Search results for "Absorption"
showing 10 items of 2701 documents
Enhancing effect of alpha-hydroxyacids on "in vitro" permeation across the human skin of compounds with different lipophilicity.
2005
The percutaneous penetration-enhancing effects of glycolic acid, lactic acid and sodium lauryl sulphate through the human epidermis was investigated using 5-fluorouracil as a hydrophilic model permeant and three compounds belonging to the phenylalcohols: 2-phenyl-ethanol, 4-phenyl-butanol and 5-phenyl-pentanol. The lipophilicity values of the compounds ranged from log Poct -0.95 to 2.89. The effect of the enhancer concentration was also studied. Skin pretreatment with aqueous solutions of the three enhancers did not increase the permeability coefficient of the most lipophilic compound (log Poct = 2.89). For the other compounds assayed, the increase in the permeability coefficients depended …
Skin-PAMPA: a new method for fast prediction of skin penetration.
2011
The goal of this study was to develop a quick, reliable, and cost-effective permeability model for predicting transdermal penetration of compounds. The Parallel Artificial Membrane Permeability Assay (PAMPA) was chosen for this purpose, as it already has been successfully used for estimating passive gastrointestinal absorption and blood-brain barrier permeability. To match the permeability of the rate-limiting barrier in human skin, synthetic certramides, which are analogs of the ceramides present in the stratum corneum, were selected for the skin-PAMPA model. The final skin-PAMPA membrane lipid mixture (certramide, free fatty acid, and cholesterol) was selected and optimized based on data …
Inhibition of skin inflammation by baicalin ultradeformable vesicles.
2016
The topical efficacy of baicalin, a natural flavonoid isolated from Scutellaria baicalensis Georgi, which has several beneficial properties, such as antioxidative, antiviral, anti-inflammatory and antiproliferative, is hindered by its poor aqueous solubility and low skin permeability. Therefore, its incorporation into appropriate phospholipid vesicles could be a useful tool to improve its local activity. To this purpose, baicalin at increasing concentrations up to saturation, was incorporated in ultradeformable vesicles, which were small in size (∼67nm), monodispersed (PI<0.19) and biocompatible, regardless of the concentration of baicalin, as confirmed by in vitro studies using fibroblasts…
Effect of loperamide on jejunal electrolyte and water transport, prostaglandin E 2-induced secretion and intestinal transit time in man
1991
Jejunal perfusion was performed in 12 healthy volunteers to evaluate the dose dependent effects of loperamide on intestinal absorption, stimulated secretion and transit. In 6 volunteers intestinal perfusion of the jejunal segment with isotonic NaCl solution was followed by addition of loperamide in increasing doses (2–8 mg·l−1). The volunteers were pretreated with 1 mg·l−1 prostaglandin E2 (PgE2) in the perfusate before addition of 4 mg·l−1 loperamide. Phenolsulphonphtalein (PSP) boluses (2 ml) were given to measure mean transit time (MTT). Loperamide 2 mg·l−1 converted the minor secretion after perfusion with the standard solution (water −1.45 ml·min−1, Na −0.09 and Cl −0.04 mmol·min−1) to…
Humidity of Anaesthetic Gases with Respect to Low Flow Anaesthesia
1994
It has been demonstrated in an experimental study in swine using the scanning electron microscope that a rebreathing technique utilising minimal fresh gas flowrates significantly improves climatization of anaesthetic gases. Consequently, effects of various anaesthetic techniques on airway climate must be assessed, which covers the need for suitable measuring devices. Basic principles and methods of humidity measurement in flowing anaesthetic gases include gravimetric hygrometry, dew point hygrometry, wet-dry bulb psychrometry, mass spectrometry, spectroscopic hygrometry and electrical hygrometry. A custom-made apparatus for continuous measurement of humidity and temperature in the inspired…
Gastrointestinal disturbances and their management in miglustat‐treated patients
2011
Miglustat (Zavesca®) is approved for the oral treatment of adult patients with mild to moderate type 1 Gaucher disease (GD1) for whom enzyme replacement therapy is unsuitable, and for the treatment of progressive neurological manifestations in adult and paediatric patients with Niemann-Pick disease type C (NP-C). Gastrointestinal disturbances such as diarrhoea, flatulence and abdominal pain/discomfort have consistently been reported as the most frequent adverse events associated with miglustat during clinical trials and in real-world clinical practice settings. These adverse events are generally mild or moderate in severity, occurring mostly during the initial weeks of therapy. The mechanis…
Internal exposure of firefighting instructors to polycyclic aromatic hydrocarbons (PAH) during live fire training
2019
Firefighting instructors in live fire training are inevitably exposed to emissions containing, carcinogenic PAH. The study investigated PAH uptake in a group of firefighting instructors during short-term exposure in live fire training by urinary biomonitoring. Six firefighting instructors (non-smokers) completed five 2 h-training sessions each in a carbonaceous-fired simulation unit using self-containing breathing apparatuses (SCBA). Complying with a minimum time interval of six days between the individual training sessions, the participants provided urine samples before and immediately after, as well as 1, 3, 6, 9, 11, and 18 h after each training session. Samples were analyzed for 10 mono…
Effects of controlled-release on the pharmacokinetics and absorption characteristics of a compound undergoing intestinal efflux in humans
2006
Abstract Objective The number of active pharmaceutical ingredients (API) undergoing inhibitable and saturable intestinal efflux is considerable. As a consequence, absorption and bioavailability may depend on the intestinal concentration profile of the drug and may vary as a function of dose and release rate of the drug from the dosage form. The impact of controlled versus immediate-release on the absorption of P-glycoprotein substrates is currently unknown. Thus, the main focus of the present study was a comparison of the pharmacokinetics of the P-gp model substrate talinolol following administration of immediate-release (IR) and controlled-release (CR) tablets to healthy human volunteers w…
Dose-dependent absorption and elimination of cefadroxil in man.
1991
The pharmacokinetic behaviour of cefadroxil was dose-dependent in healthy male volunteers following the oral administration of single doses of 5, 15, and 30 mg.kg-1. As the dose of cefadroxil increased from 5 to 15 and 30 mg.kg-1, the peak plasma concentrations, normalized to 5 mg.kg-1, decreased significantly from 15.1 to 10.7 and 7.6 mg.l-1, while the corresponding normalized areas under the plasma concentration-time curves from 0 to 2 h decreased significantly from 1258 to 946 and 801 min.mg.l-1. When the same subjects were given 5 mg.kg-1 of cefadroxil together with 45 mg.kg-1 of cephalexin, the absorption of cefadroxil was slowed to a similar or greater extent than with the high dose o…
The Influence of Chitosan on the Oral Bioavailability of Acyclovir-a Comparative Bioavailability Study in Humans
2015
Purpose The effects of chitosan hydrochloride on the oral absorption of acyclovir in humans were studied to confirm the absorption enhancing effects reported for in vitro and rat studies, respectively. Methods A controlled, open-label, randomized, 3-phase study was conducted in 12 healthy human volunteers. Zovirax 200 mg dispersible tablets co-administered with doses of 400 and 1000 mg chitosan HCl were compared with Zovirax only. Results The expected increased absorption of acyclovir was not observed. On the contrary, mean area under the plasma concentration-time curve (AUC0-12 h) and maximal plasma concentration (Cmax) decreased following concomitant chitosan intake (1402 versus 1017 and …