Effect of glucomannan and the dosage form on ethinylestradiol oral absorption in rabbits.
To the beneficial properties of dietary fiber in human health, several disadvantages can be added as the possible modification of the bioavailability of other drugs when administered by the oral route. In this study, the influence of glucomannan in the oral bioavailability of ethinyl estradiol (EE), when administered to female rabbits in two different dosage forms (enteric capsules and dispersed in water), was established. To carry out the study, three groups of six animals each were used. All animals received 1 mg kg(-1) oral EE, and rabbits in groups 2 and 3 received 1.5 g glucomannan dispersed in water or in enteric capsules, respectively, immediately before EE. When comparing the results obtained after the administration of EE/glucomannan dispersed in water with those obtained after the administration of this estrogen without fiber, we can see that Cmax is 1.4 times lower, AUC 1.9 times lower and that tmax is identical (10 min). However, after the administration of fiber in enteric capsules, AUC and Cmax are higher (4.1 and 7.8 times, respectively) than when the estrogen was administered alone, and also, there is a delay in tmax (20 min). After the administration of glucomannan in the enteric capsule, the fiber forms, as in the stomach, a highly viscous solution in the gut that would limit EE access to the mucosal surface delaying its absorption. However, this effect could be compensated by a reduction of EE metabolism in the intestinal wall, leading to a higher absorption of the estrogen.
González
Aránzazu
A
Area de Farmacología, Universidad de León, 24071-León, Spain.
Fernández
Nélida
N
Sahagún
Ana
A
García
Juan José
JJ
Diez
M José
MJ
Castro
Luis José
LJ
Sierra
Matilde
M
D000042:Absorption; D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003276:Contraceptives, Oral / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004043:Dietary Fiber / Q000494:pharmacology*; D004997:Ethinyl Estradiol / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D008351:Mannans / Q000494:pharmacology*; D011817:Rabbits; D011897:Random Allocation
D003276:Contraceptives, Oral; D004043:Dietary Fiber; D008351:Mannans; C022901:(1-6)-alpha-glucomannan; D004997:Ethinyl Estradiol