Acta Facultatis Pharmaceuticae Universitatis Comenianae

Abstract We observed the changes in electrical activity, biometric and haemodynamic parameters of hearts in animals with experimental diabetes mellitus (DM). As well the effect of carvedilol, PycnogenolR and its combination with carvedilol on DM heart function was tested. DM was induced by streptozotocin over three sequential days at a dose of 25 mg/kg body weight i.p. We started therapy by suspension of carvedilol, PycnogenolR and their combination for six weeks. Blood pressure was measured using tail cuff plethysmography. ECG, haemodynamic and biometric parameters were measured in isolated hearts perfused according to the Langendorff. DM rats had increased systolic arterial blood pressure, thicker free wall of left ventricle but weakened myocardial contractility compared with controls. In contrast to controls, electrophysiological parameters showed prolonged QT interval and increased incidence of dysrhythmias in DM rats. The PycnogenolR administration induced regression of left ventricular hypertrophy, improved left ventriculi contraction and increased coronary flow; however, it did not improve the electrical activity of the myocardium compared with DM ones. Carvedilol also reversed the myocardial remodelling, shortened the duration of QT interval and suppressed the incidence of dysrhythmias. The common combination of drugs improved biometric and haemodynamic parameters compared with DM animals, however, not so significantly as monotherapy. On the other hand, the combination of carvedilol and PycnogenolR significantly reduced the duration of the QT interval and shortened the incidence of dysrhythmias. We can conclude that the administration of PycnogenolR effectively improved haemodynamic parameters, and carvedilol affected biometric parameters and also electrical parameters in DM animals. We observed the marked synergic effect of the combination of both drugs on the electrical activity of myocardium. This combination shortened the most pathologically prolonged QT interval and reduced the number of dysrhythmias.

Kráľová E.

Jankyová S.

Pekárik A.

Čuboň J.

Stankovičová T.

Carvedilol and Pycnogenol® improve the function of diabetic hearts in rats

卡维地洛和碧萝芷®改善糖尿病大鼠心脏功能

Abstract The effect of N-dodecyl-N,N-dimethylamine N-oxide (C12NO) on the unilamellar liposomes prepared from egg yolk phosphatidylcholine (EYPC) was studied using turbidimetric and fluorescence spectroscopic methods. The concentrations of C12NO causing saturation and total solubilization of membrane were evaluated turbidimetrically. Liposomes filled with hydrophilic fluorescent probe calcein were used for the fluorescence leakage measurements. Dependence of fluorescence intensity on C12NO concentration can be divided into three linear sections. The turning points between individual sections represent two concentrations of C12NO which induce formation of small defects, specifically large pores in liposomal membrane. These pores are wide enough to enable calcein to be washed out from liposomes completely. We compared results obtained by the two methods used. Measurements of fluorescent probe leakage showed that free diffusion of calcein through pores in EYPC bilayer was observed at such C12NO concentrations when the form of liposome is still preserved and the saturation of bilayer is not yet finished. Higher C12NO concentrations are needed for solubilization, a phase transition from bilayers to micelles.

Huláková S.

Fulier B.

Gallová J.

Balgavý P.

Effect of N-dodecyl-N,N-dimethylamine N-oxide on unilamellar liposomes

N-十二烷基-N,N-二甲基胺-N-氧化物对单层脂质体的影响

Abstract Our study deals with the analysis of prescription of individually prepared medicines (IPMs) in selected community pharmacies in Slovakia and Greece during the year 2011. Throughout the given period, the total sum of processed medical prescriptions in selected Slovak pharmacies was 50,992, while in Greece it was 45,862 prescriptions. Out of the total sum of prescriptions, we selected those with prescribed IPMs. In our study, we further analysed the representation of individual age groups and both genders in prescriptions of the IPMs. Next, we examined the frequency of IPM prescriptions based on specialisation of the prescribing physicians and the most frequent diagnoses for which the IPMs were prescribed. Further, we classified the prescribed IPMs into specific groups according to their drug forms. In our study, we also described the representation of individual drug forms (oral, cutaneous and for specific use) and representation of prepared or adjusted IPMs. The relevance of this topic is supported by marked decrease of rate of preparing of IPMs in the last decades as well as by necessity to preserve it for reasons such as certain diagnoses, technological and economic aspects and differences among age groups require distinctive specification of the prepared medicines.

Lehocká Ľ.

Masaryková L.

Mináriková D.

Malovecká I.

Oleárová A.

Fulmeková M.

Foltán V.

Analysis of individually prepared medicines prescription in community pharmacy

社区药房个体化制剂处方分析

Abstract This article describes a preparation of some new compounds of the aryloxyaminopropanol type derived from 4-hydroxyphenylpropan- 1-one with phenylamino, cyclohexylamino and isobutylamino group in the hydrophilic part and methoxymethyl or ethoxymethyl substituent in the lipophilic part of the molecule. The purity of the prepared compounds was checked by thinlayer chromatography and the structure was confirmed on the basis of interpretation of the IR, UV, 1H NMR and 13C NMR spectra. An enantioseparation of the prepared compounds was performed by using high-performance liquid chromatography on an amylase tris(3,5-dimethylphenylcarbamate) (Chiralpak AD) and native teicoplanin (Chirobiotic T). The chromatographic results such as retention, separation and resolution factors have shown that Chiralpak AD is more suitable for enantioseparation of some of the prepared compounds.

Čižmáriková R.

Némethy A.

Valentová J.

Hroboňová K.

Adamcová K.

Synthesis of new compounds of the aryloxyaminopropanol type and their HPLC enantioseparation

芳氧基氨基丙醇类新化合物的合成及其高效液相色谱手性分离

Abstract The contents of selected elements (Mn, Fe, Co, Ni, Cu, Zn, Hg and Pb) in samples of loose tea of agrimony “Repikovy čaj” (Agrimonia eupatoria L.) were studied in this work. Identification and determination of the selected elements content were performed using X-ray fluorescence spectrometry - the nuclear analytical method based on the interaction between low-energy gamma and X radiation and analysed substance. Solid form samples were pressed in tablets and directly analysed. Prepared infusions were analysed after the preconcentration of the elements using precipitation with thioacetamide and ammonium diethyldithiocarbamate with subsequent filtration of created precipitates through a nitrocellulose filter. Detection limits obtained from both methods were compared and their suitability for elemental analysis of plant preparations was discussed.

Mikušová V.

Lukačovičová O.

Havránek E.

Radionuclide x-ray fluorescence analysis of selected elements in agrimony tea samples with preconcentration

选定元素在含预浓缩的龙牙草茶样品中的放射性核素X射线荧光分析

Abstract The theoretical chemistry methods were used to elucidate absorption, distribution and physicochemical properties of AT 1 receptor antagonists and dual angiotensin II and endothelin A receptor antagonist (PS-433540). Computed partition coefficients (ALOGPS method) studied for drugs varied between 2.98 and 6.66. Neutral compounds are described as lipophilic drugs. Telmisartan is a drug with the highest lipophilicity. The neutral forms of the studied AT 1 receptor antagonists are practically insoluble in water, and their computed solubilities is in interval between 2.04 and 22.65 mg/l (ALOGpS method). The calculated pK a values for tetrazolyle moiety are in the range 3.92-5.00 and for carboxylic moiety 3.12-5.50. Telmisartan (polar surface area = 72.95 A) and irbesartan (polar surface area = 87.14 A) belong to the AT 1 receptor antagonists with increased absorption.

Pavol Ježko

Viera Žufková

Milan Remko

Modelling of absorption, distribution and physicochemical properties of AT1 receptor antagonists / Modelovanie absorpcie, distribúcie a fyzikálnochemických vlastnosti antagonistov AT1 receptorov

AT1受体拮抗剂的吸收、分布及理化性质建模 / AT1受体拮抗剂的吸收、分布及理化性质建模

Abstract Sjögren’s syndrome is a slowly progressive, inflammatory autoimmune disease primarily affecting exocrine glands. Lymphocytic infiltrates replace functional epithelium and lead to decreased exocrine secretion of salivary and lacrimal glands - xerocrinopathy. Glands of intestinal system and pulmonary tract, skin and vaginal mucosa may also be affected. The most common extraglandular manifestations of primary Sjögren’s syndrome include skin vasculitis, Raynaud’s phenomenon, functional renal abnormalities, neuropathy and arthritis symptoms. This disorder may appear separately as a primary Sjögren’s syndrome or in connection with other inflammatory rheumatic diseases as secondary Sjögren’s syndrome. Treatment of the disease is based on topical ocular and oral therapy, extraglandular manifestations need to be treated with hydroxychloroquine and severe cases even with corticosteroid or immunosuppressive drugs.

Mlynáriková V.

Mičeková D.

Rovenský J.

Šteňová E.

Sjögren’s syndrome

干燥综合征

Abstract An overview of the diagnostics and treatment of phenylketonuria in Slovakia is presented in this paper. The nature of diseases, incidence and prevalence in Slovakia, its genetic characteristics, current laboratory diagnostics and treatment options are defined. A new method of phenylketonuria screening in Slovakia, which has brought substantial improvement in early detection of the disease and shortening time for definitive diagnosis since 1995 as well as the importance of a tandem MS/MS (mass spectrometry) introduced in the diagnosis of inherited metabolic disorders, is presented. The current state of phenylketonuria treatment focusing on low-protein dietary treatment and supplementation of amino acid mixtures is analysed. The use of sapropterin, enzyme replacement therapy, large neutral amino acids supplementation and gene therapy are also discussed.

Oto Ürge

A current view of the diagnostics and treatment of phenylketonuria in Slovakia

斯洛伐克苯丙酮尿症诊断与治疗现状

Abstract Pentoxifylline is a xanthine derivative used in the treatment of peripheral vascular disease, which because of its pharmacokinetic and pharmacologic profile is an ideal candidate for the development of extended release formulations. The aim of this study is to present a kinetic analysis of the pentoxifylline release from different extended release tablets formulations, using mechanistic and empirical kinetic models. A number of 28 formulations were prepared and analysed; the analysed formulations differed in the nature of the matrix forming polymers (hydrophilic, lipophilic, inert) and in their concentrations. Measurements were conducted in comparison with the reference product Trental 400 mg (Aventis Pharma). The conditions for the dissolution study were according to official regulations of USP 36: apparatus no. 2, dissolution medium water, volume of dissolution medium is 1,000 mL, rotation speed is 50 rpm, spectrophotometric assay at 274 nm. Six mathematical models, five mechanistic (0 orders, 1st-order release, Higuchi, Hopfenberg, Hixson-Crowell) and one empirical (Peppas), were fitted to pentoxifylline dissolution profile from each pharmaceutical formulation. The representative model describing the kinetics of pentoxifylline release was the 1st-order release, and its characteristic parameters were calculated and analysed.

Eleonora Mircia

Laurian Vlase

Gabriel Hancu

Monica Budău

Ruxandra Soare

Kinetic Modelling of Drug Release from Pentoxifylline Matrix Tablets based on Hydrophilic, Lipophilic and Inert Polymers

基于亲水性、疏水性和惰性聚合物的己酮可可碱缓释片释放动力学模型

Abstract Diabetes mellitus is a metabolic disorder characterised by hyperglycemia and oxidative stress. The aim of the present study is to explore the antioxidant effect of Spirulina maxima in rat model along with the histopathological observations. Diabetes was induced by feeding 10% fructose solution orally to Wistar rats (n = 6) for 30 days, analysed for plasma blood glucose and the markers of the oxidative stress [catalase (CAT), superoxide dismutase (SOD), reduced glutathione (GSH) and thiobarbituric acid reactive substances (TBARS)]. These biochemical studies were associated with histopathological examination of liver and kidney sections. The microalga Spirulina maxima being rich in proteins and other essential nutrients is widely used as a food supplement. S. maxima at a dose of 5 and 10% per kg and the metformin (500 mg/kg) as reference drug were given orally for 30 days to the diabetic rats. Diabetic rats showed significant (p &lt; 0.001) elevations in plasma blood glucose, thiobarbituric acid-reactive substances and significant reduction in catalase, superoxide dismutase and reduced glutathione activity. Oral administration of 5 and 10% aqueous extract of S. maxima for 30 days restored not only of blood glucose levels but also markers of oxidative stress. Histopathological observations of tissues manifested that the S. maxima administration had the protective and therapeutic effects against fructose-induced abnormalities in diabetic rats. It is concluded that S. maxima is effective in reinstating the antioxidant activity in addition to its antidiabetic effect in type 2 diabetic rats.

Urmila Jarouliya

Anish Zacharia

Raj K. Keservani

Godavarthi B.K.S Prasad

Spirulina maxima and its effect on antioxidant activity in fructose induced oxidative stress with histopathological observations

极大螺旋藻及其对果糖诱导氧化应激抗氧化活性的影响及组织病理学观察

出版信息	出版商: Univerzita Komenskeho，出版周期: ，期刊类型: journal，开源期刊: 否
基本数据	创刊年份: 2009，原创研究文献占比: ，自引率:， Gold OA占比:

Acta Facultatis Pharmaceuticae Universitatis Comenianae

期刊引文格式

有 1 位以上作者的期刊

有 2 位作者的期刊

有 3 位作者的期刊

有 5 位以上作者的期刊

书籍引用格式

学位论文引用格式

网页引用格式

专利引用格式

手工熬夜修改参考文献？研飞自动匹配期刊，一键轻松成稿，支持 Word/WPS

投稿经验分享