http://sedici.unlp.edu.ar:80/handle/10915/231 Sun, 15 Nov 2026 06:05:02 GMT 2026-11-15T06:05:02Z http://sedici.unlp.edu.ar:80/handle/10915/8027 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 Seveal Baccharis species known as "carquejas" are used in Argentinean folk medicine as phytotherapics. B. crispa, B. articulata, B. trimera, B. sagittalis and B. triangularis have been evaluated for their choleretic activity using Wistar rats. B. sagittalis and B. triangularis showed a significant choleretic activity (bile flow of 1.631 ± 0.089 and 1.598 ± 0.196 μl/min/g liver, respectively). B. crispa, B. trimera showed moderate activity and B. articulata exhibited the same choleretic property that the control. Only, B. articulata and B. crispa are informed as official drugs in the Argentinean Pharmacopoeia. In addition, phytochemical constituents and botanical characters are reported Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8027 2010-01-01T00:00:00Z Seveal Baccharis species known as "carquejas" are used in Argentinean folk medicine as phytotherapics. B. crispa, B. articulata, B. trimera, B. sagittalis and B. triangularis have been evaluated for their choleretic activity using Wistar rats. B. sagittalis and B. triangularis showed a significant choleretic activity (bile flow of 1.631 ± 0.089 and 1.598 ± 0.196 μl/min/g liver, respectively). B. crispa, B. trimera showed moderate activity and B. articulata exhibited the same choleretic property that the control. Only, B. articulata and B. crispa are informed as official drugs in the Argentinean Pharmacopoeia. In addition, phytochemical constituents and botanical characters are reported http://sedici.unlp.edu.ar:80/handle/10915/8026 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 Escherichia coli is known to produce enterotoxins whose properties and its role in diarrheal disease has been extensively investigated. Some species of Staphylococcus are often recognized as etiological agents of many animal and human opportunistic infections. This study is the first test of change in resistance of antibiotic activity by Cordia verbenacea DC. against multiresistant strains of Escherichia coli and Staphylococcus aureus. In this study, the hexane and methanol extract of Cordia verbenacea DC. were tested for antibacterial activity alone and in combination with aminoglycosides against bacterial strains. The synergy of the methanolic and hexane were verified by microdilution method. A synergistic effect of both extracts combined with the aminoglycosides was demonstrated. It is therefore suggested that the extracts from Cordia verbenacea DC. could be used as a source of natural products derived from this plant with resistance-modifying antibacterial activity, providing a new weapon against the problem of bacterial resistance to antibiotics. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8026 2010-01-01T00:00:00Z Escherichia coli is known to produce enterotoxins whose properties and its role in diarrheal disease has been extensively investigated. Some species of Staphylococcus are often recognized as etiological agents of many animal and human opportunistic infections. This study is the first test of change in resistance of antibiotic activity by Cordia verbenacea DC. against multiresistant strains of Escherichia coli and Staphylococcus aureus. In this study, the hexane and methanol extract of Cordia verbenacea DC. were tested for antibacterial activity alone and in combination with aminoglycosides against bacterial strains. The synergy of the methanolic and hexane were verified by microdilution method. A synergistic effect of both extracts combined with the aminoglycosides was demonstrated. It is therefore suggested that the extracts from Cordia verbenacea DC. could be used as a source of natural products derived from this plant with resistance-modifying antibacterial activity, providing a new weapon against the problem of bacterial resistance to antibiotics. http://sedici.unlp.edu.ar:80/handle/10915/8025 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 Sulphonylureas (SUs) are commonly prescribed in Malaysia and also worldwide. However, very limited information is available on their pattern of use and appropriateness of its utilization. Age, concurrent use of drugs such as beta blocker, salicylate and frusemide and also renal impairment were found to have influence on the selection of different types of SUs. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8025 2010-01-01T00:00:00Z Sulphonylureas (SUs) are commonly prescribed in Malaysia and also worldwide. However, very limited information is available on their pattern of use and appropriateness of its utilization. Age, concurrent use of drugs such as beta blocker, salicylate and frusemide and also renal impairment were found to have influence on the selection of different types of SUs. http://sedici.unlp.edu.ar:80/handle/10915/8024 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 A simple and sensitive LC-ESI-MS method for determination of norvancomycin in plasma was developed and validated over the concentration range of 20-2,000 ng/mL. After addition of vancomycin as internal standard (IS), protein precipitation with 5 % trichloroacetic acid was employed for the sample preparation. Chromatographic separation was performed on a Zorbax SB-C18 (100 mm×2.1 mm, 3.5 μm) column with 10:90 (v/v) acetonitrile-0.1 % formic acid as mobile phase. The MS data acquisition was accomplished by selective ions monitoring (SIM) mode with positive electrospray ionization (ESI) interface. The limit of quantification (LOQ) was 20 ng/mL. For inter-day and intra-day tests, the precision (RSD) for the entire validation was less than 12 %. The developed method was successfully applied to pharmacokinetic studies of norvancomycin in rats following single intravenous administration dose of 10 mg/Kg. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8024 2010-01-01T00:00:00Z A simple and sensitive LC-ESI-MS method for determination of norvancomycin in plasma was developed and validated over the concentration range of 20-2,000 ng/mL. After addition of vancomycin as internal standard (IS), protein precipitation with 5 % trichloroacetic acid was employed for the sample preparation. Chromatographic separation was performed on a Zorbax SB-C18 (100 mm×2.1 mm, 3.5 μm) column with 10:90 (v/v) acetonitrile-0.1 % formic acid as mobile phase. The MS data acquisition was accomplished by selective ions monitoring (SIM) mode with positive electrospray ionization (ESI) interface. The limit of quantification (LOQ) was 20 ng/mL. For inter-day and intra-day tests, the precision (RSD) for the entire validation was less than 12 %. The developed method was successfully applied to pharmacokinetic studies of norvancomycin in rats following single intravenous administration dose of 10 mg/Kg. http://sedici.unlp.edu.ar:80/handle/10915/8023 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 In this work, we present antibacterial activity of a 22 phenylpropanoids derived from cinnamic acid, recently reported as antifungal agents by our group. Some of these compounds are commercial, others are natural products and some of them were obtained by synthesis. Antibacterial activity was determined in two stages. At first, a screening was made by an easy, economic and fast assay using a commercial lyophilized of Gram (+) bacteria. Compounds that showed activity at the screening were tested against Gram (+) and Gram (-) pathogens. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8023 2010-01-01T00:00:00Z In this work, we present antibacterial activity of a 22 phenylpropanoids derived from cinnamic acid, recently reported as antifungal agents by our group. Some of these compounds are commercial, others are natural products and some of them were obtained by synthesis. Antibacterial activity was determined in two stages. At first, a screening was made by an easy, economic and fast assay using a commercial lyophilized of Gram (+) bacteria. Compounds that showed activity at the screening were tested against Gram (+) and Gram (-) pathogens. http://sedici.unlp.edu.ar:80/handle/10915/8022 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 A predictive in vitro-invivo correlation (IVIVC) can empower in vitro dissolution as a surrogate for in vivo bioavailability / bioequivalence. IVIVCs can decrease regulatory burden by decreasing the number of biostudies required in support of a drug product. The present study concerns the establishment of in vitro-in vivo correlation for three different sustained release nimesulide loaded ethylcellulose microparticulate formulations (M1, M2 and M3) and conventional tablet (100 mg Nimaran®-Novartis, Pakistan). In vitro dissolution study was conducted in phosphate buffer pH 6.8 stirred at 50 rpm and 37 ± 0.5ºC. A validated HPLC method was adopted to conduct bioavailability studies in young healthy human volunteers. Ultimately IVIVC of prepared microparticles and conventional tablet was established using Wagner-Nelson method. M1 and M2 formulations and Nimaran® exhibited good linear IVIVC (R² = 0.9220, 0.9124, 0.8728, respectively) as compared to M3 (R² = 0.9449). The results substantiate the success of this mathematical simulation study encourage researchers to conduct biowaiver studies for other BCS class II drugs. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8022 2010-01-01T00:00:00Z A predictive in vitro-invivo correlation (IVIVC) can empower in vitro dissolution as a surrogate for in vivo bioavailability / bioequivalence. IVIVCs can decrease regulatory burden by decreasing the number of biostudies required in support of a drug product. The present study concerns the establishment of in vitro-in vivo correlation for three different sustained release nimesulide loaded ethylcellulose microparticulate formulations (M1, M2 and M3) and conventional tablet (100 mg Nimaran®-Novartis, Pakistan). In vitro dissolution study was conducted in phosphate buffer pH 6.8 stirred at 50 rpm and 37 ± 0.5ºC. A validated HPLC method was adopted to conduct bioavailability studies in young healthy human volunteers. Ultimately IVIVC of prepared microparticles and conventional tablet was established using Wagner-Nelson method. M1 and M2 formulations and Nimaran® exhibited good linear IVIVC (R² = 0.9220, 0.9124, 0.8728, respectively) as compared to M3 (R² = 0.9449). The results substantiate the success of this mathematical simulation study encourage researchers to conduct biowaiver studies for other BCS class II drugs. http://sedici.unlp.edu.ar:80/handle/10915/8021 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 The high incidence of diarrhea in the population demands a search for new therapeutic options and easy access, mainly from plant-based sources. Leaves and bark of Guazuma ulmifolia Lam. (Sterculiaceae) are popularly employed against diarrhea. However, no information was found in the literature about this supposed property of the drug. In this study we evaluated in vivo antidiarrheal activity of stem bark extracts from G. ulmifolia in mice, and in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Salmonella sp., Shigella flexneri, and Pseudomonas aeruginosa by using the microdilution method. The n-BuOH semipurified fraction (GU#3) significantly reduced intestinal motility. The extracts did not show antimicrobial activity. G. ulmifolia Lam. had non-specific antidiarrheal, and antimotility activity in the experimental models studied, and could be used as an alternative treatment for non-infectious diarrhea. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8021 2010-01-01T00:00:00Z The high incidence of diarrhea in the population demands a search for new therapeutic options and easy access, mainly from plant-based sources. Leaves and bark of Guazuma ulmifolia Lam. (Sterculiaceae) are popularly employed against diarrhea. However, no information was found in the literature about this supposed property of the drug. In this study we evaluated in vivo antidiarrheal activity of stem bark extracts from G. ulmifolia in mice, and in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Salmonella sp., Shigella flexneri, and Pseudomonas aeruginosa by using the microdilution method. The n-BuOH semipurified fraction (GU#3) significantly reduced intestinal motility. The extracts did not show antimicrobial activity. G. ulmifolia Lam. had non-specific antidiarrheal, and antimotility activity in the experimental models studied, and could be used as an alternative treatment for non-infectious diarrhea. http://sedici.unlp.edu.ar:80/handle/10915/8020 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 A simple, rapid, sensitive and economical method has been developed for the simultaneous determination of montelukast sodium and levocetirizine dihydrochloride in combined tablet dosage form. The method was based on high performance liquid chromatography using zidovudine as an internal standard. The separation was carried out with a Eurosphere 100 C18 column (250×4.6 mm ID, 5 μm) and mobile phase 0.05 % orthophosphoric acid: methanol (10:90 v/v) at flow rate 1.2 ml/min. The UV detection was carried out at wavelength 225 nm.The method was validated statistically and by performing recovery study. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8020 2010-01-01T00:00:00Z A simple, rapid, sensitive and economical method has been developed for the simultaneous determination of montelukast sodium and levocetirizine dihydrochloride in combined tablet dosage form. The method was based on high performance liquid chromatography using zidovudine as an internal standard. The separation was carried out with a Eurosphere 100 C18 column (250×4.6 mm ID, 5 μm) and mobile phase 0.05 % orthophosphoric acid: methanol (10:90 v/v) at flow rate 1.2 ml/min. The UV detection was carried out at wavelength 225 nm.The method was validated statistically and by performing recovery study. http://sedici.unlp.edu.ar:80/handle/10915/8019 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 The purpose of this study was to attain and characterize ternary complexes of simvastatin, β-cyclodextrin (βCD) and different polymers, and then select those that lead to a greater increase in drug solubility. The complexes were prepared with the co-evaporation method and the polymers used were polyethylene glycol 1500, polyethylene glycol 4000, povidone, copovidone, crospovidone, maltodextrin and hydroxypropyl methyl cellulose. The characterization of complexes was carried out through aqueous solubility, DSC and TG. There was an increase in solubility for all the complexes prepared with βCD and the different polymers, but only when crospovidone and maltodextrin were used was there a significant difference observed between the solubility of the physical mixture and that of the complex. The DSC curves indicate that the non-complexed drug is even in the sample of the complex with higher solubility, thus none of the polymers was able to achieve a total complexation of the drug. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8019 2010-01-01T00:00:00Z The purpose of this study was to attain and characterize ternary complexes of simvastatin, β-cyclodextrin (βCD) and different polymers, and then select those that lead to a greater increase in drug solubility. The complexes were prepared with the co-evaporation method and the polymers used were polyethylene glycol 1500, polyethylene glycol 4000, povidone, copovidone, crospovidone, maltodextrin and hydroxypropyl methyl cellulose. The characterization of complexes was carried out through aqueous solubility, DSC and TG. There was an increase in solubility for all the complexes prepared with βCD and the different polymers, but only when crospovidone and maltodextrin were used was there a significant difference observed between the solubility of the physical mixture and that of the complex. The DSC curves indicate that the non-complexed drug is even in the sample of the complex with higher solubility, thus none of the polymers was able to achieve a total complexation of the drug. http://sedici.unlp.edu.ar:80/handle/10915/8018 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 Acorus calamus (Araceae) is commonly known in India as sweet flag and has been used in traditional medicine as a remedy for pain, convulsion, inflammation, and ulcer. In the present work, the methanolic extract of Acorus calamus roots (MEAC) was assessed for different psychopharmacological activities in rats and mice by evaluation of general, exploratory behaviour, phenobarbitone sodium-induced sleeping time and muscle relaxant activity. The extract at doses 100 mg/kg and above exhibited a reduction in spontaneous activity and a decrease in exploratory behavioural pattern was observed. Also a significant reduction in muscle relaxant activity and potentiated phenobarbitone sodium-induced sleeping time in mice was noted in MEAC treated groups. From our study, the results indicates that MEAC appears to have effects on alteration in general behavior pattern, evident from the spontaneous activity, sound, touch and pain responses of the MEAC treated groups. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8018 2010-01-01T00:00:00Z Acorus calamus (Araceae) is commonly known in India as sweet flag and has been used in traditional medicine as a remedy for pain, convulsion, inflammation, and ulcer. In the present work, the methanolic extract of Acorus calamus roots (MEAC) was assessed for different psychopharmacological activities in rats and mice by evaluation of general, exploratory behaviour, phenobarbitone sodium-induced sleeping time and muscle relaxant activity. The extract at doses 100 mg/kg and above exhibited a reduction in spontaneous activity and a decrease in exploratory behavioural pattern was observed. Also a significant reduction in muscle relaxant activity and potentiated phenobarbitone sodium-induced sleeping time in mice was noted in MEAC treated groups. From our study, the results indicates that MEAC appears to have effects on alteration in general behavior pattern, evident from the spontaneous activity, sound, touch and pain responses of the MEAC treated groups. http://sedici.unlp.edu.ar:80/handle/10915/8017 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 This study evaluated the effect of Cordia verbenacea essential oil (CV) and glycolic acid 70 % (GA), isolated and associated, on Wistar rats back skin. A base gel was added to 2 % of CV and/or 10 % of GA, thus forming 4 formulations: 1) GA + CV, 2) CV, 3) GA, and 4) gel base. All formulation had their final pH adjusted to 3,5 and were applied once daily, for 15 consecutive days, on 4 areas with 1 cm2, while another area without application (control). Statistical analysis of biopsies showed no difference in epidermis thickness and stratum corneum. Among fibroblast counts there was a statistical significance for groups exposed to the GA and to the association. Only in the group exposed to GAT there was significant difference in leukocytes number. The association of GA with CV proved favorable because it increased fibroblast counts without increasing leukocyte numbers, meaning inflammatory reaction may be reduced Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8017 2010-01-01T00:00:00Z This study evaluated the effect of Cordia verbenacea essential oil (CV) and glycolic acid 70 % (GA), isolated and associated, on Wistar rats back skin. A base gel was added to 2 % of CV and/or 10 % of GA, thus forming 4 formulations: 1) GA + CV, 2) CV, 3) GA, and 4) gel base. All formulation had their final pH adjusted to 3,5 and were applied once daily, for 15 consecutive days, on 4 areas with 1 cm2, while another area without application (control). Statistical analysis of biopsies showed no difference in epidermis thickness and stratum corneum. Among fibroblast counts there was a statistical significance for groups exposed to the GA and to the association. Only in the group exposed to GAT there was significant difference in leukocytes number. The association of GA with CV proved favorable because it increased fibroblast counts without increasing leukocyte numbers, meaning inflammatory reaction may be reduced http://sedici.unlp.edu.ar:80/handle/10915/8016 Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 6 Nowadays there are no official in vitro methods to determine TiO2, ZnO or other inorganic elements in sunscreen cosmetics. The objective of this work is to determine the concentration of several inorganic elements in sunscreen composition, without sample preparation, by employing a portable Energy Dispersive X-Ray Fluorescence (EDXRF) device. Particularly in the case of TiO2 and ZnO, the aim is also to estimate their Sun Protection Factor (SPF) due to the physical protection barrier. A sensitivity curve for the determination of inorganic elements in sunscreen, with atomic numbers ranging from 19 to 35, is presented. Fifteen commercial samples with different SPF from different brands were analyzed. It was determined TiO2 and ZnO concentrations with their respective SPF values, as well as to detect the presence of K, Br, Sr and Ce in the sunscreen samples by identifying and quantifying chemical elements that had not been mentioned in the formulations. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8016 2010-01-01T00:00:00Z Nowadays there are no official in vitro methods to determine TiO2, ZnO or other inorganic elements in sunscreen cosmetics. The objective of this work is to determine the concentration of several inorganic elements in sunscreen composition, without sample preparation, by employing a portable Energy Dispersive X-Ray Fluorescence (EDXRF) device. Particularly in the case of TiO2 and ZnO, the aim is also to estimate their Sun Protection Factor (SPF) due to the physical protection barrier. A sensitivity curve for the determination of inorganic elements in sunscreen, with atomic numbers ranging from 19 to 35, is presented. Fifteen commercial samples with different SPF from different brands were analyzed. It was determined TiO2 and ZnO concentrations with their respective SPF values, as well as to detect the presence of K, Br, Sr and Ce in the sunscreen samples by identifying and quantifying chemical elements that had not been mentioned in the formulations. http://sedici.unlp.edu.ar:80/handle/10915/8015 Articulo Latin American Journal of Pharmacy; vol. 29, no. 6 The aim of the present investigation was to develop a modified release effervescent floating drug delivery system of famotidine for 12 h dosage regimen to improve its bioavailability. Effervescent floating tablets were prepared by direct compression method taking into account its advantages over wet granulation by using directly compressible excipients like Carbopol® 71G and Cellactose® 80. The incorporation of sodium bicarbonate aided in the buoyancy with effervescent approach. The prepared tablets were evaluated for floating lag time (FLT), total floating time (TFT), in vitro drug release along with general parameters. 23 factorial design was used for optimization. The tablets showed desired release of more than 98 % over the period of 12 h which may increase bioavailability of selected candidate. The release of famotidine was found to be influenced by the polymer concentration. Optimized formulation showed acceptable stability over three months at 40 ºC and 75 % RH. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8015 2010-01-01T00:00:00Z The aim of the present investigation was to develop a modified release effervescent floating drug delivery system of famotidine for 12 h dosage regimen to improve its bioavailability. Effervescent floating tablets were prepared by direct compression method taking into account its advantages over wet granulation by using directly compressible excipients like Carbopol® 71G and Cellactose® 80. The incorporation of sodium bicarbonate aided in the buoyancy with effervescent approach. The prepared tablets were evaluated for floating lag time (FLT), total floating time (TFT), in vitro drug release along with general parameters. 23 factorial design was used for optimization. The tablets showed desired release of more than 98 % over the period of 12 h which may increase bioavailability of selected candidate. The release of famotidine was found to be influenced by the polymer concentration. Optimized formulation showed acceptable stability over three months at 40 ºC and 75 % RH. http://sedici.unlp.edu.ar:80/handle/10915/8014 Articulo Latin American Journal of Pharmacy; vol. 29, no. 6 This study introduced a novel phase separation technique for the microencapsulation of metoprolol tartrate as a model. Non-solvent addition coacervation technique was employed for the loading of drug into ethylcellulose, a hydrophobic plastic polymer. Dichloromethane (DCM) and paraffin oil were employed as solvent and non-solvent, respectively. Microparticle batches abbreviated as M1, M2 and M3 were formulated by embedding 1 g of drug into 1 g, 2 g and 3 g of polymer, respectively followed by direct compression into tabletted microparticulate batches named a T1, T2 and T3, respectively. The drug and polymer remained intact in encapsulated form as confirmed by FTIR, XRD and DSC. However, a slight change in drug nature from crystalline to amorphous behavior and an endothermic peak for metoprolol tartrate at 130 ºC was observed in drug and microparticle thermograms. Slightly aggregated spherical free flowing microparticles in a size range of 64 μm-103 μm were obtained. The entrapment efficiency ranged from 77% to 89%. The straight line obtained from a plot between square root of time (Hrs) versus drug release (%) and regression co-efficient (R²) confirmed that best fit model to all dissolution profiles was Higuchi's model. The modes of drug release from microparticles and tabletted microparticles were Quasi-Fickian diffusion and anomalous diffusion, respectively. T3 was selected as an optimum formulation as its dissolution profile resembled (f₂ = 76.25) Mepressor® (Novartis Pharma-Pakistan). The accelerated stability study, regarding dissolution behavior and drug contents, at 40ºC/75% RH proved T3 stable in 40 ºC/75% RH for six months. Non-solvent addition coacervation technique involving comparatively safe solvents such as dichloromethane and paraffin oil as solvent and non-solvent, respectively is a good techniques for the encapsulation of Biopharmaceutics Classification System class I drugs such as metoprolol tartrate. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8014 2010-01-01T00:00:00Z This study introduced a novel phase separation technique for the microencapsulation of metoprolol tartrate as a model. Non-solvent addition coacervation technique was employed for the loading of drug into ethylcellulose, a hydrophobic plastic polymer. Dichloromethane (DCM) and paraffin oil were employed as solvent and non-solvent, respectively. Microparticle batches abbreviated as M1, M2 and M3 were formulated by embedding 1 g of drug into 1 g, 2 g and 3 g of polymer, respectively followed by direct compression into tabletted microparticulate batches named a T1, T2 and T3, respectively. The drug and polymer remained intact in encapsulated form as confirmed by FTIR, XRD and DSC. However, a slight change in drug nature from crystalline to amorphous behavior and an endothermic peak for metoprolol tartrate at 130 ºC was observed in drug and microparticle thermograms. Slightly aggregated spherical free flowing microparticles in a size range of 64 μm-103 μm were obtained. The entrapment efficiency ranged from 77% to 89%. The straight line obtained from a plot between square root of time (Hrs) versus drug release (%) and regression co-efficient (R²) confirmed that best fit model to all dissolution profiles was Higuchi's model. The modes of drug release from microparticles and tabletted microparticles were Quasi-Fickian diffusion and anomalous diffusion, respectively. T3 was selected as an optimum formulation as its dissolution profile resembled (f₂ = 76.25) Mepressor® (Novartis Pharma-Pakistan). The accelerated stability study, regarding dissolution behavior and drug contents, at 40ºC/75% RH proved T3 stable in 40 ºC/75% RH for six months. Non-solvent addition coacervation technique involving comparatively safe solvents such as dichloromethane and paraffin oil as solvent and non-solvent, respectively is a good techniques for the encapsulation of Biopharmaceutics Classification System class I drugs such as metoprolol tartrate. http://sedici.unlp.edu.ar:80/handle/10915/8013 Articulo Prescription and dispensation of medicines for hipothyroid patientsin Córdoba city, Argentina Latin American Journal of Pharmacy; vol. 29, no. 6 Se analizaron las características de prescripción y dispensación de medicamentos en una población de pacientes hipotiroideos, así como el conocimiento de los mismos sobre su terapia. Se trabajó con un procedimiento normalizado analizando 948 prescripciones médicas en 42 farmacias comunitarias de Córdoba (Argentina). Los laboratorios autorizados para elaborar medicamentos con levotiroxina fueron siete, en 12 concentraciones distintas (desde 25 a 300 μg). En este estudio una sola marca abarcó el 59 % de las prescripciones médicas. El 85 % de los usuarios fueron mujeres, principalmente entre 41-60 años. En cuanto al uso del medicamento el 78 % manifestó tomar el mismo una vez al día y el 42 % lo utiliza desde hace más de 5 años. El 70 % eran pacientes habituales de las farmacias y el 9 % realizó una consulta al farmacéutico respecto al uso del medicamento. Los estudios de utilización de medicamentos permiten evaluar las enfermedades en un contexto comunitario, donde el farmacéutico puede aportar datos epidemiológicos que contribuyan al conocimiento, prevención y control de las patologías.; Characteristics of prescription, dispensation of medicines for hipothyroid patients and the knowledge of their therapy were analysed. We worked with a normalized procedure, analyzing 948 medical prescription in 42 community pharmacies of Córdoba (Argentina). Seven laboratories are authorized to make medicines with levotiroxine, with concentrations of 25-300 μg in 12 different forms, but only one brand included 59 % of the medical prescription 85 % of the users were women, mainly between the ages of 41-60 years. 78 % took levotiroxine once a day and 42 % had been using it for more than 5 years. 9 % realized an additional consultation to the pharmacist, and 70 % were frecuent patients of the pharmacies. The studies of utilization of medicines allow to evaluation of diseases in a community context, where the pharmacist could offer epidemiological information that may contribute to the knowledge, prevention and control of the diseases. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8013 2010-01-01T00:00:00Z Se analizaron las características de prescripción y dispensación de medicamentos en una población de pacientes hipotiroideos, así como el conocimiento de los mismos sobre su terapia. Se trabajó con un procedimiento normalizado analizando 948 prescripciones médicas en 42 farmacias comunitarias de Córdoba (Argentina). Los laboratorios autorizados para elaborar medicamentos con levotiroxina fueron siete, en 12 concentraciones distintas (desde 25 a 300 μg). En este estudio una sola marca abarcó el 59 % de las prescripciones médicas. El 85 % de los usuarios fueron mujeres, principalmente entre 41-60 años. En cuanto al uso del medicamento el 78 % manifestó tomar el mismo una vez al día y el 42 % lo utiliza desde hace más de 5 años. El 70 % eran pacientes habituales de las farmacias y el 9 % realizó una consulta al farmacéutico respecto al uso del medicamento. Los estudios de utilización de medicamentos permiten evaluar las enfermedades en un contexto comunitario, donde el farmacéutico puede aportar datos epidemiológicos que contribuyan al conocimiento, prevención y control de las patologías. Characteristics of prescription, dispensation of medicines for hipothyroid patients and the knowledge of their therapy were analysed. We worked with a normalized procedure, analyzing 948 medical prescription in 42 community pharmacies of Córdoba (Argentina). Seven laboratories are authorized to make medicines with levotiroxine, with concentrations of 25-300 μg in 12 different forms, but only one brand included 59 % of the medical prescription 85 % of the users were women, mainly between the ages of 41-60 years. 78 % took levotiroxine once a day and 42 % had been using it for more than 5 years. 9 % realized an additional consultation to the pharmacist, and 70 % were frecuent patients of the pharmacies. The studies of utilization of medicines allow to evaluation of diseases in a community context, where the pharmacist could offer epidemiological information that may contribute to the knowledge, prevention and control of the diseases. http://sedici.unlp.edu.ar:80/handle/10915/8012 Articulo Latin American Journal of Pharmacy; vol. 29, no. 6 A series of N-[(2-chloro-7-methylquinolin-3-yl)methyl]-(substituted)-aniline/butan-1-amine/cyclohexamine derivatives (4a-n) & N-benzyl-1-(2-chloro-7-methylquinolin-3-yl)methanamine (4o) was designed and synthesized based on the structural requirements essential for allylamine / benzylamine antimycotics. Compounds (4a-o) were synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-7- methylquinoline with substituted aromatic/aliphatic primary amine in absolute ethanol in presence of triethylamine. The structures of all new products were confirmed by IR, 1H & 13C-NMR and mass spectral data. The newly synthesized compounds were screened in-vitro for their antifungal activity against Aspergillus niger MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM 768 by cup plate method. Preliminary screening of compounds (4a-o) revealed that compounds viz. 4a, 4b, 4e, 4g, 4j and 4l showed excellent antifungal activity. Dihalogen and benzyl substituted compounds 4j, 4l & 4o exhibited potent antifungal activity. Replacement of phenyl ring with aliphatic groups like butyl or cyclohexyl causes substantial decrease in antifungal activity and activity decreases when phenyl ring is substituted with electron releasing groups. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8012 2010-01-01T00:00:00Z A series of N-[(2-chloro-7-methylquinolin-3-yl)methyl]-(substituted)-aniline/butan-1-amine/cyclohexamine derivatives (4a-n) & N-benzyl-1-(2-chloro-7-methylquinolin-3-yl)methanamine (4o) was designed and synthesized based on the structural requirements essential for allylamine / benzylamine antimycotics. Compounds (4a-o) were synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-7- methylquinoline with substituted aromatic/aliphatic primary amine in absolute ethanol in presence of triethylamine. The structures of all new products were confirmed by IR, 1H & 13C-NMR and mass spectral data. The newly synthesized compounds were screened in-vitro for their antifungal activity against Aspergillus niger MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM 768 by cup plate method. Preliminary screening of compounds (4a-o) revealed that compounds viz. 4a, 4b, 4e, 4g, 4j and 4l showed excellent antifungal activity. Dihalogen and benzyl substituted compounds 4j, 4l & 4o exhibited potent antifungal activity. Replacement of phenyl ring with aliphatic groups like butyl or cyclohexyl causes substantial decrease in antifungal activity and activity decreases when phenyl ring is substituted with electron releasing groups. http://sedici.unlp.edu.ar:80/handle/10915/8011 Articulo Latin American Journal of Pharmacy; vol. 29, no. 6 A simple UV-spectrophotometric method was developed and validated for the analysis and dissolution studies of sitagliptin phosphate in tablets. Specificity test indicated an adequate UV detection at 267 nm. The method was validated regarding Specificity/accuracy/precision (RSD < 2 %), linearity (r2 = 0.9999), and partial robustness. Tablets uniformity was 102.52 % (RSD = 2.54 %). The method was applied for the determination of the drug in commercial tablet preparations and proved to be reliable for quantification It was also used for the comparison of dissolution profiles of sitagliptin tablets. After dissolution tests comparing eight different conditions through dissolution efficiency (DE), the chosen condition for posterior tests was USP apparatus 1 (basket) in 0.01M HCl pH 3.0, at a stirring rate of 50 rpm. The methodology was applied to two batches of sitagliptin phosphate tablets, giving similar dissolution profiles compared by the difference and similarity factor, obtaining values within the specified limits. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8011 2010-01-01T00:00:00Z A simple UV-spectrophotometric method was developed and validated for the analysis and dissolution studies of sitagliptin phosphate in tablets. Specificity test indicated an adequate UV detection at 267 nm. The method was validated regarding Specificity/accuracy/precision (RSD < 2 %), linearity (r2 = 0.9999), and partial robustness. Tablets uniformity was 102.52 % (RSD = 2.54 %). The method was applied for the determination of the drug in commercial tablet preparations and proved to be reliable for quantification It was also used for the comparison of dissolution profiles of sitagliptin tablets. After dissolution tests comparing eight different conditions through dissolution efficiency (DE), the chosen condition for posterior tests was USP apparatus 1 (basket) in 0.01M HCl pH 3.0, at a stirring rate of 50 rpm. The methodology was applied to two batches of sitagliptin phosphate tablets, giving similar dissolution profiles compared by the difference and similarity factor, obtaining values within the specified limits. http://sedici.unlp.edu.ar:80/handle/10915/8010 Articulo Latin American Journal of Pharmacy; vol. 29, no. 6 The combination of the bulb of Fritillaria ussuriensis Maxim. (Bulbus Fritillariae ussuriensis, BFU) and the fruit of Pyrus bretschneideri Rehd. (Xuehua pear, PBR), as folk medicine, is widely used in treatment with respiratory disease. In this study, three acute inflammatory models were used to estimate the anti-inflammatory activities and cooperative interactions of them. The data were dealt with the Tallarida's improved contouring method and the Q value method to evaluate the cooperative interactions of BFU and PBR more directly. All the treated groups showed well preventive effects on xylene-induced mouse auricular edema, acetic acid-induced mouse vascular permeation and carrageenin-induced rat paw edema in a dose-dependent manner. Combination of BFU and PBR (CBP) exhibited a higher inhibitory effect than the additive effect of individuals. These results indicated that BFU and PBR both had good antiinflammatory effects and the combination of them had synergistic effects on acute inflammation, which may support and supplement the civilian utilization of Bulbus Fritillariae and Fructus Pyri in treatment with the respiratory tract diseases, just like pharyngitis, laryngitis, tonsillitis, etc. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8010 2010-01-01T00:00:00Z The combination of the bulb of Fritillaria ussuriensis Maxim. (Bulbus Fritillariae ussuriensis, BFU) and the fruit of Pyrus bretschneideri Rehd. (Xuehua pear, PBR), as folk medicine, is widely used in treatment with respiratory disease. In this study, three acute inflammatory models were used to estimate the anti-inflammatory activities and cooperative interactions of them. The data were dealt with the Tallarida's improved contouring method and the Q value method to evaluate the cooperative interactions of BFU and PBR more directly. All the treated groups showed well preventive effects on xylene-induced mouse auricular edema, acetic acid-induced mouse vascular permeation and carrageenin-induced rat paw edema in a dose-dependent manner. Combination of BFU and PBR (CBP) exhibited a higher inhibitory effect than the additive effect of individuals. These results indicated that BFU and PBR both had good antiinflammatory effects and the combination of them had synergistic effects on acute inflammation, which may support and supplement the civilian utilization of Bulbus Fritillariae and Fructus Pyri in treatment with the respiratory tract diseases, just like pharyngitis, laryngitis, tonsillitis, etc. http://sedici.unlp.edu.ar:80/handle/10915/8009 Articulo Latin American Journal of Pharmacy; vol. 29, no. 6 The purpose of this research was to formulate fast-disintegrating tablets of famotidine by using tasteless complex of famotidine. Famotidine is a commonly used antiulcer drug but major disadvantage is its bitterness and low bioavailability. A fast-disintegrating dosage form has been developed as a user- friendly formulation that disintegrates in the mouth immediately. In this study the bitter taste of famotidine was masked by making complex with ion exchange resin Indion 214. The drug-resin complexes were characterized by infrared spectroscopy and thermal analysis. Famotidine oral fast disintegrating tablets were prepared by direct compression method by using different superdisintegrants. The prepared tablets were found to comply with various official specifications. Tablet containing crospovidone as superdisintegrating agent showed superior organoleptic properties, along with excellent in vitro disintegrating time and drug release, as compared to other formulation. The in vivo anti ulcer activity in rats shown that there was no bioavailability change due to complexation and tablet had good antiulcer activity. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8009 2010-01-01T00:00:00Z The purpose of this research was to formulate fast-disintegrating tablets of famotidine by using tasteless complex of famotidine. Famotidine is a commonly used antiulcer drug but major disadvantage is its bitterness and low bioavailability. A fast-disintegrating dosage form has been developed as a user- friendly formulation that disintegrates in the mouth immediately. In this study the bitter taste of famotidine was masked by making complex with ion exchange resin Indion 214. The drug-resin complexes were characterized by infrared spectroscopy and thermal analysis. Famotidine oral fast disintegrating tablets were prepared by direct compression method by using different superdisintegrants. The prepared tablets were found to comply with various official specifications. Tablet containing crospovidone as superdisintegrating agent showed superior organoleptic properties, along with excellent in vitro disintegrating time and drug release, as compared to other formulation. The in vivo anti ulcer activity in rats shown that there was no bioavailability change due to complexation and tablet had good antiulcer activity. http://sedici.unlp.edu.ar:80/handle/10915/8008 Articulo Essential oil of Thymus vulgaris: preparation of pharmaceutical mouthwash formulation and in vitro evaluation of the bacterial plaque-inhibiting properties Latin American Journal of Pharmacy; vol. 29, no. 6 O objetivo deste estudo foi avaliar in vitro o efeito do óleo essencial de Thymus vulgaris (tomilho) puro ou incorporado em uma formulação farmacêutica de uso oral (enxaguatório bucal), frente ao Streptococcus mutans (ATCC 25175), determinando-se sua concentração inibitoria minima (CIM) e o efeito na formação da placa bacteriana. A CIM obtida para o óleo essencial de tomilho foi de 100 μg/mL (1 %). Procedeu-se o desenvolvimento de enxaguatório bucal com efeito antiplaca contendo o óleo essencial comercial de tomilho. As análises da formação da placa bacteriana (ensaios microbiológicos, análise macroscópica de aderência e análises por MEV) confirmaram a eficácia destas novas formulações de enxaguatórios, sem álcool, contendo óleo essencial de T. vulgaris como agentes antiplaca bacteriana com possível emprego na odontologia preventiva. A caracterização química do óleo essencial bioativo foi realizada por CG-MS, verificando-se a presença de carvacrol, p-cimeno e α-pineno como constituintes majoritários; The aim of this study was to evaluate the in vitro effect of the essential oil of Thymus vulgaris (thyme) pure or incorporate in a alcohol-free pharmaceutical mouthwash formulation, against Streptococcus mutans (ATCC 25175), being determined the Minimal Inhibitory Concentration (MIC) and the effect in the bacterial plate formation. The MIC value obtained for the essential oil was 100 μg/mL (1 %). The mouthwash pharmaceutical formulation containing commercial essential oil of T. vulgaris was preparated. Microbiological and macroscopic analysis as well as analyses for MEV confirmed the effectiveness of this new alcohol-free mouthwash formulation containing essential oil of T. vulgaris as agent with plaqueinhibiting properties and possible application in the preventive dentistry. The chemical characterization of the bioactive essential oil was accomplished by CG-MS, being verified the presence of carvacrol, p-cimene and α- pinene as major constituents. Fri, 01 Jan 2010 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8008 2010-01-01T00:00:00Z O objetivo deste estudo foi avaliar in vitro o efeito do óleo essencial de Thymus vulgaris (tomilho) puro ou incorporado em uma formulação farmacêutica de uso oral (enxaguatório bucal), frente ao Streptococcus mutans (ATCC 25175), determinando-se sua concentração inibitoria minima (CIM) e o efeito na formação da placa bacteriana. A CIM obtida para o óleo essencial de tomilho foi de 100 μg/mL (1 %). Procedeu-se o desenvolvimento de enxaguatório bucal com efeito antiplaca contendo o óleo essencial comercial de tomilho. As análises da formação da placa bacteriana (ensaios microbiológicos, análise macroscópica de aderência e análises por MEV) confirmaram a eficácia destas novas formulações de enxaguatórios, sem álcool, contendo óleo essencial de T. vulgaris como agentes antiplaca bacteriana com possível emprego na odontologia preventiva. A caracterização química do óleo essencial bioativo foi realizada por CG-MS, verificando-se a presença de carvacrol, p-cimeno e α-pineno como constituintes majoritários The aim of this study was to evaluate the in vitro effect of the essential oil of Thymus vulgaris (thyme) pure or incorporate in a alcohol-free pharmaceutical mouthwash formulation, against Streptococcus mutans (ATCC 25175), being determined the Minimal Inhibitory Concentration (MIC) and the effect in the bacterial plate formation. The MIC value obtained for the essential oil was 100 μg/mL (1 %). The mouthwash pharmaceutical formulation containing commercial essential oil of T. vulgaris was preparated. Microbiological and macroscopic analysis as well as analyses for MEV confirmed the effectiveness of this new alcohol-free mouthwash formulation containing essential oil of T. vulgaris as agent with plaqueinhibiting properties and possible application in the preventive dentistry. The chemical characterization of the bioactive essential oil was accomplished by CG-MS, being verified the presence of carvacrol, p-cimene and α- pinene as major constituents.