cometadata/datacite-titles-descriptions-related-identifiers huggingface dataset:
DOI: 10.6084/m9.figshare.20039112.v1
title: Floating ability and drug release evaluation of gastroretentive microparticles system containing metronidazole obtained by spray drying

description: Abstract Gastroretentive floating microparticles were developed and evaluated for the controlled metronidazole delivery for treatment of gastric disease. Floating microparticles, varying in proportions of chitosan and hydroxypropyl methylcellulose or ethylcellulose, were obtained by spray drying. Floating microparticles were characterized by physicochemical and in vitro studies, according to their floating ability and drug delivery. Microparticles presented mean diameter from 1.05 to 2.20 µm. The infrared spectroscopy confirmed the drug encapsulation and showed no chemical linkage between microparticles components. X-ray diffraction showed changes in the drug`s solid state, from crystalline to amorphous, indicating partial drug encapsulation, due to the presence of some crystalline peaks of metronidazole in microparticles. All microparticles floated immediately in contact of simulated gastric fluid and both floating and drug release profiles were dependent of microparticles composition. Microparticles samples constituted by chitosan and hydroxypropyl methylcellulose revealed the best relationship between floating duration and drug release, remaining floating during the occurrence of the drug release, ideal condition for the floating gastroretentive systems.
DOI: 10.6084/m9.figshare.20039114.v1
title: Synthesis and evaluation of platinum complexes with potential antitumor activity

description: Abstract A novel series of platinum (II) complexes was synthesized and the complexes were evaluated for their in vitro cytotoxicity against four human cancer cells lines. Five platinum complexes showed activity against at least one tumor cell line. Complexes 3 and 6 were promising, being active, at micromolar concentrations, against all the assayed tumor cell lines. Compound 3 was selected for further studies in mice with Ehrlich solid tumors and it was able to reduce the rate of tumor growth significantly during the first seven days. However, at the end of the experiments, there was no significant difference between the group of animals treated with 3 and the control group. The low solubility of the compound in the assay conditions can explain, at least in part, these results.
DOI: 10.6084/m9.figshare.20039114
title: Synthesis and evaluation of platinum complexes with potential antitumor activity

description: Abstract A novel series of platinum (II) complexes was synthesized and the complexes were evaluated for their in vitro cytotoxicity against four human cancer cells lines. Five platinum complexes showed activity against at least one tumor cell line. Complexes 3 and 6 were promising, being active, at micromolar concentrations, against all the assayed tumor cell lines. Compound 3 was selected for further studies in mice with Ehrlich solid tumors and it was able to reduce the rate of tumor growth significantly during the first seven days. However, at the end of the experiments, there was no significant difference between the group of animals treated with 3 and the control group. The low solubility of the compound in the assay conditions can explain, at least in part, these results.
DOI: 10.6084/m9.figshare.20039115
title: 1,3,4-Thiadiazole and 1,2,4-triazole-3(4 H )-thione bearing salicylate moiety: synthesis and evaluation as anti- Candida albicans

description: Abstract Dramatically increased occurrence of both superficial and invasive fungal infections has been observed. Candida albicans appear to be the main etiological agent of invasive fungal infections. The anti-C. albicans activity of thiosemicarbazide, 1,3,4-Thiadiazole, and 1,2,4-triazole-3(4H)-thione compounds (compounds 3-23) were investigated. The MIC values of thiadiazole and triazole derivatives 10-23 were in the range of 0.08-0.17 µmol mL-1, while that of fluconazole was 0.052 µmol mL-1. Compound 11 (5-(2-(4-chlorobenzyloxy)phenyl)-N-allyl-1,3,4-thiadiazol-2-amine) and compound 18 (5-(2-(4-chlorobenzyloxy)phenyl)-4-allyl-2H-1,2,4-triazole-3(4H)-thione) were found to be the most active compounds, with MIC values of 0.08 µmol mL-1. The newly synthesized thiadiazole and triazole compounds (compounds 10-23) showed promising anti-Candida activity. The allyl substituent-bearing compounds 11 and 18 exhibited significant anti-Candida albicans activity and showed a binding mode as well as the fluconazole x-ray structure.
DOI: 10.6084/m9.figshare.20039115.v1
title: 1,3,4-Thiadiazole and 1,2,4-triazole-3(4 H )-thione bearing salicylate moiety: synthesis and evaluation as anti- Candida albicans

description: Abstract Dramatically increased occurrence of both superficial and invasive fungal infections has been observed. Candida albicans appear to be the main etiological agent of invasive fungal infections. The anti-C. albicans activity of thiosemicarbazide, 1,3,4-Thiadiazole, and 1,2,4-triazole-3(4H)-thione compounds (compounds 3-23) were investigated. The MIC values of thiadiazole and triazole derivatives 10-23 were in the range of 0.08-0.17 µmol mL-1, while that of fluconazole was 0.052 µmol mL-1. Compound 11 (5-(2-(4-chlorobenzyloxy)phenyl)-N-allyl-1,3,4-thiadiazol-2-amine) and compound 18 (5-(2-(4-chlorobenzyloxy)phenyl)-4-allyl-2H-1,2,4-triazole-3(4H)-thione) were found to be the most active compounds, with MIC values of 0.08 µmol mL-1. The newly synthesized thiadiazole and triazole compounds (compounds 10-23) showed promising anti-Candida activity. The allyl substituent-bearing compounds 11 and 18 exhibited significant anti-Candida albicans activity and showed a binding mode as well as the fluconazole x-ray structure.
DOI: 10.6084/m9.figshare.20039117.v1
title: Quality indicators of pharmacists' services in community pharmacies in Paraná State, Brazil

description: ABSTRACT Pharmacists and their pharmacies have been evolving in their roles as health promoters in Brazil. Some examples are the recent legislation reaffirming the role of Brazilian pharmacies as health institutions, rather than having only a commercial profile, giving greater clarity to pharmacists about their roles as health care providers. This evolution came with the recognition that is already seen in other developed countries, confirming the need for the pharmacist as a health promoter, and not simply a dispenser of drugs in society. This study has obtained the profile and activities of community pharmacists, as well as the quality indicators of private community pharmacies throughout the State of Paraná through the application of an online survey sent to pharmacists in the state. Out of all pharmacists surveyed, 533 were part of the final analysis, being the pharmacists to complete the survey in full. Participants were mostly female (69.4%) and were, on average, 35.2 ± 9.2 years old. Of these, 60% worked in pharmacy chains and just 37% of all pharmacist respondents were issuing the Declaration of Pharmaceutical Services. The current study showed that many pharmaceutical services are not adopted by pharmacies as these services bring no significant financial reward. Regarding the structure, the Paraná State showed that pharmacies present a good overall structure. The kind of pharmacy (chain or independent) influenced the pharmaceutical services provided and the available structure, where the independent pharmacies provide a wider range of services and have better structure. This study was able to identify the profile and behaviors of pharmacists and also the quality indicators of pharmacies in Paraná State.
DOI: 10.6084/m9.figshare.20039117
title: Quality indicators of pharmacists' services in community pharmacies in Paraná State, Brazil

description: ABSTRACT Pharmacists and their pharmacies have been evolving in their roles as health promoters in Brazil. Some examples are the recent legislation reaffirming the role of Brazilian pharmacies as health institutions, rather than having only a commercial profile, giving greater clarity to pharmacists about their roles as health care providers. This evolution came with the recognition that is already seen in other developed countries, confirming the need for the pharmacist as a health promoter, and not simply a dispenser of drugs in society. This study has obtained the profile and activities of community pharmacists, as well as the quality indicators of private community pharmacies throughout the State of Paraná through the application of an online survey sent to pharmacists in the state. Out of all pharmacists surveyed, 533 were part of the final analysis, being the pharmacists to complete the survey in full. Participants were mostly female (69.4%) and were, on average, 35.2 ± 9.2 years old. Of these, 60% worked in pharmacy chains and just 37% of all pharmacist respondents were issuing the Declaration of Pharmaceutical Services. The current study showed that many pharmaceutical services are not adopted by pharmacies as these services bring no significant financial reward. Regarding the structure, the Paraná State showed that pharmacies present a good overall structure. The kind of pharmacy (chain or independent) influenced the pharmaceutical services provided and the available structure, where the independent pharmacies provide a wider range of services and have better structure. This study was able to identify the profile and behaviors of pharmacists and also the quality indicators of pharmacies in Paraná State.
DOI: 10.6084/m9.figshare.20039121
title: Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

description: ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids.
DOI: 10.6084/m9.figshare.20039121.v1
title: Gastroprotective activity of the hydroethanolic extract and ethyl acetate fraction from Kalanchoe pinnata (Lam.) Pers.

description: ABSTRACT Peptic ulcers are an important pathology, and the search for safer and more effective treatment methods is of paramount importance. In this study, we assess the gastroprotective effects of the hydroethanolic extract (HE) and ethyl acetate fraction (EAF) from Kalanchoe pinnata leaves against an ethanol/HCl-induced ulcer model in rats. The HE reduced gastric lesions by approximately 47% (400 mg/kg). A significant inhibition of the gastric lesions by 50% was observed after pretreatment with the EAF (200 mg/kg). Quercetrin and quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside were isolated and identified in the flavonoid fraction (EAF) by HPLC and NMR analyses because this fraction showed the highest gastroprotective effect. This fraction demonstrated high antioxidant activities (CE50=41.91 µg/mL) by DPPH in comparison with Trolox(r) and 11.33 mmol Trolox(r) equivalent by ORAC. In conclusion, the HE and FAE from K. pinnata displayed gastroprotective activity in rats, most likely due to the presence of flavonoids.
DOI: 10.6084/m9.figshare.20039120
title: Purchase of prescription and OTC medicines in Slovakia: factors influencing patients' expectations and satisfaction

description: ABSTRACT Slovakia is a country where the purchase of OTC (over the counter) medicines outside the pharmacy is not allowed by the government. This study aimed at evaluating patients' satisfaction and acceptance of community pharmacists. Customer's behaviour and expectations influencing the purchase of prescription and OTC medicines were analyzed. A structured questionnaire having 15 multiple-choice questions was used to analyze the descriptive parameters. Data collection lasted from January to February 2014. The sample size consisted of 357 high-school educated individuals under 40 years of age. The survey showed that the prescription and OTC medicines were bought equally. The participants reported a 96.0%, 96.3% and 90.2% satisfaction rate with willingness and approach of the community pharmacist, pharmacy services and provision of drug information respectively. As for the OTC medicines, 89.5% people considered the pharmacist an expert: 88.2% purchased medicines with pharmacist's recommendation, 97.8% needed a professional counselling and 97.2% required a pharmacist's guidance. As for the prescription drugs, only 72.1% considered the pharmacist an expert: 96.3% suggested that physician's prescription was significant and 88.3% considered pharmacist's guidance in the process of selection of prescription medicines nonessential. A comprehensible and respectable conversation was highly expected in regards to both the OTC and prescription medicines.
DOI: 10.6084/m9.figshare.20039120.v1
title: Purchase of prescription and OTC medicines in Slovakia: factors influencing patients' expectations and satisfaction

description: ABSTRACT Slovakia is a country where the purchase of OTC (over the counter) medicines outside the pharmacy is not allowed by the government. This study aimed at evaluating patients' satisfaction and acceptance of community pharmacists. Customer's behaviour and expectations influencing the purchase of prescription and OTC medicines were analyzed. A structured questionnaire having 15 multiple-choice questions was used to analyze the descriptive parameters. Data collection lasted from January to February 2014. The sample size consisted of 357 high-school educated individuals under 40 years of age. The survey showed that the prescription and OTC medicines were bought equally. The participants reported a 96.0%, 96.3% and 90.2% satisfaction rate with willingness and approach of the community pharmacist, pharmacy services and provision of drug information respectively. As for the OTC medicines, 89.5% people considered the pharmacist an expert: 88.2% purchased medicines with pharmacist's recommendation, 97.8% needed a professional counselling and 97.2% required a pharmacist's guidance. As for the prescription drugs, only 72.1% considered the pharmacist an expert: 96.3% suggested that physician's prescription was significant and 88.3% considered pharmacist's guidance in the process of selection of prescription medicines nonessential. A comprehensible and respectable conversation was highly expected in regards to both the OTC and prescription medicines.
DOI: 10.6084/m9.figshare.20039123
title: Changes in weight and body fat after use of tetracycline and Lactobacillus gasseri in rats

description: ABSTRACT Recent studies have shown a role of intestinal microbiota in obesity. The consumption of antibiotics in the last 70 years has led to changes in intestinal microbiota, which has led to weight gain and body fat accumulation. To evaluate the possibility of weight gain induced by antibiotics and the possible protective effect of probiotics, we divided 45 animals (Rattus norvegicus) into groups and administered the following treatments over two weeks: tetracycline, tetracycline + Lactobacillus gasseri, and NaCl. The animals were weighed over the course of 8 weeks, and at the end of the treatment period, they were measured and subjected to bioelectrical impedance analysis. The results show that the group receiving tetracycline alone had a higher body mass index (p=0.030), a greater Lee index (p=0.008), and a lower body water percentage than the control group, indicating a greater accumulation of body fat. The group receiving the probiotics with tetracycline presented similar results to the control group, indicating a possible protective effect of body fat accumulation in the group receiving tetracycline alone. The results show that tetracycline increased the concentration of body fat, and the use of probiotics was associated with an ability to protect the animals from the pro-obesity effect.
DOI: 10.6084/m9.figshare.20039123.v1
title: Changes in weight and body fat after use of tetracycline and Lactobacillus gasseri in rats

description: ABSTRACT Recent studies have shown a role of intestinal microbiota in obesity. The consumption of antibiotics in the last 70 years has led to changes in intestinal microbiota, which has led to weight gain and body fat accumulation. To evaluate the possibility of weight gain induced by antibiotics and the possible protective effect of probiotics, we divided 45 animals (Rattus norvegicus) into groups and administered the following treatments over two weeks: tetracycline, tetracycline + Lactobacillus gasseri, and NaCl. The animals were weighed over the course of 8 weeks, and at the end of the treatment period, they were measured and subjected to bioelectrical impedance analysis. The results show that the group receiving tetracycline alone had a higher body mass index (p=0.030), a greater Lee index (p=0.008), and a lower body water percentage than the control group, indicating a greater accumulation of body fat. The group receiving the probiotics with tetracycline presented similar results to the control group, indicating a possible protective effect of body fat accumulation in the group receiving tetracycline alone. The results show that tetracycline increased the concentration of body fat, and the use of probiotics was associated with an ability to protect the animals from the pro-obesity effect.
DOI: 10.6084/m9.figshare.20039126
title: Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides

description: ABSTRACT We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity.
DOI: 10.6084/m9.figshare.20039126.v1
title: Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides

description: ABSTRACT We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity.
DOI: 10.6084/m9.figshare.20039127.v1
title: Continuous wavelet transform methods for the simultaneous determinations and dissolution profiles of valsartan and hydrochlorothiazide in tablets

description: ABSTRACT Continuous wavelet transform (CWT) was proposed for the simultaneous determination and dissolution profiles of valsartan (VAL) and hydrochlorothiazide (HCT) in tablets, without the use of a chemical separation procedure. The CWT approach was applied to the original UV spectra and their ratio spectra in the optimal wavelength ranges. After testing several wavelet families, Mexican hat function-CWT and Daubechies7-CWT (mexh-CWT and db7-CWT, respectively) were found to be suitable for the transformation of the original UV spectra. In the following procedure, mexh-CWT and Coiflets3-CWT (coif3-CWT) were found to be appropriate for the signal analysis of ratio spectra (RS) of VAL/HCT and HCT/VAL. Calibration graphs for VAL and HCT were obtained by measuring db7-CWT and mexh-CWT amplitudes in the transformation of the original absorption spectra and RS-coif-CWT and RS-mexh-CWT amplitudes in the transformation of the ratio spectra. The validity and applicability of the proposed CWT methods were evaluated through the analysis of an independent set of synthetic binary mixtures consisting of VAL and HCT. The proposed signal processing methods were then successfully applied to the simultaneous quantitative evaluation and simultaneous dissolution profiles of the related drugs in commercial tablets, with good agreement reported for the experimental results.
DOI: 10.6084/m9.figshare.20039127
title: Continuous wavelet transform methods for the simultaneous determinations and dissolution profiles of valsartan and hydrochlorothiazide in tablets

description: ABSTRACT Continuous wavelet transform (CWT) was proposed for the simultaneous determination and dissolution profiles of valsartan (VAL) and hydrochlorothiazide (HCT) in tablets, without the use of a chemical separation procedure. The CWT approach was applied to the original UV spectra and their ratio spectra in the optimal wavelength ranges. After testing several wavelet families, Mexican hat function-CWT and Daubechies7-CWT (mexh-CWT and db7-CWT, respectively) were found to be suitable for the transformation of the original UV spectra. In the following procedure, mexh-CWT and Coiflets3-CWT (coif3-CWT) were found to be appropriate for the signal analysis of ratio spectra (RS) of VAL/HCT and HCT/VAL. Calibration graphs for VAL and HCT were obtained by measuring db7-CWT and mexh-CWT amplitudes in the transformation of the original absorption spectra and RS-coif-CWT and RS-mexh-CWT amplitudes in the transformation of the ratio spectra. The validity and applicability of the proposed CWT methods were evaluated through the analysis of an independent set of synthetic binary mixtures consisting of VAL and HCT. The proposed signal processing methods were then successfully applied to the simultaneous quantitative evaluation and simultaneous dissolution profiles of the related drugs in commercial tablets, with good agreement reported for the experimental results.