Felodipine

Felodipine Structure
Felodipine structure
Common Name Felodipine
CAS Number 72509-76-3 Molecular Weight 384.254
Density 1.3±0.1 g/cm3 Boiling Point 471.5±45.0 °C at 760 mmHg
Molecular Formula C18H19Cl2NO4 Melting Point 142-145°C
MSDS Chinese USA Flash Point 239.0±28.7 °C
Symbol GHS07
GHS07
Signal Word Warning

Screening of stabilizers for LC-MS/MS analysis of clevidipine and its primary metabolite in dog whole blood.

Bioanalysis 7 , 1457-69, (2015)

Clevidipine is an ester-containing antihypertensive agent that undergoes rapid hydrolysis in blood. A reliable stabilizer cocktail containing citric acid and ascorbic acid was established and the LC-MS/MS method was validated for simultaneous determination of...

Quantitative assessment of intestinal first-pass metabolism of oral drugs using portal-vein cannulated rats.

Pharm. Res. 32(2) , 604-16, (2015)

To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome P4503A (CYP3A) and uridine 5'-diphosphate-glucuronosyltransferases (UGT) on in vivo oral absorption of their substrate drugs.CYP3A and UGT substrates were orally administered to por...

Multilayer encapsulated mesoporous silica nanospheres as an oral sustained drug delivery system for the poorly water-soluble drug felodipine.

Mater. Sci. Eng. C. Mater. Biol. Appl. 47 , 313-24, (2014)

We used a combination of mesoporous silica nanospheres (MSN) and layer-by-layer (LBL) self-assembly technology to establish a new oral sustained drug delivery system for the poorly water-soluble drug felodipine. Firstly, the model drug was loaded into MSN, an...

Size- and time-dependent alteration in metabolic activities of human hepatic cytochrome P450 isozymes by gold nanoparticles via microsomal coincubations.

Nanoscale Res. Lett. 9(1) , 642, (2014)

Nano-sized particles are known to interfere with drug-metabolizing cytochrome P450 (CYP) enzymes, which can be anticipated to be a potential source of unintended adverse reactions, but the mechanisms underlying the inhibition are still not well understood. He...

The effect of processing on the surface physical stability of amorphous solid dispersions.

Eur. J. Pharm. Biopharm. 88(3) , 897-908, (2014)

The focus of this study was to investigate the effect of processing on the surface crystallization of amorphous molecular dispersions and gain insight into the mechanisms underpinning this effect. The model systems, amorphous molecular dispersions of felodipi...

A solid-phase extraction method for rapidly determining the adsorption coefficient of pharmaceuticals in sewage sludge.

Water Res. 67 , 292-8, (2014)

The partitioning of pharmaceuticals in the environment can be assessed by measuring their adsorption coefficients (Kd) between aqueous and solid phases. Measuring this coefficient in sewage sludge gives an indication of their partitioning behaviour in a waste...

Ramipril/felodipine extended-release fixed-dose combination: a review of its use in the management of essential hypertension.

Drugs 65(13) , 1851-68, (2005)

Ramipril/felodipine extended release (ER) [Triapin and Triapin Mite, Unimax] is a once-daily fixed-dose combination of the ACE inhibitor ramipril and the ER formulation of the dihydropyridine calcium channel antagonist felodipine. It is indicated in adult pat...

Inversion of population distribution of felodipine conformations at increased concentration in dimethyl sulfoxide is a prerequisite to crystal nucleation.

J. Pharm. Sci. 103(2) , 392-4, (2014)

Knowledge of the preferred conformations of biologically active compounds is of the utmost importance for a better understanding of the structure-activity relationships underlying their biological activity, as well as their mechanism of action. Moreover, inve...

Felodipine and isradipine: new calcium-channel-blocking agents for the treatment of hypertension.

Clin. Pharm. 12(4) , 261-75, (1993)

The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects, and dosage of felodipine and isradipine are reviewed. Felodipine and isradipine are new calcium-channel-blocking agents with FDA-approved labeling for use in the treatment of essen...

Vascular selective calcium entry blockers in the treatment of cardiovascular disorders: focus on felodipine.

Cardiovasc. Drugs Ther. 9(5) , 657-63, (1995)

Calcium entry through L-type calcium channels is essential for contraction of both arterial smooth muscle and the myocardium, and is important in cardiac conduction. First-generation calcium entry blockers lack or have a modest degree of vascular selectivity ...