167 research outputs found

    Clinical studies with oral lipid based formulations of poorly soluble compounds

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    This work is an attempt to give an overview of the clinical data available on lipid based formulations. Lipid and surfactant based formulations are recognized as a feasible approach to improve bioavailability of poorly soluble compounds. However not many clinical studies have been published so far. Several drug products intended for oral administration have been marketed utilizing lipid and surfactant based formulations. Sandimmune® and Sandimmune Neoral® (cyclosporin A, Novartis), Norvir® (ritonavir), and Fortovase® (saquinavir) have been formulated in self-emulsifying drug delivery systems (SEDDS). This review summarizes published pharmacokinetic studies of orally administered lipid based formulations of poorly aqueous soluble drugs in human subjects. Special attention has been paid to the physicochemical characteristics of the formulations, when available and the impact of these properties on the in vivo performance of the formulation. Equally important is the effect of concurrent food intake on the bioavailability of poorly soluble compounds. The effect of food on the bioavailability of compounds formulated in lipid and surfactant based formulations is also reviewed

    XAI for time-series classification leveraging image highlight methods

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    Although much work has been done on explainability in the computer vision and natural language processing (NLP) fields, there is still much work to be done to explain methods applied to time series as time series by nature can not be understood at first sight. In this paper, we present a Deep Neural Network (DNN) in a teacher-student architecture (distillation model) that offers interpretability in time-series classification tasks. The explainability of our approach is based on transforming the time series to 2D plots and applying image highlight methods (such as LIME and GradCam), making the predictions interpretable. At the same time, the proposed approach offers increased accuracy competing with the baseline model with the trade-off of increasing the training time

    In Vitro Evaluation of Self-Nano-Emulsifying Drug Delivery Systems (SNEDDS) Containing Room Temperature Ionic Liquids (RTILs) for the Oral Delivery of Amphotericin B

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    Amphotericin B (AmpB), one of the most commonly used agents in the treatment of severe fungal infections and life-threatening parasitic diseases such as visceral Leishmaniasis, has a negligible oral bioavailability, primarily due to a low solubility and permeability. To develop an oral formulation, medium chain triglycerides and nonionic surfactants in a self-nano-emulsifying drug delivery system (SNEDDS) containing AmpB were combined with room temperature ionic liquids (RTILs) of imidazolium. The presence of ionic liquids significantly enhanced the solubility of AmpB, exhibited a low toxicity and increased the transport of AmpB across Caco-2 cell monolayers. The combination of RTILs with a lipid formulation might be a promising strategy to improve the oral bioavailability of AmpB

    Effect of pomegranate juice consumption on biochemical parameters and complete blood count

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    Pomegranate has been used therapeutically for centuries. The aim of the present study was to examine the effects of pomegranate juice (PJ) supplementation on complete blood count (CBC), glucose, blood lipids and C‑reactive protein (CRP) in healthy subjects. A total of 5 males and 5 females (aged 31.8±6.6 years, weighing 66.2±12.9 kg) were randomly assigned into one of two groups and either consumed 500 ml PJ/day or no PJ for 14 days. Blood samples were obtained from participants prior to and following the experimental period. PJ consumption resulted in a significant increase in red blood cell count (P<0.05), hemoglobin levels (P<0.001) and hematocrit levels (P<0.05). Other CBC parameters, glucose, cholesterol, triglycerides, high‑density lipoprotein, low‑density lipoprotein and CRP levels did not significantly change following PJ consumption. These results indicate that PJ intake for a short period of time may result in increased erythropoiesis or decreased degradation without any significant alterations in factors associated with metabolic health and inflammation in healthy individuals