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Drug Dev Ind Pharm. 2015 Jan;41(1):170-6. doi: 10.3109/03639045.2013.850716. Epub 2013 Oct 30.

Oral bioavailability and intestinal absorption of candesartan cilexetil: role of naringin as P-glycoprotein inhibitor.

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1
Department of Pharmacology, Vaagdevi Institute of Pharmaceutical Sciences , Warangal, Andhra Pradesh , India .

Abstract

OBJECTIVE:

The aim of the study is to explore the pharmacokinetic behavior of candesartan solid dispersions prepared by different pharmaceutical interventions using P-gp inhibitor in rabbits to validate the effectiveness of naringin as a pharmaceutical excipient in enhancing the oral delivery of lipophilic candesartan cilexetil.

METHODS:

Male albino rabbits (1-1.5 kg) were orally administered pure CAN suspensions and various candesartan solid dispersions (10 mg/kg) with and without naringin (15 mg/kg) and blood samples were collected at specified time points. CAN plasma samples were measured using HPLC.

KEY FINDINGS:

After oral dosing of pure CAN suspension, the mean AUC0-8 h was found to be 0.14 ± 0.09 μgh/ml which was increased significantly, i.e. 0.52 ± 0.13 μgh/ml with freeze-dried solid dispersions in the presence of naringin (p < 0.01). Similarly, the mean Cmax of pure CAN suspension increased from 35.81 ± 0.13 μg/ml (without naringin) to 112.23 ± 0.13 μg/ml (freeze-dried solid dispersions with naringin) (p < 0.01). A 3.7-folds increase in apparent bioavailability was noticed with freeze-dried solid dispersions with naringin as compared to free CAN suspension administered alone.

CONCLUSION:

These results are quite stimulating for further development of a clinically useful oral formulation of candesartan cilexetil based on P-gp inhibition using naringin, a natural flavonoid as a pharmaceutical excipient.

KEYWORDS:

Candesartan; P-gp inhibition; lipophilic drug; naringin; oral bioavailability

PMID:
24168234
DOI:
10.3109/03639045.2013.850716
[Indexed for MEDLINE]
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