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1.
Artigo em Inglês | MEDLINE | ID: mdl-32361467

RESUMO

Antibody-Drug Conjugates (ADCs) consist of antibodies attached to cytotoxic small molecules or biological agents (i.e., payloads) through chemical linkers which may be cleavable or non-cleavable. The development of new ADCs is challenging, particularly the process of attaching the linker-payload construct to the antibody (i.e., the conjugation process). One of the major problems associated with conjugation is high hydrophobicity of the payload which can lead to low yields of the ADC through aggregation and/or lower than desired Drug-Antibody Ratios (DARs). We report here a UPLC-based assay that can be used to study the physicochemical properties of ADC payloads at an early stage of development, and to provide information on whether the hydrophilic-hydrophobic balance is suitable for conjugation or further physicochemical optimization is required. The assay is relatively simple to establish and should be of use to those working in the ADC area.


Assuntos
Bioensaio/métodos , Imunoconjugados/química , Espectrometria de Massas em Tandem/métodos , Calicheamicinas/química , Cromatografia Líquida de Alta Pressão , Doxorrubicina/química , Flurbiprofeno/química , Interações Hidrofóbicas e Hidrofílicas , Ibuprofeno/química , Irinotecano/química , Cetoprofeno/química , Maitansina/química , Conformação Molecular , Norfloxacino/química , Pentaclorofenol/química , Multimerização Proteica , Relação Estrutura-Atividade , Tolnaftato/química
2.
Spectrochim Acta A Mol Biomol Spectrosc ; 223: 117290, 2019 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-31284238

RESUMO

A comparative study using novel quadruple divisor and mean centering of ratio spectra spectrophotometric methods was developed for resolution of five- component mixture of Tolnaftate, ß-naphthol (Tolnaftate alkaline degradation product and its toxic impurity), methyl(m-tolyl)carbamic acid (Tolnaftate alkaline degradation product), N-methyl-m-toluidine (Tolnaftate toxic impurity) and methyl paraben (as a preservative). For the novel quadruple divisor method, each component in the quinary mixture was determined by dividing the quinary mixture spectrum by a sum of standard spectrum of equal concentration of the other four components as a quadruple divisor. First derivative of each ratio spectra was then obtained which allowed selective determination of each component without interference from other components in the mixture. The second method was mean centering of ratio spectra that depended on utilizing the mean centered ratio spectra in four successive steps leading to enhancement of the signal to noise ratio. The absorption spectra of the five studied components were recorded in the wavelength range of 210-350 nm. The mean centered fourth ratio spectra amplitudes for each component were used for its determination. The developed methods were successfully applied for determination of laboratory prepared quinary mixtures to ensure method's specificity, then, were further applied on Tinea Cure® cream where no interference from excipients. For the first time, Tolnaftate was determined along with its toxic impurity; ß-naphthol, that could be absorbed by the skin, causing systemic toxic effects, unlike Tolnaftate that poorly absorbed, indicating the significance of this work. The proposed methods were statistically compared with each other and with the reference method. Furthermore, ICH guidelines were followed for their validation.


Assuntos
Análise Espectral , Tolnaftato/química , Tolnaftato/toxicidade , Limite de Detecção , Espectroscopia de Prótons por Ressonância Magnética , Análise de Regressão , Espectrofotometria Infravermelho , Toluidinas/química
3.
Int J Health Policy Manag ; 7(10): 961-963, 2018 10 01.
Artigo em Inglês | MEDLINE | ID: mdl-30316250

RESUMO

CHAT has its limits. It is a three-hour exercise. However, the real world problems of healthcare rationing and priority-setting are too complex for a three-hour exercise. What is needed, as a supplement, are sustained processes of rational democratic deliberation that can address the challenges to healthcare justice posed by costly emerging medical technologies, such as these targeted cancer therapies.


Assuntos
Alocação de Recursos para a Atenção à Saúde , Tolnaftato , Suplementos Nutricionais , Humanos , Cobertura do Seguro , Justiça Social
6.
J Liposome Res ; 27(4): 324-334, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27666873

RESUMO

Tolnaftate is a thiocarbamate antifungal drug which is therapeutically active against dermatophytes that cause various forms of tinea. Due to the small amount of tolnaftate released from ordinary ointment bases and insufficient penetration through the infected skin layers the need to incorporate the drug in a more suitable pharmaceutical form has evolved. A provesicular system is one such form that can solve these problems. Once in contact with the skin, dilution with moisture occurs and the provesicular system rapidly transforms into a vesicular one. Provesicular systems were prepared according to full-factorial experimental design. Plain provesicular systems were compared with systems containing Phospholipon 80 H and Lipoid S45 as penetration enhancers. Design expert software was used to analyze the effect of formulation variables (type of Span used as well as the presence or the absence of the penetration enhancer and its type) on the dependent variables: percent encapsulation efficiency (EE%), vesicle size and percent in vitro drug released). Three formulations were chosen; a plain provesicular system (PV-2), one containing Phospholipon 80H (PV-6) and another containing Lipoid S45 (PV-10) with the goal to reveal the effect of penetration enhancer on morphology, rheological properties and ex vivo permeation using confocal laser scanning microscopy (CLSM). Analysis of CLSM results showed that the penetration enhancing effect for the tested formulations followed the order PV-10 > PV-6 > PV-2. Promising clinically active treatment for tinea patients could be expected as shown by the in vivo permeation results for the provesicular systems as suggested by the CLSM results.


Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Lipossomos/química , Tinha dos Pés/tratamento farmacológico , Tolnaftato/química , Tolnaftato/farmacologia , Administração Cutânea , Animais , Antifúngicos/administração & dosagem , Química Farmacêutica/métodos , Liberação Controlada de Fármacos , Géis , Humanos , Microscopia Confocal/instrumentação , Imagem Óptica/métodos , Tamanho da Partícula , Permeabilidade , Ratos , Reologia/métodos , Pele/metabolismo , Absorção Cutânea/fisiologia , Propriedades de Superfície , Tolnaftato/administração & dosagem
7.
J AOAC Int ; 99(2): 380-5, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26964843

RESUMO

A highly selective, sensitive, accurate, and reproducible luminescence procedure for determination of antifungal drug tolnaftate was developed. The introduced method was based on the formation of Europa Universalis III (Eu(III))-tolnaftate complex using sodium sulfite as a deoxygenated agent in the presence of acetate buffer (pH = 6) and micellar solution of anionic surfactant sodium dodecyl sulfate. The optimum conditions (effect of pH, buffer, surfactant, Eu(III), and sodium sulfite concentrations) for the luminescence signal were investigated and optimized. The luminescence signals were recorded at λex = 270 nm and λem = 460 nm. The method has a good linear response (0.2-130 µg/mL(-1)) between the luminescence intensity and the concentrations of the drug (r = 0.999), with a LOD 0.07 µg/mL(-1) and LOQ 0.2 µg/mL(-1). The luminescence signals of Eu (III)-tolnaftate-sodium dodecyl sulfate were found to be 200-fold more sensitive without the presence of micelle solution. The interferences of some additives, metals, amino acids, sugars, and other related pharmacological action drugs were examined and no interference was recorded. The proposed method was used for quick and simple determination of tolnaftate in its pharmaceuticals and biological fluids.


Assuntos
Líquidos Corporais/química , Európio/química , Substâncias Luminescentes/química , Preparações Farmacêuticas/química , Tolnaftato/análise , Humanos , Luminescência , Medições Luminescentes
8.
9.
10.
Phytopathology ; 104(4): 396-402, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24156554

RESUMO

Gray mold, caused by the fungal pathogen Botrytis cinerea, is one of the most destructive diseases of strawberry. Control of the disease in commercial fields is largely dependent on the application of fungicides, including the dicarboximide iprodione. Single-spore isolates were collected from strawberry fields in Florida, North Carolina, and South Carolina and subjected to an assay using conidial germination that distinguished sensitive (S) isolates from isolates with various levels of resistance to iprodione. Of the 245 isolates, 1 was highly resistant (HR), 5 were moderately resistant (MR), and 43 had low resistance (LR) to iprodione. LR and MR strains were found in the Florida population and in 9 of 11 locations from North Carolina and South Carolina, indicating that resistance was widespread but accounted for only a relatively small percentage of the B. cinerea population. Sequence analysis of the target gene bos1, which codes for a class III histidine kinase, revealed that the MR phenotype was associated with Q369P and N373S mutations and that the LR phenotype was associated with either a I365S or a I365N mutation. The I365S and I365N mutations were also present in five additionally included HR isolates from North Carolina and South Carolina blackberry fields and one HR isolate from a Virginia strawberry field but no mutation or mutation combinations in bos1 were uniquely associated with the HR phenotype. Expression analysis of bos1 in S and HR isolates did not reveal convincing evidence of the gene's involvement in HR resistance either. The six HR isolates had three different phenotypes with respect to their sensitivity to fludioxonil; two were S, two were LR, and two were MR. The fludioxonil LR and MR isolates were also resistant to tolnaftate, an indication of multidrug efflux pump activity. These data suggest that, in addition to point mutations in bos1, drug efflux pump activity and potentially a third mechanism of resistance may be contributing to the iprodione HR phenotype. Detached fruit studies showed that field rates of Rovral 4 Flowable (iprodione) did not control iprodione MR and HR isolates.


Assuntos
Aminoimidazol Carboxamida/análogos & derivados , Botrytis/genética , Farmacorresistência Fúngica/genética , Fragaria/microbiologia , Hidantoínas/farmacologia , Doenças das Plantas/microbiologia , Rosaceae/microbiologia , Substituição de Aminoácidos , Aminoimidazol Carboxamida/farmacologia , Sequência de Bases , Botrytis/efeitos dos fármacos , Botrytis/fisiologia , Primers do DNA/genética , DNA Fúngico/química , DNA Fúngico/genética , Dioxóis/farmacologia , Florida , Frutas/microbiologia , Proteínas Fúngicas/genética , Fungicidas Industriais/farmacologia , Testes de Sensibilidade Microbiana , Mutação de Sentido Incorreto , Micélio , North Carolina , Pirróis/farmacologia , Tolnaftato/farmacologia , Virginia
11.
Comb Chem High Throughput Screen ; 16(8): 636-43, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23713459

RESUMO

Storage of pharmaceutical discovery compounds dissolved in dimethylsulfoxide (DMSO) is commonplace within industry. Often, the DMSO stock solution is added to an aqueous system (e.g. in bioassay or kinetic solubility testing)- since most test compounds are hydrophobic, precipitation could occur. Little is known about the factors affecting this precipitation process at the low (µM) concentrations used in screening analyses. Here, a poorly water soluble test compound (tolnaftate) was used to compare manual and automated pipetting, and explore the effect of mixing variables on precipitation. The amount of drug present in the supernatant after precipitation and centrifugation of the samples was quantified. An unusual result was obtained in three different laboratories: results of experiments performed initially were statistically significantly higher than those performed after a few days in the same lab. No significant differences were found between automated and manual pipetting, including in variability. Vortex mixing was found to give significantly lower supernatant amounts compared to milder mixing types. The mixing employed affects the particle growth of the precipitate. These findings are of relevance to discovery stage bioassay and kinetic solubility analyses.


Assuntos
Antifúngicos/química , Tolnaftato/química , Água/química , Precipitação Química , Dimetil Sulfóxido/química , Solubilidade
12.
Clin Otolaryngol ; 37(4): 261-70, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22804826

RESUMO

OBJECTIVE: Primary: to compare one-off administration of boric acid powder with courses of 1% acetic acid and ciprofloxacin eardrops in treating active chronic otitis media. Secondary: to evaluate the effectiveness of Quadriderm® cream in resistant active chronic otitis media; and to document side effects of these treatments, especially hearing loss. STUDY DESIGN: Randomised controlled trial. SETTING: Outpatient department of a tertiary ENT unit. PARTICIPANTS: Hundred and fifty-nine patients over 6 years old with active chronic mucosal (without cholesteatoma) otitis media randomised to receive one of the three primary agents. METHOD: All techniques employed were suitable for primary healthcare givers as well as specialists. After confirming eligibility, patients were randomly allocated to treatment. All ears underwent toilet with irrigation using clean water, a syringe and ambient light, with or without dry mopping, until the perforation was visible. The randomised solution was flushed through the middle ear and eustachian tube using a 'tragal pump' technique: saline was used as the solution for flushing in the boric acid powder arm. Patients allocated topical ear medication were given a bottle of eardrops to administer (six drops twice daily, 'pumped in') until finished. Those allocated boric acid powder had the external ear canals filled as a one-off treatment. Patients were followed up monthly thereafter. OUTCOME MEASURES: Primary: Dry (inactive) middle ears as assessed by the doctor. Secondary: Patient assessment of success; microbiologic culture and sensitivity; audiologic changes because of treatment; complications of treatment; costs of therapies. RESULTS: Ciprofloxacin eardrops and boric acid powder were statistically superior to 1% acetic acid eardrops in rendering active chronic otitis media inactive (73% dry ears for ciprofloxacin; 67% for boric acid powder; and 24% for acetic acid). There was no difference between the success rates of ciprofloxacin eardrops and boric acid powder. Quadriderm cream was effective in 85% of patients failing first-line therapy. No agent caused significant complications and specifically no hearing loss. CONCLUSIONS: This study showed a single application of boric acid powder following external auditory canal irrigation until the perforation was visible to be as effective as the current best practice of topical quinolone eardrops in active chronic otitis media. Boric acid powder is inexpensive and does not require patient compliance. Boric acid powder is a viable, less costly alternative to topical antibiotic/steroid ear drops in the developing world for active chronic otitis media. Acetic acid eardrops 1% are ineffective. Quadriderm cream, given as a one-off therapy, also appears to be effective.


Assuntos
Ácido Acético/administração & dosagem , Ácidos Bóricos/administração & dosagem , Ciprofloxacino/administração & dosagem , Otite Média/tratamento farmacológico , Administração Tópica , Adulto , Análise de Variância , Anti-Infecciosos/administração & dosagem , Audiometria , Valerato de Betametasona , Distribuição de Qui-Quadrado , Doença Crônica , Clioquinol , Farmacorresistência Bacteriana , Feminino , Gentamicinas , Perda Auditiva/epidemiologia , Humanos , Masculino , Otite Média/microbiologia , Estudos Prospectivos , Tolnaftato , Resultado do Tratamento
13.
Acta Pol Pharm ; 68(6): 965-73, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-22125963

RESUMO

Five fatty acids (oleic, linoleic, myristic, lauric and capric) were incorporated in 10% (w/w) into ointment formulation and their influence on lipophilic model drug tolnaftate release in vitro and enhancing effect on tolnaftate penetration into epidermis and dermis of human skin ex vivo were investigated. The prepared ointments were tested for homogeneity, pH and theological properties. In vitro release studies and ex vivo skin penetration experiments were carried out using Hanson and Bronaugh-type flow-through diffusion cells, respectively. Tolnaftate cumulative amount liberated from semisolids was assayed using UV-Vis spectrophotometer. After in vitro skin penetration studies, appropriately extracted human skin layers were analyzed for tolnaftate content using a validated HPLC method. Statistical analysis revealed that release rate of tolnaftate from control ointment and ointments with fatty acids was not significantly different and only 7.34-8.98% of drug was liberated into an acceptor medium after 6 h. Tolnaftate amount penetrating into 1 cm2 of epidermis from ointments containing oleic, linoleic, myristic and lauric acids was significantly greater (p < 0.05) than from the control ointment. Penetration enhancing ratios for these fatty acids for tolnaftate penetration into epidermis ranged from 1.48 to 1.75. In conclusion, fatty acids did not increase the liberation of tolnaftate from ointment formulation, but demonstrated their enhancing effect on tolnaftate penetration into human epidermis in vitro. Results from in vitro release experiments do not suit for prediction of the situation in the skin in vitro, if chemical penetration enhancers are incorporated into the ointment formulation.


Assuntos
Antifúngicos/metabolismo , Ácidos Graxos/farmacologia , Absorção Cutânea/efeitos dos fármacos , Pele/efeitos dos fármacos , Tolnaftato/metabolismo , Administração Cutânea , Adulto , Antifúngicos/administração & dosagem , Antifúngicos/química , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Ácidos Decanoicos/farmacologia , Composição de Medicamentos , Ácidos Graxos/administração & dosagem , Ácidos Graxos/química , Feminino , Humanos , Concentração de Íons de Hidrogênio , Cinética , Ácidos Láuricos/farmacologia , Ácido Linoleico/farmacologia , Pessoa de Meia-Idade , Ácido Mirístico/farmacologia , Pomadas , Ácido Oleico/farmacologia , Permeabilidade , Reologia , Pele/metabolismo , Solubilidade , Espectrofotometria Ultravioleta , Tecnologia Farmacêutica/métodos , Tolnaftato/administração & dosagem , Tolnaftato/química
14.
Spectrochim Acta A Mol Biomol Spectrosc ; 79(5): 993-1003, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21565546

RESUMO

Vibrational analysis of the thionocarbamate fungicide tolnaftate which is antidermatophytic, antitrichophytic and antimycotic agent, primarily inhibits the ergosterol biosynthesis in the fungus, was carried out using NIR FT-Raman and FTIR spectroscopic techniques. The equilibrium geometry, various bonding features, harmonic vibrational wavenumbers and torsional potential energy surface (PES) scan studies have been computed using density functional theory method. The detailed interpretation of the vibrational spectra has been carried out with the aid of VEDA.4 program. Vibrational spectra, natural bonding orbital (NBO) analysis and optimized molecular structure show the clear evidence for electronic interaction of thionocarbamate group with aromatic ring. Predicted electronic absorption spectrum from TD-DFT calculation has been compared with the UV-vis spectrum. The Mulliken population analysis on atomic charges and the HOMO-LUMO energy were also calculated. Vibrational analysis reveals that the simultaneous IR and Raman activation of the C-C stretching mode in the phenyl and naphthalene ring provide evidence for the charge transfer interaction between the donor and acceptor groups and is responsible for its bioactivity as a fungicide.


Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Fungos/efeitos dos fármacos , Modelos Químicos , Espectroscopia de Infravermelho com Transformada de Fourier , Tolnaftato/química , Tolnaftato/farmacologia , Conformação Molecular , Estrutura Molecular , Teoria Quântica , Análise Espectral Raman , Vibração
15.
Acta Pol Pharm ; 67(4): 327-34, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-20635527

RESUMO

Abstract: Tolnaftate, an antifungal of thiocarbamate class, is used topically in 1% formulations. Its penetration into skin layers is a prerequisite for tolnaftate action against dermatophytes. The aim of this work was to optimize and validate a simple, rapid, accurate and reproducible procedure for tolnaftate assay in human skin samples and to apply this procedure for in vitro tolnaftate penetration studies. High performance liquid chromatography (HPLC) method with UV detection was used to validate tolnaftate assay for linearity, specificity, accuracy, precision, limit of quantitation, limit of detection, drug extraction recovery and stability in skin extracts. In vitro tolnaftate penetration studies were carried out using flow-through diffusion cells, mounted with human skin. Epidermis and dermis, separated by heat-separation method, were extracted using ultrasonication in methanol. Linear range of the analytical procedure was within 0.6-100 pg/mL. The assay was specific, accurate (within-day and between-day recovery values were 98.2-104.2% and 98.7-101.4%, respectively) and precise (within-day and between-day imprecision was = 3.8%). Mean extraction recoveries of tolnaftate from epidermis and dermis were satisfactory and reaching 90%. In vitro skin penetration studies revealed that after application of 1% (w/w) tolnaftate solution in polyethylene glycol 400 for 24 hours, the mean amount of tolnaftate penetrating into the epidermis and dermis was 2.60 +/- 0.28 microg/cm2 and 0.92 +/- 0.12 microg/cm2, respectively. A validated reliable HPLC method could be recommended for biopharmaceutical evaluation of tolnaftate preparations and studies of pharmacokinetics in human skin after in vitro penetration studies.


Assuntos
Antifúngicos/análise , Antifúngicos/farmacocinética , Absorção Cutânea/fisiologia , Pele/química , Tolnaftato/análise , Tolnaftato/farmacocinética , Adulto , Calibragem , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Derme/metabolismo , Epiderme/metabolismo , Feminino , Humanos , Técnicas In Vitro , Indicadores e Reagentes , Unhas/metabolismo , Controle de Qualidade , Padrões de Referência , Reprodutibilidade dos Testes , Pele/metabolismo
16.
Toxicol In Vitro ; 24(5): 1404-9, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20434536

RESUMO

In animal models, chemical disruption of the Hedgehog (Hh) signaling pathway during embryonic development causes severe birth defects including holoprosencephaly and cleft lip and palate. The exact etiological basis of correlate human birth defects remains uncertain but is likely multifactorial, involving the interaction of genetic and environmental or chemical influences. The Hh transduction mechanism relies upon endogenous small molecule regulation, conferring remarkable pathway sensitivity to inhibition by a structurally diverse set of exogenous small molecules. Here, we employed small molecule screening to identify human exposure-relevant Hh signaling inhibitors. From a library of 4240 compounds, including pharmaceuticals, natural products, and pesticides, three putative Hh pathway inhibitors were identified: tolnaftate, an antifungal agent; ipriflavone, a dietary supplement; and 17-beta-estradiol, a human hormone and pharmaceutical agent. Each compound inhibited Hh signaling in both mouse and human cells. Dose-response assays determined the three compounds to be 8- to 30-fold less potent than the index Hh pathway inhibitor cyclopamine. Despite current limitations in chemical library availability, which narrowed the scope of this study to only a small fraction of all human exposure-relevant small molecules, three structurally diverse environmental Hh signaling inhibitors were identified, highlighting an inherent pathway vulnerability to teratogenic influences.


Assuntos
Proteínas Hedgehog/antagonistas & inibidores , Transdução de Sinais/efeitos dos fármacos , Testes de Toxicidade/métodos , Animais , Antifúngicos/toxicidade , Células Cultivadas , Suplementos Nutricionais/toxicidade , Relação Dose-Resposta a Droga , Exposição Ambiental , Estradiol/toxicidade , Estrogênios/toxicidade , Humanos , Isoflavonas/toxicidade , Chumbo/toxicidade , Camundongos , Proteínas Oncogênicas/metabolismo , Receptores Patched , Receptores de Superfície Celular/metabolismo , Bibliotecas de Moléculas Pequenas , Tolnaftato/toxicidade , Transativadores/metabolismo , Proteína GLI1 em Dedos de Zinco
17.
Clin Dermatol ; 28(2): 212-6, 2010 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-20347665

RESUMO

There presently exists a wide selection of choices in the treatment of superficial mycoses. The main categories of broad-spectrum agents are the allylamines and imidazoles, which have been tried and proven over more than 2 decades of usage with good safety. Nystatin and griseofulvin have even longer experience of about 5 decades but have niche usage for yeasts and dermatophytes, respectively. Although no new therapeutic groups have appeared, extensive development of vehicles and delivery systems has enhanced therapeutic results and increased patient compliance.


Assuntos
Antibacterianos/uso terapêutico , Antifúngicos/uso terapêutico , Azóis/uso terapêutico , Dermatomicoses/tratamento farmacológico , Administração Oral , Administração Tópica , Antifúngicos/economia , Azóis/economia , Dermatomicoses/economia , Dermatomicoses/epidemiologia , Esquema de Medicação , Farmacorresistência Fúngica/efeitos dos fármacos , Fluconazol/uso terapêutico , Griseofulvina/uso terapêutico , Humanos , Itraconazol/uso terapêutico , Cetoconazol/uso terapêutico , Morfolinas/uso terapêutico , Tolnaftato/uso terapêutico , Estados Unidos/epidemiologia
18.
J Phys Chem B ; 110(17): 8877-84, 2006 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-16640448

RESUMO

Based on the fact that tolnaftate degrade to beta-naphthol sodium (RONa) at 5.00 mol/L NaOH solution and RO(-) was protonated to ROH after being acidified and adjusted to the pH 4.50 by acetic acid-sodium acetate buffer solution, we studied and discussed the mechanism of the supramolecular multirecognition interaction among the anionic surfactants sodium lauryl sulfate (SLS), beta-cyclodextrin (beta-CD), and beta-naphthol (ROH) by means of fluorescence spectrum, surface tension of the solution, infrared spectrograms, and (1)HNMR spectroscopy. The apparent formation constant of the ternary inclusion complex was determined to be (5.48 +/- 0.13) x 10(3) L(2)/mol(2). The thermodynamic parameters (DeltaG degrees, DeltaH degrees, DeltaS degrees ) for the formation of the inclusion complexes were obtained from the van't Hoff equation. It was indicated that the multiple and synergistic protection effect of SLS and beta-CD on the excited singlet state ROH played very important roles in the enhancement of the fluorescence of ROH. Results showed that, at room temperature, the naphthalene ring of ROH and the hydrophobic hydrocarbon chain of SLS were included into the cavity of beta-CD to form a ROH/SLS/beta-CD ternary inclusion complex with stoichiometry of 1:1:1, which provided effective protection for the excited state of ROH and increased the fluorescent intensity of ROH obviously.


Assuntos
Naftóis/química , Dodecilsulfato de Sódio/química , Tensoativos/química , Tolnaftato/química , beta-Ciclodextrinas/química , Ânions/química , Hidrólise , Substâncias Macromoleculares/química , Estrutura Molecular , Sensibilidade e Especificidade , Espectrometria de Fluorescência/métodos
19.
Zhonghua Yi Shi Za Zhi ; 36(4): 215-8, 2006 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-17533696

RESUMO

OBJECTIVE: In 1929, yi jing (pestilent convulsion) was prevalent in Shanghai, Yan Cangshan, a noted modern physician, was active in treating and rescuing the patients. Yi jingjia ting zi liao ji is a book of the summary on his clinical experience in the treatment of yi jing (pestilent convulsion). It is the first monograph on epidemic diseases carrying the title of yi jing (pestilent convulsion). There were many creative ideas about the name of disease, prescriptions, and medication, etc, embodying Yan's academic thought and achievements. It is of great reference value up to now.


Assuntos
Convulsões , Tolnaftato , Livros , China , Escolaridade , História Medieval , Humanos , Medicina Tradicional Chinesa , Médicos
20.
In. Ministerio de Salud Pública.Centro para el desarrollo de la Farmacoepidemiología. Formulario Nacional de Medicamentos. La Habana, Ecimed, 2006. .
Monografia em Espanhol | CUMED | ID: cum-44177
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