ubiquinone and betadex

Coenzyme Q10 (CoQ10) is a naturally occurring compound that plays a fundamental role in cellular bioenergetics and is an effective antioxidant. Numerous health benefits of CoQ10 supplementation have been reported, resulting in growing demands for its use in fortifying food. Due to its insolubility in water, the enrichment of most food products is not easily achievable and its in vivo bioavailability is known to be poor. Water solubility was increased significantly with the use of an inclusion complex with beta-cyclodextrin. This complex is widely used as Q10Vital in the food industry, while its in vivo absorption in humans has not previously been studied.. A randomized three-period crossover clinical trial was therefore performed in which a single dose of CoQ10 was administered orally to healthy human subjects. The pharmacokinetic parameters of two forms of the novel CoQ10 material were determined and compared to soft-gel capsules with CoQ10 in soybean oil that acted as a reference.. The mean increase of CoQ10 plasma concentrations after dosing with Q10Vital forms was determined to be over the reference formulation and the area under the curve values, extrapolated to infinity (AUC(inf)), were also higher with the tested forms; statistically significant 120 and 79% increases over the reference were calculated for the Q10Vital liquid and powder, respectively.. The study revealed that the absorption and bioavailability of CoQ10 in the novel formulations are significantly increased, probably due to the enhanced water solubility.

Topics: Administration, Oral; Adult; Antioxidants; Area Under Curve; beta-Cyclodextrins; Biological Availability; Capsules; Chromatography, High Pressure Liquid; Cross-Over Studies; Female; Food Additives; Humans; Intestinal Absorption; Male; Middle Aged; Solubility; Ubiquinone; Vitamins

Idebenone is a high permeable drug with very slight water solubility that affects the dissolution rate in the biological fluids, causing an irregular and limited in vivo absorption after oral administration. Moreover, it is marketed in Europe as tablets equivalent to 150 mg, with the consequent administration of multiple dose of solid unit to obtain the correct dose, a deterrent for the patients' compliance. According to these considerations, our goal was to develop spray-dried microparticles using a soluble β-cyclodextrin (CD) polymer and an enhancer of dissolution rate, such as carboxymethyl cellulose, to obtain a formulation easily dosable and soluble in water. The complex in solution was evaluated by phase solubility studies and the Idebenone/CD molar ratio selected was 1:1. According to Higuchi and Connors, adding carboxymethyl cellulose, a Bs-type profile was obtained. This result was due to the presence of carboxymethyl cellulose that competes with the CD in forming Idebenone microsystems, reducing of 10-fold the formulation bulk. UV-Vis absorption, (1)H nuclear magnetic resonance and circular dichroism showed the formation of the CD/Idebenone inclusion complex confirmed also by differential scanning calorimetry, Fourier transform infrared spectroscopy and fluorescence microscope (FM). The water solubility data and the in vitro dissolution tests performed in simulated gastric fluid, showed an increase of the drug water interaction due to the presence of the CD and carboxymethyl cellulose, both able to improve drug wettability, water solubility and dissolution rate. This approach seems to be suitable to produce microsystems which are able to enhance the in vivo absorption of Idebenone after oral administration and to increase the patient compliance.

Topics: Administration, Oral; Antioxidants; beta-Cyclodextrins; Cellulase; Chromatography, High Pressure Liquid; Drug Compounding; Drug Stability; Humans; Patient Compliance; Technology, Pharmaceutical; Ubiquinone

The bioavailability of a novel water-soluble inclusion complex of CoQ10, prepared in our laboratory was determined and compared with the bioavailability of commercially available oil-based form of CoQ10. Experimental work consisted of single dose comparative bioavailability study on seven beagle dogs, with a 14-day washout period between treatments. Identification and quantification of CoQ10 was done with HPLC-MS method using positive APCI ionization and SIM mode, M+ m/z 863.4. The bioavailability results confirm that the water-soluble formulation has nearly three times higher AUC(0-48 h), two times higher Cmax, and Tmax is shortened from 6 to 4 h.

Topics: Absorption; Animals; Area Under Curve; beta-Cyclodextrins; Biological Availability; Calibration; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Cross-Over Studies; Dogs; Drug Stability; Half-Life; Mass Spectrometry; Metabolic Clearance Rate; Methanol; Models, Molecular; Quality Control; Reference Standards; Reproducibility of Results; Sensitivity and Specificity; Solubility; Ubiquinone; Vitamins; Water