芦丁药理作用及制剂的研究进展

芦丁是一种生物活性很强、临床应用广泛的中药。芦丁具有抗自由基活性、抗脂质过氧化、抗病毒、抗急性胰腺炎等药理作用,可用于多种疾病的治疗。芦丁的制剂研究发展较快,通过广泛采用现代的制剂技术手段和方法,不仅改善了芦丁的溶出速度和提高生物利用度,而且丰富和提升了中药现代化剂型的研究基础.     

齐墩果酸的药动学研究进展

齐墩果酸具有广泛的药理作用,包括抗炎、抗肿瘤、抗糖尿病、抗动脉粥样硬化,保肝、抗骨质疏松等。但是齐墩果酸口服的生物利用度低,通过被动扩散被肠道吸收,齐墩果酸的分散体制剂能提高溶出度和生物利用度,且能浓集于肝脏,有利于治疗肝部疾病。通过综述齐墩果酸药动学参数、体内过程、齐墩果酸分散体及其前药的药动学特征,总结齐墩果酸的药动学研究进展,为合理用药提供参考。     

胆红素纳米颗粒的药理作用研究进展

胆红素具有良好的抗炎、抗氧化和免疫调节作用，但由于其水溶性差、生物利用度低，极大地限制了临床应用。研究人员将胆红素开发成各种纳米颗粒，借助剂型优势有效消除了胆红素溶解性低的限制，使其能够最大化地发挥抗炎、抗氧化、调节免疫等药理活性。胆红素纳米颗粒在多种胃肠道疾病、肝肾疾病、皮肤疾病、自身免疫性疾病、胰岛移植以及肿瘤的靶向治疗（既可直接抗肿瘤，又可作为药物递送系统）中均具有巨大的应用潜力。对胆红素纳米制剂的研究将推动胆红素的临床应用和相关的新药研发。     

熊果酸的药动学研究进展

熊果酸具有广泛的药理作用,包括抗炎、抗变态反应,抗肿瘤,保护心、血管、肝、肾、肺,抗糖尿病、调血脂抗肥胖,抗动脉粥样硬化等。但是其口服的生物利用度低,通过被动扩散被肠道吸收;将熊果酸制成分散体制剂能提高溶出度和生物利用度,且能浓集于肝脏,有利于治疗肝部疾病。综述熊果酸的药动学参数、体内过程和熊果酸分散体的药动学特征,总结其药动学研究进展,为合理用药提供参考。     

丁苯酞治疗脑缺血的研究现状

脑缺血是一种常见的中枢神经系统疾病,预后差。丁苯酞具有确切治疗脑缺血的作用,通过保护神经细胞、保护线粒体、抗氧化应激和抗炎等作用治疗脑缺血,与常规溶栓治疗比较具有优势,但其水溶性差,生物利用度不高,成为丁苯酞新剂型研发的关键问题,临床常用的丁苯酞类药物剂型主要有注射液、软胶囊和片剂等;丁苯酞通常联合依达拉奉、阿替普酶、血栓通、阿司匹林等协同增效发挥治疗作用;丁苯酞环糊精包合物、微球、胶束和微胞新型制剂有望成为未来丁苯酞治疗脑缺血的最佳给药形式。     

环孢素血药浓度的影响因素

环孢素是一种高效的免疫抑制药，其治疗范围狭窄，生物利用度和药动学参数个体差异较大，血药浓度受多种因素的影响。环孢素剂型和制剂质量、给药方案、移植器官种类、术后时间、患者自身状况、药物相互作用等因素对血浆环孢素浓度有影响。     

小檗碱的药理活性以及提升其口服生物利用度的策略

小檗碱(berberine)是一种天然存在的苄基异喹啉类生物碱,具有抗菌、抗癌、降血脂、抗糖尿病和止泻等广泛药理活性,但因其极低的口服生物利用度(<1%),限制了其在临床上的应用,尚无纯小檗碱配方被批准用于任何特定疾病。小檗碱口服生物利用度低主要是由于其在酸性条件下自聚集导致的溶解度差、渗透性低、P-gp(P-glycoprotein)介导的外排和肝肠代谢。提高小檗碱的口服生物利用度可提高小檗碱的药理活性,降低给药剂量进而减少不良反应。本文综述了小檗碱的多种药理活性、代谢过程、药代动力学特征,重点介绍了通过提高溶解度和渗透性、抑制P-gp外排和结构修饰等途径提高小檗碱口服生物利用度的策略,并对小檗碱的研究进行了展望,为其深入研究提供指导。     

熊果酸纳米制剂的研究进展

熊果酸是一种具有保肝、抗炎、抗癌等多种生物活性的五环三萜类化合物,药理活性广泛。但是,较低的水溶性和生物利用度等缺陷限制了其临床应用。因此,开发新剂型以提高熊果酸的生物利用度成为熊果酸研究的重要部分。纳米载体广泛应用于改善药物水溶性,提高药效、延长药物作用时间。本文总结了国内外熊果酸纳米制剂的相关研究,包括脂质体、胶束、纳米粒、纳米悬浮液和纳米乳,为其后续研究提供必要的思路和参考。     

环孢菌素A安全应用及药动学研究新进展

环孢菌素A(Cyclosporin A,CsA)是一种从真菌培养液中分离出来的亲脂性环多肽,为常用免疫抑制剂。目前上市的主要有注射剂、口服液和软胶囊,用于器官移植后抑制机体排斥反应及自身免疫性疾病治疗,不良反应主要表现为肾毒性和肝毒性。CsA的治疗窗窄,口服制剂的生物利用度和药动学参数存在很大的个体内、个体间差异,体内药物浓度受诸多因素影响,其疗效、毒副作用与血药浓度密切相关。刘晓磊[1]等综述了植物药、果蔬对CsA药动学的影响,本文结合国内、外的最新研究进展综述生物因素、剂型因素、食物、药物对其药动学的影响,为合理用药、剂型…     

姜黄素药物递送系统研究进展

姜黄素具有良好的药理活性,药效稳定,安全有效,尤其是抗肿瘤活性为近年研究的热点。但其水溶性差,生物利用度低,限制了其临床应用,有必要开发适当的姜黄素给药系统。该文对姜黄素国内外研究的新剂型进行了综述。     

芍药苷保肝药理作用及新剂型的研究进展

芍药苷是一种单萜糖苷类化合物,其保肝药理活性显著。但芍药苷的脂溶性差导致生物利用度低,起效较慢,限制了其广泛应用,研究和开发芍药苷新剂型以提高生物利用度和药效是当前研究的热点。基于此,本文综合国内外相关文献,对芍药苷保肝药理作用和新剂型的研究进行全面的整理综述,以期为芍药苷的应用和新剂型研发提供理论依据和思路参考。     

芦丁神经保护作用的研究现状

芦丁是广泛存在于植物中的黄酮醇配体,具有抗氧化、抗炎、降压、维持血管弹性和神经保护等多种药理活性,在心脑血管疾病的治疗与预防起到至关重要的作用,有望可以改善或预防脑血管病、神经退行性病变及其他神经系统疾病。本文根据近年来的体内、外实验研究结果,综述了芦丁在缺血性脑卒中、阿尔茨海默病、帕金森病、抗癫痫和抗抑郁发挥脑神经保护作用机制。     

奈韦拉平新剂型的研究进展

摘 要奈韦拉平（NVP）是第一代非核苷类逆转录酶抑制药,为治疗艾滋病和预防HIV 1母婴传播的一线药物。其溶解性差,生物利用度低。随着新剂型的开发,固体分散、自乳化、微粒、聚合物胶束、缓释片、胃漂浮微球等技术的应用可提高NVP的生物利用度,减少不良反应。本文通过文献检索对国内外NVP新剂型的研究进展进行了综述,为NVP新剂型的开发提供依据。     

葛根素纳米制剂的研究进展

葛根素具有多种药理活性,但其水溶性差,口服生物利用度低,限制了其临床应用.为了改善葛根素的水溶性及体内吸收,葛根素的新型纳米制剂被广泛研究,本文在总结文献的基础上对葛根素的纳米粒、微乳与自微乳、纳米结晶、胶束与树突体等的研究进展进行了介绍.     

姜黄素及其制剂的药代动力学研究进展简

姜黄素具有多种药理作用,但结构和溶解性特点导致其在体内吸收差、代谢快、生物利用度低.剂型改造是解决姜黄素应用缺陷的有效方法之一,该文对近年来姜黄素剂型的药代动力学特点进行综述,发现姜黄素制剂能有效改善姜黄素生物利用度低的不足,并显示出较好的药代动力学特点.结合纳米技术将实现姜黄素制剂的多功能化,为姜黄素的临床应用提供更多理论依据和实验基础.     

Formulation approaches for orally administered poorly soluble drugs

Despite having pharmacodynamic or target activity, many drugs fail in the drug development process due to poor bioavailability, and presently marketed conventional dosage forms of poorly soluble drugs employ high doses leading to potential toxicity. The introduction of the Biopharmaceutic Classification System (BCS) has provided a basis to categorize drugs based on the two major parameters affecting absorption, solubility and permeability. Several techniques can be employed to enhance the absorption and bioavailability of poorly soluble and poorly permeable drugs based on the BCS concept. This article is an attempt to summarize the development of various formulation approaches that are currently employed to enhance bioavailability of orally administered poorly soluble drugs.     

Pharmaceutical particle technologies: An approach to improve drug solubility,dissolution and bioavailability

Pharmaceutical particle technology is employed to improve poor aqueous solubility of drug compounds that limits in vivo bioavailability owing to their low dissolution rate in the gastrointestinal fluids following oral administration. The particle technology involves several approaches from the conventional size reduction processes to the newer, novel particle technologies that modify the solubility properties of the drugs and produce solid, powdered form of the drugs that are readily soluble in water and can be easily formulated into various dosage forms. This review highlights the solid particle technologies available for improving solubility, dissolution and bioavailability of drugs with poor aqueous solubility.     

Recent advances in oral delivery of drugs and bioactive natural products using solid lipid nanoparticles as the carriers

Chemical and enzymatic barriers in the gastrointestinal (GI) tract hamper the oral delivery of many labile drugs. The GI epithelium also contributes to poor permeability for numerous drugs. Drugs with poor aqueous solubility have difficulty dissolving in the GI tract, resulting in low bioavailability. Nanomedicine provides an opportunity to improve the delivery efficiency of orally administered drugs. Solid lipid nanoparticles (SLNs) are categorized as a new generation of lipid nanoparticles consisting of a complete solid lipid matrix. SLNs used for oral administration offer several benefits over conventional formulations, including increased solubility, enhanced stability, improved epithelium permeability and bioavailability, prolonged half-life, tissue targeting, and minimal side effects. The nontoxic excipients and sophisticated material engineering of SLNs tailor the controllable physicochemical properties of the nanoparticles for GI penetration via mucosal or lymphatic transport. In this review, we highlight the recent progress in the development of SLNs for disease treatment. Recent application of oral SLNs includes therapies for cancers, central nervous system-related disorders, cardiovascular-related diseases, infection, diabetes, and osteoporosis. In addition to drugs that may be active cargos in SLNs, some natural compounds with pharmacological activity are also suitable for SLN encapsulation to enhance oral bioavailability. In this article, we systematically introduce the concepts and amelioration mechanisms of the nanomedical techniques for drug- and natural compound-loaded SLNs.     

Soft Gelatin Capsules (Softgels)

It is estimated that more than 40% of new chemical entities (NCEs) coming out of the current drug discovery process have poor biopharmaceutical properties, such as low aqueous solubility and/or permeability. These suboptimal properties pose significant challenges for the oral absorption of the compounds and for the development of orally bioavailable dosage forms. Development of soft gelatin capsule (softgel) dosage form is of growing interest for the oral delivery of poorly water soluble compounds (BCS class II or class IV). The softgel dosage form offers several advantages over other oral dosage forms, such as delivering a liquid matrix designed to solubilize and improve the oral bioavailability of a poorly soluble compound as a unit dose solid dosage form, delivering low and ultra-low doses of a compound, delivering a low melting compound, and minimizing potential generation of dust during manufacturing and thereby improving the safety of production personnel. However, due to the very dynamic nature of the softgel dosage form, its development and stability during its shelf-life are fraught with several challenges. The goal of the current review is to provide an in-depth discussion on the softgel dosage form to formulation scientists who are considering developing softgels for therapeutic compounds.