UGT1A1*28 relationship with abnormal total bilirubin levels in chronic hepatitis C patients: Outcomes from a case-control study.

Gilbert syndrome (GS) is a frequent benign clinical condition, marked by intermittent unconjugated hyperbilirubinemia, mostly due to the polymorphism uridine diphosphate-glucuronosyltransferase 1A1*28 (UGT1A1*28). Hyperbilirubinemia has been reported in a GS patient undergoing hepatitis C treatment, and other UGT isoforms polymorphisms have been linked to worse outcomes in viral hepatitis. Yet, little is known to GS contributions' to the liver disease scenario. Our aim was to assess UGT1A1 genotypes' frequency in chronic hepatitis C (CHC) patients and correlate with total bilirubin (TB). This is a case-control study in a large tertiary medical center. Cases were CHC patients confirmed by hepatitis C virus (HCV)-polymerase chain reaction. Exclusion criteria were hepatitis B virus or human immunodeficiency virus (HIV) coinfection. Control were healthy blood donors. UGT1A1 promoter region gene genotyping was performed, and bilirubin serum levels were available for HCV patients. Genotypes and alleles frequencies were similar in case (n = 585; P = 0.101) and control groups (n = 313; P = 0.795). Total bilirubin increase was noticed according to thymine-adenine repeats in genotypes (P < 0.001), and the TB greater than 1 mg/dL group had more UGT1A1*28 subjects than in the group with TB values <1 mg/dL (18.3 vs 5.3; P < 0.001). Bilirubin levels are linked to the studied polymorphisms, and this is the first time that these findings are reported in a chronic liver disease sample. Among patients with increased TB levels, the frequency of UGT1A1*28 is higher than those with normal TB. Personalized care should be considered to GS, regarding either abnormal bilirubin levels or drug metabolism.

Assessment of Adherence to Prescribed Therapy in Patients with Chronic Hepatitis B.

INTRODUCTION: Evidence shows that treatment for hepatitis B virus (HBV) can suppress viral load. Among the factors directly linked to therapeutic success is adherence to the treatment. Several instruments to assess adherence are available, but they are not validated for use in chronic hepatitis B. The purpose of this paper was to adapt and validate the "Assessment of Adherence to Antiretroviral Therapy Questionnaire-HIV" (CEAT-VIH) for patients with chronic hepatitis B (referred to herein as CEAT-HBV). METHODS: The validity of the adapted questionnaire evidence was established through concurrent, criterion, and construct validities. RESULTS: We found negative and significant correlation between the domain "degree of compliance to antiviral therapy" assessed by CEAT-HBV and the Morisky test (r = -0.62, P < 0.001) and between the domain "barriers to adherence" and HBV viral load (r = -0.42, P < 0.001). In terms of the construct's discriminative capacity, scores greater than or equal to 80 detected antiviral therapy success, which are necessary for the prediction of an undetectable HBV viral load. Thus, a cutoff value of 80.5 was set with a value of 81% for sensitivity and 67% for specificity. CONCLUSION: The CEAT-HBV identified 43% (n = 79) non-adherent patients and was shown to be a useful tool in clinical practice.

An effective and biocompatible antibiofilm coating for central venous catheter.

The aim of this study was to investigate the in vitro and in vivo efficacy and the tissue reaction of an antibiofilm coating composed of xylitol, triclosan, and polyhexamethylene biguanide. The antimicrobial activity was analyzed by a turbidimetric method. Scanning electron microscopy was used to evaluate the antiadherent property of central venous catheter (CVC) fragments impregnated with an antibiofilm coating (I-CVC) in comparison with noncoated CVC (NC-CVC) fragments. Two in vivo assays using subcutaneous implantation of NC-CVC and I-CVC fragments in the dorsal area of rats were performed. The first assay comprised hematological and microbiological analysis. The second assay evaluated tissue response by examining the inflammatory reactions after 7 and 21 days. The formulation displayed antimicrobial activity against all tested strains. A biofilm disaggregation with significant reduction of microorganism's adherence in I-CVC fragments was observed. In vivo antiadherence results demonstrated a reduction of early biofilm formation of Staphylococcus aureus ATCC 25923, mainly in an external surface of the I-CVC, in comparison with the NC-CVC. All animals displayed negative hemoculture. No significant tissue reaction was observed, indicating that the antibiofilm formulation could be considered biocompatible. The use of I-CVC could decrease the probability of development of localized or systemic infections.

Reduced activities of phospholipases A2 in platelets of drug-naïve bipolar disorder patients.

OBJECTIVE: Phospholipases A2 (PLA2 ) comprise a family of hydrolytic enzymes that cleave membrane phospholipids and play a key role in cellular homeostasis. Alterations in enzymatic activity have been hypothesized in bipolar disorder (BD). Recent studies suggest that PLA2 activity in platelets may reflect PLA2 activity in the brain. The aim of this study was to determine PLA2 activity in platelets of BD patients. METHODS: We determined the activity of PLA2 subtypes [extracellular, calcium-dependent PLA2 (sPLA2 ), intracellular, calcium-dependent PLA2 (cPLA2 ), and intracellular, calcium-independent PLA2 (iPLA2 )] by a radioenzymatic method in platelets from 20 patients with BD (15 drug-naïve and five drug-free) and from 16 age- and gender-matched healthy controls. RESULTS: We found that iPLA2 , cPLA2 , and sPLA2 activities were lower in drug-naïve patients with BD when compared to the control group (p = 0.017, p < 0.001, and p < 0.001, respectively). CONCLUSIONS: Reduced PLA2 activity at the early stage of BD may disrupt brain function and increase the risk for the disease. Moreover, epidemiological studies show that patients with BD have a fivefold increased risk for developing Alzheimer's disease. Because patients with Alzheimer's disease also have reduced PLA2 activity, the present finding of reduced PLA2 in the BD group may be related to the risk factor for these individuals developing Alzheimer's disease in advanced age.

Relationship between viral detection and turbidity in a watershed contaminated with group A rotavirus.

Enteric viruses are present in aquatic environments due to contamination by raw sewage, even in the absence of fecal coliforms, which are considered to be significant indicators when it comes to microbial water quality assessment. This study investigated the presence of group A rotavirus (RVA) in surface water from a river basin in Minas Gerais, Brazil, assessing the influence of the urbanization, the rainfall, and the microbiological and physico-chemical parameters regarding water quality. Forty-eight surface water samples collected in urbanized and non-urbanized areas, both in dry and rainy periods, were obtained throughout the study. The viral particles were concentrated by adsorption-elution in a negatively charged membrane. Fecal coliforms, as well as physico-chemical water parameters were determined at each point in all collections. The RVA was detected in 62.5 % (30/48) of the water samples through a real-time PCR assay. All the sequenced RVA strains belonged to genotype I1. The RVA was detected in 50.0 % (11/22) of the water samples regarded as being acceptable by current microbiological standards. The presence of the RVA and the viral load were influenced by the collection area (p < 0.05). It was also observed a significant association between the RVA and detecting the turbidity of water (p < 0.05). The collected data showed a high level of contamination in this watershed by the discharge of raw sewage, highlighting the need for urgent measures to improve water quality, ensuring the safe use of this matrix.

Lower phosphorylated glycogen synthase kinase-3B levels in platelets of patients with schizophrenia: increment by olanzapine treatment.

Glycogen synthase kinase-3B (GSK-3B) is involved with important neuronal processes such as cell survival, gene regulation, mood and cognitive performance. This enzyme is inactivated by phosphorylation at the phospho-Ser9 site. We compared GSK-3B levels in patients with schizophrenia to a health control group. The levels of phosphorylated and total GSK-3B in platelets of ten drug-free patients, ten long-term olanzapine treated patients and 20 healthy controls were determined by means of an enzyme immunoassay kit. In drug-free patients, GSK-3B levels were accessed again after 8 weeks on treatment with olanzapine. At baseline, drug-free patients presented lower phosphorylated and total GSK-3B levels than healthy controls (p < 0.05). After 8 weeks on olanzapine treatment, phosphorylated and total GSK-3B levels were significantly increased (p < 0.01). Reduced phospho-Ser9-GSK-3B in schizophrenia may disrupt signal-transduction pathways and influence crucial cellular processes, such as transcription, apoptosis, stress response and cell proliferation. Further studies should clarify whether the increment of GSK-3B phosphorylation by olanzapine is related to its antipsychotic effects.

A fast and cost-effective method for identifying a polymorphism of interleukin 28B related to hepatitis C.

Approximately 170 million people are chronic carriers of hepatitis C virus (HCV). Patients with chronic hepatitis C are currently treated with pegylated interferon and ribavirin (PEG-IFN/RBV). A genome-wide association with PEG-IFN/RBV treatment response and a single nucleotide polymorphism (rs12979860) has been identified near the interleukin 28B gene that encodes interferon-λ-3. In this paper, we describe an innovative, fast, and low-cost multiplex polymerase chain reaction with confronting two-pair primers that detects the rs12979860 polymorphism. The assay is internally controlled and does not require the use of restriction endonucleases or special equipment. Moreover, the assay decreases costs, being about 40% cheaper than direct sequencing methods.

Fermentative production of ribonucleotides from whey by Kluyveromyces marxianus: effect of temperature and pH.

Ribonucleotides have shown many promising applications in food and pharmaceutical industries. The aim of the present study was to produce ribonucleotides (RNA) by Kluyveromyces marxianus ATCC 8,554 utilizing cheese whey, a dairy industry waste, as a main substrate under batch fermentation conditions. The effects of temperature, pH, aeration rate, agitation and initial cellular concentration were studied simultaneously through factorial design for RNA, biomass production and lactose consumption. The maximum RNA production (28.66 mg/g of dry biomass) was observed at temperature 30°C, pH 5.0 and 1 g/l of initial cellular concentration after 2 h of fermentation. Agitation and aeration rate did not influence on RNA concentration (p > 0.05). Maximum lactose consumption (98.7%) and biomass production (6.0 g/l) was observed after 12 h of incubation. This study proves that cheese whey can be used as an adequate medium for RNA production by K. marxianus under the optimized conditions at industrial scale.

Evaluation of inadequate anti-retroviral treatment in patients with HIV/AIDS / Avaliação do uso inadequado de antirretrovirais no tratamento de pacientes com HIV/AIDS

INTRODUCTION: Since the emergence of antiretroviral therapy, the survival of patients infected with human immunodeficiency virus has increased. Non-adherence to this therapy is directly related to treatment failure, which allows the emergence of resistant viral strains. METHODS: A retrospective descriptive study of the antiretroviral dispensing records of 229 patients from the Center for Health Care, University Hospital, Federal University of Juiz de Fora, Brazil, was conducted between January and December 2009. RESULTS: The study aimed to evaluate patient compliance and determine if there was an association between non-adherence and the therapy. Among these patients, 63.8% were men with an average age of 44.0 ± 9.9 years. The most used treatment was a combination of 2 nucleoside reverse transcriptase inhibitors with 1 non-nucleoside reverse transcriptase inhibitor (55.5%) or with 2 protease inhibitors (28.8%). It was found that patients taking lopinavir/ritonavir with zidovudine and lamivudine had a greater frequency of inadequate treatment than those taking atazanavir with zidovudine and lamivudine (85% and 83.3%, respectively). Moreover, when the combination of zidovudine/ lamivudine was used, the patients were less compliant (χ2 = 4.468, 1 degree of freedom, p = 0.035). CONCLUSIONS: The majority of patients failed to correctly adhere to their treatment; therefore, it is necessary to implement strategies that lead to improved compliance, thus ensuring therapeutic efficacy and increased patient survival.

INTRODUÇÃO: A partir do surgimento da terapia antirretroviral, o paciente soropositivo teve sua sobrevida aumentada. A não adesão a essa terapia está relacionada diretamente à falência terapêutica, a qual propicia o aparecimento de cepas virais mais resistentes. MÉTODOS: Foi realizado um estudo retrospectivo e descritivo dos registros de dispensação de antirretrovirais de 229 pacientes do Centro de Atenção à Saúde do Hospital Universitário da Universidade Federal de Juiz de Fora, no período de janeiro a dezembro de 2009. RESULTADOS: Tal estudo teve por objetivo avaliar a adesão do paciente ao tratamento e se houve associação entre a não adesão e a terapêutica. Desses pacientes, 63,8% eram do sexo masculino e apresentavam idade média de 44,0 ± 9,9 anos. Foram realizados 28 esquemas terapêuticos diferentes. Dentre esses, os mais utilizados foram aqueles que combinavam 2 inibidores da transcriptase reversa análogos de nucleosídeos/nucleotídeos com 1 inibidor da transcriptase reversa não análogo de nucleosídeo (55,5%) ou com 2 inibidores de protease (28,8%). Foi verificado que os pacientes em uso de lopinavir/ritonavir ou atazanavir associados à zidovudina e lamivudina apresentaram maiores frequências de tratamento considerado inadequado (85% e 83,3%, respectivamente). Além disso, quando a combinação zidovudina/lamivudina esteve presente no esquema medicamentoso, os pacientes aderiram menos ao tratamento (χ2 = 4,468; grau de liberdade = 1; p = 0,035). CONCLUSÕES: A maioria dos pacientes realizava tratamento considerado inadequado. Portanto, é necessário implementar estratégias que conduzam à melhoria da adesão ao tratamento, a fim de garantir eficácia terapêutica e aumento da sobrevida do paciente.

Xylitol inhibits J774A.1 macrophage adhesion in vitro

The aim of this work was to evaluate the effect of xylitol on J774A.1 macrophage adhesion. Adhesion consisted of a three-hour interval, at room temperature, followed by washing and cell incubation at 37ºC/5 percent CO2/ 48h. Xylitol was used to treat the cells either before (for 24h) or after the cell incubation (for 48h) at 5 percent as final concentration in both the situations. It was found that xylitol was effective in preventing the adhesion in both the conditions in spite of the former being 100-fold greater and significant (p < 0.001). The results pointed to an important xylitol action on macrophage adhesion, which should be further investigated as an inflammatory control.

In vitro inhibition of adhesion of Escherichia coli strains by Xylitol

The present study aimed to evaluate xylitol's antimicrobial and anti-adherence activities on Escherichia coli (ATCC 8739) and on another clinical strain enteropathogenic E. coli (EPEC). In vitro minimum inhibitory concentration (MIC) test and adhesion assays were performed using 0.5, 2.5 and 5.0 percent xylitol. It was found that xylitol did not have antimicrobial properties on these strains. The scanning electron microscopy (SEM) demonstrated that the slides treated with xylitol had a significant reduction in the number of bacilli and the inhibition of microbial adhesion was probably the xylitol's mechanism of action. Xylitol could be a possible alternative on the control of E. coli infections.

Uso contínuo de antipsicóticos modula fosfolipase A2 e glicogênico sintase quinase-3 beta em plaquetas de pacientes com esquizofrenia / Antipsychotics prolonged use modulates phospholipase A2 and glycogen synthase kinase-3 beta in platelets from patients with schizophrenia

Duas enzimas têm-se destacado como possíveis marcadores biológicos periféricos na esquizofrenia: a fosfolipase A2 (PLA2) e a glicogênio sintase quinase-3 beta (GSK-3B). Essas moléculas exercem importante influência na arquitetura e plasticidade celulares, na regulação de vias metabólicas comuns (metabolismo de fosfolípides e via Wnt), em fatores de transcrição, na regulação de genes e na sobrevivência celular. Tais aspectos tornam pertinentes as investigações a respeito da possível participação dessas enzimas na fisiopatologia da esquizofrenia. Foi verificada a atividade de subtipos de PLA2 (método radioenzimático: iPLA2, cPLA2 e sPLA2) e os níveis de GSK-3B total (GSK-3Bt) e fosforilada [p(Ser9)-GSK-3B] (ELISA) em plaquetas de pacientes com esquizofrenia inicialmente livres de tratamento medicamentoso com média de 5 anos de doença (D+5a) (n=10), aos quais foi prescrita a olanzapina. Foi avaliado também um grupo de pacientes livres de tratamento medicamentoso com menos de 6 meses de sintomas psicóticos (D-6m) (n=6) aos quais foi posteriormente prescrito o haloperidol. Esses pacientes foram comparados com um grupo controle (n = 20) e avaliados longitudinalmente após o tratamento descrito por 8 semanas. Um grupo de 40 pacientes com esquizofrenia (tempo médio da doença: 17 anos) com pelo menos 6 meses de tratamento com antipsicótico (clozapina, olanzapina ou haloperidol) foi ainda avaliado. Os sintomas clínicos foram avaliados por meio da Escala de Avaliação das Síndromes Positiva e Negativa (PANSS). Quando comparado com o grupo controle, os pacientes D+5a apresentaram aumento da atividade de iPLA2 (p<0,01) e os pacientes D-6m apresentaram aumento da atividade de sPLA2 (p<0,05). Na avaliação longitudinal, somente a olanzapina diminuiu a atividade de iPLA2, cPLA2 e sPLA2 (p<0,01)...

The enzymes phospholipases A2 (PLA2) and glycogen synthase kinase-3 beta (GSK-3B) are thought to play a role in schizophrenia by influencing cellular architecture and plasticity, common signaling pathways (phospholipids metabolism and Wnt pathway), gene transcription, regulation factors and apoptosis. These aspects motivated the investigation of both these enzymes in schizophrenia. The activities of PLA2 subtypes (iPLA2, cPLA2 and sPLA2 by radio enzymatic method) and the levels of total GSK-3B and phosphorylated GSK-3B [p(Ser9)-GSK-3B] (by immune enzyme assay) were performed in platelets of drug free patients with schizophrenia for average 5 years of disease (D+5y) (n=10), who was lately prescribed with olanzapine and in drug naïve patients with less than 6 months of psychotic symptoms (D-6m) who was lately prescribed with haloperidol. These patients were compared to a control group (n=20) and were longitudinally evaluated after 8 weeks of monotherapy treatment with the prescribed antipsychotic. These enzymes were also investigated in a group of 40 patients with schizophrenia (mean duration of disease: 17 years) who were at least 6 months treated with antipsychotic (clozapine; olanzapine or haloperidol). Psychopathology was assessed with the Positive and Negative Syndrome Scale (PANSS). Patients D+5y presented higher iPLA2 activity than control group (p < 0.01) and patients D-6m presented higher sPLA2 activity than control group (p < 0.05)...

Relative bioavailability of two oral formulations of risperidone 2 mg: A single-dose, randomized-sequence, open-label, two-period crossover comparison in healthy Brazilian volunteers.

BACKGROUND: Risperidone (RSP) is a benzisoxazole antipsychotic agent used to treat schizophrenia and other psychiatric illnesses in adults and children (including those with autism). After oral administration, RSP is completely absorbed from the gastrointestinal tract and undergoes hydroxylation to yield 9-hydroxyrisperidone (9-OH-RSP), an active metabolite that has a pharmacologic profile and potency similar to RSP. OBJECTIVES: The aims of this study were to compare the relative bioavailability of a pharmaceutical-equivalent (test) formulation with a reference formulation of oral RSP 2 mg, both available commercially on the Brazilian pharmaceutical market, and to generate data regarding the oral bioavailability of the tested drug in healthy Brazilian volunteers. METHODS: This single-dose, randomized-sequence, open-label, 2-period crossover study was conducted in healthy Brazilian volunteers from August to December 2008. Subjects were randomly assigned to receive the test formulation followed by the reference formulation or vice versa, with a 30-day washout period between doses. Study drugs were administered after a 12-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at 0 (baseline), 0.25, 0.5, 1, 1.5, 3, 5, 8, 12, 24, 48, 72, 96, and 120 hours after administration. Plasma concentrations of RSP and 9-OH-RSP were determined using LC-MS/MS. The test and reference formulations were to be considered bioequivalent if the 90% CIs for the geometric mean test/reference ratios were within a predetermined range of 80% to 125%, in accordance with the policies of the Brazilian Sanitary Surveillance Agency and the US Food and Drug Administration. Tolerability was determined using clinical assessments, monitoring of vital signs, analysis of laboratory test results, and subject interviews regarding adverse events. RESULTS: A total of 22 subjects were enrolled (11 men, 11 women; mean [SD] age, 32 [12] years [range, 1858 years]; weight, 70.4 [11.9] kg [range, 50-103 kg]; height, 1.67 [0.08] m [range, 1.56-1.80 m]; and body mass index, 25 [4] kg/m(2) [range, 18-29 kg/m(2)]). For RSP, mean (SD) C(max) values were 12.6 (2.7) and 16.0 (2.3) ng/mL for the test and reference formulations, respectively. For 9-OH-RSP, mean Cmax values were 17.8 (1.3) and 21.0 (1.7) ng/mL for the test and reference formulations. The 90% CIs for the mean test/ reference ratios for RSP C(max), AUC(0-120), and AUC(0-∞) were 74% to 82%, 75% to 85%, and 76% to 85%, respectively, and 83% to 87%, 75% to 79%, and 75% to 78% for 9-OH-RSP. The related adverse events (headache, low back pain, drowsiness, standing hypotension, local postvenipuncture ecchymoses, insomnia, nausea, and vomiting) were transient and mild. CONCLUSIONS: This single-dose study found that the test and reference formulations of oral RSP 2 mg did not meet the Brazilian and US regulatory criteria for bioequivalence in these fasting, healthy volunteers. The study formulations appeared to be well tolerated.

Perfil das intoxicações fatais registradas no instituto médico legal de Juiz de Fora - Minas Gerais / Fatal intoxications profile registered in legal medical institute of Juiz de Fora - Minas Gerais

A elevada incidência de intoxicações fatais constitui um grave problema de saúde pública no mundo todo. Dispor de informações nessa área é condição primordial para se traçar estratégias eficazes e efetivas de vigilância sanitária. O objetivo deste trabalho foi estabelecer o perfil dos dados sobre a ocorrência de mortes por intoxicações registradas no Instituto Médico Legal (IML) de Juiz de Fora - MG. Foram coletados dados mediante análise dos laudos deste instituto do período de 1997 a 2007, inclusive. Foram computados 278 óbitos causados por agentes tóxicos. A maioria das intoxicações (86%) ocorreu no município de Juiz de Fora. O perfil da população intoxicada compreendeu homens (76,6%), solteiros (51,1%), com remuneração de até dois salários mínimos (73,4%) e idade entre 31 e 45 anos (47,1%). Dentre as causas de intoxicação identificadas, 86,3% foram intencionais e 13,7% acidentais. O principal agente causador de intoxicação fatal foi o etanol (66,5%), seguido pelo grupo dos inseticidas carbamatos (11,2%) e pelos medicamentos (9,7%). A principal via de exposição foi a oral (95%). O perfil das intoxicações fatais e a aná-lise crítica destas informações poderão contribuir para o norteamento de campanhas de prevenção de intoxicações.

Fatal intoxications constitute a worldwide public health problem. Information on this subject is a major condition to draw effective strategies of sanitary surveillance. The objective of this work was to establish the data profile on the deaths occurrence from intoxications registered at the Legal Medical Institute of Juiz de Fora - Minas Gerais State, Brazil. Data from the period between 1997 and 2007 was collected and analyzed. At sum, 278 deaths caused by poisonous agents were computed. Most of the intoxications (86.0%) happened in the district of Juiz de Fora. The profile of the intoxicated population included men (76.6%), single (51.1%), with remuneration of up to two minimum wages (73.4%) and age between 31 and 45 years old (47.1%). Among the identified intoxication causes, 86.3% were intentional and 13.7% were accidental. Ethanol was the main agent responsible for fatal intoxication (66.5%), followed by the group of the carbamate insecticides (11.2%) and drugs (9.7%). The main exposition route was oral (95.0%). Alcohol, carbamate insecticides and the irrational use of drugs were revealed as the main causes of fatal intoxication in the studied population. The profile and critical analysis of the fatal intoxications will contribute to prevention of intoxications.

Leishmania amazonensis: xylitol as inhibitor of macrophage infection and stimulator of macrophage nitric oxide production.

Xylitol is a sugar alcohol being explored for clinical uses. The aim was to evaluate the effects of xylitol on Leishmania amazonensis-infected J774A.1 macrophages. Macrophages were infected with L. amazonensis for 3h, washed and incubated with 2.5 or 5.0% xylitol for 24, 48, and 72 h at 37 degrees C. Infection indexes for macrophages incubated only in medium were compared to those treated with xylitol. Cell viability and nitric oxide production were determined each time. Xylitol did not affect L. amazonensis or J774A.1 cell viabilities. Xylitol at 5.0% stimulated nitric oxide production by macrophages at 72 h (p<0.01). At 2.5 and 5.0%, xylitol inhibited nitric oxide production by L. amazonensis at 48 h (p<0.05) when compared to control. Infection indexes were significantly lower at 72 h (p<0.05), (16.9% and 9.6%) in cells cultivated with 2.5 and 5.0% xylitol, respectively, compared to control (38.4%). Results suggest a potential leishmanicidal action of the xylitol on infected macrophages.

Cromatografia líquida de alta eficiência aplicada ao controle da qualidade de cis-permetrina em loção capilar / High-performance liquid chromatography applied to the control of the quality of cis-permethrin in capillary lotion

Doenças ectoparasitárias como a escabiose, a pediculose, a tungíase e a larva migrans cutânea são epidêmicas em inúmeras comunidades carentes no Brasil e seu controle efetivo é um desafio para a Saúde Pública. Embora a permetrina seja um dos medicamentos aprovados pelo Food and Drug Administration para o tratamento da pediculose, não há um método oficial disponível para a realização do controle da qualidade deste produto em loção capilar de uso humano. Assim, o objetivo deste trabalho foi desenvolver e validar um método analítico sensível, específico, preciso e exato para esta análise, seguindo os critérios descritos na Resolução no 899/2003 da Agência Nacional de Vigilância Sanitária (ANVISA). A cromatografia líquida de alta eficiência (HPLC) com detector diode array (λ = 235nm) foi empregada na determinação de cis-permetrina em loção capilar, visando implementar um sistema de controle da qualidade em laboratórios analíticos. A cis-permetrina e a substância utilizada como padrão interno (PI), o cloridrato de nafazolina, foram separados em coluna analítica S5W (4,6 x 150mm) Waters Spherisorb® e eluídos isocraticamente (fluxo de 1,2mL/min). A cis-permetrina e o PI foram caracterizados pelos tempos de retenção de 1,52 e 8,66 minutos respectivamente. O método mostrou-se linear na faixa de 1,6 a 127,5µg/mL e, nos estudos de precisão intra e interensaio, foram obtidos coeficientes de variação inferiores a 5%, calculados a partir dos resultados. A exatidão média do método foi de 103%. Os limites de detecção e quantificação foram 1,6µg/mL e 2,4µg/mL respectivamente. A cis-permetrina manteve-se estável por 24 horas à temperatura ambiente; por 15 dias a 4ºC e 30 dias a -20ºC. O método mostrou-se simples e apropriado para a determinação de cis-permetrina em loção capilar.

Parasitic skin diseases such as scabies, pediculosis, tungiasis, and cutaneous larva migrans are epidemic in numerous communities in Brazil and their effective control is a major challenge to public health. Permethrim is one of the medications approved by the Food and Drug Administration to treat pediculosis. However, official methods of quality control for permethrin's use as hair lotion are currently unavailable. Thus, a specific and accurate method was validated using high performance liquid chromatography (HPLC) with a diode array detector (λ = 235 nm) in order to determine cis-permethrin in hair lotion, aiming to establish a systemof quality control in analytical laboratories. Cis-permethrin and naphazolinechloride (internal standard - IS) were separated in an analytical S5W column (4.6 x 150 mm) Waters Spherisorb® and isocratically eluted (flow rate =1.2 mL/min). Cis-permethrin and IS were characterized by their retention times: 1.52 and 8.66 minutes, respectively. The accuracy of this method was 103%. A linear range was detected from 1.6 to 127.5µg/ml and CV < 5% calculated from intra and inter-essay precision results. LOD and LOQ were 1.6µg/mL and 2.4µg/mL, respectively. Cis-permethrin remained stable for 24 hours at room temperature; for 15 days at 4ºC and 30 days at -20ºC. The method was considered simple and suitable for determination of cis-permethrin in hair lotion.