Coffee inhibition of CYP3A4 in vitro was not translated to a grapefruit‐like pharmacokinetic interaction clinically
Abstract
Grapefruit can augment oral medication bioavailability through irreversible (mechanism‐based) inhibition of intestinal CYP3A4. Supplementary data from our recent coffee–drug interaction clinical study showed some subjects had higher area under the plasma drug concentration ‐ time curve (AUC) and plasma peak drug concentration (Cmax) of the CYP3A4 probe felodipine compared to aqueous control. It was hypothesized that coffee might interact like grapefruit in responsive individuals. Beans from six geographical locations were consistently brewed into coffee that was separated chromatographically to a methanolic ...
Source: Pharmacology Research and Perspectives - September 27, 2017 Category: Drugs & Pharmacology Authors: George K. Dresser, Brad L. Urquhart, Julianne Proniuk, Alvin Tieu, David J. Freeman, John Malcolm Arnold, David G. Bailey Tags: Original Article Source Type: research
Abstract P480: Effects Of Long And Intermediate Acting Dihydropyridine Calcium Channel Blockers In Hypertension: A Systematic Review And Aeta-analysis Of 18 Prospective, Actively Controlled, Randomized Clinical Trials [Session Title: Antihypertensive Drugs and Pharmacology, Patient-Provider-Healthcare System Issues, and Pediatric and Adolescent Hypertension]
Conclusions: This study suggests that Amlodipine offers greater protection against major complications of hypertension compared to intermediate acting dihydropyridine calcium channel blockers. (Source: Hypertension)
Source: Hypertension - September 14, 2017 Category: Cardiology Authors: Sandip Chaugai, Hisatomi Arima, Lhamo Yangchen Sherpa, Amir Sepehry Tags: Poster Abstract Presentations Source Type: research
Felodipine inhibits ox-LDL-induced reactive oxygen species production and inflammation in human umbilical vein endothelial cells.
In conclusion, felodipine was demonstrated to inhibit oxidative stress and inflammatory responses, suggesting that it may be used to treat atherosclerosis.
PMID: 28791379 [PubMed - as supplied by publisher] (Source: Molecular Medicine Reports)
Source: Molecular Medicine Reports - August 11, 2017 Category: Molecular Biology Tags: Mol Med Rep Source Type: research
Simultaneous Determination of Felodipine and Metoprolol in Beagle Dog Plasma by Online SPE-LC-MS/MS and Its Application in a Pharmacokinetic Study.
Abstract
In order to overcome deficiencies for simultaneously determining felodipine (FDP) and metoprolol (MPL) with low recovery and low sensitivity, a new online SPE coupled with the liquid chromatography-tandem mass spectrometry (SPE-LC-MS/MS) method for the simultaneous quantitative determination of FDP and MPL in beagle dog plasma was established. The SPE extraction of FDP and MPL was performed on a Retain PEP Javelin column (10 × 2.1 mm, 5 μm), while the chromatographic separation was achieved on a ZORBAX SB-C18 (50 × 2.1 mm, 3.5 μm) analytical column. Multiple reaction monitoring operated in the...
Source: Analytical Sciences : the international journal of the Japan Society for Analytical Chemistry - July 12, 2017 Category: Chemistry Authors: Chen M, Zhou J, Mei L, Yu F, Xie X, Liu Y, Yang Y, Li Y, Mei X Tags: Anal Sci Source Type: research
Erratum
In the article “Differential effects of enalapril–felodipine versus enalapril–lercanidipine combination drug treatment on sympathetic nerve traffic and metabolic profile in obesity-related hypertension” (Grassi G, et al. J Am Soc Hypertens. 2016; 10:244-251), author affiliations listed for Cesare Cuspidi were incorrect. The correct affiliations are presented below. (Source: Journal of the American Society of Hypertension)
Source: Journal of the American Society of Hypertension - July 1, 2017 Category: Cardiology Tags: Erratum Source Type: research
A multi-technique characterization of the stability of surfactant containing solid dispersion based buccal patches prepared by hot melt injection moulding
This study investigates the stability of typically complex multi-component hydrophilic solid dispersions that could be used in a clinical application. Felodipine solid dispersions in two types of blends consisting of PEG, PEO and Tween 80 or Vit E TPGS were prepared by hot melt-injection moulding (HMIM) across a range of drug loadings and subjected to a range of storage conditions. Microscopy, thermal analysis, spectroscopy and powder X-ray diffraction were used to characterize the systems. The semi-solid surfactant TPGS showed a better solubilizing effect on the drug than the liquid surfactant Tween 80 in the fresh state ...
Source: International Journal of Pharmaceutics - June 21, 2017 Category: Drugs & Pharmacology Source Type: research
Biomimetic Dissolution: A Tool to Predict Amorphous Solid Dispersion Performance.
Abstract
The presented study describes the development of a membrane permeation non-sink dissolution method that can provide analysis of complete drug speciation and emulate the in vivo performance of poorly water-soluble Biopharmaceutical Classification System class II compounds. The designed membrane permeation methodology permits evaluation of free/dissolved/unbound drug from amorphous solid dispersion formulations with the use of a two-cell apparatus, biorelevant dissolution media, and a biomimetic polymer membrane. It offers insight into oral drug dissolution, permeation, and absorption. Amorphous sol...
Source: AAPS PharmSciTech - May 30, 2017 Category: Drugs & Pharmacology Authors: Puppolo MM, Hughey JR, Dillon T, Storey D, Jansen-Varnum S Tags: AAPS PharmSciTech Source Type: research
Studies on Core-Shell Nanocapsules of Felodipine: In Vitro-In Vivo Evaluations.
Abstract
The present study aimed for in vitro-in vivo-in silico simulation studies of experimentally designed (3(2)-factorial) Capmul PG-8-cored, Eudragit RSPO-Lutrol F 127 nanocapsules to ferry felodipine using GastroPlus™. The in silico parameter sensitivity analysis for pharmacokinetic parameters was initially assessed to justify the preparation of felodipine-loaded nanocapsules (FLNs) with enhanced solubility to overcome the bioavailability issues of felodipine. The overall integrated desirability ranged between 0.8187 and 0.9488 for three optimized FLNs when analyzed for mean particle size, zeta pot...
Source: AAPS PharmSciTech - April 19, 2017 Category: Drugs & Pharmacology Authors: Geroge JK, Verma PRP, Venkatesan J, Lee JY, Yoon DH, Kim SK, Singh SK Tags: AAPS PharmSciTech Source Type: research
Characterization of Heterogeneity and Spatial Distribution of Phases in Complex Solid Dispersions by Thermal Analysis by Structural Characterization and X-ray Micro Computed Tomography
ConclusionTASC and X μCT can provide unique information regarding the phase separation behavior of solid dispersions which can be closely associated with important product quality indicators such as heterogeneity and microstructure. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - April 6, 2017 Category: Drugs & Pharmacology Source Type: research
Evaluation of the chiral recognition properties and the column performances of three chiral stationary phases based on cellulose for the enantioseparation of six dihydropyridines by high-performance liquid chromatography.
Abstract
Separations of six dihydropyridine enantiomers on three commercially available cellulose-based chiral stationary phases (Chiralcel OD-RH, Chiralpak IB, and Chiralpak IC) were evaluated with high-performance liquid chromatography (HPLC). The best enantioseparation of the six chiral drugs was obtained with a Chiralpak IC (250 × 4.6 mm i.d., 5 μm) column. Then the influence of the mobile phase including an alcohol-modifying agent and alkaline additive on the enantioseparation were investigated and optimized. The optimal mobile phase conditions and maximum resolution for every analyte were as fo...
Source: Chirality - March 28, 2017 Category: Molecular Biology Authors: Yu J, Tang J, Yuan X, Guo X, Zhao L Tags: Chirality Source Type: research
Long-term outcomes of lercanidipine versus other calcium channel blockers in newly-diagnosed hypertension: a nationwide cohort study.
CONCLUSION: In newly diagnosed patients with hypertension, lercanidipine was superior than nifedipine in the six-year period when the analyzed endpoint was stroke.
PMID: 28300435 [PubMed - as supplied by publisher] (Source: Current Medical Research and Opinion)
Source: Current Medical Research and Opinion - March 19, 2017 Category: Research Tags: Curr Med Res Opin Source Type: research
Dual-mechanism gastroretentive drug delivery system loaded with an amorphous solid dispersion prepared by hot-melt extrusion.
Abstract
In the present study, we aimed to prepare a gastroretentive drug delivery system that would be both highly resistant to gastric emptying via multiple mechanisms and would also potentially induce in situ supersaturation. The bioadhesive floating pellets, loaded with an amorphous solid dispersion, were prepared in a single step of hot-melt extrusion technology. Hydroxypropyl cellulose (Klucel™ MF) and hypromellose (Benecel™ K15M) were used as matrix-forming polymers, and felodipine was used as the model drug. The foam pellets were fabricated based on the expansion of CO2, which was generated fro...
Source: European Journal of Pharmaceutical Sciences - February 27, 2017 Category: Drugs & Pharmacology Authors: Vo AQ, Feng X, Pimparade M, Ye X, Kim DW, Martin ST, Repka MA Tags: Eur J Pharm Sci Source Type: research
Molecules, Vol. 22, Pages 296: Amorphous-Amorphous Phase Separation in API/Polymer Formulations
In this study, the crystallization behavior, APS, and glass-transition temperatures formulations of ibuprofen and felodipine in polymeric PLGA excipients exhibiting different ratios of lactic acid and glycolic acid monomers in the PLGA chain were investigated by means of hot-stage microscopy and DSC. APS and recrystallization was observed in ibuprofen/PLGA formulations, while only recrystallization occurred in felodipine/PLGA formulations. Based on a successful modeling of the crystallization behavior using the Perturbed-Chain Statistical Associating Fluid Theory (PC-SAFT), the occurrence of APS was predicted in agreement ...
Source: Molecules - February 14, 2017 Category: Chemistry Authors: Christian Luebbert Fabian Huxoll Gabriele Sadowski Tags: Article Source Type: research
The influence of CYP3A5*3 and BCRPC421A genetic polymorphisms on the pharmacokinetics of felodipine in healthy Chinese volunteers
This study showed that the genetic polymorphisms of CYP3A5*3 and BCRPC421A might explain the variability in the pharmacokinetics of felodipine in the Chinese population.
CYP3A5*3 and BCRP421A genetic polymorphisms should influence felodipine metabolism. (Source: Journal of Clinical Pharmacy and Therapeutics)
Source: Journal of Clinical Pharmacy and Therapeutics - January 31, 2017 Category: Drugs & Pharmacology Authors: Q. Xiang, C. Li, X. Zhao, Y. M. Cui Tags: Original Article Source Type: research
Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in ‐vivo studies
ConclusionsMechanochemical approach was successful to prepare multicomponent solid forms that have the potential to improve biopharmaceutical parameters of the poorly soluble drug, FEL. (Source: Journal of Pharmacy and Pharmacology)
Source: Journal of Pharmacy and Pharmacology - January 29, 2017 Category: Drugs & Pharmacology Authors: Renu Chadha, Mohit Sharma, Jamshed Haneef Tags: Research Paper Source Type: research
