Pharmaceutical development of tablets containing a spray-dried optimized extract from Lippia origanoides H. B. K.: influence of excipients and toxicological assessment

Lippia origanoides is a honey shrub which has showed hypotensive potential assessed by in vivo studies. The aim of this work is the development of a pharmaceutical formulation composed by an optimized extract obtained from aerial parts of L. origanoides. The quantification of the naringenin marker in the dry extract and tablets developed was performed, as well as the assessment of the oral acute toxicity in rats. The hydroalcoholic extract of L. origanoides was spray-dried with the addition of colloidal silicon dioxide (Lo-HAE/CSD), and then applied in the preparation of eight different lots of tablets. The influence of the diluent (cellulose or babassu mesocarp), the presence of binder, and the percentage of lubricant, as well as organoleptic and physicochemical characteristics were screened. For the quantification of the marker content both in Lo-HAE/CSD and in the tablets, an analytical curve of the naringenin standard was fitted, and the samples were then analyzed in UFLC. The toxicological assessment was performed in female Wistar rats according to the Acute Toxic Class Method from OECD. The developed tablets produced meet acceptable macroscopic characteristics, and the presence of babassu as diluent provided improved physicochemical properties. The best content of Lo-HAE/CSD in the tablet (100.27%) was identified for the lot containing babassu, composed by 1.0% magnesium stearate, without PVP binder in its formulation. Moreover, Lo-HAE/CSD showed no signs of toxicity. Therefore, the babassu mesocarp powder is a promising pharmaceutical excipient for the development of herbal tablets containing the Lippia origanoides extract

PROSPECÇÃO TECNOLÓGICA DE EXTRATOS VEGETAIS EM FORMAS MUCOADESIVAS

O Uso de plantas medicinais para o tratamento de males que afetam a sociedade torna-se vais evidente a cada dia, pois se trata de novos medicamentos de matéria-prima provenientes da natureza sendo mais barata e com menos efeitos colaterais. A presente prospecção tem o intuito de mostrar o potencial e a necessidade de proteger o conhecimento tecnológico a cerca de extratos vegetais na forma mucoadesiva. Vegetais, com diversas matérias-prima disponíveis em nosso país, e poucas propriedades protegidas.</p

Commercial babassu mesocarp: microbiological evaluation and analysis of label information

<p>The babassu mesocarp is easily found in supermarkets and other commercial establishments in Brazil. Despite its widespread use in both pharmaceutical and food industries, the literature has neither scientific studies about microbial contamination for these products nor about legal information expressed on label. The aim of this study was to evaluate the level of microbiological contamination in babassu mesocarp sold in commercial establishments in Teresina-PI/Brazil besides the conformity of label information according to the rules of Brazilian Sanitary Surveillance Agency (ANVISA). Ten samples of babassu mesocarp powder sold in the region were selected for study. Determination of heterotrophic microorganisms was carried out using the seeding technique of Plate Count Agar (CFU g-1). It was used Sabouraud Dextrose Agar medium for cultivation of fungi. For the analysis of label information, the resolutions (RDC), 259 of September 20, 2002, and 360 of December 23, 2003, beyond the law 10,674 of May 16, 2003 were used. The results of levels of contamination for heterotrophic bacteria and fungi showed high contamination for all samples. Most of the label samples were according to the rules. Therefore, the results suggest a more comprehensive monitoring of these microorganisms besides the development of more effective methods for decontamination of these products sold in Brazil.</p><p>Keywords: Babassu. Label. Contamination. Food. Pharmacy.</p><p> </p><p>RESUMO</p><p> </p><p>O mesocarpo de babaçu é encontrado facilmente em supermercados e em outros estabelecimentos comercias e apesar de sua ampla utilização, tanto na indústria farmacêutica e de alimentos, na literatura não há trabalhos científicos que avaliem sua contaminação microbiológica ou informações legais necessárias para rótulos. O objetivo do estudo foi avaliar o nível de contaminação microbiológica do mesocarpo de babaçu, vendidos no comércio de Teresina-PI, bem como verificar a conformidade das informações dos rótulos com as normas da Agencia de Vigilância Sanitária (ANVISA). Foram selecionadas dez amostras do pó comercializadas no mercado regional. Para a determinação de microrganismos heterotróficos foi realizada a técnica de semeadura utilizando o meio Plate Count Agar, para fungos, utilizou-se o meio Sabouraud Dextrose Ágar e para a avaliação dos rótulos tomaram-se como base as resoluções, RDC 259, de 20/09/2002, RDC 360, de 23/12/2003, e a Lei nº10.674, de 16/05/2003. Os resultados dos índices de contaminação para bactérias heterotróficas e fungos mostraram-se bastante elevados. Quanto à rotulagem, a maioria das amostras estava de acordo com as regras. Com os resultados obtidos sugere-se um monitoramento mais abrangente desses microrganismos além do desenvolvimento de métodos de descontaminação mais efetivos para esses produtos comercializados no Brasil.</p><p>Palavras-chave: Babaçu. Rótulos. Contaminação. Alimentos. Farmácia.</p

Pharmaceutical development of tablets containing a spray-dried optimized extract from Lippia origanoides H. B. K.: influence of excipients and toxicological assessment

ABSTRACT Lippia origanoides is a honey shrub which has showed hypotensive potential assessed by in vivo studies. The aim of this work is the development of a pharmaceutical formulation composed by an optimized extract obtained from aerial parts of L. origanoides. The quantification of the naringenin marker in the dry extract and tablets developed was performed, as well as the assessment of the oral acute toxicity in rats. The hydroalcoholic extract of L. origanoides was spray-dried with the addition of colloidal silicon dioxide (Lo-HAE/CSD), and then applied in the preparation of eight different lots of tablets. The influence of the diluent (cellulose or babassu mesocarp), the presence of binder, and the percentage of lubricant, as well as organoleptic and physicochemical characteristics were screened. For the quantification of the marker content both in Lo-HAE/CSD and in the tablets, an analytical curve of the naringenin standard was fitted, and the samples were then analyzed in UFLC. The toxicological assessment was performed in female Wistar rats according to the Acute Toxic Class Method from OECD. The developed tablets produced meet acceptable macroscopic characteristics, and the presence of babassu as diluent provided improved physicochemical properties. The best content of Lo-HAE/CSD in the tablet (100.27%) was identified for the lot containing babassu, composed by 1.0% magnesium stearate, without PVP binder in its formulation. Moreover, Lo-HAE/CSD showed no signs of toxicity. Therefore, the babassu mesocarp powder is a promising pharmaceutical excipient for the development of herbal tablets containing the Lippia origanoides extract