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  1 / 1530 MEDLINE  
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[PMID]:29216584
[Au] Autor:DeBoyace K; Zdaniewski C; Wildfong PLD
[Ad] Endereço:Duquesne University Graduate School of Pharmaceutical Sciences, 600 Forbes Ave, Pittsburgh, PA 15282, United States.
[Ti] Título:Differential scanning calorimetry isothermal hold times can impact interpretations of drug-polymer dispersability in amorphous solid dispersions.
[So] Source:J Pharm Biomed Anal;150:43-50, 2018 Feb 20.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Differential scanning calorimetry (DSC) is a commonly employed analytical technique for the analysis and characterization of amorphous solid dispersions. However, steps typical of standard temperature programs can alter the material in situ. Data for two active pharmaceutical ingredients are detailed, wherein isothermal hold times, traditionally employed to remove thermal history and/or residual solvent, were observed to impact the observed dispersability of the compounds in polyvinylpyrrolidone vinyl-acetate copolymer (PVPva). Re-crystallized tolbutamide was observed to re-dissolve in PVPva, while terfenadine was observed to crystallize during the isothermal hold period. Exposing co-solidified drug-polymer mixtures to temperature changes and experimental hold times can potentially confound correct categorization of dispersability, particularly when DSC is used as the lone characterization technique. This work illustrates the importance of using a combination of techniques to improve the certainty of conclusions made with respect to the true, initial physical state of a co-solidified mixture.
[Mh] Termos MeSH primário: Varredura Diferencial de Calorimetria/métodos
Pirrolidinas/química
Terfenadina/química
Tolbutamida/química
Compostos de Vinila/química
[Mh] Termos MeSH secundário: Química Farmacêutica/métodos
Cristalização
Polímeros/química
Solubilidade
Solventes/química
Temperatura Ambiente
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Polymers); 0 (Pyrrolidines); 0 (Solvents); 0 (Vinyl Compounds); 0 (poly(vinylpyrrolidone-co-vinyl-acetate)); 7BA5G9Y06Q (Terfenadine); 982XCM1FOI (Tolbutamide)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180130
[Lr] Data última revisão:
180130
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171208
[St] Status:MEDLINE


  2 / 1530 MEDLINE  
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[PMID]:28768941
[Au] Autor:Kawakami M; Kitada R; Kurita T; Tokumura T
[Ad] Endereço:Laboratory of Pharmaceutics, Kagawa School of Pharmaceutical Sciences, Tokushima Bunri University.
[Ti] Título:A Method for Decreasing the Amount of the Drug Remaining on the Surfaces of the Mortar and Pestle after Grinding Small Amount of Tablets.
[So] Source:Yakugaku Zasshi;137(8):1017-1025, 2017.
[Is] ISSN:1347-5231
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo:The aim of the present study was to develop a method for grinding tablets with a mortar and pestle while reducing drug loss because grinding tablets is known to be associated with reductions in tablet weight and loss of the active drug. Seven kinds of tablets were subjected to grinding. The proportion (%) of the amount of the active drug in the powder remaining on the surfaces of the mortar and pestle relative to the total amount of the drug recovered (the recovery percent) was calculated. The recovery percent of the 7 kinds of tablets ranged from 17.2-35.9%, and the tablets' recovery percent decreased as the tablet weight increased. When the grinding was performed with 1 g of lactose monohydrate or 1 g of D-mannitol moistened with water, the recovery percent of the tablets decreased to 2.6-9.9% and 3.8-9.9%, respectively. The effects of the weight of lactose monohydrate on the recovery percent of Allegra 60 mg tablets were examined. It was found that at least 0.6 g of lactose monohydrate was required to have a sufficient effect on drug recovery. Therefore, additives that have stronger effects at lower amounts were sought. As a result, calcium monohydrogen phosphate was found to have the strongest effect on drug recovery. The addition of 0.4 g calcium monohydrogen phosphate resulted in the recovery percent of 5.1%, which was significantly lower than that of 15.0% observed after the addition of 0.4 g lactose monohydrate, and lower than the 6.8% of 1 g lactose monohydrate.
[Mh] Termos MeSH primário: Fosfatos de Cálcio
Composição de Medicamentos/instrumentação
Composição de Medicamentos/métodos
Excipientes
Comprimidos
Terfenadina/análogos & derivados
[Mh] Termos MeSH secundário: Adsorção
Lactose
Manitol
Pós
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Phosphates); 0 (Excipients); 0 (Powders); 0 (Tablets); 3OWL53L36A (Mannitol); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine); J2B2A4N98G (Lactose); O7TSZ97GEP (calcium phosphate, dibasic, dihydrate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170804
[St] Status:MEDLINE
[do] DOI:10.1248/yakushi.17-00041


  3 / 1530 MEDLINE  
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[PMID]:28570227
[Au] Autor:Teo SL; Santosa A; Bigliardi PL
[Ad] Endereço:National University Hospital, Singapore.
[Ti] Título:Stevens-Johnson Syndrome/Toxic Epidermal Necrolysis Overlap Induced by Fexofenadine.
[So] Source:J Investig Allergol Clin Immunol;27(3):191-193, 2017 Jun.
[Is] ISSN:1018-9068
[Cp] País de publicação:Spain
[La] Idioma:eng
[Mh] Termos MeSH primário: Antialérgicos/efeitos adversos
Hipersensibilidade a Drogas/etiologia
Síndrome de Stevens-Johnson/etiologia
Terfenadina/análogos & derivados
[Mh] Termos MeSH secundário: Hipersensibilidade a Drogas/diagnóstico
Feminino
Seres Humanos
Meia-Idade
Testes Cutâneos
Terfenadina/efeitos adversos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Allergic Agents); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine)
[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:170602
[St] Status:MEDLINE
[do] DOI:10.18176/jiaci.0158


  4 / 1530 MEDLINE  
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[PMID]:28188296
[Au] Autor:Turkanovic J; Ward MB; Gerber JP; Milne RW
[Ad] Endereço:School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, Australia.
[Ti] Título:Effect of Garlic, Gingko, and St. John's Wort Extracts on the Pharmacokinetics of Fexofenadine: A Mechanistic Study.
[So] Source:Drug Metab Dispos;45(5):569-575, 2017 May.
[Is] ISSN:1521-009X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to determine the effects of garlic and ginkgo herbal extracts on the pharmacokinetics of the P-glycoprotein (P-gp)/organic anion-transporting polypeptides (Oatps) substrate fexofenadine. Male rats were dosed orally with garlic (120 mg/kg), ginkgo (17 mg/kg), St. John's wort (SJW; 1000 mg/kg; positive control), or Milli-Q water for 14 days. On day 15, rats either were administered fexofenadine (orally or i.v.), had their livers isolated and perfused with fexofenadine, or had their small intestines divided into four segments (SI-SIV) and analyzed for P-gp and Oatp1a5. In vivo, SJW increased the clearance of i.v. administered fexofenadine by 28%. Garlic increased the area under the curve and maximum plasma concentration of orally administered fexofenadine by 47% and 85%, respectively. Ginkgo and SJW had no effect on the oral absorption of fexofenadine. In the perfused liver, garlic, ginkgo, and SJW increased the biliary clearance of fexofenadine with respect to perfusate by 71%, 121%, and 234%, respectively. SJW increased the biliary clearance relative to the liver concentration by 64%. The ratio of liver to perfusate concentrations significantly increased in all treated groups. The expression of Oatp1a5 in SI was increased by garlic (88%) and SJW (63%). There were no significant changes in the expression of P-gp. Induction of intestinal Oatp1a5 by garlic may explain the increased absorption of orally administered fexofenadine. Ginkgo had no effect on the expression of intestinal P-gp or Oatp1a5. A dual inductive effect by SJW on opposing intestinal epithelial transport by Oatp1a5 and P-gp remains a possibility.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Alho/química
Ginkgo biloba/química
Hypericum/química
Transportadores de Ânions Orgânicos Sódio-Independentes/metabolismo
Extratos Vegetais/farmacologia
Terfenadina/análogos & derivados
[Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética
Administração Oral
Animais
Interações Medicamentosas
Injeções Intravenosas
Intestinos/metabolismo
Fígado/metabolismo
Masculino
Transportadores de Ânions Orgânicos Sódio-Independentes/genética
Perfusão
Extratos Vegetais/isolamento & purificação
Ratos
Especificidade por Substrato
Terfenadina/administração & dosagem
Terfenadina/sangue
Terfenadina/farmacocinética
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Organic Anion Transporters, Sodium-Independent); 0 (Plant Extracts); 0 (Slco1a5 protein, rat); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine)
[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:170212
[St] Status:MEDLINE
[do] DOI:10.1124/dmd.116.073528


  5 / 1530 MEDLINE  
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[PMID]:28102715
[Au] Autor:Bedada SK; Appani R; Boga PK
[Ad] Endereço:a Drug Metabolism and Pharmacokinetics Division , University College of Pharmaceutical Sciences, Kakatiya University , Warangal , India.
[Ti] Título:Capsaicin pretreatment enhanced the bioavailability of fexofenadine in rats by P-glycoprotein modulation: in vitro, in situ and in vivo evaluation.
[So] Source:Drug Dev Ind Pharm;43(6):932-938, 2017 Jun.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND AND OBJECTIVE: Capsaicin is the main pungent principle present in chili peppers has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro, which may have the potential to modulate bioavailability of P-gp substrates. Therefore, purpose of this study was to evaluate the effect of capsaicin on intestinal absorption and bioavailability of fexofenadine, a P-gp substrate in rats. METHODS: The mechanistic evaluation was determined by non-everted sac and intestinal perfusion studies to explore the intestinal absorption of fexofenadine. These results were confirmed by an in vivo pharmacokinetic study of oral administered fexofenadine in rats. RESULTS: The intestinal transport and apparent permeability (P ) of fexofenadine were increased significantly by 2.8 and 2.6 fold, respectively, in ileum of capsaicin treated rats when compared to control group. Similarly, absorption rate constant (K ), fraction absorbed (F ) and effective permeability (P ) of fexofenadine were increased significantly by 2.8, 2.9 and 3.4 fold, respectively, in ileum of rats pretreated with capsaicin when compared to control group. In addition, maximum plasma concentration (C ) and area under the concentration-time curve (AUC) were increased significantly by 2.3 and 2.4 fold, respectively, in rats pretreated with capsaicin as compared to control group. Furthermore, obtained results in rats pretreated with capsaicin were comparable to verapamil (positive control) treated rats. CONCLUSIONS: Capsaicin pretreatment significantly enhanced the intestinal absorption and bioavailability of fexofenadine in rats likely by inhibition of P-gp mediated cellular efflux, suggesting that the combined use of capsaicin with P-gp substrates may require close monitoring for potential drug interactions.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Capsaicina/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacocinética
Terfenadina/análogos & derivados
[Mh] Termos MeSH secundário: Antagonistas Adrenérgicos beta/farmacocinética
Animais
Área Sob a Curva
Disponibilidade Biológica
Antagonistas dos Receptores Histamínicos H1/administração & dosagem
Íleo/efeitos dos fármacos
Íleo/metabolismo
Técnicas In Vitro
Absorção Intestinal/efeitos dos fármacos
Masculino
Perfusão
Permeabilidade/efeitos dos fármacos
Propranolol/farmacocinética
Ratos
Ratos Wistar
Terfenadina/administração & dosagem
Terfenadina/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Adrenergic beta-Antagonists); 0 (Histamine H1 Antagonists); 7BA5G9Y06Q (Terfenadine); 9Y8NXQ24VQ (Propranolol); E6582LOH6V (fexofenadine); S07O44R1ZM (Capsaicin)
[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:170120
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1285310


  6 / 1530 MEDLINE  
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[PMID]:28090646
[Au] Autor:Li F; Howard KD; Myers MJ
[Ad] Endereço:Division of Applied Veterinary Research, Office of Research, Center for Veterinary Medicine, U.S. Food and Drug Administration, Laurel, MD, USA.
[Ti] Título:Influence of P-glycoprotein on the disposition of fexofenadine and its enantiomers.
[So] Source:J Pharm Pharmacol;69(3):274-284, 2017 Mar.
[Is] ISSN:2042-7158
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: P-glycoprotein (P-gp) is responsible for the efflux of a broad variety of human and veterinary drugs. Canine P-gp polymorphisms alter drug disposition and toxicity, but their impact on the disposition of enantiomeric drugs is unknown. Using fexofenadine as a model compound, we developed and validated HPLC-fluorescence methods to determine the effect of P-gp on the disposition of fexofenadine and its enantiomers. METHODS: A chiral CD-Ph column was used for the separation of (R) and (S)-fexofenadine. Determination of racemic fexofenadine was achieved on an XDB-CN column. Fexofenadine and its enantiomers were detected by fluorescence at the excitation wavelength of 220 nm and emission wavelength of 300 nm. These methods were used to measure concentrations of fexofenadine and its enantiomers in Collie plasma after oral administration. KEY FINDINGS: This study demonstrates that P-gp prefers to transport (S)-fexofenadine, and P-gp deficiency causes the increase in both (R)-fexofenadine and (S)-fexofenadine in plasma. Racemic fexofenadine, (R)-fexofenadine and (S)-fexofenadine were increased in ABCB1-1Δ Collies (118.7, 72.0 and 48.3 ng/ml) compared to wild-type Collies (25.0, 16.5 and 7.7 ng/ml) at 1 h postadministration. The results demonstrate that the stereoselectivity of P-gp plays a key role in the disposition of fexofenadine enantiomers. CONCLUSIONS: The information derived from this drug model will be used to determine whether additional safety or efficacy requirements are necessary for enantiomeric drugs that would be used in dogs or humans.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo
Terfenadina/análogos & derivados
[Mh] Termos MeSH secundário: Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo
Animais
Cromatografia Líquida de Alta Pressão/métodos
Cães
Fluorescência
Estereoisomerismo
Terfenadina/sangue
Terfenadina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ABCB1 protein, human); 0 (ATP Binding Cassette Transporter, Sub-Family B); 0 (ATP-Binding Cassette, Sub-Family B, Member 1); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170117
[St] Status:MEDLINE
[do] DOI:10.1111/jphp.12687


  7 / 1530 MEDLINE  
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[PMID]:28058761
[Au] Autor:Kanthiah S; Kannappan V
[Ad] Endereço:Department of Pharmacy, Faculty of Engineering and Technology, Annamalai University, Annamalai Nagar, Tamil Nadu, India.
[Ti] Título:D-Optimal mixture design optimization of an HPLC method for simultaneous determination of commonly used antihistaminic parent molecules and their active metabolites in human serum and urine.
[So] Source:Biomed Chromatogr;31(8), 2017 Aug.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:This study describes a specific, precise, sensitive and accurate method for simultaneous determination of hydroxyzine, loratadine, terfenadine, rupatadine and their main active metabolites cetirizine, desloratadine and fexofenadine, in serum and urine using meclizine as an internal standard. Solid-phase extraction method for sample clean-up and preconcentration of analytes was carried out using Phenomenex Strata-X-C and Strata X polymeric cartridges. Chromatographic analysis was performed on a Phenomenex cyano (150 × 4.6 mm i.d., 5 µm) analytical column. A D-optimal mixture design methodology was used to evaluate the effect of changes in mobile phase compositions on dependent variables and optimization of the response of interest. The mixture design experiments were performed and results were analyzed. The region of ideal mobile phase composition consisting of acetonitrile-methanol-ammonium acetate buffer (40 mm; pH 3.8 adjusted with acetic acid): 18:36:46% v/v/v was identified by a graphical optimization technique using an overlay plot. While using this optimized condition all analytes were baseline resolved in <10 min. Solvent mixtures were delivered at 1.5 mL/min flow rate and analytes peaks were detected at 222 nm. The proposed bioanalytical method was validated according to US Food and Drug Administration guidelines. The proposed method was sensitive with detection limits of 0.06-0.15 µg/mL in serum and urine samples. Relative standard deviation for inter- and intra-day precision data was found to be <7%. The proposed method may find application in the determination of selected antihistaminic drugs in biological fluids.
[Mh] Termos MeSH primário: Antialérgicos/sangue
Antialérgicos/urina
Cromatografia Líquida de Alta Pressão/métodos
Antagonistas dos Receptores Histamínicos H1/sangue
Antagonistas dos Receptores Histamínicos H1/urina
[Mh] Termos MeSH secundário: Antialérgicos/metabolismo
Ciproeptadina/análogos & derivados
Ciproeptadina/sangue
Ciproeptadina/metabolismo
Ciproeptadina/urina
Antagonistas dos Receptores Histamínicos H1/metabolismo
Seres Humanos
Hidroxizina/sangue
Hidroxizina/metabolismo
Hidroxizina/urina
Limite de Detecção
Loratadina/sangue
Loratadina/metabolismo
Loratadina/urina
Extração em Fase Sólida/métodos
Terfenadina/sangue
Terfenadina/metabolismo
Terfenadina/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Anti-Allergic Agents); 0 (Histamine H1 Antagonists); 2AE8M83G3E (rupatadine); 2YHB6175DO (Cyproheptadine); 30S50YM8OG (Hydroxyzine); 7AJO3BO7QN (Loratadine); 7BA5G9Y06Q (Terfenadine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170107
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.3932


  8 / 1530 MEDLINE  
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[PMID]:28040476
[Au] Autor:Hishinuma S; Kosaka K; Akatsu C; Uesawa Y; Fukui H; Shoji M
[Ad] Endereço:Department of Pharmacodynamics, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan. Electronic address: hishi@my-pharm.ac.jp.
[Ti] Título:Asp73-dependent and -independent regulation of the affinity of ligands for human histamine H receptors by Na .
[So] Source:Biochem Pharmacol;128:46-54, 2017 Mar 15.
[Is] ISSN:1873-2968
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The affinity of ligands for G-protein-coupled receptors (GPCRs) is allosterically regulated by Na via a highly conserved aspartate residue (Asp ) in the second transmembrane domain of GPCRs. In the present study, we examined the Na -mediated regulation of the affinity of ligands for G -protein-coupled human histamine H receptors in Chinese hamster ovary cells. The affinities of 3 agonists and 20 antihistamines were evaluated by their displacement curves against the binding of [ H]-mepyramine to membrane preparations in the presence or absence of 100mM NaCl. The affinities of most drugs including histamine, an agonist, and d-chlorpheniramine, a first-generation antihistamine, were reduced by NaCl, with the extent of NaCl-mediated changes varying widely between drugs. In contrast, the affinities of some second-generation antihistamines such as fexofenadine were increased by NaCl. These changes were retained in intact cells. The mutation of Asp (Asp73) to asparagine abrogated NaCl-induced reductions in affinities for histamine and d-chlorpheniramine, but not NaCl-induced increases in the affinity for fexofenadine. Quantitative structure-activity relationship (QSAR) analyses showed that these Na -mediated changes were explained and predicted by a combination of the molecular energies and implicit solvation energies of the compounds. These results suggest that Na diversely regulates the affinity of ligands for H receptors from the extracellular sites of receptors via Asp73-dependent and -independent mechanisms in a manner that depends on the physicochemical properties of ligands. These results may contribute to a deeper understanding of the fundamental mechanisms by which the affinity of ligands for their receptors is allosterically regulated by Na .
[Mh] Termos MeSH primário: Ácido Aspártico/genética
Receptores Histamínicos H1/fisiologia
Cloreto de Sódio/farmacologia
[Mh] Termos MeSH secundário: Animais
Células CHO
Cátions Monovalentes
Clorfeniramina/farmacologia
Cricetulus
Histamina/farmacologia
Agonistas dos Receptores Histamínicos/farmacologia
Antagonistas dos Receptores Histamínicos H1/farmacologia
Seres Humanos
Ligantes
Mutação
Relação Quantitativa Estrutura-Atividade
Ensaio Radioligante
Receptores Histamínicos H1/genética
Terfenadina/análogos & derivados
Terfenadina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cations, Monovalent); 0 (Histamine Agonists); 0 (Histamine H1 Antagonists); 0 (Ligands); 0 (Receptors, Histamine H1); 30KYC7MIAI (Aspartic Acid); 3U6IO1965U (Chlorpheniramine); 451W47IQ8X (Sodium Chloride); 7BA5G9Y06Q (Terfenadine); 820484N8I3 (Histamine); E6582LOH6V (fexofenadine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170502
[Lr] Data última revisão:
170502
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170102
[St] Status:MEDLINE


  9 / 1530 MEDLINE  
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[PMID]:27983859
[Au] Autor:Sjögren E; Thörn H; Tannergren C
[Ad] Endereço:Department of Pharmacy, Uppsala University , Box 580, S-751 23 Uppsala, Sweden.
[Ti] Título:Reply to "Comment on 'In Silico Modeling of Gastrointestinal Drug Absorption: Predictive Performance of Three Physiologically Based Absorption Models'".
[So] Source:Mol Pharm;14(1):340-343, 2017 Jan 03.
[Is] ISSN:1543-8392
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This is a reply to the comment on "In Silico Modeling of Gastrointestinal Drug Absorption: Predictive Performance of Three Physiologically Based Absorption Models" by Turner and other Simcyp associates. In the reply we address the major concerns raised by Turner et al. regarding the methodology to compare the predictive performance of the different absorption models and at the same time ensure that the systemic pharmacokinetic input was exactly the same for the different models; the selection of the human effective permeability value of fexofenadine; the adoption of model default values and settings; and how supersaturation/precipitation was handled. In addition, we also further discuss aspects related to differences in in silico models and the potential implications of such differences. Our original report should be viewed as the starting point in a thorough and transparent review of absorption prediction models with the overall aim of improving their application as validated tools for bridging studies of active pharmaceutical ingredients from various sources and origins in a regulatory context. With this reply we encourage other independent investigators to perform further model evaluations of commercial as well as other existing or recently implemented models. This will boost the overall progression of physiologically based biopharmaceutical models for predicting and simulating intestinal drug absorption both in research and development and in a regulatory context.
[Mh] Termos MeSH primário: Fármacos Gastrointestinais/metabolismo
Absorção Intestinal/fisiologia
Intestinos/metabolismo
Preparações Farmacêuticas/metabolismo
[Mh] Termos MeSH secundário: Biofarmácia/métodos
Simulação por Computador
Seres Humanos
Modelos Biológicos
Terfenadina/análogos & derivados
Terfenadina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Gastrointestinal Agents); 0 (Pharmaceutical Preparations); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171025
[Lr] Data última revisão:
171025
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161217
[St] Status:MEDLINE
[do] DOI:10.1021/acs.molpharmaceut.6b00775


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[PMID]:27981349
[Au] Autor:Bedada SK; Boga PK
[Ad] Endereço:Drug Metabolism and Pharmacokinetics Division, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, 506009, Telangana State, India. satishbedada@gmail.com.
[Ti] Título:The influence of piperine on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers.
[So] Source:Eur J Clin Pharmacol;73(3):343-349, 2017 Mar.
[Is] ISSN:1432-1041
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Piperine (PIP) has been found to inhibit P-glycoprotein (P-gp) function in rats, suggesting that it may have the potential to modulate P-gp-mediated drug efflux in humans. The aim of this study was to evaluate the effect of PIP on the pharmacokinetics of fexofenadine (FEX), a P-gp substrate, in healthy volunteers. METHODS: An open-label, two-period, sequential study involving 12 healthy volunteers was conducted. A single oral dose of FEX 120 mg was given to volunteers during the control phase and after the treatment phase. A once-daily oral dose of PIP 20 mg was given to volunteers during the treatment phase (10 days). Blood samples were collected at predefined time intervals, and plasma samples containing FEX were analyzed by liquid chromatography-tandem mass spectrometry. RESULTS: Treatment with PIP significantly increased maximum plasma concentration of FEX [406.9 (control) vs. 767 ng/mL (treatment)] and area under the plasma concentration-time curve [3403.7 (control) vs. 5724.7 ng.h/mL (treatment)] when compared to the control phase. In contrast, PIP treatment significantly decreased apparent oral clearance of FEX [35.4 (control) vs. 20.7 L/h (treatment)] as compared to the control. There was no significant change observed in the half life and renal clearance of FEX between the treatment phase and control phase. CONCLUSIONS: The results suggest that altered pharmacokinetics and enhanced bioavailability of FEX might be attributed to PIP-mediated inhibition of P-gp drug efflux. Therefore, intake of PIP or dietary supplements containing PIP may potentially enhance the absorption or bioavailability of P-gp substrate drugs in addition to FEX.
[Mh] Termos MeSH primário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/efeitos dos fármacos
Alcaloides/farmacologia
Benzodioxóis/farmacologia
Antagonistas dos Receptores Histamínicos H1 não Sedativos/farmacocinética
Piperidinas/farmacologia
Alcamidas Poli-Insaturadas/farmacologia
Terfenadina/análogos & derivados
[Mh] Termos MeSH secundário: Adulto
Área Sob a Curva
Disponibilidade Biológica
Meia-Vida
Voluntários Saudáveis
Antagonistas dos Receptores Histamínicos H1 não Sedativos/farmacologia
Seres Humanos
Masculino
Terfenadina/farmacocinética
Terfenadina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Alkaloids); 0 (Benzodioxoles); 0 (Histamine H1 Antagonists, Non-Sedating); 0 (Piperidines); 0 (Polyunsaturated Alkamides); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine); U71XL721QK (piperine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161217
[St] Status:MEDLINE
[do] DOI:10.1007/s00228-016-2173-3



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