http://sedici.unlp.edu.ar:80/handle/10915/243 2013-05-24T22:38:06Z 2013-05-24T22:38:06Z Lin, Guanyang Chen, Xiaole Zheng, Meiqin Wang, Youpei Pang, Lingxia Wang, Qing http://sedici.unlp.edu.ar:80/handle/10915/8420 2012-12-28T02:01:55Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 10 A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of ramosetron in rat plasma using one-step protein precipitation was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm × 150 mm, 5 μm) column with acetonitrile-0.1 % formic acid as the mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantification using target fragment ions m/z 280 for ramosetron and m/z 326 for the IS. Calibration plots were linear over the range of 10-1000 ng/mL for ramosetron in rat plasma. Lower limit of quantification (LLOQ) for Ramosetron was 10 ng/mL. Mean recovery of ramosetron from plasma was in the range of 88.5-92.8 %. CV of intra-day and inter-day precision were both less than 15 %. This method is simple and sensitive enough to be used in pharmacokinetic study for determination of ramosetron in rat plasma.

2011-01-01T00:00:00Z A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of ramosetron in rat plasma using one-step protein precipitation was developed and validated. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm × 150 mm, 5 μm) column with acetonitrile-0.1 % formic acid as the mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantification using target fragment ions m/z 280 for ramosetron and m/z 326 for the IS. Calibration plots were linear over the range of 10-1000 ng/mL for ramosetron in rat plasma. Lower limit of quantification (LLOQ) for Ramosetron was 10 ng/mL. Mean recovery of ramosetron from plasma was in the range of 88.5-92.8 %. CV of intra-day and inter-day precision were both less than 15 %. This method is simple and sensitive enough to be used in pharmacokinetic study for determination of ramosetron in rat plasma. Menarim, Daniele O. Matzenbacher, Nelson I. Budel, Jane M. Duarte, Márcia do Rocio http://sedici.unlp.edu.ar:80/handle/10915/8419 2012-12-28T02:01:55Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 10 Lucilia nitens is a herb used in folk medicine for treating diarrhoea and popularly called in Brazil "erva-pombinha". Aiming to expand the knowledge on this medicinal plant, this work has dealt with anatomical analysis of the leaf and stem for microscopic diagnosis. Standard procedures of light and scanning electron microscopy were carried out. The leaf is amphistomatous and has abundant non-glandular trichomes and few glandular ones. The mesophyll is isobilateral and the midrib, in transection, is planoconvex. It is traversed by a collateral vascular bundle presenting sclerenchymatic caps. The stem has onelayered epidermis, lacunar collenchyma and parenchymatic pith. Among the sieve elements and parenchymatic cells, there are strips of fibres in the phloem. The xylem is wholly lignified and the tracheary elements are aligned in rows. These combined characters, with emphasis on the peculiar type of the non-glandular trichomes, are useful for anatomical diagnosis of the species for pharmacognostical purposes.

2011-01-01T00:00:00Z Lucilia nitens is a herb used in folk medicine for treating diarrhoea and popularly called in Brazil "erva-pombinha". Aiming to expand the knowledge on this medicinal plant, this work has dealt with anatomical analysis of the leaf and stem for microscopic diagnosis. Standard procedures of light and scanning electron microscopy were carried out. The leaf is amphistomatous and has abundant non-glandular trichomes and few glandular ones. The mesophyll is isobilateral and the midrib, in transection, is planoconvex. It is traversed by a collateral vascular bundle presenting sclerenchymatic caps. The stem has onelayered epidermis, lacunar collenchyma and parenchymatic pith. Among the sieve elements and parenchymatic cells, there are strips of fibres in the phloem. The xylem is wholly lignified and the tracheary elements are aligned in rows. These combined characters, with emphasis on the peculiar type of the non-glandular trichomes, are useful for anatomical diagnosis of the species for pharmacognostical purposes. Hu, Lufeng Chen, Xiaole Ma, Jianshe Wang, Xianqin Sun, Wei Dong, Wei Yang, Fangfang Ding, Chen http://sedici.unlp.edu.ar:80/handle/10915/8418 2012-12-28T02:01:55Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 10 A sensitive and selective liquid chromatography-mass spectrometry (LC-MS) method for determination of ibudilast in rabbit plasma was developed and validated. After addition of estazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 mm x 50 mm, 3.5 μm) using 0.1 % formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragment ions m/z 230.7 for ibudilast and m/z 294.7 for estazolam (internal standard, IS). The assay was linear over the range of 20-2000 ng/mL for ibudilast, with a lower limit of quantitation (LLOQ) of 20 ng/mL for ibudilast. Intra- and inter-day precisions were less than 15 % and the accuracies were in the range of 90.78 %- 105.60 % for ibudilast. This developed method was successfully applied for the determination of ibudilast in rabbit plasma for pharmacokinetic study

2011-01-01T00:00:00Z A sensitive and selective liquid chromatography-mass spectrometry (LC-MS) method for determination of ibudilast in rabbit plasma was developed and validated. After addition of estazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation, and chromatography involved Agilent SB-C18 column (2.1 mm x 50 mm, 3.5 μm) using 0.1 % formic acid in water and acetonitrile as a mobile phase with gradient elution. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragment ions m/z 230.7 for ibudilast and m/z 294.7 for estazolam (internal standard, IS). The assay was linear over the range of 20-2000 ng/mL for ibudilast, with a lower limit of quantitation (LLOQ) of 20 ng/mL for ibudilast. Intra- and inter-day precisions were less than 15 % and the accuracies were in the range of 90.78 %- 105.60 % for ibudilast. This developed method was successfully applied for the determination of ibudilast in rabbit plasma for pharmacokinetic study Barberato Fihlo, Silvio Lopes, Luciane C. Zabotto, Cláudia B. Gerenutti, Marli Del Fiol, Fernando S. http://sedici.unlp.edu.ar:80/handle/10915/8417 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 10 The prescription of antibiotics worldwide remains large, especially in children. The lack of accurate diagnoses leads to overuse of these drugs, increasing bacterial resistance. A large number of studies have shown that another important factor in the onset of upper respiratory infections (URI) is inadequate intake of nutrients for these children, especially vitamins A, C and D. This study aimed to understand the use of antibiotics and the profile of nutrient intake in children diagnosed with URI. During 12 months, a survey (24 h dietary recall) was applied in 131 parents of children using antibiotics. The results showed antibiotic prescriptions for viral infections (37 %), pointing out incorrect prescriptions. The presence of URI was directly related to the lack of intake of vitamins, especially A and D. Countries with poor sources of these vitamins (fish oil), in regular diet, should increase the dietary supplementation of vitamins to diminish the appearance of URIs.

2011-01-01T00:00:00Z The prescription of antibiotics worldwide remains large, especially in children. The lack of accurate diagnoses leads to overuse of these drugs, increasing bacterial resistance. A large number of studies have shown that another important factor in the onset of upper respiratory infections (URI) is inadequate intake of nutrients for these children, especially vitamins A, C and D. This study aimed to understand the use of antibiotics and the profile of nutrient intake in children diagnosed with URI. During 12 months, a survey (24 h dietary recall) was applied in 131 parents of children using antibiotics. The results showed antibiotic prescriptions for viral infections (37 %), pointing out incorrect prescriptions. The presence of URI was directly related to the lack of intake of vitamins, especially A and D. Countries with poor sources of these vitamins (fish oil), in regular diet, should increase the dietary supplementation of vitamins to diminish the appearance of URIs. Singh, Narender Arora, Ashish Kaushik, Deepak http://sedici.unlp.edu.ar:80/handle/10915/8416 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 10 This article investigates enhancement of the dissolution profile of gliclazide, an antidiabetic drug, using the combination of solid dispersions and melt adsorption techniques. Poloxamer and PEG 6000 were utilized as hydrophilic carriers for solid dispersions preparation and lactose selected on the basis of preliminary studies was utilized as an adsorbent for the preparation of solid dispersion adsorbates. The techniques of FTIR spectroscopy, differential scanning calorimetry (DSC), and X-ray diffractometry (XRD) were performed to characterize the solid dispersions and to identify the physicochemical interaction between drug and carriers. Dissolution rate of gliclazide was higher in case of solid dispersion adsorbates as compared to solid dispersion alone and one of the marketed products. Thus the solid dispersion adsorbates can be successfully used for improvement of dissolution rate of gliclazide.

2011-01-01T00:00:00Z This article investigates enhancement of the dissolution profile of gliclazide, an antidiabetic drug, using the combination of solid dispersions and melt adsorption techniques. Poloxamer and PEG 6000 were utilized as hydrophilic carriers for solid dispersions preparation and lactose selected on the basis of preliminary studies was utilized as an adsorbent for the preparation of solid dispersion adsorbates. The techniques of FTIR spectroscopy, differential scanning calorimetry (DSC), and X-ray diffractometry (XRD) were performed to characterize the solid dispersions and to identify the physicochemical interaction between drug and carriers. Dissolution rate of gliclazide was higher in case of solid dispersion adsorbates as compared to solid dispersion alone and one of the marketed products. Thus the solid dispersion adsorbates can be successfully used for improvement of dissolution rate of gliclazide. Zhao, Ziming Jiang, Xianglan Yin, Xiaoxin Tang, Daoquan An, Yi-qiang Chen, Xu Wu, Jing http://sedici.unlp.edu.ar:80/handle/10915/8415 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The objective of this paper was to develop a high performance liquid chromatography with diode array detection both for chromatographic fingerprint and simultaneous determination of twelve analytes of Shuang-Huang-Lian (SHL) capsule. The chromatographic separation was performed on an Aglient Zorbax SB-C₁₈ column with a gradient elution program using a mixture of acetonitrile and 0.2 % acetic acid as mobile phase within 110 min detected at 278 nm wavelength. For fingerprint analysis, 50 peaks were selected as the common peaks to evaluate the similarities of different samples collected from different pharmaceutical companies in China, and two kinds of data, relative retention time and relative peak area were used to identify the common peaks in samples for investigation. SHL capsules from different batches of the same manufacturer or different manufacturers showed a close similarity. For quantitative analysis, linear regressions, limit of detection and quantification, intra-day and inter-day precisions, recovery, repeatability and stability were all tested and good results were obtained to simultaneously determine the 12 marker compounds in the samples. The validated method coupled with multiple compounds determination and fingerprint analysis is a powerful and meaningful tool to comprehensively conduct the quality control of TCM.

2011-01-01T00:00:00Z The objective of this paper was to develop a high performance liquid chromatography with diode array detection both for chromatographic fingerprint and simultaneous determination of twelve analytes of Shuang-Huang-Lian (SHL) capsule. The chromatographic separation was performed on an Aglient Zorbax SB-C₁₈ column with a gradient elution program using a mixture of acetonitrile and 0.2 % acetic acid as mobile phase within 110 min detected at 278 nm wavelength. For fingerprint analysis, 50 peaks were selected as the common peaks to evaluate the similarities of different samples collected from different pharmaceutical companies in China, and two kinds of data, relative retention time and relative peak area were used to identify the common peaks in samples for investigation. SHL capsules from different batches of the same manufacturer or different manufacturers showed a close similarity. For quantitative analysis, linear regressions, limit of detection and quantification, intra-day and inter-day precisions, recovery, repeatability and stability were all tested and good results were obtained to simultaneously determine the 12 marker compounds in the samples. The validated method coupled with multiple compounds determination and fingerprint analysis is a powerful and meaningful tool to comprehensively conduct the quality control of TCM. Antunes, Marina V. Linden, Rafael Pasqualotto, Alessandro C. Andreolla, Huander F. Spaniol, Bárbara Bordin, Natália A. http://sedici.unlp.edu.ar:80/handle/10915/8414 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 A fast and reliable method for the determination of voriconazole in oral fluid using microextraction by packed sorbent and liquid chromatography with fluorescence detection was developed and validated. MEPS was performed at basic pH with only 50 μL of oral fluid and the extract was injected without an evaporation step. The overall procedure, including extraction and chromatographic analysis, took only 15 min. Voriconazole and internal standard were separated on a Lichrospher RP 8ec column (250 x 4 mm, particle diameter 5 μm) eluted with a mobile phase composed of phosphate pH 2.3 (containing 0.1 % triethylamine) and acetonitrile (64:36, v/v) at a flow rate of 1.4 mL min-1 . Total run time was 11 min, with detection being performed with excitation at 254 and emission at 372 nm. The method was successfully applied to oral fluid samples, with voriconazole concentrations presenting an average of 57.6 % of those measured in paired plasma samples.

2011-01-01T00:00:00Z A fast and reliable method for the determination of voriconazole in oral fluid using microextraction by packed sorbent and liquid chromatography with fluorescence detection was developed and validated. MEPS was performed at basic pH with only 50 μL of oral fluid and the extract was injected without an evaporation step. The overall procedure, including extraction and chromatographic analysis, took only 15 min. Voriconazole and internal standard were separated on a Lichrospher RP 8ec column (250 x 4 mm, particle diameter 5 μm) eluted with a mobile phase composed of phosphate pH 2.3 (containing 0.1 % triethylamine) and acetonitrile (64:36, v/v) at a flow rate of 1.4 mL min-1 . Total run time was 11 min, with detection being performed with excitation at 254 and emission at 372 nm. The method was successfully applied to oral fluid samples, with voriconazole concentrations presenting an average of 57.6 % of those measured in paired plasma samples. Gonzalez, Cristina Tust, Patrícia B. http://sedici.unlp.edu.ar:80/handle/10915/8413 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 We aimed to evaluate the incidence of adverse drug reactions (ADRs) at a hospital, determine the variation in the incidence of ADRs between genders and among age groups, and determine the pharmacological class most often involved in ADRs. A longitudinal prospective study was conducted over a period of 5 months by using an active search in all hospital units. Four hundred forty-six patients were followed during their hospitalization; 103 showed ADRs, resulting in a 23 % overall incidence. Suspected ADRs were identified in 136 patients. From this group of patients, 9 reactions were classified as definite (6.6 %), 77 as probable (56.6 %), and 50 as possible (36.8 %). Female gender, patient age less than 65 years, and hospitalization in the Gynecology and Obstetrics Ward were factors associated with a higher incidence of ADR development. The active search is a suitable instrument for assessing the incidence of ADRs in the hospital.

2011-01-01T00:00:00Z We aimed to evaluate the incidence of adverse drug reactions (ADRs) at a hospital, determine the variation in the incidence of ADRs between genders and among age groups, and determine the pharmacological class most often involved in ADRs. A longitudinal prospective study was conducted over a period of 5 months by using an active search in all hospital units. Four hundred forty-six patients were followed during their hospitalization; 103 showed ADRs, resulting in a 23 % overall incidence. Suspected ADRs were identified in 136 patients. From this group of patients, 9 reactions were classified as definite (6.6 %), 77 as probable (56.6 %), and 50 as possible (36.8 %). Female gender, patient age less than 65 years, and hospitalization in the Gynecology and Obstetrics Ward were factors associated with a higher incidence of ADR development. The active search is a suitable instrument for assessing the incidence of ADRs in the hospital. Hu, Rong Jiang, Hui Zhang, Lei Cheng, Wen-Ming Li, Jun Chen, Xiao-Yu http://sedici.unlp.edu.ar:80/handle/10915/8412 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 Chrysanthemum is a traditional Chinese medicine used in China to treated inflammatory disease. The total flavonoids of Chrysanthemum indicum (TFC) were extracted from the dried bud of C. indicum. Our previous study had demonstrated TFC was a new class of effective anti- inflammation, analgesia and immunoloregulation agents. In this study, we established an adjuvant arthritis (AA) model by injection of Freund’s Complete Adjuvant (FCA) to investigate the effect of TFC on chronic autoimmune disease. Secondary paw swelling of AA rats was measured with volume meter and polyarthritis index was scored. IL-1β and TNF-α production in synoviocytes were determined by radioimmunoassay. RT-PCR observed mRNA expressions of IL-1β and TNF-α in the synovial membrane. The morphological alteration of synoviocytes organell was followed by transmission electron microscopy.

2011-01-01T00:00:00Z Chrysanthemum is a traditional Chinese medicine used in China to treated inflammatory disease. The total flavonoids of Chrysanthemum indicum (TFC) were extracted from the dried bud of C. indicum. Our previous study had demonstrated TFC was a new class of effective anti- inflammation, analgesia and immunoloregulation agents. In this study, we established an adjuvant arthritis (AA) model by injection of Freund’s Complete Adjuvant (FCA) to investigate the effect of TFC on chronic autoimmune disease. Secondary paw swelling of AA rats was measured with volume meter and polyarthritis index was scored. IL-1β and TNF-α production in synoviocytes were determined by radioimmunoassay. RT-PCR observed mRNA expressions of IL-1β and TNF-α in the synovial membrane. The morphological alteration of synoviocytes organell was followed by transmission electron microscopy. Martínez, Fleming Romdhani, Asma Delgado, Daniel R. http://sedici.unlp.edu.ar:80/handle/10915/8411 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; p. 2024-2030 The solubility of sulfanilamide (SA) in propylene glycol + water cosolvent mixtures was determined at temperatures from 293.15 to 313.15 K. The thermodynamic functions: Gibbs energy, enthalpy, and entropy of solution and mixing were obtained from these solubility data by using the van’t Hoff and Gibbs equations. The solubility was maximal in propylene glycol and very low in water at all the temperatures. A non linear enthalpy–entropy relationship was observed from a plot of enthalpy vs. Gibbs energy of solution. The maximum point in plot of Δ_solnH° vs. Δ_solnnG° (0.20 mass fraction of propylene glycol) separates two different trends, one with negative slope from water up to 0.20 mass fraction of propylene glycol and the other one positive beyond this composition up to propylene glycol. Accordingly, the driving mechanism for SA solubility in water-rich mixtures is the entropy, probably due to water-structure loss around the drug non-polar moieties by propylene glycol, whereas, above 0.20 mass fraction of propylene glycol the driving mechanism is the enthalpy, probably due to SA solvation increase by the co-solvent molecules.

2011-01-01T00:00:00Z The solubility of sulfanilamide (SA) in propylene glycol + water cosolvent mixtures was determined at temperatures from 293.15 to 313.15 K. The thermodynamic functions: Gibbs energy, enthalpy, and entropy of solution and mixing were obtained from these solubility data by using the van’t Hoff and Gibbs equations. The solubility was maximal in propylene glycol and very low in water at all the temperatures. A non linear enthalpy–entropy relationship was observed from a plot of enthalpy vs. Gibbs energy of solution. The maximum point in plot of Δ_solnH° vs. Δ_solnnG° (0.20 mass fraction of propylene glycol) separates two different trends, one with negative slope from water up to 0.20 mass fraction of propylene glycol and the other one positive beyond this composition up to propylene glycol. Accordingly, the driving mechanism for SA solubility in water-rich mixtures is the entropy, probably due to water-structure loss around the drug non-polar moieties by propylene glycol, whereas, above 0.20 mass fraction of propylene glycol the driving mechanism is the enthalpy, probably due to SA solvation increase by the co-solvent molecules. Negi, Bhawana Bansal, Ruchi Singh, Dhirendra P. Singh, Lokesh K. http://sedici.unlp.edu.ar:80/handle/10915/8410 2012-12-28T02:01:56Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 A simple, economic and time-efficient, isocratic reverse-phase ultra performance liquid chromatographic (RP-UPLC) method has been developed to analyze aripiprazole in tablets. Successful chromatographic elution and quantification of the drug was achieved on a Waters Symmetry C18, 100 mm x 4.6mm, 3.5 μm column, UV detection at 220 nm with a isocratic mobile phase comprising a mixture of component A (pH 2.5, phosphate buffer) and component B (methanol and acetonitrile (1:1, v/v) in the ratio of 45:55 (v/v). The flow rate was 1.0 mL/min. The method was validated for specificity, precision, linearity, accuracy, range, stability in analytical solution, robustness and system suitability. The linearity concentration range was 5.4-67.8 μg/mL with the correlation coefficient of 0.9997. Total elution time was about 6 min which allowed quantification of more than 100 samples per day.

2011-01-01T00:00:00Z A simple, economic and time-efficient, isocratic reverse-phase ultra performance liquid chromatographic (RP-UPLC) method has been developed to analyze aripiprazole in tablets. Successful chromatographic elution and quantification of the drug was achieved on a Waters Symmetry C18, 100 mm x 4.6mm, 3.5 μm column, UV detection at 220 nm with a isocratic mobile phase comprising a mixture of component A (pH 2.5, phosphate buffer) and component B (methanol and acetonitrile (1:1, v/v) in the ratio of 45:55 (v/v). The flow rate was 1.0 mL/min. The method was validated for specificity, precision, linearity, accuracy, range, stability in analytical solution, robustness and system suitability. The linearity concentration range was 5.4-67.8 μg/mL with the correlation coefficient of 0.9997. Total elution time was about 6 min which allowed quantification of more than 100 samples per day. Rao, J. Venkateswara Pore, Yogesh V. Shinde, Vikram R. http://sedici.unlp.edu.ar:80/handle/10915/8409 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The ternary solid dispersion systems of poorly water soluble olmesartan medoxomil (OLM) were prepared by conventional kneading method in order to improve its physicochemical performance. A 3² full factorial design approach was employed to optimize influence of concentration of polyvinylpyrrolidone K30 (PVP) and poloxamer 407 (PLX) on physicochemical characteristics of these dispersions. All formulations were characterized by XRPD, DSC and dissolution studies. Physical studies revealed complete loss of crystallinity and formation of uniform molecular dispersion of OLM in its ternary systems. All dispersion systems showed significant improvement in dissolution profile in comparison to pure drug alone (p < 0.001). The optimized formulation provided superior solubility and dissolution behaviour (F1; DP₂ : 68.43 ± 2.8 %) of OLM suggesting optimum ratio of carrier system. The kinetic study of dissolution displayed to follow the Korsmeyer-Peppas model (r² = 0.9835).

2011-01-01T00:00:00Z The ternary solid dispersion systems of poorly water soluble olmesartan medoxomil (OLM) were prepared by conventional kneading method in order to improve its physicochemical performance. A 3² full factorial design approach was employed to optimize influence of concentration of polyvinylpyrrolidone K30 (PVP) and poloxamer 407 (PLX) on physicochemical characteristics of these dispersions. All formulations were characterized by XRPD, DSC and dissolution studies. Physical studies revealed complete loss of crystallinity and formation of uniform molecular dispersion of OLM in its ternary systems. All dispersion systems showed significant improvement in dissolution profile in comparison to pure drug alone (p < 0.001). The optimized formulation provided superior solubility and dissolution behaviour (F1; DP₂ : 68.43 ± 2.8 %) of OLM suggesting optimum ratio of carrier system. The kinetic study of dissolution displayed to follow the Korsmeyer-Peppas model (r² = 0.9835). Harikumar, S. L. Singh, Satish http://sedici.unlp.edu.ar:80/handle/10915/8408 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The objective of the present investigation was to investigate the effects of selected drugs (captopril and celecoxib) properties on different parameters drug entrapment, in vitro drug release, release pattern, in vitro drug permeation and buoyancy in the formulation of Eudragit S100 non effervescent floating microparticulates. Microparticulates were in size ranges 268.36-352.27 μm (captopril) and 271.36- 365.54 μm (celecoxib). Encapsulation efficiency of celecoxib was good as compare to captopril. In vitro permeation studies showed in range (ES6) 74.83 μg – (ES1) 79.84 μg (celecoxib), (EU6) 57.01 μg - (EU1) 67.38 μg (captopril). In vitro release followed Non-Fickian diffusion mechanism while in vitro permeation kinetics revealed the super case II transport mechanism. Taken together, water insoluble (celecoxib) drug showed suitable combination with Eudragit S100. This study concluded that the effect of various parameter on the characteristics of Eudragit gastroretentive drug delivery system by non effervescent technique using celecoxib and captopril having different physicochemical characterization.

2011-01-01T00:00:00Z The objective of the present investigation was to investigate the effects of selected drugs (captopril and celecoxib) properties on different parameters drug entrapment, in vitro drug release, release pattern, in vitro drug permeation and buoyancy in the formulation of Eudragit S100 non effervescent floating microparticulates. Microparticulates were in size ranges 268.36-352.27 μm (captopril) and 271.36- 365.54 μm (celecoxib). Encapsulation efficiency of celecoxib was good as compare to captopril. In vitro permeation studies showed in range (ES6) 74.83 μg – (ES1) 79.84 μg (celecoxib), (EU6) 57.01 μg - (EU1) 67.38 μg (captopril). In vitro release followed Non-Fickian diffusion mechanism while in vitro permeation kinetics revealed the super case II transport mechanism. Taken together, water insoluble (celecoxib) drug showed suitable combination with Eudragit S100. This study concluded that the effect of various parameter on the characteristics of Eudragit gastroretentive drug delivery system by non effervescent technique using celecoxib and captopril having different physicochemical characterization. Santos, Orlando D. H. Mezadri, Hygor Aguiar, Tatiana A. Oliveira, Juliana S. http://sedici.unlp.edu.ar:80/handle/10915/8407 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 Nanoemulsions are special emulsions that consist in a very small drop with sizes between 20 to 500 nm. When they are intended for topical application, the main problem of nanoemulsions is their low viscosity, which is reflex of the small drop size. It was proposed the attainment of hydrogel-thickned nanoemulsions with vitamin A palmitate (retinyl palmitate) with green coffee seed oil by phase inversion. Hydrogel-thickned nanoemulsions with drops size ranging between 77 to 110 nm were obtained, depending on the polymer used, with increased viscosity. Rheological profile of developed hydrogel-thickned nanoemulsions was determined, showing the influence of the kind of polymer used, here all presented pseudo-plastic behaviour, with different viscosity measurement. The improvement of the viscosity of the systems, associated with the small droplet size, can be very interesting for vitamin A delivery under the skin.

2011-01-01T00:00:00Z Nanoemulsions are special emulsions that consist in a very small drop with sizes between 20 to 500 nm. When they are intended for topical application, the main problem of nanoemulsions is their low viscosity, which is reflex of the small drop size. It was proposed the attainment of hydrogel-thickned nanoemulsions with vitamin A palmitate (retinyl palmitate) with green coffee seed oil by phase inversion. Hydrogel-thickned nanoemulsions with drops size ranging between 77 to 110 nm were obtained, depending on the polymer used, with increased viscosity. Rheological profile of developed hydrogel-thickned nanoemulsions was determined, showing the influence of the kind of polymer used, here all presented pseudo-plastic behaviour, with different viscosity measurement. The improvement of the viscosity of the systems, associated with the small droplet size, can be very interesting for vitamin A delivery under the skin. Mohammed, Kaleemullah Fadli, Mohd Yusuf, Eddy Hamid, Junainah Abd Chitneni, Mallikarjun Elhassan, Gamal O. Al-Dhalli, Samer Wong, Jia W. NG, Bee H. Yuen, Kah H. Khan, Jiyauddin http://sedici.unlp.edu.ar:80/handle/10915/8406 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The aim of this study was to evaluate the in vivo behavior of matrix tablets formulated with ketoprofen as a model drug after oral administrations in healthy Malaysian male volunteers and to compare its rate and extent of absorption with the commercially available tablet Apo-Keto SR® as a reference product. The test formulation containing 20 % HPC (GXF) as release retardant was selected in this regards. The bioequivalence study was conducted according to a single dose, randomized, 2-treatment, 2-sequence, 2-period crossover study design on six healthy non-smoking Malaysian adult male volunteers. Plasma concentrations of ketoprofen were determined by a high-performance liquid chromatographic method with UV detection. The pharmacokinetic parameters, T_max , C_max , AUC_{0–∞}, K_e , and T_1/2 were determined. The 90 % confidence intervals of the mean values for the test/reference ratios were 96.89-107.03 % for AUC_{0–∞} and 99.64-104.62 % for C_max , respectively. The results of this study suggest that the two preparations, the test formulation of ketoprofen 200 mg tablets were bioequivalent to the marketed reference tablet of Apo-Keto SR® 200 mg in these healthy Malaysian male volunteers. However, this study results are to be further confirmed by carrying out a pivotal biostudy using more number of subjects.

2011-01-01T00:00:00Z The aim of this study was to evaluate the in vivo behavior of matrix tablets formulated with ketoprofen as a model drug after oral administrations in healthy Malaysian male volunteers and to compare its rate and extent of absorption with the commercially available tablet Apo-Keto SR® as a reference product. The test formulation containing 20 % HPC (GXF) as release retardant was selected in this regards. The bioequivalence study was conducted according to a single dose, randomized, 2-treatment, 2-sequence, 2-period crossover study design on six healthy non-smoking Malaysian adult male volunteers. Plasma concentrations of ketoprofen were determined by a high-performance liquid chromatographic method with UV detection. The pharmacokinetic parameters, T_max , C_max , AUC_{0–∞}, K_e , and T_1/2 were determined. The 90 % confidence intervals of the mean values for the test/reference ratios were 96.89-107.03 % for AUC_{0–∞} and 99.64-104.62 % for C_max , respectively. The results of this study suggest that the two preparations, the test formulation of ketoprofen 200 mg tablets were bioequivalent to the marketed reference tablet of Apo-Keto SR® 200 mg in these healthy Malaysian male volunteers. However, this study results are to be further confirmed by carrying out a pivotal biostudy using more number of subjects. Dias Junior, Carlos A.C. Ribeiro, Andréia Soares, Adriana C. Pereira, Mariana L. Nascimento, Mariana M.G. http://sedici.unlp.edu.ar:80/handle/10915/8405 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The elderly population and the incidence of chronic diseases are growing rapidly in Brazil. This raises the demand for health services (like Nursing Homes - NH) and drugs, exposing this population to Potential Drug Therapy Problems (PDTP). A cross-sectional study in a Brazilian NH was developed through prescription analyses. PDTP were accounted when one of the following were detected: double therapy (DT); sub-dose; overdose; drug-drug interaction (DDI); food-drug interaction (FDI); Potentially Inappropriate Medication (PIM) according to the Beers Criteria; PIM according to the STOPP (Screening Tool for Older Persons’ Prescriptions). 116 PDTP were identified (17 DT, 16 sub-doses, an overdose, 52 DDI, 10 FDI, and 20 PIM according to Beers). With the STOPP, 143 PDTP were detected. Safety PDTP were the most frequent. The high number of PDTP detected indicates a low level of quality of the prescriptions, showing the need for the pharmacist work towards elderly drug therapy upgrade.

2011-01-01T00:00:00Z The elderly population and the incidence of chronic diseases are growing rapidly in Brazil. This raises the demand for health services (like Nursing Homes - NH) and drugs, exposing this population to Potential Drug Therapy Problems (PDTP). A cross-sectional study in a Brazilian NH was developed through prescription analyses. PDTP were accounted when one of the following were detected: double therapy (DT); sub-dose; overdose; drug-drug interaction (DDI); food-drug interaction (FDI); Potentially Inappropriate Medication (PIM) according to the Beers Criteria; PIM according to the STOPP (Screening Tool for Older Persons’ Prescriptions). 116 PDTP were identified (17 DT, 16 sub-doses, an overdose, 52 DDI, 10 FDI, and 20 PIM according to Beers). With the STOPP, 143 PDTP were detected. Safety PDTP were the most frequent. The high number of PDTP detected indicates a low level of quality of the prescriptions, showing the need for the pharmacist work towards elderly drug therapy upgrade. Flores Pérez, Carmen Juárez Olguín, Hugo Flores Pérez, Janett Ramírez Mendiola, Blanca González Zamora, José F. Alemón Medina, Radamés Rivera Espinosa, Liliana Chávez Pacheco, Juan L. http://sedici.unlp.edu.ar:80/handle/10915/8404 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The aim of this work was to assess the stability and sedative effect of midazolam in chocolate bars. The stability of 5 g chocolate bars containing 6 mg midazolam hydrochloride was evaluated at room temperature (25 ± 2 °C), at 4 and 40 °C, by HPLC. Drug plasma levels were measured and the sedative effect was confirmed in six healthy volunteers according to the Ramsay’s scale. Data regarding chocolate bar administration were compared to those from the apple juice solution. Pharmacokinetic data were processed using the WinNonLin 5.2 software. Midazolam in chocolate bars remained stable for 14 days at room temperature and exposed to light; for 90 days at 4 and 40 °C protected from light, and showed a longer shelf life, better flavour and appearance, inducing the same sedative effect as the apple juice preparation. Raspberry flavour masked midazolam unpleasing taste most favourably.

2011-01-01T00:00:00Z The aim of this work was to assess the stability and sedative effect of midazolam in chocolate bars. The stability of 5 g chocolate bars containing 6 mg midazolam hydrochloride was evaluated at room temperature (25 ± 2 °C), at 4 and 40 °C, by HPLC. Drug plasma levels were measured and the sedative effect was confirmed in six healthy volunteers according to the Ramsay’s scale. Data regarding chocolate bar administration were compared to those from the apple juice solution. Pharmacokinetic data were processed using the WinNonLin 5.2 software. Midazolam in chocolate bars remained stable for 14 days at room temperature and exposed to light; for 90 days at 4 and 40 °C protected from light, and showed a longer shelf life, better flavour and appearance, inducing the same sedative effect as the apple juice preparation. Raspberry flavour masked midazolam unpleasing taste most favourably. Barik, B. B. Premchandani, T. A. http://sedici.unlp.edu.ar:80/handle/10915/8403 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The present study involves preparation and characterization of floating multiparticulate microcapsules with Simvastatin as model drug for prolongation of gastric residence time. The main objective is to improve solubility of simvastatin β-CD complex (1:2) by co-precipitation method and then to deliver the same in sustained release dosage form. Sustained-release simvastatin microcapsules were prepared by the ionic gelation technique, using carbopol-941 as self-swelling polymer. A 3³ Full factorial design was used to study the effect of polymer concentration, Drug complex and sodium alginate. The formed microcapsules were subjected to various evaluation tests such as drug encapsulation efficiency, in vitro drug release and surface morphology was studied using SEM, powdered X-Ray diffractometer and FTIR to investigate the complexation of simvastatin in the microcapsules. As carbopol 941 is self swellable polymer, immediate floating was observed. The in vitro release studies and floating behavior were performed in HCl buffer pH 1.2. The best fit release kinetics was achieved with first order release. The microcapsules were subjected to long term stability studies. It was concluded that porous carbopol 941 microcapsules are promising sustained release as well as stomach specific carriers for delivery of simvastatin.

2011-01-01T00:00:00Z The present study involves preparation and characterization of floating multiparticulate microcapsules with Simvastatin as model drug for prolongation of gastric residence time. The main objective is to improve solubility of simvastatin β-CD complex (1:2) by co-precipitation method and then to deliver the same in sustained release dosage form. Sustained-release simvastatin microcapsules were prepared by the ionic gelation technique, using carbopol-941 as self-swelling polymer. A 3³ Full factorial design was used to study the effect of polymer concentration, Drug complex and sodium alginate. The formed microcapsules were subjected to various evaluation tests such as drug encapsulation efficiency, in vitro drug release and surface morphology was studied using SEM, powdered X-Ray diffractometer and FTIR to investigate the complexation of simvastatin in the microcapsules. As carbopol 941 is self swellable polymer, immediate floating was observed. The in vitro release studies and floating behavior were performed in HCl buffer pH 1.2. The best fit release kinetics was achieved with first order release. The microcapsules were subjected to long term stability studies. It was concluded that porous carbopol 941 microcapsules are promising sustained release as well as stomach specific carriers for delivery of simvastatin. Rathore, Devashish Dahima, Rashmi http://sedici.unlp.edu.ar:80/handle/10915/8402 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 The present investigation concerns the development of floating tablets of tramadol hydrochloride, which after oral administration are designed to prolong the gastric residence time; improves the drug bioavailability, reduces drug waste and diminish the side effects of drug. The D-optimal experimental design was employed to evaluate contribution of hydroxypropyl methyl cellulose (HPMC) K4M concentration, lactose concentration and kollidone SR concentration on drug release from floating tablets. Tablets were prepared using direct compression technique. Formulations were evaluated for in vitro buoyancy and drug release study using United States Pharmacopoeia (USP) 24 paddle type dissolution apparatus using 0.1 N HCl as dissolution medium. Multiple regression analysis was performed for factorial design batches to evaluate the response. All formulation had floating lag time below 2 min and constantly floated on dissolution medium for more than 24 h. It was found that optimized HPMC K4M (100 mg), kollidone SR (25 mg) and lactose (17.5 mg) have shown the release of 98.4 % in 22 h which was better as compare to marketed product (i.e. Tramazac-SR). Kinetic treatment to dissolution profiles revealed the diffusion mechanism so called as Fickian diffusion (Case I transport) which was mainly dependent on all the independent variables.

2011-01-01T00:00:00Z The present investigation concerns the development of floating tablets of tramadol hydrochloride, which after oral administration are designed to prolong the gastric residence time; improves the drug bioavailability, reduces drug waste and diminish the side effects of drug. The D-optimal experimental design was employed to evaluate contribution of hydroxypropyl methyl cellulose (HPMC) K4M concentration, lactose concentration and kollidone SR concentration on drug release from floating tablets. Tablets were prepared using direct compression technique. Formulations were evaluated for in vitro buoyancy and drug release study using United States Pharmacopoeia (USP) 24 paddle type dissolution apparatus using 0.1 N HCl as dissolution medium. Multiple regression analysis was performed for factorial design batches to evaluate the response. All formulation had floating lag time below 2 min and constantly floated on dissolution medium for more than 24 h. It was found that optimized HPMC K4M (100 mg), kollidone SR (25 mg) and lactose (17.5 mg) have shown the release of 98.4 % in 22 h which was better as compare to marketed product (i.e. Tramazac-SR). Kinetic treatment to dissolution profiles revealed the diffusion mechanism so called as Fickian diffusion (Case I transport) which was mainly dependent on all the independent variables. Hanif, Muhammad Muhammad, Iyad N. Effet, Wajhia Yousuf, Rabia I. Ghiasuddin, Muhammad Shoaib, Harris M. http://sedici.unlp.edu.ar:80/handle/10915/8401 2012-12-28T02:01:57Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 10 Effervescent tablets have always been convenient, simple and measured dosage form. The phenomenon of carbonation, in this type of dosage form, accelerates the solubility and enhances the bioavailability of the drug and the addition of flavorant also masks the objectionable taste of the medicament in a more patient compliant way. The present study focuses on developing a new, simple, cost effective formulation of naproxen sodium 250 mg as an effervescent tablet using direct compression technique. Nine different trial formulations of naproxen 250 mg were designed with varying proportions of sodium carbonate, sodium bicarbonate, citric acid and PEG 6000 and were prepared by direct compression method, and evaluated for pharmaceutical quality attributes. Quality assessment proved formulations F8 as a satisfactory one showing respectively mean weight of 2200 ± 50.52 having hardness and friability of 14.78421 ± 1.3791 kg and 1.241 %. Tablets took 4 min and 36 s to disintegrate completely. The average pH of the solution was within the range of 5.65 to 5.85. Dissolution profile comparison with the conventional formulation was carried out and maximum drug release by the trial formulation was observed within 15 min. spectrophotometric determination of drug content was found to be 99.82 ± 1.754. Stability characterization was also conducted on the formulations under stress (40 °C/75 % R.H.) that showed formulations remained stable throughout the study duration with acceptable difference in physical and chemical characteristics. Such formulations increases patient compliance and have possibly improved bioavailability. The work also emphasizes on the benefit of using direct compression method as a cost effective technique in terms of process, materials handling with productivity.

2011-01-01T00:00:00Z Effervescent tablets have always been convenient, simple and measured dosage form. The phenomenon of carbonation, in this type of dosage form, accelerates the solubility and enhances the bioavailability of the drug and the addition of flavorant also masks the objectionable taste of the medicament in a more patient compliant way. The present study focuses on developing a new, simple, cost effective formulation of naproxen sodium 250 mg as an effervescent tablet using direct compression technique. Nine different trial formulations of naproxen 250 mg were designed with varying proportions of sodium carbonate, sodium bicarbonate, citric acid and PEG 6000 and were prepared by direct compression method, and evaluated for pharmaceutical quality attributes. Quality assessment proved formulations F8 as a satisfactory one showing respectively mean weight of 2200 ± 50.52 having hardness and friability of 14.78421 ± 1.3791 kg and 1.241 %. Tablets took 4 min and 36 s to disintegrate completely. The average pH of the solution was within the range of 5.65 to 5.85. Dissolution profile comparison with the conventional formulation was carried out and maximum drug release by the trial formulation was observed within 15 min. spectrophotometric determination of drug content was found to be 99.82 ± 1.754. Stability characterization was also conducted on the formulations under stress (40 °C/75 % R.H.) that showed formulations remained stable throughout the study duration with acceptable difference in physical and chemical characteristics. Such formulations increases patient compliance and have possibly improved bioavailability. The work also emphasizes on the benefit of using direct compression method as a cost effective technique in terms of process, materials handling with productivity.