Spray Freeze-drying – The Process of Choice for Low Water Soluble Drugs?

Most of the novel highly potent drugs, developed on the basis of modern molecular medicine, taking into account cell surface recognition techniques, show poor water solubility. A chemical modification of the drug substance enhancing the solubility often decreases the pharmacological activity. Thus, as an alternative an increase of the solubility can be obtained by the reduction of the size of the drug particles. Unfortunately, it is often difficult to obtain micro or nanosized drug particles by classical or more advanced crystallization using supercritical gases or by milling techniques. In addition, nanosized particles are often not physically stable and need to be stabilized in an appropriate matrix. Thus, it may be of interest to manufacture directly nanosized drug particles stabilized in an inert hydrophilic matrix, i.e. nanostructured and nanocomposite systems. Solid solutions and solid dispersions represent nanostructured and nanocomposite systems. In this context, the use of the vacuum-fluidized-bed technique for the spray-drying of a low water soluble drug cosolubilized with a hydrophilic excipient in a polar organic solvent is discussed. In order to avoid the use of organic solvents, a special spray-freeze-drying technique working at atmospheric pressure is presented. This process is very suitable for temperature and otherwise sensitive drugs such as pharmaproteins.     

Fabrication of Micron Level Particles of Amoxicillin by Rapid Expansion of Supercritical Solution

In this study, the rapid expansion of supercritical solution (RESS) process was used to precipitate fine solid particles of amoxiccilin where supercritical carbon dioxide was used as a solvent. The process has been done by changing the RESS parameters, including extraction pressure (150–210 bar), extraction temperature (313–333 K), nozzle length (2–15 mm), effective nozzle diameter (450–1700 µm), and spraying distance (1–10 cm), to investigate the effect of these parameters on the size and morphology of the precipitated amoxicillin particles. The characterization (size and morphology) of the particles was examined using scanning electron microscopy (SEM). Based on the different experimental conditions, the mean particle size of the fabricated particles were between 1.08 and 5.72 µm, while the intact particles of amoxicillin were about 41.46 µm. Also, no regular changes in the morphology of the processed particles were observed.     

Properties of the Polycomplex of Apple Pectin with Benzimidazolyl-2-methylcarbamate Hydrochloride after Micronization

X-ray diffraction, microscopic, and sorption studies of benzimidazolyl-2-methylcarbamate hydrochloride (BMCHC) with various types of pectin showed that the structure of the mixtures depends on the composition, grinding conditions, and pectin type.     

微细化交联木薯淀粉醋酸酯的制备与研究

本文以三偏磷酸钠为交联剂,醋酸酐为酯化剂,采用先交联、后酯化,先酯化、后交联,两种方案对木薯淀粉进行改性,并对木薯淀粉醋酸酯进行微细化处理。利用IR、SEM、XRD和TGA对合成产物进行表征;并对其冷热粘度进行了研究。结果表明,理想合成路线为:先酯化,后交联合成交联木薯淀粉醋酸酯。通过机械球磨,能有效地将木薯淀粉颗粒微细化,并可通过球磨时间控制淀粉颗粒的粒度和形貌。测试表明,微细化交联木薯淀粉醋酸酯的耐热性下降、结晶度下降;冷粘度增高,但热粘度性质有所下降。     

Effect of the Micronization of Pulp Fibers on the Properties of Green Composites

Green composites, composed of bio-based matrices and natural fibers, are a sustainable alternative for composites based on conventional thermoplastics and glass fibers. In this work, micronized bleached Eucalyptus kraft pulp (BEKP) fibers were used as reinforcement in biopolymeric matrices, namely poly(lactic acid) (PLA) and poly(hydroxybutyrate) (PHB). The influence of the load and aspect ratio of the mechanically treated microfibers on the morphology, water uptake, melt flowability, and mechanical and thermal properties of the green composites were investigated. Increasing fiber loads raised the tensile and flexural moduli as well as the tensile strength of the composites, while decreasing their elongation at the break and melt flow rate. The reduced aspect ratio of the micronized fibers (in the range from 11.0 to 28.9) improved their embedment in the matrices, particularly for PHB, leading to superior mechanical performance and lower water uptake when compared with the composites with non-micronized pulp fibers. The overall results show that micronization is a simple and sustainable alternative for conventional chemical treatments in the manufacturing of entirely bio-based composites.     

Micronization of the officinal component baicalin by SEDS‐PA process

Application of micronizing technologies in processing Chinese herbal medicines is very important to improve the forms of prepared Chinese herbal medicines and promote their therapeutic efficacy. Baicalin, a major active component of the typical Chinese herb medicine Scullateria baicallensis Georgi, was micronized using the Solution Enhanced Dispersion by Supercritical fluids though Prefilming Atomization (SEDS‐PA) process with the aim of evaluating the efficiency of applying supercritical fluid precipitation technologies in Chinese herb medicine. This study has shown that acicula or rod‐like baicalin crystals with Particle Size (PS) of about 20×100 μm were successfully micronized by the SEDS‐PA process to long rod‐like, twisted fiber‐like or fibrous net‐like microparticles with PS of 0.1‐2.2 μm in width within the range of experiments performed. It was found that a substantial reduction of baicalin microparticles' sizes could lead to a marked increase of adhesions among them and subsequent microparticles agglomeration. With the increase of supercritical CO₂ flow rate and the decrease of solution concentration and solution flow rate, smaller and much more agglomerated microparticles were obtained. Increasing pressure led to formation of smaller microparticles. A larger tendency of particles agglomeration was produced at a higher temperature. (© 2007 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)     

Fiber Preparation from Micronized Oat By-Products: Antioxidant Properties and Interactions between Bioactive Compounds

This study aimed to investigate the possibility of utilizing oat by-products for fiber preparation. Oat husk (OH) and oat bran (OB) were micronized and used to prepare a novel product rich in fiber and with enhanced antioxidant properties. The basic chemical composition and phenolic acid profile were determined in OH and OB. The antioxidant properties of OH and OB were also analyzed. The type and strength of interactions between the biologically active compounds from their mixtures were characterized by an isobolographic analysis. The analyses showed that the sum of phenolic acids was higher in OH than in OB. Ferulic acid was dominant in both OH and OB; however, its content in OH was over sixfold higher than that in OB. The results also suggested that both OH and OB can be used for preparing fiber with enhanced antioxidant properties. The optimal composition of the preparation, with 60–70% of OH and 30–40% of OB, allows for obtaining a product with 60–70% fiber and enhanced antioxidant activity due to bioactive substances and their synergistic effect. The resulting product can be a valuable additive to various food and dietary supplements.