药物制剂中薄膜包衣微丸的研究与应用

综述近年来薄膜包衣微丸在药物制剂中的研究与应用。微丸属于多单元型药物传递系统，具有众多优点。而将微丸制备技术和薄膜包衣技术相结合制成的具有特殊释药性质的薄膜包衣微丸，已经成为缓、控释制剂研究领域的热点。     

药物制剂研究的科研设计

众所周知，药物制剂是达到治疗目的的一种形式。只有把合成的药物结晶、粉末或中药提取物制成某种制剂，如片剂、注射剂，病人才能服用这种药或者接受这种药物的治疗。那么，怎样才能制得“安全、有效”的药物制剂呢？在有关药物制剂的研究工作中应该注意哪些问题呢？这就是我要介绍的内容，主要侧重点在于医院制剂研究中的一些比较实际的问题。本文主要分为两大部分：第一部分　药物制剂研究开发前的科研设计；第二部分　药物制剂研究开发过程中的科研设计。第一部分　药物制剂研究开发前科研设计这部分内容主要是指尚未动手作实验之前必须…     

薄膜包衣技术在中药固体制剂防潮中的应用

中药制剂易吸潮严重影响药品的稳定性.本文简要介绍了中药制剂吸湿性原理、薄膜包衣的优点及应用现状,重点从薄膜包衣的成膜原理、处方组成、影响包衣制剂的工艺参数等方面综述薄膜包衣在中药防潮中的应用.近几年,虽然薄膜包衣已广泛应用于药物制剂,但由于中药成分的复杂性,薄膜包衣在中药防潮方面的研究和应用还不够深入.随着对新型薄膜包衣材料及薄膜包衣技术的研究,薄膜包衣在中药方面的应用将得到进一步的关注,并将在中药现代化发展进程中发挥较大的潜力.     

热熔包衣技术及其在药物传递系统中的应用

热熔包衣技术在缓控释制剂、掩盖药物不良口味、（中药）防潮、提高药物稳定性及生物利用度方面具有突出的优势,已成为制剂技术药物传递系统中的一个新热点,现综述热熔包衣技术的原理、包衣材料和近年来的研究应用情况。     

口服固体制剂掩味技术的研究进展

综述各种新兴口服固体制剂掩味技术的原理、特点及制备过程,并简述口服掩味技术评价方法的最新进展。口服固体制剂中许多药物由于受到不良口味的影响,致使病人的用药顺应性差、临床应用受限。近年来在使用矫味剂、麻痹剂等掩味手段的基础上产生了许多新兴的掩味技术,如喷动床包衣、粉末包衣和盐析包衣等。     

羟丙甲纤维素衍生物研究概述

目的：了解羟丙甲纤维素衍生物的研究概况,为药用新辅料及新剂型的研究提供参考。方法：通过查阅中国期刊网和万方数据库2001-2012年国内外相关文献资料,从材料角度对羟丙甲纤维素衍生物的制备方法、结构确认、性能以及在药物制剂中的应用等方面进行综述。结果与结论：羟丙甲纤维素衍生物能显著提高药物的生物利用度和靶向性。作为新型药用辅料,已广泛应用于肠溶制剂、缓控释制剂和结肠处药物定位释放给药系统的包衣材料,为药物制剂新剂型提供了新型辅料,在药物新剂型的研制方面发挥着重要作用。     

pH依赖型尤特奇应用研究进展

鉴于药用辅料尤特奇所展现出的多功能性和特殊性质,现已成为国内外制剂研究的重要辅料。尤特奇根据溶解特性主要分为pH依赖型和渗透型两大类,主要用作缓控释制剂、口服定位释药系统、微球与微囊等制剂中的包衣材料及载体,可达到缓控释或定位释放的目的,还可起到掩味、增溶、防潮防辐、提高药物稳定性或生物利用度等作用。本文在文献调研的基础上,综述了pH依赖型尤特奇的理化性质及其在药物制剂领域应用的最新进展。     

药用丙烯酸树脂在制剂中的应用进展

目的:介绍药用丙烯酸树脂在药物制剂中应用的最新进展。方法:根据文献,以药用丙烯酸树脂中的德国商品尤特奇为代表,综述了该类辅料的理化性质及在制剂领域中的应用。结果:丙烯酸树脂根据溶解特性分为pH依赖型与pH非依赖型2种;主要用作缓控释制剂、口服定位释药系统、微球与微囊等制剂中的包衣材料及载体,可达到缓、控释或定位释放的目的,还可起到掩味、提高药物稳定性等作用。结论:丙烯酸树脂因具有多种功能和特殊性质而成为多种制剂的重要辅料,在制剂领域中具有广阔的前景。     

药物固体制剂的接触角与湿润性

<正> 固体药物的湿润性对于粉末的吸湿性、化学稳定性和片剂包衣的粘着力以及粉末在液体中的分散性等有着重要的影响,尤其是固体粉末的湿润性作为溶出初始阶段的首要条件,对片剂的溶出速度影响很大。如片剂压制过程添加的润滑剂大多为疏水性,由此引起颗粒湿润性的改变常常影响片剂的崩解时限与溶出速率,而难溶性药物片剂的水透入速度及崩解后粒子的絮凝或分散等均与粉末的湿润性有关,进而影响片剂的溶出和疗效。无论是直接以接触角衡量药物固体制剂的湿润性,还是以固体表面自由能所求的极性指数作为湿润性的定量指标,都基于测定固体的接触角。固体接触角的测定方法众多,而原理不一,在药物制剂中的应用日趋见多,文献报道值也各有出入。本文将着重讨论接触角的测定方法及应用。     

缓控释包衣技术及聚合物包衣材料的应用进展

缓控释制剂是当代固体药物制剂研究的重要领域之一,为了达到缓控释的目的,研究者主要采用骨架控制、聚合物膜控制和骨架膜控制3种方法。其中,聚合物膜控制方法在近几年得到迅速的发展。随着科学技术的进步,包衣技术的发展使膜控型缓控释制剂更加普遍。     

螺旋霉素超细粉的喷干法和反溶剂法制备及性质研究

目的 螺旋霉素原料药粉的粒径大、团聚现象严重,因此极大的限制了其临床应用;有研究报道超细粉制备技术可以很好地解决这些问题;方法 采用了两种代表性的方法制备螺旋霉素的超细粉：分别为喷雾干燥法和反溶剂法;并以粒径为指标,采用单因素实验优化得到最佳结果,对上述两种方法制备的粉体分别进行粒径、形貌特征和物化性质对比。结果 两种方法的最佳条件为：喷雾干燥法的进料速度为5 mL/min,雾化空气速度为800 L/h,进口温度为150℃,出口温度为85℃,平均粒径为(1638±10.99) nm。反溶剂法在25℃条件进行实验,溶剂与反溶剂的比例为1:5,最佳搅拌速度为1000 r/min,获得的平均粒径为(230±7.31)nm,以上结果经过扫描电子显微镜(SEM),动态光散射(DLS),傅立叶变换红外光谱(FTIR),差示扫描量热仪(DSC)和X射线衍射(XRD)进行表征;经气相色谱检测,两种方法中的溶剂残留均符合ICH最低标准(5000 ppm);结论 与喷雾干燥法相比,反溶剂法制备的螺旋霉素粒径更小、粉体分散性更佳,其溶解度更高。因此反溶剂法制备的螺旋酶素微粉更适用于制药业,为微粉技术提供技术...     

Solventless Pharmaceutical Coating Processes: A Review

Coatings are an essential part in the formulation of pharmaceutical dosage form to achieve superior aesthetic quality (e.g., color, texture, mouth feel, and taste masking), physical and chemical protection for the drugs in the dosage forms, and modification of drug release characteristics. Most film coatings are applied as aqueous- or organic-based polymer solutions. Both organic and aqueous film coating bring their own disadvantages. Solventless coating technologies can overcome many of the disadvantages associated with the use of solvents (e.g., solvent exposure, solvent disposal, and residual solvent in product) in pharmaceutical coating. Solventless processing reduces the overall cost by eliminating the tedious and expensive processes of solvent disposal/treatment. In addition, it can significantly reduce the processing time because there is no drying/evaporation step. These environment-friendly processes are performed without any heat in most cases (except hot-melt coating) and thus can provide an alternative technology to coat temperature-sensitive drugs. This review discusses and compares six solventless coating methods—compression coating, hot-melt coating, supercritical fluid spray coating, electrostatic coating, dry powder coating, and photocurable coating—that can be used to coat the pharmaceutical dosage forms.     

Solventless pharmaceutical coating processes: a review

Coatings are an essential part in the formulation of pharmaceutical dosage form to achieve superior aesthetic quality (e.g., color, texture, mouth feel, and taste masking), physical and chemical protection for the drugs in the dosage forms, and modification of drug release characteristics. Most film coatings are applied as aqueous- or organic-based polymer solutions. Both organic and aqueous film coating bring their own disadvantages. Solventless coating technologies can overcome many of the disadvantages associated with the use of solvents (e.g., solvent exposure, solvent disposal, and residual solvent in product) in pharmaceutical coating. Solventless processing reduces the overall cost by eliminating the tedious and expensive processes of solvent disposal/treatment. In addition, it can significantly reduce the processing time because there is no drying/evaporation step. These environment-friendly processes are performed without any heat in most cases (except hot-melt coating) and thus can provide an alternative technology to coat temperature-sensitive drugs. This review discusses and compares six solventless coating methods - compression coating, hot-melt coating, supercritical fluid spray coating, electrostatic coating, dry powder coating, and photocurable coating - that can be used to coat the pharmaceutical dosage forms.     

螺旋霉素超细粉的喷干法和反溶剂法制备及性质研究

摘要：目的 螺旋霉素原料药粉的粒径大、团聚现象严重,因此极大的限制了其临床应用;有研究报道超细粉制备技术可 以很好地解决这些问题; 方法 采用了两种代表性的方法制备螺旋霉素的超细粉：分别为喷雾干燥法和反溶剂法;并以粒径为 指标,采用单因素实验优化得到最佳结果,对上述两种方法制备的粉体分别进行粒径、形貌特征和物化性质对比。结果 两种 方法的最佳条件为：喷雾干燥法的进料速度为5 mL/min,雾化空气速度为800 L/h,进口温度为150℃,出口温度为85℃,平均 粒径为(1638±10.99) nm。反溶剂法在25℃条件进行实验,溶剂与反溶剂的比例为1:5,最佳搅拌速度为1000 r/min,获得的平均 粒径为(230±7.31)nm,以上结果经过扫描电子显微镜(SEM),动态光散射(DLS),傅立叶变换红外光谱(FTIR),差示扫描量热仪 (DSC)和X射线衍射(XRD)进行表征;经气相色谱检测,两种方法中的溶剂残留均符合ICH最低标准(5000 ppm);结论 与喷雾干 燥法相比,反溶剂法制备的螺旋霉素粒径更小、粉体分散性更佳,其溶解度更高。因此反溶剂法制备的螺旋酶素微粉更适用于 制药业,为微粉技术提供技术思路。     

高分辨三维X射线显微成像在药物制剂结构分析中的应用

药物制剂的结构研究能够帮助更加全面地评价药物制剂的质量,也有助于新型药物制剂的设计和创新。高分辨三维X射线显微成像技术能够在微米级甚至纳米级空间分辨率上原位、无损地展示粉末、颗粒、片剂、胶囊等固体制剂的三维结构信息,为新型制剂的创新和质量控制提供新方法。本文在介绍高分辨三维X射线显微成像技术的原理、发展及其研究药物制剂结构的基本流程的基础上,综述了其在药物制剂结构研究方面的国内外进展,为相关研究提供参考。     

Biopharmaceutical powders: particle formation and formulation considerations

It is well known that protein/peptide-based drug formulations are more stable in the solid state than in the liquid state, thereby offering stability advantages in ambient temperature storage, product shipping/distribution, and long-term shelf life. Novel powder-based drug delivery systems recently emerging for applications in sustained release, inhalation, intradermal delivery, etc, add more value to protein solid dosage forms. Despite great research interests in understanding the drying effects on protein stability and a large collection of publications focusing on this area, systematic accounts of powder formation techniques are lacking. This review is to summarize a number of methods currently available for protein powder preparation. Some are common methods such as lyophilization, spray drying, pulverization, and precipitation, and some methods are more recently developed such as supercritical fluid precipitation, spray-freeze drying, fluidized-bed spray coating and emulsion precipitation. In addition to examining the individual process effect on protein stability that is always the focus of formulation scientists, this review also likes to evaluate each method from a more practical sense in terms of process versatility and scalability. The conclusion is that each method has its own advantages and the use of a method is formulation and application specific. With the understanding of the principles and advantages of these methods, it can benefit our choice on selecting appropriate techniques for preparing a desired protein powder formulation for specific applications.     

Particle formation of budesonide from alcohol-modified subcritical water solutions

Recently, subcritical water (SBCW: water that has been heated to a temperature between 100°C and 200°C at pressures of up to 70bar) has been used to dissolve several hydrophobic pharmaceutical compounds (Carr et al., 2010a). Furthermore, a number of active pharmaceutical ingredients (APIs) have been rapidly precipitated from SBCW solutions (Carr et al., 2010b,c). It is possible to alter the precipitate morphology by altering the processing variables; including the SBCW-API solution injection temperature and adding impurities (such as pharmaceutical excipients, e.g. lactose) to the precipitation chamber. The work presented in this article demonstrates that the morphology of pharmaceutical particles can be tuned by adding organic solvents (ethanol and methanol) to the SBCW-API solutions. Particle morphology has also been tuned by adding different pharmaceutical excipients (polyethylene glycol 400 and lactose) to the precipitation chamber. Different morphologies of pharmaceutical particles were produced, ranging from nanospheres of 60nm diameter to 5μm plate particles. Budesonide was used as the model API in this study. Two experimental products were spray dried to form dry powder products. The aerodynamic particle size of the powder was established by running the powder through an Andersen Cascade Impactor. It has been shown that the drug particles produced from the SBCW micronization process, when coupled with a spray drying process, are suitable for delivery to the lungs.     

Evaluation of the Nano Spray Dryer B-90 for pharmaceutical applications

The vibrating mesh spray technology implemented in the Nano Spray Dryer B-90 was evaluated for pharmaceutical applications by spray drying common pharmaceutical excipients (e.g. trehalose, mannitol) and model drugs (e.g. griseofulvin). Aerosol droplet size measurements investigated the influence of spray solution factors (e.g. viscosity, surface tension) and of vibrating mesh aperture sizes on particle characteristics. Particle deposition on the spray nozzle was addressed by analyzing the influence of spray solute concentration and solvent on the process outcome. Submicron particles with 0.5 µm and 0.8 µm mean particle size were obtained at high yields for 50?mg powder amounts.     

固体制剂干法包衣工艺的研究进展

目的对近年来国内外固体制剂的非溶剂包衣工艺进行介绍。方法通过查阅文献,综述了目前比较常用的几种包衣方式,包括静电干粉包衣、增塑剂干法包衣、增塑剂静电干粉包衣、热溶包衣、压制包衣和光固化包衣,以及各种包衣工艺的原理、过程与特点。结果干法包衣工艺可以避免水性或有机溶剂的使用。结论干法包衣工艺具有很大潜力,可用于固体制剂包衣的工业化生产。     

Pharmaceutical spray drying: solid-dose process technology platform for the 21st century

Requirement for precise control of solid-dosage particle properties created with a scalable process technology are continuing to expand in the pharmaceutical industry. Alternate methods of drug delivery, limited active drug substance solubility and the need to improve drug product stability under room-temperature conditions are some of the pharmaceutical applications that can benefit from spray-drying technology. Used widely for decades in other industries with production rates up to several tons per hour, pharmaceutical uses for spray drying are expanding beyond excipient production and solvent removal from crystalline material. Creation of active pharmaceutical-ingredient particles with combinations of unique target properties are now more common. This review of spray-drying technology fundamentals provides a brief perspective on the internal process 'mechanics', which combine with both the liquid and solid properties of a formulation to enable high-throughput, continuous manufacturing of precision powder properties.