ArticleSaudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society2014
Enhanced solubility and intestinal absorption of candesartan cilexetil solid dispersions using everted rat intestinal sacs.
Article in Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 75 citations in OpenAlex.
- Preparation and Evaluation of Candesartan Cilexetil Solid Supersaturated Self-nanoemulsion Containing Phospholipids.AAPS PharmSciTech · 2026Article
- Dissolution enhancement of Gefitinib by solid dispersion and complexation with β-cyclodextrins: In vitro testing, cytotoxic activity, and tablet formulation.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Article
- Supersaturated Drug Delivery System of Oxyberberine Based on Cyclodextrin Nanoaggregates: Preparation, Characterization, and in vivo Application.International journal of nanomedicine · 2024Article
- Formulation and characterization of glipizide solid dosage form with enhanced solubility.PloS one · 2024Article
- How to Improve Solubility and Dissolution of Irbesartan by Fabricating Ternary Solid Dispersions: Optimization and In-Vitro Characterization.Pharmaceutics · 2022Article
- Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats.Membranes · 2021Article
- Phytophospholipid Complex of Caffeic Acid: Development, In vitro Characterization, and In Vivo Investigation of Antihyperlipidemic and Hepatoprotective Action in Rats.AAPS PharmSciTech · 2021Article
- Enhancing the Oral Bioavailability of Candesartan Cilexetil Loaded Nanostructured Lipid Carriers: In Vitro Characterization and Absorption in Rats after Oral Administration.Pharmaceutics · 2020Article
- Oral Bioavailability Enhancement and Anti-Fatigue Assessment of the Andrographolide Loaded Solid Dispersion.International journal of molecular sciences · 2020Article
- In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glucoside.BMC pharmacology & toxicology · 2020Article
- In Vitro and In Situ Characterization of the Intestinal Absorption of Capilliposide B and Capilliposide C fromMolecules (Basel, Switzerland) · 2019Article
- Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats.Experimental animals · 2018Article
- The effects of 18β-glycyrrhetinic acid and glycyrrhizin on intestinal absorption of paeoniflorin using the everted rat gut sac model.Journal of natural medicines · 2017Article
- Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir.BioMed research international · 2017Article
- Development of surface stabilized candesartan cilexetil nanocrystals with enhanced dissolution rate, permeation rate across CaCo-2, and oral bioavailability.Drug delivery and translational research · 2016Article
- Design and development and evaluation of candesartan cilexetil liquid filling formulations.International journal of pharmaceutical investigationArticle
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
objectiveCandesartan cilexetil (CAN) is a poor aqueous soluble compound and a P-glycoprotein (P-gp) efflux pump substrate. These key factors are responsible for its incomplete intestinal absorption.
methodsIn this study, we investigated to enhance the absorption of CAN by improving its solubility and inhibiting intestinal P-gp activity. A phase solubility method was used to evaluate the aqueous solubility of CAN in PVP K30 (0.2-2%). Gibbs free energy [Formula: see text] values were all negative. Solubility was enhanced by the freeze drying technique. The in vitro dissolution was evaluated using the USP paddle method. The interaction between drug and carrier was evaluated by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and Differential scanning calorimetry (DSC) studies. Naringin was selected as P-gp inhibitor. Absorption studies were performed using the everted gut sac model from rat jejunum. The drug analysis was performed by HPLC.
resultsFTIR spectra revealed no interaction between drug and PVP K30. From XRD and DSC data, CAN was in the amorphous form, which explains the cumulative release of drug from its prepared systems. We noticed an enhancement of CAN absorption by improving its solubility and inhibiting the P-gp activity. The significant results (p < 0.05) were obtained for freeze dried solid dispersions in the presence of P-gp inhibitor than without naringin (15 mg/kg) with an absorption enhancement of 8-fold.
conclusionNaringin, a natural flavonoid, has no undesirable side effects. Therefore, it could be employed as an excipient in the form of solid dispersions to increase CAN intestinal absorption and its oral bioavailability.
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