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Felodipine

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https://www.readbyqxmd.com/read/28625814/a-multi-technique-characterization-of-the-stability-of-surfactant-containing-solid-dispersion-based-buccal-patches-prepared-by-hot-melt-injection-moulding
#1
Muqdad Alhijjaj, Peter Belton, Sheng Qi
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 and offered some degree of protection over the chemical degradation of PEG/PEO...
June 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28611390/protective-and-therapeutic-effect-of-felodipine-against-bleomycin-induced-pulmonary-fibrosis-in-mice
#2
Ken-Ichiro Tanaka, Tomomi Niino, Tomoaki Ishihara, Ayaka Takafuji, Takahiro Takayama, Yuki Kanda, Toshifumi Sugizaki, Fumiya Tamura, Shota Kurotsu, Masahiro Kawahara, Tohru Mizushima
Idiopathic pulmonary fibrosis (IPF) involves alveolar epithelial injury and abnormal collagen production caused by activated fibroblasts; transforming growth factor (TGF)-β1 is implicated in this activation. In this study, we screened for chemicals capable of inhibiting TGF-β1-induced collagen production in cultured fibroblasts from medicines already in clinical use. We selected felodipine based on its extent of collagen production inhibition, clinical safety profile, and other pharmacological activity. Felodipine is a dihydropyridine Ca(2+) channel blocker that has been used clinically to treat patients with high blood pressure...
June 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28560506/biomimetic-dissolution-a-tool-to-predict-amorphous-solid-dispersion-performance
#3
Michael M Puppolo, Justin R Hughey, Traciann Dillon, David Storey, Susan Jansen-Varnum
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...
May 30, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28480807/tri-block-co-polymer-nanocarriers-for-enhancement-of-oral-delivery-of-felodipine-preparation-in-vitro-characterization-and-ex-vivo-permeation
#4
Sinar Sayed, Basant A Habib, Ghada M Elsayed
This study aimed to prepare, optimize and characterize novel felodipine-loaded polymeric nanomicelles, using a pluronic mixture of F127 and P123. Thin-film hydration method was adopted for the preparation of different polymeric nanomicelles (T1-T12) according to a 4(1).3(1) full factorial design. Factors studied were: Pluronic®:drug ratio (P:D ratio) (10, 20, 30 and 40 w/w) and percent of hydrophilic polymer (F127%) (33.33%, 50% and 66.67% w/w). Optimization criteria were to maximize transmittance percent (T%) and entrapment efficiency percent (EE%) and to minimize particle size (PS) and polydispersity index (PDI)...
May 25, 2017: Journal of Liposome Research
https://www.readbyqxmd.com/read/28424979/studies-on-core-shell-nanocapsules-of-felodipine-in-vitro-in-vivo-evaluations
#5
Jerome K Geroge, Priya Ranjan Prasad Verma, Jayachandran Venkatesan, Jin-Young Lee, Dong-Han Yoon, Se-Kwon Kim, Sandeep Kumar Singh
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...
April 19, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28375107/formulation-evaluation-and-optimization-of-the-felodipine-nanosuspension-to-be-used-for-direct-compression-to-tablet-for-in-vitro-dissolution-enhancement
#6
Dhaval Mori, Jalpa Makwana, Ramesh Parmar, Kalpesh Patel, Jayant Chavda
The oral bioavailability of felodipine very low, nearly just 15% due to its limited solubility and high first pass metabolism. The present study was aimed to improve the rate of the dissolution of Felodipine by formulating a nano suspension of it by combination of high-speed homogenization and media milling technique. Stabilizers screened in this study were Poloxamer 401, HPMC K15M and Tween 80. Concentration of stabilizers were optimized by simplex lattice design for Mean Particle Size (MPS), Poly dispersity Index (PDI), saturation solubility (SS) and in vitro drug release in 30 min...
November 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28349560/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
#7
Jia Yu, Jing Tang, Xiaowei Yuan, Xingjie Guo, Longshan Zhao
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...
March 28, 2017: Chirality
https://www.readbyqxmd.com/read/28300435/long-term-outcomes-of-lercanidipine-versus-other-calcium-channel-blockers-in-newly-diagnosed-hypertension-a-nationwide-cohort-study
#8
Kai-Hung Cheng, Kai-Chun Cheng, Kai-Yuan Cheng, Yi-Hsin Yang, Chung-Wei Lee, Wen-Ter Lai
OBJECTIVE: Calcium channel blockers (CCBs) have been proved to have beneficial effects on cardiovascular (CV) outcomes, especially in stroke. Lercanidipine, a highly lipophilic CCB, lacks data regarding long-term outcomes including: CV, stroke, renal and all-cause mortality. This retrospective cohort study aims to clarify this. PATIENTS AND METHODS: A total of 144,630 newly diagnosed hypertension (HTN) patients (age: 18-65 years) in 2005 from the Taiwan's National Health Insurance Research Database were enrolled in this observational study...
June 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28257881/dual-mechanism-gastroretentive-drug-delivery-system-loaded-with-an-amorphous-solid-dispersion-prepared-by-hot-melt-extrusion
#9
Anh Q Vo, Xin Feng, Manjeet Pimparade, Xinyou Ye, Dong Wuk Kim, Scott T Martin, Michael A Repka
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...
February 28, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28244604/the-influence-of-cyp3a5-3-and-bcrpc421a-genetic-polymorphisms-on-the-pharmacokinetics-of-felodipine-in-healthy-chinese-volunteers
#10
Q Xiang, C Li, X Zhao, Y M Cui
WHAT IS KNOWN AND OBJECTIVE: The role of CYP3A5 in drug metabolism has been receiving attention because CYP3A5 may be more involved in the metabolism of CYP3A substrates in vivo than previously thought. The polymorphism of transporters, such as P-gp (P-glycoprotein) and breast cancer-related protein (BCRP), influences the metabolism of these substrates, and felodipine is a substrate of P-gp. The aim of this study was to evaluate the pharmacogenetic variability in the disposition of felodipine in healthy Chinese subjects...
February 28, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28212300/amorphous-amorphous-phase-separation-in-api-polymer-formulations
#11
Christian Luebbert, Fabian Huxoll, Gabriele Sadowski
The long-term stability of pharmaceutical formulations of poorly-soluble drugs in polymers determines their bioavailability and therapeutic applicability. However, these formulations do not only often tend to crystallize during storage, but also tend to undergo unwanted amorphous-amorphous phase separations (APS). Whereas the crystallization behavior of APIs in polymers has been measured and modeled during the last years, the APS phenomenon is still poorly understood. 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...
February 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28134976/multicomponent-solid-forms-of-felodipine-preparation-characterisation-physicochemical-and-in-vivo-studies
#12
Renu Chadha, Mohit Sharma, Jamshed Haneef
OBJECTIVES: This study aimed to improve biopharmaceutical parameters of the poorly soluble antihypertensive drug, felodipine, by preparing multicomponent solid forms using three coformers, viz. imidazole, nicotinamide and malonic acid. METHODS: The multicomponent solid forms were prepared by mechanochemical synthesis and characterised by various analytical techniques. These solid forms were further assessed for their physicochemical parameters. Pharmacokinetic and in-vivo antihypertensive activity was performed in rats...
March 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27987515/-study-on-the-properties-of-felodipine-solid-dispersions-prepared-by-different-technologies
#13
N Q Shi, H Zhang, Y Zhang, B Feng, Z Q Li, X R Qi
OBJECTIVE: To prepare felodipine/copovidone solid dispersions, which were made based on different preparation technologies. Insoluble felodipine was selected as the model drug in this research. This drug belonged to Biopharmaceutics Classification System II (BCSII) with insoluble property and good permeability across intestinal mucosa simultaneously. A comparative study was carried out for further investigating their corresponding pharmaceutical properties. METHODS: Felodipine/copovidone solid dispersions were achieved by four methods including spray-drying method, microwave-induced fusion quench cooling method, freeze-drying method and co-precipitation method...
December 18, 2016: Beijing da Xue Xue Bao. Yi Xue Ban, Journal of Peking University. Health Sciences
https://www.readbyqxmd.com/read/27986292/molecular-dynamics-simulation-of-amorphous-hydroxypropylmethylcellulose-and-its-mixtures-with-felodipine-and-water
#14
Tian-Xiang Xiang, Bradley D Anderson
Understanding drug-polymer molecular interactions, their miscibility, supersaturation potential, and the effects of water uptake may be invaluable for selecting amorphous polymer dispersions that can maximize the oral bioavailability of poorly water-soluble drugs. Molecular dynamics simulations were performed using a model for hydroxypropylmethylcellulose (HPMC) resembling the substitution patterns found experimentally. HPMC at low and high water contents (0.9%-23.0% wt/wt) and mixtures with a hydrophobic drug, felodipine (FEL), were constructed...
December 13, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27940083/statistical-investigation-of-simulated-fed-intestinal-media-composition-on-the-equilibrium-solubility-of-oral-drugs
#15
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
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...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27934534/partitioning-into-colloidal-structures-of-fasted-state-intestinal-fluid-studied-by-molecular-dynamics-simulations
#16
Michael Holmboe, Per Larsson, Jamshed Anwar, Christel A S Bergström
We performed molecular dynamics (MD) simulations to obtain insights into the structure and molecular interactions of colloidal structures present in fasted state intestinal fluid. Drug partitioning and interaction were studied with a mixed system of the bile salt taurocholate (TCH) and 1,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLiPC). Spontaneous aggregation of TCH and DLiPC from unconstrained MD simulations at the united-atom level using the Berger/Gromos54A7 force fields demonstrated that intermolecular hydrogen bonding between TCH molecules was an important factor in determining the overall TCH and DLiPC configuration...
December 6, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/27779454/effects-of-lercanidipine-hydrochloride-versus-felodipine-sustained-release-on-day-to-day-home-blood-pressure-variability
#17
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
https://www.readbyqxmd.com/read/27754044/os-14-01-an-estimated-optimal-hypertension-level-of-goals-on-drug-therapy-from-the-fever-trial
#18
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
https://www.readbyqxmd.com/read/27732883/optical-isomers-of-dihydropyridine-calcium-channel-blockers-display-enantiospecific-effects-on-the-expression-and-enzyme-activities-of-human-xenobiotics-metabolizing-cytochromes-p450
#19
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...
November 16, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/27681386/xylitol-as-a-potential-co-crystal-co-former-for-enhancing-dissolution-rate-of-felodipine-preparation-and-evaluation-of-sublingual-tablets
#20
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
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