http://sedici.unlp.edu.ar:80/handle/10915/230 Sun, 15 Nov 2026 06:40:09 GMT 2026-11-15T06:40:09Z http://sedici.unlp.edu.ar:80/handle/10915/7995 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 Caesalpinia ferrea and Chrysobalanus icaco are plants commonly used by the folk medicine for the treatment of diabetes mellitus. In this work, the effects of the chronic treatment with aqueous extracts of C. ferrea (AECF) and C. icaco (AECI) on the vascular reactivity of alloxan-induced diabetic rats were evaluated. In rings of mesenteric artery, AECF and AECI were not able to modify the contractions induced by phenylephrine or relaxations induced by carbachol. However, treatment with AECI was able to prevent the potentiation of the relaxations induced by sodium nitroprusside in diabetic rats. In brief, this study found possible benefits of the treatment with C. icaco on the reactivity vascular of diabetic rats. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7995 2010-01-01T00:00:00Z Caesalpinia ferrea and Chrysobalanus icaco are plants commonly used by the folk medicine for the treatment of diabetes mellitus. In this work, the effects of the chronic treatment with aqueous extracts of C. ferrea (AECF) and C. icaco (AECI) on the vascular reactivity of alloxan-induced diabetic rats were evaluated. In rings of mesenteric artery, AECF and AECI were not able to modify the contractions induced by phenylephrine or relaxations induced by carbachol. However, treatment with AECI was able to prevent the potentiation of the relaxations induced by sodium nitroprusside in diabetic rats. In brief, this study found possible benefits of the treatment with C. icaco on the reactivity vascular of diabetic rats. http://sedici.unlp.edu.ar:80/handle/10915/7994 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 A highly sensitive liquid chromatographic tandem mass spectrometric (LC-MS/MS) method for determination of dextromethorphan in rabbit plasma using triazolam as the internal standard (IS) was developed. Plasma samples were extracted with ethyl acetate and separated on a SB-C18 column with a mobile phase of acetonitrile-water 60:40 (v/v) at a flow of 0.3 mL/min. Detection is carried out by multiple reaction monitoring (MRM) on a ion-trap LC-MS/MS system with an electrospray ionization interface. The lower limit of quantification (LLOQ) was 1 ng/mL. After intravenous administration of a single dose of dextromethorphan 2 mg/kg, the main pharmacokinetic parameters were as follows: AUC_0→t 636.13 ± 47.13 (ng/mL·h); CL 2.60 ± 0.24 (L/h), C_max 874 ± 67.16 (ng/mL), Vz 1.58 ± 0.11 (L/kg), T1/2 2.41 ± 0.35 (h), MRT 1.26 ± 0.08 (h). Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7994 2010-01-01T00:00:00Z A highly sensitive liquid chromatographic tandem mass spectrometric (LC-MS/MS) method for determination of dextromethorphan in rabbit plasma using triazolam as the internal standard (IS) was developed. Plasma samples were extracted with ethyl acetate and separated on a SB-C18 column with a mobile phase of acetonitrile-water 60:40 (v/v) at a flow of 0.3 mL/min. Detection is carried out by multiple reaction monitoring (MRM) on a ion-trap LC-MS/MS system with an electrospray ionization interface. The lower limit of quantification (LLOQ) was 1 ng/mL. After intravenous administration of a single dose of dextromethorphan 2 mg/kg, the main pharmacokinetic parameters were as follows: AUC_0→t 636.13 ± 47.13 (ng/mL·h); CL 2.60 ± 0.24 (L/h), C_max 874 ± 67.16 (ng/mL), Vz 1.58 ± 0.11 (L/kg), T1/2 2.41 ± 0.35 (h), MRT 1.26 ± 0.08 (h). http://sedici.unlp.edu.ar:80/handle/10915/7993 Comunicacion Quantification of (-) hydroxycitric acid in marketed extracts of Garcinia cambogia by high performance liquid chromatography Latin American Journal of Pharmacy; vol. 29, no. 5 O extrato de Garcinia cambogia (GC), utilizado no tratamento da obesidade, é padronizado por quantificação de ácido hidroxicítrico (AHC) em sua forma salina (CaAHC). Assim, objetivou-se quantificar AHC em duas amostras comerciais de GC (A e B) com 50 % de AHC, de acordo com os laudos de origem. O rendimento extrativo por maceração foi 23,83 % (A) e 22,37 % (B). O teor do analito, quantificado por CLAE-DAD utilizando calibração com padrão de CaAHC, foi 36,09 % (A) e 41,57 % (B) sobre a fração hidrossolúvel e 8,82 % (A) e 9,70 % (B) sobre o extrato inicial. Na quantificação sobre a fração hidrossolúvel, os resultados encontram-se similares aos especificados pelos distribuidores. Entretanto, considerando o extrato inicial, os resultados encontram-se significativamente abaixo dos especificados. Visto que parte considerável do extrato não é solúvel em meio aquoso, dosear o analito apenas em relação à fração hidrossolúvel pode ser um viés para a adequação de doses deste fitoterápico.; Garcinia cambogia extract, used in the treatment of obesity, is standardized by quantification of hydroxycitric acid (HCA) in its salt form (CaHCA). The aim of this study was to quantify HCA in two samples of marketed GC extracts (A and B) containing 50 % of HCA, as origins specifications. The maceration extraction yield was 23.83 % (A) and 22.37 % (B). The quantification, performed by HPLC-DAD using calibration with CaHCA standard, was 36.09 % (A) and 41.57 % (B) related to the water-soluble portion and 8.82 % (A) and 9.70 % (B), related to the initial extract. On the water-soluble portion quantification, results are similar to those specified by the distributors. However, considering the quantification over the initial extract, results are significantly below of the specified values. Observing that part of the extract is insoluble in water, to quantify the analyte considering only the water-soluble portion could lead to considerable error for the adequacy of dose of this phytotherapic. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7993 2010-01-01T00:00:00Z O extrato de Garcinia cambogia (GC), utilizado no tratamento da obesidade, é padronizado por quantificação de ácido hidroxicítrico (AHC) em sua forma salina (CaAHC). Assim, objetivou-se quantificar AHC em duas amostras comerciais de GC (A e B) com 50 % de AHC, de acordo com os laudos de origem. O rendimento extrativo por maceração foi 23,83 % (A) e 22,37 % (B). O teor do analito, quantificado por CLAE-DAD utilizando calibração com padrão de CaAHC, foi 36,09 % (A) e 41,57 % (B) sobre a fração hidrossolúvel e 8,82 % (A) e 9,70 % (B) sobre o extrato inicial. Na quantificação sobre a fração hidrossolúvel, os resultados encontram-se similares aos especificados pelos distribuidores. Entretanto, considerando o extrato inicial, os resultados encontram-se significativamente abaixo dos especificados. Visto que parte considerável do extrato não é solúvel em meio aquoso, dosear o analito apenas em relação à fração hidrossolúvel pode ser um viés para a adequação de doses deste fitoterápico. Garcinia cambogia extract, used in the treatment of obesity, is standardized by quantification of hydroxycitric acid (HCA) in its salt form (CaHCA). The aim of this study was to quantify HCA in two samples of marketed GC extracts (A and B) containing 50 % of HCA, as origins specifications. The maceration extraction yield was 23.83 % (A) and 22.37 % (B). The quantification, performed by HPLC-DAD using calibration with CaHCA standard, was 36.09 % (A) and 41.57 % (B) related to the water-soluble portion and 8.82 % (A) and 9.70 % (B), related to the initial extract. On the water-soluble portion quantification, results are similar to those specified by the distributors. However, considering the quantification over the initial extract, results are significantly below of the specified values. Observing that part of the extract is insoluble in water, to quantify the analyte considering only the water-soluble portion could lead to considerable error for the adequacy of dose of this phytotherapic. http://sedici.unlp.edu.ar:80/handle/10915/7992 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 The objective was to develop and validate a method for the determination of total polyphenols in a vaginal gel containing a dried extract of Aroeira (Schinus terebinthifolius Raddi). The method was developed by UV spectrophotometry, and proved to be precise, accurate, reproducible, and easy to perform. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7992 2010-01-01T00:00:00Z The objective was to develop and validate a method for the determination of total polyphenols in a vaginal gel containing a dried extract of Aroeira (Schinus terebinthifolius Raddi). The method was developed by UV spectrophotometry, and proved to be precise, accurate, reproducible, and easy to perform. http://sedici.unlp.edu.ar:80/handle/10915/7991 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 The solubility of pioglitazone hydrochloride in polyethylene glycol 600-ethanol-water mixtures at 25 °C was determined using flask shake method. The generated data extended the solubility database for further computational investigations and also was used to assess the prediction capability of a trained version of the Jouyban-Acree model for solubility prediction in mixed solvents at various temperatures. The accuracy of the predicted solubilities was evaluated by the mean percentage deviation (MPD) between the predicted and experimental solubilities. The overall MPD of the Jouyban-Acree model for the back-calculated solubility data in binary and ternary solvent mixtures was 13.1 ± 12.9 % Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7991 2010-01-01T00:00:00Z The solubility of pioglitazone hydrochloride in polyethylene glycol 600-ethanol-water mixtures at 25 °C was determined using flask shake method. The generated data extended the solubility database for further computational investigations and also was used to assess the prediction capability of a trained version of the Jouyban-Acree model for solubility prediction in mixed solvents at various temperatures. The accuracy of the predicted solubilities was evaluated by the mean percentage deviation (MPD) between the predicted and experimental solubilities. The overall MPD of the Jouyban-Acree model for the back-calculated solubility data in binary and ternary solvent mixtures was 13.1 ± 12.9 % http://sedici.unlp.edu.ar:80/handle/10915/7990 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 The present work was to study the anti-inflammatory activity of Coccinia indica Wight and Arn fruits belonging to family Cucurbitaceae. The fruit powder of C. indica was subjected to successive extraction with petroleum ether, chloroform, ethanol and water in a Soxhlet extractor. The ethanol extract after preliminary phytochemical investigation shown the presence of glycosides, triterpenoids, flavonoids, tannins and phenolic compounds. The anti-inflammatory activity was studied using carrageenan-induced rat paw oedema and cotton pellet granuloma at three different doses (100, 200 and 400 mg/kg b.w. p.o.) of each extract. The ethanol extract of C. indica fruits exhibited significant anti-inflammatory activity at the dose of 200 mg/kg and 400 mg/kg in both models when compared with control group. Indomethacin (10 mg/kg b.w. p.o) also showed significant anti-inflammatory activity in both models. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7990 2010-01-01T00:00:00Z The present work was to study the anti-inflammatory activity of Coccinia indica Wight and Arn fruits belonging to family Cucurbitaceae. The fruit powder of C. indica was subjected to successive extraction with petroleum ether, chloroform, ethanol and water in a Soxhlet extractor. The ethanol extract after preliminary phytochemical investigation shown the presence of glycosides, triterpenoids, flavonoids, tannins and phenolic compounds. The anti-inflammatory activity was studied using carrageenan-induced rat paw oedema and cotton pellet granuloma at three different doses (100, 200 and 400 mg/kg b.w. p.o.) of each extract. The ethanol extract of C. indica fruits exhibited significant anti-inflammatory activity at the dose of 200 mg/kg and 400 mg/kg in both models when compared with control group. Indomethacin (10 mg/kg b.w. p.o) also showed significant anti-inflammatory activity in both models. http://sedici.unlp.edu.ar:80/handle/10915/7989 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 Se ensayó la actividad antimicobacteriana in vitro de los extractos diclorometánico (DCM) y metanólico (MeOH) de G. cabrerae y G. megapotamica var. scabiosoides frente a dos cepas de Mycobacterium tuberculosis (H37Rv y MDR), por medio del test colorimétrico TEMA, determinándose la concentración inhibitoria minima (MIC) en ug extracto/ml. Los extractos DCM de ambas especies de Gaillardia y el extracto MeOH de G. cabrerae exhibieron actividad antimicobacteriana frente a ambas cepas con MICs de 50-100 ug/ml. Dos de las fracciones obtenidas a partir del extracto metanólico de G. cabrerae presentaron actividad antimicobacteriana. El screening fitoquímico de las fracciones activas reveló la presencia de sesquiterpenlactonas, flavonoides glicosilados y sus aglicones como componentes mayoritarios.; Dichloromethane and methanol extracts from two argentine species of Gaillardia (Asteraceae): G. cabrerae Covas and G. megapotamica (Spreng.) Baker var. scabiosoides (Arn. ex DC.) Baker were assayed for their in vitro activity against two strains of Mycobacterium tuberculosis (H37Rv y MDR) by means of the TEMA colorimetric test. The minimum inhibitory concentration (MIC) in ug/ml was determinate. Dichloromethane extracts of both Gaillardia spp. and methanol extract of Gaillardia cabrerae exhibited antimycobacterial activity against both strains with a MIC range 50-100 ug/ml. The methanol extract of G. cabrerae was fractionated and two fractions were active. Phytochemical screening of the active fractions showed the presence of sesquiterpene lactones, aglycones and glycosilated flavonoids as main compounds. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7989 2010-01-01T00:00:00Z Se ensayó la actividad antimicobacteriana in vitro de los extractos diclorometánico (DCM) y metanólico (MeOH) de G. cabrerae y G. megapotamica var. scabiosoides frente a dos cepas de Mycobacterium tuberculosis (H37Rv y MDR), por medio del test colorimétrico TEMA, determinándose la concentración inhibitoria minima (MIC) en ug extracto/ml. Los extractos DCM de ambas especies de Gaillardia y el extracto MeOH de G. cabrerae exhibieron actividad antimicobacteriana frente a ambas cepas con MICs de 50-100 ug/ml. Dos de las fracciones obtenidas a partir del extracto metanólico de G. cabrerae presentaron actividad antimicobacteriana. El screening fitoquímico de las fracciones activas reveló la presencia de sesquiterpenlactonas, flavonoides glicosilados y sus aglicones como componentes mayoritarios. Dichloromethane and methanol extracts from two argentine species of Gaillardia (Asteraceae): G. cabrerae Covas and G. megapotamica (Spreng.) Baker var. scabiosoides (Arn. ex DC.) Baker were assayed for their in vitro activity against two strains of Mycobacterium tuberculosis (H37Rv y MDR) by means of the TEMA colorimetric test. The minimum inhibitory concentration (MIC) in ug/ml was determinate. Dichloromethane extracts of both Gaillardia spp. and methanol extract of Gaillardia cabrerae exhibited antimycobacterial activity against both strains with a MIC range 50-100 ug/ml. The methanol extract of G. cabrerae was fractionated and two fractions were active. Phytochemical screening of the active fractions showed the presence of sesquiterpene lactones, aglycones and glycosilated flavonoids as main compounds. http://sedici.unlp.edu.ar:80/handle/10915/7988 Comunicacion Development and validation of a high performance liquid chromatography method for the determination of paracetamol in tablets Latin American Journal of Pharmacy; vol. 29, no. 5 Um método simples e sensível por CLAE foi desenvolvido para a determinação quantitativa de paracetamol em comprimidos. Condições cromatográficas para uma eficiente separação foram obtidas empregando-se fase estacionária C8, fase móvel de KH₂ PO₄ 40 mM pH 6,0 e metanol 85:15 (v/v), com fluxo de 1,2 mL/min. A análise de regressão mostrou um coeficiente de correlação superior a 0,99. O método apresentou recuperação consistente para paracetamol (97,03-100,57 %). A precisão intra-dia e precisão intermediária não ultrapassou 1,87 e 0,95 % do CV, respectivamente. O desenvolvimento e a validação do método apresentaram-se adequados para o controle de qualidade de rotina da análise de paracetamol em comprimidos.; A simple and sensitive HPLC assay method has been developed for the quantitative determination of paracetamol in tablets. Efficient chromatographic separation was achieved on a C8 stationary phase with mobile phase of KH₂ PO₄ 40 mM pH 6.0 and methanol 85:15 (v/v), at a flow rate of 1.2 mL/min. Regression analysis showed a correlation coefficient greater than 0.99. The method has shown consistent recoveries for paracetamol (97.03-100.57 %). Intra-day and intermediate precision did not exceed 1.87 and 0.95 % of the CV, respectively. The developed and validated method is suitable for the routine quality control analysis of paracetamol in tablets. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7988 2010-01-01T00:00:00Z Um método simples e sensível por CLAE foi desenvolvido para a determinação quantitativa de paracetamol em comprimidos. Condições cromatográficas para uma eficiente separação foram obtidas empregando-se fase estacionária C8, fase móvel de KH₂ PO₄ 40 mM pH 6,0 e metanol 85:15 (v/v), com fluxo de 1,2 mL/min. A análise de regressão mostrou um coeficiente de correlação superior a 0,99. O método apresentou recuperação consistente para paracetamol (97,03-100,57 %). A precisão intra-dia e precisão intermediária não ultrapassou 1,87 e 0,95 % do CV, respectivamente. O desenvolvimento e a validação do método apresentaram-se adequados para o controle de qualidade de rotina da análise de paracetamol em comprimidos. A simple and sensitive HPLC assay method has been developed for the quantitative determination of paracetamol in tablets. Efficient chromatographic separation was achieved on a C8 stationary phase with mobile phase of KH₂ PO₄ 40 mM pH 6.0 and methanol 85:15 (v/v), at a flow rate of 1.2 mL/min. Regression analysis showed a correlation coefficient greater than 0.99. The method has shown consistent recoveries for paracetamol (97.03-100.57 %). Intra-day and intermediate precision did not exceed 1.87 and 0.95 % of the CV, respectively. The developed and validated method is suitable for the routine quality control analysis of paracetamol in tablets. http://sedici.unlp.edu.ar:80/handle/10915/7987 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 The present study was undertaken to evaluate the possible antinociceptive effect of Coleus aromaticus Benth oil. The pain sensitivity was assessed by the acetic acid induced writhing and hotplate models in mice. The essential oil exhibited a significant reduction in acetic acid induced writhing response, a dose dependent increase in reaction time against thermal pain and a moderate motor impairment at analgesic doses and significant reduction in endurance time at higher dose on rotarod apparatus. These experimental results suggest that essential oil (250 and 500 mg/kg) produced analgesic effect in mice and may be a candidate for the development of pharmacological agents used in the pain management. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7987 2010-01-01T00:00:00Z The present study was undertaken to evaluate the possible antinociceptive effect of Coleus aromaticus Benth oil. The pain sensitivity was assessed by the acetic acid induced writhing and hotplate models in mice. The essential oil exhibited a significant reduction in acetic acid induced writhing response, a dose dependent increase in reaction time against thermal pain and a moderate motor impairment at analgesic doses and significant reduction in endurance time at higher dose on rotarod apparatus. These experimental results suggest that essential oil (250 and 500 mg/kg) produced analgesic effect in mice and may be a candidate for the development of pharmacological agents used in the pain management. http://sedici.unlp.edu.ar:80/handle/10915/7986 Comunicacion Physico-chemical characterization of trypanomicide benznidazole for drug development Latin American Journal of Pharmacy; vol. 29, no. 5 Este trabalho objetivou a caracterização físico-química do benznidazol (BNZ), utilizando diversas técnicas analíticas. Os dados obtidos nos espectrogramas de infravermelho mostram as características principais da carbonila e deformação N-H; as vibrações devido ao grupo benzílico e imidazólico. O BNZ apresentou pico endotérmico em aproximadamente 190 ºC referente a fusão. O perfil difractométrico revela a presença de picos de maior intensidade a 7,5; 16,5 e 22 º2θ, evidenciando o comportamento cristalino do BNZ, corroborando com as micrografias obtidas. Obteve-se um percentual dissolvido de BNZ de aproximadamente 25% em 60 min. Os resultados permitiram a determinação detalhada das características do fármaco (classe II), passo relevante na produção de medicamentos.; The aim of this work was the benznidazole (BNZ) physical-chemical characterization by diverse analytical techniques. The infrared spectrum obtained show carbonyl stretch, N-H deformation and vibrations from benzyl and imidazole group. The BNZ show endothermic melting peak at 190°C. The diffractometry profile show two major peaks at 7.5, 16.5 and 22° 2θ, showing the crystalline state of the drug, corroborating with the obtained micrographics. The dissolution rate of the drug is approximately 25% in 60 min. The data obtained allowed an important step for medicines development, the drug characterization. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7986 2010-01-01T00:00:00Z Este trabalho objetivou a caracterização físico-química do benznidazol (BNZ), utilizando diversas técnicas analíticas. Os dados obtidos nos espectrogramas de infravermelho mostram as características principais da carbonila e deformação N-H; as vibrações devido ao grupo benzílico e imidazólico. O BNZ apresentou pico endotérmico em aproximadamente 190 ºC referente a fusão. O perfil difractométrico revela a presença de picos de maior intensidade a 7,5; 16,5 e 22 º2θ, evidenciando o comportamento cristalino do BNZ, corroborando com as micrografias obtidas. Obteve-se um percentual dissolvido de BNZ de aproximadamente 25% em 60 min. Os resultados permitiram a determinação detalhada das características do fármaco (classe II), passo relevante na produção de medicamentos. The aim of this work was the benznidazole (BNZ) physical-chemical characterization by diverse analytical techniques. The infrared spectrum obtained show carbonyl stretch, N-H deformation and vibrations from benzyl and imidazole group. The BNZ show endothermic melting peak at 190°C. The diffractometry profile show two major peaks at 7.5, 16.5 and 22° 2θ, showing the crystalline state of the drug, corroborating with the obtained micrographics. The dissolution rate of the drug is approximately 25% in 60 min. The data obtained allowed an important step for medicines development, the drug characterization. http://sedici.unlp.edu.ar:80/handle/10915/7985 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 Although octyldodecanol has been used for several decades as an ingredient for emulsions, no required Hydrophilic-Lipophilic Balance (HLB) values for this alcohol were found in the literature. The purpose of this paper is to present the results of the experimental determination of the required HLB values, from emulsion stability tests and from low-frequency relative dielectric permittivity measurements. The required HLB values obtained from emulsion stability tests for oil-in-water and water-in-oil emulsions are 11.2 and 5.9, respectively. By relative dielectric permittivity measurements, the required HLB value obtained for oil-in-water emulsions was 10.9 ± 0.4, in agreement with the results from emulsion stability tests. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7985 2010-01-01T00:00:00Z Although octyldodecanol has been used for several decades as an ingredient for emulsions, no required Hydrophilic-Lipophilic Balance (HLB) values for this alcohol were found in the literature. The purpose of this paper is to present the results of the experimental determination of the required HLB values, from emulsion stability tests and from low-frequency relative dielectric permittivity measurements. The required HLB values obtained from emulsion stability tests for oil-in-water and water-in-oil emulsions are 11.2 and 5.9, respectively. By relative dielectric permittivity measurements, the required HLB value obtained for oil-in-water emulsions was 10.9 ± 0.4, in agreement with the results from emulsion stability tests. http://sedici.unlp.edu.ar:80/handle/10915/7984 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 A simple and rapid procedure has been developed and validated for the simultaneous determination of benzoylecgonine and ecgonine methyl ester in human urine samples. After extraction and sample cleanup by solid-phase extraction (SPE), the extracts were derivatized with 50 uL of MTBSTFA and analyzed by gas chromatography/mass spectrometry (GC/MS). The limit of detection (LOD) was 50 ng/mL for both metabolites. The recoveries were 81% and 75.3% for benzoylecgonine and ecgonine methyl ester, respectively. The intra-assay precision (% relative standard deviation) at two different added amounts (200 and 1000 ng/mL) in urine matrix varied from 4.8 to 8.4 and from 4.4 to 5.7, respectively. The mass spectra obtained for each compound have many diagnostics ions with relative abundance in accordance with the WADA requirements. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7984 2010-01-01T00:00:00Z A simple and rapid procedure has been developed and validated for the simultaneous determination of benzoylecgonine and ecgonine methyl ester in human urine samples. After extraction and sample cleanup by solid-phase extraction (SPE), the extracts were derivatized with 50 uL of MTBSTFA and analyzed by gas chromatography/mass spectrometry (GC/MS). The limit of detection (LOD) was 50 ng/mL for both metabolites. The recoveries were 81% and 75.3% for benzoylecgonine and ecgonine methyl ester, respectively. The intra-assay precision (% relative standard deviation) at two different added amounts (200 and 1000 ng/mL) in urine matrix varied from 4.8 to 8.4 and from 4.4 to 5.7, respectively. The mass spectra obtained for each compound have many diagnostics ions with relative abundance in accordance with the WADA requirements. http://sedici.unlp.edu.ar:80/handle/10915/7983 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 5 A sensitive and selective liquid chromatography-tandem mass spectrometry method (LC-MS/MS) for the determination of tolbutamide in rabbit plasma was developed and validated over the concentration range of 4-1000 ng mL-1. After addition of bupivacaine as internal standard (IS), a simplified protein precipitation with acetonitrile was employed for the sample preparation. Chromatographic separation was performed by an Agilent Zorbax SB-C18 column (150 mmu2.1 mm, 3.5 um). The mobile phase was acetonitrile-1% formic acid in water (50:50 v/v) delivered at a flow rate of 0.3 mL min-1. The MS data acquisition was accomplished by multiple reactions monitoring (MRM) mode with positive electrospray ionization (ESI) interface. The lower limit of quantification (LLOQ) was 4 ng mL-1. For interday and intra-day tests, the precision (RSD) for the entire validation was less than 10%, and the accuracy was within the 94.7% to 105.6% range. The validated method is successfully used to analyze the drug in samples of rabbit plasma for pharmacokinetic study. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7983 2010-01-01T00:00:00Z A sensitive and selective liquid chromatography-tandem mass spectrometry method (LC-MS/MS) for the determination of tolbutamide in rabbit plasma was developed and validated over the concentration range of 4-1000 ng mL-1. After addition of bupivacaine as internal standard (IS), a simplified protein precipitation with acetonitrile was employed for the sample preparation. Chromatographic separation was performed by an Agilent Zorbax SB-C18 column (150 mmu2.1 mm, 3.5 um). The mobile phase was acetonitrile-1% formic acid in water (50:50 v/v) delivered at a flow rate of 0.3 mL min-1. The MS data acquisition was accomplished by multiple reactions monitoring (MRM) mode with positive electrospray ionization (ESI) interface. The lower limit of quantification (LLOQ) was 4 ng mL-1. For interday and intra-day tests, the precision (RSD) for the entire validation was less than 10%, and the accuracy was within the 94.7% to 105.6% range. The validated method is successfully used to analyze the drug in samples of rabbit plasma for pharmacokinetic study. http://sedici.unlp.edu.ar:80/handle/10915/7982 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 Antioxidant activity of ethanol and water extracts and infusion of the flowers of Phrygilanthus acutifolius were evaluated. Total phenolic contents were determined using Folin- Ciocalteau reagent. The ethanol extract was more effective in scavenging radical 1,1 biphenyl -2-picrylhydrazyl (DPPH), with lower IC50 values. The water and ethanol extracts were the most effective antioxidants based on the inhibition of lipid peroxidation (β carotene bleaching method). The acute toxicity test in rats indicated that oral administration of 3.200 mg/Kg of flowers produced neither mortality, nor changes in behaviour or any other physiological activities. There were no significant differences in the body and organ weight between controls and treated animals. In blood chemistry analysis, aspartate transaminase, alanine transaminase, and alkaline phosphatase activities, no significant changes occurred. In view of the doses consumed empirically in traditional medicine of Amaicha del Valle, Tucumán, Argentina, there is a wide margin of safety for the therapeutic use of Phrygilanthus acutifolius flowers. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7982 2010-01-01T00:00:00Z Antioxidant activity of ethanol and water extracts and infusion of the flowers of Phrygilanthus acutifolius were evaluated. Total phenolic contents were determined using Folin- Ciocalteau reagent. The ethanol extract was more effective in scavenging radical 1,1 biphenyl -2-picrylhydrazyl (DPPH), with lower IC50 values. The water and ethanol extracts were the most effective antioxidants based on the inhibition of lipid peroxidation (β carotene bleaching method). The acute toxicity test in rats indicated that oral administration of 3.200 mg/Kg of flowers produced neither mortality, nor changes in behaviour or any other physiological activities. There were no significant differences in the body and organ weight between controls and treated animals. In blood chemistry analysis, aspartate transaminase, alanine transaminase, and alkaline phosphatase activities, no significant changes occurred. In view of the doses consumed empirically in traditional medicine of Amaicha del Valle, Tucumán, Argentina, there is a wide margin of safety for the therapeutic use of Phrygilanthus acutifolius flowers. http://sedici.unlp.edu.ar:80/handle/10915/7981 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 The present study describes the in vivo bronchodilatory and analgesic activities of the crude extract of Hyoscyamus niger (Hn.Cr) and Aspalathus linearis (Al.Cr), which tested positive for alkaloids, coumarins, flavonoids, sterols, tannins, terpenes and flavonoids, tannins, saponins respectively. Hn.Cr (0.3-3.0 mg/kg) and Al.Cr (10-100 mg/kg) caused inhibition of the CCh (1 μmol/kg)-induced increase in the inspiratory pressure of anaesthetized rats. Hn.Cr and Al.Cr dose-dependently (50-100 mg/kg) reduced the numbers of acetic acid-mediated writhes in mice. These results indicate that Hyoscyamus niger and Aspalathus linearis exhibit airways-relaxant and anti-nociceptive effects, hence justifying their medicinal use in asthma and pain. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7981 2010-01-01T00:00:00Z The present study describes the in vivo bronchodilatory and analgesic activities of the crude extract of Hyoscyamus niger (Hn.Cr) and Aspalathus linearis (Al.Cr), which tested positive for alkaloids, coumarins, flavonoids, sterols, tannins, terpenes and flavonoids, tannins, saponins respectively. Hn.Cr (0.3-3.0 mg/kg) and Al.Cr (10-100 mg/kg) caused inhibition of the CCh (1 μmol/kg)-induced increase in the inspiratory pressure of anaesthetized rats. Hn.Cr and Al.Cr dose-dependently (50-100 mg/kg) reduced the numbers of acetic acid-mediated writhes in mice. These results indicate that Hyoscyamus niger and Aspalathus linearis exhibit airways-relaxant and anti-nociceptive effects, hence justifying their medicinal use in asthma and pain. http://sedici.unlp.edu.ar:80/handle/10915/7980 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 Transdermal drug delivery systems of venlafaxine hydrochloride were prepared by using combination of hydrophilic (HPMC E15) and hydrophobic (ERS100 and ERL 100) polymers in 1:5, 2:4, 3:3, 4:2, 5:1 ratios by solvent casting technique with 15 % v/w propylene glycol as plasticizer. The drug permeation studies revealed that drug permeation increased proportionally with increasing HPMC ratio where ERS 100 as hydrophobic polymer but in case of ERL 100 as hydrophobic polymer proportional increase was not obtained this may be due to increased diffusion path length. The drug permeation kinetics followed zero order profile with diffusion mechanism. The average steady state flux obtained with HPMC: ERL 100 (3:3) was 193.2 μg/cm² /h and the same was increased to 257 μg/cm² /h with the incorporation of 5 % v/w of dimethyl sulfoxide as permeation enhancer that was 3 fold of target flux (86 μg/cm² /h). The FTIR studies showed drug-polymer compatibility. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7980 2010-01-01T00:00:00Z Transdermal drug delivery systems of venlafaxine hydrochloride were prepared by using combination of hydrophilic (HPMC E15) and hydrophobic (ERS100 and ERL 100) polymers in 1:5, 2:4, 3:3, 4:2, 5:1 ratios by solvent casting technique with 15 % v/w propylene glycol as plasticizer. The drug permeation studies revealed that drug permeation increased proportionally with increasing HPMC ratio where ERS 100 as hydrophobic polymer but in case of ERL 100 as hydrophobic polymer proportional increase was not obtained this may be due to increased diffusion path length. The drug permeation kinetics followed zero order profile with diffusion mechanism. The average steady state flux obtained with HPMC: ERL 100 (3:3) was 193.2 μg/cm² /h and the same was increased to 257 μg/cm² /h with the incorporation of 5 % v/w of dimethyl sulfoxide as permeation enhancer that was 3 fold of target flux (86 μg/cm² /h). The FTIR studies showed drug-polymer compatibility. http://sedici.unlp.edu.ar:80/handle/10915/7979 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 The present study involves development and investigation of liposomal system for improving skin residence of ciclopirox olamine in cutaneous mycosis. Spherical unilamellar liposomes of ciclopirox olamine were prepared by ethanol injection method. The vesicle size and % entrapment efficiency were in the range of 196 ± 1.73 to 1040.66 ± 7.02 nm and 34.28 ± 4.4 to 54.89 ± 1.9 respectively. The electrokinetic potential varied from -52.4 ± 2.0 to -71.7 ± 1.3 mV. A 32 factorial design was utilized to optimize the concentrations of cholesterol and Phospholipon® 90H. Cholesterol was found to be primarily responsible for the behaviour of the liposomes as compared to the phospholipid. FTIR study revealed that liposomal encapsulation preserved the principal characteristic group of ciclopirox olamine required for antifungal action. In-vitro artificial membrane and ex-vivo excised rat skin studies demonstrated reasonably higher cutaneous deposition of the drug. Liposomes proved interesting tool for maximizing the drug retention in skin, an important requisite in treatment of cutaneous fungal infections. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7979 2010-01-01T00:00:00Z The present study involves development and investigation of liposomal system for improving skin residence of ciclopirox olamine in cutaneous mycosis. Spherical unilamellar liposomes of ciclopirox olamine were prepared by ethanol injection method. The vesicle size and % entrapment efficiency were in the range of 196 ± 1.73 to 1040.66 ± 7.02 nm and 34.28 ± 4.4 to 54.89 ± 1.9 respectively. The electrokinetic potential varied from -52.4 ± 2.0 to -71.7 ± 1.3 mV. A 32 factorial design was utilized to optimize the concentrations of cholesterol and Phospholipon® 90H. Cholesterol was found to be primarily responsible for the behaviour of the liposomes as compared to the phospholipid. FTIR study revealed that liposomal encapsulation preserved the principal characteristic group of ciclopirox olamine required for antifungal action. In-vitro artificial membrane and ex-vivo excised rat skin studies demonstrated reasonably higher cutaneous deposition of the drug. Liposomes proved interesting tool for maximizing the drug retention in skin, an important requisite in treatment of cutaneous fungal infections. http://sedici.unlp.edu.ar:80/handle/10915/7978 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 High fat diet (30 % fat) was used to induce obesity in rats. Male wistar rats were kept at high fat diet for 90 days and subjected to partial abdominal aortic constriction (PAAC) at 62nd day and continued upto 90th day. Similarly rats were kept at high fat diet for 90 days and subjected to chronic swimming training (CST) at 46th day and continued upto 90th day. Obesity was assessed by measuring body weight, WHR ratio, obesity index and adiposity index. Cardiac hypertrophy was assessed by measuring left ventricular weight, left ventricular weight to body weight, left ventricular wall thickness, cardiomyocyte diameter, left ventricular protein content and left ventricular collagen content. Mean arterial blood pressure (MABP) was also recorded. Oxidative stress was assessed in terms of thiobarbituric acid reactive species (TBARS) level, superoxide anion generation level and reduced glutathione level in left ventricular tissue. Obesity, cardiac hypertrophy and oxidative stress were increased in high fat diet groups. Orlistat, lipase inhibitor, significantly attenuated the impact of obesity in experimental cardiac hypertrophy. Furthermore orlistat significantly attenuated the oxidative stress. So it can be concluded that by decreasing the impact of obesity, orlistat significantly attenuated the extent of cardiac hypertrophy. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7978 2010-01-01T00:00:00Z High fat diet (30 % fat) was used to induce obesity in rats. Male wistar rats were kept at high fat diet for 90 days and subjected to partial abdominal aortic constriction (PAAC) at 62nd day and continued upto 90th day. Similarly rats were kept at high fat diet for 90 days and subjected to chronic swimming training (CST) at 46th day and continued upto 90th day. Obesity was assessed by measuring body weight, WHR ratio, obesity index and adiposity index. Cardiac hypertrophy was assessed by measuring left ventricular weight, left ventricular weight to body weight, left ventricular wall thickness, cardiomyocyte diameter, left ventricular protein content and left ventricular collagen content. Mean arterial blood pressure (MABP) was also recorded. Oxidative stress was assessed in terms of thiobarbituric acid reactive species (TBARS) level, superoxide anion generation level and reduced glutathione level in left ventricular tissue. Obesity, cardiac hypertrophy and oxidative stress were increased in high fat diet groups. Orlistat, lipase inhibitor, significantly attenuated the impact of obesity in experimental cardiac hypertrophy. Furthermore orlistat significantly attenuated the oxidative stress. So it can be concluded that by decreasing the impact of obesity, orlistat significantly attenuated the extent of cardiac hypertrophy. http://sedici.unlp.edu.ar:80/handle/10915/7977 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 Obesity was induced by high fat diet (30 % fat by weight). Wistar rats of 225-250 g were kept on high fat diet to induce obesity for 90 days. Sodium tungstate (2 mg/ml, in drinking water) was administered for 90 days. Obesity was assessed by measuring % age change in body weight, WHR ratio, adiposity index and obesity index. Left ventricular cardiac hypertrophy was assessed in terms of left ventricular weight, left ventricular wall thickness, left ventricular protein content and left ventricular collagen content. Oxidative stress was measured in terms of levels of thiobarbituric acid reactive substances (TBARS), superoxide anion generation (SAG) and level of reduced glutathione. Sodium tungstate significantly attenuated the increase in body weight adiposity index, obesity index, TBARS, SAG and reduced glutathione, whereas no significant change was observed the parameters of cardiac hypertrophy. So, it can be concluded that sodium tungstate significantly attenuated high fat diet induced obesity and oxidative stress but no significant decrease was observed in the parameters of cardiac hypertrophy. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7977 2010-01-01T00:00:00Z Obesity was induced by high fat diet (30 % fat by weight). Wistar rats of 225-250 g were kept on high fat diet to induce obesity for 90 days. Sodium tungstate (2 mg/ml, in drinking water) was administered for 90 days. Obesity was assessed by measuring % age change in body weight, WHR ratio, adiposity index and obesity index. Left ventricular cardiac hypertrophy was assessed in terms of left ventricular weight, left ventricular wall thickness, left ventricular protein content and left ventricular collagen content. Oxidative stress was measured in terms of levels of thiobarbituric acid reactive substances (TBARS), superoxide anion generation (SAG) and level of reduced glutathione. Sodium tungstate significantly attenuated the increase in body weight adiposity index, obesity index, TBARS, SAG and reduced glutathione, whereas no significant change was observed the parameters of cardiac hypertrophy. So, it can be concluded that sodium tungstate significantly attenuated high fat diet induced obesity and oxidative stress but no significant decrease was observed in the parameters of cardiac hypertrophy. http://sedici.unlp.edu.ar:80/handle/10915/7976 Articulo Latin American Journal of Pharmacy; vol. 29, no. 5 The objective of the present study was to stabilize doxorubicin hydrochloride in sugar-phosphate amorphous mixtures at ambient temperature by drying it with vacuum foam drying. Finished products were evaluated for foam characteristic, residual moisture content, reconstitution time, percent drug recovery and drug-excipient interactions. FTIR studies revealed existence of physical interaction of drug with sugar. Light microscopy showed formation of amorphous glass which was supported by the observations of XRPD analyses. The optimized composition in vacuum foam drying was processed by lyophilization and their stability was compared. Storage at ambient temperature for 6 months showed that stability of vacuum foam dried product was better than lyophilized products. The amount of residual moisture affected the stability of drug. The detailed study revealed lactose and sodium dihydrogen phosphate is best suited for stabilization of doxorubicin hydrochloride at room temperature. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/7976 2010-01-01T00:00:00Z The objective of the present study was to stabilize doxorubicin hydrochloride in sugar-phosphate amorphous mixtures at ambient temperature by drying it with vacuum foam drying. Finished products were evaluated for foam characteristic, residual moisture content, reconstitution time, percent drug recovery and drug-excipient interactions. FTIR studies revealed existence of physical interaction of drug with sugar. Light microscopy showed formation of amorphous glass which was supported by the observations of XRPD analyses. The optimized composition in vacuum foam drying was processed by lyophilization and their stability was compared. Storage at ambient temperature for 6 months showed that stability of vacuum foam dried product was better than lyophilized products. The amount of residual moisture affected the stability of drug. The detailed study revealed lactose and sodium dihydrogen phosphate is best suited for stabilization of doxorubicin hydrochloride at room temperature.