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Mengdan Xu, Ying Wu, Hao Wang, Xin Xu, Shuiping Zhao, Mei Zhang, Huigen- Jin, Jinchuan Yan, Bangning Wang, Jianbin Gong, Xiang Lu, Jianqiang Peng, Qiuyan Dai
OBJECTIVE: The objective of this study was to compare the effectiveness of lercanidipine with felodipine in patients with mild-to-moderate hypertension on day-to-day home blood pressure variability. METHODS: This is a sub-study of a multicenter, randomized, open-label, parallel group and active controlled clinical trial. Hypertensive patients aged 18-75 (i.e. diastolic blood pressure ≥90 mmHg and <110 mmHg; systolic blood pressure ≥140 mmHg and <180 mmHg) and 24 h mean BP >130/80 mmHg) were eligible for this study...
October 2016: Current Medical Research and Opinion
Xuezhong Zhang, Yuqing Zhang, Lisheng Liu, Alberto Zanchetti
OBJECTIVE: There is some debate as to optimal BP goals with antihypertensive treatment derived mostly in post-hoc analysis of large trials. Because there was limited number of subjects and outcomes within the larger study which may cloud the analytical accuracy of the findings. We suggest a new method to estimate the J-curve. DESIGN AND METHOD: Felodipine Event Reduction (FEVER) study randomized 9711 Chinese hypertensive patients to more or less intense anti-hypertensive treatment with 159,844 BP measurements...
September 2016: Journal of Hypertension
Martina Štěpánková, Kristýna Krasulová, Aneta Dořičáková, Ondřej Kurka, Pavel Anzenbacher, Zdeněk Dvořák
Dihydropyridine calcium channel blockers (CCBs) are used as anti-hypertensives and in the treatment of angina pectoris. Structurally, CCBs have at least one chiral center in the molecule, thereby existing in two or more different enantiomers. In the current paper we examined effects of benidipine, felodipine and isradipine enantiomers on the expression and enzyme activities of human xenobiotics-metabolizing cytochromes P450. All CCBs dose-dependently activated aryl hydrocarbon receptor (AhR) and pregnane X receptor (PXR), as revealed by gene reporter assays...
October 9, 2016: Toxicology Letters
Mona F Arafa, Sanaa A El-Gizawy, Mohamed A Osman, Gamal M El Maghraby
Dissolution enhancement is a promising strategy for improving drug bioavailability. Co-crystallization of drugs with inert material can help in this direction. The benefit will become even greater if the inert material can form co-crystal while maintaining its main function as excipient. Accordingly, the objective of the current study was to investigate xylitol as a potential co-crystal co-former for felodipine with the goal of preparing felodipine sublingual tablets. Co-crystallization was achieved by wet co-grinding of the crystals deposited from methanolic solutions containing felodipine with increasing molar ratios of xylitol (1:1, 1:2 and 1:3)...
September 28, 2016: Pharmaceutical Development and Technology
Xuezhong Zhang, Yuqing Zhang, Lisheng Liu, Alberto Zanchetti
OBJECTIVE: There is some debate as to optimal BP goals with antihypertensive treatment derived mostly in post-hoc analysis of large trials. Because there was limited number of subjects and outcomes within the larger study which may cloud the analytical accuracy of the findings. We suggest a new method to estimate the J-curve. DESIGN AND METHOD: Felodipine Event Reduction (FEVER) study randomized 9711 Chinese hypertensive patients to more or less intense anti-hypertensive treatment with 159,844 BP measurements...
September 2016: Journal of Hypertension
Muqdad Alhijjaj, Peter Belton, Sheng Qi
FDM 3D printing has been recently attracted increasing research efforts towards the production of personalized solid oral formulations. However, commercially available FDM printers are extremely limited with regards to the materials that can be processed to few types of thermoplastic polymers, which often may not be pharmaceutically approved materials nor ideal for optimizing dosage form performance of poor soluble compounds. 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...
September 1, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Li Wu, Lebing Wang, Shuxia Wang, Tiqiao Xiao, Min Chen, Qun Shao, Peter York, Vikaramjeet Singh, Xianzhen Yin, Jingkai Gu, Jiwen Zhang
The orifice drilled in the membrane as a channel for drug delivery is the key functional part of the osmotic pumps for a controlled drug release system. Reported conventional microscopic evaluations of these orifices have been limited to measurement of two-dimensional cross-section diameters. This study was aimed at establishing a novel method to measure quantitatively the three-dimensional architectures of orifices based on synchrotron radiation X-ray microcomputed tomography (SR-μCT). Quantitative analysis of architectures extracted from captopril osmotic pumps drilled by a range of operating parameters indicated that laser power correlated with the cross section area, volume, surface area and depth of the orifices, while scanning speed of laser beam showed inverse relationships with the above structure characters...
October 10, 2016: European Journal of Pharmaceutical Sciences
Y Zhang, X Zhang, L Liu, A Zanchetti
OBJECTIVE: In the setting of rapidly increasing trend of hypertension, a post-hoc subgroup analysis of the Felodipine Event Reduction (FEVER) Study was conducted to determine the effects of early blood pressure control on cardiovascular (CV) outcomes. DESIGN AND METHOD: The FEVER Study was a double-blind randomized trial conducted in 9711 Chinese hypertensive patients in which the CV outcomes were significantly reduced by felodipine compared with placebo. In this analysis, patients were regrouped to either the uncontrolled BP group (SBP/DBP, > = 140/90 mmHg) or the controlled BP group (<140/90 mmHg) at 1 and 6 months...
September 2016: Journal of Hypertension
M D Lobo, M Y Adeel, C B Wolff, P O Julu, M Shah, D M Collier, M Saxena, C Floyd, T Brier, V Kapil, O Mukhtar, A Radunovic, N Sutcliffe, F Sharif
OBJECTIVE: Profound BP variability (BPV) is a major cause of cardiovascular morbidity and poor quality of life as there are no optimal pharmacological strategies to help patients. We hypothesised that in a patient with baroreflex dysfunction and preserved efferent baroreflex pathway, carotid sinus stimulation may help control BP, BPV and heart rate variability (HRV). DESIGN AND METHOD: A 52 year old man was referred with profound HR and BPV. Home SBPs were in a range of 60-250 mmHg and DBPs were 40-130 mmHg and heart rate (HR) of 60-200 bpm (confirmed with ABPM, see Figure) despite multiple medications including felodipine 30 mg daily, terazosin 16 mg daily, doxazosin 8 mg daily, bisoprolol 20 mg daily and butrans patch 17...
September 2016: Journal of Hypertension
Henrik Palmelund, Cecilie Maria Madsen, Jakob Plum, Anette Müllertz, Thomas Rades
Supersaturating drug delivery systems can enhance the oral bioavailability of poorly soluble drug compounds. Supersaturation of such compounds has been studied in many different ways; however, a more standardized method is required. The rationale of choosing suitable concentrations of supersaturation to study has previously been very inconsistent. This makes comparisons between studies and compounds difficult, as the propensity of compounds to supersaturate varies greatly. This study presents a standardized method to study the supersaturation of drug compounds...
October 2016: Journal of Pharmaceutical Sciences
Marco A Paz, Alejandro de-La-Sierra, Marc Sáez, María Antonia Barceló, Juan José Rodríguez, Sonia Castro, Cristina Lagarón, Josep M Garrido, Pilar Vera, Gabriel Coll-de-Tuero
BACKGROUND: The relative efficacy of antihypertensive drugs/combinations is not well known. Identifying the most effective ones and the patients' characteristics associated with best performance of the drugs will improve management of hypertensive patients. OBJECTIVE: To assess the blood pressure (BP) reduction attributed to antihypertensive drugs and identify characteristics associated with BP decrease. DATA SOURCES: MEDLINE, Cochrane Central Register of Controlled Trials from inception through July 2012 and selected papers...
July 2016: Medicine (Baltimore)
Peter J Skrdla, Philip D Floyd, Philip C Dell'orco
Use of amorphous phases can mitigate the low in vivo exposures of poorly soluble, crystalline active pharmaceutical ingredients. However, it remains challenging to accurately predict the solubility enhancement offered even by a pure amorphous phase relative to the crystalline form. In this work, a methodology is presented that allows estimation of the amorphous:crystalline solubility ratio, α, using only measured thermodynamic quantities for each of the pure phases. With this approach, α values of 7.6 and 4...
September 2016: Journal of Pharmaceutical Sciences
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 were examined and the interaction between the PEGylated lipids and the nanocrystal surface as well as a macroscopic model surface was investigated...
August 20, 2016: International Journal of Pharmaceutics
Mehak Mehta, Raj Suryanarayanan
The goal was to develop an accelerated physical stability testing method of amorphous dispersions. Water sorption is known to cause plasticization and may accelerate drug crystallization. In an earlier investigation, it was observed that both the increase in mobility and decrease in stability in amorphous dispersions was explained by the "plasticization" effect of water (Mehta et al. Mol. Pharmaceutics 2016, 13 (4), 1339-1346). In this work, the influence of water concentration (up to 1.8% w/w) on the correlation between mobility and crystallization in felodipine dispersions was investigated...
August 1, 2016: Molecular Pharmaceutics
Pius Fasinu, Yahya E Choonara, Pradeep Kumar, Lisa C du Toit, Divya Bijukumar, Riaz A Khan, Viness Pillay
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 a typical Michaelis-Menten plot through the application of Enzyme Kinetic Module software from where the enzyme kinetic parameters were determined...
May 12, 2016: AAPS PharmSciTech
Muqdad Alhijjaj, Samy Yassin, Mike Reading, J Axel Zeitler, Peter Belton, Sheng Qi
PURPOSE: This study investigated the effect of drug-excipient miscibility on the heterogeneity and spatial distribution of phase separation in pharmaceutical solid dispersions at a micron-scale using two novel and complementary characterization techniques, thermal analysis by structural characterization (TASC) and X-ray micro-computed tomography (XμCT) in conjunction with conventional characterization methods. METHOD: Complex dispersions containing felodipine, TPGS, PEG and PEO were prepared using hot melt extrusion-injection moulding...
April 19, 2016: Pharmaceutical Research
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 drug stability evaluation. The simultaneous determination of the drugs and their photoproducts was carried out by applying the multivariate curve resolution (MCR) methodology to the spectral data recorded along the irradiation test...
May 30, 2016: International Journal of Pharmaceutics
Shiqing Zhao, Fanglin Yu, Nan Liu, Zhong Di, Kun Yan, Yan Liu, Ying Li, Hui Zhang, Yang Yang, Zhenbo Yang, Zhiping Li, Xingguo Mei
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 blocking agents were used in monolithic osmotic pump tablets and the synchronous sustained-release of FMOP was acquired in vitro...
November 2016: Drug Development and Industrial Pharmacy
Nabil Khzam, David Bailey, Helen S Yie, Mahmoud M Bakr
We present a case of a 47-year-old male who suffered from GE around his lower anterior teeth as soon as he started treatment with Felodipine 400 mg. We show that oral hygiene measures, antibiotics, and conventional periodontal treatment (scaling and root planing SRP) were all not sufficient to resolve the drug induced GE, which will persist and/or recur provided that systemic effect of the offending medication is still present. The condition immediately resolved after switching to a different medication. The mechanism of GE is complex and not fully understood yet...
2016: Case Reports in Dentistry
Rareş Iuliu Iovanov, Ioan Tomuţă, Sorin Emilian Leucuţa
BACKGROUND AND AIMS: Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method. METHODS: The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release...
2016: Clujul Medical (1957)
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