１μｇ／ｍｌ，尿药浓度明显高于血药浓度。本研究结果与进口硫酸奈替米星注射液药动学过程基本一致。根据其药动学特征，建议一般给药方案为１００ｍｇ每日２次，可达到和维持有效血药浓度。     

诺氟沙星滴入兔眼与注入球结膜下其组织分布及药动学比较

用高效液相色谱法对诺氟沙星点眼与球结膜下注射后眼各组织药物浓度进行测定，比较两种给药途径的眼各组织浓度及其药物动力学参数。结果表明，诺氟沙星点眼与球结膜下注射后４ｈ，泪液诺氟沙星浓度分别为２．０８±０．１９与１６．０７±３．１４μｇ／ｍｌ（Ｐ＜０．０１）；角膜分别为０．７１±０．０７与１．６５±０．２４μｇ／ｇ（Ｐ＜０．０１）。泪液ＡＵＣ分别为９８．３３±７．３１与２７９．８２±３１．７ｈ·μｇ／ｍｌ；角膜ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ、Ｔ１／２Ｋｃ分别为１７．４２±１．２１ｈ·μｇ／ｇ、８．９４±０．８μｇ／ｇ、０．５７±０．０６ｈ、０．９１７±０．１６ｈ与２０．０１±１．０１ｈ·μｇ／ｇ、１０．０５±０．０７μｇ／ｇ、０．４５±０．０５ｈ、１．１５±０．２０ｈ；房水ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ分别为１．１３±０．２１ｈ·μｇ／ｍｌ、０．３９±０．０５μｇ／ｍｌ、０．６２±０．０９ｈ与１．７９±０．０７ｈ·μｇ／ｍｌ、１．００±０．１５μｇ／ｍｌ、０．４７±０．１０ｈ。诺氟沙星点眼与球结膜下注射两种给药途径的上述药动学参数有明显差异（Ｐ＜０．０５或０．０１）。     

对乙酰氨基酚凝胶在人体的药动学和生物利用度

８名健康男性志愿者交叉服用５００ｍｇ剂量的对乙酰氨基酚凝胶剂和片剂。血药浓度采用ＨＰＬＣ测定。对乙酰氨基酚凝胶剂的药动学参数：Ｔ１／２（Ｋａ）０．３０±０．２２ｈ，Ｔ１／２（Ｋｅ）２．１±０．４ｈ，Ｔｍａｘ１．０±０．４ｈ，Ｃｍａｘ５．１±１．５μｇ／ｍｌ，ＡＵＣ２１±５（μｇ／ｍｌ）·ｈ。这些参数与片剂的相似，凝胶剂相当于片剂的生物利用度为１０５．１％     

优喘平在人体内药物动力学及体内外相关性

以紫外分光光度法测定优喘平体外释放度，结果表明优喘平在各介质（ｐＨ１～８．４）释药量恒定；以荧光偏振免疫法测定血药浓度，６名志愿者单剂量口服４００ｍｇ·ｄ－１，Ｔｍａｘ１２．７±２．７６ｈ，Ｃｍａｘ３．８±０．９μｇ·ｍｌ－１，Ｔ１／２１１．８±６．２ｈ，ＡＵＣ６３．５±２９．３μｇ·ｈ·ｍｌ－１；多剂量口服４００ｍｇ·ｄ－１，显示间隔２４ｈ用药，茶碱血清浓度差异无显著性，可维持治疗血药浓度（５～１０μｇ·ｍｌ－１）；体外释药量与体内吸收量呈良好的相关性。     

进口和国产索他洛尔片剂的相对生物利用度研究

目的：本文对进口和国产索他洛尔片剂在１２名男性健康志愿者中的药物动力学和相对生物利用度进行了研究。方法：建立了一个检测血清中索他洛尔浓度的反相高效液相色谱－荧光检测法。结果：单剂量口服索他洛尔１６０ｍｇ后的血药浓度数据用３Ｐ８７药物动力学程序进行模型拟合，国产片剂ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ、Ｔ１／２分别为１６．２±３．６ｈ·μｇ·ｍｌ－１，１．２±０．２μｇ·ｍｌ－１，２．１±０．７ｈ，１７．０±７．２ｈ；进口片剂ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ、Ｔ１／２分别为１５．９±３．５ｈ·μｇ·ｍｌ－１，１．２±０．４μｇ·ｍｌ－１，２．１±０．６ｈ，１８．６±９．４ｈ。国产片剂的相对生物利用度为１０３．５％。结论：两种片剂的所有药动学参数经统计学（ＳＰＳＳ软件）处理差异均无显著性（Ｐ＞０．０５）。     

布洛芬混悬液人体生物利用度和药物动力学研究

用反相高效液相色谱法，血样甲醇沉淀蛋白后直接进样测定。１０名受试者随机分组自身交叉对照试验，单剂量口服布洛芬片或混悬液３００ｍｇ，布洛芬药时数据经３Ｐ８７程序拟合为一房室模型，其主要药动学参数，片剂和混悬液分别为：Ｋａ０．７２±０．１８ｈ－１，２．５０±０．８ｈ－１；Ｔ１／２ｋｅ２．０４±０．３２ｈ，２．２±０．５ｈ；ＡＵＣ０－∞１１１±２５ｍｇ·ｌ·ｈ－１，１１９±２８ｍｇ·ｌ·ｈ；Ｔｍａｘ２．８±０．６ｈ，０．９８±０．２３ｈ；Ｃｍａｘ１９．９±３．４μｇ·ｍｌ－１，２７．３±３．３μｇ·ｍｌ；相对生物利用度１０７．１６±８．１２％。     

氧氟沙星和环丙沙星在老年人中的药物动力学

对氧氟沙星和环丙沙星在老年和年轻健康志愿者中的药物动力学进行同期比较研究。上述两药全部血、尿浓度均以高效液相色谱法测定。老年组单剂口服氧氟沙星３００ｍｇ后的平均血清Ｔ＿（１／２β）为７．０８±０．８１ｈ，Ｃｌ＿ｒ为９５．９±２１．０ｍｌ／ｍｉｎ，ＡＵＣ为３２．６±４．１ｈ·ｍｇ／Ｌ，与年轻组相比，血清Ｔ＿（１／２β）延长，Ｃｌ＿ｒ降低以及ＡＵＣ增大。老年组与年轻组的Ｃ＿（ｍａｘ）则相近，分别为４．６７±０．９８和４．７２±０．５１ｍｇ／Ｌ。老年组每１２ｈ口服氧氟沙星３００ｍｇ连续７天后的Ｃ＿（ｍａｘ）和ＡＵＣ较单剂者明显增高。老年组和年轻组单剂口服环丙沙星５００ｍｇ后的Ｔ＿（１／２ｋｅｌ）分别为３．３２±０．４３和２．７６±０．４３ｈ，Ｃｌ＿ｒ分别为２３１．４±６８．８和２５６．９±６４．０ｍｌ／ｍｉｎ，ＡＵＣ分别为１７．７±４．９和１５．９±３．５ｈ·ｍｇ／Ｌ。根据本研究结果，对上述两药在治疗老年人感染时给药方案的调整提出了建议。     

阿莫维酸钾胶囊的相对生物利用度

１０名健康志愿者随机交叉口服等剂量阿莫维酸钾胶囊或安奇颗粒剂,采用微生物法分别测定阿莫西林和克拉维酸钾的血药浓度。单剂量空腹口服３１２．５ｍｇ的受试药与参比药后,阿莫西林的Ｔｍａｘ。分别为０．９８±０．２ｍ和０．６７±０．２４ｈ　,Ｃｍａｘ　３．９９±１．６２ｇ／ｍｌ和４．７１±１．４９ｇ／ｍｌ,ＡＵＣ０１０．１５±２．６１ｇ／（ｍｌ·ｈ）和９．５５±２．０３ｇ／（ｍｌ·ｈ）;克拉维酸钾的Ｔｍａｘ分别为０．８９±０．３１ｈ和０．６６±０．１３ｈ,Ｃｍａｘ。则为０．７６±０．２４ｇ／ｍｌ和０．９２±０．３３ｇ／ｍｌ,ＡＵＣ０为１．９４±０．５４ｇ／（ｍｌ·ｈ）和１．９４±０．５９ｇ／（ｍｌ·ｈ）。阿莫维酸钾胶囊的阿莫西林相对生物利用度为１０６．９％,克拉维酸钾的相对生物利用度为１０６．７％。结果表明,阿莫维酸钾胶囊与安奇颗粒剂的药动学参数相似,两者具有生物等效性。     

环丙沙星在健康人中药物动力学研究

本文对３０例健康男子口服环丙沙星胶囊后的药物动力学特性进行研究。受试者单剂量口服７５０ｍｇ胶囊，其血药浓度用ＨＰＬＣ离子对色谱，荧光检测器测定环丙沙星浓度。健康人口服环丙沙星的药物动力学特性显示一房室和二房室模型。其主要药动学参数：Ｔ１／２为３．６５±０．７８ｈ；Ｋａ为２．０７±０．９３１／ｈ；Ｖｄ２．０３±０．５６Ｌ／ｋｇ；Ｃｍａｘ４．９４±０．９７μｇ／ｍｌ；Ｔｍａｘ１．４６±０．３７ｈ；ＣＬＴ０．３９±０．０３Ｌ／ｈ·ｋｇ。     

克拉霉素两种制剂的生物等效性研究

采用微生物管碟检定法，以短小芽孢杆菌ＣＭＣＣ（Ｂ）６３２０２为检定菌，测定了１２名男性健康受试者口服克拉霉素（ＣＲＭ）胶囊（被试制剂）和片剂（标准对照制剂）后不同时刻血浆中活性药物的浓度，绘制了血药浓度－时间曲线。受试者交叉口服含ＣＲＭ５００ｍｇ的被试制剂和标准对照制剂后，血浆药物浓度达峰时间分别为１．３９±０．７４和１．１６±０．４１ｈ，血浆药物浓度峰值分别为２．５４±０．６２和２．７１±０．６１μｇ／ｍｌ，消除半衰期分别为４．５９±０．９９和４．７２±０．８５ｈ，用梯形法计算，ＡＵＣ０→∞分别为２１．７０±２．７１和２２．４２±３．５３ｈμｇ／ｍｌ。被试制剂中ＣＲＭ的相对生物利用度平均为（９９．３±１０．３）％，经统计学分析与对照制剂生物等效。两种制剂中ＣＲＭ的药动学过程均符合一室开放模型     

Therapeutic application of Carica papaya leaf extract in the management of human diseases

IntroductionPapaya (Carica papaya Linn.) belongs to the family Caricaceae and is well known for its therapeutic and nutritional properties all over the world. The different parts of the papaya plant have been used since ancient times for its therapeutic applications. Herein, we aimed to review the anticancer, anti-inflammatory, antidiabetic and antiviral activities of papaya leaf.MethodsAll information presented in this review article regarding the therapeutic application of Carica papaya leaf extract has been acquired by approaching various electronic databases, including Scopus, Google scholar, Web of science, and PubMed. The keywords Carica papaya, anticancer, anti-inflammatory, immunomodulatory, and phytochemicals were explored until December 2019.ResultsThe papaya plant, including fruit, leaf, seed, bark, latex, and their ingredients play a major role in the management of disease progression. Carica papaya leaf contains active components such as alkaloids, glycosides, tannins, saponins, and flavonoids, which are responsible for its medicinal activity. Additionally, the leaf juice of papaya increases the platelet counts in people suffering from dengue fever.ConclusionThe major findings revealed that papaya leaf extract has strong medicinal properties such as antibacterial, antiviral, antitumor, hypoglycaemic and anti-inflammatory activity. Furthermore, clinical trials are needed to explore the medicative potential of papaya leaf. Graphical abstractOpen in a separate windowGraphical abstract showing the medicinal properties of Carica papaya leaf     

环丙沙星治疗急性细菌性痢疾29例临床疗效观察

食源性急性菌例２９例中２８例大便培养为弗氏２ａ志贺氏菌。经２天吡哌酸加ＴＭＰ短程快速治疗，２９例无一例治愈。依据药敏试验改用环丙沙星治疗，其中１１例感染严重者先予静脉点滴，每１２小时２００ｍｇ，１￣２天，症状好转即改口服，每１２小时２５０ｍｇ。另１８例口服，疗程均为４天。用药后，平均退热时间１．３２天，大便次数恢复正常时间平均２．１０天，大便常规正常时间平均２．８６天，２８例大便培养阳性者，平均阴     

自由基对爪蟾卵母细胞表达的大白鼠脑皮层谷氨酸受体和5－羟色胺受体的作用

采用爪蟾卵母细胞和黄嘌呤氧化酶一次黄嘌呤反应系统研究了自由基对大白鼠脑皮层谷氨酸受体和５－羟色胺受体的作用。自由基抑制谷氨酸和５－羟色胺引起的去极化反应，但不影响膜的被动电学参数。自由基对受体的作用表现为去极化幅度下降及半衰退时间缩短；去极化的潜伏期和上升时间延长（Ｐ＜０．００１或Ｐ＜００１），说明白由基作用于移植到卵母细胞膜上的受体，抑制了谷氨酸和５－羟色胺引起的去极化反应。提示在本实验条件下，神经递质受体自由基作用的敏感性高于卵母细胞的质膜。此标本适于研究自由基对神经递质受体的作用。     

X钼靶及高频超声对乳腺微钙化灶的的诊断价值

目的:比较乳腺钼靶摄影与超声在乳腺微钙化灶诊断中的价值。方法:收集经X线钼靶摄影确诊伴微钙化灶的乳腺良恶性疾病患者178例,分析超声对乳腺微钙化的检出率,比较2者诊断的敏感性、特异性及准确性。同时比较2者良恶性病例伴有或不伴有包块的构成比,分析包块对微钙化发现的意义。结果:乳腺微钙化的超声检出率为44.94%,其中乳腺病灶恶性病变的微钙化检出率为80%,良性病变的钙化检出率为34.78%。超声诊断乳腺微钙化病例的敏感性、特异性及准确性分别为96.8%、66.7%、63.5%,X线钼靶摄影诊断乳腺微钙化病例的敏感性、特异性及准确性分别为97.5%、89.%8、87.3%;钙化伴有包块的构成比超声检查结果达71.2%,较钼靶检查结果的47.8%高。结论:钼靶摄影对乳腺微钙化的发现及良恶性的判断价值较超声高。     

天麻3个不同变型遗传关系的SRAP分析

目的 从分子水平上分析对比天麻的3个不同变型,探索其种内变异,为资源保护和良种选育奠定基础.方法 采用SRAP分子标记分析天麻3个不同变型的遗传关系.结果 筛选出7对SRAP引物,用PCR扩增11批天麻样品,得到145条清晰的带,其中110条具有多态性,多态百分率为75.86％;通过Nei&Li遗传相似系数(GS)计算,11批天麻的种质两两间的相似系数分布在0.36 ～ 0.93;UPGMA聚类分析将乌天麻聚为一类,红天麻与绿天麻聚为一类.结论 天麻的3个不同变型中,绿天麻和红天麻的亲缘关系较近,而乌天麻与前两者的遗传差异较大,亲缘关系较远.     

环丙沙星与氧氟沙星注射液治疗细菌性感染的疗效观察

以乳酸环丙沙星（ＣＰＬＸ）注射液和氧氟沙星（ＯＦＬＸ）注射液随机分组治疗各种细菌性感染４０例及４２例，并以注射用头孢噻肟钠（ＣＴＸ）治疗４９例作对照。三组平均年龄、体重、疗程及病情程度相比无显著性差异，具可比性。病种分布以消化道感染最多，共８１例，占总数的６１．８％。三组１３１例病人细菌阳性率为９４．７％。一疗程ＣＰＬＸ组、ＯＦＬＸ组、ＣＴＸ组治愈率分别为８７．２％、８３．３％、７１．４％，有效率     

Effects of steroids on beta-adrenergic binding sites in sheep pineal glands

As an initial step in investigations of putative differences between central nervous system light-sensitive mechanisms in seasonally shedding and non-shedding breeds of sheep, some beta-adrenoceptor characteristics of Merino sheep pineal glands were determined, using [3H]dihydroalprenolol as the labelled ligand. Overall, a dissociation constant of 17.2 +/- 2.6 nmoles/l and a daytime beta-receptor density of 1.6 +/- 0.3 pmoles/mg were determined at 37 degrees. The binding sites exhibited stereospecificity, saturability and apparent homogeneity. 17 beta-Estradiol and progesterone implants that provided hormone concentrations in the physiological range had no significant effect on pineal beta-receptors in male sheep castrated shortly after birth. Dexamethasone injections, on the other hand, in doses sufficient to loosen the attachment of wool fibres to the skin, resulted in decreased pineal beta-receptor density and increased receptor affinity for dihydroalprenolol. This effect was apparently not mediated by altered plasma catecholamine concentrations, since the glucocorticoid treatment did not affect jugular venous noradrenaline, adrenaline or dopamine levels. The possible involvement of glucocorticoids in the regulation of wool growth could thus have a central neuronal component, medicated via action on pineal beta-adrenoceptors in sheep; however, the existence of the putative gonadal steroid feedback on beta-adrenoceptor-mediated pineal function remains to be demonstrated in this species.     

Changes in tissue cyclic AMP concentrations following an intravenous lethal dose of cholera enterotoxin in rabbits

The purpose of this study was to test the hypothesis that a generalized increase in tissue cAMP concentrations after an i.v. injection of cholera enterotoxin may play a role in the development of biochemical and pathological changes leading to death. Dutch rabbits were injected i.v. with highly purified cholera enterotoxin at a dose of 100 or 200 μg/kg. When death appeared imminent (20–30 hr after inoculation), rabbits were anesthetized; plasma, urine, and 13 different tissue samples were obtained for cAMP determinations. Enterotoxin (200 μg/kg) produced significant increases in cAMP concentrations in lung, spinal cord, skeletal muscle, renal cortex, renal medulla and liver, whereas a lower dose (100 μg/kg) had no effect on cAMP levels in any tissue. The elevation of cAMP values in selected tissues suggests differences in tissue sensitivity to cholera enterotoxin; the data fail to support in toto the proposed hypothesis.