cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.20039076.v1
title: Use of a commercial agarose gel for analysis of urinary glycosaminoglycans in mucopolysaccharidoses

description: ABSTRACT Mucopolysaccharidoses (MPS) are a group of inherited metabolic disorders caused by deficiency of enzymes that degrade glycosaminoglycans (GAGs). Urinary excretion of GAGs is a common feature of MPS, and is considered their major biomarker. We aimed to adapt the GAG electrophoresis method to a commercial agarose gel which would be able to separate urinary GAGs in a simpler way with good sensitivity and reproducibility. Urine samples from patients previously diagnosed with MPS I, IV, and VI were used as electrophoretic standards. Samples from patients on enzyme replacement therapy (ERT) were also assessed. Commercial agarose gel electrophoresis was effective, showing proper definition and separation of GAG bands. Detection sensitivity exceeded 0.1 µg and band reproducibility were consistent. GAG bands quantified in urine samples from patients on ERT correlated very strongly (correlation coefficient = 0.98) with total GAG concentrations. This application of gel electrophoresis demonstrates the possibility of monitoring patients with MPS treated with ERT by analyzing separately the GAGs excreted in urine. We suggest this process should be applied to MPS screening as well as to follow-up of patients on treatment.
DOI: 10.6084/m9.figshare.20039078
title: Exposure to potentially inappropriate medications in Brazilian elderly outpatients with metabolic diseases

description: ABSTRACT Management of pharmacotherapy in elderly with metabolic diseases is challenging and potentially inappropriate medications (PIMs) are risk factors for drug interactions and adverse events. The exposure to PIMs in elderly outpatients with metabolic diseases and its relationship with polypharmacy and other variables was investigated. PIMs prescribed to 207 elderly patients (aged 60 to 96 years) with metabolic diseases who attended a University Hospital of Sao Paulo city, Brazil, from April/2010 to January/2011, were evaluated. PIMs were detected using both 2003 Beers and 2008 STOPP criteria. The association between PIMs and age, gender and polypharmacy was also examined. 2008 STOPP criteria detected more PIMs (44.4 %) than 2003 Beers criteria (16.0%, p&lt;0.001). Beers detected mainly PIMs antihypertensive (clonidine, 20.0%; doxazosin, 10.0%) and antidepressant (fluoxetine, 15.0%; amitriptyline, 10.0%) PIMs. Medicines used for cardiovascular (aspirin, 53.7%) and endocrine system (glibenclamide, 21.3%) were PIMs more frequently detected by 2008 STOPP. Unlike age and gender, polypharmacy increased the risk of PIMs by both 2003 Beers (OR: 4.0, CI95%: 1.2-13.8, p&lt;0.031) and 2008 STOPP (OR: 6.8, CI95%: 3.0-15.3, p&lt;0.001). Beers and STOPP criteria are important tools to evaluate the exposure to PIMs, which is strongly associated with polypharmacy in elderly outpatients with metabolic diseases.
DOI: 10.6084/m9.figshare.20039078.v1
title: Exposure to potentially inappropriate medications in Brazilian elderly outpatients with metabolic diseases

description: ABSTRACT Management of pharmacotherapy in elderly with metabolic diseases is challenging and potentially inappropriate medications (PIMs) are risk factors for drug interactions and adverse events. The exposure to PIMs in elderly outpatients with metabolic diseases and its relationship with polypharmacy and other variables was investigated. PIMs prescribed to 207 elderly patients (aged 60 to 96 years) with metabolic diseases who attended a University Hospital of Sao Paulo city, Brazil, from April/2010 to January/2011, were evaluated. PIMs were detected using both 2003 Beers and 2008 STOPP criteria. The association between PIMs and age, gender and polypharmacy was also examined. 2008 STOPP criteria detected more PIMs (44.4 %) than 2003 Beers criteria (16.0%, p&lt;0.001). Beers detected mainly PIMs antihypertensive (clonidine, 20.0%; doxazosin, 10.0%) and antidepressant (fluoxetine, 15.0%; amitriptyline, 10.0%) PIMs. Medicines used for cardiovascular (aspirin, 53.7%) and endocrine system (glibenclamide, 21.3%) were PIMs more frequently detected by 2008 STOPP. Unlike age and gender, polypharmacy increased the risk of PIMs by both 2003 Beers (OR: 4.0, CI95%: 1.2-13.8, p&lt;0.031) and 2008 STOPP (OR: 6.8, CI95%: 3.0-15.3, p&lt;0.001). Beers and STOPP criteria are important tools to evaluate the exposure to PIMs, which is strongly associated with polypharmacy in elderly outpatients with metabolic diseases.
DOI: 10.6084/m9.figshare.20039082
title: Kinetics study of hydrochlorothiazide lactose liquid state interaction using conventional isothermal arrhenius method under basic and neutral conditions

description: ABSTRACT The Maillard reaction of hydrochlorothiazide (HCTZ) and lactose has been previously demonstrated in pharmaceutical formulations. In this study, the activation energy of - hydrohlorothiazide and lactose interaction in the liquid state was ascertained under basic and neutral conditions. Conventional isothermal High Performance Liquid Chromatography (HPLC) technique was employed to ascertain the kinetic parameters using Arrhenius method. Results: The activation energy obtained was 82.43 and 100.28 kJ/mol under basic and neutral conditions, respectively. Consequently, it can be inferred that Maillard reaction is significantly affected by pH, which can be used as a control factor whenever the reaction potentially occurs.
DOI: 10.6084/m9.figshare.20039082.v1
title: Kinetics study of hydrochlorothiazide lactose liquid state interaction using conventional isothermal arrhenius method under basic and neutral conditions

description: ABSTRACT The Maillard reaction of hydrochlorothiazide (HCTZ) and lactose has been previously demonstrated in pharmaceutical formulations. In this study, the activation energy of - hydrohlorothiazide and lactose interaction in the liquid state was ascertained under basic and neutral conditions. Conventional isothermal High Performance Liquid Chromatography (HPLC) technique was employed to ascertain the kinetic parameters using Arrhenius method. Results: The activation energy obtained was 82.43 and 100.28 kJ/mol under basic and neutral conditions, respectively. Consequently, it can be inferred that Maillard reaction is significantly affected by pH, which can be used as a control factor whenever the reaction potentially occurs.
DOI: 10.6084/m9.figshare.20039084
title: A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability

description: ABSTRACT Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this property significantly increased with higher pH values. SDs allowed drug dissolution to occur in a controlled manner. HPMCP decreased the dissolution rates in the acid medium. The mucoadhesiveness of SDs was demonstrated and the permeability of AZT carried in solid dispersions was significantly improved. The effect of the SD carrier polymers on blocking efflux pump can be an important approach to improve the bioavailability of AZT.
DOI: 10.6084/m9.figshare.20039084.v1
title: A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability

description: ABSTRACT Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this property significantly increased with higher pH values. SDs allowed drug dissolution to occur in a controlled manner. HPMCP decreased the dissolution rates in the acid medium. The mucoadhesiveness of SDs was demonstrated and the permeability of AZT carried in solid dispersions was significantly improved. The effect of the SD carrier polymers on blocking efflux pump can be an important approach to improve the bioavailability of AZT.
DOI: 10.6084/m9.figshare.20039085
title: Improvement of physicochemical parameters of acyclovir using cocrystallization approach

description: ABSTRACT Acyclovir is an antiviral drug having potent activity against the virus of herpes family and varicella zoster. Unfortunately, drug suffers very poor oral bioavailability (15-30%). The main objective of present study was to develop acyclovir cocrystals with improved solubility which may result in improvement of bioavailability. Hansen solubility approach was used as a tool to predict the cocrystal formation of a drug with selected coformer. Cocrystals of acyclovir with various coformers were screened in order to enhance their water solubility. Cocrystals of the drug were prepared using various methods like solvent evaporation, wet grinding, and antisolvent addition. Formation of cocrystals by solvent evaporation method was found to be better method amongst all. Optimization of cocrystal formation was carried out by employing different solvents as well as the stoichiometric ratio of acyclovir with that of coformer. Synthesis of cocrystals was optimized using water as a solvent system resulted in good agreements. The potential cocrystal formation of acyclovir was characterized by IR, PXRD and DSC techniques. An in-vitro dissolution study was performed to determine the dissolution rate of cocrystals. The results suggest that acyclovir forms cocrystals with tartaric acid and the initial dissolution rate of synthesized cocrystals were considerably faster as compared to pure acyclovir.
DOI: 10.6084/m9.figshare.20039085.v1
title: Improvement of physicochemical parameters of acyclovir using cocrystallization approach

description: ABSTRACT Acyclovir is an antiviral drug having potent activity against the virus of herpes family and varicella zoster. Unfortunately, drug suffers very poor oral bioavailability (15-30%). The main objective of present study was to develop acyclovir cocrystals with improved solubility which may result in improvement of bioavailability. Hansen solubility approach was used as a tool to predict the cocrystal formation of a drug with selected coformer. Cocrystals of acyclovir with various coformers were screened in order to enhance their water solubility. Cocrystals of the drug were prepared using various methods like solvent evaporation, wet grinding, and antisolvent addition. Formation of cocrystals by solvent evaporation method was found to be better method amongst all. Optimization of cocrystal formation was carried out by employing different solvents as well as the stoichiometric ratio of acyclovir with that of coformer. Synthesis of cocrystals was optimized using water as a solvent system resulted in good agreements. The potential cocrystal formation of acyclovir was characterized by IR, PXRD and DSC techniques. An in-vitro dissolution study was performed to determine the dissolution rate of cocrystals. The results suggest that acyclovir forms cocrystals with tartaric acid and the initial dissolution rate of synthesized cocrystals were considerably faster as compared to pure acyclovir.
DOI: 10.6084/m9.figshare.20039087.v1
title: In vitro evaluation of sustained released matrix tablets containing ibuprofen: a model poorly water-soluble drug

description: ABSTRACT A matrix system was developed that releases ibuprofen (IB) over a 12-hour period and the influence of the polymer type and concentration on the release rate of the drug was evaluated. Tablets containing different concentrations of Carbopol (CP), hydroxypropyl methylcellulose (HPMC), or ethyl cellulose (EC) were prepared using direct compression and the drug content, content uniformity, hardness, friability, dissolution performance, and in vitro release kinetics were examined. Formulated tablets were found to be within acceptable limits for physical and chemical parameters. The release kinetics of the Carbopol(r)971P 8% formulation showed the best linearity (r 2 =0.977) in fitting zero-order kinetics, suggesting the release rate was time independent. The drug release from tablets containing 8% CP was extended over approximately 18 hours and the release kinetics were nearly linear, suggesting that this system has the potential to maintain constant plasma drug concentrations over 12 hours, which could reduce the frequency of administration and the occurrence of adverse effects associated with repeated administration of conventional IB tablets.
DOI: 10.6084/m9.figshare.20039087
title: In vitro evaluation of sustained released matrix tablets containing ibuprofen: a model poorly water-soluble drug

description: ABSTRACT A matrix system was developed that releases ibuprofen (IB) over a 12-hour period and the influence of the polymer type and concentration on the release rate of the drug was evaluated. Tablets containing different concentrations of Carbopol (CP), hydroxypropyl methylcellulose (HPMC), or ethyl cellulose (EC) were prepared using direct compression and the drug content, content uniformity, hardness, friability, dissolution performance, and in vitro release kinetics were examined. Formulated tablets were found to be within acceptable limits for physical and chemical parameters. The release kinetics of the Carbopol(r)971P 8% formulation showed the best linearity (r 2 =0.977) in fitting zero-order kinetics, suggesting the release rate was time independent. The drug release from tablets containing 8% CP was extended over approximately 18 hours and the release kinetics were nearly linear, suggesting that this system has the potential to maintain constant plasma drug concentrations over 12 hours, which could reduce the frequency of administration and the occurrence of adverse effects associated with repeated administration of conventional IB tablets.
DOI: 10.6084/m9.figshare.20039088
title: Influence of high-dose gamma radiation and particle size on antioxidant properties of Maize ( Zea mays L.) flour

description: ABSTRACT Influence of high-dose gamma radiation and particle size on antioxidant properties of maize (Zea mays L.) flour was studied using response surface methodology. A central composite design based on three levels of each of particle size, in terms of mesh number (40, 60 and 80 meshes), and gamma radiation dose (25, 50 and 75 kGy) was constructed. A statistically significant dose-dependent decrease (p&lt;0.05) in antioxidant properties of gamma irradiated flour was observed. However, an increase in the mesh number (decrease in particle size of flour) resulted in an increase in antioxidant properties. The optimum level of radiation dose to achieve maximum value of responses was found to be 50 kGy for Trolox equivalent total antioxidant activity (TETAOA), 25 kGy for iron chelating ability (ICA), 25 kGy for reducing power (RP) and 75 kGy for linoleic acid reduction capacity (LARC). However, the optimum level of mesh number to achieve desired levels of TETAOA, ICA, RP and LARC was found to be 80 meshes.
DOI: 10.6084/m9.figshare.20039088.v1
title: Influence of high-dose gamma radiation and particle size on antioxidant properties of Maize ( Zea mays L.) flour

description: ABSTRACT Influence of high-dose gamma radiation and particle size on antioxidant properties of maize (Zea mays L.) flour was studied using response surface methodology. A central composite design based on three levels of each of particle size, in terms of mesh number (40, 60 and 80 meshes), and gamma radiation dose (25, 50 and 75 kGy) was constructed. A statistically significant dose-dependent decrease (p&lt;0.05) in antioxidant properties of gamma irradiated flour was observed. However, an increase in the mesh number (decrease in particle size of flour) resulted in an increase in antioxidant properties. The optimum level of radiation dose to achieve maximum value of responses was found to be 50 kGy for Trolox equivalent total antioxidant activity (TETAOA), 25 kGy for iron chelating ability (ICA), 25 kGy for reducing power (RP) and 75 kGy for linoleic acid reduction capacity (LARC). However, the optimum level of mesh number to achieve desired levels of TETAOA, ICA, RP and LARC was found to be 80 meshes.
DOI: 10.6084/m9.figshare.20039090
title: Internal consistency and interrater reliability of the Brazilian version of Martín-Bayarre-Grau (MBG) adherence scale

description: ABSTRACT This paper aims to analyze the measurement equivalence aspects (internal consistency and interrater reliability) of a Brazilian version of Martín-Bayarre-Grau (MBG) adherence questionnaire as part of its cross-cultural adaptation. Item-total correlation and Cronbach's alpha coefficients were used as internal consistency estimates. Stability was evaluated through test and retest comparison and expressed through intraclass correlation coefficient (ICC) and kappa with quadratic weighting. ICC for the overall scale was 0.81, indicating an "almost perfect" agreement. However, some cases of "poor" and "slight" agreements were found while analyzing individual items. The translated version of the MBG questionnaire showed good homogeneity (alpha 0.78), higher than cutoff points suggested in the literature. The scale has proved capable of measuring the level of adherence to treatment in hypertensive and/or diabetic patients in a reliable way.
DOI: 10.6084/m9.figshare.20039090.v1
title: Internal consistency and interrater reliability of the Brazilian version of Martín-Bayarre-Grau (MBG) adherence scale

description: ABSTRACT This paper aims to analyze the measurement equivalence aspects (internal consistency and interrater reliability) of a Brazilian version of Martín-Bayarre-Grau (MBG) adherence questionnaire as part of its cross-cultural adaptation. Item-total correlation and Cronbach's alpha coefficients were used as internal consistency estimates. Stability was evaluated through test and retest comparison and expressed through intraclass correlation coefficient (ICC) and kappa with quadratic weighting. ICC for the overall scale was 0.81, indicating an "almost perfect" agreement. However, some cases of "poor" and "slight" agreements were found while analyzing individual items. The translated version of the MBG questionnaire showed good homogeneity (alpha 0.78), higher than cutoff points suggested in the literature. The scale has proved capable of measuring the level of adherence to treatment in hypertensive and/or diabetic patients in a reliable way.
DOI: 10.6084/m9.figshare.20039091
title: Unsatisfactory glycemic control in type 2 Diabetes mellitus patients: predictive factors and negative clinical outcomes with the use of antidiabetic drugs

description: ABSTRACT Many factors can interfere with glycemic control in patients with type 2 diabetes mellitus and this patient group has an increased risk of experiencing drug-related negative outcomes (DNO). The aim of this study was to identify the predictive factors of unsatisfactory glycemic control and DNO in this group of patients. A cross-sectional study was conducted collecting data from prescriptions and interviews with 100 patients of the Endocrinology Clinic of the Hospital Complex of Sorocaba, São Paulo, Brazil. Variables associated with unsatisfactory glycemic control were determined and the DNO associated with antidiabetic drugs identified. Age (&lt;65 years) (OR=4.09), family history of diabetes (OR=3.24), use of combined therapy to treat diabetes (2-4 antidiabetic drugs) (OR=5.13) and presence of DNO (OR=5.92) were found to be predictive factors for poor patient glycemic control. DNO were observed in 49% of the patients and were caused predominantly by ineffectiveness in patients with poor glycemic control (p&lt;0.05). There was no significant difference between groups (satisfactory and unsatisfactory glycemic control) for DNO caused by safety issues (p&gt;0.05). Characterization of the profile of patients with uncontrolled diabetes and of aspects associated with drug treatment can contribute to the planning of interventions to improve patient care.
DOI: 10.6084/m9.figshare.20039091.v1
title: Unsatisfactory glycemic control in type 2 Diabetes mellitus patients: predictive factors and negative clinical outcomes with the use of antidiabetic drugs

description: ABSTRACT Many factors can interfere with glycemic control in patients with type 2 diabetes mellitus and this patient group has an increased risk of experiencing drug-related negative outcomes (DNO). The aim of this study was to identify the predictive factors of unsatisfactory glycemic control and DNO in this group of patients. A cross-sectional study was conducted collecting data from prescriptions and interviews with 100 patients of the Endocrinology Clinic of the Hospital Complex of Sorocaba, São Paulo, Brazil. Variables associated with unsatisfactory glycemic control were determined and the DNO associated with antidiabetic drugs identified. Age (&lt;65 years) (OR=4.09), family history of diabetes (OR=3.24), use of combined therapy to treat diabetes (2-4 antidiabetic drugs) (OR=5.13) and presence of DNO (OR=5.92) were found to be predictive factors for poor patient glycemic control. DNO were observed in 49% of the patients and were caused predominantly by ineffectiveness in patients with poor glycemic control (p&lt;0.05). There was no significant difference between groups (satisfactory and unsatisfactory glycemic control) for DNO caused by safety issues (p&gt;0.05). Characterization of the profile of patients with uncontrolled diabetes and of aspects associated with drug treatment can contribute to the planning of interventions to improve patient care.
DOI: 10.6084/m9.figshare.20039093
title: Simvastatin treatment reduces the cholesterol content of membrane/lipid rafts, implicating the N -methyl-D-aspartate receptor in anxiety: a literature review

description: ABSTRACT Membrane/lipid rafts (MLRs) are plasmalemmal microdomains that are essential for neuronal signaling and synaptic development/stabilization. Inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme-A reductase (statins) can disable the N-methyl-D-aspartate (NMDA) receptor through disruption of MLRs and, in turn, decrease NMDA-mediated anxiety. This hypothesis will contribute to understanding the critical roles of simvastatin in treating anxiety via the NMDA receptor.
DOI: 10.6084/m9.figshare.20039093.v1
title: Simvastatin treatment reduces the cholesterol content of membrane/lipid rafts, implicating the N -methyl-D-aspartate receptor in anxiety: a literature review

description: ABSTRACT Membrane/lipid rafts (MLRs) are plasmalemmal microdomains that are essential for neuronal signaling and synaptic development/stabilization. Inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme-A reductase (statins) can disable the N-methyl-D-aspartate (NMDA) receptor through disruption of MLRs and, in turn, decrease NMDA-mediated anxiety. This hypothesis will contribute to understanding the critical roles of simvastatin in treating anxiety via the NMDA receptor.