水滑石@凹凸棒石的制备及其吸附性能

采用共沉淀法制备镁铝水滑石,探讨化学沉淀法和物理球磨法两种复合方式对水滑石@凹凸棒石复合材料物相、微观结构和吸附性能的影响,利用X射线衍射(XRD)仪、扫描电镜(SEM)、傅里叶红外光谱(FTIR)仪对反应产物进行表征.结果表明,物理球磨法制备的复合材料对盐酸四环素吸附效果较好.当凹凸棒石用量为水滑石质量70％时,凹凸...     

N-(2-甲胺基乙基)邻苯二甲酰亚胺盐酸盐的合成

以乙醇胺为原料合成N-甲基乙二胺,采用新方法将其N-邻苯二甲酰化合成N-（2-甲胺基乙基）邻苯二甲酰亚胺,用于胺基保护以提高N-甲基乙二胺在亲核反应中的选择性,总收率32．5％。     

Drug release from lipid liquid crystalline phases: relation with phase behavior

Introduction: We studied the release of propranolol hydrochloride (PHCl), a water-soluble amphiphilic drug, from monoolein (MO)/water and phytantriol/water systems. Methods: We related the dissolution profiles with phase behavior and viscosity of the different liquid crystalline phases. Diolein has been added aiming to stabilize the cubic phases and thus preventing formation of less viscous (lamellar) phases. Results: Formulations display first-order release rates and diffusion release mechanism. Some formulations (mostly MO) were close to zero-order release in the first 120 minutes. Discussion: Release mechanism can be influenced by phase changes during dissolution. Conclusions: Both MO and phytantriol show good potential to be used for propranolol hydrochloride sustained drug release.     

X-Ray Diffraction and Electron Microscopy in the Polymorphism Study of Ondansetron Hydrochloride

Using different techniques, we studied the possible formation of ondansetron polymorphs. Ondansetron is a carbazol antiemetic that acts as a competitive, selective inhibitor of 5-HT₃ serotonin receptors. The polymorphs were determined by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The results suggest that the compounds are not true crystallographic polymorphs, but instead are the product of physical structural changes in the drug, which would be of interest pharmaceutically.     

Production of stable amorphous form by means of spray drying

Spray drying is a very useful method for manufacturing of amorphous solid materials. This is mainly due to the possibility of fast solvent evaporation that leads to a rapid transformation of solution to a solid state. Besides evaporation kinetics, there are various process parameters that influence physical and chemical characteristics of such obtained material. The possibility of obtaining a stable amorphous structure of the active pharmaceutical ingredient in a spray dryer was examined. A solution of the hydrochloride crystalline structure of the active pharmaceutical ingredient in a mixture of water and acetonitrile was dried at different temperatures and flowrates of nitrogen used for atomization, as well as the flowrates of the solution. The influence of the process conditions on the properties of the product was analyzed. The final dried products were characterized and identified with a variety of analytical and physical methods. The results showed that a stable amorphous structure of the high purity active pharmaceutical ingredient is obtained, and that the optimal conditions of the process are defined. The amorphous structure is stable at temperatures below 200°C when it is transformed into a new crystal structure. Conditions of high relative air humidity lead to partial transformation.     

The aggregation behavior and structure of blends of κ-carrageenan and ε-polylysine hydrochloride

Polypeptides play a key role in improving food quality, and understanding their interactions with polysaccharides would be beneficial to developing new foods. Herein, κ-carrageenan (KC) and ε-polylysine hydrochloride (PLH) were chosen as the model polysaccharide and polypeptide, respectively, to study polysaccharide/polypeptide complexes. The KC/PLH solutions were characterized for turbidity as a function of mass ratio, pH, salts and stirred conditions at 0.5 and 1 mg mL^–1 concentrations. The solutions at a KC/PLH mass ratio of 7:3 have the highest turbidity, and the turbidity is stable in acidic conditions, decreases with increase in pH in alkaline conditions and salt concentration, and increases with increase of stirred time and temperature. The Fourier transform infrared spectra suggest that the amide I band of PLH disappears along with a change in the amide II band upon complexing with KC. These changes further influence the microstructure and reveal a rough, non-uniform and large irregular cavity network structure. Indeed, these observations are intimately associated with the dynamic interactions persistent at the molecular level between the KC and PLH. © 2021 Society of Industrial Chemistry.     

Monitoring of the manufacturing process for ambroxol hydrochloride tablet using NIR-chemometric methods: compression effect on content uniformity model and relevant process parameters testing

This study aimed at using near-infrared (NIR) spectroscopy to monitor compaction pressure for simultaneously determining the tensile strength and content uniformity, as well as moisture and mean particle size of ambroxol hydrochloride tablets. The content uniformity, compression force and tensile strength of the laboratory samples were obtained by pressing a mixture of active principle and excipient components into tablets. To reduce the spectral baseline shift of the laboratory samples, the compaction pressure applied to the mixture was assessed by a variable pressure test. Production samples were added to the test and subjected to principal component analysis. The expanded partial least-squares (PLS) calibration model used to quantify the active content was more accurate than the model constructed from laboratory samples using the production tablets included in the calibration set. The model showed good predictability, with correlation coefficient (R) 0.9977. The validation and reliability of the content model were evaluated to determine trueness and reliability for the measurement of individual production tablets and the laboratory tablets with drug content ranging from 24 to 36?mg. The PLS calibration models for compression force and tensile strength were constructed using the same spectral set assuming both were highly related. These models yielded high R values (0.9955 and 0.9910). The R values of the moisture and mean particle size were 0.9994 and 0.9919, respectively. This study demonstrated that NIR spectroscopy combined with chemometric techniques can be successfully used to quantitatively monitor the tablet manufacturing process in the pharmaceutical industry.     

Development of topical hydrogels of terbinafine hydrochloride and evaluation of their antifungal activity

The purpose of this study was to prepare hydrogels and microemulsion (ME)-based gel formulations containing 1% terbinafine hydrochloride (TER-HCL) and to evaluate the use of these formulations for the antifungal treatment of fungal infections. Three different hydrogel formulations were prepared using chitosan, Carbopol® 974 and Natrosol® 250 polymers. A pseudo-ternary phase diagram was constructed, and starting from ME formulation, a ME gel form containing 1% Carbopol 974 was prepared. We also examined the characteristic properties of the prepared hyrogels. The physical stability of hydrogels and the ME -based gels were evaluated after storage at different temperatures for a period of 3 months. The release of TER-HCL from the gels and the commercial product (Lamisil®) was carried out by using a standard dialysis membrane in phosphate buffer (pH 5.2) at 32?°C. The results of the in vitro release study showed that the Natrosol gel released the highest amount of drug, followed by Carbopol gel, chitosan gel, commercial product, and the microoemulsion-based gel in that order. In vitro examination of antifungal activity revealed that all the prepared and commercial products were effective against Candida parapsilosis, Penicillium, Aspergillus niger and Microsporum. These results indicate that the Natrosol®-based hydrogel is a good candidate for the topical delivery of TER-HCL.     

氨化酵母吸附剂处理盐酸四环素废水研究

120℃下将废弃酵母与尿素混合,半干法制备了氨化酵母吸附剂,SEM分析表明氨化酵母产品呈椭球状,分散性好,粒径约为3μm。FT-IR表明在3 300 cm-1左右出现氨基峰。以盐酸四环素模拟废水为处理对象,考察了各因素对吸附过程的影响,研究了吸附动力学和吸附等温模型。实验表明最佳吸附pH为7;3.0 h后吸附量达到平衡;吸附过程遵循准二级动力学方程,受颗粒内扩散控制。饱和吸附后的氨化酵母吸附剂在强酸条件下可实现再生。