紫杉醇新剂型的研究进展

紫杉醇是一种广谱、高效的抗肿瘤药物,但由于其水溶性差,临床上应用的注射剂加入聚氧乙烯蓖麻油以增加紫杉醇的水溶性,但聚氧乙烯蓖麻油在体内会产生严重的毒副作用.为了解决紫杉醇注射剂中聚氧乙烯蓖麻油的毒性问题,开发紫杉醇新剂型是近年来新药研发的热点之一.该文综述了近年来研发的一些紫杉醇新剂型,如乳剂、胶束、环糊精包合物、脂质体、微球、纳米粒和药物释放支架等,并对其可行性进行了分析.     

环取代8-氨基喹啉类抗疟药研究进展

1891年Ehrlich等发现亚甲蓝对间日疟有一定抑制作用,进而用碱性的二烷基氨基取代其环外的一个甲基,抗疟作用明显增强,从而确定碱性侧链在抗疟作用上的意义。为了寻找更理想的抗疟药,研究者将类似的碱性氨基侧链接到喹啉环的8-位氨基上,导致了扑疟喹的问世。间日疟是四种人疟中发病率极高、地域分布最广的一种,未经根治的间日疟患者即为继续传播的传染源。因为奎宁等药物都是     

青蒿素类抗疟药研究进展

青蒿素类抗疟药研究进展陈扬朱世民陈洪渊（南京大学化学化工学院配位化学国家重点实验室，南京２１００９３）疟疾仍然是危害严重的世界性流行病。据１９９６年世界卫生组织报告［１］，全球十大流行病中，每年疟疾患者达５亿人，在热带、亚热带地区死于疟疾者有２７０...     

抗疟药物的研究进展

报告青蒿素及其衍生物，ＬｉｃｏｃｈａｌｏｎｅＡ，铁鳖合剂，ＷＲ２４３２５１，利福平等抗疟药物研究进展。     

三氧化二砷新剂型的研究进展

三氧化二砷是急性早幼粒细胞白血病的一线用药,对多种实体瘤也具有抑制作用。然而,三氧化二砷肾脏清除速率快,无组织特异性分布,靶向性较差,易产生心、肝和肾等毒性作用,限制了其在实体瘤的临床应用。近年来,科学家开发大量三氧化二砷新剂型以提高其疗效,降低其不良反应,包括脂质体、微球、纳米粒、乳剂和悬浮剂等。本文对三氧化二砷的新剂型研究进展进行梳理,以期为三氧化二砷新剂型的合理开发和应用提供新思路。     

抗疟药在苏丹疟疾发病区的合理应用

目前疟疾在我国已属少见 ,但在非洲国家仍很普遍。在苏丹几乎无人不被感染 ,婴幼儿感染也很多 ,恶性疟疾感染最多 ,亦有不少脑性疟。笔者在苏丹医疗队援外工作 5年 ,接触了 5 0 0余病例 ,现就几种主要国产、进口抗疟药在疟疾发病区的临床应用进行了探讨。1　氯喹 ( chloroquine)临床一般用其磷酸盐 ,硫酸盐及二磷酸盐很少用 ,有注射剂、片剂和糖浆剂 ,该药为应用时间最长 ,疗效确切的抗疟药。主要作用于红内期 ,通过干扰疟原虫裂殖体 DNA复制与转录过程或阻碍其内吞作用 ,使虫体缺乏氨基酸而死亡。主要用于治疗恶性疟 ,控制症状发作及症状…     

抗疟药在非洲使用情况的门诊处方分析

目的:了解门诊疟疾患者用药基本情况,为合理用药提供参考。方法:对2010年8月—2011年3月非洲驻地门诊收治疟疾患者的处方进行统计分析。结果:非洲全年任何月份均有疟疾传播,抗疟药用药量雨季大于旱季;287张疟疾患者门诊处方中,用量排序前3位的抗疟药为双氢青蒿素哌喹片(113张,占39.37%)、蒿甲醚注射剂(65张,占22.65%)、注射用青蒿琥酯(46张,占16.03%)。结论:青蒿素类药是治疗疟疾安全、有效的首选药物;赴非洲工作的医务人员应该充分了解各种抗疟药,依据其作用机制和不同特点,采用最佳治疗方案,以促进临床合理用药。     

姜黄素剂型研究进展

目的阐述姜黄素剂型研究的进展。方法围绕姜黄素的溶解性及其体内行为的改善,对其剂型的研究概况进行综述。结果通过对姜黄素各种剂型进行的实验,结果表明,均能在一定程度上提高姜黄素的溶解度和生物利用度。结论姜黄素是天然来源的药物,鉴于其广泛的药理作用,改善姜黄素的溶解度及其生物利用度对改善其体内的吸收有着重要意义。     

我国药物新剂型研究进展

随着药剂学发展突飞猛进,对药物新剂型和新技术的研究与应用也日益广泛、深入。通过查阅2012年我国学者在国内外期刊上发表的相关论文,分类概述我国在纳米制剂、微球、亚微乳、复合物、纳米晶体、立方液晶和碳纳米管等药物新剂型方面的研究进展。     

Changing the pill: developments toward the promise of an ultra-long-acting gastroretentive dosage form

ABSTRACT

Introduction: The development of oral sustained release dosage forms has been a longstanding goal due to the potential for ease of administration, improved pharmacokinetics, reduced dosing frequency, and improved adherence. The benefits of multiday single-dose drug delivery are evident in the success and patient adoption of injected and implanted dosage forms. However, in the space of oral medications, all current commercially available gastric resident dosage forms, and most in development, are limited to gastric residence of less than 1 day.

Areas covered: Reviews of systems to extend gastric residence reveal that 1 day or more residence has been an unmet challenge. New dosage forms are in development that seek to address many of the key physiological and design challenges of long-term gastric retention beyond 24 h and up to a week or longer. The present analysis highlights the design, material considerations and implications of unfolding dosage form systems with ultra-long-term gastric residence.

Expert opinion: The development of oral dosage forms providing sustained release of high potency medications over days or weeks could transform care, significantly decrease patient burden in chronic disease management and improve outcomes.     

Antimalarial Activity of the Novel Quinoline/6‐Thiopurine Conjugate in Gallus gallus Linnaeus,Infected Experimentally by Plasmodium (Novyella) juxtanucleare

This study aimed to evaluate the 4‐(6′‐thiopurine)‐7‐chloroquinoline, a novel quinoline/6‐thiopurine conjugate, for the treatment of Gallus gallus experimentally infected with Plasmodium juxtanucleare, an avian malaria agent. The avian group treated with 4‐(6′‐thiopurine)‐7‐chloroquinoline showed a significative parasite clearance and maintained a low level of parasitaemia, when compared with the untreated control group and to the chloroquine treated avian group.     

咪康唑乳膏与咪康唑乳膏加散剂治疗足癣疗效对比

目的 :比较咪康唑乳膏和咪康唑乳膏加散剂治疗足癣疗效和安全性。方法 :足癣病人 60例随机分成 2组。咪康唑乳膏加散剂组 3 0例 [男性 2 4例 ,女性 6例 ,年龄 (4 3±s1 4)a];咪康唑乳膏组 3 0例 [男性 2 3例 ,女性 7例 ,年龄 (4 4± 1 3 )a]。分别用咪康唑乳膏或咪康唑乳膏加散剂涂于患部 ,每日 2次 ,疗程 4wk。结果 :咪康唑乳膏加散剂和咪康唑乳膏治疗足癣 ,总痊愈率分别为 73 %和 5 7% ,总有效率分别为 97%和 90 % ,真菌消除率分别为 97%和90 %。 2组的临床疗效和真菌学疗效 ,差异无显著意义 (P >0 .0 5 )。 2组的不良反应发生率分别为 0和 3 %。结论 :咪康唑乳膏加散剂和咪康唑乳膏治疗足癣有相似疗效及安全性     

Absorption and urinary excretion of clindamycin palmitate in the elderly

Summary

Clindamycin palmitate hydrochloride is a water-soluble salt which in vivo undergoes hydrolysis into the active base. Following a single-dose administration of either 150 or 300mg. of the drug to elderly patients, serial blood sample estimations revealed that satisfactory therapeutic plasma levels were achieved and maintained in all patients with peak levels usually occurring at 2 hours and with a serum half-life of over 4 hours. The rate of urinary excretion was variable but, irrespective of dose, about 7% of the drug was recoverable from the urine in an active form during the following 24 hours. This study shows that clindamycin palmitate in suspension form provides an effective method of administering the antibiotic to elderly patients who may find difficulty in swallowing clindamycin in capsule form and suggests that 150?mg. every 8 hours comprises effective treatment.     

Artemisinin drugs: novel antimalarial agents

Artemisinin and its derivatives, artesunate and artemether, represent a new class of antimicrobial drug with potent activity against Plasmodium falciparum. Although they show excellent efficacy in both severe and uncomplicated malaria, dosage regimens still need to be optimised and pharmacokinetic profiles defined. In the treatment of uncomplicated malaria, the artemisinin drugs should be used in combination with a long acting antimalarial to protect both drugs against the emergence of resistance. In the treatment of severe malaria, parenteral artemether is at least as effective as quinine and is simpler to use. The use of rectal preparations of artesunate and artemisinin at the rural health level will facilitate early initiation of the treatment of falciparum malaria and this may reduce the proportion of patients progressing to severe disease. All of the artemisinin drugs have comparable efficacy; the choice of derivative should be based upon availability, cost and quality of the preparation. Artemisinin, artesunate and artemether are well-tolerated in both adults and children, with no evidence to date of serious clinical toxicity.     

Pharmacokinetic analysis of sustained-release dosage forms of theophylline in humans: comparison of single and multiple dose studies

A pharmacokinetic analysis of two sustained-release dosage forms of theophylline (Theo-Dur and Theotrim) was carried out following single and multiple dose administrations of the two formulations in five healthy subjects. Despite the prolonged absorption after administration of the two sustained-release formulations, theoretical predictions of theophylline steady-state levels following multiple dosages based upon data obtained from the single dose study, correlated with the data of the multiple dose study. This study shows that the recommended dose and dosage regimen of new sustained-release formulations of theophylline can be based upon single dose studies. In the population studied, repetitive doses of 450 mg b.i.d. of Theo-Dur and Theotrim maintain steady-state concentrations of theophylline within the drug's therapeutic window.     

口服胰岛素制剂的研究进展

综述了近年来国内外口服胰岛素制剂的研究现状 .     

青蒿素哌喹片治疗无并发症恶性疟的剂量探索试验

目的探索青蒿素哌喹片治疗无并发症恶性疟的安全有效的适宜剂量。方法收治7～65岁男性和女性病人共100例,按区组随机化方案分成2组,成人总量1400 mg组年龄(22±s12)岁,1750 mg组年龄(21±12)岁。分别于0h和24h给药一次,比较2组的平均原虫转阴和退热时间、28d治愈率及原虫复燃率。结果2组的平均原虫转阴时间分别是(61±19)h和(57±21)h,平均退热时间为(20±15)h和(18±10)h,P>0.05;28 d治愈率是80%和96%,原虫复燃率为20%和4%,总量1750 mg组显著优于1400 mg组(P<0.05)。2组耐受性均良好,未发现明显的不良反应。结论推荐青蒿素哌喹片的临床治疗剂量为总量1750 mg,每日1次,分2d服完为1个疗程。     

固体制剂工艺对药物晶型的影响

综述了固体制剂加工生产各因素对药物晶型的影响。指出精制、粉碎、制粒、干燥和压片都可能引起药物晶型发生变化,从而影响药物的生物利用度和治疗的有效性。     

Pharmacokinetic evaluation of novel sustained-release dosage forms of valproic acid in humans

Five new sustained-release dosage forms of valproic acid (VPA) were developed. The new sustained-release formulations were administered to six healthy subjects for comparison with a standard tablet and an i.v. preparation of the drug. Three of the formulations exhibited a more prolonged and uniform absorption rate and yielded more sustained serum levels after ingestion. These three formulations maintained serum therapeutic levels of VPA for 24 h after a single oral administration of 1 g, and were bioequivalent to a marketed standard tablet of VPA. The absorption profile of the various oral formulations was analysed pharmacokinetically, using the Loo-Riegelman procedure.