Metformin hydrochloride entrapment in sorbitan monostearate for intestinal permeability enhancement and pharmacodynamics

Penetration enhancement of metformin hydrochloride via its molecular dispersion in sorbitan monostearate microparticles is reported. This represents basic philosophy to maximize its entrapment for maximum penetration effect. Drug dispersion in sorbitan monostearate with different theoretical drug contents (TDC) were prepared. Products showed excellent micromeritics and actual drug content (ADC) increased by increasing TDC. The partition coefficient of the drug products showed huge improvement. This indicates the drug entrapped in the polar part of sorbitan monostearate as a special image which effects on the drug release. The drug permeation profiles from the different products are overlapped with nearly equal permeation parameters. The permeation results suggested the main driving force for improving the drug paracellular pathway is its dispersion in sorbitan monostearate and is independent of ADC. Pharmacodynamic of the products showed a significant improvement than the drug alone at p ˂ 0.05. ANOVA test indicated the insignificant pharmacodynamic difference between the low, middle, and high ADC of the products. An excellent correlation founded between the drug permeation and pharmacodynamic precents. Drug permeation driving force via the paracellular pathway is its entrapment in sorbitan monostearate and independent on ADC. The technique is simple and the products had excellent micromeritics.

Penetration Driving Force of Metformin Hydrochloride via Paracellular Pathway in Relation to its Pharmacodynamic Effect

Background: Penetration enhancement of metformin hydrochloride via its molecular dispersion in sorbitan monostearate microparticles is reported. Metformin dispersion in sorbitan monostearate as a carrier was thought to be the basic philosophy to maximize its entrapment in the matrix for maximum penetration effect.Methods: Drug dispersion in sorbitan monostearate with different theoretical drug contents (TDC) were prepared. Results: All products showed excellent micromeritics and actual drug content (ADC) increased by increasing TDC. These two features are essential for industry concerning processing and cost. The partition coefficient of the drug products showed huge improvement. This indicates the drug entrapment should be in the polar part of sorbitan monostearate as a special image. The drug entrapment process was also reflected in the drug release process due to the insolubility of the matrix in the dissolution medium. The drug permeation profiles from the different drug-sorbitan monostearate products are overlapped and its permeation parameters (permeation coefficient, total drug permeation percent & drug absorption enhancement percent) are nearly equal. The results of the permeation study by using modified non-everted sac suggested the main driving force for 11 improving the drug paracellular pathway is its dispersion in sorbitan monostearate (special image) and is independent of ADC. Pharmacodynamic of the drug products showed a significant improvement than that from the drug alone at p ˂ 0.05. ANOVA test indicated the insignificant pharmacodynamic difference between the low, middle, and high ADC of the products. There is an excellent point-to-point correlation between the drug permeation percent and the drug pharmacodynamic percent. The total amount of the drug permeation percent is equal to the mean of the total drug pharmacodynamic percent. Conclusion: The results concluded that the drug permeation driving force via the paracellular pathway is its entrapment in sorbitan monostearate as a special image and it does not depend on ADC. This entrapment mechanism improved the drug pharmacodynamic effect. The technique is simple and the products are easy to process due to having an excellent micromeritics property.

Stability, Viscosity, and Tribology Properties of Polyol Ester Oil-Based Biolubricant Filled with TEMPO-Oxidized Bacterial Cellulose Nanofiber

This research is aimed at studying the stability and tribology properties of the polyol ester oil- (POE-) based biolubricant mixed with various filler loadings from microparticle of TEMPO-oxidized bacterial cellulose (NDCt) as an additive and sorbitan monostearate (Span 60) as a surfactant. Morphology, rheology, and tribology tests were conducted. The addition of NDCt and Span 60 to pure POE as a base fluid showed elevated viscosity, lower value of coefficient friction (COF), and a remarkable decrease in the wear rate (WR). The presence of 0.6 wt% NDCt and 1.8 wt% Span 60 in POE (N2S4) decreased the COF value by 79% in comparison to POE. At room temperature, this N2S4 biolubricant sample showed a higher thermal conductivity by 4% and lower WR value by 49% compared to POE. This study introduced the preparation of the ecofriendly biolubricant filled with NDCt improving the tribology properties remarkably.

Effect of emulsifiers on viscosity and emulsion stability of the cocoa powder mixture

The study was initiated to generate data on the effectiveness of emulsifiers in the cocoa mixture (use as a beverage) with the suitable cocoa butter content remaining in cocoa powder. The experimental designs and comparative analyses will provide the information and knowledge needed in using emulsifiers for improving cocoa powder dispersibility, through viscosity and emulsion stability analysis. The present study was conducted to improved cocoa powder mixtures which have good dispersibility in liquids. Emulsifier of four types (polysorbate, sorbitan monostearate, lecithin from egg yolk/vegetable oil) with the concentrations ranging from 0.25 to 0.7% on the viscosity and emulsion stability of cocoa powder (16 and 20% of cocoa butter contents remained in cocoa powder) were investigated. The obtained results showed that stabilizer levels markedly affected the viscosity and emulsion stability of whipped mixture which increased with higher levels of emulsifiers and cocoa butter contents. The dispersibility of cocoa powder can be significantly increased by adding emulsifiers with the best results achieved at 0.572 and 0.668% of sorbitan monostearate and polysorbate, respectively, in comparison with lecithin. The organoleptic evaluation on the cocoa powder samples also showed there were significant differences (P0.05) in the sensory attributes of the product at this concentration. This sample was adjudged the best based on the overall acceptance.

PREPARATION OF OLIVE OIL EMULSIONS IN AQUEOUS SOLUTIONS STABILIZED BY OC-20 AND SPAN-60

Методом определения температуры инверсии фаз (ТИФ) получены и исследованы обратные эмульсии оливкового масла в воде с применением в качестве стабилизаторов неионогенных поверхностноактивных веществ синтанола OC-20, сорбитана моностеарата Span 60 и их смесей. Reverse emulsions of olive oil in water with the use of non-ionic surfactants syntanol OC-20, sorbitan monostearate Span 60 and their mixtures as stabilizers were obtained and studied by the method of determining the temperature of phase inversion (TIF).

Thermal Triggered Release of Menthol from Different Carriers: A Comparative Study

The design of appropriate thermally responsive fragrance carrier systems is of significant importance for the application of fragrance in the food and tobacco industries. In this study, we investigate the potential of sorbitan monostearate and guar gum for the stabilization of menthol under ambient conditions and the thermally-induced release of menthol. Our results show that the sorbitan monostearate carrier could well stabilize the menthol for at least up to 15 days with neglectable menthol loss due to the favorable binding of menthol on the sorbitan monostearate carrier. In addition, rapid and controlled release of menthol could take place at a temperature of 80 °C in the sorbitan monostearate carrier system. As a comparison, guar gum could not stabilize menthol as a result of its poor compatibility. Our results suggest that sorbitan monostearate can be an ideal carrier material for the support of fragrance. In addition, our results also provide a useful guide for the tailored design of thermally responsive fragrance carriers.