药物化学教学研究

药物化学是一门综合性很强的药学专业必修课,涉及到药理学、生理学、药剂学、药物分析、有机化学等专业,特别是与有机化学、药理学联系更加紧密。而对于药学专业的学生而言,有机化学是其学习药物化学的软肋,因为药学专业用的有机化     

波谱解析试题库的建设

波谱解析在化学、生物、医药、材料、食品、卫生、环境等重要领域都有广泛的应用。波谱解析课程包括紫外光谱、红外光谱、核磁共振波谱以及质谱。波谱解析是药学专业重要的基础课程之一,是学习天然药物化学、药物化学的基础。编写试题库可有助于学生复习提高所学知识,本文通过详细例子阐述了波谱解析试题库的建设。     

浅谈药学专业无机化学课程考核方法改革

无机化学课程是药学类专业本科生的第一门专业基础必修课,相比其他专业而言,药学类专业对学生的化学知识要求更高。它承接中学化学与大学化学课程以及药学专业课程,对药学专业学生的分析化学、有机分析、物理化学以及药物化学、药物分析、药理学、药物动力学等专业课程的学习都起到重要作用。     

有机化合物波谱分析课程教学方法探讨

有机化合物波谱分析是制药、药学、中药学等药学类专业及相关专业本科生、研究生的专业基础课.主要教学目的是使学生掌握有机化合物结构分析的基本技能和方法,从而培养学生掌握解析简单有机化合物波谱图的能力.     

探讨如何提高有机化合物波谱解析课程教学效果

通过改进教学方法、改革考核方式、调整课程开设时间提高药学、中药学专业学生的有机化合物波谱解析课程教学效果。     

对药学专业实践教学的思考

随着我国药学学科的发展,教学水平也在不断提高。然而重理论、轻实践的现状却一直存在,造成学生专业综合素质的缺失,也成为我国药学教育发展的瓶颈。如何培养药学生的实践能力,加强实践教学,是药学教育的一个长期而艰巨的历史任务。对我国药学专业实践教学的现状进行深入解析,针对现状提出相应的解决方案。     

药学类高校构建药学多学科综合性实验的探索

药学实验对于培养高素质的药学人才起着至关重要的作用,本校开展了药学多学科综合性实验,将药学相关的二级学科实验进行有机地结合,提高了本科生对药学专业多学科知识的理解和综合运用能力。     

有机和药化实验互相渗透的教学方法

有机化学实验是药学专业重要的基础课之一,它既是基本知识和理论的验证,又是对学生基本操作技能的培养和训练。而药物化学实验则是综合有机实验的操作技能和实验方法,进行药物合成、化学结构改造和修饰。     

药学专业学生多元化综合实践技能培养模式的构建

摘要药学专业学生综合实践技能的培养与理论知识的掌握同等重要,构建药学专业学生多元化综合实践技能培养模式,完善药学专业学生实践教学体系,在专业课课堂教学中采用案例教学法,实验课教学中采用多环节强化训练法,新增认知实习、综合性、设计性实验、中试放大实验及实践技能竞赛,毕业设计采用目标化管理模式,将药学专业课课堂教学和实践教学有机结合。经过几年的教学实践,提高了学生实验技能和创新能力,对完善药学专业本科教学体系有积极意义。     

执业药师考前辅导药事法规与管理部分

药事法规和管理知识是药学专业的一个分支,是国家执业药师资格考试的主要内容之一,它融合了药学、管理科学、法学、经济学和社会学等学科知识,是执业药师必备知识的重要组成部分。在发达国家的药学类课程中,《药事法规和管理》早在20世纪初就被列为重要的专业课程之一,目前,已经占药学专业学生总课程量的9％,是所有药学专业人     

Effect of storage on microstructural changes of Carbopol polymers tracked by the combination of positron annihilation lifetime spectroscopy and FT-IR spectroscopy

Different types of Carbopols are frequently applied excipients of various dosage forms. Depending on the supramolecular structure, their water sorption behaviour could significantly differ. The purpose of the present study was to track the supramolecular changes of two types of Carbopol polymers (Carbopol 71G and Ultrez 10NF) alone and in their physical mixture with a water-soluble drug, vitamin B₁₂, as a function of storage time. The combination of FT-IR spectroscopy, positron annihilation lifetime spectroscopy (PALS) and Doppler-broadening spectroscopy was applied to follow the effect of water uptake on the structural changes. Our results indicate that water-induced interactions between polymeric chains can be sensitively detected. This enables the prediction of stability of dosage forms in the course of storage.     

Quantitative determination of crystallin insulin in insulin-zinc suspensions as an in-process control]

A method is described for the quantitative determination of amorphous and crystalline insulin contents in insulin zinc suspensions. The different resolving rates of the modifications in acid dilutions are utilized for the test. Measurements are made by UV spectroscopy. Information is given on the application of this method for the analysis of the course of insulin crystallization and it is compared with the USP XXI method.     

A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp

In the course of a search for small-molecule inhibitors of 5-hydroxytryptamine receptors we have identified a novel ergoline derivative (1) from the fungal culture of Dicyma sp. This compound has a pK(i) of 10.2 versus the 5-hydroxytryptamine(1A) receptor subtype. The structure was elucidated by extensive NMR spectroscopy and mass spectrometry.     

Hydrolysis of N,N- and N,S-dimethyl derivatives of 2-thiophenobarbital

Kinetics of hydrolysis of N,N- and N,S-dimethyl-2-thiophenobarbital and products of this reaction were investigated. The UV spectroscopy served as a tool for kinetic investigations and chromatography was used to separate and isolate the main products of hydrolysis. These products were identified by spectroscopic methods and the course of hydrolysis of both isomers was compared.     

Application of difference circular dichroism (CD) spectroscopy for determination of pharmaceutical compounds. Analysis of stereoisomers by the HPLC-CD/UV method

Circular dichroism (CD) spectroscopy is gaining an increasing importance in pharmaceutical analysis. One of the main advantages of the CD spectroscopic method is its inherent selectivity, which provides the selective analysis of chiral molecules possessing optically active absorbance bands. In addition to direct CD spectroscopic methods, several new procedures have been developed based on CD spectroscopy for the analysis and determination of pharmaceutical compounds in the past few years. One of the most progressive fields of chiroptical analysis is the combination of high performance liquid chromatographic separation and CD spectroscopy and the application of simultaneous dual CD/UV detection. The aim of our research work was to work out new procedures based on CD and CD related techniques and to investigate the application of these methods in pharmaceutical analysis. This work presents a new, selective and sensitive difference CD spectroscopic method based on oxime formation of the keto group for the determination of delta 4-3-ketosteroids and 6-keto-morphinans. Molar CD and UV spectral parameters of E and Z oxime isomers, produced in the course of oxime formation reaction, have been determined by HPLC separation and simultaneous dual CD and UV detection, without isolation of the isomers. The stereochemistry of spirocyclic pyridopyridazine compounds has been investigated by simultaneous dual CD and UV spectroscopy following HPLC separation. The enantiomeric relationship of the pyridopyridazine stereoisomers has been proved by the application of ellipticity-absorbance ratio spectra in a novel way.     

Pphysical ageing of amorphous polymeric excipients II. Tracking possibilities

In the course of physical ageing of amorphous polymers, both macro- and microstructural changes occur in the materials. Volume and enthalpy relaxation can be considered as macrostructural aspects of ageing, and can be tracked by dilatometry and calorimetry, respectively. In dilatometric measurements, volume changes are usually traced back to the changes in the length of the examined materials. Among calorimetric methods, differential scanning calorimetry (DSC) is the most widely used technique for monitoring enthalpy changes. Considering microstructural aspects of polymer ageing, free volume plays a critical role in the interpretation of the experimental results. Changes in the size and distribution of the free volume holes can be tracked by spectroscopic methods like positron annihilation lifetime spectroscopy (PALS), electron spin resonance spectroscopy (ESR) and fluorescence spectroscopy. Other techniques, as the use of photochromic probes and labels or small angle X-ray scattering (SAXS) can be informative, as well. The morphological aspects of ageing, on the other hand, can be studied by scanning electron microscopy (SEM).     

Free radicals in skin exposed to dithranol and its derivatives

The generation of persistent free radical species derived from antipsoriatic drugs in their target tissue under use conditions is reported. Dithranol (anthralin, 1,8-dihydroxy-9-anthrone) and chemical analogues were applied topically to the ear of the pig and the time course of the production of the resulting free radicals was followed by electron spin resonance spectroscopy in biopsy samples. The spectral characteristics observed correspond to data previously reported in vitro for the anthralin-10-yl radical. The role of these radical species in the mode of action of the drug is discussed.     

Studies on mechanism of thermal crystal transformation of sitafloxacin hydrates through melting and recrystallization, yielding different anhydrates depending on initial crystalline forms

The polymorphic and pseudopolymorphic forms of sitafloxacin, a novel fluoroquinolone antibiotic, were characterized by infrared spectroscopy, X-ray diffractometry, and thermal analysis. Hydrates of sitafloxacin underwent thermal transformation during the course of heating to 300°C. Monohydrate melted at 130°C and crystallized at 147°C to yield α-form (anhydrate) while sesquihydrate melted at 127°C and crystallized at 146°C to yield β-form (anhydrate). The crystal structural analysis revealed that monohydrate and sesquihydrate had opposite torsion at quinolone ring and the conformation of quinolone ring tended to be retained during hydrates to anhydrates crystal conversion. The infrared spectroscopy showed that hydrates and anhydrate α-from exists in zwitterion while β-from is consist of neutral molecule. Detail investigation of thermal behavior of hydrates suggested that water vapor also affected anhydrous crystal forms obtained by heating hydrates, though promoting ionization at carboxyl group and amine group.     

Ultrasonic resonator technology as a new quality control method evaluating gelatin nanoparticles

Nanomedicine is a quickly evolving field where more and more possible applications become evident and start entering clinical trials or even the market. However, the analytic methods are not always able to keep pace with the new formulations’ demands. One example of a promising medical implementation is oligodeoxynucleotide (ODN) delivery by gelatin nanoparticles (GNPs). Currently, quality control is dependent on either some time consuming or destructive spectrometric, chromatographic or electrophoretic methods. A possible enlargement of the portfolio by Ultrasonic Resonator Technology (URT) is investigated here by subjecting plain GNPs in various sizes and concentrations as well as ODN-loaded GNPs to URT analysis. If calibrated by photon correlation spectroscopy (PCS) and other spectroscopy methods for each single nanoparticle system parameter, URT is an efficient and non-destructive technique and serves as a broad characterization method. URT is emphasized to play a possible future part in the size, concentration and ODN loading monitoring, e.g. of gelatin nanoparticles in the course of formulation development.