Statistical investigation of simulated fed intestinal media composition on the equilibrium solubility of oral drugs.
Abstract
Gastrointestinal fluid is a complex milieu and it is recognised that gut drug solubility is different to that observed in simple aqueous buffers. Simulated gastrointestinal media have been developed covering fasted and fed states to facilitate in vitro prediction of gut solubility and product dissolution. However, the combination of bile salts, phospholipids, fatty acids and proteins in an aqueous buffered system creates multiple phases and drug solubility is therefore a complex interaction between these components, which may create unique environments for each API. The impact on solubility can be...
Source: European Journal of Pharmaceutical Sciences - December 6, 2016 Category: Drugs & Pharmacology Authors: Zhou Z, Dunn C, Khadra I, Wilson CG, Halbert GW Tags: Eur J Pharm Sci Source Type: research
An investigation into the use of polymer blends to improve the printability of and regulate drug release from pharmaceutical solid dispersions prepared via fused deposition modeling (FDM) 3D printing.
This study explored the use of polymer blends as a formulation strategy to overcome this processability issue and to provide adjustable drug release rates from the printed dispersions. Solid dispersions of felodipine, the model drug, were successfully fabricated using FDM 3D printing with polymer blends of PEG, PEO and Tween 80 with either Eudragit E PO or Soluplus. As PVA is one of most widely used polymers in FDM 3D printing, a PVA based solid dispersion was used as a benchmark to compare the polymer blend systems to in terms processability. The polymer blends exhibited excellent printability and were suitable for proces...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 31, 2016 Category: Drugs & Pharmacology Authors: Alhijjaj M, Belton P, Qi S Tags: Eur J Pharm Biopharm Source Type: research
Three dimensional structural insight of laser drilled orifices in osmotic pump tablets.
In conclusion, the first three-dimensional structural insight of orifices in osmotic pump tablets by SR-μCT and structural reconstruction for the architectures has provided deeper insight into improving the design of advanced osmotic pumps for controlled drug release.
PMID: 27562708 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - August 21, 2016 Category: Drugs & Pharmacology Authors: Wu L, Wang L, Wang S, Xiao T, Chen M, Shao Q, York P, Singh V, Yin X, Gu J, Zhang J Tags: Eur J Pharm Sci Source Type: research
Coffee-Antihypertensive Drug Interaction: A Hemodynamic and Pharmacokinetic Study With Felodipine.
CONCLUSION: Intermittent coffee ingestion might complicate hypertension diagnosis and management for many individuals.
PMID: 27481881 [PubMed - as supplied by publisher] (Source: American Journal of Hypertension)
Source: American Journal of Hypertension - July 31, 2016 Category: Cardiology Authors: Bailey DG, Dresser GK, Urquhart BL, Freeman DJ, Arnold JM Tags: Am J Hypertens Source Type: research
Probing adsorption of DSPE-PEG2000 and DSPE-PEG5000 to the surface of felodipine and griseofulvin nanocrystals
Publication date: 20 August 2016 Source:International Journal of Pharmaceutics, Volume 510, Issue 1 Author(s): Hanna A. Rydberg, Marianna Yanez Arteta, Staffan Berg, Lennart Lindfors, Kalle Sigfridsson Nanosized formulations of poorly water-soluble drugs show great potential due to improved bioavailability. In order to retain colloidal stability, the nanocrystals need to be stabilized. Here we explore the use of the poly(ethylene glycol) (PEG) conjugated phospholipids DSPE-PEG2000 and DSPE-PEG5000 as stabilizers of felodipine and griseofulvin nanocrystals. Nanocrystal stability and physicochemical properties ...
Source: International Journal of Pharmaceutics - July 1, 2016 Category: Drugs & Pharmacology Source Type: research
Treatment efficacy of anti-hypertensive drugs in monotherapy or combination: ATOM systematic review and meta-analysis of randomized clinical trials according to PRISMA statement
Conclusions and implications: Certain drug combinations achieve BP reductions ranging from 20 to 25/10 to 15 mm Hg. Sex, ethnicity, and obesity are associated with antihypertensive response. This information can contribute to better selection of the antihypertensive drug, depending on the magnitude of pretreatment BP elevation. Guidelines should be revised. (Source: Medicine)
Source: Medicine - July 1, 2016 Category: Internal Medicine Tags: Research Article: Systematic Review and Meta-Analysis Source Type: research
Enhancement of the Oral Bioavailability of Felodipine Employing 8-Arm-Poly(Ethylene Glycol): In Vivo, In Vitro and In Silico Evaluation.
Abstract
Poor oral bioavailability is the single most important challenge in drug delivery. Prominent among the factors responsible for this is metabolic activity of the intestinal and hepatic cytochrome P450 (CYP450) enzymes. In preliminary studies, it was demonstrated that 8-arm-PEG was able to inhibit the felodipine metabolism. Therefore, this report investigated the oral bioavailability-enhancing property of 8-arm-PEG employing detailed in vitro, in vivo, and in silico evaluations. The in vitro metabolism of felodipine by cytochrome P450 3A4-expressed human liver microsomes (HLM) was optimized yielding...
Source: AAPS PharmSciTech - May 11, 2016 Category: Drugs & Pharmacology Authors: Fasinu P, Choonara YE, Kumar P, du Toit LC, Bijukumar D, Khan RA, Pillay V Tags: AAPS PharmSciTech Source Type: research
Photostabilization studies of antihypertensive 1,4-dihydropyridines using polymeric containers
Publication date: 30 May 2016 Source:International Journal of Pharmaceutics, Volume 505, Issues 1–2 Author(s): Michele De Luca, Giuseppina Ioele, Claudia Spatari, Gaetano Ragno 1,4-dihydropyridine antihypertensives (DHPs) are almost all dispensed in solid pharmaceutical formulations for their easy lability when exposed to light. This paper reports a study on the photoprotective effect of containers in different glassy or polymeric matrices with regard to four known DHPs when in solutions. The samples were subjected to forced degradation by means of a Xenon lamp, in accordance with the international rules on d...
Source: International Journal of Pharmaceutics - April 19, 2016 Category: Drugs & Pharmacology Source Type: research
Synchronous delivery of felodipine and metoprolol tartrate using monolithic osmotic pump technology.
Authors: Zhao S, Yu F, Liu N, Di Z, Yan K, Liu Y, Li Y, Zhang H, Yang Y, Yang Z, Li Z, Mei X
Abstract
The synchronous sustained-release of two drugs was desired urgently for patients needing combination therapy in long term. However, sophisticated technologies were used generally to realize the simultaneous delivery of two drugs especially those with different physico-chemical properties. The purpose of this study was to obtain the concurrent release of felodipine and metoprolol tartrate, two drugs with completely different solubilities, in a simple monolithic osmotic pump system (FMOP). Two types of block...
Source: Drug Development and Industrial Pharmacy - April 16, 2016 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
Liquisolid technology applied to pellets: Evaluation of the feasibility and dissolution performance using felodipine as a model drug
This study evaluated the feasibility of liquisolid pellets as an innovative drug delivery system to improve the dissolution rate of low solubility drugs, combining the advantageous properties of multiple-unit dosage forms and the liquisolid formulations. The effects of crospovidone (Kollidon® CL-SF) as a coating and disintegrating material (4 or 8%) and the type of non-volatile solvent, PEG 400 or Cremophor® EL, on the felodipine (model drug) dissolution profile were assessed. All liquisolid formulations had increased drug dissolution rates compared to their correspondent conventional formulations. Cremophor® EL was mor...
Source: Chemical Engineering Research and Design - February 19, 2016 Category: Chemistry Source Type: research
Solid-state characterization of Felodipine-Soluplus amorphous solid dispersions.
In conclusion, solubility of FEL was enhanced while a homogeneous SD was achieved for 10% drug loading.
PMID: 26530290 [PubMed - in process] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - February 16, 2016 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
Liquisolid technology applied to pellets I: evaluation of the feasibility and dissolution performance using felodipine as a model drug
This study evaluated the feasibility of liquisolid pellets as an innovative drug delivery system to improve the dissolution rate of low solubility drugs, combining the advantageous properties of multiple-unit dosage forms and the liquisolid formulations. The effects of crospovidone (Kollidon® CL-SF) as a coating and disintegrating material (4 or 8%) and the type of non-volatile solvent, PEG 400 or Cremophor® EL, on the felodipine (model drug) dissolution profile were assessed. All liquisolid formulations had increased drug dissolution rates compared to its correspondent conventional formulations. Cremophor® EL was more ...
Source: Chemical Engineering Research and Design - February 8, 2016 Category: Chemistry Source Type: research
Differential effects of enalapril–felodipine versus enalapril–lercanidipine combination drug treatment on sympathetic nerve traffic and metabolic profile in obesity-related hypertension
Scanty information is available on the effects of combination drug treatment based on an ACE inhibitor and a calcium channel blocker on the neurometabolic alterations characterizing obesity-related hypertension (OHT). After 2-week run-in with enalapril (20 mg), 36 OHTs were randomized according to a double-blind crossover design to a combination therapy with either lercanidipine 10 mg (L) or felodipine extended release 5 mg (F), each lasting 8 weeks. Measurements included clinic and ambulatory blood pressure (BP) and heart rate, homeostasis model assessment index, plasma norepinephrine, and muscle sympathetic nerve a...
Source: Journal of the American Society of Hypertension - January 9, 2016 Category: Cardiology Authors: Gino Seravalle, Gianmaria Brambilla, Daniela Prata Pizzalla, Anna Casati, Marta Riva, Cesare Cuspidi, Michele Bombelli, Giuseppe Mancia, Guido Grassi Tags: Research Article Source Type: research
Differential Effects of Enalapril-Felodipine vs Enalapril-Lercanidipine Combination Drug Treatment on Sympathetic Nerve Traffic and Metabolic Profile in Obesity-Related Hypertension
Scanty information is available on the effects of combination drug treatment based on an ACE-inhibitor and a calcium channel blocker on the neurometabolic alterations characterizing obesity-related hypertension (OHT). After 2 weeks run-in with enalapril (E, 20 mg), 36 OHTs were randomized according to a double-blind crossover design to a combination therapy with either lercanidipine 10 mg (L) or felodipine extended release 5 mg (F), each lasting 8 weeks. Measurements included clinic and ambulatory blood pressure (BP) and heart rate, homeostasis model assessment (HOMA) index, plasma norepinephrine (NE) and muscle sympatheti...
Source: Journal of the American Society of Hypertension - January 9, 2016 Category: Cardiology Authors: Gino Seravalle, Gianmaria Brambilla, Daniela Prata Pizzalla, Anna Casati, Marta Riva, Cesare Cuspidi, Michele Bombelli, Giuseppe Mancia, Guido Grassi Tags: Research Article Source Type: research
Optimising Drug Solubilisation in Amorphous Polymer Dispersions: Rational Selection of Hot-melt Extrusion Processing Parameters.
Abstract
The aim of this article was to construct a T-ϕ phase diagram for a model drug (FD) and amorphous polymer (Eudragit® EPO) and to use this information to understand the impact of how temperature-composition coordinates influenced the final properties of the extrudate. Defining process boundaries and understanding drug solubility in polymeric carriers is of utmost importance and will help in the successful manufacture of new delivery platforms for BCS class II drugs. Physically mixed felodipine (FD)-Eudragit(®) EPO (EPO) binary mixtures with pre-determined weight fractions were analysed using DSC ...
Source: AAPS PharmSciTech - January 4, 2016 Category: Drugs & Pharmacology Authors: Li S, Tian Y, Jones DS, Andrews GP Tags: AAPS PharmSciTech Source Type: research
