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[PMID]:28867759
[Au] Autor:Kadhum WR; Hada T; Hijikuro I; Todo H; Sugibayashi K
[Ad] Endereço:Faculty of Pharmacy and Pharmaceutical Sciences, Josai University.
[Ti] Título:Development and Optimization of Orally and Topically Applied Liquid Crystal Drug Formulations.
[So] Source:J Oleo Sci;66(9):939-950, 2017.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Liquid crystal (LC)-forming lipids represent an important class of biocompatible amphiphiles and their application extends to cosmeceutical, dietary, and pharmaceutical technologies. In the present study, we aimed to develop strategies for designing and optimizing oral and topical LC formulations by evaluating their in vitro and in vivo drug absorption performances. C -Monoglycerol ester (MGE) was used as a LC-forming lipid. p-Amino benzoic acid, methyl PABA, ethyl PABA, and sodium fluorescein were selected as drug models with different physiochemical properties. Various oral and topical LC formulations were designed based on changes in the LC forming lipid contents in the formulations and entrapped with different physiochemical properties of the drugs. The LC phase structures were evaluated using small-angle X-ray scattering (SAXS). The drug-release profiles from LC formulations were determined using a dialysis membrane method. In vivo oral absorption of LC formulations was conducted in Wistar rats. Furthermore, the skin penetration of drugs from LC formulations was investigated by in vitro skin permeation studies. As a result, although the release profile was influenced by changes in MGE concentration, it was more dramatically influenced by changes in the physiochemical properties of the entrapped drugs. Drug absorption after oral and topical administration of LC formulations was dramatically affected by the concentration of MGE. The concentration of LC-forming lipid and the physiochemical properties of entrapped drugs are key issues for good performance of the LC formulations in various pharmaceutical applications. The present results could enable researchers to manipulate LC formulation approaches intended to improve the oral absorption and skin permeation of drugs.
[Mh] Termos MeSH primário: Composição de Medicamentos
Cristais Líquidos
[Mh] Termos MeSH secundário: Administração Oral
Administração Tópica
Fenômenos Químicos
Desenho de Drogas
Absorção pela Mucosa Oral
Absorção Cutânea
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170905
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess17032


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[PMID]:28351211
[Au] Autor:Hayashi T; To M; Saruta J; Sato C; Yamamoto Y; Kondo Y; Shimizu T; Kamata Y; Tsukinoki K
[Ad] Endereço:a Division of Environmental Pathology, Department of Oral Science , Graduate School of Dentistry, Kanagawa Dental University , Yokosuka , Japan.
[Ti] Título:Salivary lactoferrin is transferred into the brain via the sublingual route.
[So] Source:Biosci Biotechnol Biochem;81(7):1300-1304, 2017 Jul.
[Is] ISSN:1347-6947
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Lactoferrin (LF) is produced by exocrine glands including salivary gland, and has various functions including infection defense. However, the transfer of LF from peripheral organs into the brain remains unclear. To clarify the kinetics of salivary LF (sLF), we investigated the consequences of sialoadenectomy and bovine LF (bLF) sublingual administration in rats. The salivary glands were removed from male Wistar rats, and we measured rat LF levels in the blood and brain at 1 week post-surgery. We also examined the transfer of LF into the organs of the rats after sublingual administration of bLF. Rat LF levels in the blood and brain were significantly reduced by sialoadenectomy. Sublingual bLF administration significantly increased bLF levels in the brain, which then decreased over time. These results indicate that LF is transferred from the sublingual mucosa to the brain, in which favorable effects of sLF on brain will be expected via the sublingual mucosa.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Lactoferrina/farmacocinética
Mucosa Bucal/metabolismo
Glândulas Salivares/metabolismo
[Mh] Termos MeSH secundário: Administração Sublingual
Animais
Transporte Biológico
Bovinos
Lactoferrina/sangue
Masculino
Absorção pela Mucosa Oral/fisiologia
Ratos
Ratos Wistar
Glândulas Salivares/cirurgia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
EC 3.4.21.- (Lactoferrin)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170707
[Lr] Data última revisão:
170707
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170330
[St] Status:MEDLINE
[do] DOI:10.1080/09168451.2017.1308241


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[PMID]:27671542
[Au] Autor:Senta-Loys Z; Bourgeois S; Pailler-Mattei C; Agusti G; Briançon S; Fessi H
[Ad] Endereço:Université de Lyon, Université Lyon 1, Laboratoire d'Automatique et de Génie des Procédés (LAGEP), UMR CNRS 5007, Villeurbanne, France.
[Ti] Título:Formulation of orodispersible films for paediatric therapy: investigation of feasibility and stability for tetrabenazine as drug model.
[So] Source:J Pharm Pharmacol;69(5):582-592, 2017 May.
[Is] ISSN:2042-7158
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: Orodispersible films (ODF) were formulated to facilitate tetrabenazine (TBZ) administration to paediatric population for the treatment of hyperkinetic movement disorders. METHODS: ODF were obtained by solvent casting/evaporation method using four different polymers (HPMC, PVP, pullulan and HEC). Physicochemical, mechanical and biopharmaceutical characterizations as well as API state in ODF by thermal analysis were investigated to define and compare formulations. ODF stability was also monitored during 6 months to follow evolution of properties. KEY FINDINGS: Analyses at T0 showed few differences between formulations: results of physicochemical and mechanical characterizations were almost similar for each formulation and TBZ appeared at the amorphous state in all cases. ODF delivery system allowed a major improvement of TBZ dissolution profile in buccal conditions compared with pure drug. However, after 3 and 6 months of stability, a TBZ recrystallization occurred for formulations based on PVP and HEC associated with a decrease of drug release in saliva conditions. CONCLUSIONS: HPMC-ODF (F1) appeared as the best formulation. Indeed, physicochemical, mechanical and biopharmaceutical characteristic remained intact. In addition, TBZ remained in amorphous state during stability study.
[Mh] Termos MeSH primário: Tetrabenazina/química
[Mh] Termos MeSH secundário: Administração Bucal
Administração Oral
Química Farmacêutica/métodos
Liberação Controlada de Fármacos/efeitos dos fármacos
Estabilidade de Medicamentos
Seres Humanos
Hipercinese/tratamento farmacológico
Absorção pela Mucosa Oral
Polímeros/química
Saliva/metabolismo
Solubilidade
Solventes/química
Tetrabenazina/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Polymers); 0 (Solvents); Z9O08YRN8O (Tetrabenazine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170714
[Lr] Data última revisão:
170714
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160928
[St] Status:MEDLINE
[do] DOI:10.1111/jphp.12627


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[PMID]:27655276
[Au] Autor:Heard A; Toner AJ; Evans JR; Aranda Palacios AM; Lauer S
[Ad] Endereço:From the *Department of Anaesthesia and Pain Medicine, Royal Perth Hospital, Perth, Australia; †Department of Anaesthesia, Fremantle Hospital, Perth, Australia; and ‡Department of Anesthesiology, Intensive Care and Pain Medicine, University Hospital Muenster, Germany.
[Ti] Título:Apneic Oxygenation During Prolonged Laryngoscopy in Obese Patients: A Randomized, Controlled Trial of Buccal RAE Tube Oxygen Administration.
[So] Source:Anesth Analg;124(4):1162-1167, 2017 Apr.
[Is] ISSN:1526-7598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Despite optimal preoxygenation, obese patients undergoing induction of general anesthesia exhibit significant hypoxemia after 2 to 4 minutes of apnea. Apneic oxygenation techniques can assist airway management by extending the safe apnea time. We hypothesized that a novel method of apneic oxygenation via the oral route would effectively prolong safe apnea in an obese surgical population. METHODS: In this open-label, parallel-arm, randomized-controlled efficacy trial, 40 ASA physical status I-II obese patients with body mass index (BMI) 30-40 were randomly assigned to standard care (n = 20) or buccal oxygenation (n = 20) during induction of total IV anesthesia. Buccal oxygen was administered via a modified 3.5-mm Ring-Adair-Elwyn (RAE) tube apposed to the left internal cheek. Prolonged laryngoscopy maintained apnea with a patent airway until SpO2 dropped below 95% or 750 seconds elapsed. The primary outcome was time to reach SpO2 < 95%. RESULTS: Patient characteristics were similar in both study arms. Recipients of buccal oxygenation were less likely to exhibit SpO2 < 95% during 750 seconds of apnea; hazard ratio 0.159 (95% confidence interval 0.044-0.226, P < .0001). Median (interquartile range [IQR]) apnea times with SpO2 ≥ 95% were prolonged in this group; 750 (389-750) versus 296 (244-314) seconds, P < .0001. CONCLUSIONS: Clinically important prolongation of safe apnea times can be achieved delivering buccal oxygen to obese patients on induction of anesthesia. This novel use of apneic oxygenation via the oral route may improve management of the difficult airway and overcome some of the limitations of alternative techniques.
[Mh] Termos MeSH primário: Manuseio das Vias Aéreas/métodos
Apneia/terapia
Laringoscopia/métodos
Obesidade/terapia
Absorção pela Mucosa Oral
Oxigenoterapia/métodos
[Mh] Termos MeSH secundário: Administração Bucal
Adulto
Idoso
Idoso de 80 Anos ou mais
Manuseio das Vias Aéreas/instrumentação
Apneia/epidemiologia
Feminino
Seres Humanos
Laringoscopia/efeitos adversos
Laringoscopia/instrumentação
Masculino
Meia-Idade
Obesidade/epidemiologia
Absorção pela Mucosa Oral/fisiologia
Oxigenoterapia/instrumentação
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170713
[Lr] Data última revisão:
170713
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160923
[St] Status:MEDLINE
[do] DOI:10.1213/ANE.0000000000001564


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[PMID]:27430990
[Au] Autor:Mogensen S; Sverrisdóttir E; Sveinsdóttir K; Treldal C; Jensen K; Jensen AB; Kristensen CA; Jacobsen J; Kreilgaard M; Petersen J; Andersen O
[Ad] Endereço:Clinical Research Centre, Copenhagen University Hospital, Hvidovre, Denmark.
[Ti] Título:Absorption of Bupivacaine after Administration of a Lozenge as Topical Treatment for Pain from Oral Mucositis.
[So] Source:Basic Clin Pharmacol Toxicol;120(1):71-78, 2017 Jan.
[Is] ISSN:1742-7843
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The aim was to investigate systemic exposure after administration of a novel bupivacaine lozenge in healthy individuals with normal mucosa and in head and neck cancer (HNC) patients with oral mucositis. A lozenge containing 5, 10, 25 and 50 mg bupivacaine, respectively, was administered as single dose to 10 healthy individuals, and a lozenge containing 25 mg bupivacaine was administered as single dose to 10 HNC patients with oral mucositis and as multiple doses to five patients with HNC. Blood samples were collected for 6 hr from the healthy individuals and 3 hr from the patients with HNC, respectively, after administration. The plasma concentration-time profiles of bupivacaine were fitted to pharmacokinetic models using nonlinear mixed-effects modelling, evaluating demographics and health status as covariates. The population pharmacokinetics (PK) of bupivacaine lozenge was best described by a two-compartment distribution model with absorption transit compartments. All the observed plasma concentrations were well below the bupivacaine concentrations (2000-2250 ng/ml) which have caused toxic symptoms. The PK model suggested that relative bioavailability was two times higher in HNC patients with oral mucositis grade 1-2 and three times higher in HNC patients with oral mucositis grade 3-4 than in the healthy individuals. Simulations showed that the plasma concentrations would be below the toxic limit after repeated dosing every second hour with 25 mg bupivacaine for five days. The 25-mg bupivacaine lozenges were safe without systemic toxic levels of bupivacaine or risk of side effects. Based on PK simulations of repeated doses of 25 mg every two hours for 16 hr a day, the lozenges can be administered with minimum risk of exceeding the toxic limit.
[Mh] Termos MeSH primário: Anestésicos Locais/farmacocinética
Bupivacaína/farmacocinética
Modelos Biológicos
Mucosa Bucal/efeitos dos fármacos
Mucosite/tratamento farmacológico
Absorção pela Mucosa Oral
Dor/prevenção & controle
[Mh] Termos MeSH secundário: Administração através da Mucosa
Adulto
Anestésicos Locais/administração & dosagem
Anestésicos Locais/efeitos adversos
Anestésicos Locais/uso terapêutico
Disponibilidade Biológica
Bupivacaína/administração & dosagem
Bupivacaína/efeitos adversos
Bupivacaína/uso terapêutico
Relação Dose-Resposta a Droga
Esquema de Medicação
Feminino
Neoplasias de Cabeça e Pescoço/radioterapia
Seres Humanos
Absorção Intestinal
Masculino
Taxa de Depuração Metabólica
Mucosa Bucal/metabolismo
Mucosa Bucal/efeitos da radiação
Mucosite/sangue
Mucosite/metabolismo
Mucosite/fisiopatologia
Dor/etiologia
Lesões por Radiação/tratamento farmacológico
Lesões por Radiação/metabolismo
Lesões por Radiação/fisiopatologia
Índice de Gravidade de Doença
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE I; CLINICAL TRIAL, PHASE II; COMPARATIVE STUDY; CONTROLLED CLINICAL TRIAL; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anesthetics, Local); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170208
[Lr] Data última revisão:
170208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160720
[St] Status:MEDLINE
[do] DOI:10.1111/bcpt.12644


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[PMID]:27291554
[Au] Autor:Walicová V; Gajdziok J; Pavloková S; Vetchý D
[Ad] Endereço:a Department of Pharmaceutics, Faculty of Pharmacy , University of Veterinary and Pharmaceutical Sciences , Brno , Czech Republic.
[Ti] Título:Design and evaluation of mucoadhesive oral films containing sodium hyaluronate using multivariate data analysis.
[So] Source:Pharm Dev Technol;22(2):229-236, 2017 Mar.
[Is] ISSN:1097-9867
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Mucoadhesive oral films, with their prolonged residence time at the site of application, offer a promising approach for protection of the oral lesion surface. The addition of sodium hyaluronate of different molecular weights as a second mucoadhesive polymer into the film matrix could positively influence the physico-mechanical and mucoadhesive properties of films. OBJECTIVE: The aim of this study was to investigate the formulation of a monolayered film matrix containing varying amounts of sodium hyaluronate and to test the properties of such matrices by applying different characterization methods. MATERIALS AND METHODS: Film matrix was composed of two mucoadhesive polymers, carmellose sodium and sodium hyaluronate, plasticized with glycerol. Resulting films were characterized with regard to their viscosity and physico-mechanical properties. RESULTS AND DISCUSSION: Multivariate data analysis was employed to evaluate the influence of varying amounts of mucoadhesive polymers on the main mucoadhesive oral films' properties. The lower content of sodium hyaluronate caused improvements in mechanical properties and residence time on the artificial oral mucosa, both of which are the main characteristics that determine the quality of the final product. CONCLUSIONS: The best results were obtained by samples containing carmellose sodium with a small amount of sodium hyaluronate (about 0.5% in casting dispersion).
[Mh] Termos MeSH primário: Adesivos/química
Carboximetilcelulose Sódica/química
Sistemas de Liberação de Medicamentos/métodos
Ácido Hialurônico/química
[Mh] Termos MeSH secundário: Adesividade
Adesivos/metabolismo
Carboximetilcelulose Sódica/metabolismo
Liberação Controlada de Fármacos
Glicerol/química
Glicerol/metabolismo
Seres Humanos
Ácido Hialurônico/metabolismo
Mucosa Bucal/metabolismo
Análise Multivariada
Absorção pela Mucosa Oral
Plastificantes/química
Plastificantes/metabolismo
Polímeros
Resistência à Tração
Viscosidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adhesives); 0 (Plasticizers); 0 (Polymers); 9004-61-9 (Hyaluronic Acid); K679OBS311 (Carboxymethylcellulose Sodium); PDC6A3C0OX (Glycerol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170315
[Lr] Data última revisão:
170315
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160614
[St] Status:MEDLINE
[do] DOI:10.1080/10837450.2016.1194857


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[PMID]:27280934
[Au] Autor:Jaisamut P; Wiwattanawongsa K; Wiwattanapatapee R
[Ad] Endereço:Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla, Thailand.
[Ti] Título:A Novel Self-Microemulsifying System for the Simultaneous Delivery and Enhanced Oral Absorption of Curcumin and Resveratrol.
[So] Source:Planta Med;83(5):461-467, 2017 Mar.
[Is] ISSN:1439-0221
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The use of curcumin and resveratrol in combination has now become increasingly of interest because of their synergistic effects as therapeutic agents for various diseases, especially cancer. To overcome the poor oral bioavailability of both compounds and improve patient compliance, a novel self-microemulsifying formulation containing curcumin together with resveratrol was developed. Capryol 90, Cremophor EL, and Labrasol were selected as the oil, surfactant, and co-surfactant in the formulation, respectively, based on the solubility study of both compounds. More than 70 % and 80 % of curcumin and resveratrol, respectively, were released in 20 min. The formulation formed a fine oil in water microemulsion with droplet sizes in aqueous media of 15-20 nm. In addition, the formulation containing curcumin and resveratrol showed greater antioxidant activity than that of the formulations with individual compounds, while the cytotoxic activity against HT-29 of the co-formulation (IC = 18.25 µM; curcumin and resveratrol in the ratio 1 : 1) was less than the formulation with only curcumin (IC = 30.1 µM) and only resveratrol (IC = 25.4 µM). After oral administration to rabbits, the self-microemulsifying formulation containing curcumin together with resveratrol increased the total plasma concentrations of curcumin and resveratrol by 10-fold and 6-fold, respectively, compared to the unformulated combination. This study clearly demonstrated the potential use of the self-microemulsifying formulation for co-delivery, and enhanced oral absorption of poorly water-soluble natural compounds. In addition, the combination was found to produce synergistic antioxidant activity and cytotoxicity against HT-29 cells.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/administração & dosagem
Antioxidantes/administração & dosagem
Curcumina/administração & dosagem
Estilbenos/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oral
Animais
Antineoplásicos Fitogênicos/farmacologia
Antioxidantes/farmacologia
Cápsulas
Curcumina/farmacologia
Sistemas de Liberação de Medicamentos
Emulsões
Células HT29
Seres Humanos
Absorção pela Mucosa Oral
Veículos Farmacêuticos
Coelhos
Solubilidade
Estilbenos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 0 (Antioxidants); 0 (Capsules); 0 (Emulsions); 0 (Pharmaceutical Vehicles); 0 (Stilbenes); IT942ZTH98 (Curcumin); Q369O8926L (resveratrol)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170406
[Lr] Data última revisão:
170406
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160610
[St] Status:MEDLINE
[do] DOI:10.1055/s-0042-108734


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[PMID]:27723791
[Au] Autor:Yang X; Duan J; Fisher J
[Ad] Endereço:National Center for Toxicological Research, Food and Drug Administration, Jefferson, Arkansas, United States of America.
[Ti] Título:Application of Physiologically Based Absorption Modeling to Characterize the Pharmacokinetic Profiles of Oral Extended Release Methylphenidate Products in Adults.
[So] Source:PLoS One;11(10):e0164641, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A previously presented physiologically-based pharmacokinetic model for immediate release (IR) methylphenidate (MPH) was extended to characterize the pharmacokinetic behaviors of oral extended release (ER) MPH formulations in adults for the first time. Information on the anatomy and physiology of the gastrointestinal (GI) tract, together with the biopharmaceutical properties of MPH, was integrated into the original model, with model parameters representing hepatic metabolism and intestinal non-specific loss recalibrated against in vitro and in vivo kinetic data sets with IR MPH. A Weibull function was implemented to describe the dissolution of different ER formulations. A variety of mathematical functions can be utilized to account for the engineered release/dissolution technologies to achieve better model performance. The physiological absorption model tracked well the plasma concentration profiles in adults receiving a multilayer-release MPH formulation or Metadate CD, while some degree of discrepancy was observed between predicted and observed plasma concentration profiles for Ritalin LA and Medikinet Retard. A local sensitivity analysis demonstrated that model parameters associated with the GI tract significantly influenced model predicted plasma MPH concentrations, albeit to varying degrees, suggesting the importance of better understanding the GI tract physiology, along with the intestinal non-specific loss of MPH. The model provides a quantitative tool to predict the biphasic plasma time course data for ER MPH, helping elucidate factors responsible for the diverse plasma MPH concentration profiles following oral dosing of different ER formulations.
[Mh] Termos MeSH primário: Metilfenidato
Modelos Biológicos
Absorção pela Mucosa Oral
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Preparações de Ação Retardada/administração & dosagem
Preparações de Ação Retardada/farmacocinética
Seres Humanos
Masculino
Metilfenidato/administração & dosagem
Metilfenidato/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Delayed-Action Preparations); 207ZZ9QZ49 (Methylphenidate)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170428
[Lr] Data última revisão:
170428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161011
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0164641


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[PMID]:27697631
[Au] Autor:Meng-Lund E; Jacobsen J; Müllertz A; Jørgensen EB; Holm R
[Ad] Endereço:Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
[Ti] Título:Buccal absorption of diazepam is improved when administered in bioadhesive tablets-An in vivo study in conscious Göttingen mini-pigs.
[So] Source:Int J Pharm;515(1-2):125-131, 2016 Dec 30.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Buccal delivery may be clinically beneficial for compounds with a high gastrointestinal and hepatic first pass metabolism or in situations where a fast systemic absorption is desired. The delivery of a crystalline low soluble compounds, e.g. diazepam, may be limited due to the low volume of saliva available to facilitate solvation in order to drive the permeation of drug through the buccal mucosa. Therefore, the present study investigated the potential benefits of administering diazepam either as an amorphous or as a crystalline form in mucoadhesive tablets to conscious Göttingen mini-pigs. Presentation of the compound in the amorphous form lead to a very fast absorption, however, the obtained bioavailability was at the same level observed following buccal administration of a commercially immediate release tablet. Addition of chitosan, as a mucoadhesive excipient, resulted in a higher absolute bioavailability compared to tablets without chitosan. The absorption rate for the chitosan-based tablets was significant slower, probably due to the slower diffusion of the compound out of the tablet. In vitro release data was able to predict the variations in t , but otherwise no correlation could be found between in vitro and in vivo data.
[Mh] Termos MeSH primário: Adesivos/administração & dosagem
Adesivos/metabolismo
Diazepam/administração & dosagem
Diazepam/metabolismo
Mucosa Bucal/metabolismo
Comprimidos/administração & dosagem
Comprimidos/metabolismo
[Mh] Termos MeSH secundário: Adesividade/efeitos dos fármacos
Administração Bucal
Animais
Disponibilidade Biológica
Química Farmacêutica/métodos
Quitosana/química
Difusão
Excipientes/química
Concentração de Íons de Hidrogênio
Masculino
Absorção pela Mucosa Oral
Suínos
Porco Miniatura
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adhesives); 0 (Excipients); 0 (Tablets); 9012-76-4 (Chitosan); Q3JTX2Q7TU (Diazepam)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170828
[Lr] Data última revisão:
170828
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161106
[St] Status:MEDLINE


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[PMID]:27575434
[Au] Autor:Jain A; Thakur D; Ghoshal G; Katare OP; Singh B; Shivhare US
[Ad] Endereço:Dr. S. S. Bhatnagar University Institute of Chemical Engineering & Technology, Panjab University, Chandigarh, India; Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India; UGC-Centre of Excellence
[Ti] Título:Formation and functional attributes of electrostatic complexes involving casein and anionic polysaccharides: An approach to enhance oral absorption of lycopene in rats in vivo.
[So] Source:Int J Biol Macromol;93(Pt A):746-756, 2016 Dec.
[Is] ISSN:1879-0003
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The current work entails a novel strategy of formulating the microparticles of lycopene solely using rational blends of biopolymers without using equipment-intensive techniques. The study is intended to enhance oral bioavailability of lycopene by controlling its release from micro-formulation and facilitating its absorption though lymphatic pathways. Considering the minimum particle size, maximum entrapment efficiency and loading capacity, the amounts of casein (i.e., protein) and gum tragacanth (i.e., polysaccharide) were selected as the critical factors for formulation of microparticles. Complex formation and electrostatic interaction was confirmed by Fourier transform infra red (FTIR) spectra. Size and surface properties of microparticles were studied using scanning electron microscopy (SEM). The optimized formulation (mean particle size: ∼130µm; % entrapment efficiency: ∼67% and loading capacity: ∼71%) designated noticeable improvement in lycopene release profile (over 80% in 24h). Increment in the values of C (2.22-fold) and AUC (1.97-fold) further indicated noteworthy augmentation in the rate and extent of bioavailability by the microparticles formulation compared to plain lycopene. The resulting formulation was found to be quite stable all through two months of study episode. The resultant microparticles formulation was evaluated for antioxidant activity and tested for their effectiveness in self life enhancement of vegetable oil by calculating peroxide value under temperature and storage condition. Encapsulation strongly increased the stability of micronutrients. The current investigations, therefore, report the successful development of biopolymeric microparticles with improved bioavailability potential of lycopene.
[Mh] Termos MeSH primário: Portadores de Fármacos
Absorção pela Mucosa Oral
Polissacarídeos
[Mh] Termos MeSH secundário: Animais
Carotenoides/química
Carotenoides/farmacocinética
Carotenoides/farmacologia
Caseínas/química
Caseínas/farmacocinética
Caseínas/farmacologia
Portadores de Fármacos/química
Portadores de Fármacos/farmacocinética
Portadores de Fármacos/farmacologia
Masculino
Polissacarídeos/química
Polissacarídeos/farmacocinética
Polissacarídeos/farmacologia
Ratos
Ratos Wistar
Eletricidade Estática
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Caseins); 0 (Drug Carriers); 0 (Polysaccharides); 36-88-4 (Carotenoids); SB0N2N0WV6 (lycopene)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170317
[Lr] Data última revisão:
170317
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160831
[St] Status:MEDLINE



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