Preparation and Evaluation of Self-Microemulsifying Drug Delivery System Containing Vinpocetine

The main purpose of current investigation is to prepare a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of vinpocetine, a poorly water-soluble drug. Suitable vehicles were screened by determining the solubility of vinpocetine in them. Certain surfactants were selected according to their emulsifying ability with different oils. Ternary phase diagrams were used to identify the efficient self-microemulsifying region and to screen the effect of surfactant/cosurfactant ratio (K_m). The optimized formulation for in vitro dissolution and bioavailability assessment was oil (ethyl oleate, 15%), surfactant (Solutol HS 15, 50%), and cosurfactant (Transcutol^® P, 35%). The release rate of vinpocetine from SMEDDS was significantly higher than that of the commercial tablet. Pharmacokinetics and bioavailability of SMEDDS were evaluated. It was found that the oral bioavailability of vinpocetine of SMEDDS was 1.72-fold higher as compared with that of the commercial tablet. These results obtained demonstrated that vinpocetine absorption was enhanced significantly by employing SMEDDS. Therefore, SMEDDS might provide an efficient way of improving oral bioavailability of poorly water-soluble drugs.     

Pharmaceutical applications of hot-melt extrusion: Part II

The advent of high through-put screening in the drug discovery process has resulted in compounds with high lipophilicity and poor solubility. Increasing the solubility of such compounds poses a major challenge to formulation scientists. Various approaches have been adopted to address this including preparation of solid dispersions and solid solutions. Hot-melt extrusion is an efficient technology for producing solid molecular dispersions with considerable advantages over solvent-based processes such as spray drying and co-precipitation. Hot-melt extrusion has been demonstrated to provide sustained, modified, and targeted drug delivery. Improvements in bioavailability utilizing the hot-melt extrusion technique demonstrate the value of the technology as a potential drug delivery processing tool. The interest in hot-melt extrusion technology for pharmaceutical applications is evident from the increasing number of patents and publications in the scientific literature. Part II of this article reviews the myriad of hot-melt extrusion applications for pharmaceutical dosage forms including granules, pellets, tablets, implants, transmucosal, and transdermal systems.     

Ruminal degradability and lysine bioavailability of soybean meals and effects on performance of dairy cows

Evaluations of 4 soybean meal (SBM) products were conducted in 3 experiments. The 4 products were 1) solvent SBM (SSBM), 2) SSBM treated with 0.05% baker's yeast and toasted at 100°C (YSBM), 3) expeller SBM (ESBM), and 4) lignosulfonate-treated SBM (LSBM). Multiparous Holstein cows (n = 32; 152 ± 63 d in milk; body weight = 708 ± 77 kg; producing 41 ± 7 kg/d of milk at the beginning of the study) were used in a 4 × 4 Latin square design with 28-d periods to investigate cow responsiveness to supplemental ruminally undegradable protein (RUP) from the SBM products. Dietary treatments were formulated by substituting all of the SSBM and part of the ground corn with YSBM, ESBM, or LSBM to yield isonitrogenous diets. Diets were formulated to provide adequate ruminally degradable protein, but deficient RUP and metabolizable protein supplies. No differences among dietary treatments were observed for dry matter intake, body weight gain, milk and component yields, or efficiency of milk production. The lack of response to changes in SBM source was likely due to an adequate RUP and metabolizable protein supply by all the diets. In situ ruminal degradations of YSBM and LSBM were slower than those of SSBM or ESBM; thus, RUP contents of YSBM and LSBM were greater than those of SSBM or ESBM. The RUP of all SBM products had similar small intestinal digestibility. Available Lys contents, estimated chemically or by using a chick growth assay, were less for YSBM and LSBM than for SSBM or ESBM, suggesting deleterious effects of processing on Lys availability in YSBM and LSBM.     

Food content, processing, absorption and metabolism of onion flavonoids

The question as to how far the development of chronic diseases in humans depends on diet still remains open. Simultaneously, epidemiological studies suggest the consumption of a flavonoids rich diet might decrease the risk of degenerative changes and certain diseases. The intake of this group of compounds as to quality and quantity depends on dietary habits and a widespread presence of quercetin in the diet makes this compound one of the key factors. Onion, one of the richest and most common quercetin sources, was particularly often studied in different aspects. Quercetin is present in onion mainly as glycosides, of which the distribution within the onion bulb changes in onion processing, and biological activities attracted a lot of attention. Especially antioxidative activity demonstrated in vitro was initially associated with most of the beneficial effects of quercetin on the human body. However, after ingestion quercetin undergoes extensive metabolism and microbial action resulting in its altered or degraded structure; therefore, most of the effects shown in in vitro experiments with the pure compound cannot be directly extrapolated to in vivo systems. Yet, this does not mean that quercetin simultaneously loses its positive impact on consumer health. Even after being metabolized it may still affect the redox balance by inducing antioxidative and detoxifying enzymes or compounds which may be involved in sustaining homeostasis.     

Epigallocatechin-3-gallate (EGCG) for Clinical Trials: More Pitfalls than Promises?

Epigallocatechin-3-gallate (EGCG), the main and most significant polyphenol in green tea, has shown numerous health promoting effects acting through different pathways, as antioxidant, anti-inflammatory and anti-atherogenic agent, showing gene expression activity, functioning through growth factor-mediated pathways, the mitogen-activated protein kinase-dependent pathway, the ubiquitin/proteasome degradation pathway, as well as eliciting an amyloid protein remodeling activity. However, epidemiological inferences are sometimes conflicting and in vitro and in vivo studies may seem discrepant. Current knowledge on how to enhance bioavailability could be the answer to some of these issues. Furthermore, dose levels, administration frequency and potential side effects remain to be examined.     

Bioavailability of iron from a heat treated glucose‐lysine model food system: assays in rats and in Caco‐2 cells

The influence of Maillard reaction products (MRP) from glucose–lysine on iron bioavailability was investigated. Equimolar glucose–lysine mixtures (GL, 40% moisture) were heated (150 °C, for 30, 60 and 90 min) to prepare samples GL30, GL60 and GL90, respectively, and were used to study the influence of MRP on iron solubility, iron uptake and transport in Caco‐2 cells and iron balance in rats. After an initial increase with GL30, in vitro iron solubility decreased in the presence of most of the heated samples. The Caco‐2 cell experiments showed that Fe cell content increased in the presence of heated mixtures with respect to GL, whereas transport was less affected. Iron balance was determined in rats fed diets containing the GL30 and GL90 samples (3%) for a 21 day period and compared with that measured in a control group. Consumption of glucose–lysine heated mixtures increased total iron retention, although hemoglobin values decreased. Iron accumulations in organs such as the spleen, kidney and small intestine were observed. Copyright © 2004 Society of Chemical Industry     

Acylated anthocyanins: A review on their bioavailability and effects on postprandial carbohydrate metabolism and inflammation

Anthocyanins, the natural red and purple colorants of berries, fruits, vegetables, and tubers, improve carbohydrate metabolism and decrease the risk factors of metabolic disorders, but their industrial use is limited by their chemical instability. Acylation of the glycosyl moieties of anthocyanins, however, changes the chemical properties of anthocyanins and provides enhanced stability. Thus, acylated anthocyanins are more usable as natural colorants and bioactive components of innovative functional foods. Acylated anthocyanins are common in pigmented vegetables and tubers, the consumption of which has the potential to increase the intake of health-promoting anthocyanins as part of the daily diet. For the first time, this review presents the current findings on bioavailability, absorption, metabolism, and health effects of acylated anthocyanins with comparison to more extensively investigated nonacylated anthocyanins. The structural differences between nonacylated and acylated anthocyanins lead to enhanced color stability, altered absorption, bioavailability, in vivo stability, and colonic degradation. The impact of phenolic metabolites and their potential health effects regardless of the low bioavailability of the parent anthocyanins as such is discussed. Here, purple-fleshed potatoes are presented as a globally available, eco-friendly model food rich in acylated anthocyanins, which further highlights the industrial possibilities and nutritional relevance of acylated anthocyanins. This work supports the academic community and industry in food research and development by reviewing the current literature and highlighting gaps of knowledge.     

载体油对槲皮素纳米乳液理化稳定性和生物利用度的影响

研究载体油种类和体积分数对纳米乳液稳定性和槲皮素生物利用度的影响。以中链甘油三酯（medium-chain triglyceride,MCT）和长链甘油三酯（long-chain triglyceride,LCT）为油相,梨小豆蛋白为乳化剂制备槲皮素负载型纳米乳液。通过光散射粒径分析、Zeta电位、物理稳定性、游离脂肪酸释放率和槲皮素生物利用度探究乳液稳定性。结果表明,与LCT-纳米乳液相比,由MCT制得的槲皮素纳米乳液表现出更高的稳定性和更慢的槲皮素降解速率,油体积分数为5%时,MCT-纳米乳液粒径（（152.80±1.73）nm）小于LCT-纳米乳液（（180.42±1.98）nm）。通过模拟胃肠道模型测得槲皮素的生物保留率在MCT-纳米乳液体系中得到了极大改善。该信息可以促进设计更有效的槲皮素强化的递送系统。     

热加工方式对香菇营养特性和抗氧化活性的影响

为探索科学合理的香菇热处理方式,采用水煮、微波、汽蒸、高温高压、油炸5 种加工方式对香菇进行热处理,通过营养成分含量测定、体外模拟胃肠消化实验以及抗氧化活性分析,研究不同热加工方式对香菇营养特性、生物利用度和抗氧化活性的影响。结果表明,水煮、油炸和微波处理总体显著降低了香菇中多糖、总膳食纤维、蛋白质、总酚含量以及1,1-二苯基-2-三硝基苯肼自由基清除率和还原力（P＜0.05）,而汽蒸和高温高压处理对上述指标总体无显著影响或略有提高。水煮使香菇麦角甾醇的含量升高30.22%,而油炸导致其降低24.00%,微波、汽蒸和高温高压处理对其无显著影响。5 种热加工方式总体都能显著提高香菇中多糖、蛋白质和总酚的生物利用度（P＜0.05）,热加工后的香菇蛋白质含量与其生物利用度呈极显著负相关（P＜0.01）,而多糖和总酚含量与其生物利用度无显著相关性（P＞0.05）。热加工后香菇抗氧化活性与其多糖、总膳食纤维和总酚含量呈显著正相关（P＜0.05或P＜0.01）。总体来看,汽蒸和高温高压处理有利于香菇营养成分和抗氧化活性的保留和提高。本研究为科学合理地加工、烹饪、食用香菇及其他食用菌提供了一定的参考。     

Effects of polymerization of casein and sources of lysine on amino acid bioavailability among calves fed liquid-based diets

Two experiments were conducted to evaluate the bioavailability of AA between polymerized and less polymerized or unpolymerized sources of AA. In the first experiment, 6 bull calves (53.8 ± 0.6 kg of body weight) were bottle-fed milk replacer that contained 0, 60, or 120 additional grams of AA from casein or acid hydrolyzed casein every 12 h. Plasma essential AA increased linearly with increasing intake of casein from either source. Branched-chain amino acids accounted for 74% of increases in essential AA, regardless of source of AA. Concentrations of nonessential AA increased linearly with increased intake of AA from acid hydrolyzed casein but only tended to increase in response to casein. Also, the rate of increase in total plasma AA concentration in response to acid hydrolyzed casein (4.3 µM increase per g of supplemental AA) tended to be 145% greater than casein (3.0 µM per g of supplemental AA). In a separate experiment, 6 additional bull calves (52.1 ± 0.9 kg of body weight) were bottle-fed milk replacer that contained 0, 4.8, or 9.6 additional grams of Lys from ε-polylysine or Lys-HCl each 12 h to measure Lys bioavailability between a polymerized and unpolymerized source of Lys. Plasma Lys concentrations increased linearly in response to greater Lys intake from Lys-HCl (slope = 13.51 µM/g Lys,), but plasma Lys concentrations did not change in response to increased intake of Lys from ε-polylysine. Plasma concentrations of Thr, Met, Glu, and Gln decreased linearly with increasing ε-polylysine intake, whereas concentrations of His, Val, Leu, and Ile increased linearly with increasing ε-polylysine intake. Data from these experiments suggest that the form of AA provided to calves should be considered when formulating diets to meet AA requirements.