Abstract Aleurites moluccanus L. (Willd.), Euphorbiaceae, is a tree that is native to Indonesia and India. Various parts of this tree are commonly used in traditional medicine to treat pain, fever, inflammation, hepatitis, gastric ulcer and other ailments. An oral suspension containing dried extract of A. moluccanus was developed and in vivo anti-inflammatory activity was evaluated. Extract 100 and 50 mg/ml loaded oral suspensions were prepared using different suspending agents. The formulations were analysed by their appearance, pH, density, redispersion time, rate of settling, rheological behaviour, distribution of particle size and zeta potential. The dose uniformity was determined by measuring the content of total phenolic compounds expressed in swertisin by a validated HPLC method, as well as the dissolution profile. The stability of oral suspensions was analysed in accelerated studies (40 °C for 6 months). The anti-inflammatory activity was analysed using an in vivo paw oedema model. The taste and odour of the suspensions were shown to be characteristic of the extract. Carmellose sodium (CS; 0.5%) and microcrystalline cellulose and carmellose sodium mixture (MCCS; 1%) showed better physical behaviour. The content of total phenolic compounds was 1.6 mg/ml and approximately 100% of the total phenolic compounds dissolved within 10 min. During the stability study, the formulations were approved by their physical–chemical properties and were shown to lose 12–14% of total phenolic compounds at 40 °C after 6 months. Suspensions containing 50 mg/ml of standardised dried extract inhibited around 35 ± 7.6% of paw oedema. Formulations containing CS showed more anti-inflammatory activity. Suspensions containing dry extract of A. moluccanus were successfully obtained and showed physical and physical–chemistry properties that were appropriate and characteristic of this dosage form, suitable for administration in paediatric and elderly populations, making this an alternative to tablets.

Polygala cyparissias is a plant widespread in Southern Latin America. Recently, we demonstrated the gastroprotective activity of the extract, as well as for one of the isolated metabolites-1,7-dihydroxy-2,3-methylenedioxyxanthone (MDX). In this study, a HPLC method for the quantification of MDX was validated. The HPLC method was linear (0.5-24 µg mL-1 of MDX) with good accuracy, precision and robustness. The content of MDX in the extracts from whole and different parts of the plant ranged from 0 to 5.4 mg g-1 and the gastroprotective index ranged from 72.1 to 99.1%. Thus, the method might be used for the standardization of the extracts based on the MDX marker.

Among other applications, Ipomoea pes-caprae is popularly used to treat jellyfish stings, supporting the development of a product for dermatological use. Hydroethanolic spray-dried extract was chosen for the further development of phytomedicines, and a stability-indicative HPLC-UV method was developed and validated for the determination of isoquercitrin and isochlorogenic acids A, B and C. The method was developed using a C18 column (250 x 4.6 mm, 5 µm) with an acetonitrile:water mobile phase at pH 3.0 in a gradient run. The four constituents and other unidentified components of the extract were appropriately resolved without interference of degradation products after stress tests (acid, alkali, neutral, oxidant, photolysis). The method showed linearity in the isoquercitrin concentration range from 5.0-50.0 µg mL-1, with adequate precision (RSD% < 2.5% for the intra- and inter-day studies), accuracy (recovery of 100.0 ± 2.0%), and robustness. Both the herbal drug and spray-dried extract of I. pes-caprae were subjected to stability studies in accelerated and long-term conditions over four months. The samples maintained their characteristics and marker contents (< 10% of variation).

The pharmaceutical use of galactomannans from different sources, commercial and noncommercial, has been extensively studied over the past decade. Galactomannans show potential in the global trend towards the use of more plant-based products for ecological motives, and their production and application do not cause pollution or disturb the ecosystem. There is a variety of galactomannan sources and various pharmaceutical forms of application, such as tablets or capsules, hydrogels and films. Besides the simple use as inert excipient this polysaccharides play role in the modification of drug release, especially in colonic environmental, as a matrix or coating material.

Formulações de piroxicam com base Lanette® (L) ou Net Fs ® (N), com ou sem promotores de absorção (etanol-E ou propilenoglicol-P), foram desenvolvidas. O estudo de permeação de piroxicam das formulações foi realizado em célula de Franz, usando pele de porco e o desempenho foi comparado com a especialidade farmacêutica. O fármaco permeado foi analisado por método desenvolvido por CLAE usando uma coluna analítica C18 de 15 x 0,46 cm, com fase móvel metanol: tampão fosfato (60:40), comprimento de onda de 354 nm e o tempo de corrida foi de 10 min. O ensaio foi validado e apresentou limite de quantificação de 0,138 mg/mL , linearidade na faixa de 0,02-5 µg/mL e não ocorreu interferência de substâncias endógenas da pele ou da formulação. A ordem de permeação de piroxicam, após 24 horas, foi LE > L> Feldene® > N > LP > NP > NE. As formulações com L mostraram maior permeação de piroxicam quando comparado com as formulações de base N. Entre os promotores, o etanol promoveu a maior permeação do fármaco. Os resultados mostraram o desenvolvimento de formulações tópicas econômicas, de fácil obtenção, com efetiva permeação de piroxicam possibilitando a escolha de formulações com maior ou menor permeação do fármaco.

Formulations of piroxicam in Lanette® (L) or Net Fs® (N) vehicles, with or without permeation enhancers, the ethanol (E) or propylene glycol (P) were developed. The piroxicam permeation through porcine ear skin, in a Franz Cell was evaluated, comparing with a commercial product. The permeate was analyzed by high performance liquid chromatography (HPLC) using a 5 mm C18 column with mobile phase methanol:phosphate buffer (60:40), at 354 nm and the run time of 10 min. This method was validated and the limit of quantification was 0.138 mg/mL, with linearity over 0.02-5 µg/mL, without endogenous skin interference. The order of piroxicam permeation after 24 h was: LE > L> Feldene® > N > LP > NP > NE. The L based formulations showed greater piroxicam permeation compared with N based formulations, particularly up to 10 h of experiment. The ethanol enhancer provided the highest piroxicam permeation. The commercial product shows a different behavior, providing piroxicam permeation almost after 10 h. These results show the development of effective, simple and economic percutaneous formulations of piroxicam allowing the choice of formulations for higher or lower piroxicam permeation.

Os fermentadores tipo air lift oferecem vantagens tais como: eficiente homogeneização dos componentes, baixo cisalhamento e economia de energia, pois o meio é agitado pelo processo de aeração, sem necessidade de agitação mecânica. O objetivo deste trabalho foi analisar a cinética de crescimento de Saccharomyces boulardii neste fermentador, com aeração de 1 e 1,5 vvm (volume de ar por volume de meio, por minuto), comparada com o crescimento em frascos agitados em shaker, visando a futura aplicação deste fermentador, em escala industrial. Os resultados indicaram que houve uma diminuição do pH com o consumo da glicose do meio, a qual foi totalmente consumida até o final da fase exponencial, de 5 e 6 horas para o shaker e o air lift, respectivamente. Após este período houve uma alteração na velocidade de crescimento de S. boulardii, em ambos os equipamentos, indicando uma possível mudança na fonte de carbono utilizada, uma vez que toda a glicose foi consumida após estes períodos. Os valores de velocidades específicas de crescimento foram semelhantes para o shaker e air-lift com 1,0 vvm, porém inferiores ao air-lift com 1,5 vvm, indicando que neste último reator há possibilidades de se conseguir uma velocidade de produção celular maior, dependendo apenas da eficiência de oxigenação oferecida.

This work aimed to analyze the kinetics of S. boulardii growth in an air lift fermentor under two aeration conditions: 1 and 1.5 air vvm (air volume per volume of culture medium per minute), in comparison with growth in shaken flasks, with a view to the future application of this fermenter on an industrial scale. Air lift fermentors offer advantages such as efficient homogenization of the components, low shear stress, and energy savings because the medium is stirred by aeration and does not require mechanical stirring. The pH of the medium decreased with the glucose uptake during the exponential phase, probably due to the formation of secondary metabolites. The entire process showed a similar specific growth rate during the exponential phase (up to 5 hours in the case of the shaker and 6 hours in that of the air-lift fermentor), indicating a possible change in the carbon source, since all the glucose was depleted after the aforementioned periods. After 6 hours, the growth rates in the shaker and the fermentor were similar under 1.0 vvm, but lower than in the fermentor under 1.5 vvm, suggesting that the fermentor may reach a higher cell production rate depending only on the oxygenation efficiency.