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Acta Pharmaceutica

Ahmed Refaat, Magda Sokar, Fatma Ismail, Nabila Boraei
Quetiapine (QT) is a short acting atypical antipsychotic drug effective in schizophrenia and bipolar disorder. This study aims at designing a novel dosage form of sustained release taste-masked QT orally disintegrating tablets (ODTs) based on solid lipid micro-pellets (SLMPs). QT SLMPs were prepared using the hot melt extrusion technique and utilizing three lipid carriers: Compritol, Precirol and white beeswax either alone or in mixtures. They showed sustained QT release and a taste masking effect. The selected QT SLMP was further blended with an aqueous solution containing polyvinylpyrollidone (2...
December 1, 2016: Acta Pharmaceutica
Zhaoxiang Zhou, Meng Wang, Zengjun Guo, Xiaoying Zhang
This study was aimed at investigating the effect of ethanol on oral bioavailability of kaempferol in rats, namely, at disclosing their possible interaction. Kaempferol (100 or 250 mg kg-1 bm) was administered to the rats by oral gavage with or without ethanol (600 mg kg-1 bm) co-administration. Intravenous administration (10 and 25 mg kg-1 bm) of kaempferol was used to determine the bioavailability. The concentration of kaempferol in plasma was estimated by ultra high performance liquid chromatography. During coadministration, a significant increase of the area under the plasma concentration-time curve as well as the peak concentration were observed, along with a dramatic decrease in total body clearance...
December 1, 2016: Acta Pharmaceutica
Fugen Gu, Weina Ma, Gendalai Meng, Chunzhi Wu, Yi Wang
The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax', cmax and AUC of oral and nasal routes were significantly different (p < 0...
December 1, 2016: Acta Pharmaceutica
Said A Hassan, Eman S Elzanfaly, Salem Badr A El-Zeany, Maissa Y Salem
Two methods were developed for separation and quantitation of amlodipine (AML) and atorvastatin (ATV) in the presence of their acidic degradation products. The first method was a simple isocratic RP-HPLC method while the second was capillary electrophoresis (CE). Degradation products were obtained by acidic hydrolysis of the two drugs and their structures were elucidated for the first time by IR and MS spectra. Degradation products did not interfere with the determination of either drug and the assays were therefore stability-indicating...
December 1, 2016: Acta Pharmaceutica
Miroslav Zeman, Marek Vecka, František Perlík, Barbora Staňková, Robert Hromádka, Eva Tvrzická, Jakub Širc, Jakub Hrib, Aleš Žák
Niacin was the first hypolipidemic drug to significantly reduce both major cardiovascular events and mortality in patients with cardiovascular disease. Niacin favorably influences all lipoprotein classes, including lipoprotein[a],and belongs to the most potent hypolipidemic drugs for increasing HDL-C. Moreover, niacin causes favorable changes to the qualitative composition of lipoprotein HDL. In addition to its pronounced hypolipidemic action, niacin exerts many other, non-hypolipidemic effects (e.g., antioxidative, anti-inflammatory, antithrombotic), which favorably influence the development and progression of atherosclerosis...
December 1, 2016: Acta Pharmaceutica
Beata Bergler-Czop, Monika Bilewicz-Stebel, Anna Stańkowska, Teresa Bilewicz-Wyrozumska
Retinoids are compounds chemically related to vitamin A, which are frequently used in dermatological practice (1). They are characterized by numerous mechanisms of action leading to normalization of keratinocyte proliferation and maturation. They have anti-seborrhoeic, immunomodulatory and anti-inflammatory effects (1, 2). A number of side effects to retinoid treatment have been recorded; one group of such side effects relates to eyes and vision. Dry eye syndrome and blepharoconjunctivitis are the most common side effects, appearing in 20-50 % of patients treated with retinoids...
December 1, 2016: Acta Pharmaceutica
Sedar Karakurt
Expression of a drug and xenobiotic metabolizing enzymes, cytochrome P450s (CYPs), and antioxidant enzymes can be modulated by various factors. The flavonoid rutin was investigated for its anti-carcinogen and protective effects as well as modulatory action on CYPs and phase II enzymes in human hepatocellular carcinoma cells. Rutin inhibited proliferation of HEPG2 cells in a dose-dependent manner with the IC50 value of 52.7 μmol L-1 and invasion of HEPG2 cells (21.6 %, p = 0.0018) and colony formation of those invaded cells (57...
December 1, 2016: Acta Pharmaceutica
Haitham Alrabiah, Abdulrahman Al-Majed, Mohammed Abounassif, Gamal A E Mostafa
The fabrication and development of two polyvinyl chloride (PVC) membrane sensors for assaying phenobarbitone sodium are described. Sensors 1 and 2 were fabricated utilizing β- or γ-cyclodextrin as ionophore in the presence of tridodecylmethylammonium chloride as a membrane additive, and PVC and dioctyl phthalate as plasticizer. The analytical parameters of both sensors were evaluated according to the IUPAC guidelines. The proposed sensors showed rapid, stable anionic response (-59.1 and -62.0 mV per decade) over a relatively wide phenobarbitone concentration range (5...
December 1, 2016: Acta Pharmaceutica
Loretta Pobłocka-Olech, Daniel Głód, Maria E Żebrowska, Małgorzata Sznitowska, Miroslawa Krauze-Baranowska
This study comprises the optimization and validation of a new TLC method for determination of flavonols in the bulbs of seven cultivars of onions and shallots. Separation was performed on RP-18 plates with the solvent mixture tetrahydrofuran/water/formic acid (40+60+6, V/V/V) as a mobile phase. The method was evaluated for precision, linearity, LOD, LOQ, accuracy and robustness. Chromatographic analysis of the extracts revealed the presence of three main flavonols, quercetin, quercetin-4'-O-glucoside and quercetin-3,4'-O-diglucoside in the majority of analyzed cultivars...
December 1, 2016: Acta Pharmaceutica
Moamen S Refat, Hosam A Saad, Abdel Majid A Adam, Mohamed A Al-Omar, Ahmed M Naglah
The topic of charge-transfer (CT) complexation of vital drugs has attracted considerable attention in recent years owing to their significant physical and chemical properties. In this study, CT complexes derived from the reaction of the anti-hyperuricemic drug allopurinol (Allop) with organic p-acceptors [(picric acid (PA), dichlorodicyanobenzoquinone (DDQ) and chloranil (CHL)] were prepared, isolated and characterized by a range of physicochemical methods, such as IR, Raman, 1H NMR and 13C NMR spectroscopy...
December 1, 2016: Acta Pharmaceutica
David Calderón Guzmán, Norma Osnaya Brizuela, Maribel Ortíz Herrera, Ernestina Hernández García, Gerardo Barragán Mejía, Hugo Juárez Olguín, Armando Valenzuela Peraza, Jonas Attilus, Norma Labra Ruíz
The study tested the hypothesis that cerebrolysin protects the brain from free radicals in rats treated with 3-nitropropionic acid (3-NPA). To address this hypothesis, the levels of dopamine (DA) and some oxidative stress biomarkers were measured after administration of 3-NPA. Young male Fischer rats were treated for three days with cerebrolysin, 3-NPA or both substances. Their brains were extracted, and DA, lipid peroxidation (LP), glutathione (GSH), calcium, and H2O2 were measured using validated methods...
September 1, 2016: Acta Pharmaceutica
Jitka Mužíková, Alena Kubíčková
The paper evaluates and compares the compressibility and compactibility of directly compressible tableting materials for the preparation of hydrophilic gel matrix tablets containing tramadol hydrochloride and the coprocessed dry binders Prosolv® SMCC 90 and Disintequik™ MCC 25. The selected types of hypromellose are Methocel™ Premium K4M and Methocel™ Premium K100M in 30 and 50 % concentrations, the lubricant being magnesium stearate in a 1 % concentration. Compressibility is evaluated by means of the energy profile of compression process and compactibility by the tensile strength of tablets...
September 1, 2016: Acta Pharmaceutica
Gleysson De Paula Terra, Marcus Vinícius De Farias, Marcello Garcia Trevisan, Jerusa Simone Garcia
Pancreatin is a biotechnological product containing an enzyme complex, obtained from porcine pancreas, that is employed in treating pancreatic diseases. Experiments regarding the stability of the pharmaceutical formulation containing pancreatin were performed using standard binary mixtures with 6 excipients in a 1:1 ratio (m/m) and a commercial formulation. To accomplish these goals, samples were stored for 1, 3 and 6 months at 40 ± 1 °C and 75 ± 5 % relative humidity (RH) and 40 ± 1 °C and 0 % RH. Stress testing was also performed...
September 1, 2016: Acta Pharmaceutica
Nataša Zorić, Nevenka Kopjar, Klara Kraljić, Nada Oršolić, Siniša Tomić, Ivan Kosalec
Olive leaf extract is characterized by a high content of polyphenols (oleuropein, hydroxytyrosol and their derivatives), which is associated with its therapeutic properties. The objective of the present research was to evaluate the antifungal activity of olive leaf extract against Candida albicans ATCC 10231 and C. dubliniensis CBS 7987 strains. Minimum inhibitory concentrations (MIC) of the extract were determined by several in vitro assays. The extract showed a concentration depended effect on the viability of C...
September 1, 2016: Acta Pharmaceutica
Peace Mabeta
PF573,228 is a compound that targets focal adhesion kinase (FAK), a non-receptor protein kinase, which is over-expressed in various tumors. The aim of this study was to evaluate the effects of PF573,228 on the cells derived from mouse vascular tumors, namely, endothelioma cells. The treatment of endothelioma cells with PF573,228 reduced their growth with an IC50 of approximately 4.6 μmol L-1 and inhibited cell migration with an IC50 of about 0.01 μmol L-1. Microscopic studies revealed morphological attributes of apoptosis...
September 1, 2016: Acta Pharmaceutica
Ezzat Abdel-Lateef, Faten Mahmoud, Olfat Hammam, Eman El-Ahwany, Eman El-Wakil, Sherihan Kandil, Hoda Abu Taleb, Mortada El-Sayed, Hanaa Hassenein
The present study was designed to identify the chemical constituents of the methanolic extract of Curcuma longa L. rhizomes and their inhibitory effect on a hepatoma cell line. The methanolic extract was subjected to GC-MS analysis to identify the volatile constituents and the other part of the same extract was subjected to liquid column chromatographic separation to isolate curcumin. The inhibition of cell growth in the hepatoma cell line and the cytopathological changes were studied. GC-MS analysis showed the presence of fifty compounds in the methanolic extract of C...
September 1, 2016: Acta Pharmaceutica
Suphannee Thanyaphoo, Jasadee Kaewsrichan
Silicon-substituted calcium phosphate (Si-CaP) was developed in our laboratory as a biomaterial for delivery in bone tissue engineering. It was fabricated as a 3D-construct of scaffolds using chitosan-trisodium polyphosphate (TPP) cross-linked networks. In this study, heparin was covalently bonded to the residual -NH2 groups of chitosan on the scaffold applying carbodiimide chemistry. Bonded heparin was not leached away from scaffold surfaces upon vigorous washing or extended storage. Recombinant human bone morphogenetic protein 2 (rhBMP-2) was bound to conjugated scaffolds by ionic interactions between the negatively charged SO42- clusters of heparin and positively charged amino acids of rhBMP-2...
September 1, 2016: Acta Pharmaceutica
Ashok K Shakya, Mehnaz Kamal, Vishal M Balaramnavar, Sanna K Bardaweel, Rajashri R Naik, Anil K Saxena, H H Siddiqui
A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran- 3-yl)-2-(substituted)-acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg-1 body mass during 0...
September 1, 2016: Acta Pharmaceutica
Hend N Hafez, Abdel-Rhman B A El-Gazzar, Magdi E A Zaki
6'-(4-Chlorophenyl)-spiro[cyclohexane-1,2'-thieno[3,2-d][1,3] oxazin]-4'(1'H)-one (1) was synthesized and used as a starting material for the synthesis of a novel series of spiro compounds having biologically active sulfonamide 2a-e and 3'-(4-acetylphenyl)-6'- (4-chlorophenyl)-1'H-spiro[cyclohexane-1,2'-thieno[3,2-d] pyrimidine-4'(3'H)-one (3). Compound 2a was used as a key intermediate for the synthesis of sulfonyl carbothioamide derivatives 4a-c. Also, compound 3 was used as an intermediate for the synthesis of 3'H-spiro[cyclohexane-1,2'-thieno[3,2-d]pyrimidin]-3'-yl] phenyl}-2-imino-4-(substituted phenyl and/or thienyl)-1,2-dihydropyridine- 3-carbonitrile derivatives 5a-e, 3'H-spiro[cyclohexane- 1,2'- thieno[3,2-d]pyrimidin]-3'-yl]phenyl}-2-oxo-4-(substituted phenyl and/or thienyl)-1,2-dihydropyridine-3-carbonitrile derivatives 6a-e, and 4-[(2Z)-3-substituted-arylprop-2-enoyl] phenyl-1'H-spiro[cyclohexane-1,2'-thieno[3,2-d]pyrimidine derivatives 7a-e...
September 1, 2016: Acta Pharmaceutica
Mateja Egart, Biljana Janković, Stane Srčič
Nanoindentation allows quantitative determination of a material's response to stress such as elastic and plastic deformation or fracture tendency. Key instruments that have enabled great advances in nanomechanical studies are the instrumented nanoindenter and atomic force microscopy. The versatility of these instruments lies in their capability to measure local mechanical response, in very small volumes and depths, while monitoring time, displacement and force with high accuracy and precision. This review highlights the application of nanoindentation for mechanical characterization of pharmaceutical materials in the preformulation phase (primary investigation of crystalline active ingredients and excipients)...
September 1, 2016: Acta Pharmaceutica
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