The importance and safety of calcium antagonists in the treatment of hypertension in pregnant women
Publication date: Available online 6 March 2019Source: Pregnancy HypertensionAuthor(s): Grzegorz Grześk, Łukasz Wołowiec, Marcin Walukiewicz, Daniel Rogowicz, Wojciech Gilewski, Joanna BanachAbstractThe use of CCBs, including newer dihydropyridine derivatives like felodipine and amlodipine, seems to be an effective, safe and more modern option in HDP therapy and during breast-feeding. (Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health)
Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health - March 6, 2019 Category: OBGYN Source Type: research

[One-year persistence of fixed-dose combinations of angiotensin-converting enzyme inhibitor and calcium channel blocker in hypertensive patients].
CONCLUSIONS: The authors demonstrated that the one-year persistence of ACEI/CCB FDCs was significantly different in hypertensive patients. Ramipril/amlodipine FDC was more advantageous for patient adherence. Orv Hetil. 2019; 160(9): 343-348. PMID: 30798621 [PubMed - in process] (Source: Orvosi Hetilap)
Source: Orvosi Hetilap - February 27, 2019 Category: General Medicine Authors: Simonyi G, Ferenci T, Finta E, Igaz I, Balogh S, Gasparics R, Medvegy M Tags: Orv Hetil Source Type: research

Low Dose Scanning Transmission Electron Microscopy of Organic Crystals by Scanning Moiré Fringes
Publication date: Available online 1 February 2019Source: MicronAuthor(s): Mark S’ari, James Cattle, Nicole Hondow, Rik Brydson, Andy BrownAbstractIn the pharmaceutical industry, it is important to determine the effects of crystallisation and processes, such as milling, on the generation of crystalline defects in formulated products. Conventional transmission electron microscopy and scanning transmission electron microscopy (STEM) can be used to obtain information on length scales unobtainable by other techniques, however, organic crystals are extremely susceptible to electron beam damage. This work demonstrates a bright...
Source: Micron - February 2, 2019 Category: Biology Source Type: research

The Influence of Cellulosic Polymer's Variables on Dissolution/Solubility of Amorphous Felodipine and Crystallization Inhibition from a Supersaturated State.
Abstract The collective impact of cellulosic polymers on the dissolution, solubility, and crystallization inhibition of amorphous active pharmaceutical ingredients (APIs) is still far from being adequately understood. The goal of this research was to explore the influence of cellulosic polymers and incubation conditions on enhancement of solubility and dissolution of amorphous felodipine, while inhibiting crystallization of the drug from a supersaturated state. Variables, including cellulosic polymer type, amount, ionic strength, and viscosity, were evaluated for effects on API dissolution/solubility and c...
Source: AAPS PharmSciTech - December 17, 2018 Category: Drugs & Pharmacology Authors: Shi NQ, Jin Y, Zhang Y, Che XX, Xiao X, Cui GH, Chen YZ, Feng B, Li ZQ, Qi XR Tags: AAPS PharmSciTech Source Type: research

Targeting Nrf2/HO-1 signaling by crocin: Role in attenuation of AA-induced ulcerative colitis in rats
In conclusion; crocin demonstrated anti-ulcerogenic and coloprotective effect mediated primarily by its antioxidant, anti-inflammatory and anti-apoptotic properties. The therapeutic impact is mediated primarily via enhancement of colon Nrf2 content by 211% in protective protocol and by 350% in curative and HO-1 signaling by 49% in protective protocol and, 288% in the curative protocol. Enhancement of Nrf2 and HO-1 signaling and down-regulation of caspase-3 activity are believed to underly the observed therapeutic effect.Graphical abstract (Source: Biomedicine and Pharmacotherapy)
Source: Biomedicine and Pharmacotherapy - December 5, 2018 Category: Drugs & Pharmacology Source Type: research

Targeting Nrf2/HO-1 signaling by crocin: Role in attenuation of AA-induced ulcerative colitis in rats.
In conclusion; crocin demonstrated anti-ulcerogenic and coloprotective effect mediated primarily by its antioxidant, anti-inflammatory and anti-apoptotic properties. The therapeutic impact is mediated primarily via enhancement of colon Nrf2 content by 211% in protective protocol and by 350% in curative and HO-1 signaling by 49% in protective protocol and, 288% in the curative protocol. Enhancement of Nrf2 and HO-1 signaling and down-regulation of caspase-3 activity are believed to underly the observed therapeutic effect. PMID: 30530041 [PubMed - as supplied by publisher] (Source: Biomedicine and pharmacotherapy = B...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - December 4, 2018 Category: Drugs & Pharmacology Authors: Khodir AE, Said E, Atif H, ElKashef HA, Salem HA Tags: Biomed Pharmacother Source Type: research

Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine
In this study pooled human saliva was characterised and utilised as dissolution media for biorelevant oral cavity dissolution studies and to assess drug release. Lipophilic drug felodipine with challenging biopharmaceutical properties was selected for assessment in oral cavity dissolution studies. These saliva dissolution studies investigated for the first time how biorelevant dissolution can be implemented as a screening tool to guide the formulation development process and to predict dosage form performance within the mouth. In this study a combination of three dissolution enhancement strategies (cryomilling, solid dispe...
Source: International Journal of Pharmaceutics - November 19, 2018 Category: Drugs & Pharmacology Source Type: research

Predicted Amorphous Solubility and Dissolution Rate Advantages Following Moisture Sorption: Case Studies of Indomethacin and Felodipine
Publication date: Available online 15 November 2018Source: International Journal of PharmaceuticsAuthor(s): Peter J. Skrdla, Philip D. Floyd, Philip C. Dell'OrcoAbstractWater is often readily absorbed by amorphous compounds, lowering their glass transition temperature (Tg) and facilitating their recrystallization (via nucleation-and-growth). At the same time, the increase in moisture content translates to a decrease in both the thermodynamic solubility and intrinsic dissolution rate, as compared to the corresponding dry (pure) amorphous phase, e.g. see [Murdande SB, Pikal MJ, Shanker RM, Bogner RH. 2010. Solubility advanta...
Source: International Journal of Pharmaceutics - November 17, 2018 Category: Drugs & Pharmacology Source Type: research

Diversity of methyl group dynamics in felodipine: a DFT supported NMR and QENS study
CrystEngComm, 2018, Advance Article DOI: 10.1039/C8CE01605D, PaperAleksandra Pajzderska, Kacper Dru żbicki, Miguel Angel Gonzalez, Jacek Jenczyk, Jadwiga Mielcarek, Jan Wąsicki Computationally-supported NMR and neutron scattering experiments were combined to provide new insights into the structure –dynamics relationship in the most stable polymorph of felodipine. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - CrystEngComm latest articles)
Source: RSC - CrystEngComm latest articles - November 7, 2018 Category: Chemistry Authors: Aleksandra Pajzderska Source Type: research

Diversity of Methyl Group Dynamics in Felodipine: a DFT Supported NMR and Neutron Scattering Study
CrystEngComm, 2018, Accepted Manuscript DOI: 10.1039/C8CE01605D, PaperAleksandra Pajzderska, Kacper Druzbicki, Miguel A. Gonzalez, Jacek Jenczyk, Jadwiga Mielcarek, Jan Wasicki Molecular and vibrational dynamics in a widely used calcium channel blocker, felodipine form I (FLD), have been thoroughly explored by combining periodic density functional theory (plane-wave DFT) with solid-state nuclear... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - CrystEngComm latest articles)
Source: RSC - CrystEngComm latest articles - October 31, 2018 Category: Chemistry Authors: Aleksandra Pajzderska Source Type: research

Identification of crucial genes and prediction of small molecules for multidrug resistance of Hodgkin's lymphomas.
CONCLUSIONS: The present study offered new insights into the molecular mechanisms of multidrug resistance and identified a series of important hub genes and small agents that might be critical for treatment of multidrug-resistant HL. PMID: 30347596 [PubMed - as supplied by publisher] (Source: Cancer Biomarkers)
Source: Cancer Biomarkers - October 24, 2018 Category: Cancer & Oncology Tags: Cancer Biomark Source Type: research

Early stages of drug crystallization from amorphous solid dispersion via fractal analysis based on chemical imaging.
Abstract Early stages of crystallization from amorphous solid dispersion (ASD) are typically not detected by means of standard methods like powder X-ray diffraction (XRPD). The aim of this study is therefore to evaluate if fractal analysis based on energy dispersive x-ray imaging can provide the means to identify early signs of physical instability. ASDs of the poorly water-soluble compound, felodipine (FEL) were prepared by solvent evaporation using different grades of HPMCAS, at 50wt. % drug loading. Samples were stored at accelerated conditions of 40°C. Scanning electron microscopy equipped with an ene...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 6, 2018 Category: Drugs & Pharmacology Authors: Abreu-Villela R, Schönenberger M, Caraballo I, Kuentz M Tags: Eur J Pharm Biopharm Source Type: research

Structural studies of calcium channel blockers used in the treatment of hypertension - 1 H and 13 C NMR characteristics of nifedipine analogues.
Abstract The 1 H and 13 C NMR spectroscopy in solution was applied to characterize a series of active pharmaceutical ingredients (API) belonging to the class of calcium channel blockers, a group of drug substances extremely sensitive to UV radiation: nifedipine (1), nitrendipine (2), nisoldipine (3), nimodipine (4), nilvadipine (5), felodipine (6) isradipine (7) nicardipine (8) and amlodipine besylate (9). Two-dimensional NMR experiments (COSY, HSQC, HMBC) allowed the unequivocal assignments of peaks in the 1 H and 13 C spectra in solution and in some cases enabled editing of incorrect assignments appearin...
Source: Magnetic Resonance in Chemistry : MRC - September 26, 2018 Category: Chemistry Authors: Szeleszczuk Ł, Zielińska-Pisklak M, Pisklak DM Tags: Magn Reson Chem Source Type: research

Validated RP-HPLC method for quantification of felodipine in rabbit plasma: Application in a bioequivalence study.
CONCLUSION: Thus, developed method is simple, convenient and suitable for the analysis of felodipine in bulk and pharmaceutical formulations. PMID: 30243471 [PubMed - as supplied by publisher] (Source: Annales Pharmaceutiques Francaises)
Source: Annales Pharmaceutiques Francaises - September 19, 2018 Category: Drugs & Pharmacology Authors: Salunkhe NH, Jadhav NR, Bhinge SD Tags: Ann Pharm Fr Source Type: research

Polyvinylpyrrolidone affects thermal stability of drugs in solid dispersions
Publication date: Available online 11 September 2018Source: International Journal of PharmaceuticsAuthor(s): Yasmine Ben Osman, Tatsiana Liavitskaya, Sergey VyazovkinAbstractThe present study explores the hypothesis that a polymer can affect the thermal stability of a drug in solid polymer-drug dispersions. The hypothesis is tested in a systematic fashion by combining isoconversional kinetic analysis with thermogravimetric measurements on several solid dispersions. Experimental systems involve three drugs: indomethacin (IMC), felodipine (FD), and nifedipine (ND) and their solid dispersions with polyvinylpyrrolidone (PVP). ...
Source: International Journal of Pharmaceutics - September 12, 2018 Category: Drugs & Pharmacology Source Type: research