ABSTRACT
The stability of human erythrocytes to sodium dodecyl sulfate (SDS) was assessed spectrophotometrically in the presence of different concentrations of bovine serum albumin (BSA) and at different temperatures (27-45 °C). The absorbance at 540 nm (A540) was correlated with the SDS concentration by sigmoidal regression based on the Boltzmann equation. Erythrocyte stability was characterized on the basis of the SDS concentration that induces hemolysis in 50% of the cells (D50). Progressive increases in the albumin concentration led to increases in the D50 value. The protective effect of BSA against SDS-induced hemolysis was attributed to the binding of the surfactant to the hydrophobic binding sites of this protein. The D50 values decreased sigmoidally with an increase in the temperature. This trend, which could not be explained by changes in the spectral properties of hemoglobin, maybe due to heterogeneity in the erythrocyte population.
Subject(s)
Erythrocytes/metabolism , Serum Albumin, Bovine/pharmacology , Sodium Dodecyl Sulfate/toxicity , Temperature , Animals , Cattle , Erythrocytes/drug effects , Hemolysis , Humans , Regression Analysis , Sodium Dodecyl Sulfate/metabolism , Spectrophotometry, UltravioletABSTRACT
In this work, the effects of 1 mol/L glycerol or sorbitol on the thermal dependence (27-47 degrees C) of the lysis of human erythrocytes by ethanol in saline solution (0.154 mol/L NaCl) have been evaluated. Lysis was monitored by measurement of the absorbance at 540 nm. Ethanol produced either lysis or protection against lysis depending on the conditions. These antagonistic effects are attributed to the existence of expanded (R) and compacted (T) erythrocytes, present under conditions of low and high osmolarity, respectively. The transitions of lysis of the R state and formation and lysis of the T state were all found to be sigmoidally defined. The ethanol concentration at the midpoint of the lysis transition of the R state (D(50R)) was found to decrease with increasing temperature and osmolarity. In the presence of glycerol or sorbitol, an increase in temperature led to smaller decreases in D(50R) and osmotic protection against lysis. The ethanol concentration at the midpoint of formation (S(50T)) and lysis (D(50T)) of the T state also decreased with increasing temperature and osmolarity. Lysis of R state erythrocytes is determined by the chaotropic action of ethanol, but the formation and lysis of T state erythrocytes are determined by osmotic pressure effects.
Subject(s)
Erythrocytes/drug effects , Ethanol/pharmacology , Glycerol , Sorbitol , Humans , TemperatureABSTRACT
As ciclodextrinas (CDs) constituem uma nova classe de excipientes farmacêuticos com capacidade para formar complexos de inclusão reversíveis com moléculas apolares. A habilidade das CDs em encapsular fármacos tem conseguido melhoras na biodisponibilidade, estabilidade e segurança de inúmeras fórmulas farmacêuticas atualmente comercializadas. Esta revisão bibliográfica compila os principais procedimentos empregados para a obtenção de complexos de inclusão em solução e em estado sólido utilizando CDs, discutindo seus diferentes aspectos. As técnicas utilizadas para caracterização e controle são analisadas criticamente quanto a suas aportações e limitações. Os aspectos relacionados à sua utilização pela indústria farmacêutica também são abordados
Cyclodextrins (CDs) have found application in a new family of pharmaceutical excipients with the ability to form reversible inclusion complexes with non-polar molecules. CDs capable of encapsulating drugs have led to improvements in the bioavailability, stability and safety of several dosage forms on the market. The main procedures employed to produce CD inclusion complexes, both in dissolved and solid forms, are brought together in this review of the literature and several aspects of these methods are examined. The techniques used in research and quality control of CD formulations are analysed critically with respect to their particular features and limitations. Aspects of their use in the drugs industry are also discussed.
Subject(s)
Cyclodextrins/pharmacokinetics , Pharmaceutic Aids , Biological AvailabilityABSTRACT
A vaginose bacteriana é a mais comum das infecções do trato genital feminino.O metronidazol, droga de escolha no tratamento, possui boa resposta terapêutica, mas, devido à sua toxicidade após doses contínuas, tem sua capacidade de combate e reversão da doença limitada pela efemeridade do tratamento.Desenvolveu-se a forma farmacêutica comprimido matricial bioadesivo vaginal contendo metronidazol que levou em conta, tanto a redução das quantidades administradas da droga, quanto o uso de atributos que desfavoreçam a permanência da flora patógena no meio vaginal, como a liberação prolongada e a acentuada adesão da forma à mucosa.Foram obtidos durante o estudo três formulações chamadas de lotes de bancada (LB I, LB II e LB III) com variações quali-quantitativas dos excipientes utilizados.Nos LB I e LB II utilizou-se o hidropropilmetilcelulose e carbopol como constituintes da matriz, porém no LB III foi utilizado uma composição de hidropropilmetilcelulose, etilcelulose e carbopol.As formulações apresentaram resultados dentro das especificações frente aos testes físico-químicos habituais de acordo com a Farmacopéia brasileira.Os comprimidos LB I e LB II liberaram todo seu conteúdo após seis e 12 horas, respectivamente, a partir de matrizes de caráter notadamente adesivo e ao fim dos ensaios mantiveram-se na forma de pequena estrutura gelificada.Mesmo sob essas condições, e após 48 horas de ensaio, a formulação LB III não liberou todo seu conteúdo, pode-se levar em conta a mudança da natureza dos componentes da matriz assim como a necessidade de um desenvolvimento e validação de método mais específico para dissolução
Subject(s)
Tablets/pharmacology , Drug Delivery Systems , Metronidazole/administration & dosageABSTRACT
An evaluation of cellular alterations in the smoker's oral mucosal cells was performed. The Exfoliative Cytology technique was applied and the cytological smears stained with silver for the enumeration of Argyrophilic nucleolar organizer regions (AgNORs). Cytological smears were collected from two anatomic sites: floor of the mouth and tongue border, in both groups, smokers and non smokers, with a purpose of correlating the smoking habit to possible cellular alterations. The enumeration of the AgNORs showed that the average number of AgNORs is higher in smokers. There is a significant difference (P=0.0001) between smears from the floor of the mouth and from tongue border in the smoking group. In this study, no correlation between number of cigarettes, age and gender was found, but the results suggest that there might be a correlation between the smoking habit and an increased rate of cellular proliferation in the oral mucosal cells.
Subject(s)
Mouth Mucosa/cytology , Nuclear Proteins/chemistry , Nucleolus Organizer Region/chemistry , Smoking/adverse effects , Aged , Case-Control Studies , Cell Division/physiology , Female , Humans , Male , Middle Aged , Mouth Floor/cytology , Silver Staining , Statistics, Nonparametric , Tongue/cytology , Vaginal SmearsABSTRACT
The authors analysed the visceral leishmaniasis (VL) aspects in the state of Maranhão, Brazil, from 1982 to 1993. The disease happens to occur predominantly in São Luís Island (MA) and during the epidemic period, town of São Luís was pointed out as the main endemic area. The greatest frequency of cases occurred in 1993, despite the use of insecticide and dogs control. There was predominance of age between 0- to 4-year-old population with 58.04% of cases. Neither the human disease nor the rainfall index had significant seasonal variation. However they were correlated moderately, with high number of cases after the period of great precipitation of rain. After this study, the data obtained will allow a better control of the disease, despite some factors such as: the urbanization, localization and dynamic of transmission in endemic areas in the Maranhão state.