RESUMO
Blackcurrant press cake (BPC) is a source of anthocyanins, and this study evaluated the bioactivity and gut microbiota modulation of blackcurrant diets with or without 1,2 dimethylhydrazine (DMH)-induced colon carcinogenesis in rats. In colon cancer-induced rats (CRC), BPC at the highest dosages increased pro-inflammatory parameters and the expression of anti-apoptotic cytokines, accentuating colon cancer initiation by aberrant crypts and morphological changes. Fecal microbiome analysis showed that BPC altered the composition and function of the gut microbiome. This evidence suggests that high doses of BPC act as a pro-oxidant, accentuating the inflammatory environment and CRC progression.
Assuntos
Neoplasias do Colo , Microbiota , Animais , Ratos , Antocianinas/farmacologia , Estresse Oxidativo , Inflamação , Veículos FarmacêuticosRESUMO
Aluminum chlorohydrate (ACH) is a major aerosol component frequently used as the active ingredient in antiperspirants, and in vivo studies have raised a concern about its inhalation toxicity. Still, few studies have addressed its effects on the human respiratory tract. Therefore, we developed a study on ACH inhalation toxicity using an in vitro human alveolar cell model (A549 cells) with molecular and cellular markers of oxidative stress, immunotoxicity, and epigenetic changes. The chemical characterization of ACH suspensions indicated particle instability and aggregation; however, side-scatter analysis demonstrated significant particle uptake in cells exposed to ACH. Exposure of A549 cells to non-cytotoxic concentrations of ACH (0.25, 0.5, and 1 mg/ml) showed that ACH induced reactive oxygen species. Moreover, ACH upregulated TNF, IL6, IL8, and IL1A genes, but not the lncRNAs NEAT1 and MALAT1. Finally, no alterations on the global DNA methylation pattern (5-methylcytosine and 5-hydroxymethylcytosine) or the phosphorylation of histone H2AX (γ-H2AX) were observed. Our data suggest that ACH may induce oxidative stress and inflammation on alveolar cells, and A549 cells may be useful to identify cellular and molecular events that may be associated with adverse effects on the lungs. Still, further research is needed to ensure the inhalation safety of ACH.
Assuntos
Alumínio , Cosméticos , Humanos , Administração por Inalação , Aerossóis , Veículos Farmacêuticos , Exposição por Inalação/efeitos adversosRESUMO
OBJECTIVE: To compare plasma concentrations of cannabidiol (CBD) following oral administration of two formulations of the drug (powder and dissolved in oil), and to evaluate the effects of these distinct formulations on responses to emotional stimuli in healthy human volunteers. METHODS: In a randomized, double-blind, placebo-controlled, parallel-group design, 45 healthy male volunteers were randomly assigned to three groups of 15 subjects that received either 150 mg of CBD powder; 150 mg of CBD dissolved in corn oil; or placebo. Blood samples were collected at different times after administration, and a facial emotion recognition task was completed after 150 min. RESULTS: There were no significant differences across groups in the subjective and physiological measures, nor in the facial emotion recognition task. However, groups that received the drug showed statistically significant differences in baseline measures of plasma CBD, with a significantly greater difference in favor of the oil formulation. CONCLUSION: When administered as a single 150-mg dose, neither formulation of oral CBD altered responses to emotional stimuli in healthy subjects. The oil-based CBD formulation resulted in more rapid achievement of peak plasma level, with an approximate fourfold increase in oral bioavailability.
Assuntos
Canabidiol , Emoções , Reconhecimento Facial , Veículos Farmacêuticos , Administração Oral , Canabidiol/química , Canabidiol/farmacologia , Método Duplo-Cego , Composição de Medicamentos , Humanos , MasculinoRESUMO
La enfermedad de Chagas, tripanosomiasis americana o simplemente Chagas, es una infección parasitaria que afecta a más de 8 millones de personas a nivel mundial. La Organización Mundial de la Salud ha incluido a esta patología dentro de la categoría de enfermedades tropicales desatendidas (junto a la malaria, leishmaniasis y dengue, entre otras), ya que afecta mayoritariamente a grupos vulnerables de la sociedad sin acceso a condiciones adecuadas de sanidad ni tratamientos médicos, y en contacto continuo con los vectores de contagio. La terapia actual incluye fármacos utilizados desde hace ya más de 50 años que, si bien son efectivos en la fase inicial de la enfermedad, fallan en la erradicación total del parásito, a la vez que generan graves efectos adversos. En vista de este panorama, surge la necesidad de nuevas estrategias de bajo costo para optimizar la terapia. Una posible alternativa para mejorar el tratamiento, diagnóstico y prevención surge desde la nanotecnología: el presente artículo revisa el estado actual de la investigación de nanomedicinas para tratar la enfermedad de Chagas. Cabe mencionar que, si bien se ha avanzado enormemente en dirección a una terapia que disminuya los efectos adversos de la droga, aún no se ha logrado diseñar y producir un nanovehículo farmacéutico óptimo contra el agente etiológico de la enfermedad.
Chagas disease, American trypanosomiasis or Chagas disease, is a parasitic infection that affects more than 8 million people worldwide. This pathology was included by the World Health Organization within the category of neglected tropical diseases (along with malaria, leishmaniasis and dengue, among others), since it mainly affects vulnerable groups in society without access to adequate health conditions nor medical treatments, and in continuous contact with the transmission vectors. Current therapy includes drugs used for more than 50 years that, although effective in the initial phase of the disease, fail in the total eradication of the parasite, while generating serious adverse effects. In light of this situation, new low-cost approach strategies are necessary to optimize therapy. A possible alternative to improve treatment, diagnosis and prevention arises from nanotechnology: this article reviews the current state of research in nanomedicines to treat Chagas disease. It is worth mentioning that, although great progress has been made towards a therapy that reduces the adverse effects of the drug, it has not yet been possible to design and produce an optimal pharmaceutical nanovehicle against the etiologic agent of the disease.
Assuntos
Veículos Farmacêuticos , Doença , Doença de Chagas , NanomedicinaRESUMO
Compounded liquid medication is frequently required in children to allow easy dose adjustment and overcome swallowing difficulties. The objective of this study was to evaluate the stability of oral suspensions compounded with SyrSpend SF PH4 and the commonly used active pharmaceutical ingredients baclofen 2.0 mg/mL, carvedilol 5.0 mg/mL, hydrochlorothiazide 2.0 mg/mL, mercaptopurine 10.0 mg/mL, methadone hydrochloride 10.0 mg/mL, oseltamivir phosphate 6.0 mg/mL, phenobarbital 9.0 mg/mL and 15.0 mg/mL, propranolol hydrochloride 0.5 mg/mL and 5.0 mg/mL, pyrazinamide 100.0 mg/mL, spironolactone 2.0 mg/mL and 2.5 mg/mL, sotalol hydrochloride 5.0 mg/mL, tacrolimus monohydrate 0.5 mg/mL, ursodeoxycholic acid 20.0 mg/mL, and vancomycin hydrochloride 25.0 mg/mL. Suspensions were compounded with raw powders, except for mercaptopurine, pyrazinamide, and sotalol hydrochloride, which were made from commercial tablets. Stability was assessed by measuring the percentage recovery at 0 (baseline), 60 days, and 90 days after compounding for suspensions made with raw powders, which were stored at 2ÅãC to 8ÅãC. The stability of tablets, which were stored at 2ÅãC to 8ÅãC and 20ÅãC to 25ÅãC, was assessed by measuring the percentage recovery at 0 (baseline), 7 days, 14 days, 30 days, 60 days, and 90 days. Active pharmaceutical ingredients quantification was performed by ultraviolet high-performance liquid chromatography via a stability-indicating method. Given the percentage of recovery of the active pharmaceutical ingredients within the suspensions, the beyond-use date of the final products (active pharmaceutical ingredients + vehicle) was at least 90 days for all suspensions in the conditions tested. This suggests that SyrSpend SF PH4 is suitable for compounding active pharmaceutical ingredients from different pharmacological classes.
Assuntos
Baclofeno/química , Carvedilol/química , Hidroclorotiazida/química , Mercaptopurina/química , Metadona/química , Oseltamivir/química , Veículos Farmacêuticos/química , Fenobarbital/química , Propranolol/química , Sotalol/química , Espironolactona/química , Amido/química , Tacrolimo/química , Ácido Ursodesoxicólico/química , Vancomicina/química , Administração Oral , Baclofeno/administração & dosagem , Carvedilol/administração & dosagem , Composição de Medicamentos , Estabilidade de Medicamentos , Hidroclorotiazida/administração & dosagem , Concentração de Íons de Hidrogênio , Mercaptopurina/administração & dosagem , Metadona/administração & dosagem , Oseltamivir/administração & dosagem , Soluções Farmacêuticas , Fenobarbital/administração & dosagem , Propranolol/administração & dosagem , Pirazinamida/administração & dosagem , Sotalol/administração & dosagem , Espironolactona/administração & dosagem , Suspensões , Tacrolimo/administração & dosagem , Temperatura , Fatores de Tempo , Ácido Ursodesoxicólico/administração & dosagem , Vancomicina/administração & dosagemRESUMO
Methylene Blue (MB) has been widely used in antimicrobial Photodynamic Therapy (aPDT), however, the mechanisms of action (Type I or Type II) are defined by its state of aggregation. In this sense, the identification of the relationships between aggregation, the mechanisms of action and the effectiveness against microorganisms, as well as the establishment of the means and the formulations that may favor the most effective mechanisms, are essential. Thus, the objective of this study was to assess the in vitro aPDT efficacies against Candida albicans, by using MB in vehicles which may influence the aggregation and present an oral formulation (OF) containing MB, to be used in clinical aPDT procedures. The efficacy of MB at 20 mg L-1 was tested in a range of vehicles (water, physiological solution - NaCl 0.9%, phosphate saline buffer - PBS, sodium dodecyl sulfate 0.25% - SDS and urea 1 mol L-1) in a C. albicans planktonic culture, when using 4.68 J cm-2 of 640 ± 12 nm LED for the irradiations, as well as 5 minutes of pre-irradiation time, together with measuring the UFC mL-1. Based upon these analyses, an OF containing MB in the most effective vehicle was tested in the biofilms, as a proposal for clinical applications. When comparing some of the vehicles, sodium dodecyl sulfate was the only one that enhanced an MB aPDT efficacy in a planktonic C. albicans culture. This OF was tested in the biofilms and 50 mg L-1 MB was necessary, in order to achieve some reduction in the cell viabilities after the various treatments. The light dosimetries still need further adaptations, in order for this formulation to be used in clinical applications. The present research has indicated that the development of this formulation for the control of MB aggregations may result in more effective clinical protocols.
Assuntos
Candida albicans/efeitos dos fármacos , Candidíase/tratamento farmacológico , Dimerização , Azul de Metileno/administração & dosagem , Veículos Farmacêuticos/química , Fármacos Fotossensibilizantes/administração & dosagem , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/farmacologia , Biofilmes/efeitos dos fármacos , Candida albicans/fisiologia , Candidíase/microbiologia , Humanos , Azul de Metileno/química , Azul de Metileno/farmacologia , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/farmacologia , Dodecilsulfato de Sódio/químicaRESUMO
BACKGROUND: The fruits acerola and red plum are known to be good sources of antioxidants, particularly vitamin C. Antioxidants are compounds that protect organisms from biomolecular damage, such as accelerated aging, caused by free radicals. OBJECTIVE: The objective of this study was to extract vitamin C from acerola and red plum, incorporate these extracts into different topical formulations, and evaluate the physicochemical stabilities of these formulations under stress conditions. METHODS: Vitamin C was extracted from acerola and red plum via dynamic maceration for 2 h at 50 ± 2°C and was quantified via HPLC. In vitro antioxidant activities were evaluated using DPPH assays. The extracts were then incorporated into emulsion and gel formulations in two types of packaging, and stability studies were carried out. RESULTS: Red plum and acerola extracts were orange and red and contained vitamin C concentrations of 2732.70 ± 93.01 mg/100 g and 2.60 ± 1.2 mg/100 g, respectively. In vitro antioxidant activity resulted in over 90.0% inhibition of free radicals at 0.01 mL/mL acerola extract and 0.1 mL/mL red plum extract. In the stability study, pH values decreased for both acerola formulations when stored in the oven or in transparent glass containers. Formulations containing red plum extract were stable under all conditions. Acerola extracts contained a higher concentration of vitamin C than red plum extracts. Both extracts possessed antioxidant activity, although the acerola-based formulation was unstable when stored at high temperatures or in transparent glass containers. HIGHLIGHTS: Extracts from red plum and acerola contained vitamin C; antioxidant activity of the extracts resulted in over 90.0% inhibition of free radicals. Formulations containing red plum were stable under all tested conditions, and formulations containing acerola were unstable when stored in the oven or in transparent glass containers.
Assuntos
Antioxidantes/análise , Ácido Ascórbico/análise , Cromatografia Líquida de Alta Pressão/métodos , Malpighiaceae/química , Extratos Vegetais/análise , Prunus domestica/química , Administração Tópica , Antioxidantes/administração & dosagem , Antioxidantes/farmacologia , Ácido Ascórbico/administração & dosagem , Ácido Ascórbico/farmacologia , Composição de Medicamentos , Estabilidade de Medicamentos , Emulsões/química , Radicais Livres/química , Frutas/química , Géis/química , Veículos Farmacêuticos/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologiaRESUMO
The aim of this study was to evaluate edemogenic activity and subcutaneous inflammatory reaction induced by Psidium cattleianum leaf extracts associated with Ca(OH)2. Thirty male Wistar rats, split equally into three groups [aqueous extract + Ca(OH)2; ethanolic extract + Ca(OH)2; and propylene glycol + Ca(OH)2], were assessed every 3 h or 6 h (five animals in each period). Under general anesthesia, 0.2 mL of 1% Evans blue per 100 g of body weight was injected into the penile vein and each combination to be evaluated was subcutaneously injected into the dorsal region 30 min thereafter. Edemogenic activity was analyzed by spectrophotometry (λ=630 nm). For inflammatory reaction analysis, 50 rats received four polyethylene tubes (three experimental groups) and an empty tube (control group). The assessments were made at 7, 15, 30, 60, and 90 days, followed by hematoxylin-eosin staining and by the assignment of scores for evaluation of tissue response intensity. Ethanolic extract + Ca(OH)2 yielded the largest edemogenic activity at 3 h. Intergroup differences at 6 h were not significant. The histological analysis showed progressive repair over time (p<0.05) and aqueous and ethanolic extracts produced similar responses to those of the control and Ca(OH)2 + propylene glycol groups. Psidium cattleianum leaf extracts used as Ca(OH)2 vehicles evoked similar tissue response when compared to Ca(OH)2 associated with propylene glycol.
Assuntos
Hidróxido de Cálcio/farmacologia , Extratos Vegetais/farmacologia , Psidium/química , Tela Subcutânea/efeitos dos fármacos , Animais , Anti-Infecciosos/farmacologia , Portadores de Fármacos , Avaliação Pré-Clínica de Medicamentos , Etanol/farmacologia , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Teste de Materiais , Veículos Farmacêuticos/química , Veículos Farmacêuticos/farmacologia , Folhas de Planta/química , Propilenoglicol/farmacologia , Ratos Wistar , Reprodutibilidade dos Testes , Tela Subcutânea/patologia , Fatores de Tempo , Água/químicaRESUMO
Abstract The aim of this study was to evaluate edemogenic activity and subcutaneous inflammatory reaction induced by Psidium cattleianum leaf extracts associated with Ca(OH)2. Thirty male Wistar rats, split equally into three groups [aqueous extract + Ca(OH)2; ethanolic extract + Ca(OH)2; and propylene glycol + Ca(OH)2], were assessed every 3 h or 6 h (five animals in each period). Under general anesthesia, 0.2 mL of 1% Evans blue per 100 g of body weight was injected into the penile vein and each combination to be evaluated was subcutaneously injected into the dorsal region 30 min thereafter. Edemogenic activity was analyzed by spectrophotometry (λ=630 nm). For inflammatory reaction analysis, 50 rats received four polyethylene tubes (three experimental groups) and an empty tube (control group). The assessments were made at 7, 15, 30, 60, and 90 days, followed by hematoxylin-eosin staining and by the assignment of scores for evaluation of tissue response intensity. Ethanolic extract + Ca(OH)2 yielded the largest edemogenic activity at 3 h. Intergroup differences at 6 h were not significant. The histological analysis showed progressive repair over time (p<0.05) and aqueous and ethanolic extracts produced similar responses to those of the control and Ca(OH)2 + propylene glycol groups. Psidium cattleianum leaf extracts used as Ca(OH)2 vehicles evoked similar tissue response when compared to Ca(OH)2 associated with propylene glycol.
Assuntos
Animais , Masculino , Hidróxido de Cálcio/farmacologia , Extratos Vegetais/farmacologia , Tela Subcutânea/efeitos dos fármacos , Psidium/química , Fatores de Tempo , Veículos Farmacêuticos/farmacologia , Veículos Farmacêuticos/química , Teste de Materiais , Portadores de Fármacos , Água/química , Reprodutibilidade dos Testes , Ratos Wistar , Folhas de Planta/química , Propilenoglicol/farmacologia , Tela Subcutânea/patologia , Etanol/farmacologia , Avaliação Pré-Clínica de Medicamentos , Inflamação/patologia , Inflamação/tratamento farmacológico , Anti-Infecciosos/farmacologiaRESUMO
OBJECTIVE:: Enterococcus faecalis is the dominant microbial species responsible for persistent apical periodontitis with ability to deeply penetrate into the dentin. Exopolysaccharides (EPS) contribute to the pathogenicity and antibiotic resistance of E. faecalis. Our aim was to investigate the antimicrobial activity of calcium hydroxide (CH), camphorated parachlorophenol (CMCP), and chlorhexidine (CHX) against E. faecalis in dentinal tubules. MATERIAL AND METHODS:: Decoronated single-canal human teeth and semicylindrical dentin blocks were incubated with E. faecalis for 3 weeks. Samples were randomly assigned to six medication groups for 1 week (n=10 per group): CH + 40% glycerin-water solution (1:1, wt/vol); CMCP; 2% CHX; CH + CMCP (1:1, wt/vol); CH + CMCP (2:3, wt/vol); and saline. Bacterial samples were collected and assayed for colony-forming units. After dentin blocks were split longitudinally, confocal laser scanning microscopy was used to assess the proportion of viable bacteria and EPS production in dentin. RESULTS:: CMCP exhibited the best antimicrobial activity, while CH was the least sensitive against E. faecalis (p<0.05). CHX showed similar antimicrobial properties to CH + CMCP (1:1, wt/vol) (p>0.05). CH combined with CMCP inhibited EPS synthesis by E. faecalis, which sensitized biofilms to antibacterial substances. Moreover, increasing concentrations of CMCP decreased EPS matrix formation, which effectively sensitized biofilms to disinfection agents. CONCLUSION:: The EPS matrix dispelled by CH paste with CMCP may be related to its bactericidal effect; the visualization and analysis of EPS formation and microbial colonization in dentin may be a useful approach to verify medicaments for antimicrobial therapy.
Assuntos
Antibacterianos/farmacologia , Hidróxido de Cálcio/farmacologia , Dentina/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Veículos Farmacêuticos/farmacologia , Polissacarídeos Bacterianos/química , Irrigantes do Canal Radicular/farmacologia , Adolescente , Adulto , Biofilmes/efeitos dos fármacos , Cânfora/farmacologia , Clorexidina/farmacologia , Clorofenóis/farmacologia , Contagem de Colônia Microbiana , Cavidade Pulpar/efeitos dos fármacos , Cavidade Pulpar/microbiologia , Dentina/microbiologia , Combinação de Medicamentos , Humanos , Viabilidade Microbiana/efeitos dos fármacos , Microscopia Confocal , Reprodutibilidade dos Testes , Estatísticas não Paramétricas , Fatores de Tempo , Adulto JovemRESUMO
ABSTRACT Objective: Enterococcus faecalis is the dominant microbial species responsible for persistent apical periodontitis with ability to deeply penetrate into the dentin. Exopolysaccharides (EPS) contribute to the pathogenicity and antibiotic resistance of E. faecalis. Our aim was to investigate the antimicrobial activity of calcium hydroxide (CH), camphorated parachlorophenol (CMCP), and chlorhexidine (CHX) against E. faecalis in dentinal tubules. Material and Methods: Decoronated single-canal human teeth and semicylindrical dentin blocks were incubated with E. faecalis for 3 weeks. Samples were randomly assigned to six medication groups for 1 week (n=10 per group): CH + 40% glycerin-water solution (1:1, wt/vol); CMCP; 2% CHX; CH + CMCP (1:1, wt/vol); CH + CMCP (2:3, wt/vol); and saline. Bacterial samples were collected and assayed for colony-forming units. After dentin blocks were split longitudinally, confocal laser scanning microscopy was used to assess the proportion of viable bacteria and EPS production in dentin. Results: CMCP exhibited the best antimicrobial activity, while CH was the least sensitive against E. faecalis (p<0.05). CHX showed similar antimicrobial properties to CH + CMCP (1:1, wt/vol) (p>0.05). CH combined with CMCP inhibited EPS synthesis by E. faecalis, which sensitized biofilms to antibacterial substances. Moreover, increasing concentrations of CMCP decreased EPS matrix formation, which effectively sensitized biofilms to disinfection agents. Conclusion: The EPS matrix dispelled by CH paste with CMCP may be related to its bactericidal effect; the visualization and analysis of EPS formation and microbial colonization in dentin may be a useful approach to verify medicaments for antimicrobial therapy.
Assuntos
Humanos , Adolescente , Adulto , Adulto Jovem , Polissacarídeos Bacterianos/química , Irrigantes do Canal Radicular/farmacologia , Veículos Farmacêuticos/farmacologia , Hidróxido de Cálcio/farmacologia , Enterococcus faecalis/efeitos dos fármacos , Dentina/efeitos dos fármacos , Antibacterianos/farmacologia , Fatores de Tempo , Cânfora/farmacologia , Contagem de Colônia Microbiana , Clorofenóis/farmacologia , Reprodutibilidade dos Testes , Estatísticas não Paramétricas , Microscopia Confocal , Biofilmes/efeitos dos fármacos , Cavidade Pulpar/efeitos dos fármacos , Cavidade Pulpar/microbiologia , Dentina/microbiologia , Combinação de Medicamentos , Viabilidade Microbiana/efeitos dos fármacosRESUMO
In Brazil there is no classification of dermatological products by the presence of vehicles with sensitizing potential. The objective of this study is to create a database to classify such products based on the absence of the selected allergens, aiming at making it available for medical consultation. We conducted an observational study, from the content of labels and/or inserts on the composition of 966 dermatological products in the Brazilian market. No chemical analysis was performed. The database called Programa para Pesquisa de Alérgenos de Contato (www.ppac.com.br) was created, in which safe products for patients allergic to dermatological vehicles are provided.
Assuntos
Bases de Dados Factuais , Dermatite Alérgica de Contato/prevenção & controle , Serviços de Informação sobre Medicamentos , Rotulagem de Medicamentos , Brasil , Humanos , Veículos Farmacêuticos/efeitos adversosAssuntos
Anti-Inflamatórios/administração & dosagem , Budesonida/administração & dosagem , Esofagite Eosinofílica/tratamento farmacológico , Administração Oral , Adolescente , Biópsia , Criança , Pré-Escolar , Esofagite Eosinofílica/patologia , Esôfago/patologia , Frutas , Mel , Humanos , Lactente , Veículos Farmacêuticos/administração & dosagem , Sacarose/administração & dosagem , Sacarose/análogos & derivados , Edulcorantes/administração & dosagemRESUMO
Clobetasol benefits to control psoriasis lesions are well defined, but there were not studies about its action when used in lacquer vehicle to control skin lesions. A double-blind study was conducted with 40 patients that utilized clobetasol 0.05% in one hemibody and just the vehicle in the other hemibody. Twenty of them used petrolatum as vehicle and the others used lacquer. An assessment was conducted using the clinical index PASI and a quality of life questionnaire (Dermatological Life Quality Index). There was no statistical difference between groups. There was a trend of favorable response particularly in the hemibody treated with clobetasol.
Assuntos
Clobetasol/administração & dosagem , Glucocorticoides/administração & dosagem , Laca , Psoríase/tratamento farmacológico , Administração Tópica , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Veículos Farmacêuticos , Estudos Prospectivos , Qualidade de Vida , Índice de Gravidade de Doença , Inquéritos e Questionários , Resultado do Tratamento , Adulto JovemRESUMO
Oral liquids are safe alternatives to solid dosage forms, notably for elderly and pediatric patients that present dysphagia. The use of ready-to-use suspending vehicles such as SyrSpend SF PH4 is a suitable resource for pharmacists as they constitute a safe and timesaving option that has been studied often. The objective of this study was to evaluate the stability of 10 commonly used active pharmaceutical ingredients (allopurinol 20 mg/mL; amitriptyline hydrochloride 10 mg/mL; carbamazepine 25 mg/mL; domperidone 5 mg/mL; isoniazid 10 mg/mL; ketoconazole 20 mg/mL; lisinopril 1 mg/mL; naproxen 25 mg/mL; paracetamol [acetaminophen] 50 mg/mL; and sertraline hydrochloride 10 mg/mL) compounded in oral suspensions using SyrSpend SF PH4 as the vehicle throughout the study period and stored both at controlled refrigerated (2°C to 8°C) and room temperature (20°C to 25°C). Stability was assessed by means of measuring the percent recovery at varying time points throughout a 90-day period. The quantification of the active pharmaceutical ingredients was performed by high-performance liquid chromatography through a stability-indicating method. Methods were adequately validated. Forced-degradation studies showed that at least one parameter influenced the stability of the active pharmaceutical ingredients. All suspensions were assayed and showed active pharmaceutical ingredient contents between 90% and 110% during the 90-day study period. Although the forced-degradation experiments led to visible fluctuations in the chromatographic responses, the final preparations were stable in the storage conditions. The beyond-use dates of the preparations were found to be at least 90 days for all suspensions, both for controlled refrigerated temperature and room temperature. This confirms that SyrSpend SF PH4 is a stable suspending vehicle for compounding with a broad range of different active pharmaceutical ingredients for different medical usages.
Assuntos
Veículos Farmacêuticos/análise , Suspensões/análise , Cromatografia Líquida de Alta Pressão , Combinação de Medicamentos , Estabilidade de Medicamentos , Padrões de Referência , RefrigeraçãoRESUMO
Objetivo: O objetivo deste estudo foi avaliar a capacidade antimicrobiana do hidróxido de cálcio associado à dois veículos convencionais (anestésico líquido e azeite de oliva) e um novo veículo (Trietanolamina). Material e Métodos: Inicialmente, os micro-organismos foram coletados de quatro incisivos superiores de um mesmo paciente que apresentavam tratamentos endodônticos insatisfatórios e periodontites apicais persistentes utilizando cones de papel absorvente esterilizados inseridos nos canais radiculares após a remoção do material obturador. Em seguida, estes foram cultivados em BHI durante 24 h e colocados em 10 placas de Petri com três orifícios preenchidos com as medicações avaliadas. Após 48 e 72 h, os halos de inibição foram aferidos. Resultados: Após aplicação do teste de Kruskal-Wallis com nível de significância de 1% (α = 0,01) foi observado que, hidróxido de cálcio associado à Trietanolamina, apresentou resultados semelhantes àqueles produzidos pelo líquido anestésico. Ambas as combinações foram superiores ao hidróxido de cálcio veiculado ao azeite de oliva. Conclusão: Considerando os resultados deste estudo in vitro, é possível concluir que Trietanolamina pode ser uma alternativa viável para ser utilizada como veículo associado ao hidróxido de cálcio.
Objective: The aim of this study was to evaluate the antimicrobial effectiveness of calcium hydroxide associated with a two conventional (anesthetic liquidand olive oil) and a new vehicle (Triethanolamine). Material and methods: Initially, microorganisms were collected from four upper incisors presenting unsatisfactory root canal treatments and persistent apical periodontitis from the same patient using sterile absorbent paper cones placed inside the root canal following initial access and root filling removal. Next, they were grown in a BHI culturemedium for 24 h. Afterwards, they were placed in 10 Petri dishes with 3 holes, where different formulations of the medications studied were placed. After 48 and 72 h, readings were taken of the growth inhibition halos. Results: After using Kruskal-Wallis test with significance level of 1% (α = 0.01) it was observed that, calcium hydroxide associated with Triethanolamine, produced results similar to those produced by the anesthetic liquid. Both combinations were superior to the association with olive oil. Conclusion: Considering the results of this in vitrostudy, it is possible to consider that Triethanolamine can be a viable alternative to be used as a vehicleassociated with the calcium hydroxide.
Assuntos
Hidróxido de Cálcio , Endodontia , Veículos FarmacêuticosRESUMO
The aim of this study was to evaluate the subcutaneous tissue response in rats and the antimicrobial activity of intracanal calcium hydroxide dressings mixed with different substances against E. faecalis. Fifty four rats were divided into three experimental groups according to the vehicle in the calcium hydroxide treatment: 0.4% chlorohexidine in propylene glycol (PG),Casearia sylvestris Sw in PG and calcium hydroxide+PG (control group). The pastes were placed into polyethylene tubes and implanted into the subcutaneous tissue. After 7, 14 and 30 days, the samples were processed and histologically evaluated (hematoxylin and eosin). The tissue surface in contact with the material was analyzed, and the quantitative analysis determined the volume density occupied by the inflammatory infiltrate (giant cells, polymorphonuclear cells and mononuclear cells), fibroblasts, collagen fibers and blood vessels. For the antimicrobial analysis, 20 dentin blocks infected with E. faecalis were treated with calcium hydroxide pastes in different vehicles; 0.4% chlorhexidine in PG, PG, extract fromCasearia sylvestris Sw in PG and a positive control (infection and without medication) for 7 days. The efficiency of the pastes was evaluated by the live/dead technique and confocal microscopy. The results showed that 0.4% chlorhexidine induced a higher inflammatory response than the other groups. The Casearia sylvestris Sw extract showed satisfactory results in relation to the intensity of the inflammatory response. In the microbiological test, there were no statistical differences between the evaluated intracanal dressings and the percentage of bacterial viability was between 33 and 42%. The control group showed an 86% viability. Antimicrobial components such as chlorhexidine or Casearia sylvestris Sw did not improve the antimicrobial activity against E. faecalis in comparison to the calcium hydroxide+PG treatment. In addition, the incorporation of chlorhexidine in the calcium hydroxide paste promoted the highest inflammatory response.
Assuntos
Animais , Bovinos , Anti-Infecciosos/farmacologia , Hidróxido de Cálcio/farmacologia , Casearia/química , Clorexidina/farmacologia , Tela Subcutânea/efeitos dos fármacos , Anti-Infecciosos/química , Hidróxido de Cálcio/química , Células Cultivadas , Clorexidina/química , Colágeno/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Teste de Materiais , Viabilidade Microbiana/efeitos dos fármacos , Pomadas , Veículos Farmacêuticos/química , Veículos Farmacêuticos/farmacologia , Propilenoglicol/química , Propilenoglicol/farmacologia , Ratos Wistar , Tela Subcutânea/patologia , Fatores de TempoRESUMO
The aim of this study was to evaluate the subcutaneous tissue response in rats and the antimicrobial activity of intracanal calcium hydroxide dressings mixed with different substances against E. faecalis. Fifty four rats were divided into three experimental groups according to the vehicle in the calcium hydroxide treatment: 0.4% chlorohexidine in propylene glycol (PG),Casearia sylvestris Sw in PG and calcium hydroxide+PG (control group). The pastes were placed into polyethylene tubes and implanted into the subcutaneous tissue. After 7, 14 and 30 days, the samples were processed and histologically evaluated (hematoxylin and eosin). The tissue surface in contact with the material was analyzed, and the quantitative analysis determined the volume density occupied by the inflammatory infiltrate (giant cells, polymorphonuclear cells and mononuclear cells), fibroblasts, collagen fibers and blood vessels. For the antimicrobial analysis, 20 dentin blocks infected with E. faecalis were treated with calcium hydroxide pastes in different vehicles; 0.4% chlorhexidine in PG, PG, extract from Casearia sylvestris Sw in PG and a positive control (infection and without medication) for 7 days. The efficiency of the pastes was evaluated by the live/dead technique and confocal microscopy. The results showed that 0.4% chlorhexidine induced a higher inflammatory response than the other groups. The Casearia sylvestris Sw extract showed satisfactory results in relation to the intensity of the inflammatory response. In the microbiological test, there were no statistical differences between the evaluated intracanal dressings and the percentage of bacterial viability was between 33 and 42%. The control group showed an 86% viability. Antimicrobial components such as chlorhexidine or Casearia sylvestris Sw did not improve the antimicrobial activity against E. faecalis in comparison to the calcium hydroxide+PG treatment. In addition, the incorporation of chlorhexidine in the calcium hydroxide paste promoted the highest inflammatory response.
Assuntos
Anti-Infecciosos/farmacologia , Hidróxido de Cálcio/farmacologia , Casearia/química , Clorexidina/farmacologia , Tela Subcutânea/efeitos dos fármacos , Animais , Anti-Infecciosos/química , Hidróxido de Cálcio/química , Bovinos , Células Cultivadas , Clorexidina/química , Colágeno/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Teste de Materiais , Viabilidade Microbiana/efeitos dos fármacos , Pomadas , Veículos Farmacêuticos/química , Veículos Farmacêuticos/farmacologia , Propilenoglicol/química , Propilenoglicol/farmacologia , Ratos Wistar , Tela Subcutânea/patologia , Fatores de TempoRESUMO
O preparo biomecânico acompanhado pela irrigação no tratamento endodôntico de canais infectados tem se mostrado efetivo, porém alguns micro-organismos ainda sobrevivem. A espécie bacteriana mais frequentemente encontrada em casos de fracasso endodôntico é Enterococcus faecalis. Para combatê-lo diferentes medicações intra-canal são utilizadas, principalmente as pastas a base de hidróxido de cálcio e outras substâncias vem sendo associadas a estas para potencializar seu efeito antimicrobiano. Desta forma, é pertinente comparar in vitro a capacidade antimicrobiana do hidróxido de cálcio com diferentes veículos e aditivos, sobre Enterococcus faecalis, através de cultura microbiológica e microscopia confocal de varredura a laser (MCVL). Para isso, tubos de dentina bovina padronizados foram previamente esterilizados e em seguida contaminados durante 5 dias com a bactéria. Os espécimes receberam a medicação por 15 dias e foram divididos em cinco grupos-teste: pasta de hidróxido de cálcio veiculado em água destilada (G1), pasta veiculada em propilenoglicol(G2), pasta de hidróxido de cálcio veiculado em propilenoglicol com os aditivos extrato etanólico de própolis (G3), clorexidina (G4) e paramonoclorofenol canforado - PMCC (G5). Após o período da medicação, a coleta bacteriana dos fragmentos de dentina foi realizada com brocas de Largo em dispositivo esterilizado, para contagem dos micro-organismos ainda viáveis em unidades formadoras de colônias. A MCVL analisou as bactérias viáveis (verde) e mortas (vermelho) no interior dos túbulos dentinários, com o auxílio do corante Live and Dead®. Houve ação antimicrobiana intra-tubular dentinária sobre Enterococcus faecalis por todas as pastas de hidróxido de cálcio testadas. A partir deste trabalho foi possível observar a melhor ação antimicrobiana contra E. faecalis pela pasta de hidróxido de cálcio com propilenoglicol e PMCC nas regiões superficial e profunda da massa dentinária.
Biomechanical preparation followed by irrigation in endodontic treatment of infected root canals has been shown, however, some micro-organisms still survive. The most frequently founded bacterial specie in endodontic treatment fail is Enterococcus faecalis. To combat it, different intra-canal medications are used, mainly the calcium hydroxide pastes and other substances have been associated to calcium hydroxide to leverage it antimicrobial effect. Thus, its relevant to compare in vitro the antimicrobial ability of calcium hydroxide with different vehicles and additives, against Enterococcus faecalis, through microbiological culture and confocal laser scanning microscopy (CLSM). For this, standard dentine tubes were sterilized and then infected with the bacteria for 5 days and were divided in five test-groups, submitted to medication for 15 days with calcium hydroxide paste in distilled water (G1), in propylene glycol (G2), besides clacium hydroxide in propylene glycol with ethanol extract of propolis (G3), chlorexidine (G4) and CPMC (G5). After the medication period, the bacterial collection of the dentine´s fragments was done with Largos drill in a sterilized device, to count micro-organisms still viable in colony forming units. The CLSM evaluated the viable (green) and dead (red) bacteria inside the dentinal tubules with the aid of the Live and Dead® dye. There was dentinal intra-tubular antimicrobial action against Enterococcus faecalis for all the tested calcium hydroxide pastes. From this work was possible to observe a better antimicrobial activity against Enterococcus faecalis by the calcium hydroxide paste in propylene glycol and CPMC in superficial and deep areas of the dentine.
Assuntos
Animais , Bovinos , Dentina , Dentina/microbiologia , Enterococcus faecalis , Hidróxido de Cálcio/farmacologia , Irrigantes do Canal Radicular/farmacologia , Veículos Farmacêuticos/farmacologia , Anti-Infecciosos/farmacologia , Clorexidina/farmacologia , Teste de Materiais , Microscopia Confocal , Propilenoglicol/farmacologia , Própole/farmacologia , Reprodutibilidade dos Testes , Propriedades de Superfície , Fatores de TempoRESUMO
Efavirenz (EFV) used as a part of the treatment of first choice in antiretroviral therapy for AIDS has low aqueous solubility and presents problems of absorption. We thus initially present a phase solubility diagram with carriers of different classes. With a view to obtaining a solid dispersion (SD) with suitable consistency to that of a solid formulation, we chose to use PVP K-30, since polymers present some of the best results. The kneading (KN) and solvent evaporation (EV) methods were thus used at different rates. These were characterized by the way of DSC, FT-IR, SEM, DR-X and dissolution. SD EV proved unsatisfactory, resulting in a decreased dissolution rate, despite the amorphous state of the samples, while the SD KN 4:1 (EFV:polymer) and physical mixtures (PM) had a higher rate of dissolution. SD KN and PM 4:1 were also evaluated for stability after storage, with benefits being observed in relation to EFV.