Recebido em 23/9/11; aceito em 27/11/11; publicado na web em 28/2/12Prior to obtain a standardized dried extract from V. ferruginea, lupeol was first time isolated from leaves and used as chemical maker. An analytical method using HPLC-PDA for lupeol determination in V. ferruginea intermediate products was developed using a C8 reverse-phase column, acetonitrile-acetic acid (99.99:0.01, v/v) as mobile phase at 0.8 mL min -1 , oven temperature at 23-25 °C, sample injection volume at 30 μL and detection at 210 nm. The method presented linearity from 10 to 160 μg mL -1 , accuracy, precision, robustness and suitable sensitivity proving to be a useful tool to the obtainment process of lupeol standardized dried extracts of V. ferruginea.Keywords: quality control; triterpene; standardized dried extract.
INTRODUCTIONPharmaceutical companies have a special interest in herbal dried extracts since that its use in pharmaceutical formulations has advantages compared to the powdered plant and conventional fluid forms, such as greater chemical, physical-chemical and microbiological stabilities, easier standardization, higher concentration of active compounds and higher processing capacity in different types of solid dosage forms. 1 However, the chemical complexity inherent to phytopharmaceuticals turns its quality control a complex task. 2 Therefore, the establishment of validated analytical methods plays an important role on the quality assurance of both herbal raw material and intermediate products, 3 allowing at least its standardization on the content of active principles.The Vernonanthura ferruginea (Less.) H. Rob., known as Assapeixe in Brazil, is a plant widely used in folk medicine and it has showed antiulcer activity in preclinical studies. 4 In our laboratory, the same activity was observed to the spray dried extract of V. ferruginea leaves. 5 Despite the pharmacological potential of this plant, efforts to develop a technological product that aims to increase its effectiveness in therapeutic application has been not yet observed.The lupeol is a pentacyclic triterpene commonly found in species of the Asteraceae family, mainly in the typical Vernoniinae. 6,7 It has been known that lupeol has a number of important bioactivities, 8 among them its gastroprotective effect. 9 The lupeol has also been identified as the active principle of Vernonia polyanthes (Less.) antiulcerogenic activity. 10 Although the literature reports several methods for the quantification of lupeol, [11][12][13] no studies of the isolation and quantification of lupeol on the V. ferruginea species have been reported.In order to obtain a standardized dried extract of V. ferruginea, the aims of this work were to isolate a majority compound with an important biological activity to be used as the chemical marker for this species. And then, develop and validate an analytical method for quantitative determination of this compound in V. ferruginea intermediate phytopharmaceutical products.
RESULTS AND DISCUSSION
Isolation and identification of lupeolThe phy...
A 2³ full factorial design was used to assess the impact of spraying air flow rate (30-50 L/min), drying air inlet temperature (90-150 ºC) and extract feed rate (4-6 g/min) on the quality of Eugenia dysenterica DC., Myrtaceae, spray-dried extracts. Response surface methodology (RSM) was applied to analyze the significance of the effects of process factors on product quality and to obtain fitted equations to predict dry powder properties. Powder yields were satisfactory, ranging from 34.64 to 63.92%. The dried products showed moisture contents and water activities below 5% and 0.5, respectively. The recuperation ratios of total polyphenols, tannins and flavonoids ranged from 88.66 to 99.07%, 70.38 to 81.87% and 74.51 to 98.68%, respectively. Additionally, in some conditions the parameters related to dry product’s flowability and compressibility varied over a range acceptable for pharmaceutical purposes. RSM proved that studied factors significantly affected most of the quality indicators at different levels. The spray drying technology is an attractive and promising alternative for the development of intermediate phytopharmaceutical products of E. dysenterica
Our results demonstrated that S. umbellatum decreased the viability of EAT cells using both methods. Morphological analyses revealed that S. umbellatum-treatment induced EAT cell death by apoptotic pathway. We demonstrated the occurrence of reactive oxygen species (ROS) overgeneration, increased intracellular Ca(2+) concentration, alteration in mitochondrial membrane potential, phosphatydylserine externalization, and activation of caspases 3, 8, and 9. However, S. umbellatum produced myelotoxicity in bone marrow cells in a concentration-dependent manner. In comparison to EAT cells, the effects of S. umbellatum in bone marrow cells were 8-fold lower. Taken together, our results showed that S. umbellatum induced apoptosis in EAT cells at several levels and seems more toxic to tumor cells than to normal bone marrow cells.
Aims
The objective of the current study was to evaluate paediatric dosing regimens for meropenem plus fosfomycin that generate sufficient coverage against multidrug‐resistant bacteria.
Methods
The physiologically based pharmacokinetic (PBPK) models of meropenem and fosfomycin were developed from previously published pharmacokinetic studies in five populations: healthy subjects of Japanese origin, and healthy adults, geriatric, paediatric and renally impaired of primarily Caucasian origins. Pharmacodynamic (PD) analyses were carried out by evaluating dosing regimens that achieved a ≥90% joint probability of target attainment (PTA), which was defined as the minimum of the marginal probabilities to achieve the target PD index of each antibiotic. For meropenem, the percentage of time over a 24‐hour period wherein the free drug concentration was above the minimum inhibitory concentration (fT > MIC) of at least 40% was its PD target. The fosfomycin PD index was described by fAUC/MIC of at least 40.8.
Results
For coadministration consisting of 20 mg/kg meropenem q8h as a 3‐hour infusion and 35 mg/kg fosfomycin q8h also as a 3‐hour infusion in a virtual paediatric population between 1 month and 12 years of age with normal renal function and a corresponding body weight between 3 and 50 kg, a joint PTA ≥ 90% is achieved at MICs of 16 and 64 mg/L for meropenem and fosfomycin coadministration, respectively, against Klebsiella pneumoniae and Pseudomonas aeruginosa.
Conclusion
The current study identified potentially effective paediatric dosing regimens for meropenem plus fosfomycin coadministration against multidrug‐resistant bacteria.
Instruction:Despite the increased use of Brosimum gaudichaudii roots as raw material on medicine to treatment of vitiligo, there are not studies that showing the impact of unit operations on the quality and standardized of the extract of B. gaudichaudii. The quality of the herbal extract is essential to ensure the safety and efficacy of pharmaceutical product. Due the medical and commercial importance, this study aimed to evaluate the impact of the extraction method (ultrasound or percolation) on the quality of herbal extract and optimize the extraction of psoralen and 8-methoxypsoralen (8-MOP) from B. gaudichaudii.Materials and Methods:The extraction recovery was evaluate by high-performance liquid chromatography (C8 reverse phase column and acetonitrile: Water 45:55 and flow rate 0.6 mL/min). The extraction was performed by ultrasound-assisted extraction (UEA) or percolation using a Box-Behnken design.Results:From both chemical markers (psoralen and bergapten), the optimal conditions for the UEA were an extraction time of 25 min, the mean particle size of 100 μm, and an ethanol: Water ratio of 55:45 (v/v).Conclusion:The extraction by percolation revealed that ethanol 55% was more efficient than ethanol 80% to extract psoralen and bergapten.
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