1.
Low-fluoride dentifrice and gastrointestinal fluoride absorption after meals.
Cury, JA, Del Fiol, FS, Tenuta, LM, Rosalen, PL
Journal of dental research. 2005;(12):1133-7
Abstract
A low-fluoride (F) dentifrice has been recommended to reduce the risk of dental fluorosis, but its anti-caries efficacy is questionable compared with that of conventional dentrifices (1000-1100 microg F/g). The tested hypothesis was that conventional dentifrices might be safe if used soon after meals, since food interferes with F absorption. In a crossover, double-blind study, 11 volunteers ingested a dentifrice slurry containing 0 (placebo), 550 (low F), or 1100 microg F/g in 3 gastric content situations: on fasting, or 15 min after breakfast or lunch. F was analyzed in saliva and 24-hour urine samples. The conventional dentifrice ingested after lunch resulted in only 10% higher F absorption than the low-F ingested on fasting. Analysis of the data suggests that the risk of fluorosis could be reduced by the use of either a low-F dentifrice or a conventional dentifrice, if toothbrushing occurred soon after meals.
2.
Absorption pattern of trospium chloride along the human gastrointestinal tract assessed using local enteral administration.
Schröder, S, Jetter, A, Zaigler, M, Weyhenmeyer, R, Krumbiegel, G, Wächter, W, Fuhr, U
International journal of clinical pharmacology and therapeutics. 2004;(10):543-9
Abstract
BACKGROUND AND OBJECTIVES The antimuscarinic drug trospium chloride is hydrophilic and therefore does not enter the CNS when used for the treatment of overactive bladder disturbances. However, the same property is the main reason for low and variable oral bioavailability. The present study was performed to assess the influence of intestinal site on absorption of the drug as the basis for the development of modified release preparations. METHODS In a change-over pilot study, 8 healthy male volunteers received single 20 mg doses oftrospium chloride orally as a tablet (reference), as Eudragit-coated tablets dissolving at pH 6.0 (local administration into the small intestine), and rectally via a mini enema (corresponding to local administration into the large intestine). Plasma concentrations of trospium chloride were determined up to 36 hours after administration using GC/MS. RESULTS Extent and rate of trospium chloride absorption declined rapidly upon administration into more distal regions of the gastrointestinal tract. C(max) (median: 6.42 ng/ml) and AUC(0.tlast) (42.28 ng/ml x h) were highest and t(max) (3.5 h) was shortest after administration of the reference tablet. AUC(0-tlast) reached 78% (90% CI 43 - 139%) after small intestine administration and 2% (90% CI 1 - 9%) following rectal administration, respectively, relative to the values for the oral tablet. CONCLUSION Trospium chloride is absorbed primarily in the upper gastrointestinal tract. Development of modified release preparations must balance prolonged apparent absorption rates of the drug against a decrease in bioavailability.