Oral bioavailability improvement of felodipine using tailored microemulsion: Surface science, ex vivo and in vivo studies
Publication date: Available online 23 January 2021Source: International Journal of PharmaceuticsAuthor(s): Akshay R. Koli, Ketan M. Ranch, Hetal P. Patel, Rajesh K. Parikh, Dinesh O. Shah, Furqan A. Maulvi (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 25, 2021 Category: Drugs & Pharmacology Source Type: research
In-Silico Screening of Lipid-Based Drug Delivery Systems
ConclusionThe API solubility individually depends on the choice of excipients. The proposed in-silico-screening approach allows formulators to quickly determine most-appropriate types of lipid-based formulations for a given API with low experimental effort.Graphical abstract (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - November 23, 2020 Category: Drugs & Pharmacology Source Type: research
Spectroscopic Methodology and Molecular Docking Studies on Changes in Binding Interaction of Felodipine with Bovine Serum Albumin Induced by Cocrystallization with β-Resorcylic Acid.
Abstract
In the present study, a novel cocrystal of felodipine (FEL) and β-resorcylic acid (βRA) was developed. We specially focused on the change of binding pattern with bovine serum albumin (BSA) induced by cocrystallization of FEL with βRA. The solid characterizations and density functional theory (DFT) simulation verified that FEL-βRA cocrystal formed in equimolar ratio (1 : 1 M ratio) through C=O…H-O hydrogen bond between C=O group in FEL and O-H group in βRA. The binding interactions between FEL-βRA system and BSA were studied using fluorescence spectral and molecular docking methods. T...
Source: Chemical and Pharmaceutical Bulletin - October 2, 2020 Category: Drugs & Pharmacology Authors: Li C, Du P, Zhou M, Yang L, Zhang H, Wang J, Yang C Tags: Chem Pharm Bull (Tokyo) Source Type: research
Investigating drug permeation across a lipid membrane supported on mesoporous silica.
In this study, we established a new means to monitor membrane permeation kinetics, using total internal reflection fluorescence (TIRF) microscopy strictly confined to a ~500 nm thick silica mesoporous substrate, positioned underneath a planar supported cell membrane mimic. This way, we demonstrate spatiotemporally resolved membrane-permeation kinetics of a small molecule model drug, felodipine, while simultaneously being able to control the integrity of, and follow drug binding to, the cell membrane mimic. By contrasting the permeation behaviour of pure felodipine with felodipine coupled to the permeability enhancer capryl...
Source: Angewandte Chemie - September 13, 2020 Category: Chemistry Authors: Joyce P, Jõemetsa S, Isaksson S, Hossain S, Larsson P, Bergström C, Höök F Tags: Angew Chem Int Ed Engl Source Type: research
Patterns of drug release as a function of drug loading from amorphous solid dispersions: A comparison of five different polymers.
Abstract
To reduce the pill burden associated with amorphous solid dispersions (ASDs), which arises from the large quantity of polymer used in the formulation, it is of interest to understand the relationship between drug loading and release properties. The aim of this study was to comprehensively evaluate drug release mechanisms from ASDs with polymers of varying hydrophobicity as a function of drug loading. Surface normalized dissolution rates of drug and polymer were studied for felodipine ASDs with polyvinylpyrrolidone (PVP), polyvinylpyrrolidone/vinyl acetate (PVPVA), Eudragit® S 100 (EUDS), hydroxyp...
Source: European Journal of Pharmaceutical Sciences - August 14, 2020 Category: Drugs & Pharmacology Authors: Saboo S, Moseson DE, Kestur US, Taylor LS Tags: Eur J Pharm Sci Source Type: research
Enhanced Oral Bioavailability of Felodipine from Solid Lipid Nanoparticles Prepared Through Effervescent Dispersion Technique.
Abstract
Felodipine (FLD), a dihydropyridine calcium channel blocker with excellent antihypertensive effect, is poorly soluble and undergoes extensive hepatic metabolism, which lead to poor oral bioavailability (about 15%) and limit its clinic application. The goal of this study was to develop solid lipid nanoparticles (SLNs) loading FLD to improve the oral bioavailability. The FLD loaded solid lipid nanoparticles (FLD-SLNs) were prepared by the effervescent dispersion technique developed by our laboratory, which might have some advantages over traditional methods. The FLD-SLNs showed desired particle char...
Source: AAPS PharmSciTech - June 10, 2020 Category: Drugs & Pharmacology Authors: He Y, Zhan C, Pi C, Zuo Y, Yang S, Hu M, Bai Y, Zhao L, Wei Y Tags: AAPS PharmSciTech Source Type: research
Comparison of induction methods for supersaturation: amorphous dissolution versus solvent shift.
This study develops and compares a small-scale non-sink amorphous dissolution method to a solvent shift method as induction methods for supersaturation of the model drugs albendazole, felodipine and tadalafil with respect to the maximum dissolved drug concentration, and the solid form of the precipitate. The study also investigates the effect of pre-dispersed precipitation inhibitors (hydroxypropyl methyl cellulose (HPMC) or polyvinylpyrrolidone (PVP)) on tadalafil supersaturation induced by both amorphous dissolution and solvent shift with respect to maximum dissolved drug concentration, precipitation rate and solid form ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 2, 2020 Category: Drugs & Pharmacology Authors: Plum J, Bavnhøj CG, Eliasen JN, Rades T, Müllertz A Tags: Eur J Pharm Biopharm Source Type: research
Impact of 14 types of genetic polymorphisms on antihypertensive efficacy of felodipine in healthy Chinese subjects
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CONCLUSION: The efficacy of felodipine is individually different, influenced especially by CACNA1C rs1051375 and ABCB1 rs1045642. ΔDBP is associated with ΔSBP in multiple-dosing of felodipine in healthy Chinese subjects.
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PMID: 32301702 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Pharmacology and Therapeutics)
Source: International Journal of Clinical Pharmacology and Therapeutics - April 19, 2020 Category: Drugs & Pharmacology Tags: Int J Clin Pharmacol Ther Source Type: research
Thermal properties of drug polymorphs: A case study with felodipine form I and form IV
Publication date: Available online 18 April 2020Source: Journal of Saudi Chemical SocietyAuthor(s): Wei Guo, Congwei Li, Pengfei Du, Yalin Wang, Shuangli Zhao, Jing Wang, Caiqin Yang (Source: Journal of Saudi Chemical Society)
Source: Journal of Saudi Chemical Society - April 18, 2020 Category: Chemistry Source Type: research
Application of solid-state 13C relaxation time to prediction of the recrystallization inhibition strength of polymers on amorphous felodipine at low polymer loading
Publication date: Available online 5 April 2020Source: International Journal of PharmaceuticsAuthor(s): Keisuke Ueda, Hitomi Okada, Zhijing Zhao, Kenjirou Higashi, Kunikazu Moribe (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 6, 2020 Category: Drugs & Pharmacology Source Type: research
A validated LC–MS/MS method for the quantification of amlodipine, bisoprolol, enalapril and enalaprilat—Application to pharmacokinetic study in healthy volunteers
Publication date: June 2020Source: Microchemical Journal, Volume 155Author(s): Liliya Logoyda, Sergiy Kovalenk, Moustafa Gaafar, Ahmed M. Abdel-Megied, Fawzy A. ElbarbryAbstractIn this work, a highly sensitive and rapid liquid chromatography-tandem mass spectrometry (LC–MS/MS) method for the simultaneous determination of amlodipine (AML), bisoprolol (BIS) and enalapril maleate (ENA) in the presence of its metabolite enalaprilat (ENT) in real human plasma was developed and validated using felodipine, propranolol, ramipril, and captopril, as internal standards (IS), respectively. The prepared samples were chromatographed u...
Source: Microchemical Journal - February 14, 2020 Category: Chemistry Source Type: research
Small scale design of experiment investigation of equilibrium solubility in simulated fasted and fed intestinal fluid.
Abstract
It is widely recognised that drug solubility within the gastrointestinal tract (GIT) differs from values determined in a simple aqueous buffer and to circumvent this problem measurement in biorelevant fluids is determined. Biorelevant fluids are complex mixtures of components (sodium taurocholate, lecithin, sodium phosphate, sodium chloride, pancreatin and sodium oleate) at various concentrations and pH levels to provide systems simulating fasted (FaSSIF) or fed (FeSSIF) intestinal media. Design of Experiment (DoE) studies have been applied to investigate FaSSIF and FeSSIF and indicate that a drug...
Source: European Journal of Pharmaceutics and Biopharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Authors: McPherson S, Perrier J, Dunn C, Khadra I, Davidson S, Ainousah B, Wilson CG, Halbert G Tags: Eur J Pharm Biopharm Source Type: research
Bile acid transporter mediated STC/Soluplus self-assembled hybrid nanoparticles for enhancing the oral drug bioavailability
In conclusion, STC/Soluplus SHNPs via ASBT are a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 5, 2020 Category: Drugs & Pharmacology Source Type: research
Felodipine and Renal Function in Lung Transplantation: A Randomized Placebo-controlled Trial
Calcium channel blockers may ameliorate the decline in renal function caused by calcineurin inhibitors in lung transplant (LTX) recipients. We hypothesized that preoperative and 12-week postoperative treatment with the calcium channel blocker, felodipine, would reduce the decline in glomerular filtration rate (GFR). (Source: The Journal of Heart and Lung Transplantation)
Source: The Journal of Heart and Lung Transplantation - January 28, 2020 Category: Transplant Surgery Authors: M Hornum, M Iversen, P Oturai, MJ Andersen, M Zemtsovski, P Bredahl, N.H Bjarnason, K.B Christensen, J. Carlsen, CH M øller, B Feldt-Rasmussen, M Perch Tags: Original Clinical Science Source Type: research
An in vitro dissolution-digestion-permeation assay for the study of advanced drug delivery systems.
Abstract
Advanced drug delivery systems (ADDS) are widely explored to overcome poor aqueous solubility of orally administered drugs. However, the prediction of their in vivo performance is challenging, as in vitro models typically do not capture the interplay between processes occurring in the gut. In additions, different models are used to evaluate the different systems. We therefore present a method that allows monitoring of luminal processing (dissolution, digestion) and its interplay with permeation to better inform on the absorption of felodipine formulated as ADDS. Experiments were performed in a µF...
Source: European Journal of Pharmaceutics and Biopharmaceutics - January 22, 2020 Category: Drugs & Pharmacology Authors: Alvebratt C, Keemink J, Edueng K, Cheung O, Strømme M, Bergström CAS Tags: Eur J Pharm Biopharm Source Type: research
