http://sedici.unlp.edu.ar:80/handle/10915/17765 Sat, 31 Oct 2026 08:33:29 GMT 2026-10-31T08:33:29Z http://sedici.unlp.edu.ar:80/handle/10915/18151 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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–t , 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 % CI was 0.9737-1.1150 and for Cmax was 0.99876- 1.2425. Hence, the mean ratio of 90 % confidence interval of AUC0–t and Cmax lie within the acceptable limit of (0.80-1.25) for bioequivalence. Therefore, it was concluded that Ferinil and Ferriprox was proved to be bioequivalent in healthy Pakistani men. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18151 2012-01-01T00:00:00Z 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–t , 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 % CI was 0.9737-1.1150 and for Cmax was 0.99876- 1.2425. Hence, the mean ratio of 90 % confidence interval of AUC0–t and Cmax lie within the acceptable limit of (0.80-1.25) for bioequivalence. Therefore, it was concluded that Ferinil and Ferriprox was proved to be bioequivalent in healthy Pakistani men. http://sedici.unlp.edu.ar:80/handle/10915/18148 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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 4 and 18.9 % stage 5) and were intervened: 220 (78.3 %) dose reduction, 32 (11.4 %) contraindicated, 21 (7.5 %) follow up, and 8 (2.8 %) dose increment. Fifty per cent of the interventions were accepted. Antibiotics became in 45 % of the interventions. Intervention and education about the important of drug adjustment in CKD is still needed to improve safety on these patients. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18148 2012-01-01T00:00:00Z 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 4 and 18.9 % stage 5) and were intervened: 220 (78.3 %) dose reduction, 32 (11.4 %) contraindicated, 21 (7.5 %) follow up, and 8 (2.8 %) dose increment. Fifty per cent of the interventions were accepted. Antibiotics became in 45 % of the interventions. Intervention and education about the important of drug adjustment in CKD is still needed to improve safety on these patients. http://sedici.unlp.edu.ar:80/handle/10915/18147 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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 [M+H] + 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 detection of molecular ions, and the fragment ions obtained by LC-ESI-MS experiments with those of the authentic standards and data reported in the literature. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18147 2012-01-01T00:00:00Z 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 [M+H] + 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 detection of molecular ions, and the fragment ions obtained by LC-ESI-MS experiments with those of the authentic standards and data reported in the literature. http://sedici.unlp.edu.ar:80/handle/10915/18146 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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 as crude antibacterial and anti-inflammatory agent. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18146 2012-01-01T00:00:00Z 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 as crude antibacterial and anti-inflammatory agent. http://sedici.unlp.edu.ar:80/handle/10915/18145 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18145 2012-01-01T00:00:00Z 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. http://sedici.unlp.edu.ar:80/handle/10915/18144 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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 the range of 10-2000 ng/mL for febuxostat, with a lower limit of quantitation (LLOQ) of 10 ng/mL for febuxostat. Intra- and inter-day RSDs were less than 15% and the accuracies were in the range of 93.8-111.9% for febuxostat. This developed method was successfully applied to determinate of febuxostat in rat plasma for pharmacokinetic study. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18144 2012-01-01T00:00:00Z 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 the range of 10-2000 ng/mL for febuxostat, with a lower limit of quantitation (LLOQ) of 10 ng/mL for febuxostat. Intra- and inter-day RSDs were less than 15% and the accuracies were in the range of 93.8-111.9% for febuxostat. This developed method was successfully applied to determinate of febuxostat in rat plasma for pharmacokinetic study. http://sedici.unlp.edu.ar:80/handle/10915/18143 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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 sampling was applied to three consecutive industrial batches and the results met the specification limits for contaminants. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18143 2012-01-01T00:00:00Z 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 sampling was applied to three consecutive industrial batches and the results met the specification limits for contaminants. http://sedici.unlp.edu.ar:80/handle/10915/18130 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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: m/z 325.2 > 109.2 and 330.0 > 192.0 for ETP and I.S., respectively. The assay was linear in the concentration range of 0.5-50 ng/mL. The mean recovery for ETP was 97.69 %. Intra- and inter-day precision (R.S.D.) were < 10.5 % and <8.2 %, respectively and the accuracy (R.E.) was in the range ± 12.23 %. The method was successfully applied to a single oral dose pharmacokinetics study in 28 healthy Brazilian human volunteers. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18130 2012-01-01T00:00:00Z 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: m/z 325.2 > 109.2 and 330.0 > 192.0 for ETP and I.S., respectively. The assay was linear in the concentration range of 0.5-50 ng/mL. The mean recovery for ETP was 97.69 %. Intra- and inter-day precision (R.S.D.) were < 10.5 % and <8.2 %, respectively and the accuracy (R.E.) was in the range ± 12.23 %. The method was successfully applied to a single oral dose pharmacokinetics study in 28 healthy Brazilian human volunteers. http://sedici.unlp.edu.ar:80/handle/10915/18129 Comunicacion Latin American Journal of Pharmacy; vol. 31, no. 02 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 assay was linear over the range of 5–1000 ng/mL for ondansetron, with a lower limit of quantitation (LLOQ) of 5 ng/mL for ondansetron. Intra- and inter-day precisions were less than 14 % and the accuracies were in the range of 94.7-113.5 % for ondansetron. This developed method was successfully applied for the determination of ondansetron in rat plasma for pharmacokinetic study. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18129 2012-01-01T00:00:00Z 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 assay was linear over the range of 5–1000 ng/mL for ondansetron, with a lower limit of quantitation (LLOQ) of 5 ng/mL for ondansetron. Intra- and inter-day precisions were less than 14 % and the accuracies were in the range of 94.7-113.5 % for ondansetron. This developed method was successfully applied for the determination of ondansetron in rat plasma for pharmacokinetic study. http://sedici.unlp.edu.ar:80/handle/10915/18128 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 (ACEIs, 26.17 %) were the preferred agents in hypertensive patients with coronary heart disease (CHD). Among 1327 inpatients with combination therapy, two-drug regimen was the most popular, except for the hypertensive patients with stroke. The pattern of antihypertensive utilization appears to be partly in accordance with the recommendations of international guidelines. There was a tendency to use CCBs in hypertensive patients with stroke, whereas BBs and ACEI were the most prescribed in those with CHD. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18128 2012-01-01T00:00:00Z 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 (ACEIs, 26.17 %) were the preferred agents in hypertensive patients with coronary heart disease (CHD). Among 1327 inpatients with combination therapy, two-drug regimen was the most popular, except for the hypertensive patients with stroke. The pattern of antihypertensive utilization appears to be partly in accordance with the recommendations of international guidelines. There was a tendency to use CCBs in hypertensive patients with stroke, whereas BBs and ACEI were the most prescribed in those with CHD. http://sedici.unlp.edu.ar:80/handle/10915/18127 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18127 2012-01-01T00:00:00Z 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. http://sedici.unlp.edu.ar:80/handle/10915/18126 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 Group CG (n = 4) were evaluated and samples were obtained in the same way and within the same time periods as G2. The concentration-time curves of cefepime were determined using a biological method, and it was analysed through a non-compartmental model. The pharmacokinetic results (Mean ± S.D.) were: t½ = 1.6 ± 0.4 h; AUC = 212.1 ± 82.1 μg/mL.h; AUMC = 387.4 ± 132.2 μg/mL.h; Vss = 216.7 ± 63.4 mL/kg; CL = 99.7 ± 19.4 mL/kg y TMR = 2.0 ± 0.4 h. The cefepime administered to rabbits in therapeutic doses did not produce any biochemical, electrocardiographic or renal modification. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18126 2012-01-01T00:00:00Z 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 Group CG (n = 4) were evaluated and samples were obtained in the same way and within the same time periods as G2. The concentration-time curves of cefepime were determined using a biological method, and it was analysed through a non-compartmental model. The pharmacokinetic results (Mean ± S.D.) were: t½ = 1.6 ± 0.4 h; AUC = 212.1 ± 82.1 μg/mL.h; AUMC = 387.4 ± 132.2 μg/mL.h; Vss = 216.7 ± 63.4 mL/kg; CL = 99.7 ± 19.4 mL/kg y TMR = 2.0 ± 0.4 h. The cefepime administered to rabbits in therapeutic doses did not produce any biochemical, electrocardiographic or renal modification. http://sedici.unlp.edu.ar:80/handle/10915/18125 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 (A) ACNdiethylamine (0.05 mL), (B) methanol, (C) 10 mM ammonium acetate and (D) Water. For HPTLC method separation was achieved by using mobile phase chloroform and methanol in the ratio 9.5:0.5. Both of the validated methods can be utilized for the assay of these α1 adrenoreceptors in pharmaceutical industries. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18125 2012-01-01T00:00:00Z 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 (A) ACNdiethylamine (0.05 mL), (B) methanol, (C) 10 mM ammonium acetate and (D) Water. For HPTLC method separation was achieved by using mobile phase chloroform and methanol in the ratio 9.5:0.5. Both of the validated methods can be utilized for the assay of these α1 adrenoreceptors in pharmaceutical industries. http://sedici.unlp.edu.ar:80/handle/10915/18124 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 acetonitrile and 10 mM ammonium acetate solution (pH = 5.2) in a ratio of 15:85 as mobile phase. Stability studies under stress were conducted on selected formulations according to ICH guidelines. It was conclusive that stable CA formulations could be developed by direct compression method. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18124 2012-01-01T00:00:00Z 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 acetonitrile and 10 mM ammonium acetate solution (pH = 5.2) in a ratio of 15:85 as mobile phase. Stability studies under stress were conducted on selected formulations according to ICH guidelines. It was conclusive that stable CA formulations could be developed by direct compression method. http://sedici.unlp.edu.ar:80/handle/10915/18101 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 low cost and toxicity, besides presenting operational ease. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18101 2012-01-01T00:00:00Z 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 low cost and toxicity, besides presenting operational ease. http://sedici.unlp.edu.ar:80/handle/10915/18100 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 and 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 the surviving bacteria were grown in trypticase soy broth using the most probable number technique. Plasma antimicrobial activity depended on the catheter’s internal diameter and radio frequency powers. The O2 + H2O2 mixture exhibited higher microbial efficacy than pure O2 in both plasma systems. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18100 2012-01-01T00:00:00Z 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 and 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 the surviving bacteria were grown in trypticase soy broth using the most probable number technique. Plasma antimicrobial activity depended on the catheter’s internal diameter and radio frequency powers. The O2 + H2O2 mixture exhibited higher microbial efficacy than pure O2 in both plasma systems. http://sedici.unlp.edu.ar:80/handle/10915/18099 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 %. The method was used to determine the plasma concentration–time profiles for AUR after oral doses of 50, 100 and 200 mg/kg in dogs. A nonlinear pharmacokinetics was found in dogs at doses from 50 to 200 mg/kg. No significant accumulation of AUR in dogs following multiple doses was observed. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18099 2012-01-01T00:00:00Z 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 %. The method was used to determine the plasma concentration–time profiles for AUR after oral doses of 50, 100 and 200 mg/kg in dogs. A nonlinear pharmacokinetics was found in dogs at doses from 50 to 200 mg/kg. No significant accumulation of AUR in dogs following multiple doses was observed. http://sedici.unlp.edu.ar:80/handle/10915/18098 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 % w/v, indicating that the absence of steric hindrance from methoxyl groups improves the effect of N-trimethylchitosan chloride, but at expense of a narrow range of action and higher cytotoxicity. The results of in vitro permeation studies conducted in bicameral Transwell® systems suggested that the permeability of capreomycin sulfate is low, although it was not established if the transport is exclusively paracellular or membrane transporters are involved. By using increasing concentrations of the polymer in the range of 0.001 - 0.003% w/v, it was observed a slight increase in the transport of capreomycin. Therefore, it was concluded that further studies should use N-trimethylchitosan chloride with a lower degree of quaternization or controlled methoxylation, in order to increase the mass to use and obtain a product that is able to remain retained in the intestinal lumen and which in turn interacts with the epithelium. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18098 2012-01-01T00:00:00Z 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 % w/v, indicating that the absence of steric hindrance from methoxyl groups improves the effect of N-trimethylchitosan chloride, but at expense of a narrow range of action and higher cytotoxicity. The results of in vitro permeation studies conducted in bicameral Transwell® systems suggested that the permeability of capreomycin sulfate is low, although it was not established if the transport is exclusively paracellular or membrane transporters are involved. By using increasing concentrations of the polymer in the range of 0.001 - 0.003% w/v, it was observed a slight increase in the transport of capreomycin. Therefore, it was concluded that further studies should use N-trimethylchitosan chloride with a lower degree of quaternization or controlled methoxylation, in order to increase the mass to use and obtain a product that is able to remain retained in the intestinal lumen and which in turn interacts with the epithelium. http://sedici.unlp.edu.ar:80/handle/10915/18097 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 plots were linear over the range of 10-2000 ng/mL for cilostazol in rat plasma. Lower limit of quantification (LLOQ) for cilostazol was 10 ng/mL. Mean recovery of cilostazol from plasma was in the range 90.14- 95.10 %. RSD of intra-day and inter-day precision were both less than 15 %. This method is simple and sensitive enough to be used in pharmacokinetic research for determination of cilostazol in rat plasma. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18097 2012-01-01T00:00:00Z 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 plots were linear over the range of 10-2000 ng/mL for cilostazol in rat plasma. Lower limit of quantification (LLOQ) for cilostazol was 10 ng/mL. Mean recovery of cilostazol from plasma was in the range 90.14- 95.10 %. RSD of intra-day and inter-day precision were both less than 15 %. This method is simple and sensitive enough to be used in pharmacokinetic research for determination of cilostazol in rat plasma. http://sedici.unlp.edu.ar:80/handle/10915/18095 Articulo Latin American Journal of Pharmacy; vol. 31, no. 02 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 IC50 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 (IC50 = 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. Sun, 01 Jan 2012 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/18095 2012-01-01T00:00:00Z 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 IC50 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 (IC50 = 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.