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4.
Chemosphere ; 238: 124658, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31548174

RESUMO

Adsorption is a common process used to remove pharmaceuticals, personal care products and endocrine disrupting chemicals (PPCPs/EDCs) from water. However, as PPCPs/EDCs cover a wide range of molecules and chemical structures, prediction of the adsorption capacity is very challenging. In this study, a novel model was developed to predict adsorption isotherms of PPCPs/EDCs onto various types of adsorbents using a combination of Polanyi potential theory, molecular connectivity indices (MCIs) and molecular characteristics. Polanyi theory provided the basic mathematical form for the correlation. MCIs, hydrophobicity and H-bond count were used to normalize the Polanyi equation based on the molecular structure and interactions among the chemicals, the adsorbents, and the solution. In total, adsorption data were collected from 158 reports for 55 PPCPs/EDCs onto 306 different adsorbent materials. The correlation was first trained with 46 PPCPs/EDCs adsorbed onto 162 carbonaceous adsorbents (CAs), with 44.8% SDEV. Then the model was employed to predict 46 PPCPs/EDCs onto 118 other CAs and 9 new PPCPs/EDCs onto 23 CAs in ultrapure water, with error from 42 to 48% SDEV. When applying to non-carbonaceous adsorbents, the models can still predict the adsorption of PPCPs/EDCs with 90.09% SDEV. For the first time, a model, the PD - MCI - hydrophobic - H bond model, was developed to predict adsorption of a wide group of complicated PPCPs/EDCs onto a big variety of carbonaceous and non-carbonaceous adsorbents. The proposed model approach may provide a simple means for predicting adsorption capacities of PPCPs/EDCs onto various adsorbents.


Assuntos
Cosméticos/isolamento & purificação , Disruptores Endócrinos/isolamento & purificação , Preparações Farmacêuticas/isolamento & purificação , Poluentes Químicos da Água/isolamento & purificação , Purificação da Água/métodos , Adsorção , Disruptores Endócrinos/análise , Interações Hidrofóbicas e Hidrofílicas , Água/química , Poluentes Químicos da Água/análise
5.
Chemosphere ; 238: 124689, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31524624

RESUMO

Pharmaceutical effluents released from industries are accountable to deteriorate the aquatic and soil environment through indirect toxic effects. Microbes are adequately been used to biodegrade pharmaceutical industry wastewater and present study was envisaged to determine biodegradation of pharmaceutical effluent by Micrococcus yunnanensis. The strain showed 42.82% COD (Chemical oxygen demand) reduction before optimization. After applying Taguchi's L8 array as an optimization technique, the biodegradation rate was enhanced by 82.95% at optimum conditions (dextrose- 0.15%, peptone 0.1%, inoculum size 4% (wv-1), rpm 200, pH 8 at 25 °C) within 6 h. The confirmation of pharmaceuticals degradation was done by 1H NMR (Nuclear magnetic resonance) studies followed by elucidation of transformation pathways of probable drugs in the effluent through Q-Tof-MS (Quadrupole Time of Flight- Mass Spectrometry). The cytotoxicity evaluation of treated and untreated wastewater was analyzed on Human Embryonic Kidney (HEK 293) cells using Alamar Blue assay, which showed significant variance.


Assuntos
Biodegradação Ambiental , Resíduos Industriais/análise , Micrococcus/metabolismo , Preparações Farmacêuticas/análise , Águas Residuárias/química , Poluentes Químicos da Água/análise , Análise da Demanda Biológica de Oxigênio , Linhagem Celular , Indústria Farmacêutica , Células HEK293 , Humanos
6.
Chemosphere ; 240: 124949, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31568949

RESUMO

Pharmaceutically active compounds are of great concern due to their detection frequency in the environment and the unexpected risks. In this study, the simultaneous removal of mixed pharmaceuticals by microalgae was explored using a typical freshwater diatom Navicula sp. Results showed that Navicula sp. could efficiently remove atenolol, carbamazepine, ibuprofen and naproxen with the efficiencies of >90% after 21 d of exposure. As compared to the removal efficiencies of each pharmaceutical in the individual pharmaceutical treatments, the degradation of sulfamethoxazole, bezafibrate, and naproxen was improved in the mixed treatment, whereas the removal efficiencies of carbamazepine and atenolol decreased. Additionally, the presence of hydrophobic pharmaceuticals (i.e., ibuprofen and naproxen) accelerated the degradation of carbamazepine and sulfamethoxazole and inhibited the removal of atenolol in the mixture with the combination of six pharmaceuticals, while the addition of other pharmaceuticals show no significant effect on the removal of ibuprofen and naproxen. The bioaccumulation of pharmaceuticals in Navicula sp. increased as their log KOW values decreased. Four bezafibrate metabolites were identified and the degradation pathways of bezafibrate in diatom were proposed. It is the first report on the metabolism of BEZ in diatom, and further studies on the environmental risk of the metabolites should be investigated.


Assuntos
Bezafibrato/análise , Biodegradação Ambiental , Diatomáceas/metabolismo , Preparações Farmacêuticas/análise , Preparações Farmacêuticas/metabolismo , Poluentes Químicos da Água/análise , Atenolol/análise , Carbamazepina/análise , Água Doce/química , Ibuprofeno/análise , Inativação Metabólica , Naproxeno/análise , Sulfametoxazol/análise
7.
J Environ Manage ; 254: 109752, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31733478

RESUMO

Awareness about the rising detection and reported (eco)toxicological effects of contaminants of emerging concern (CECs, e.g. pharmaceuticals and personal care products - PPCPs - and modern pesticides) in the aquatic environment is growing. CECs are increasingly reported in the African aquatic environment, although the amount of data available is still limited. In this work, a comprehensive review is presented on the occurrence of CECs in wastewater, sludge, surface water, sediment, groundwater and drinking water of Africa. Further attention is given to the performance of wastewater stabilization ponds (WSPs) and trickling filters (TF) with respect to CECs removal. For the first time, we also look at the state of knowledge on the performance of point-of-use technologies (POUs) regarding the removal of CECs in drinking water. Generally, CECs in Africa occur at the same order of magnitude as in the Western world. However, for particular groups of compounds and at specific locations such as informal settlements, clearly higher concentrations are reported in Africa. Whereas antiretroviral and antimalarial drugs are rarely detected in the Western world, occurrence patterns in Africa reveal concentrations up to >100 µg L-1. Removal efficiencies of WSPs and TFs focus mainly on PPCPs and vary significantly, ranging from no removal (e.g. carbamazepine) to better than 99.9% (e.g. paracetamol). Despite the rising adoption of POUs, limited but promising information is available on their performance regarding CECs treatment in drinking water, particularly for the low-cost devices (e.g. ceramic filters and solar disinfection - SODIS) being adopted in Africa and other developing countries.


Assuntos
Praguicidas , Preparações Farmacêuticas , Poluentes Químicos da Água , África , Monitoramento Ambiental , Águas Residuárias
8.
J Environ Manage ; 254: 109800, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31739091

RESUMO

Treatment of highly polluted pharmaceutical effluents is a major challenge all over the world for technical and economic considerations. In this study, scientometric study is performed on the application of various methods for the treatment of pharmaceutical effluents to explore further developments. In this regard, a total of 1964 documents were retrieved from the Web of Science (WoS) database using a set of relevant keywords to cover all published documents. The extracted documents were subjected to scientometric study including the contributed authors, publications, citations received, contributing countries and institutions as well as the subject categories. From the data retrieved, the status of scientific knowledge on the subject history and current trends were identified and scientific gaps were critically discussed. Publications in this area started to appear since the sixties and were considerably promoted around the beginning of 2000s. Scientific publications of years 1960-2018 followed sigmoidal trend. It was found that leading countries are China and the United States in terms of scientific output on treatment technologies for pharmaceutical effluents. Among the active journals published, "Water Research" has received the most citations. A detailed discussion on the science and developments in this field is provided including the potential applications of scientometry.


Assuntos
Bibliometria , Preparações Farmacêuticas , China , Bases de Dados Factuais , Tecnologia , Estados Unidos
9.
J Environ Manage ; 254: 109794, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31780268

RESUMO

Pharmaceuticals are a subset of micropollutants, present in the environment in trace concentrations. Because of their persistent nature, these chemicals are of particular concern. Little is known about how mixtures of pharmaceutical residues, found in WWTP effluents, affect the environment or public health. Yet, numerous studies show negative outcomes for both aquatic and terrestrial organisms, suggesting that they are given both to bioaccumulation and uptake in plants. Israel leads the world in effluent reuse (86%), almost exclusively utilized for purposes of agricultural irrigation. Pharmaceuticals, however, are not included in Israel's water regulatory oversight or management, essentially creating an epidemiological experiment among its citizens and environment. Globally, these compounds also are not commonly subject to monitoring or regulation. This study reviews and analyzes water policies and regulation worldwide that address the presence of pharmaceuticals in water resources, with a particular focus on Australia, Singapore, Switzerland, and the USA. Furthermore, the study investigates the reasons why these chemicals are not yet regulated in Israel. Based on a comprehensive evaluation of the data and analysis of the regulatory rationale in other countries, a list of recommended pharmaceutical standards that should be measured and monitored in Israel's wastewater treatment system is proposed. The suggested prioritization criteria should be at the heart of a new regulatory agenda for controlling pharmaceutical contamination in wastewater.


Assuntos
Preparações Farmacêuticas , Poluentes Químicos da Água , Austrália , Monitoramento Ambiental , Israel , Singapura , Suíça , Eliminação de Resíduos Líquidos , Águas Residuárias
10.
Huan Jing Ke Xue ; 41(1): 194-204, 2020 Jan 08.
Artigo em Chinês | MEDLINE | ID: mdl-31854920

RESUMO

At present, research findings on pharmaceuticals and personal care products (PPCPs) in coastal areas are still unclear, and there is a need to develop a method to detect more PPCPs simultaneously in seawater. In this study, nine compounds of non-steroidal anti-inflammatory drugs, antibiotics, lipid regulators. and stimulants were selected as analytes. Solid phase extraction (SPE) was used to extract the compounds, which were then analyzed by high-performance liquid chromatography coupled to mass spectrometry (HPLC-MS). The optimum experimental conditions, such as the filler, eluent, pH, flow rate, and the reduction of matrix effect were optimized during the SPE. The results showed that the best extraction column was CNW HLB, the best eluent was methanol:acetonitrile (1:1, volume ratio), the best eluent volume was 6 mL, the best pH was 7, the best flow rate was 5 mL·min-1, the amount of EDTA-Na2 added was 1 g, and the best concentration multiple was 500. The linear regression equations of all PPCPs had good linearity. Correlation coefficients were>0.999, recovery rates were between 82%-106%, relative standard deviations were between 1.6%-14%, and detection limits were between 0.01-2 ng·L-1, thus satisfying the requirement of trace analysis in seawater. Distribution characteristics and sources of PPCPs were studied in the Yellow Sea and the East China Sea during summer 2018. All nine PPCPs were detected and the main pollutants were NAP, IBU, GEM, CAF, and ASA. High concentrations of PPCPs were generally detected in the nearshore area and displayed conspicuous decreasing tendencies from the inshore towards the offshore. The concentrations of PPCPs in the Yellow Sea were higher than of those in the East China Sea, and this was related to there being more sources of pollutions and poor water exchange capacity in the Yellow Sea. Principal component analysis showed that the main source of PPCPs was terrestrial input. The environmental risk assessment of PPCPs indicated that risk quotients (RQs) of IBU and NAP (0.1-1) posed a medium risk to the aquatic environment, while others posed low risk to organisms.


Assuntos
Cosméticos/análise , Monitoramento Ambiental , Preparações Farmacêuticas/análise , Poluentes Químicos da Água/análise , China , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas , Oceanos e Mares , Medição de Risco , Extração em Fase Sólida
11.
Huan Jing Ke Xue ; 41(1): 313-320, 2020 Jan 08.
Artigo em Chinês | MEDLINE | ID: mdl-31854932

RESUMO

Wastewater treatment plants hold a vast pool of antibiotic resistant bacteria (ARB) and antibiotic resistance genes (ARGs). The aim of this study is to analyze the ARB and ARGs in a pharmaceutical and chemical wastewater treatment plant using a metagenomic technique. The results of taxonomic annotation revealed that bacteria were the predominant domain. The most abundant phyla and genus was Proteobacteria and Hyphomicrobium, respectively. A total of 74 categories of ARGs were predicted using CARD with the most dominant types being sav 1866, dfrE, and mfd. Furthermore, a network analysis was conducted to investigate the co-occurrence patterns between ARGs and microbial taxa. ARGs were found to be highly connected to microbial taxa at the genus level. With respect to the antibiotic resistance mechanisms, antibiotic-specific efflux pumps appeared to be the most common mechanisms. Among these, resistance-nodulation-cell division (RND) was the major type. The most important functional pathway of this microbial community was metabolic correlation. Interestingly, there were many genes related to human diseases, among which bacterial infectious diseases were the main ones. On the one hand, these data further confirmed that pharmaceutical and chemical wastewater treatment plants are rich in ARB and ARGs. The accumulation of ARGs increases the potential environmental risks, and hence it is necessary to strengthen the active monitoring of ARB and ARGs in pharmaceutical and chemical wastewater treatment plants. On the other hand, research on ARB and ARGs offers important information for the selection of deep processing technology to effectively remove ARB and ARGs.


Assuntos
Bactérias/classificação , Farmacorresistência Bacteriana , Genes Bacterianos , Águas Residuárias , Purificação da Água , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Humanos , Metagenoma , Preparações Farmacêuticas
12.
Med Oral Patol Oral Cir Bucal ; 25(1): e71-e83, 2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31880288

RESUMO

BACKGROUND: Medication-related osteonecrosis of the jaw (MRONJ) is a rare, but serious adverse effect of certain drugs, of which bisphosphonates are the most widely known. This pathology is also associated with other medications such as the biologic antiresorptive agent, denosumab and some antiangiogenics such as sunitinib, bevacizumab or aflibercept. Very recently, new medications have also been associated with osteonecrosis of the jaw (ONJ). The objectives were to update the list of medications associated with ONJ, to analyze the fundamental aspects of this list and to describe the level of evidence available. MATERIAL AND METHODS: A narrative bibliographic review was made, using the PubMed-MedLine, DOAJ and SCIELO databases. Additional information was obtained through the online Medication Information Centre of the Spanish Agency of Medicines and Medical Devices (AEMPS - CIMA), the websites of the US Food & Drugs Administration (Drugs@FDA) and the European Medicines Agency (EMA). RESULTS: The latest drugs identified as potential facilitators of this pathology include a number of anti-VEGF based antiangiogenic drugs and anti-TKI and different types of immunomodulators. Neither the level of evidence in this association nor the risk are equal for all these drugs. On the other hand, over the coming years, new drugs will be marketed with similar action mechanisms to those that are recognized as having this adverse effect. CONCLUSIONS: No effective therapy is currently known for the treatment of ONJ. Therefore, in order to prevent new cases of MRONJ, it is essential for all oral healthcare professionals to be fully up-to-date with the etiopathogenic aspects of this pathology and to be aware of those drugs considered to be a risk.


Assuntos
Osteonecrose da Arcada Osseodentária Associada a Difosfonatos , Conservadores da Densidade Óssea , Osteonecrose , Preparações Farmacêuticas , Denosumab , Difosfonatos , Humanos
13.
Chemosphere ; 238: 124553, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31442776

RESUMO

Although, several recent greenhouse studies are beginning to address the uptake of pharmaceuticals and personal care products (PPCPs) by a variety of crops, few studies have assessed the effects of exposure to complex, realistic wastewater effluents on uptake. Hence, in this study, a greenhouse experiment was conducted in order to study the interactions occurring exclusively between PPCPs in soil, and in the edible plant part of beets (Beta vulgaris) after exposure to treated wastewater effluent. According to the findings, the interactions between the pharmaceuticals caffeine (CFN) with bisoprolol (BSP), carbamezapine (CMZ), clarithromycin (CMC), metoprolol (MPL), sulfamethoxazole (SMX), and trimethoprim (TMP) occurring in soil were almost 99% synergistic; it was noted variability in the interactive capacity of the pharmaceuticals; the concentrations of pharmaceuticals which measured did not affect unfavorably beet yield; interactions between the PPCPs via the PPCPs contribution in plant and soil affect the qualitative and quantitative characteristics of the beets.


Assuntos
Beta vulgaris/crescimento & desenvolvimento , Cosméticos/análise , Preparações Farmacêuticas/análise , Poluentes do Solo/análise , Solo/química , Águas Residuárias/química , Poluentes Químicos da Água/análise , Beta vulgaris/metabolismo , Cosméticos/metabolismo , Preparações Farmacêuticas/metabolismo , Poluentes do Solo/metabolismo , Poluentes Químicos da Água/metabolismo
14.
Zhongguo Zhong Yao Za Zhi ; 44(22): 4800-4805, 2019 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-31872585

RESUMO

Due to the increasing incidence of central nervous system diseases,especially the increasing incidence and mortality of stroke,brain-targeted drug delivery has attached more and more attention. Nasal administration,as one of the ways of brain-targeted administration,can effectively make the drug delivered to the brain in a targeted way after by passing the blood-brain barrier,providing a new idea for the treatment of central nervous system diseases. Therefore,it is a promising administration way. In recent years,the treatment of encephalopathy by nasal administration of traditional Chinese medicine has become a hot topic in the research of traditional Chinese medicine. Ischemic stroke is one of the most important diseases endangering human health. Nasal administration has a history of thousands of years in treatment of stroke. Modern medical research has proved that there is a subtle connection between the nasal cavity and the brain,and the complex and ingenious structure of the nasal cavity provides the possibility for drugs delivery to the brain through the nose. Drug administration through nasal cavity has obvious advantages in treatment of central nervous system diseases represented by ischemic stroke. Nasal administration is characterized by non-invasion,low infection,rapid absorption and brain targeting. The author will expound the theoretical basis of brain targeting of nasal administration from the aspects of anatomy and physiology,and summarize the transport pathway of drugs through the nose into the brain,the in vitro and in vivo experimental research basis of the " nose-brain"pathway,and the clinical nasal administration of traditional Chinese medicine to prevent cerebral ischemia. It provides a reference for better research of drugs to prevent and treat cerebral ischemia injury through the " nose-brain"pathway and lays a foundation for further research of the " nose-brain" pathway.


Assuntos
Isquemia Encefálica/tratamento farmacológico , Medicina Tradicional Chinesa , Preparações Farmacêuticas , Administração Intranasal , Encéfalo , Sistemas de Liberação de Medicamentos , Humanos , Mucosa Nasal
15.
Recurso na Internet em Português | LIS - Localizador de Informação em Saúde, LIS-bvsms | ID: lis-LISBR1.1-46906

RESUMO

A partir do próximo ano, o Governo do Brasil deve passar a oferecer um novo medicamento para tratar a tuberculose latente, aquela em que há a presença da bactéria adormecida, mas sem doença, ou seja, não há os sintomas como tosse prolongada e febre. A estimativa é de que há 30 mil pessoas nestas condições no país e que, caso contraiam doenças como o HIV/aids, quando o sistema imunológico está mais fragilizado, podem vir a desenvolver a forma ativa da tuberculose.


Assuntos
Tuberculose Latente , Brasil , Preparações Farmacêuticas/normas
16.
Hautarzt ; 70(12): 953-959, 2019 Dec.
Artigo em Alemão | MEDLINE | ID: mdl-31712975

RESUMO

Topical preparations are by far the most frequently used therapeutic or prophylactic pharmaceuticals by dermatologists. Although only a few new active ingredients in topical pharmaceuticals have reached the market in recent years, some innovative galenic concepts and strategies considering the intrinsic effect of topical preparations have been developed, and it is quite certain that we can count on more genuine innovations in the near future. In particular small molecules, but also biological drugs, can be expected to be delivered by topical preparations, especially for inflammatory diseases. Also, we await innovative strategies for the substitution or regulation of the physicochemical and microbiological barrier function of the skin, including completely new options relating to the application of ribonucleic acid derivatives or their inhibitors aiming at influencing gene expression. Overall, it can be stated that the potential of epicutaneous application will take shape in modern vehicle strategies and procedures that deploy the intrinsic effect of topical preparations and that progress in biotechnology and physical chemistry will become increasingly relevant in practice.


Assuntos
Administração Tópica , Preparações Farmacêuticas , Preparações Farmacêuticas/administração & dosagem , Pele
17.
Zhonghua Yi Xue Za Zhi ; 99(42): 3298-3302, 2019 Nov 12.
Artigo em Chinês | MEDLINE | ID: mdl-31715664

RESUMO

Objective: To study the improvement of lower urinary tract symptoms and related influencing factors in patients with prostate cancer complicated with lower urinary tract symptoms after drugs endocrine therapy. Methods: The clinical data of 80 patients with prostate cancer with lower urinary tract symptoms and receiving drug endocrine therapy in Guizhou Provincial People's Hospital from March 2015 to June 2019 were analyzed retrospectively. All patients were followed up, and the mode of administration of the endocrine therapy, the time of administration, and the international prostate symptom score (IPSS2) and quality of life score (QOL2) after treatment were recorded. The improvement of IPSS score and quality of life score after endocrine therapy was observed. The correlation between variance and age, the prostate volume, PSA, tumor stage, Gleason score, symptom severity, medication mode, and medication time were analyzed by variance, chi-square test and paired sample t test. Results: The differences of QOL and IPSS before and after therapy were statistically significant (P<0.05). Chi-square test found that the effective rate of drug endocrine therapy was not related to age (χ2=0.800; P=0.371), tumor stage (χ2=0.094; P=0.759), PSA (χ2=0.651; P=0.420), prostate volume (χ2=0.216; P=0.642), Gleason score (χ2=0.157; P=0.692), symptom severity (χ2=0.457; P=0.499), medication mode (χ2=2.910; P=0.233), and medication time (χ2=4.159; P=0.385). Analysis of variance found that prostate volume and the severity of symptoms was significantly associated with improvement in lower urinary tract symptoms. Conclusions: Drug endocrine therapy can effectively improve the lower urinary tract symptoms of patients with prostate cancer, and the more severe the symptoms and prostate volumeof the patients, the more obvious the improvement of lower urinary tract symptoms. The age, tumor stage, PSA, Gleason score, time and manner of administration were not significantly correlated with improvement in lower urinary tract symptoms.


Assuntos
Sintomas do Trato Urinário Inferior , Preparações Farmacêuticas , Hiperplasia Prostática , Neoplasias da Próstata , Humanos , Sintomas do Trato Urinário Inferior/tratamento farmacológico , Sintomas do Trato Urinário Inferior/etiologia , Masculino , Neoplasias da Próstata/complicações , Qualidade de Vida , Estudos Retrospectivos
18.
Bratisl Lek Listy ; 120(11): 867-871, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31747770

RESUMO

BACKGROUND: Drug usage in pregnant women is associated with a problem of possible negative influence on prenatal development. It is always necessary to judge the need for drug administration during pregnancy. OBJECTIVE: The aim of presented study was to analyse data about pregnant women hospitalized in the postpartum period. METHODS: The study was designed as a retrospective observational study including 300 women hospitalized at the 2nd Department of Gynaecology and Obstetrics, University Hospital, Bratislava. Data were obtained through questionnaires in form of an interview. RESULTS: The average age of women was 30.79 ± 4.40 years. Risk pregnancy occured in 20.59 % of women. Chronic disorders before pregnancy required regular pharmacotherapy in 29.24 %. Drug usage analysis: I. trimester, 31 % used at least one drug, 52 % nutritional supplements, 63.3 % drug and/or nutritional supplement; II. trimester, 23 % used at least one drug, 45 % nutritional supplements, 58.3 % drug and/or nutritional supplement; III. trimester, 32 % used at least one drug, 67 % nutritional supplements, 75.3 % drug and/or nutritional supplement. CONCLUSION: Drug usage during pregnancy requires great precaution at choosing pharmacotherapy. The benefit of pharmacotherapy should always outweight the potential risk of administered drug (Tab. 3, Fig. 3, Ref. 37).


Assuntos
Suplementos Nutricionais , Preparações Farmacêuticas/administração & dosagem , Adulto , Feminino , Humanos , Período Pós-Parto , Gravidez , Estudos Retrospectivos
19.
Eur J Pharm Biopharm ; 145: 113-120, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31682903

RESUMO

Lipid-based drug delivery systems (LBDDS) are highly relevant as pharmaceutical formulations significantly enhancing the bioavailability of active pharmaceutical ingredients (APIs). These formulations often are complex mixtures of APIs, various lipids, and other excipients (e.g. surfactants). In their simplest form, LBDDS contain one API being dissolved in a pure lipid, which often is a triglyceride (TG). In this work, solubilities of the APIs indomethacin, ibuprofen, and fenofibrate in pure TGs of different chain lengths (C chain 8-18) and degree of saturation were investigated. Solubilities of APIs in TGs were measured via differential scanning calorimetry, hot-stage microscopy, high-performance liquid chromatography, and Raman spectroscopy. The influence of fatty-acid chain length and degree of saturation on the API solubility in the TGs was investigated. APIs showed a higher solubility in saturated (wIBU = 10.5 wt% at 25 °C in tricaprylin) TGs compared to unsaturated ones (wIBU = 4.0 wt% at 25 °C in triolein). The fatty-acid chain length of TGs only slightly affects the solubility of ibuprofen and fenofibrate, but strongly influences the eutectic temperature of the API/TG mixtures. API solubilities in TGs and TG mixtures (mixtures of tricaprylin and tricaprin) were successfully modeled using the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT) accounting for the intermolecular API/TG interactions providing a deep understanding of the energetic and structural impact of the TGs on API solubility.


Assuntos
Preparações Farmacêuticas/química , Solubilidade/efeitos dos fármacos , Triglicerídeos/química , Varredura Diferencial de Calorimetria/métodos , Química Farmacêutica/métodos , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Excipientes/química , Fenofibrato/química , Ibuprofeno/química , Indometacina/química , Lipídeos/química
20.
Nature ; 575(7782): 336-340, 2019 11.
Artigo em Inglês | MEDLINE | ID: mdl-31723273

RESUMO

Organoboron reagents are important synthetic intermediates that have a key role in the construction of natural products, pharmaceuticals and organic materials1. The discovery of simpler, milder and more efficient approaches to organoborons can open additional routes to diverse substances2-5. Here we show a general method for the directed C-H borylation of arenes and heteroarenes without the use of metal catalysts. C7- and C4-borylated indoles are produced by a mild approach that is compatible with a broad range of functional groups. The mechanism, which is established by density functional theory calculations, involves BBr3 acting as both a reagent and a catalyst. The potential utility of this strategy is highlighted by the downstream transformation of the formed boron species into natural products and drug scaffolds.


Assuntos
Compostos de Boro/química , Compostos de Boro/síntese química , Boro/química , Produtos Biológicos/síntese química , Produtos Biológicos/química , Teoria da Densidade Funcional , Descoberta de Drogas , Indóis/química , Compostos Organometálicos/química , Preparações Farmacêuticas/síntese química , Preparações Farmacêuticas/química
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