国内口腔黏膜粘附给药剂型的研究进展

口腔黏膜粘附给药系统利用有粘附性的高分子聚合物与口腔黏膜产生粘附作用，延长药物在口腔中的滞留时间，控制药物的释放速度和释药量，发挥局部或全身治疗作用。近年来国内口腔黏膜粘附给药系统的剂型有口腔贴膜剂、片剂、口腔粘附凝胶剂、喷雾剂、含袋等多种，给药方式独特，药物吸收利用充分，有着广阔的发展前景。     

凝胶剂的研究进展及应用概况

凝胶剂是近年来兴起的一种药物新剂型,国外的研究较早、发展较快。国内发展从医院制剂起步,现已有多种凝胶剂获国家批文,展现出凝胶剂更多的优势效用。凝胶剂按基质类型分为亲水性凝胶、亲脂性凝胶和乳剂型凝胶,亲水性凝胶的基质材料目前采用得最多,常见的有卡波姆、壳聚糖、海藻酸钙、羧甲基纤维素钠等。凝胶剂较常采用的给药途径是经皮给药、经口给药、眼部给药、鼻腔给药、阴道给药和直肠给药,不同的给药途径均能收到药物浓度高、作用时间持续的满意效果。随着新技术的应用,还研发出了环境敏感性凝胶、脂质体凝胶、β-环糊精包合物凝胶等新产品,提高了临床疗效。凝胶剂的应用范围还将不断拓宽,前景十分广阔。我国药学研究工作者应在发展化学药凝胶剂的同时,促进中药凝胶剂的发展,将祖国传统医药的精髓发扬光大。     

两种扩散池在透皮实验中的应用

经典的药物给药方式以口服给药、血管内给药为主，皮肤给药只是用于治疗皮肤局部的病变及炎症、烧伤、烫伤、冻伤以及局部的皮肤黏膜的保护，其靶组织为皮肤、黏膜，而不是透过皮肤来发挥全身治疗作用。近10年来应用皮肤给药达到全身治疗作用的新剂型不断出现，皮肤作为一个新的药物全身治疗给药途径逐渐受到重视，除了传统的软膏剂、硬膏剂外，日前外用凝胶剂、贮库型经皮给药系统(TTS)、离子导入制剂也正在兴起，有关药物透皮吸收的实验研究也不断增多，实验技术及手段不断完善，为研究皮肤用药的吸收提供了有力的技术支持，为透皮促进…     

胰岛素黏膜给药系统研究进展

几十年来,人们为了提高INS的疗效,不断改进INS的剂型,随着新技术和吸收促进剂的发展,INS非注射给药途径,如黏膜给药系统也在不断发展。由于注射给药病人依从性差,非注射途径应用INS一直是人们探索的理想途径。本文就目前INS黏膜给药系统研究进展进行综述。     

药物透皮给药系统技术进展

透皮给药系统（TDDS）或称经皮治疗系统（175）。系指经皮肤给药发挥全县治疗作用的一类控释膜制剂。175是一种新颖、可行，有相当潜力的新剂型，成为第三代制剂开发研究的中心课体之一。由于皮肤的结构、药物的性质及人体的生理状态作用，药物难以扩散、穿透、渗入吸收。因此，在制备中添加透皮吸收促进剂和应用离子电渗、超声等技术，可提高药物对皮肤渗透率及皮肤贮库效应的影响。本文试述国内外有关促进透皮技术研究的进展和生产研究方向。It应吸收促进制剂理想的透皮给药系统渗透促进剂应符合下列各项要求：①本身不具有药理作用。②…     

口腔黏膜给药系统的药物动力学研究进展

口腔黏膜给药(oral transmucosal drug delivery)指药物经过口腔黏膜吸收进入体循环而发挥药效,具有生物利用度高、起效快等优势。本文介绍了口腔黏膜的生理特点,详细分析了影响口腔黏膜给药系统药物动力学性质的因素,如口腔生理屏障、不同给药部位、药物理化性质、剂型因素和处方因素,阐述了体外渗透性、在体口腔吸收、体内药物动力学以及生理药代动力学模型等研究在口腔黏膜给药系统药物动力学研究中的应用,为口腔黏膜给药系统开发提供方法和借鉴。     

透皮吸收促进剂的临床应用

透皮吸收促进剂(简称穿透促进剂)系指可以加快药物穿透皮肤的速度而不对皮肤形成严重刺激和损害的物质。最早主要应用于软膏剂、擦剂、涂布剂等,随着制剂技术的不断发展、外用制剂的剂型不断增加,其用途不断扩大如骨架型透皮释放给药系统、压敏微储库型给药系统、贴布剂等。     

鼻黏膜给药剂型的研究进展

鼻黏膜给药以往多用于局部作用,如杀菌、抗病毒、血管收缩、抗过敏等,通过将药物制成溶液剂滴入鼻腔或制成气雾剂喷入鼻腔。近年来,研究发现一些甾体激素类、抗高血压、镇痛、抗生素类以及抗病毒药物,在鼻腔内用药,通过鼻黏膜吸收,生物利用度比口服更高。某些很难从鼻腔吸收的多肽和蛋白质类药物,当选用合适的黏膜促透剂或制成生物降解性微球等新剂型给药时,能提高鼻腔吸收的生物利用度[1]。近年对鼻黏膜给药达到全身作用的研究报道较多,成为药物新剂型研究的重要领域。本文对近年来有关鼻黏膜给药新剂型、新技术进行了综述。1优点与不足鼻…     

透皮给药近况选述

目的：介绍近年来国内外透皮给药的研究进展。以促进透皮给药系统的开发。方法：查阅《国际药学文摘》（IPA）2000年文摘及重要文章,结合国内近年发表的文章进行综述。结果：在透皮吸收促进剂,透皮给药剂型研究和用物理方法提高透皮吸收效果等方面进展较快。结论：透皮给药仍然是一个方兴未艾的研究领域。     

本刊制剂与技术栏目介绍

介绍普通药物制剂的制备工艺、质量控制、新药剂型研究以及药物传递系统和制剂新技术,包括控缓释与靶向制剂、经皮给药系统、植入剂与黏膜给药系统、生物药物制剂、中药现代化制剂、制剂新技术(脂质体、微乳与纳米乳、     

药物口腔黏膜吸收机理的研究进展

口腔黏膜给药途径已成为目前药学研究领域的热点之一。笔者检索国内外文献,简要介绍口腔黏膜的屏障结构和药物吸收途径,进而对口腔黏膜的吸收机理进行系统整理和分析。最终归纳出扩散理论、pH分配学说、黏膜结构变化理论、酶抑制理论、生物黏附理论、解聚理论和新型载药体系等七大理论,同时指出目前存在的问题和研究方向。主要包括:进一步完善药物口腔黏膜吸收机理的理论,使其系统化;研究和开发新型安全低毒有效的吸收促进剂以及新型载药体系;根据不同的吸收机理,改进促透剂、黏附剂、酶抑制剂等辅料筛选方法,建立合理的处方设计和评价方法。     

Permeation enhancers in the transmucosal delivery of macromolecules

The present article presents a compilation of information regarding various chemical permeation enhancers useful for transmucosal delivery of macromolecules. In the recent past, biotechnology has provided a great number of macromolecules for treatment of various disorders. With the rise in importance of macromolecules, especially proteins and peptides, an enormous volume of research on various novel routes of drug delivery has been carried out. Inspite of its giving the highest and fastest bioavailability, the parenteral route is not a preferred option, due to its inconvenience and the noncompliance of patients. Mucosal surfaces are the most common and convenient routes for delivering drugs to the body. However, macromolecular drugs such as peptides and proteins are unable to overcome the mucosal barriers and/or are degraded before reaching the blood stream. Transmucosal drug delivery with various bioavailability enhancers is receiving increasing attention as a possible alternative to parenteral delivery of macromolecules. Among the various bioavailability enhancers, chemical permeation enhancers have been most studied. Permeation enhancers reversibly modulate the permeability of the barrier layer in favor of drug absorption. Newer permeation enhancers like zonula occludin toxin, poly-L-arginine, chitosan derivatives etc have shown a significant increase in drug absorption through transmucosal routes without serious damage to the barrier layer. In particular delivery of macromolecules via the nasal and pulmonary routesusing newer permeation enhancers has emerged as a possible alternative to the parenteral delivery ofmacromolecules.     

Chitosan and its derivatives in mucosal drug and vaccine delivery.

Numerous studies have demonstrated that chitosan and their derivatives (N-trimethyl chitosan, mono-N-carboxymethyl chitosan) are effective and safe absorption enhancers to improve mucosal (nasal, peroral) delivery of hydrophylic macromolecules such as peptide and protein drugs and heparins. This absorption enhancing effect of chitosans is caused by opening of the intercellular tight junctions, thereby favouring the paracellular transport of macromolecular drugs. Chitosan nano- and microparticles are also suitable for controlled drug release. Association of vaccines to some of these particulate systems has shown to enhance the antigen uptake by mucosal lymphoid tissues, thereby inducing strong systemtic and mucosal immune responses against the antigens. The aspecific adjuvant activity of chitosans seems to be dependent on the degree of deacetylation and the type of formulation. From the studies reviewed it is concluded that chitosan and chitosan derivatives are promising polymeric excipients for mucosal drug and vaccine delivery.     

Biomembrane permeability of peptides: strategies to improve their mucosal uptake

In order to gain a therapeutic response after mucosal administration peptide drugs have to permeate the absorption membrane based on the mucus layer (I) and the epithelial tissue (II) in significant quantities. The peptide drug transport across the membrane can be improved by the use of mucolytic agents and the permeation enhancers. The generation of novel, more potent permeation enhancers, based on an improved knowledge of the absorption membrane in combination with the appropriate delivery systems will strongly improve the bioavailability of mucosally applied peptide drugs.     

吸收促进剂的作用机制及其在鼻腔给药中的研究进展

随着新的蛋白质及肽类治疗药物的开发,非侵入性给药途径-鼻腔给药日益受到关注。与口服给药和注射给药相比,鼻腔给药既可避免注射给药带来的生理和心理创伤,也可消除口服给药过程中肝脏的首过效应;且鼻腔黏膜下血管丰富,有助于药物的吸收,也更加便于患者的抢救和自救。然而,由于鼻黏膜屏障的存在,药物很难达到理想的治疗效果,因此需要加入鼻黏膜吸收促进剂来增强药物的吸收。该文主要探讨鼻黏膜吸收促进剂的作用机制及分类,并对FDA已上市鼻腔制剂中的吸收促进剂进行汇总,同时对新型黏膜吸收促进剂在鼻腔给药制剂中的应用进行阐述,以期为鼻腔给药制剂的开发提供依据。     

经皮给药促透方法的研究进展

目的由于皮肤的屏障作用,经皮给药系统的应用受到限制,促透方法的研究成为焦点。许多方法可用于促进药物的经皮吸收。本文主要从化学法、物理法、药剂学法、生物法及促透方法的综合应用等方面阐述了近年来国内外在经皮给药促透方法的研究上所取得的进展。     

Drug delivery systems. 6. Transdermal drug delivery

Transdermal drug delivery system has been in existence for a long time. In the past, the most commonly applied systems were topically applied creams and ointments for dermatological disorders. The occurrence of systemic side-effects with some of these formulations is indicative of absorption through the skin. A number of drugs have been applied to the skin for systemic treatment. In a broad sense, the term transdermal delivery system includes all topically administered drug formulations intended to deliver the active ingredient into the general circulation. Transdermal therapeutic systems have been designed to provide controlled continuous delivery of drugs via the skin to the systemic circulation. The relative impermeability of skin is well known, and this is associated with its functions as a dual protective barrier against invasion by micro-organisms and the prevention of the loss of physiologically essential substances such as water. Elucidation of factors that contribute to this impermeability has made the use of skin as a route for controlled systemic drug delivery possible. Basically, four systems are available that allow for effective absorption of drugs across the skin. The microsealed system is a partition-controlled delivery system that contains a drug reservoir with a saturated suspension of drug in a water-miscible solvent homogeneously dispersed in a silicone elastomer matrix. A second system is the matrix-diffusion controlled system. The third and most widely used system for transdermal drug delivery is the membrane-permeation controlled system. A fourth system, recently made available, is the gradient-charged system. Additionally, advanced transdermal carriers include systems such as iontophoretic and sonophoretic systems, thermosetting gels, prodrugs, and liposomes. Many drugs have been formulated in transdermal systems, and others are being examined for the feasibility of their delivery in this manner (e.g., nicotine antihistamines, beta-blockers, calcium channel blockers, non-steroidal anti-inflammatory drugs, contraceptives, anti-arrhythmic drugs, insulin, antivirals, hormones, alpha-interferon, and cancer chemotherapeutic agents). Research also continues on various chemical penetration enhancers that may allow delivery of therapeutic substances. For example, penetration enhancers such as Azone may allow delivery of larger-sized molecules such as proteins and polypeptides.     

Intravail: highly effective intranasal delivery of peptide and protein drugs

Recent development of a new class of patented alkylsaccharide transmucosal delivery enhancement agents, collectively designated as Intravail (Aegis Therapeutics) absorption enhancers, has created opportunities for new therapeutic options across a broad spectrum of human diseases. Intravail absorption enhancers provide unsurpassed intranasal bioavailabilities, comparable to those that are achieved by injection for protein, peptide and other macromolecular therapeutics. These novel, highly effective and non-irritating excipients circumvent the two primary limitations of intranasal drug delivery, namely mucosal irritation and poor bioavailability, and offer the promise of more convenient, more effective and safer therapeutics for patients and physicians alike. For pharmaceutical companies, Intravail provides a means to capitalise on two important industry dynamics: rapidly growing industry interest in commercialising peptide and protein drugs, and increasing interest in, and use of, the intranasal route for systemic drug delivery.     

Non-invasive administration of drugs through the skin: challenges in delivery system design

Vehicles designed to enhance drug delivery through the skin must incorporate specific elements that improve the ability of the delivery system to overcome the barrier posed by the stratum corneum. This review discusses several chemical penetration enhancers that have been investigated as potential tools to increase drug flux. In addition, lipid-based delivery systems offer an attractive alternative to traditional drug vehicles. The relationship between liposome composition and drug permeation is discussed, in addition to the possible mechanism of action of lipid vesicle-mediated drug delivery.