Amounts Of Medium-chain Triglycerides Research Articles

Naturally occurring kaolinite as a sorbent for solid-phase extraction of calcitriol in soft capsules

An environmentally friendly, simple and reliable method to quantify calcitriol in soft capsules was developed. Calcitriol with strong physiological activity has a low content (1.55 μg·g−1) in calcitriol soft capsules. Due to the poor stability of calcitriol, a large amount of medium chain triglycerides (>99.99%) need to be used as excipients to protect it. Herein, to achieve accurate quantification of the active ingredients in the calcitriol soft capsules, removing the interference of fat-soluble matrix is the main challenge. This experiment developed a cost-effective solid-phase extraction (SPE) clean-up method based on natural kaolinite (Kaol), which is followed by liquid chromatography coupled with Photodiode array detector (HPLC-DAD) analysis. In the self-made Kaol-SPE, calcitriol could remain on the Kaol sorbent (Al2O3: 39.5%, SiO2: 46.5% and H2O: 14.0%) by polar interactions, n-π interaction and lewis acid base interaction, whereas the hydrophobic medium chain triglycerides could be sufficiently washed off by n-hexane. Thus, the selective extraction of calcitriol and clean-up of fat-soluble matrix were achieved. Kaol was characterized by Fourier transform infrared spectrometry, scanning electron microscopy, transmission electron microscopy, X-ray diffraction and nitrogen adsorption-desorption. Adsorption isotherms were determined to infer the adsorption mechanism and adsorption capacity of calcitriol on Kaol. The fitting results showed that it was followed Langmuir model and the maximum adsorption capacity was 5.495 mg·g−1 (fast adsorption rate, 1 min). Various parameters such as SPE cartridges, Sorbent dosage (20–120 mg), washing solvent, eluting solvent and its volume (0.2–4.0 mL) were investigated. Under optimized conditions, good linear range was 0.15–2.99 μg∙g−1. Recoveries is satisfactory (98.15–101.64%), and the relative standard deviations (RSDs) are only 1.22%. Minor matrix effect was 96.72%, which was excellent. Moreover, low quantitation limit (LOQ) of calcitriol is 0.015 μg·g−1. This method was further validated to determine the content of calcitriol in different batches of commercial calcitriol capsules. The method can directly process diluted samples without liquid-liquid extraction, and has the feature of automation. Thus, this work provides a simple, convenient and economical platform for the determination of calcitriol in complex matrices on a large scale and promotes natural-based materials in pharmaceutical analysis field.

Oleic acid, hydroxytyrosol and n-3 fatty acids collectively modulate colitis through reduction of oxidative stress and IL-8 synthesis; in vitro and in vivo studies

Our recent study has demonstrated that medium chain triglycerides (MCT) and monounsaturated fatty acids potentiate the beneficial effects of fish oil on risk factors of cardiovascular disease. In the present study, we have investigated the influence of MCT or olive oil on the protective and mucosal healing ability of fish oil in ulcerative colitis using cell simulation and animal models. Caco-2 cells grown in medium chain fatty acids enriched medium has exaggerated t-butyl hydroperoxide induced cell damage, GSH depletion, and IL-1β induced IL-8 synthesis, compared to the cells grown in oleic acid & hydroxytyrosol (OT) enriched medium. Further, combined treatment of cells with eicosapentaenoic acid, docosahexaenoic acid, and OT has remarkably attenuated the cell damage, and IL-8 synthesis, compared to individual treatments. To evaluate the effect of these lipid formulations in vivo, adult Wistar rats were fed diet enriched with high amount of medium chain triglycerides (MCT), virgin olive oil, or their combination with fish oil. Colitis was induced in rats using dextran sulfate sodium (DSS) for 7days followed by 10-days of recovery period. Rats of MCT group exhibit severe disease activity, higher levels of inflammatory cytokines in the colon compared to the olive oil group. Furthermore, there was persistent body weight loss, loose stools, higher levels of inflammatory cytokines in the rats of MCT group, even after DSS was withdrawn from drinking water. Conversely, fish oil has remarkably attenuated the DSS induced alterations in both MCT and olive oil diet groups with significantly greater effect in the olive oil group. Thus, MCT increase the susceptibility to colitis through oxidative damage and IL-8 synthesis in intestinal epithelial cells. The beneficial effects of virgin olive oil could be partially attributed to hydroxytyrosol. Combined treatment of hydroxytyrosol, oleic acid and n-3 fatty acids exhibit huge therapeutic benefits in colitis.

Formation, optical property and stability of orange oil nanoemulsions stabilized by Quallija saponins

Nanoemulsions have the potential to deliver insoluble materials and yet provide a transparent appearance in clear beverage applications. The influence of oil phase composition, phase viscosity and homogenization conditions on the formation, stability and optical properties of orange oil-based nanoemulsions was investigated. The nanoemulsions were formed using Quillaja saponins (QS) and homogenization accomplished using Microfluidization®. The results indicated oil phase composition and viscosity ratio between phases are key parameters determining the mean droplet diameter (MDD) of the prepared nanoemulsions. Orange oil nanoemulsions stabilized by QS showed MDD as small as 67 nm corresponding to turbidity of 71 NTU at dispersed phase concentration of 0.5 mg/g. Lipid phase refractive index showed no effect on turbidity of orange oil nanoemulsions at MDD<150 nm, while MDD was linearly related to the turbidity with MDD ranging from 60 nm to 120 nm. Ostwald ripening was identified as main destabilization mechanism of orange oil nanoemulsions stabilized by QS at the early stage of storage. The rate of Ostwald ripening was reduced with increasing amounts of medium chain triglycerides (MCT) in the dispersed phase. An insoluble material, e.g., ester gum or MCT, was required to form stable orange oil-based nanoemulsions.

Design and characterization of Amoitone B-loaded nanostructured lipid carriers for controlled drug release

Amoitone B, a novel compound chemically synthesized as the analogue of cytosporone B, has been proved to own superior affinity with Nur77 than its parent compound and exhibit notable anticancer activity. However, its application is seriously restricted due to the water-insolubility and short biological half-time. The aim of this study was to construct an effective delivery system for Amoitone B to realize sustained release, thus prolong drug circulation time in body and improve the bioavailability. Nanostructured lipid carriers (NLC) act as a new type of colloidal drug delivery system, which offer the advantages of improved drug loading and sustained release. Amoitone B-loaded NLC (AmB-NLC) containing glyceryl monostearate (GMS) and various amounts of medium chain triglycerides (MCT) were successfully prepared by emulsion-evaporation and low temperature-solidification technology with a particle size of about 200 nm and a zeta potential value of about −20 mV. The results of X-ray diffraction and DSC analysis showed amorphous crystalline state of Amoitone B in NLC. Furthermore, the drug entrapment efficacy (EE) was improved compared with solid lipid nanoparticles (SLN). The EE range was from 71.1% to 84.7%, enhanced with the increase of liquid lipid. In vitro drug release studies revealed biphasic drug release patterns with burst release initially and prolonged release afterwards and the release was accelerated with augment of liquid lipid. These results demonstrated that AmB-NLC could be a promising delivery system to control drug release and improve loading capacity, thus prolong drug action time in body and enhance the bioavailability.

In vivo evaluation of tablets and capsules containing spray-dried o/w-emulsions for oral delivery of poorly soluble drugs

It is recognised that poorly soluble drugs may show an increased oral bioavailability when incorporated in o/w-emulsions. Encapsulating the emulsion lipid droplets in hydroxypropyl methylcellulose (HPMC) by spray drying has been demonstrated to preserve an improved bioavailability releasing lipid droplets from the powder in vivo. However, the spray-dried powder is cohesive and bulky requiring additional processing to improve handling. This was resolved in previous work where a directly compressible dry emulsion formulation was described. The purpose of the present study is to investigate the oral bioavailability resulting from administration of a directly compressible dry emulsion as a tablet and compare it with a HPMC dry emulsion powder and a simple lipid solution. Four female Beagle dogs received a single dose of each formulation containing the same amount of medium-chain triglycerides (MCT) and a model drug, Lu 28-179. Cyclodextrin solutions administered orally and intravenously were used as references. The absolute bioavailability decreased in the order cyclodextrin solution (0.14), HPMC dry emulsion (0.11), technically improved dry emulsion (0.10) and MCT solution (0.06). The directly compressible dry emulsion tablets were concluded to be comparable to a HPMC dry emulsion powder in terms of bioavailability. The lack of statistically significant differences relative to a MCT solution was ascribed to a low and variable absolute oral bioavailability of the model drug.

Consumption of Carbohydrate or Medium- or Long-Chain Triglycerides by Unfed Rats Exerts Different Protein-Sparing Effects

Consumption of nonprotein energy is reported to promote nitrogen retention (the protein-sparing effect). The present study was conducted to determine whether consumption of medium-chain triglycerides (MCT), long-chain triglycerides (LCT) or carbohydrate by unfed rats would exert different proteinsparing effects over 48 h. The amounts of MCT, LCT and carbohydrate were adjusted to be isoenergetic. The control group received only water. The urinary excretion of urea in the groups fed carbohydrate or MCT was significantly lower than in the LCT and control groups within the first 24 h. Urinary excretion of urea in the group fed LCT was similar to that of the control group for the first 24 h but was significantly lower after 48 h. Liver serine dehydratase activities in the groups fed MCT or LCT were similar, although they were significantly lower than in the control group. Serine dehydratase activity in the carbohydrate-fed group was the lowest. Liver L-lysine-2-oxoglutarate reductase activity was significantly lower in the groups fed carbohydrate, MCT or LCT than in the control group. Rats fed MCT had the lowest plasma concentrations of lysine and branched-chain amino acids. However, the plasma concentration of glutamic acid in the rats fed MCT was the highest. These results indicate that rats fed MCT, LCT or carbohydrate exhibit different protein-sparing effects and that the difference between rats fed MCT and those fed LCT is not attributable to differences in amino acid-degrading enzymes. Consumption of MCT may conserve some amino acid-derived nitrogen as glutamic acid.

Further investigations of enhancing effect of medium-chain triglycerides on d-alpha-tocopherol acetate absorption from lecithin-dispersed preparations in rat small intestine.

The effect of medium-chain triglycerides (MCTG) in lecithin-dispersed d-alpha-tocopherol acetate (VEA) preparation on intestinal absorption of VEA was investigated in rats using the in situ loop experiment. When VEA preparations containing soybean phosphatidylcholine (PC) and various amounts of MCTG were administered, the amount of VEA absorbed in 2 h was not significantly different among them. However, the amounts of total VE, sum of VEA and d-alpha-tocopherol (VE), remaining in the luminal fluid and the intestinal tissue were dependent on the MCTG content. Total VE remaining in the intestinal tissue after the administration of a VEA/PC/MCTG (5/16/1 by weight) preparation was nearly twice of VEA/PC (5/16) preparation, although the effect of MCTG varied with the increase or decrease in the MCTG content. Moreover, the increased tissue accumulation of total VE by the VEA/PC/MCTG (5/16/1) preparation resulted in an increase in the plasma VE concentration after the removal of the luminal fluid. No effect of pretreatment with PC/MCTG (1/1) dispersion on the tissue accumulation of total VE from VEA/PC (5/16) preparation was observed. Furthermore, the plasma concentration of VE from VEA and/or VE taken up in the tissue from the VEA/PC preparation was not increased by the treatment with the PC/MCTG dispersion. These results suggest that MCTG should coexist in the luminal VEA preparation to enhance the mucosal uptake. A similar enhancing effect was also observed by the addition of the metabolite of MCTG, a medium-chain fatty acid.(ABSTRACT TRUNCATED AT 250 WORDS)

Absorption of Medium Chain Triglycerides in the Stomach of the Human Infant

SummaryFollowing previous observations that medium chain triglycerides (MCT) are absorbed from the stomach of suckling rats, this study was devoted to studying absorption of MCTs in human infants. Four groups of patients were studied: (a) infants suffering from pyloric stenosis, (b) premature infants, (c) children suffering from cystic fibrosis, (d) infants with miscellaneous conditions. Infant formulae with known amounts of MCT were introduced by gastric tube and samples were removed at 0, 20, 40, and 60 min. In patients with pyloric stenosis there was an 18.1% decrease in MCT during the first 20 min. No significant changes in MCT took place during the subsequent 40 min. A similar response was observed in the group of premature infants. Older infants with miscellaneous diagnoses and children with cystic fibrosis showed an even rate of disappearance of MCT during the 60‐min test period, and ∼30% of the original MCTs present disappeared during this period. We conclude that MCTs are absorbed in the stomach of infants and children. Absorption appears to improve with age. Because MCT are an important constituent of formulae for premature infants and children with defects of small intestinal digestion and absorption of fat, these observations have practical implications.