Influence of two dietary fibers in the oral bioavailability and other pharmacokinetic parameters of ethinyloestradiol

García, José Alejos; Fernández, Nélida; Diez, M. José; Sahagún, Ana M.; González, Aranzazu; Alonso, M.L.; Prieto, Carlos; Calle, Ángela P.; Sierra, Matilde

doi:10.1016/s0010-7824(00)00175-x

Cited by 17 publications

(19 citation statements)

References 23 publications

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“…In addition, the results of these studies are variable, reporting increases, decreases or even no modification in the drug concentrations after the fiber administration [15][16][17][18][19][20][21][22][23][24]. Even when the same drug and dietary fiber were used, the data obtained can be contradictory [25][26][27][28].…”

Section: Discussionmentioning

confidence: 99%

“…However, when animals received EE with psyllium, the extent absorbed did not change, but there was a delay in the absorption of the estrogen [16].…”

Section: Introductionmentioning

confidence: 91%

“…There are not many studies regarding this aspect, and the results obtained are controversial: several studies show that fiber can increase the bioavailability of other drugs, other authors find a decrease, or no modification is observed [15][16][17][18][19][20][21][22][23][24][25][26][27][28][29]. The main mechanism of interaction may be that the fiber retains by adsorption part of the administered dose, which would be higher with a very viscous fiber.…”

Section: Introductionmentioning

confidence: 99%

“…In two previous studies performed in female rabbits, it was shown that when EE was administered with two commercial fibers containing a high proportion of insoluble components [(A) wheat bran (76.5%), fiber fruit (12%) and guar gum (2%); (B) Plantago ovata seeds (65%) and P. ovata seed cuticles (psyllium) (2.2%)] [15] or with guar gum [16], the extent of EE absorbed decreased without modifying the rate of absorption. However, when animals received EE with psyllium, the extent absorbed did not change, but there was a delay in the absorption of the estrogen [16].…”

Section: Introductionmentioning

confidence: 99%

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Effect of glucomannan and the dosage form on ethinylestradiol oral absorption in rabbits

González¹,

Fernández²,

Sahagún³

et al. 2004

Contraception

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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 À1 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 C max is 1.4 times lower, AUC 1.9 times lower and that t max is identical (10 min). However, after the administration of fiber in enteric capsules, AUC and C max are higher (4.1 and 7.8 times, respectively) than when the estrogen was administered alone, and also, there is a delay in t max (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. D 2004 Elsevier Inc. All rights reserved.

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Section: Discussionmentioning

confidence: 99%

“…However, when animals received EE with psyllium, the extent absorbed did not change, but there was a delay in the absorption of the estrogen [16].…”

Section: Introductionmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effect of glucomannan and the dosage form on ethinylestradiol oral absorption in rabbits

González¹,

Fernández²,

Sahagún³

et al. 2004

Contraception

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“…Also the time of drug administration in relation to food intake may influence the bioavailability of the drug. Soluble fibres may influence the bioavailability of statins and other drugs by direct binding or by altering luminal pH, gastric emptying, intestinal transit, mucosal absorption and metabolism of the drug (58,82) .…”

Section: Safety Aspects Of Combination Therapy With Soluble Dietary Fmentioning

confidence: 99%

Support of drug therapy using functional foods and dietary supplements: focus on statin therapy

et al. 2010

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Functional foods and dietary supplements might have a role in supporting drug therapy. These products may (1) have an additive effect to the effect that a drug has in reducing risk factors associated with certain conditions, (2) contribute to improve risk factors associated with the condition, other than the risk factor that the drug is dealing with, or (3) reduce drug-associated side effects, for example, by restoring depleted compounds or by reducing the necessary dose of the drug. Possible advantages compared with a multidrug therapy are lower drug costs, fewer side effects and increased adherence. In the present review we have focused on the support of statin therapy using functional foods or dietary supplements containing plant sterols and/or stanols, soluble dietary fibre, n-3 PUFA or coenzyme Q 10 . We conclude that there is substantial evidence that adding plant sterols and/or stanols to statin therapy further reduces total and LDL-cholesterol by roughly 6 and 10 %, respectively. Adding n-3 PUFA to statin therapy leads to a significant reduction in plasma TAG of at least 15 %. Data are insufficient and not conclusive to recommend the use of soluble fibre or coenzyme Q 10 in patients on statin therapy and more randomised controlled trials towards these combinations are warranted. Aside from the possible beneficial effects from functional foods or dietary supplements on drug therapy, it is important to examine possible (negative) effects from the combination in the long term, for example, in post-marketing surveillance studies. Moreover, it is important to monitor whether the functional foods and dietary supplements are taken in the recommended amounts to induce significant effects. Combination therapy: Dyslipidaemia: Statins: Functional foodsThe world market for functional foods (FF) and dietary supplements (DS) is expanding rapidly. In 2010 FF are expected to represent 5 % of the total global food market (1) and the market for DS is estimated at more than $60 billion worldwide (2) . In general, the target population of FF or DS is healthy individuals with slightly elevated risk factors or some physical discomfort. However, due to the fast growing market of FF or DS and the accompanying strong advertising and marketing, also patients on medication may be stimulated to use FF or DS. This may have several consequences for the quality of drug treatment as stated by de Jong et al. with the example of the combined intake of plant sterols and/or stanols and statins (3) . Whereas they addressed the additive effect of plant sterols and/or stanols on reducing LDL-cholesterol values in patients on statin treatment, their main focus was the possible negative aspects of the combination, such as unfavourable effects on patient adherence with drug treatment and increasing the potential for food-drug interactions.In the present review we will focus on the possible beneficial effects that FF or DS may have on drug therapy. Because of the large number of subjects treated suboptimally with statins (hydroxymethylglutaryl Co...

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Delivery of soluble ethinylestradiol complex by pH‐responsive core‐shell composite hydrogel capsules

Gong

Jiang

Gao

et al. 2023

J of Applied Polymer Sci

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Ethinylestradiol (EE) is a potent estrogen widely used to treat diseases such as breast cancer, prostate cancer, and menopausal syndrome. The poor aqueous solubility of EE leads to erratic oral absorption, resulting in suboptimal plasma levels. Developing a formulation to enhance the solubility of EE in the gastrointestinal tract would be beneficial to increase the bioavailability of EE. Thereafter, we prepare diethylenetriamine-β-cyclodextrin/ethinylestradiol (DETA-β-CD/EE) complex, aiming to increase the solubility of EE in water, and design and prepare core-shell composite hydrogel capsules with aldocellulose and hydroxyethyl cellulose as the core and sodium alginate as the shell. The stability, swelling, drug release behavior and biocompatibility of the core-shell hydrogel capsules are carefully investigated. And the results show that the prepared hydrogel capsules have the controlled and sustained release ability of soluble DETA-β-CD/ EE, can achieve pH-responding to intestinal fluid, and are non-toxic to normal human cells.

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Influence of two dietary fibers in the oral bioavailability and other pharmacokinetic parameters of ethinyloestradiol

Cited by 17 publications

References 23 publications

Effect of glucomannan and the dosage form on ethinylestradiol oral absorption in rabbits

Effect of glucomannan and the dosage form on ethinylestradiol oral absorption in rabbits

Support of drug therapy using functional foods and dietary supplements: focus on statin therapy

Delivery of soluble ethinylestradiol complex by pH‐responsive core‐shell composite hydrogel capsules

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