Abbas, Mateen; Khan, Abdul M.; Waheed, Naila; Riffat, Sualeha; Ashraf, Muhammad; Amin, Sadia
The study was conducted to evaluate the bioequivalence of deferiprone 500 mg with innovator drug in Pakistani men. Twenty four healthy volunteers were enrolled in this study. Each volunteer
take two tablets of generic and innovator deferiprone with two-week washout period. Blood samples were
collected at predetermined time intervals. Plasma deferiprone levels were analyzed using validated HPLC
method. Pharmacokinetic parameters computed non-compartmentally after logarithmic transformation
of data. The mean relative bioavailability was 104 %. The mean Cmax
, AUC0–∞ for generic drug
were 14.41, 40.49, and 42.84 μg.h/mL and for innovator were 12.68, 38.63, and 40.75 μg.h/mL, respectively. Mean ratio (generic/innovator) of AUC0–t
at 90 %...
Gómez Lobón, Ana; Delgado Sánches, Olga; Modamio, Pilar; Álvarez Arroyo, Laura; Campoamor Ladín, Francisco; Mariño, Eduardo L.
An intervention study of 3 months was performed at a third-level university hospital to investigate if drug adjustment interventions towards chronic kidney disease (CKD) patients are still needed.
Patients with a glomerular filtration rate < 60 mL/min/1.73 m2
and a prescribed medication that needed
an adjustment for CKD were selected. Demographic and clinical data, prescription information, non-adjusted medication, interventions, and acceptance of recommendation were registered. A total of 706 patients were included (77.5 % stage 3 of CKD, 13.2 % stage 4 and 7.2 % stage 5), 281 (8.5 %) of 3,315 prescriptions were considered non-adjusted (52.3 % stage 3, 28.8 % stage...
Li, Li; Gui, Yuge; Wang, Jing; Zong, Xiaofei; Zhang, Huirong; Liu, Chun Ming
The present work describes a liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) method for rapid identification of four chromones, prim-O-glucosylcimifugin, 4’-O-
β-D-glucosyl-5-O-methylvisamminol, cimifugin and 5-O-methylvisamminol in the seeds extract from
Saposhnikovia divaricata for the first time. By using a binary mobile phase system consisting of 0.5 %
acetic acid and acetonitrile under gradient conditions, a good separation was achieved in 25 min. The
ions, the [2M+Na]
ions, the molecular weights, and the fragment ions of the four chromones were
obtained in the positive ion mode using LC-ESI-MS. The identification of the chromones (peaks 1-4) in
seeds extract of S. divaricata was based on matching their retention times, the...
Amir, Faheem; Wong, Keng C.; Eldeen, Ibrahim M.; Asmawi, Mohammad Z.; Osman, Hasnah
The volatile constituents of the flowers of Mumusops elengi were isolated by hydrodistllation
and identified by capillary GC and GC-MS. The most abundant components were 2-phenylethanol (29.8
%), (E)-2-hexenal (11.8 %) and benzyl alcohol (10.4 %). The flower volatiles were tested for antibacterial
activity using the micro-dilution antibacterial assay, and anti-inflammatory activity using the cyclooxygenase inhibitory screening assay. The flower oil showed antibacterial activity against Gram-negative bacteria (78-156 μg/mL) and selective COX-1 inhibition was observed for the flower oil. This present report is
the first describing the anti-inflammatory potential of M. elengi flowers. The results of this study support
the traditional uses of the plant...
Peng, You; Li, Xue-Qin; Hu, Xiao-Ming
7-Enthyl-4’-phenylsulfonyldaidzein (EPD 3), a potential prodrug for daidzein, was synthesized in high yield and its crystal structure was reported firstly. It possesses better physical and chemical properties such as solubility, lipid/water partition coefficient LogP, and hydrolysis kinetics than its original form. The LogP value (3.07) and the half-life of the hydrolysis value (24.06 h) show that its oral bioavailability is possibly improved evidently compared with that of daidzein. These results indicate that EPD can be considered a potential prodrug for daidzein.
Ding, Xitao; Zhang, Qingwei; Wang, Zhiyi; Lin, Guanyang
A selective liquid chromatography-mass spectrometry (LC–MS) method for determination of febuxostat in rat plasma was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 x150 mm, 5 μm) using 0.1% formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragment ions m/z 317 for febuxostat and m/z 326 for midazolam (internal standard, IS). The assay was linear over...
Oliveira, Amanda T. C.; Santana, Davi P.; Alencar, Joao Rui B.; Ribas, Lais A.S.; Monteiro, Deborah B.; Santos, Bruno A.; Oliveira, Antônio D. P.; Santana, Aíla K.M.
This work evaluated the cleanliness of equipment involved in manufacturing the product
LAFEPE Zidovudine (AZT) + Lamivudine (3TC) 300 mg + 150 mg coated tablets in a antiretroviral plant.
A method for simultaneous determination of AZT+3TC in High Performance Liquid Chromatography
HPLC-UV is selective and presented a linear range from 2.5 to 15 μg/mL, and Limit of Detection (LOD)
(AZT: 0.13 μg/mL; 3TC: 0.15 μg/mL) and Limit of Quantification (LOQ) (AZT: 0.20 μg/mL; 3TC: 0.23
μg/mL). Recoveries of 82.00 and 83.00 % for the active AZT and 3TC, respectively, were obtained with
the use of swab on stainless steel surfaces 316L. The method of cleaning and...
Sousa, Carlos E.M.; Bonifácio, F. N.; Bedor, Danilo C. G.; Silva, T. M.; Ramos, Virna L.S.; Souza Filho, J. P.; Leal, Leila B.; Oliveira, Amanda T. C.; Santana, Davi P.
A rapid (3.0 min) and sensitive (LLOQ 0.5 ng/mL) analytical method for the quantitation of
Escitalopram (ETP) in human plasma is described. The method is based on High-Performance Liquid
Chromatography-Tandem Mass Spectrometry (LC-MS/MS) using paroxetine as internal standard (I.S.).
Sample preparation involved precipitation extraction with acetonitrile. The chromatographic separation
was achieved on a ACE C18 (125 x 4,6 mm) reversed-phase column and a mobile phase containing acetonitrile/water (60:50 v/v, add 0.2 % formic acid), in isocratic conditions. The target analytes were transferred into a triple quadrupole mass spectrometer equipped with an electrospray ionization source for
mass detection. The ion transitions selected for MRM detection were:...
Chen, Yin; Hu, Shilian; Shen, Gan; Wu, Lei; Xu, Weiping; Wang, Li; Li, Youping
The aim of this study was to assess the prescribing pattern of antihypertensive treatment among inpatients with uncomplicated and complicated hypertension at Anhui Provincial Hospital (First Class Public Hospital) in the central region of China in accordance with the recommendations of current international guidelines. A retrospective cross-sectional study was performed from 1 January to 31 December, 2009. A total of 2010 hypertensive inpatients were included. Among 683 inpatients receiving monotherapy, calcium channel blockers (CCBs) were the most frequently drugs used in uncomplicated hypertensive patients (57.41 %) and those with stroke (61.73 %). Beta-blockers (BBs) (27.90 %) and angiotensin-converting enzyme inhibitors...
Pang, Lingxia; Wang, Qing; Wang, Youpei; Zheng, Meiqin; Wu, Haiya; Wang, Zhiyi
A selective and sensitive liquid chromatography-mass spectrometry (LC–MS) method for determination of ondansetron in rat plasma was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 x 150 mm, 5 μm) using 0.1 % formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and multiple reaction monitoring (MRM) mode was used for quantification of target fragment
ions m/z 294.0→169.7 for ondansetron and m/z 326.0→291.0 for midazolam (internal standard, IS). The
Lu, Jie; Liu, Zhen; Wang, Jing
The solid-state characterization, dimorphic nature, solubility and solvent-mediated transformation of the anhydrous form and the monohydrate form of L-phenylalanine have been firstly conducted
in detail. The results have shown that, the two forms are enantiotropically related, and the transformation
rate can be prohibited by increasing temperature and reducing water content in the solvent mixtures.
These results will contribute to a better understanding about the pseudopolymorphic systems for pharmaceutical industry.
Rule, Roberto; Petinelli, A.; Cordiviola, C.; Prozzi, Guillermo Rafael; Farina, Osvaldo H.; Villagra, Sergio
The aim of this study was to determine the kinetic behaviour and the safety of cefepime administered to rabbits. For this, rabbits (n = 29) were used and distributed in Groups 1 (G1), 2 (G2) and
Control (CG). Animals from G1 (n = 21) received a monodose of cefepime intravenously, (20 mg/kg
weight) and, after this, blood samples were collected, controlling the time. Rabbits from Group G2 (n = 4)
received multidoses of cefepime (20 mg/kg weight, intravenously), and blood and urine samples were taken
in order to analyse them. Animals from Groups G2 and CG were controlled electrocardiographically
(ECG) throughout the treatment. Rabbits from...
Shrivatava, Alankar; Gupta, Vipin B.
Alpha-blockers (alfuzosin, tamsulosin, doxazosin, prazosin and terazosin) relax the smooth
muscles in the prostate and are indicated for the symptomatic treatment of benign prostatic hyperplasia
due to evidence of their positive and rapid effect on lower urinary tract symptoms. Our objective was to
develop and validate simultaneous estimation of these drugs. Same class of drugs may have almost same
functional groups and therefore research focused on development of RPLC and HPTLC method for simultaneous quantitative determination. The separation was achieved in HPLC method on a C18 column, a
UV detector at 230 nm and a elution was performed under a gradient mobile phase composed of...
Muhammad, Iyad N.; Yousuf, Rabia I.; Hanif, Muhammad; Shoaib, Muhammad Harris; Jabeen, Sabahat; Ali, Tariq
Cefuroxime axetil (CA) immediate release (IR) tablets were developed and optimized by direct compression method. Ten formulations were designed and optimized using central composite design with two main variables, microcrystalline cellulose PH 102 and croscarmellose. Pharmaceutical evaluation of the formulations was conducted emphasizing on dissolution profile of the drug by USP dissolution test using apparatus II in 0.07 N HCl and in medium of pH 1.2, 4.5 and 6.8 to determine the dissolution pattern of the low soluble drug. Test formulations were compared against reference brand using f2 similarity factor. Test formulations were assayed by a validated HPLC method, with...
Araujo, Rian F. M.; Coelho, Mayara L.; Soares, Mônica F.L.R.; Rolim, Larissa A.; Neto, Pedro; Soares Sobrinho, José L.
Dapsone is the drug of choice for leprosy treatment. Despite the existence of previous analytical methods, this study aimed to develop a new analytical alternative for dapsone quantification by UV spectrophotometry. Since the pharmacopeial method uses methanol, a toxic solvent, the method was developed using first dilution in ethanol (500 μg/mL) and second dilution in water (5 μg/mL), with quantification in 295 nm. For validation, the specificity was confirmed by quantification of degraded samples using the developed method in comparison with a second analytical technique (HPLC-DAD). The proposed method proved to be specific, linear, precise, accurate and robust, with analytical...
Oliveira, Débora M. F.; Kikuchi, Irene S.; Moreira, Adir J.; Silva, Juliano M. F.; Pinto, Terezinha J. A.; Mansano, Ronaldo D.
New technologies and sterilization agents for heat-sensitive materials are under intense investigation. Plasma sterilization, an atoxic low-temperature substitute for conventional sterilization, uses various gases that are activated by an electrical discharge, generating reactive species that promote lethality
in microorganisms. Here, assays were performed using pure O2
+ H2O2 mixture gas plasmas
against a standard load of Bacillus atrophaeus spores inoculated on glass carriers inside PVC catheters.
The sterilization efficiency was studied as a function of plasma system (reactive ion etching or inductively
coupled plasma), biological monitor lumen diameter, gas, radio frequency power, and sub-lethal exposition time. After sterilization, the biological monitors were disassembled and...
Li, Ming; Yuan, Jinbin; Chen, Heifang; Yang, Wuliang; Luo, Xiaoquan; Liu, Yingin; Zhang, Yu
A simple and sensitive high-performance liquid chromatography (HPLC) method was developed and validated for the determination of auraptene (AUR) in dog plasma. The chromatographic separation of AUR was achieved on a C18 column using isocratic elution with acetonitrile-0.1 % formic acid
(volume ratio 84.5:15.5). AUR was detected at 322 nm. Sample extraction with ethyl acetate resulted in
high recoveries of AUR. A linear curve over the concentration range 10.2-408.8 ng/mL (r2
= 0.9995) was
obtained. Satisfactory intra-day and inter-day precisions were achieved with RSDs less than 9.5 % and the
average recovery factors were in the range of 99.1-106.2 %....
Plessing, Carlos von; Torres, Pablo; Rivas, Coralia; Guzmán, Paula; Núñes, Christian; Sepúlveda, Jacqueline
The effect of N-trimethylchitosan chloride on the intestinal permeability of capreomycin sulfate, a polypeptide antibiotic, using an in vitro model, was evaluated. To improve the mucoadhesivity and permeation enhancer properties of N-trimethylchitosan chloride, it was used a synthetic pathway that selectively alkylated the amino groups and not the hydroxyl groups in carbons 3 and 6, which decreases the potency of the polymer, leading to use higher quantities and limit its potential as a functional excipient.
This non-methoxylated derivative of the studied polymer reduced in a reversible way the transepithelial electrical resistance of CaCo-2 monolayers at concentrations not higher than 0.003 %...
Wang, Jinjin; Wang, Zhibin; Wang, Zhiyi; Chen, Chan; Liu, Naihua; Ma, Jianshe; Wang, Xianqin; Hu, Lufeng
A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of cilostazol in rat plasma using one-step protein precipitation was developed.
After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographic separation was achieved on an SB-C18 (2.1 × 50 mm, 5.0 μm) column with acetonitrile-0.1 % formic acid as mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantification using target fragment ions m/z 370.0 for cilostazol and m/z 325.9 for the IS. Calibration...
Neto, Eraldo A. G.; Araújo, Janete M.; Rodrigues, Maria D.; Silva, Teresinha G.; Nascimento, Silene C.; Militão, Gardênia C.G.; Góes, Alexandre J. S.; Lima, José G.
A novel series of 5-benzylidene-2-[(pyridine-2-ylmethylene)hydrazono]-thiazolidin-4-ones 3a-i has
been synthesized. 2-[(Pyridine-2-ylmethylene)hydrazono]-thiazolidin-4-ones 2a-c were also obtained and used as
intermediates to give the target compounds. The in vitro cytotoxic activity was evaluated for both series. The
findings obtained showed that the compounds 2a, 2b, 3b and 3c were effective against the HEp-2 cell lines with
in the 1.6 - 0.5 μg/mL range, whereas the compounds 2a (IC50
= 3.6 μg/mL), 2b (IC50
= 2.4 μg/mL) and 3f
= 3.5 μg/mL) showed good inhibitory effects against HT-29 cell lines. As complementary biological test,
all 4-thiazolidinones were evaluated for antimicrobial activity against various bacterial and fungal species.