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Scientia Pharmaceutica

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https://www.readbyqxmd.com/read/28218683/antimutagenic-activity-of-ethanol-extract-of-rhaphidophora-pinnata-l-f-schott-leaves-on-mice
#1
Masfria, Sumaiyah, Aminah Dalimunthe
Rhaphidophora pinnata is suggested to prevent or treat cancer of genetic mutations. In this study, antimutagenic activity of an ethanol extract of Rhaphidophora pinnata leaves was evaluated by using a bone marrow micronucleus assay on mice. Male mice (20-30 g) were treated for sevendays with an ethanol extract of Rhaphidophora pinnata leaves at a dose of 500, 750 and 1000 mg/kg/day/orally, prior to exposure to cyclophosphamide (i.p. 30 mg/kg), 24 h after the end of the treatment. Antimutagenic activity was determined by the decrease of micronuclei (MN)...
February 17, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28212319/a-validated-stability-indicating-hplc-method-for-simultaneous-determination-of-amoxicillin-and-enrofloxacin-combination-in-an-injectable-suspension
#2
Nidal Batrawi, Shorouq Wahdan, Fuad Al-Rimawi
The combination of amoxicillin and enrofloxacin is a well-known mixture of veterinary drugs; it is used for the treatment of Gram-positive and Gram-negative bacteria. In the scientific literature, there is no high-performance liquid chromatography (HPLC)-UV method for the simultaneous determination of this combination. The objective of this work is to develop and validate an HPLC method for the determination of this combination. In this regard, a new, simple and efficient reversed-phase HPLC method for simultaneous qualitative and quantitative determination of amoxicillin and enrofloxacin, in an injectable preparation with a mixture of inactive excipients, has been developed and validated...
February 16, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28157163/transmission-electron-microscopy-of-xdr-mycobacterium-tuberculosis-isolates-grown-on-high-dose-of-o%C3%AF-oxacin
#3
Mohammad Arjomandzadegan, Maryam Sadrnia, Leonid Titov, Larissa Surkova, Hossein Sarmadian, Reza Ghasemikhah, Hossein Hosseiny
The aim of the study was to investigate behavior of resistant Mycobacterium tuberculosis (MTB) isolates under a high dose of ofloxacin and its morphological changes. 19 extensively drug resistant (XDR) clinical isolates of MTB were grown on Löwenstein-Jensen medium containing progressively increasing concentrations of ofloxacin (2, 4, 8, 16, 32 mg/L). Ultra-structure analyses of resistant isolates grown on ofloxacin were conducted by transmission electron microscopy (TEM). Fixation was carried out by 4% glutaraldehyde in 0...
February 2, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28134827/natural-products-as-new-treatment-options-for-trichomoniasis-a-molecular-docking-investigation
#4
Mary Snow Setzer, Kendall G Byler, Ifedayo Victor Ogungbe, William N Setzer
Trichomoniasis, caused by the parasitic protozoan Trichomonas vaginalis, is the most common non-viral sexually-transmitted disease, and there can be severe complications from trichomoniasis. Antibiotic resistance in T. vaginalis is increasing, but there are currently no alternatives treatment options. There is a need to discover and develop new chemotherapeutic alternatives. Plant-derived natural products have long served as sources for new medicinal agents, as well as new leads for drug discovery and development...
January 27, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28134775/chrysin-protects-rat-kidney-from-paracetamol-induced-oxidative-stress-inflammation-apoptosis-and-autophagy-a-multi-biomarker-approach
#5
Fatih Mehmet Kandemir, Sefa Kucukler, Eyup Eldutar, Cuneyt Caglayan, İlhami Gülçin
Paracetamol (PC) is a safe analgesic and antipyretic drug at therapeutic doses, and it is widely used in clinics. However, at high doses, it can induce hepatotoxicity and nephrotoxicity. Chrysin (CR) is a natural flavonoid that has biological activities that include being an antioxidant, an anti-inflammatory, and an anti-cancer agent. The main objective of this study was to investigate the efficacy of CR against PC-induced nephrotoxicity in rats. CR was given orally via feeding needle to male Sprague Dawley rats as a single daily dose of 25 or 50 mg/kg for six days...
January 26, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28085092/new-synthesis-structure-and-analgesic-properties-of-methyl-1-r-4-methyl-2-2-dioxo-1h-2%C3%AE-%C3%A2-1-benzothiazine-3-carboxylates
#6
Liliana Azotla-Cruz, Irina V Lijanova, Igor V Ukrainets, Natalya V Likhanova, Octavio Olivares-Xometl, Natalya L Bereznyakova
According to the principles of the methodology of bioisosteric replacements a series of methyl 1-R-4-methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxylates has been obtained as potential analgesics. In addition, a fundamentally new strategy for the synthesis of compounds of this chemical class involving the introduction of N-alkyl substituent at the final stage in 2,1-benzothiazine nucleus already formed has been proposed. Using nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry and X-ray diffraction analysis it has been proven that in the DMSO/K₂CO₃ system the reaction of methyl 4-methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxylate and alkyl halides leads to formation of N-substituted derivatives with good yields regardless of the structure of the alkylating agent...
January 12, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28054999/interaction-between-dna-and-drugs-having-protonable-basic-groups-characterization-through-affinity-constants-drug-release-kinetics-and-conformational-changes
#7
Liliana P Alarcón, Yolima Baena, Rubén H Manzo
This paper reports the in vitro characterization of the interaction between the phosphate groups of DNA and the protonated species of drugs with basic groups through the determination of the affinity constants, the reversibility of the interaction, and the effect on the secondary structure of the macromolecule. Affinity constants of the counterionic condensation DNA-drug were in the order of 10⁶. The negative electrokinetic potential of DNA decreased with the increase of the proportion of loading drugs. The drugs were slowly released from the DNA-drug complexes and had release kinetics consistent with the high degree of counterionic condensation...
January 4, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27918429/correction-budiarto-bugi-ratno-and-desriani-detection-of-her2-gene-polymorphism-in-breast-cancer-pcr-optimization-study-sci-pharm-2016-84-103-111
#8
Bugi Ratno Budiarto, Desriani
The authors wish to make the following corrections to their paper [1]:[...].
December 2, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27916830/influence-of-fragrances-on-human-psychophysiological-activity-with-special-reference-to-human-electroencephalographic-response
#9
REVIEW
Kandhasamy Sowndhararajan, Songmun Kim
The influence of fragrances such as perfumes and room fresheners on the psychophysiological activities of humans has been known for a long time, and its significance is gradually increasing in the medicinal and cosmetic industries. A fragrance consists of volatile chemicals with a molecular weight of less than 300 Da that humans perceive through the olfactory system. In humans, about 300 active olfactory receptor genes are devoted to detecting thousands of different fragrance molecules through a large family of olfactory receptors of a diverse protein sequence...
November 29, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27869754/a-comparative-pharmacokinetics-study-of-the-anti-parkinsonian-drug-pramipexole
#10
Ratih S I Putri, Effi Setiawati, Syifa A Aziswan, Fenny Ong, Raymond R Tjandrawinata, Liana W Susanto
The present study aimed to compare pharmacokinetic parameters of two pramipexole 0.25 mg formulations in order to show bioequivalence. The study was conducted in a randomized, open-label, two-period, two-sequence, and crossover design, involving 23 healthy volunteers. One of the 0.25 mg formulations of pramipexole evaluated in the study was manufactured by PT Dexa Medica, Palembang, Indonesia, the other, used as the reference, by Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim am Rhein, Germany. All eligible subjects were required to fast before each drug administration period, which was separated by a one-week washout period...
November 18, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27775559/synthesis-spatial-structure-and-analgesic-activity-of-sodium-3-benzylaminocarbonyl-1-methyl-2-2-dioxo-1h-2%C3%AE-%C3%A2-1-benzothiazin-4-olate-solvates
#11
Igor V Ukrainets, Lidiya A Petrushova, Svitlana V Shishkina, Lina A Grinevich, Galina Sim
In order to obtain and then test pharmocologically any possible conformers of the new feasible analgesic N-benzyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxamide, its 4-O-sodium salt was synthesized using two methods. X-ray diffraction study made possible to determine that, depending on the chosen synthesis conditions, the above-mentioned compound forms either monosolvate with methanol or monohydrate, where organic anion exists in the form of three different conformers. Pharmacological testing of the two known pseudo-enantiomeric forms of the original N-benzylamide and of the two solvates of its sodium salt was performed simultaneously under the same conditions and in equimolar doses...
October 19, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27763573/effect-of-cyclodextrin-types-and-co-solvent-on-solubility-of-a-poorly-water-soluble-drug
#12
Suporn Charumanee, Siriporn Okonogi, Jakkapan Sirithunyalug, Peter Wolschann, Helmut Viernstein
The aim of the study was to investigate the solubility of piroxicam (Prx) depending on the inclusion complexation with various cyclodextrins (CDs) and on ethanol as a co-solvent. The phase-solubility method was applied to determine drug solubility in binary and ternary systems. The results showed that in systems consisting of the drug dissolved in ethanol-water mixtures, the drug solubility increased exponentially with a rising concentration of ethanol. The phase solubility measurements of the drug in aqueous solutions of CDs, β-CD and γ-CD exhibited diagrams of AL-type, whereas 2,6-dimethyl-β-CD revealed AP-type...
October 18, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27763572/destabilization-mechanism-of-ionic-surfactant-on-curcumin-nanocrystal-against-electrolytes
#13
Heni Rachmawati, Annisa Rahma, Loaye Al Shaal, Rainer H Müller, Cornelia M Keck
We have successfully developed curcumin nanosuspension intended for oral delivery. The main purpose is to improve bioavailability through enhancing its solubility. The nanoparticles were stabilized using various stabilizers, including polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA), sodium carboxymethylcellulose (Na-CMC), d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), and sodium dodecyl sulfate (SDS). The average diameter of particles, microscopic appearance, and sedimentation of each preparation was observed and compared...
October 18, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27763526/analytical-enantio-separation-of-linagliptin-in-linagliptin-and-metformin-hcl-dosage-forms-by-applying-two-level-factorial-design
#14
Sushant B Jadhav, Rahul M Mane, Kalyanraman L Narayanan, Popatrao N Bhosale
A novel, stability indicating, reverse phase high-performance liquid chromatography (RP-HPLC) method was developed to determine the S-isomer of linagliptin (LGP) in linagliptin and metformin hydrochloride (MET HCl) tablets (LGP-MET HCl) by implementing design of experiment (DoE), i.e., two-level, full factorial design (2³ + 3 centre points = 11 experiments) to understand the critical method parameters (CMP) and its relation with the critical method attribute (CMA), and to ensure robustness of the method. The separation of the S-isomer, LGP and MET HCl in the presence of their impurities was achieved on Chiralpak(®) IA-3 (Amylose tris (3, 5-dimethylphenylcarbamate), immobilized on 3 µm silica gel) stationary phase (250 × 4...
October 17, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27754407/development-and-validation-of-miglitol-and-its-impurities-by-rp-hplc-and-characterization-using-mass-spectrometry-techniques
#15
Kesavan Balakumaran, Mosesbabu Janagili, Nagaraju Rajana, Sureshbabu Papureddy, Jayashree Anireddy
Alpha glucoside inhibitors used to treat type-2 diabetes mellitus (DM) are likely to be safe and effective. These agents are most effective for postprandial hyperglycemia. Miglitol is a type of drug used to treat type-2 DM. A simple, selective, linear, precise and accurate reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed and validated for a related substance of miglitol and its identification, and characterization was done by different mass spectrometry techniques. The gradient method at a flow rate of 1...
October 14, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27727195/evaluation-of-certain-pharmaceutical-quality-attributes-of-lisinopril-split-tablets
#16
Khairi M S Fahelelbom, Moawia M M Al-Tabakha, Nermin A M Eissa, Jeevani Javadi
Tablet splitting is an accepted practice for the administration of drugs for a variety of reasons, including dose adjustment, ease of swallowing and cost savings. The purpose of this study was to evaluate the physical properties of lisinopril tablets as a result of splitting the tablets either by hand or with a splitting device. The impact of the splitting technique of lisinopril (Zestril(®) tablets, 20 mg) on certain physical parameters such as weight variation, friability, disintegration, dissolution and drug content were studied...
October 11, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28117319/investigation-of-the-bioequivalence-of-rosuvastatin-20-mg-tablets-after-a-single-oral-administration-in-mediterranean-arabs-using-a-validated-lc-ms-ms-method
#17
Abdel Naser Zaid, Rowa Al Ramahi, Rita Cortesi, Ayman Mousa, Nidal Jaradat, Nadia Ghazal, Rana Bustami
There is a wide inter-individual response to statin therapy including rosuvastatin calcium (RC), and it has been hypothesized that genetic differences may contribute to these variations. In fact, several studies have shown that pharmacokinetic (PK) parameters for RC are affected by race. The aim of this study is to demonstrate the interchangeability between two generic RC 20 mg film-coated tablets under fasting conditions among Mediterranean Arabs and to compare the pharmacokinetic results with Asian and Caucasian subjects from other studies...
June 30, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28117318/synthesis-structure-and-analgesic-properties-of-halogen-substituted-4-hydroxy-2-2-dioxo-1h-2%C3%AE-%C3%A2-1-benzothiazine-3-carboxanilides
#18
Igor V Ukrainets, Lidiya A Petrushova, Svitlana V Shishkina, Lyudmila V Sidorenko, Galina Sim, Olga V Kryvanych
As potential new analgesics, the corresponding 4-hydroxy-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxanilides have been obtained by amidation of ethyl 4-hydroxy-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxylate with aniline and its halogenated analogsin boiling dry xylene. The peculiarities of the mass and nuclear magnetic resonance (¹Н and (13)С) spectra of the synthesized compounds are discussed. Using X-ray diffraction analysis, the ability of the compounds to form stable solvates with N,N-dimethylformamide has been shown on the example of 4-bromo-substituted derivative...
June 17, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28117317/bioequivalence-study-of-two-orodispersible-rizatriptan-formulations-of-10-mg-in-healthy-volunteers
#19
Mercè Cánovas, Francisco Polonio, Francesc Cabré
The aim of the study was to assess the bioequivalence and tolerability of two different oral formulations of rizatriptan. A bioequivalence study was carried out in 40 healthy volunteers according to an open label, randomized, two-period, two-sequence, crossover, single dose, and fasting conditions design. The test and reference formulations were administered in two treatment days, separated by a washout period of seven days. Plasma concentrations of rizatriptan were obtained by the LC/MS/MS (Liquid chromatography tandem-mass spectrometry) method...
June 13, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28117316/anomalous-separation-of-small-y-chromosomal-dna-fragments-on-microchip-electrophoresis
#20
Mohammad Jabasini, Ashraf Ewis, Youichi Sato, Yutaka Nakahori, Yoshinobu Baba
We investigated an anomalous DNA separation where two DNA fragments from the human Y-chromosome sY638 (64 bp) and sY592 (65 bp), with only one base pair difference, were separated. This result is abnormal since in a previous study, we found that 5 bp was the minimum difference between two DNA fragments that the microchip electrophoresis system can separate. The formation of a mini-loop in the structure of the DNA fragment of sY638 (64 bp) was strongly expected to be the reason. To investigate this, we synthesized three modified DNA fragments for sY638 (64 bp), and the modifications were in two expected locations for possible mini-loop formation...
May 26, 2016: Scientia Pharmaceutica
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