不同碳链脂肪乳剂的临床应用

脂肪乳剂作为一种能通过静脉输注的营养要素，广泛应用于临床。最早是由瑞典科学家Wretilind在1961年成功使用大豆油、卵磷脂和甘油等物质首次制成脂肪乳剂，至今已安全使用40余年，相当数量的临床研究显示脂肪乳剂有很好的有效性和安全性。在国内，于20世纪80年代末期开始研制和生产脂肪乳剂，华瑞制药有限公司生产r脂肪乳剂经过近10a的临床应用，其性能已得到广泛证实。脂肪乳剂也由长链剂型(LCT)发展到现在的中长链剂型(MCT／LCT)，由于其代谢过程不同，理论上MCT/LCT比LCT更具优势。     

脂肪乳剂的临床应用

目的合理应用并减少与之有关的代谢性并发症。方法根据甘油三酯的碳原子数不同,分为长链、中链和短链甘油三酯。目前临床常用的有单纯LCT和MCT/LCT物理混合的脂肪乳剂。处于研究和临床试用阶段的还有结构脂肪乳、含ω-3的脂肪剂和含橄榄油的脂肪乳等制剂。结果脂肪乳剂可提供能量和必需脂肪酸、维持细胞结构和脂肪组织的恒定。结论不同链长和结构的甘油三酯,构成的脂肪乳剂的不同代谢特点,决定了它们在临床的选择应用。     

静滴脂肪乳剂的观察和护理

脂肪乳剂在人体内代谢不依赖胰岛素,不会引起葡萄糖代谢所引起的代谢紊乱,目前已趋向将脂肪乳剂作为能源物质应用,以替代部分葡萄糖,特别是患者处于应激状态,葡萄糖的利用受到限制的时候,脂肪乳剂更是理想的能源物质.乳肪乳剂除能供给机体较多的热能外,还能供给机体必需脂肪酸,以维持组织器官正常生理功能,调节胆固醇代谢,是长期完全依赖胃肠外营养治疗患者的一种必不可少的物质.为了安全有效地使用脂肪乳剂,根据临床应用经验结合有关文献,将脂肪乳剂的观察和护理报道如下.     

关于统计学符号使用的说明

脂肪乳剂在人体内代谢不依赖胰岛素．不会引起葡萄糖代谢所引起的代谢紊乱，目前已趋向将脂肪乳剂作为能源物质应用，以替代部分葡萄糖．特别是患者处于应激状态，葡萄糖的利用受到限制的时候．脂肪乳剂更是理想的能源物质。乳肪乳剂除能供给机体较多的热能外．还能供给机体必需脂肪酸．以维持组织器官正常生理功能，调节胆固醇代谢．是长期完全依赖胃肠外营养治疗患者的一种必不可少的物质。为了安全有效地使用脂肪乳剂，根据临床应用经验结合有关文献，将脂肪乳剂的观察和护理报道如下。     

含药脂肪乳剂的靶向作用研究进展

作为药物载体的脂肪乳剂由于其自身毒性小,能减小药物的毒性和副作用,增加药物疗效,并具有良好的靶向作用,从而在临床上逐渐得到应用。综述了含药脂肪乳剂作为被动靶向制剂和主动靶向制剂两方面的应用进展。     

脂肪乳剂的研究

脂肪乳剂是一种水包油性乳剂,其结构和代谢过程类似于乳糜微粒,能够提供能量,临床应用脂肪乳剂的意义在于提供必需脂肪酸和能量,维持细胞结构和人体脂肪组织的恒定.现对脂肪乳剂的发展和各类脂肪乳剂的情况等做一综述.     

脂肪乳剂治疗布比卡因心脏毒性的研究进展

 布比卡因是临床常用的长效酰胺类局部麻醉药,大剂量的布比卡因快速入血容易引起室性心律失常甚至心跳骤停,临床常规的复苏治疗成功率低。而临床作为静脉营养物质的脂肪乳剂却能逆转布比卡因心脏毒性,并在很多临床病例和动物实验中得到证实。目前研究的结果支持脂肪乳剂是通过“脂肪池”假说和改善心肌能量代谢来产生治疗作用的。进一步阐明脂肪乳剂逆转布比卡因心脏毒性的量效关系以及如何将脂肪乳剂的治疗和常规生命支持治疗结合起来,将为临床上布比卡因的应用提供更加可靠的安全保障。      

脂肪乳剂对重症肝炎患者血脂的影响

重症肝炎患者由于肝糖原含量减少，体内脂肪分解和脂肪酸氧化供能加强，对脂类的需要量增加。同时由于肝源性水解脂肪的酶类和脂肪水解激酶等的台成减少，脂肪水和脂肪酸氧化代谢的功能却降低。在临床上往往由于营养供能物质的不合理应用导致营养失衡，且由此又带来一系列并发症。当前重症肝炎患者的营养问题十分重要，脂肪乳剂是临     

依托咪酯脂肪乳剂致血压异常升高不良反应一例分析

<正>依托咪酯在临床麻醉中应用多年,过去以水作溶媒,其常见不良反应有注射痛、静脉炎、肌肉震颤、术后恶心呕吐、心律失常、抑制皮质功能及肝药酶活性和过敏反应等,经过改良后依托咪酯脂肪乳剂上市,上述部分不良反应发生率显著下降,但心律失常等不良反应发生率未见显著降低。依托咪酯脂肪乳剂作为全身麻醉诱导的常规用药,其对循环功能的影响轻微,且主要表现为循环抑制,笔者近期在临床工作中遇到依托咪酯脂肪乳剂引起血压、心率异常     

静脉滴注脂肪乳剂应注意的问题

脂肪乳剂在人体内代谢不依赖胰岛素，不会引起葡萄糖代谢所引起的代谢紊乱，目前已趋向将脂肪乳剂作为能源物质应用，以替代部分葡萄糖，特别是在病人处于应激状态，葡萄糖的利用受到限制的时候，脂肪乳剂更是理想的能源物质。脂肪乳剂除能供给机体较多的热能体，还能供给机体必需脂肪酸，以维持组织器官正常生理功能，调节胆固醇代谢，是长期完全依赖胃肠外营养治疗病人的一种必不可少的物质。其中10％的脂肪乳剂渗透压为288毫渗量，PH值为6．5左右，与血浆相似，因此可经周围静脉滴注，应用方便。我科自使用脂肪乳剂以来，除用为长期完全…     

载药脂肪乳注射液的研究进展

目的介绍载药脂肪乳注射液作为一种新型药物载体,在药学中的研究进展。方法参阅国内外相关文献29篇,进行分析、整理、归纳和总结。结果阐述了近几年来其制备材料和工艺、质量评价体系、临床应用范围的研究情况,并对未来的发展前景进行了综述。结论载药脂肪乳注射液具有较好的开发前景和临床应用价值。     

Preparation of Uniform-Sized Multiple Emulsions and Micro/Nano Particulates for Drug Delivery by Membrane Emulsification

Much attention has in recent years been paid to fine applications of drug delivery systems, such as multiple emulsions, micro/nano solid lipid and polymer particles (spheres or capsules). Precise control of particle size and size distribution is especially important in such fine applications. Membrane emulsification can be used to prepare uniform-sized multiple emulsions and micro/nano particulates for drug delivery. It is a promising technique because of the better control of size and size distribution, the mildness of the process, the low energy consumption, easy operation and simple equipment, and amendable for large scale production. This review describes the state of the art of membrane emulsification in the preparation of monodisperse multiple emulsions and micro/nano particulates for drug delivery in recent years. The principles, influence of process parameters, advantages and disadvantages, and applications in preparing different types of drug delivery systems are reviewed. It can be concluded that the membrane emulsification technique in preparing emulsion/particulate products for drug delivery will further expand in the near future in conjunction with more basic investigations on this technique.     

Effect of Injection Volume on the Pharmacokinetics of Oil Particles and Incorporated Menatetrenone after Intravenous Injection as O/W Lipid Emulsions in Rats

Oil-in-water lipid emulsions are promising drug carriers for lipophilic drugs, however, the pharmacokinetics after entering the circulation should be clarified at clinical injection volume in order to utilize them in a clinical situation. In the present study, the standard lipid emulsions, consisting of soybean oil, egg yolk phosphatides and menatetrenone with diameters of about 150nm, were prepared using a microfluidizer system. The pharmacokinetics of menatetrenone and the oil particles after intravenous injection as standard lipid emulsions at various injection volumes, from the clinical injection volume (0.1 ml/kg) to the experimental injection volume (3.0 ml/kg), were examined in rats.

The plasma concentrations of menatetrenone and the oil particles were similar after administration, showing that menatetrenone was not released even after entering the circulation. Menatetrenone was delivered to the liver and spleen at the clinical injection volume, and more menatetrenone was delivered to the liver at clinical injection volume compared with the experimental volume. Moreover, additional information on injection volume-dependency was also obtained from these findings. These results at various injection volumes suggested that the standard lipid emulsions can be utilized as a useful drug delivery system at the clinical injection volume, especially for liver and spleen targeting.     

新型复合脂肪乳在肠外营养中的应用

摘 要自20世纪60年代以来,肠外营养支持迅速发展,用于肠外营养的各种脂肪乳剂相继应用于临床。新型复合型（SMOF）脂肪乳而作为最新一代脂肪乳,集合了前代脂肪乳诸多优点,并优化了脂肪乳中脂肪酸的比例,为各种需要肠外营养的患者群体提供更为有效的营养支持。现有的研究证据表明,SMOF脂肪乳安全性及有效性优于被广泛使用的豆油脂肪乳,在婴幼儿及长期肠外营养的患者中具有更好的肝脏耐受性,在抗炎及抗氧化方面也发挥重要作用。本文就SMOF脂肪乳在肠外营养中的应用及研究进展进行综述。     

膜乳化技术在微粒给药系统中的应用

膜乳化技术可用于制备各种乳剂、微粒和脂质体等，制备过程能耗低，条件温和，设备简单，操作方便，有望实现扩大生产。本文综述了膜乳化过程、影响因素，及该技术在乳剂、微球、纳米粒等剂型制备中的应用。     

Disposition characteristics of emulsions and incorporated drugs after systemic or local injection

Lipid emulsions are useful tools for controlling the in vivo disposition of drugs and plasmid DNA. The dispositions of lipid emulsions are determined by their tissue interaction depending on the anatomical and physiological characteristics of each tissue and the physicochemical and biological properties of lipid emulsions. In addition, the retention of drugs is another issue, as too rapid a release of the drug would lead to failure of exerting its therapeutic potency. This review presents an overview about the disposition profiles and various physicochemical properties of lipid emulsions and incorporated drugs after systemic or local injection. Controlled biodistribution of lipid emulsions and incorporated drugs are also discussed.     

The delivery and antinociceptive effects of morphine and its ester prodrugs from lipid emulsions

Long-acting analgesia is critical for patients suffering from long-acting pain. The purpose of this study was to develop lipid emulsions as parenteral drug delivery systems for morphine and its ester prodrugs. Morphine prodrugs with various alkyl chain lengths, including morphine propionate (MPR), morphine enanthate (MEN), and morphine decanoate (MDE), were synthesized. The prodrugs were stable against chemical hydrolysis in an aqueous solution, but were quickly hydrolyzed to the parent drug when exposed to esterase and plasma. Lipid emulsions were prepared using phosphatidylethanolamine (PE) as an emulsifier, while squalene was used as an inner oil phase. Drug release was found to be a function of the drug/prodrug lipophilicity, with a lower release rate for more-lipophilic drug/prodrugs. The inclusion of morphine and its prodrugs into lipid emulsions retarded their release. Lipid emulsions, which incorporated cholesterol, generally exhibited a drug/prodrug release comparable to that of emulsions without co-emulsifiers. Pluronic F68 (PF68) further slowed down the release of morphine and its prodrugs from the emulsions. The antinociceptive activity through the parenteral administration of these emulsions was examined using a cold ethanol tail-flick study. Compared with an aqueous solution, a prolonged analgesic duration was detected after application of the drug/prodrug emulsions. Incorporation of co-emulsifiers such as PF68 and cholesterol further increased the duration of action. The combination of prodrug strategy and lipid emulsions may be practically useful for improving analgesic therapy with morphine.     

Therapeutic applications of lipid-coated microbubbles

Lipid-coated microbubbles represent a new class of agents with both diagnostic and therapeutic applications. Microbubbles have low density. Stabilization of microbubbles by lipid coatings creates low-density particles with unusual properties for diagnostic imaging and drug delivery. Perfluorocarbon (PFC) gases entrapped within lipid coatings make microbubbles that are sufficiently stable for circulation in the vasculature as blood pool agents. Microbubbles can be cavitated with ultrasound energy for site-specific local delivery of bioactive materials and for treatment of vascular thrombosis. The blood-brain barrier (BBB) can be reversibly opened without damaging the neurons using ultrasound applied across the intact skull to cavitate microbubbles within the cerebral microvasculature for delivery of both low and high molecular weight therapeutic compounds to the brain. The first lipid-coated PFC microbubble product is currently marketed for diagnostic ultrasound imaging. Clinical trials are currently in process for treatment of vascular thrombosis with ultrasound and lipid-coated PFC microbubbles (SonoLysis Therapy). Targeted microbubbles and acoustically active PFC nanoemulsions with specific ligands can be developed for detecting disease at the molecular level and targeted drug and gene delivery. Bioactive compounds can be incorporated into these carriers for site-specific delivery. Our aim is to cover the therapeutic applications of lipid-coated microbubbles and PFC emulsions in this review.     

脂质乳剂释药机制及其靶向性的研究进展

简要介绍了脂质乳剂释药机制、体内外试验方法及影响释药特性和靶向性的因素，如粒径、药物性质、表面修饰等研究进展。