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[PMID]: 28189955 [Au] Autor: Ahmed S; Atia NN; Bakr Ali MF [Ad] Endereço: Pharmacognosy and Pharmaceutical Chemistry Department, College of Pharmacy Taibah University, Al Madinah AlMunawarah 30001, Saudi Arabia; Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. Electronic address: sameh_aa@yahoo.com. [Ti] Título: Ultrasound assisted dispersive liquid-liquid microextraction coupled with high performance liquid chromatography designated for bioavailability studies of felodipine combinations in rat plasma. [So] Source: J Chromatogr B Analyt Technol Biomed Life Sci;1046:200-210, 2017 Mar 01. [Is] ISSN: 1873-376X [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: Felodipine (FLD), a calcium channel antagonist, is commonly prescribed for the treatment of hypertension either with Metoprolol (MET) or Ramipril (RAM) in two different drug combinations. FLD has high plasma protein binding ability affecting its extraction recoveries from plasma samples. Hence, a specific ultrasound assisted dispersive liquid-liquid microextraction (UA-DLLME) method coupled with HPLC using photodiode array detector was developed and validated for the simultaneous determination of FLD, MET and RAM in rat plasma after oral administration of these combinations. The factors affecting UA-DLLME were carefully optimized. In this study, UA-DLLME method could provide simple and efficient plasma extraction procedures with superior recovery results. Under optimum condition, all target drugs were separated within 13min. The validation procedures was carried out in agreement with US-FDA guidelines and shown to be suitable for anticipated purposes. Linear calibration ranges were obtained in the range 0.05-2.0µgmL for FLD and MET and 0.1-2.0µgmL for RAM with detection limits of 0.013-0.031µgmL for all the studied drug combinations. The%RSD for inter-day and intra-day precisions was in range of 0.63-3.85% and the accuracy results were in the range of 92.13-100.5%. The validated UA-DLLME-HPLC method was successfully applied for the bioavailability studies of FLD, MET and RAM. The pharmacokinetic parameters were calculated for all the investigated drugs in rats after single-dose administrations of two different drug combinations. Although FLD was bioequivalent in the two formulations, a small increase in plasma levels of MET and RAM was found in the presence of FLD. [Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos Felodipino/sangue Microextração em Fase Líquida/métodos Sonicação/métodos [Mh] Termos MeSH secundário: Animais Disponibilidade Biológica Monitoramento de Medicamentos Estabilidade de Medicamentos Felodipino/química Felodipino/farmacocinética Limite de Detecção Modelos Lineares Masculino Ratos Ratos Wistar Reprodutibilidade dos Testes [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: OL961R6O2C (Felodipine) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170522 [Lr] Data última revisão: 170522 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170213 [St] Status: MEDLINE

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[PMID]: 28134976 [Au] Autor: Chadha R; Sharma M; Haneef J [Ad] Endereço: University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Chandigarh, India. [Ti] Título: Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies. [So] Source: J Pharm Pharmacol;69(3):254-264, 2017 Mar. [Is] ISSN: 2042-7158 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: 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. KEY FINDINGS: Felodipine (FEL) was found to be cocrystallised with imidazole (FEL-IM) while it formed eutectic with nicotinamide (FEL-NCT) and malonic acid (FEL-MA). Cocrystal was sustained by NH…N and NH….O hydrogen-bonded network. Solubility and intrinsic dissolution studies in 0.1 N HCl (pH 1.2) revealed that eutectics exhibited higher solubility and release rate than cocrystal vis-a-vis pure drug and were found to be stable under accelerated storage condition. Significant enhancement of bioavailability was observed in eutectics (3.5- to twofold) and cocrystal (1.3-fold) compared with the pure drug. Antihypertensive activity of new solid forms in an animal model showed a marked decrease in systolic blood pressure. CONCLUSIONS: Mechanochemical approach was successful to prepare multicomponent solid forms that have the potential to improve biopharmaceutical parameters of the poorly soluble drug, FEL. [Mh] Termos MeSH primário: Anti-Hipertensivos/química Anti-Hipertensivos/farmacologia Felodipino/química Felodipino/farmacologia [Mh] Termos MeSH secundário: Animais Anti-Hipertensivos/metabolismo Disponibilidade Biológica Química Farmacêutica/métodos Cristalização/métodos Composição de Medicamentos/métodos Estabilidade de Medicamentos Felodipino/metabolismo Masculino Malonatos/química Ratos Ratos Wistar Solubilidade Difração de Raios X [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antihypertensive Agents); 0 (Malonates); 9KX7ZMG0MK (malonic acid); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 170608 [Lr] Data última revisão: 170608 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170131 [St] Status: MEDLINE [do] DOI: 10.1111/jphp.12685

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[PMID]: 27173987 [Au] Autor: Fasinu P; Choonara YE; Kumar P; du Toit LC; Bijukumar D; Khan RA; Pillay V [Ad] Endereço: Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193, South Africa. [Ti] Título: Enhancement of the Oral Bioavailability of Felodipine Employing 8-Arm-Poly(Ethylene Glycol): In Vivo, In Vitro and In Silico Evaluation. [So] Source: AAPS PharmSciTech;18(3):617-628, 2017 Apr. [Is] ISSN: 1530-9932 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: 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. In vitro investigation of 8-arm-poly(ethylene glycol) against CYP3A4-catalyzed felodipine metabolism employing human liver microsomes compared closely with naringenin, a typical grapefruit flavonoid, yielding IC values of 7.22 and 121.97 µM, respectively. The investigated potential of 8-arm-poly(ethylene glycol) in oral drug delivery yielded satisfactory in vitro drug release results. The in vivo studies of the effects of 8-arm-poly(ethylene glycol) on the oral bioavailability of felodipine as performed in the Large White pig model showed a >100% increase in plasma felodipine levels compared to controls, with no apparent effect on systemic felodipine clearance. The outcome of this research presents a novel CYP3A4 inhibitor, 8-arm-poly(ethylene glycol) for oral bioavailability enhancement. [Mh] Termos MeSH primário: Etilenoglicóis/química Felodipino/química Felodipino/metabolismo [Mh] Termos MeSH secundário: Administração Oral Adulto Idoso Animais Disponibilidade Biológica Citocromo P-450 CYP3A Sistemas de Liberação de Medicamentos/métodos Feminino Flavanonas/metabolismo Flavonoides/metabolismo Seres Humanos Cinética Fígado/metabolismo Masculino Microssomos Hepáticos/metabolismo Meia-Idade Suínos Adulto Jovem [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Ethylene Glycols); 0 (Flavanones); 0 (Flavonoids); EC 1.14.14.1 (Cytochrome P-450 CYP3A); HN5425SBF2 (naringenin); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1707 [Cu] Atualização por classe: 170713 [Lr] Data última revisão: 170713 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160514 [St] Status: MEDLINE [do] DOI: 10.1208/s12249-016-0545-8

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[PMID]: 28375107 [Au] Autor: Mori D; Makwana J; Parmar R; Patel K; Chavda J [Ad] Endereço: BK Mody Government Pharmacy College, Rajkot, Gujarat, India. [Ti] Título: Formulation, evaluation and optimization of the felodipine nanosuspension to be used for direct compression to tablet for in vitro dissolution enhancement. [So] Source: Pak J Pharm Sci;29(6):1927-1936, 2016 Nov. [Is] ISSN: 1011-601X [Cp] País de publicação: Pakistan [La] Idioma: eng [Ab] Resumo: 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. The particle size of 201 nm and increase in saturation solubility of nearly 9 folds were obtained for optimize batch. The prepared nano suspension of drug was used as a granulating agent to form tablets having Microcrystalline Cellulose (MCC) as diluents. In vitro Drug release study indicates that more than 90% of the drug releases in 30 minutes. Preparing the nano suspension of the low solubility drug is an effective method to increase its saturation solubility. This nano suspension can be prepared effectively by combination of high-speed homogenization and media milling which is also very economical as well. [Mh] Termos MeSH primário: Bloqueadores dos Canais de Cálcio/química Felodipino/química Nanopartículas [Mh] Termos MeSH secundário: Administração Oral Bloqueadores dos Canais de Cálcio/administração & dosagem Celulose/química Composição de Medicamentos Estabilidade de Medicamentos Excipientes/química Felodipino/administração & dosagem Derivados da Hipromelose/química Cinética Nanotecnologia Tamanho da Partícula Poloxâmero/química Polissorbatos/química Solubilidade Espectroscopia de Infravermelho com Transformada de Fourier Comprimidos Tecnologia Farmacêutica/métodos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Calcium Channel Blockers); 0 (Excipients); 0 (Polysorbates); 0 (Tablets); 106392-12-5 (Poloxamer); 3NXW29V3WO (Hypromellose Derivatives); 9004-34-6 (Cellulose); OL961R6O2C (Felodipine); OP1R32D61U (microcrystalline cellulose) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171103 [Lr] Data última revisão: 171103 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170405 [St] Status: MEDLINE

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[PMID]: 27987515 [Au] Autor: Shi NQ; Zhang H; Zhang Y; Feng B; Li ZQ; Qi XR [Ad] Endereço: Jilin Medical University, Jilin 132013, Jilin, China; School of Life Science, Jilin University, Changchun 130012, China. [Ti] Título: [Study on the properties of felodipine solid dispersions prepared by different technologies]. [So] Source: Beijing Da Xue Xue Bao Yi Xue Ban;48(6):1067-1073, 2016 12 18. [Is] ISSN: 1671-167X [Cp] País de publicação: China [La] Idioma: chi [Ab] Resumo: 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. These solid dispersions were produced based on corresponding processes that corresponded to these methods. Internal properties of co-povidone solid dispersions were analyzed by various approaches including scanning electron microscope (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). The improvement on insoluble properties of felodipine by solid dispersions produced by different technologies was characterized by dissolution experiments based on dissolution instrument. Crystallization inhibition effect of polymers against drugs was studied by supersaturated experiments through determining the concentration value at different time points. RESULTS: The internal drug was dispersed in amorphous form in solid dispersions produced by spray-drying, microwave method, microwave/quench-cooling method and co-precipitation method. Freeze-drying method resulted in a form of crystal in felodipine/copovidone solid dispersions. Compared with other technologies, microwave-induced quench cooling method could significantly improve the dissolution of insoluble drug felodipine (P<0.05). The dissolution concentration reached approximately 4.65 mg/L at 60 min time point. Copovidone could inhibit or retard the crystallization of felodipine in a supersaturated state. In the solution pre-dissolved with maximum copoyidone polymer, the minimum crystallization rate of supersaturated felodipine was observed at 240 min time point. The value of crystallization rate was 0.19 mg/(L×min). CONCLUSION: The study is helpful to understand and clarify the internal properties of solid dispersions obtained by different technologies. The research also provides beneficial consultation for the choice of technology in practical production of drug-polymer solid dispersions. [Mh] Termos MeSH primário: Composição de Medicamentos/métodos Felodipino/química Pirrolidinas/química Solubilidade Compostos de Vinila/química [Mh] Termos MeSH secundário: Varredura Diferencial de Calorimetria Precipitação Química Cristalização Dessecação Portadores de Fármacos/química Micro-Ondas Polímeros Povidona Difração de Raios X [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Drug Carriers); 0 (Polymers); 0 (Pyrrolidines); 0 (Vinyl Compounds); 0 (poly(vinylpyrrolidone-co-vinyl-acetate)); FZ989GH94E (Povidone); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161218 [St] Status: MEDLINE

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[PMID]: 27594210 [Au] Autor: Alhijjaj M; Belton P; Qi S [Ad] Endereço: School of Pharmacy, University of East Anglia, Norwich, Norfolk NR4 7TJ, UK; Department of Pharmaceutics, College of Pharmacy, University of Basrah, Basrah, Iraq. [Ti] Título: 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. [So] Source: Eur J Pharm Biopharm;108:111-125, 2016 Nov. [Is] ISSN: 1873-3441 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: 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. 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 of processability. The polymer blends exhibited excellent printability and were suitable for processing using a commercially available FDM 3D printer. With 10% drug loading, all characterization data indicated that the model drug was molecularly dispersed in the matrices. During in vitro dissolution testing, it was clear that the disintegration behavior of the formulations significantly influenced the rates of drug release. Eudragit EPO based blend dispersions showed bulk disintegration; whereas the Soluplus based blends showed the 'peeling' style disintegration of strip-by-strip. The results indicated that interplay of the miscibility between excipients in the blends, the solubility of the materials in the dissolution media and the degree of fusion between the printed strips during FDM process can be used to manipulate the drug release rate of the dispersions. This brings new insight into the design principles of controlled release formulations using FDM 3D printing. [Mh] Termos MeSH primário: Portadores de Fármacos/química Sistemas de Liberação de Medicamentos Liberação Controlada de Fármacos Polímeros/química Impressão Tridimensional [Mh] Termos MeSH secundário: Varredura Diferencial de Calorimetria Excipientes Felodipino/química Concentração de Íons de Hidrogênio Microscopia Eletrônica de Varredura Tamanho da Partícula Polietilenoglicóis/química Solubilidade Espectroscopia de Infravermelho com Transformada de Fourier Temperatura Ambiente Termogravimetria [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Drug Carriers); 0 (Excipients); 0 (Polymers); 30IQX730WE (Polyethylene Glycols); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170924 [Lr] Data última revisão: 170924 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160906 [St] Status: MEDLINE

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[PMID]: 27562708 [Au] Autor: Wu L; Wang L; Wang S; Xiao T; Chen M; Shao Q; York P; Singh V; Yin X; Gu J; Zhang J [Ad] Endereço: School of Life Sciences, Jilin University, Changchun 130012, China; Center for Drug Delivery Systems, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201210, China. [Ti] Título: Three dimensional structural insight of laser drilled orifices in osmotic pump tablets. [So] Source: Eur J Pharm Sci;93:287-94, 2016 Oct 10. [Is] ISSN: 1879-0720 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: 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. The synchrotron radiation based Fourier transform infrared microspectroscopy mapping showed that there was no apparent chemical change in the surrounding area of the orifice compared with the normal membrane region. Thus SR-µCT was successfully applied to marketed felodipine osmotic pumps for architectural evaluation of the orifices. 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. [Mh] Termos MeSH primário: Osmose Comprimidos/química [Mh] Termos MeSH secundário: Preparações de Ação Retardada/química Sistemas de Liberação de Medicamentos Felodipino/química Lasers Síncrotrons Microtomografia por Raio-X [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Delayed-Action Preparations); 0 (Tablets); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170417 [Lr] Data última revisão: 170417 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160827 [St] Status: MEDLINE

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[PMID]: 27481881 [Au] Autor: Bailey DG; Dresser GK; Urquhart BL; Freeman DJ; Arnold JM [Ad] Endereço: Lawson Health Research Institute, London Health Sciences Centre, Western University, London, Ontario, Canada. [Ti] Título: Coffee-Antihypertensive Drug Interaction: A Hemodynamic and Pharmacokinetic Study With Felodipine. [So] Source: Am J Hypertens;29(12):1386-1393, 2016 Dec 01. [Is] ISSN: 1941-7225 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: OBJECTIVES: A period of abstinence from coffee to permit caffeine elimination appears to enable increased blood pressure on subsequent exposure. We hypothesized that this would offset the antihypertensive effect of the dihydropyridine calcium channel blocker felodipine. METHODS: A randomized, single-dose, crossover study assessed hemodynamic and pharmacokinetic effects following 2 days without coffee and caffeine-containing foods. Consistently brewed black coffee (2×300ml), felodipine maximum recommended dose (10mg), and coffee plus felodipine were tested in middle-aged normotensive subjects. RESULTS: Pretreatment plasma caffeine concentrations were unquantifiable. After coffee, blood pressure changes (mm Hg) averaged over study hours 1-4 were increased for brachial systolic (7.6, P < 0.001) and diastolic (4.9, P < 0.001) and aortic systolic (7.4, P < 0.001), pulse (3.0, P < 0.05) and augmentation (1.4, P < 0.05) relative to baseline. After coffee plus felodipine, they were higher for brachial systolic (4.0, P < 0.05) and diastolic (3.9, P < 0.001) and aortic systolic (4.6, P < 0.05) compared to felodipine alone. The pressor effects of coffee and its modulation by felodipine were variable among individuals. Coffee containing caffeine (127mg) caused maximum pressor effect. Caffeine and felodipine pharmacokinetics were similar for coffee and felodipine given alone or in combination indicating an interaction having a pharmacodynamic basis. Plasma felodipine concentration-diastolic blood pressure reduction relationship shifted with coffee such that doubling the felodipine concentration would eliminate the pressor effect. However, this may increase the risk of adverse drug events particularly during the timeframe without coffee. CONCLUSION: Intermittent coffee ingestion might complicate hypertension diagnosis and management for many individuals. [Mh] Termos MeSH primário: Pressão Arterial/efeitos dos fármacos Cafeína/farmacocinética Bloqueadores dos Canais de Cálcio/farmacocinética Café Felodipino/farmacocinética Interações Alimento-Droga Vasodilatadores/farmacocinética [Mh] Termos MeSH secundário: Adulto Idoso Área Sob a Curva Cafeína/administração & dosagem Cafeína/efeitos adversos Cafeína/sangue Bloqueadores dos Canais de Cálcio/administração & dosagem Bloqueadores dos Canais de Cálcio/sangue Café/efeitos adversos Estudos Cross-Over Felodipino/administração & dosagem Felodipino/sangue Feminino Meia-Vida Seres Humanos Masculino Taxa de Depuração Metabólica Meia-Idade Resistência Vascular/efeitos dos fármacos Vasodilatadores/administração & dosagem Vasodilatadores/sangue [Pt] Tipo de publicação: JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL [Nm] Nome de substância: 0 (Calcium Channel Blockers); 0 (Coffee); 0 (Vasodilator Agents); 3G6A5W338E (Caffeine); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171023 [Lr] Data última revisão: 171023 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160803 [St] Status: MEDLINE [do] DOI: 10.1093/ajh/hpw081

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[PMID]: 27329674 [Au] Autor: Rydberg HA; Yanez Arteta M; Berg S; Lindfors L; Sigfridsson K [Ad] Endereço: Pharmaceutical Science, AstraZeneca R&D Gothenburg, S-431 83 Mölndal, Sweden. [Ti] Título: Probing adsorption of DSPE-PEG2000 and DSPE-PEG5000 to the surface of felodipine and griseofulvin nanocrystals. [So] Source: Int J Pharm;510(1):232-9, 2016 Aug 20. [Is] ISSN: 1873-3476 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: 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. Using quartz crystal microbalance with dissipation monitoring both mass adsorption and the thickness of the adsorbed layer were estimated. The results indicate that the PEGylated lipids are adsorbed as flat layers of around 1-3nm, and that DSPE-PEG5000 forms a thicker layer compared with DSPE-PEG2000. In addition, the mass adsorption to the drug crystals and the model surface are seemingly comparable. Furthermore, both DSPE-PEG2000 and DSPE-PEG5000 rendered stable drug nanocrystals, with a somewhat higher surface binding and stability seen for DSPE-PEG2000. These results suggest DSPE-PEG2000 and DSPE-PEG5000 as efficient nanocrystal stabilizers, with DSPE-PEG2000 giving a somewhat higher surface coverage and superior colloidal stability, whereas DSPE-PEG5000 shows a more extended structure that may have advantages for prolongation of circulation time in vivo and facilitation for targeting modifications. [Mh] Termos MeSH primário: Felodipino/metabolismo Griseofulvina/metabolismo Nanopartículas/metabolismo Fosfatidiletanolaminas/metabolismo Polietilenoglicóis/metabolismo [Mh] Termos MeSH secundário: Adsorção Felodipino/química Griseofulvina/química Nanopartículas/química Tamanho da Partícula Fosfatidiletanolaminas/química Polietilenoglicóis/química Propriedades de Superfície [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000)); 0 (Phosphatidylethanolamines); 30IQX730WE (Polyethylene Glycols); 32HRV3E3D5 (Griseofulvin); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170419 [Lr] Data última revisão: 170419 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160623 [St] Status: MEDLINE

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[PMID]: 27299377 [Au] Autor: Mehta M; Suryanarayanan R [Ad] Endereço: Department of Pharmaceutics, University of Minnesota , Minneapolis, Minnesota 55455, United States. [Ti] Título: Accelerated Physical Stability Testing of Amorphous Dispersions. [So] Source: Mol Pharm;13(8):2661-6, 2016 Aug 01. [Is] ISSN: 1543-8392 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: 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. With an increase in water content, the α-relaxation time as well as the time for 1% w/w felodipine crystallization decreased. The relaxation times of the systems, obtained with different water concentration, overlapped when the temperature was scaled (Tg/T). The temperature dependencies of the α-relaxation time as well as the crystallization time were unaffected by the water concentration. Thus, the value of the coupling coefficient, up to a water concentration of 1.8% w/w, was approximately constant. Based on these findings, the use of "water sorption" is proposed to build predictive models for crystallization in slow crystallizing dispersions. [Mh] Termos MeSH primário: Felodipino/química [Mh] Termos MeSH secundário: Varredura Diferencial de Calorimetria Cristalização Espectroscopia Dielétrica Água/química Difração de Raios X [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 059QF0KO0R (Water); OL961R6O2C (Felodipine) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171020 [Lr] Data última revisão: 171020 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160615 [St] Status: MEDLINE [do] DOI: 10.1021/acs.molpharmaceut.6b00218

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