电合成芳醛生产中的监控分析方法

本工作研究了盐酸羟胺法测定芳醛的适宜条件，测定了本方法的精密度和准确度，结果令人满意。用此方法对电合成芳醛生产中料液及产品中的醛含量进行了分析，测定结果和色谱法、电位滴定法测定一致。     

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.     

新型抗精神病药物盐酸鲁拉西酮的合成研究进展

盐酸鲁拉西酮是一种新型的抗精神病药物。归纳了该原料药的合成方法,根据起始原料的光学纯度、中间体的不同可将合成路线分为三大类,并且对这三类方法进行了比较分析,总结出各自的优缺点,从而为该原料药的制备研究提供参考。     

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.     

Formulation,characterization and clinical evaluation of propranolol hydrochloride gel for transdermal treatment of superficial infantile hemangioma

The objective of the present study is to formulate and characterize propranolol hydrochloride (PPL?·?HCl) gel, and to evaluate the efficacy of this formulation in transdermal treatment for superficial infantile hemangioma (IH). The transdermal PPL?·?HCl gel was prepared by a direct swelling method, which chose hydroxypropyl methylcellulose (HPMC) as the matrix and used terpenes plus alcohols as permeation enhancer. Permeation studies of PPL?·?HCl were carried out with modified Franz diffusion cells through piglet skin. Our results pointed to that among all studied permeation enhancers, farnesol plus isopropanol was the most effective combination (Q_24, 6027.4?±?563.1?μg/cm², ER, 6.8), which was significantly higher than that of control gel (p?相似文献