http://sedici.unlp.edu.ar:80/handle/10915/239 2013-05-20T14:54:54Z 2013-05-20T14:54:54Z Chahin, Cecilia L. Delfino, Mario R. Sarno, María del C. http://sedici.unlp.edu.ar:80/handle/10915/8290 2012-12-27T02:02:11Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 A spectrophotometric method was developed for the analysis of metformin, based on its reaction with the biuret reagent. A complex with λ_max = 495 nm and stoichiometry 2:1 (metformin-Cu) is generated wich allows the quantification of metformin in tablets. Physicochemical parameters of the product were determined. Sample conditioning by centrifugation was necessary to separate insoluble excipients. Polyvinylpyrrolidone (PVP) was isolated by a solid-liquid extraction with SPE-SCX resin in order to eliminate its interference on the absorbance of the complex. The proposed method was found to be highly precise, having a relative standard deviation, CV % = 0.68. Using this approach the calibration curve showed r² = 0.9949 with 95 % confidence level, value included inside the limits established by USP. Accuracy based on the average recovery of known amounts of drug in placebo was in the range of 98.61 to 99.97. Results allow the application of this analytical methodology to metformin tablets.

2011-01-01T00:00:00Z A spectrophotometric method was developed for the analysis of metformin, based on its reaction with the biuret reagent. A complex with λ_max = 495 nm and stoichiometry 2:1 (metformin-Cu) is generated wich allows the quantification of metformin in tablets. Physicochemical parameters of the product were determined. Sample conditioning by centrifugation was necessary to separate insoluble excipients. Polyvinylpyrrolidone (PVP) was isolated by a solid-liquid extraction with SPE-SCX resin in order to eliminate its interference on the absorbance of the complex. The proposed method was found to be highly precise, having a relative standard deviation, CV % = 0.68. Using this approach the calibration curve showed r² = 0.9949 with 95 % confidence level, value included inside the limits established by USP. Accuracy based on the average recovery of known amounts of drug in placebo was in the range of 98.61 to 99.97. Results allow the application of this analytical methodology to metformin tablets. Erbano, Marianna Duarte, Márcia do Rocio http://sedici.unlp.edu.ar:80/handle/10915/8289 2012-12-27T02:02:11Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 Randia armata (Sw.) DC., Rubiaceae is a shrub or small tree known as limoeiro-do-mato in Portuguese and widely distributed in Brazil. The vegetative parts are used as wound healing and anti-inflammatory in folk medicine. Due to the interest in expanding the knowledge on this species, this work has investigated the macro and microscopic characters of the leaf and stem, in order to contribute to the quality control analysis in pharmacognosy. Mature leaves and young stems were collected at the Embrapa (Colombo-PR), fixed in FAA, sectioned either by free hand or microtome, and examined in light microscopy. Microchemical tests and scanning electron microscopy were also performed. Macroscopically, the leaves are opposite, simple and obovate to elliptic-lanceolate. Microscopically, they have paracytic stomata exclusively on the abaxial side and non-glandular trichomes, either uni or multicellular and uniseriate. The mesophyll is dorsiventral and the midrib is biconvex with a collateral vascular bundle in a centric arrangement. The stem has a partially detached uniseriate epidermis, phellogen originated superficially and a complete sclerenchymatic sheath encircling the phloem cylinder. Prisms and druses of calcium oxalate are present.

2011-01-01T00:00:00Z Randia armata (Sw.) DC., Rubiaceae is a shrub or small tree known as limoeiro-do-mato in Portuguese and widely distributed in Brazil. The vegetative parts are used as wound healing and anti-inflammatory in folk medicine. Due to the interest in expanding the knowledge on this species, this work has investigated the macro and microscopic characters of the leaf and stem, in order to contribute to the quality control analysis in pharmacognosy. Mature leaves and young stems were collected at the Embrapa (Colombo-PR), fixed in FAA, sectioned either by free hand or microtome, and examined in light microscopy. Microchemical tests and scanning electron microscopy were also performed. Macroscopically, the leaves are opposite, simple and obovate to elliptic-lanceolate. Microscopically, they have paracytic stomata exclusively on the abaxial side and non-glandular trichomes, either uni or multicellular and uniseriate. The mesophyll is dorsiventral and the midrib is biconvex with a collateral vascular bundle in a centric arrangement. The stem has a partially detached uniseriate epidermis, phellogen originated superficially and a complete sclerenchymatic sheath encircling the phloem cylinder. Prisms and druses of calcium oxalate are present. Junior, Eduardo A. Duarte, Luciana F. Vanunci, Moisés L. P. Silva, Lara C. Pereira, Renata Calafatti, Silvana Junior, José P. http://sedici.unlp.edu.ar:80/handle/10915/8288 2012-12-27T02:02:11Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 The present study was performed to compare the bioavailability of two digoxin 0.25 mg tablet formulation in 30 volunteers of both sexes. The study was conducted open with randomized two period crossover design and a three-week washout period. Plasma samples were obtained over a 144 h interval. Digoxin concentrations were analyzed by a validated microparticle enzyme immunoassay with optical detection by fluorescence. Bioequivalence between the products was determined by calculating 90 % confidence intervals (90 % I.C) for the ratio of AUC_0-72h and C_max values for the test and reference products, using logarithmic transformed data. The 90 % confidence intervals were 86.98-118.33 %, and 84.52–98.76 %, respectively. Since the 90 % confidence intervals for C_max and AUC_0-72h were within the 80-125 % interval proposed by Food and Drug Administration, it was concluded that the two Digoxin formulations are bioequivalent in their rate and extent of absorption.

2011-01-01T00:00:00Z The present study was performed to compare the bioavailability of two digoxin 0.25 mg tablet formulation in 30 volunteers of both sexes. The study was conducted open with randomized two period crossover design and a three-week washout period. Plasma samples were obtained over a 144 h interval. Digoxin concentrations were analyzed by a validated microparticle enzyme immunoassay with optical detection by fluorescence. Bioequivalence between the products was determined by calculating 90 % confidence intervals (90 % I.C) for the ratio of AUC_0-72h and C_max values for the test and reference products, using logarithmic transformed data. The 90 % confidence intervals were 86.98-118.33 %, and 84.52–98.76 %, respectively. Since the 90 % confidence intervals for C_max and AUC_0-72h were within the 80-125 % interval proposed by Food and Drug Administration, it was concluded that the two Digoxin formulations are bioequivalent in their rate and extent of absorption. Perazzo, Fábio F. Souza, Gustavo H. B. Maistro, Edson L. Rodrigues, Marcelo Fonseca, Fernando L. A. Carvalho, José C. T. http://sedici.unlp.edu.ar:80/handle/10915/8287 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 This study aimed to stablish the efficacy of a multivitamin and polyminerals supplemented with Panax ginseng extract (Natus Gerin®) on patients subjected to common physical or mental stress. Patients were randomly divided in two groups and underwent a thorough clinical examination. Group A received Natus Gerin® capsules and B placebo capsules. Two capsules were taken daily during meals during four weeks. Mood and physical activity were evaluated through a questionnaire assessing quality of life. From the 176 patients enrolled, 17 were excluded due to voluntary withdrawal, 81 completed the study in group A and 78 in group B. The treatment with Natus Gerin® increased the quality of life when compared to placebo. After 15 and 30 days, group A showed a significant increase in average scoring score from 1.78 to 3.78, and finally 5.32 points. The study has shown that the daily use of Natus Gerin® can be effective in improving quality of life in patients suffering from physical and mental stress

2011-01-01T00:00:00Z This study aimed to stablish the efficacy of a multivitamin and polyminerals supplemented with Panax ginseng extract (Natus Gerin®) on patients subjected to common physical or mental stress. Patients were randomly divided in two groups and underwent a thorough clinical examination. Group A received Natus Gerin® capsules and B placebo capsules. Two capsules were taken daily during meals during four weeks. Mood and physical activity were evaluated through a questionnaire assessing quality of life. From the 176 patients enrolled, 17 were excluded due to voluntary withdrawal, 81 completed the study in group A and 78 in group B. The treatment with Natus Gerin® increased the quality of life when compared to placebo. After 15 and 30 days, group A showed a significant increase in average scoring score from 1.78 to 3.78, and finally 5.32 points. The study has shown that the daily use of Natus Gerin® can be effective in improving quality of life in patients suffering from physical and mental stress Taur, Dnyaneshwar J. Patil, Ravindra Y. http://sedici.unlp.edu.ar:80/handle/10915/8286 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 Clonidine, an α2 adrenoreceptor agonist, induces dose dependent catalepsy in mice, which releases histamine from mast cells which is responsible for different asthmatic conditions. Ricinus communis Linn (Euphorbiaceae) is a medicinal plant; root is sweetish and has been used traditionally in the treatment of inflammation, pain fever, asthma, bronchititis and leprosy. In present study ethanol extract of R. communis roots (ERCR) at doses 100, 125 and 150 mg/kg intraperitoneally was evaluated for antihistaminic activity using clonidine induced catalepsy in mice. Finding of investigation showed that chlorpheniramine maleate and ERCR inhibit clonidine induced catalepsy significantly P < 0.001 when compare to control group. Present study concludes that ERCR possesses antihistaminic activity.

2011-01-01T00:00:00Z Clonidine, an α2 adrenoreceptor agonist, induces dose dependent catalepsy in mice, which releases histamine from mast cells which is responsible for different asthmatic conditions. Ricinus communis Linn (Euphorbiaceae) is a medicinal plant; root is sweetish and has been used traditionally in the treatment of inflammation, pain fever, asthma, bronchititis and leprosy. In present study ethanol extract of R. communis roots (ERCR) at doses 100, 125 and 150 mg/kg intraperitoneally was evaluated for antihistaminic activity using clonidine induced catalepsy in mice. Finding of investigation showed that chlorpheniramine maleate and ERCR inhibit clonidine induced catalepsy significantly P < 0.001 when compare to control group. Present study concludes that ERCR possesses antihistaminic activity. Zhang, Zhidan Gao, Wenyuan Ma, Chaoyi Liu, Changxiao http://sedici.unlp.edu.ar:80/handle/10915/8285 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 Semen Persicae was a traditional Chinese medicine for the treatment of diseases such as inflammation and hyperlipemia. Amygdalin was one of the main active ingredients of this traditional Chinese medicine. In this paper, pharmacokinetic study was conducted to obtain pharmacokinetic parameters of amygadalin after oral administration of Semen Persicae extraction in rat plasma. HPLC-UV was used to determine the concentration of amygdalin in rat plasma at different time points after administration. The main pharmacokinetic parameters of amygdalin in rat were obtained based on the analysis of the plasma sample. The pharmacokinetics of amygdalin was fitted with a one-compartment model and it eliminated relative slowly in rats.

2011-01-01T00:00:00Z Semen Persicae was a traditional Chinese medicine for the treatment of diseases such as inflammation and hyperlipemia. Amygdalin was one of the main active ingredients of this traditional Chinese medicine. In this paper, pharmacokinetic study was conducted to obtain pharmacokinetic parameters of amygadalin after oral administration of Semen Persicae extraction in rat plasma. HPLC-UV was used to determine the concentration of amygdalin in rat plasma at different time points after administration. The main pharmacokinetic parameters of amygdalin in rat were obtained based on the analysis of the plasma sample. The pharmacokinetics of amygdalin was fitted with a one-compartment model and it eliminated relative slowly in rats. Silva, Fabiana E. B. da Ziech, Cristiane Dias, Yara P. Moreira, Eduardo C. Flores, Érico M. M. Ferrão, Marco F. http://sedici.unlp.edu.ar:80/handle/10915/8284 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 Raman spectroscopy in combination with partial least-squares (PLS) regression method was developed for sulphamethoxazole (SMZ) and trimethoprim (TMP) simultaneous determination in powder mixtures. The calibration set was designed with 18 samples and validation set with 9 samples, containing different SMZ and TMP concentrations. The concentration ranges were 400-900 mg/g for SMZ and 80- 240 mg/g for TMP. The proposed procedure was validated by comparison with the official method (HPLC). Mean root square error of calibration (RMSEC) and mean root square error of prediction (RMSEP) were calculated. RMSEC found was 30.96 mg/g to SMZ and 14.36 mg/g to TMP, respectively. RMSEP found was 25.60 mg/g to SMZ and 14.36 mg/g to TMP, respectively. Correlation coefficient (R2) was 0.99 for SMZ and 0.99 for TMP. This parameter evidences a very good agreement between estimated and real values. The results showed that PLS regression model combined with Raman spectroscopy provides a sensitive, fast and simple method for the quantitative analysis of SMZ and TMP mixtures in powder quality control.

2011-01-01T00:00:00Z Raman spectroscopy in combination with partial least-squares (PLS) regression method was developed for sulphamethoxazole (SMZ) and trimethoprim (TMP) simultaneous determination in powder mixtures. The calibration set was designed with 18 samples and validation set with 9 samples, containing different SMZ and TMP concentrations. The concentration ranges were 400-900 mg/g for SMZ and 80- 240 mg/g for TMP. The proposed procedure was validated by comparison with the official method (HPLC). Mean root square error of calibration (RMSEC) and mean root square error of prediction (RMSEP) were calculated. RMSEC found was 30.96 mg/g to SMZ and 14.36 mg/g to TMP, respectively. RMSEP found was 25.60 mg/g to SMZ and 14.36 mg/g to TMP, respectively. Correlation coefficient (R2) was 0.99 for SMZ and 0.99 for TMP. This parameter evidences a very good agreement between estimated and real values. The results showed that PLS regression model combined with Raman spectroscopy provides a sensitive, fast and simple method for the quantitative analysis of SMZ and TMP mixtures in powder quality control. Marques, Lucas M. M. Medeiros, Maria G. F. de Nunes, Lívio C. C. Citó, Antônia M.G.L. Lopes, José A. D. Souza, Alexandre A. Souza, Claide M. L. http://sedici.unlp.edu.ar:80/handle/10915/8283 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) were used to investigate drug-excipient interactions and, in consequence, their compatibility. For this purpose, binary mixtures of olanzapine drug substance and the excipients croscarmellose sodium, magnesium stearate and microcrystalline cellulose, were prepared and analysed. By the analysis of the binary mixtures DSC and TG curves it were observed changes on the temperature and enthalpy values of the drug melting and decomposition peak, with the likely formation of intermediate substances.

2011-01-01T00:00:00Z Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) were used to investigate drug-excipient interactions and, in consequence, their compatibility. For this purpose, binary mixtures of olanzapine drug substance and the excipients croscarmellose sodium, magnesium stearate and microcrystalline cellulose, were prepared and analysed. By the analysis of the binary mixtures DSC and TG curves it were observed changes on the temperature and enthalpy values of the drug melting and decomposition peak, with the likely formation of intermediate substances. D'Souza, Marina G. Bheemappa, Eswarappa Pai, Vasantakumar K. Byahatti, Vivek V. Tule, Chandramouli http://sedici.unlp.edu.ar:80/handle/10915/8282 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 6 The present study has been undertaken to screen the anthelmintic potential of aqueous root extracts of Aristolochia indica Linn. and A. tagala Cham. against adult Indian earthworm Pheritima posthuma and round worms Ascaridia galli. Different concentrations of the extracts ranging from 2-8 mg/mL were screened. Piperazine citrate was used as reference standard. Extract of A. tagala was found to be more potent and effective at the dose level of 2 mg/mL compared to the extract of A. indica. Extracts showed dose dependant activity. The study reports that the plants A. indica and A. tagala roots possess potent anthelmintic properties.

2011-01-01T00:00:00Z The present study has been undertaken to screen the anthelmintic potential of aqueous root extracts of Aristolochia indica Linn. and A. tagala Cham. against adult Indian earthworm Pheritima posthuma and round worms Ascaridia galli. Different concentrations of the extracts ranging from 2-8 mg/mL were screened. Piperazine citrate was used as reference standard. Extract of A. tagala was found to be more potent and effective at the dose level of 2 mg/mL compared to the extract of A. indica. Extracts showed dose dependant activity. The study reports that the plants A. indica and A. tagala roots possess potent anthelmintic properties. Barboza, Fernanda M. Stulzer, Hellen Karine http://sedici.unlp.edu.ar:80/handle/10915/8281 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 Hydrophilic matrix tablets were developed with carvedilol (CRV), using different molecular weights of polyethylene oxide (PEO). Investigations were carried out in order to verify the tablets performance. All formulations satisfied the official requirements. Water uptake studies were influenced by pH value and polymer concentration. CRV release was sustained for 23 and 19 h, in acid and neutral conditions, respectively. The mechanism involved in drug release was characterized by anomalous behavior for all formulations in phosphate buffer whereas in acid conditions they presented a Fickian kinetics, Case II transport and Super Case II transport kinetics for different formulations.

2011-01-01T00:00:00Z Hydrophilic matrix tablets were developed with carvedilol (CRV), using different molecular weights of polyethylene oxide (PEO). Investigations were carried out in order to verify the tablets performance. All formulations satisfied the official requirements. Water uptake studies were influenced by pH value and polymer concentration. CRV release was sustained for 23 and 19 h, in acid and neutral conditions, respectively. The mechanism involved in drug release was characterized by anomalous behavior for all formulations in phosphate buffer whereas in acid conditions they presented a Fickian kinetics, Case II transport and Super Case II transport kinetics for different formulations. Francescato, Leandro N. Quinteros, Dayane A. Bordignon, Sérgio Bassani, Valquiria L. Henriques, Amélia T. http://sedici.unlp.edu.ar:80/handle/10915/8280 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 This work presents physicochemical and chemical characterization of Equisetum giganteum L. stems, an endemic species of Latin America widely used in the traditional medicine, mainly as diuretic. The loss on drying, total ash and acid-insoluble ash values were 11.85 ± 0.11 %, ≥13.61 ± 0.38 %, and ≥ 9.43 ± 0.35 %, respectively. The total phenolic and flavonoid content were 7.27 ± 0.05 mg GAE/g and 0.42 ± 0.0141 g %, respectively. Data on drying, adsorption and sorption isotherms and other physicochemical determinations are also presented. Thin layer and liquid chromatography profiles revealed the presence of polyphenols. These results will provide important information for future studies involving the standardization and quality control of E. giganteum raw material and products.

2011-01-01T00:00:00Z This work presents physicochemical and chemical characterization of Equisetum giganteum L. stems, an endemic species of Latin America widely used in the traditional medicine, mainly as diuretic. The loss on drying, total ash and acid-insoluble ash values were 11.85 ± 0.11 %, ≥13.61 ± 0.38 %, and ≥ 9.43 ± 0.35 %, respectively. The total phenolic and flavonoid content were 7.27 ± 0.05 mg GAE/g and 0.42 ± 0.0141 g %, respectively. Data on drying, adsorption and sorption isotherms and other physicochemical determinations are also presented. Thin layer and liquid chromatography profiles revealed the presence of polyphenols. These results will provide important information for future studies involving the standardization and quality control of E. giganteum raw material and products. Dixit, Raghav Verma, Anurag Soni, Shashank Mishra, Arun K. Bansal, Ashok K. Pandit, Jayant K. http://sedici.unlp.edu.ar:80/handle/10915/8279 2012-12-27T02:02:12Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 The purpose of the present investigation was to prepare gellan-chitosan polyelectrolyte complex beads in one step and to explore the potential of the prepared beads in the oral delivery of metronidazole (log P = 0.0) and metronidazole benzoate (log P = 2.19). Beads were prepared by extruding aqueous solution of gellan gum (with or without drugs) into chitosan solution in acetic acid pH adjusted to 3.5. Prepared beads exhibited poor encapsulation and burst release for metronidazole, while very high encapsulation and extended release was observed for metronidazole benzoate in simulated gastric fluid (SGF, pH 1.2). Incorporation of type A & B gelatin significantly improved the metronidazole encapsulation in the beads but the release pattern remained the same. Overall, gellan-chitosan beads showed poor retardant capacity of drug release for metronidazole whereas good retardant capacity was observed for metronidazole benzoate.

2011-01-01T00:00:00Z The purpose of the present investigation was to prepare gellan-chitosan polyelectrolyte complex beads in one step and to explore the potential of the prepared beads in the oral delivery of metronidazole (log P = 0.0) and metronidazole benzoate (log P = 2.19). Beads were prepared by extruding aqueous solution of gellan gum (with or without drugs) into chitosan solution in acetic acid pH adjusted to 3.5. Prepared beads exhibited poor encapsulation and burst release for metronidazole, while very high encapsulation and extended release was observed for metronidazole benzoate in simulated gastric fluid (SGF, pH 1.2). Incorporation of type A & B gelatin significantly improved the metronidazole encapsulation in the beads but the release pattern remained the same. Overall, gellan-chitosan beads showed poor retardant capacity of drug release for metronidazole whereas good retardant capacity was observed for metronidazole benzoate. Petkar, Kailash C. Pore, Yogesh V. Kuchekar, Bhanudas S. http://sedici.unlp.edu.ar:80/handle/10915/8278 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 Formulation and in vitro evaluation of losartan potassium (LP) loaded transdermal delivery system (TDS) was investigated for controlled release and improved therapeutic efficacy. TDS (patches) were prepared by varying the composition of Eudragit RL 100 and Eudragit RS 100 (5:0, 4:1, 3:2, 2.5:2.5, 2:3, 1:4 and 0:5). Patches were evaluated for thickness, content uniformity, mechanical properties, moisture uptake and in vitro drug release. Technological parameters for all the formulations were found to be within the limit. In vitro studies showed relatively high permeation of LP (F1- 42.17 ± 1.13 %) from the formulation comprising 4:1 ratio of polymer. Inclusion of capsaicin (55.70 ± 1.55 %) and pluronic F-68 (70.88 ± 1.20 %) to formulation F1 resulted increased permeation of LP across human skin. In conclusion, this study demonstrated the potential of simple transdermal adhesive patch incorporating LP to deliver therapeutically useful dose in-vivo for the treatment of hypertension.

2011-01-01T00:00:00Z Formulation and in vitro evaluation of losartan potassium (LP) loaded transdermal delivery system (TDS) was investigated for controlled release and improved therapeutic efficacy. TDS (patches) were prepared by varying the composition of Eudragit RL 100 and Eudragit RS 100 (5:0, 4:1, 3:2, 2.5:2.5, 2:3, 1:4 and 0:5). Patches were evaluated for thickness, content uniformity, mechanical properties, moisture uptake and in vitro drug release. Technological parameters for all the formulations were found to be within the limit. In vitro studies showed relatively high permeation of LP (F1- 42.17 ± 1.13 %) from the formulation comprising 4:1 ratio of polymer. Inclusion of capsaicin (55.70 ± 1.55 %) and pluronic F-68 (70.88 ± 1.20 %) to formulation F1 resulted increased permeation of LP across human skin. In conclusion, this study demonstrated the potential of simple transdermal adhesive patch incorporating LP to deliver therapeutically useful dose in-vivo for the treatment of hypertension. Echarri Martínez, Lara Rodríguez González, Carmen G. Castillo Romera, Isabel Trovato López, Nicolás Ais Larisgoitia, Arantza Bellón Cano, José M. Sanjurjo Sáez, María http://sedici.unlp.edu.ar:80/handle/10915/8277 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 The aim of this study was to analyze the evolution of adherence to highly active antiretroviral therapy (HAART) in the Hospital General Universitario Gregorio Marañón (Madrid, Spain) over the last 8 years and determine the variables associated with the complexity of treatment and suboptimal adherence. An observational, retrospective method was used to measure adherence during the first 6 months of HAART in 3 cohorts: 2001 cohort (n = 90), 2005 cohort (n = 98), and 2008 cohort (n = 110). The adherence rate was determined using 2 methods: Pharmacy Department dispensation records and virologic response data. The evolution of the complexity of treatment and its influence on the adherence rate was analyzed by logistic regression. Adherence to HAART increased progressively from 45.6 % in 2001 to 56.1 % in 2005 and 77.3 % in 2008. Statistically significant differences were only observed between cohorts in 2005 and 2008. The average daily pill burden was 7, 4, and 4.5 tablets, respectively. The percentage of patients on twice-daily regimens decreased from 93.3 % in 2001 to 63.6 % in 2008, with a parallel increase in once-daily regimens. The proportion of patients with dietary restrictions decreased from 24.4 % to 3.6 %. A statistically significant association was found between the number of medication units per day and adherence and between frequency of administration and adherence. Adherence to HAART has improved significantly in the last 8 years. While the complexity of the treatment was significantly reduced in 2005, the largest increase in adherence occurred in the last cohort, which shows the influence of factors other than treatment simplification.

2011-01-01T00:00:00Z The aim of this study was to analyze the evolution of adherence to highly active antiretroviral therapy (HAART) in the Hospital General Universitario Gregorio Marañón (Madrid, Spain) over the last 8 years and determine the variables associated with the complexity of treatment and suboptimal adherence. An observational, retrospective method was used to measure adherence during the first 6 months of HAART in 3 cohorts: 2001 cohort (n = 90), 2005 cohort (n = 98), and 2008 cohort (n = 110). The adherence rate was determined using 2 methods: Pharmacy Department dispensation records and virologic response data. The evolution of the complexity of treatment and its influence on the adherence rate was analyzed by logistic regression. Adherence to HAART increased progressively from 45.6 % in 2001 to 56.1 % in 2005 and 77.3 % in 2008. Statistically significant differences were only observed between cohorts in 2005 and 2008. The average daily pill burden was 7, 4, and 4.5 tablets, respectively. The percentage of patients on twice-daily regimens decreased from 93.3 % in 2001 to 63.6 % in 2008, with a parallel increase in once-daily regimens. The proportion of patients with dietary restrictions decreased from 24.4 % to 3.6 %. A statistically significant association was found between the number of medication units per day and adherence and between frequency of administration and adherence. Adherence to HAART has improved significantly in the last 8 years. While the complexity of the treatment was significantly reduced in 2005, the largest increase in adherence occurred in the last cohort, which shows the influence of factors other than treatment simplification. Pan, Jian Wu, Zeyu Yuan, Yuan Hui, Ailing Yang, Yi http://sedici.unlp.edu.ar:80/handle/10915/8276 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 A simple and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method was established and validated for the determination of prodrug of ginkgolide B (PGB) and its metabolite, ginkgolide B (GB) in rat plasma. The separation was achieved on a Waters Symmetry Shield RP18 column (150 mm × 3.9 mm i.d., 5 μm particle size), using a mobile phase composed of methanol/water with 10 mM ammonium acetate (85:15, v/v) at a flow rate of 800 μL/min in 2 min. An API 3200 triple quadrupole mass spectrometer equipped with electrospray ionization source was operated in negative ionization mode. Multiple reaction monitoring (MRM) was performed to quantify PGB, GB and the internal standard (IS) at m/z transitions of 528.1 → 122.0, 423.4 → 367.3, 407.5 → 351.2, respectively. A good linearity was found. Intra- and inter-day precision, accuracy, extraction recovery, matrix effect and stability were validated to be within an acceptable range. The developed method was successfully applied to a pharmacokinetic study after intravenous administration of a 10 mg/kg dose of PGB to rats.

2011-01-01T00:00:00Z A simple and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method was established and validated for the determination of prodrug of ginkgolide B (PGB) and its metabolite, ginkgolide B (GB) in rat plasma. The separation was achieved on a Waters Symmetry Shield RP18 column (150 mm × 3.9 mm i.d., 5 μm particle size), using a mobile phase composed of methanol/water with 10 mM ammonium acetate (85:15, v/v) at a flow rate of 800 μL/min in 2 min. An API 3200 triple quadrupole mass spectrometer equipped with electrospray ionization source was operated in negative ionization mode. Multiple reaction monitoring (MRM) was performed to quantify PGB, GB and the internal standard (IS) at m/z transitions of 528.1 → 122.0, 423.4 → 367.3, 407.5 → 351.2, respectively. A good linearity was found. Intra- and inter-day precision, accuracy, extraction recovery, matrix effect and stability were validated to be within an acceptable range. The developed method was successfully applied to a pharmacokinetic study after intravenous administration of a 10 mg/kg dose of PGB to rats. Ribeiro, Paulo R. S.. Pezza, Leonardo Pezza, Helena Tognolli, João O. http://sedici.unlp.edu.ar:80/handle/10915/8275 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 A new spectrophotometric method was developed for the determination of captopril (n donor) through charge transfer complex formation with p-chloranil (π acceptor). The different experimental parameters that affect the absorbance intensity were carefully studied. Thus, these parameters were optimized using chemometric methods of fractional factorial and central composite design. At the optimum reaction conditions, the rectilinear calibration graphs were obtained in the concentration range 1.86 x 10^-4 to 7.38 x 10^-4 mol/L captopril with an excellent correlation coefficient (r = 0.9996). The proposed procedure could be applied successfully for the determination of the investigated drug in their pharmaceutical dosage forms with a good precision and accuracy compared to official and reported method as revealed by F- and t-tests at 95 % confidence level. No interference was observed from common excipients in formulations.

2011-01-01T00:00:00Z A new spectrophotometric method was developed for the determination of captopril (n donor) through charge transfer complex formation with p-chloranil (π acceptor). The different experimental parameters that affect the absorbance intensity were carefully studied. Thus, these parameters were optimized using chemometric methods of fractional factorial and central composite design. At the optimum reaction conditions, the rectilinear calibration graphs were obtained in the concentration range 1.86 x 10^-4 to 7.38 x 10^-4 mol/L captopril with an excellent correlation coefficient (r = 0.9996). The proposed procedure could be applied successfully for the determination of the investigated drug in their pharmaceutical dosage forms with a good precision and accuracy compared to official and reported method as revealed by F- and t-tests at 95 % confidence level. No interference was observed from common excipients in formulations. Jiang, Xianglan Wu, Jing Tang, Daoquan Gao, Yuanyuan Yang, Dongzhi Zhao, Ziming Chen, Hui http://sedici.unlp.edu.ar:80/handle/10915/8274 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 Gastric ulcer is one of ulcerous diseases and may result in some changes of many enzymes and transporters concerned with metabolism and disposal of drug. The pharmacokinetic of drug should be different between peptic ulcer and normal animals. Lansoprazole has been one of important medicine for treatment of ulcerous diseases. So, this paper investigated the difference of pharmacokinetic profiles of lansoprazole in gastric ulcer and normal rabbits in vivo by HPLC-DAD method. In this work, a liquid-liquid extraction and enrichment method with RP-HPLC determination route was taken. The pharmacokinetic parameters were analyzed by double-compartmental method (DAS2.0). The pharmacokinetic parameters of lansoprazole in normal and ulcer rabbits were as follows: (614.42 ± 152.25) and (875.73 ± 316.34) mg h/L for AUC(_0-6.5); (0.68 ± 0.12) and (0.83 ± 0.22) h for MRT(_0-6.5), (0.52 ± 0.23) and (0.87 ± 0.42) h for t_1/2 ; (6.13 ± 2.11) and (2.54 ± 1.65) L/h/kg for CL, respectively; Gastric ulcer is one of ulcerous diseases and may result in some changes of many enzymes and transporters concerned with metabolism and disposal of drug. The pharmacokinetic of drug should be different between peptic ulcer and normal animals. Lansoprazole has been one of important medicine for treatment of ulcerous diseases. So, this paper investigated the difference of pharmacokinetic profiles of lansoprazole in gastric ulcer and normal rabbits in vivo by HPLC-DAD method. In this work, a liquid-liquid extraction and enrichment method with RP-HPLC determination route was taken. The pharmacokinetic parameters were analyzed by double-compartmental method (DAS2.0). The pharmacokinetic parameters of lansoprazole in normal and ulcer rabbits were as follows: (614.42 ± 152.25) and (875.73 ± 316.34) mg h/L for AUC(_0-6.5); (0.68 ± 0.12) and (0.83 ± 0.22) h for MRT(_0-6.5 , (0.52 ± 0.23) and (0.87 ± 0.42) h for t_1/2 ; (6.13 ± 2.11) and (2.54 ± 1.65) L/h/kg for CL, respectively

2011-01-01T00:00:00Z Gastric ulcer is one of ulcerous diseases and may result in some changes of many enzymes and transporters concerned with metabolism and disposal of drug. The pharmacokinetic of drug should be different between peptic ulcer and normal animals. Lansoprazole has been one of important medicine for treatment of ulcerous diseases. So, this paper investigated the difference of pharmacokinetic profiles of lansoprazole in gastric ulcer and normal rabbits in vivo by HPLC-DAD method. In this work, a liquid-liquid extraction and enrichment method with RP-HPLC determination route was taken. The pharmacokinetic parameters were analyzed by double-compartmental method (DAS2.0). The pharmacokinetic parameters of lansoprazole in normal and ulcer rabbits were as follows: (614.42 ± 152.25) and (875.73 ± 316.34) mg h/L for AUC(_0-6.5); (0.68 ± 0.12) and (0.83 ± 0.22) h for MRT(_0-6.5), (0.52 ± 0.23) and (0.87 ± 0.42) h for t_1/2 ; (6.13 ± 2.11) and (2.54 ± 1.65) L/h/kg for CL, respectively Gastric ulcer is one of ulcerous diseases and may result in some changes of many enzymes and transporters concerned with metabolism and disposal of drug. The pharmacokinetic of drug should be different between peptic ulcer and normal animals. Lansoprazole has been one of important medicine for treatment of ulcerous diseases. So, this paper investigated the difference of pharmacokinetic profiles of lansoprazole in gastric ulcer and normal rabbits in vivo by HPLC-DAD method. In this work, a liquid-liquid extraction and enrichment method with RP-HPLC determination route was taken. The pharmacokinetic parameters were analyzed by double-compartmental method (DAS2.0). The pharmacokinetic parameters of lansoprazole in normal and ulcer rabbits were as follows: (614.42 ± 152.25) and (875.73 ± 316.34) mg h/L for AUC(_0-6.5); (0.68 ± 0.12) and (0.83 ± 0.22) h for MRT(_0-6.5 , (0.52 ± 0.23) and (0.87 ± 0.42) h for t_1/2 ; (6.13 ± 2.11) and (2.54 ± 1.65) L/h/kg for CL, respectively Narendra, Chikkanna Srinath, Mayasandra S. http://sedici.unlp.edu.ar:80/handle/10915/8273 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 The objective of the present study was to develop an oral timed-released press-coated tablet containing theophylline as a model drug. A D-optimal design of experiment was employed to systematically study the effect of ternary blend of ethylcellulose (X₁), hydroxypropylcellulose (X₂), and Mg stearate (X₃) as independent variables. The design was quantitatively evaluated by quadratic model and the results from the statistical analysis revealed that interaction factors X₁X₂ and X₂X₃ were found to be highly significant on the studied response variables; percent drug release at 8 h (Y₁), percent drug release at 10 h (Y₂) and lag time (Y₃). A numerical optimization technique by desirability function was used to optimize the response variables each having a different target and the observed responses were highly agreed with experimental values. The dissolution profiles of the optimal formulation before and after stability studies were evaluated by using similarity factor (ƒ2 ) and were found to be similar. The results of in vivo studies showed an increased T_max and MRT values with high statistical significant difference between optimal press-coated and core tablets. The time point at which the drug first appeared in the plasma for the optimal press-coated tablet was found to be longer than that of core tablet, indicating a time controlled release profile. Moreover, a good linear relationship was observed between the fraction dissolved and fraction absorbed.

2011-01-01T00:00:00Z The objective of the present study was to develop an oral timed-released press-coated tablet containing theophylline as a model drug. A D-optimal design of experiment was employed to systematically study the effect of ternary blend of ethylcellulose (X₁), hydroxypropylcellulose (X₂), and Mg stearate (X₃) as independent variables. The design was quantitatively evaluated by quadratic model and the results from the statistical analysis revealed that interaction factors X₁X₂ and X₂X₃ were found to be highly significant on the studied response variables; percent drug release at 8 h (Y₁), percent drug release at 10 h (Y₂) and lag time (Y₃). A numerical optimization technique by desirability function was used to optimize the response variables each having a different target and the observed responses were highly agreed with experimental values. The dissolution profiles of the optimal formulation before and after stability studies were evaluated by using similarity factor (ƒ2 ) and were found to be similar. The results of in vivo studies showed an increased T_max and MRT values with high statistical significant difference between optimal press-coated and core tablets. The time point at which the drug first appeared in the plasma for the optimal press-coated tablet was found to be longer than that of core tablet, indicating a time controlled release profile. Moreover, a good linear relationship was observed between the fraction dissolved and fraction absorbed. Vemula, Sateesh K. Veerareddy, Prabhakar Reddy http://sedici.unlp.edu.ar:80/handle/10915/8272 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 The purpose of development oral fast disintegrating drug delivery is not only to give fast relief but also to overcome difficulty in swallowing tablets and capsules, resulting in non-compliance and ineffective therapy. The aim of present study is to formulate fast disintegrating of flurbiprofen by using superdisintegrants. Flurbiprofen fast disintegrating tablets were prepared by using direct compression method and were characterized for both pre-compression parameters and post-compression parameters to comply with pharmacopoeial limits. From the in vitro drug release studies the optimized formulation showed almost complete drug release (above 99 %) within 15 min. DSC and FTIR studies were carried out to understand the drug-polymer compatibility and revealed that there was no possible interaction between them. Thus developed fast disintegrating tablets may be suitable to give rapid drug delivery and rapid onset of action.

2011-01-01T00:00:00Z The purpose of development oral fast disintegrating drug delivery is not only to give fast relief but also to overcome difficulty in swallowing tablets and capsules, resulting in non-compliance and ineffective therapy. The aim of present study is to formulate fast disintegrating of flurbiprofen by using superdisintegrants. Flurbiprofen fast disintegrating tablets were prepared by using direct compression method and were characterized for both pre-compression parameters and post-compression parameters to comply with pharmacopoeial limits. From the in vitro drug release studies the optimized formulation showed almost complete drug release (above 99 %) within 15 min. DSC and FTIR studies were carried out to understand the drug-polymer compatibility and revealed that there was no possible interaction between them. Thus developed fast disintegrating tablets may be suitable to give rapid drug delivery and rapid onset of action. Ul Islam, S.M. Bakhtiar Hossain, Khalid Gomes, Isidore Gomes, Donald J. Rahman, Sabita Rezwana Rahman, Mohammad S. Rashid, Mohammad A. http://sedici.unlp.edu.ar:80/handle/10915/8271 2012-12-27T02:02:13Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 6 Bixa orellana Linn., commonly known as "lipstick plant", is used in folk medicines to treat infections of microbial origin as well as coloring agents in food stuffs in the LDCs like Bangladesh. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the warm water extract of leaves of B. orellana were evaluated against 25 multidrug resistant (MDR) clinical isolates and 6 food-borne pathogens using the micro-dilution broth method modified to comply with the NCCLS standards. The total phenolic content and antioxidant capacity of warm water, ethanol, and methanol extracts of the seeds and leaves of B. orellana were also evaluated. The brine shrimp lethality assay was conducted to assess the toxicity of the extracts. Except Pseudomonas spp., all the MDR isolates and food-borne pathogens tested were susceptible to the warm water extract of the leaves. The MIC and MBC ranged between 8-256 μg/mL and 16 - 256 μg/mL, respectively. Among the test organisms, Streptococcus spp. and Shigella dysenteriae-1 MJ-84 showed highest susceptibility while Escherichia coli exhibited moderate susceptibility to warm water extract of the leaves. The highest total phenolic content (99.99 mg of GAE/g of extractives) and antioxidant capacity (IC₅₀ value 13 μg/mL) were observed in ethanolic extract of seeds of B. orellana, whereas the IC₅₀ of the reference standard BHT (tert-butyl-1-hydroxytoluene) was 59.2 μg/mL. On the other hand, in the brine shrimp lethality bioassay the methanolic extract of the seeds of B. orellana demonstrated strong cytotoxic activity with IC₅₀ value of 19.3 μg/mL. These results suggest that the extracts of B. orellana possess bioactive compounds

2011-01-01T00:00:00Z Bixa orellana Linn., commonly known as "lipstick plant", is used in folk medicines to treat infections of microbial origin as well as coloring agents in food stuffs in the LDCs like Bangladesh. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the warm water extract of leaves of B. orellana were evaluated against 25 multidrug resistant (MDR) clinical isolates and 6 food-borne pathogens using the micro-dilution broth method modified to comply with the NCCLS standards. The total phenolic content and antioxidant capacity of warm water, ethanol, and methanol extracts of the seeds and leaves of B. orellana were also evaluated. The brine shrimp lethality assay was conducted to assess the toxicity of the extracts. Except Pseudomonas spp., all the MDR isolates and food-borne pathogens tested were susceptible to the warm water extract of the leaves. The MIC and MBC ranged between 8-256 μg/mL and 16 - 256 μg/mL, respectively. Among the test organisms, Streptococcus spp. and Shigella dysenteriae-1 MJ-84 showed highest susceptibility while Escherichia coli exhibited moderate susceptibility to warm water extract of the leaves. The highest total phenolic content (99.99 mg of GAE/g of extractives) and antioxidant capacity (IC₅₀ value 13 μg/mL) were observed in ethanolic extract of seeds of B. orellana, whereas the IC₅₀ of the reference standard BHT (tert-butyl-1-hydroxytoluene) was 59.2 μg/mL. On the other hand, in the brine shrimp lethality bioassay the methanolic extract of the seeds of B. orellana demonstrated strong cytotoxic activity with IC₅₀ value of 19.3 μg/mL. These results suggest that the extracts of B. orellana possess bioactive compounds