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[PMID]:26771454
[Au] Autor:Fang L; Yu J; Jiang Z; Guo X
[Ad] Endereço:Department of Pharmaceutical Analysis, School of Pharmacy, Shenyang Pharmaceutical University, Ministry of Education, Shenyang, Liaoning Province, P. R. China.
[Ti] Título:Preparation of a ß-Cyclodextrin-Based Open-Tubular Capillary Electrochromatography Column and Application for Enantioseparations of Ten Basic Drugs.
[So] Source:PLoS One;11(1):e0146292, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:An open-tubular capillary electrochromatography column was prepared by chemically immobilized ß-cyclodextrin modified gold nanoparticles onto new surface with the prederivatization of (3-mercaptopropyl)-trimethoxysilane. The synthesized nanoparticles and the prepared column were characterized by transmission electron microscopy, scanning electron microscopy, infrared spectroscopy and ultraviolet visible spectroscopy. When the column was employed as the chiral stationary phase, no enantioselectivity was observed for ten model basic drugs. So ß-cyclodextrin was added to the background electrolyte as chiral additive to expect a possible synergistic effect occurring and resulting in a better separation. Fortunately, significant improvement in enantioselectivity was obtained for ten pairs of drug enantiomers. Then, the effects of ß-cyclodextrin concentration and background electrolyte pH on the chiral separation were investigated. With the developed separation mode, all the enantiomers (except for venlafaxine) were baseline separated in resolutions of 4.49, 1.68, 1.88, 1.57, 2.52, 2.33, 3.24, 1.63 and 3.90 for zopiclone, chlorphenamine maleate, brompheniramine maleate, dioxopromethazine hydrochloride, carvedilol, homatropine hydrobromide, homatropine methylbromide, venlafaxine, sibutramine hydrochloride and terbutaline sulfate, respectively. Further, the possible separation mechanism involved was discussed.
[Mh] Termos MeSH primário: Eletrocromatografia Capilar
Técnicas de Química Analítica/métodos
Nanopartículas Metálicas/química
beta-Ciclodextrinas/química
[Mh] Termos MeSH secundário: Compostos Azabicíclicos/química
Compostos Azabicíclicos/isolamento & purificação
Bromofeniramina/química
Bromofeniramina/isolamento & purificação
Carbazóis/química
Carbazóis/isolamento & purificação
Ciclobutanos/química
Ciclobutanos/isolamento & purificação
Ciclodextrinas/química
Microscopia Eletrônica de Transmissão
Piperazinas/química
Piperazinas/isolamento & purificação
Propanolaminas/química
Propanolaminas/isolamento & purificação
Estereoisomerismo
Terbutalina/química
Terbutalina/isolamento & purificação
Tropanos/química
Tropanos/isolamento & purificação
Cloridrato de Venlafaxina/química
Cloridrato de Venlafaxina/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Azabicyclo Compounds); 0 (Carbazoles); 0 (Cyclobutanes); 0 (Cyclodextrins); 0 (Piperazines); 0 (Propanolamines); 0 (Tropanes); 0 (beta-Cyclodextrins); 03A5ORL08Q (zopiclone); 0K47UL67F2 (carvedilol); 68JRS2HC1C (homatropine methylbromide); 7D7RX5A8MO (Venlafaxine Hydrochloride); 8QS6WCL55Z (homatropine); H57G17P2FN (Brompheniramine); JV039JZZ3A (betadex); N8ONU3L3PG (Terbutaline); WV5EC51866 (sibutramine)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160116
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0146292


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[PMID]:24603514
[Au] Autor:McEnery-Stonelake M; Silvestri DL
[Ad] Endereço:From the *University of Massachusetts Medical School; and †UMass Memorial Medical Center, Worcester, MA.
[Ti] Título:Contact allergens in oral antihistamines.
[So] Source:Dermatitis;25(2):83-8, 2014 Mar-Apr.
[Is] ISSN:2162-5220
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Excipients in various formulations of active drugs occasionally include known contact allergens. Their ingestion may trigger dermatitis or cause it to become widespread or refractory to therapy. OBJECTIVE: The aim of this study was to investigate the prevalence of common contact allergens among the excipients of oral antihistamines available in this country. METHODS: We gathered the complete ingredient lists of 2119 different preparations of 12 oral antihistamines from the National Library of Medicine data bank and entered them into an electronic database for analysis. RESULTS: More than half the formulations (55.0%) contained at least 1 member of the 10 allergen families assessed. Most brompheniramine and doxepin preparations included potentially allergenic excipients, whereas fexofenadine was most often free of them. Sorbitan group members, azo dyes, and propylene glycol were the allergens found most frequently in the antihistamines, each present in over 25% of the products. Elixirs, liquids, solutions, suspensions, and syrups were more likely than nonchewable caplets, capsules, and tablets to contain the allergens tabulated (100% vs 39.3%, respectively). Chewable pills frequently contained azo dyes. CONCLUSIONS: Ingestion of antihistamines could precipitate a systemic contact dermatitis in a patient sensitized to an allergen present as an excipient in the medicine.
[Mh] Termos MeSH primário: Alérgenos/análise
Excipientes/análise
Antagonistas dos Receptores Histamínicos/química
[Mh] Termos MeSH secundário: Administração Oral
Compostos Azo/análise
Bromofeniramina/química
Química Farmacêutica
Corantes/análise
Bases de Dados de Produtos Farmacêuticos
Dermatite Alérgica de Contato/etiologia
Formas de Dosagem
Doxepina/química
Antagonistas dos Receptores Histamínicos/administração & dosagem
Medicamentos sem Prescrição/química
Polissorbatos/análise
Medicamentos sob Prescrição/química
Propilenoglicol/análise
Terfenadina/análogos & derivados
Terfenadina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Allergens); 0 (Azo Compounds); 0 (Coloring Agents); 0 (Dosage Forms); 0 (Excipients); 0 (Histamine Antagonists); 0 (Nonprescription Drugs); 0 (Polysorbates); 0 (Prescription Drugs); 1668-19-5 (Doxepin); 6DC9Q167V3 (Propylene Glycol); 7BA5G9Y06Q (Terfenadine); E6582LOH6V (fexofenadine); H57G17P2FN (Brompheniramine)
[Em] Mês de entrada:1411
[Cu] Atualização por classe:151029
[Lr] Data última revisão:
151029
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140308
[St] Status:MEDLINE
[do] DOI:10.1097/DER.0000000000000028


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[PMID]:23587439
[Au] Autor:Leiria TL; Mantovani A; de March Ronsoni R; Martins Pires L; Lapa Kruse M; Glotz de Lima G
[Ad] Endereço:Serviço de Eletrofisiologia, Instituto de Cardiologia, Fundação Universitária de Cardiologia do Rio Grande Do Sul, Porto Alegre, Brasil. drleiria@gmail.com
[Ti] Título:Brugada syndrome after using cold medicine: is there any relation?
[So] Source:Rev Port Cardiol;32(5):415-7, 2013 May.
[Is] ISSN:2174-2030
[Cp] País de publicação:Portugal
[La] Idioma:eng; por
[Ab] Resumo:Brugada syndrome (BrS) is associated with increased risk of ventricular arrhythmias and sudden death. Some drugs can trigger the electrocardiographic and arrhythmic manifestations of this syndrome. Cold medicines for symptom relief are sold without prescription in Brazil and most contain antihistamines and adrenergic agonists. We report a case of BrS probably triggered by the use of such medication.
[Mh] Termos MeSH primário: Bromofeniramina/efeitos adversos
Síndrome de Brugada/induzido quimicamente
Antagonistas dos Receptores Histamínicos H1/efeitos adversos
Descongestionantes Nasais/efeitos adversos
Fenilefrina/efeitos adversos
[Mh] Termos MeSH secundário: Adulto
Seres Humanos
Masculino
Medicamentos Compostos contra Resfriado, Influenza e Alergia/efeitos adversos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Multi-Ingredient Cold, Flu, and Allergy Medications); 0 (Nasal Decongestants); 1WS297W6MV (Phenylephrine); H57G17P2FN (Brompheniramine)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:130603
[Lr] Data última revisão:
130603
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130417
[St] Status:MEDLINE


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[PMID]:23587318
[Au] Autor:DeSoi D; Kier LB; Cheng CK; Karnes HT
[Ad] Endereço:Virginia Commonwealth University, School of Pharmacy, Department of Pharmaceutics, Richmond, VA 23298-0533, USA. desoidj@mymail.vcu.edu
[Ti] Título:An expanded cellular automata model for enantiomer separations using a ß-cyclodextrin stationary phase.
[So] Source:J Chromatogr A;1291:73-83, 2013 May 24.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Chromatographic scale enantiomer separation has not been modeled using cellular automata (CA). CA uses easy to adjust equations to different enantiomers under various chromatographic conditions. Previous work has demonstrated that CA modeling can accurately predict the strength of one-to-one binding interactions between enantiomers and ß-cyclodextrin (CD) [1]. In this work, the model is expanded to a chromatographic scale grid environment in order to transform model output into HPLC chromatograms. The model accurately predicted the lack of chromatographic selectivity of mandelic enantiomers (1.05 published, 1.01 modeled) and the separation of brompheniramine enantiomers (1.13 published, 1.12 modeled) previously modeled in one-to-one interactions. By examining cyclohexylphenylglycolic acid (CHPGA) enantiomers, the model accurately predicted both the selectivity and resolution of the enantiomer peaks at varying chromatographic temperatures. Modeled changes in mobile phase pH agree with laboratory outcomes when examining peak resolution and selectivity. Changes in injection volume resulted in an increase in retention time of the modeled enantiomers as was observed in the published laboratory results.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/instrumentação
Cromatografia Líquida de Alta Pressão/métodos
Modelos Estatísticos
beta-Ciclodextrinas/química
[Mh] Termos MeSH secundário: Bromofeniramina/química
Bromofeniramina/isolamento & purificação
Glicolatos/química
Glicolatos/isolamento & purificação
Interações Hidrofóbicas e Hidrofílicas
Ácidos Mandélicos/química
Ácidos Mandélicos/isolamento & purificação
Projetos de Pesquisa
Estereoisomerismo
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycolates); 0 (Mandelic Acids); 0 (beta-Cyclodextrins); H57G17P2FN (Brompheniramine); NH496X0UJX (mandelic acid)
[Em] Mês de entrada:1310
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130417
[St] Status:MEDLINE


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[PMID]:23043884
[Au] Autor:Soares DN; Valinoti AC; Pierro VS; Antonio AG; Maia LC
[Ad] Endereço:Federal University of Rio de Janeiro, Rio de Janeiro, Brazil. rorefa@terra.com.br
[Ti] Título:Cross-sectional microhardness of bovine enamel subjected to three paediatric liquid oral medicines: an in vitro study.
[So] Source:Eur Arch Paediatr Dent;13(5):261-5, 2012 Oct.
[Is] ISSN:1818-6300
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIM: This study aimed to investigate the in vitro effects of three paediatric liquid oral medicines on bovine dental enamel subsurfaces under pH cycling conditions. METHODS: Bovine enamel blocks were evaluated for surface hardness at baseline for sample selection. 52 intact bovine enamel blocks (16mm(2)) were randomly divided into four groups (n=13) according to the immersion treatments: G1: antibiotic (Klaricid®), G2: antihistamine (Claritin®), G3: antihistamine (Dimetapp®) and G4: control (de-ionised water). The blocks were submitted to pH cycling treatments twice a day for 12 days. The medicines were evaluated for pH, viscosity, and concentration of calcium, phosphate and fluoride. After the treatment period, cross-sectional microhardness (CSMH) measurements of the enamel blocks were taken and the data, expressed in Knoop hardness number (kg/mm(2)) was used to calculate the ΔS. STATISTICS: ANOVA followed by the Tukey test were used for statistical analyses (p<0.05). RESULTS: The antibiotic Klaricid® showed the highest concentration of fluoride, calcium and phosphate. Considering pH and viscosity, the following pattern was observed according to the treatment group: G4>G1>G2>G3 and G1>G2>G3>G4 respectively. Regarding the demineralisation pattern, the following results were observed: G4>G3>G2>G1. Compared to the control, the antibiotic and both the antihistamines provoked less demineralisation of the enamel blocks (p<0.05). CONCLUSIONS: Antibiotic G1 (Klaricid®) presented an in vitro protective effect against acid attacks probably due to its mineral content and viscosity.
[Mh] Termos MeSH primário: Esmalte Dentário/efeitos dos fármacos
Excipientes Farmacêuticos/efeitos adversos
[Mh] Termos MeSH secundário: Anatomia Transversal
Animais
Antibacterianos/efeitos adversos
Antibacterianos/química
Bromofeniramina/efeitos adversos
Bromofeniramina/química
Cálcio/análise
Bovinos
Claritromicina/efeitos adversos
Claritromicina/química
Solubilidade do Esmalte Dentário/efeitos dos fármacos
Combinação de Medicamentos
Fluoretos/análise
Dureza
Antagonistas dos Receptores Histamínicos H1 não Sedativos/efeitos adversos
Antagonistas dos Receptores Histamínicos H1 não Sedativos/química
Concentração de Íons de Hidrogênio
Loratadina/efeitos adversos
Loratadina/química
Descongestionantes Nasais/efeitos adversos
Descongestionantes Nasais/química
Excipientes Farmacêuticos/química
Fosfatos/análise
Pseudoefedrina/efeitos adversos
Pseudoefedrina/química
Distribuição Aleatória
Soluções
Desmineralização do Dente/induzido quimicamente
Viscosidade
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Drug Combinations); 0 (Histamine H1 Antagonists, Non-Sedating); 0 (Nasal Decongestants); 0 (Pharmaceutic Aids); 0 (Phosphates); 0 (Solutions); 0 (brompheniramine, pseudoephedrine drug combination); 7AJO3BO7QN (Loratadine); 7CUC9DDI9F (Pseudoephedrine); H1250JIK0A (Clarithromycin); H57G17P2FN (Brompheniramine); Q80VPU408O (Fluorides); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1302
[Cu] Atualização por classe:171114
[Lr] Data última revisão:
171114
[Sb] Subgrupo de revista:D; IM
[Da] Data de entrada para processamento:121010
[St] Status:MEDLINE


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[PMID]:22612655
[Au] Autor:Tardioli S; Lammers I; Hooijschuur JH; Ariese F; van der Zwan G; Gooijer C
[Ad] Endereço:Department of Biomolecular Analysis and Spectroscopy, LaserLaB, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
[Ti] Título:Complementary fluorescence and phosphorescence study of the interaction of brompheniramine with human serum albumin.
[So] Source:J Phys Chem B;116(24):7033-9, 2012 Jun 21.
[Is] ISSN:1520-5207
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Binding of the antihistamine drug brompheniramine (BPA) to human serum albumin (HSA) is studied by measuring quenching of the fluorescence and room temperature phosphorescence (RTP) of tryptophan. The modified Stern-Volmer equation was used to derive association constants and accessible fractions from the steady-state fluorescence data. Decay associated spectra (DAS) revealed three tryptophan fluorescence lifetimes, indicating the presence of three HSA conformations. BPA causes mainly static quenching of the long-living, solvent-exposed conformer. RTP spectra and lifetimes, recorded under deoxygenated conditions in the presence of 0.2 M KI, provided additional kinetic information about the HSA-BPA interactions. Fluorescence DAS that were also recorded in the presence of 0.2 M KI revealed that the solvent-exposed conformer is the major contributor to the RTP signal. The phosphorescence quenching is mostly dynamic at pH 7 and mostly static at pH 9, presumably related to the protonation state of the alkylamino chain of BPA. This provides direct insight into the binding mode of the antihistamine drug, as well as kinetic information at both the nanosecond and the millisecond time scales.
[Mh] Termos MeSH primário: Bromofeniramina/metabolismo
Albumina Sérica/metabolismo
[Mh] Termos MeSH secundário: Bromofeniramina/química
Seres Humanos
Concentração de Íons de Hidrogênio
Cinética
Ligação Proteica
Albumina Sérica/química
Espectrometria de Fluorescência
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Serum Albumin); H57G17P2FN (Brompheniramine)
[Em] Mês de entrada:1210
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120523
[St] Status:MEDLINE
[do] DOI:10.1021/jp300055c


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[PMID]:22372713
[Au] Autor:Tardioli S; Buijs J; Gooijer C; van der Zwan G
[Ad] Endereço:Amsterdam LaserLaB, Department of Biomolecular Analysis and Spectroscopy, Vrije Universiteit, Amsterdam, The Netherlands.
[Ti] Título:pH-dependent complexation of histamine H1 receptor antagonists and human serum albumin studied by UV resonance Raman spectroscopy.
[So] Source:J Phys Chem B;116(12):3808-15, 2012 Mar 29.
[Is] ISSN:1520-5207
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:UV resonance Raman spectroscopy was used to characterize the binding of three first-generation histamine H(1) receptor antagonists-tripelennamine (TRP), mepyramine (MEP), and brompheniramine (BPA)-to human serum albumin (HSA) at pH 7.2 and pH 9.0. Binding constants differ at these pH values, which can be ascribed to the different extent of protonation of the ethylamino side chain of the ligands. We have recently shown [Tardioli et al. J. Raman Spectrosc. 2011, 42, 1016-1024] that for the solution conformation of TRP and MEP the side chain plays an important role by allowing an internal hydrogen bond with the aminopyridine nitrogen in TRP and MEP. Results presented in this paper suggest that the existence of such molecular structures has serious biological significance on the binding affinity of those ligands to HSA. At pH 7.2, only the stretched conformers of protonated TRP and MEP bind in HSA binding site I. Using UV absorption data, we derived binding constants for the neutral and protonated forms of TRP to HSA. The neutral species seems to be conjugated to a positive group of the protein, affecting both the tryptophan W214 and some of the tyrosine (Y) vibrations. BPA, for which the structure with an intramolecular hydrogen bonded side chain is not possible, is H bound to the indole ring nitrogen of W214, of which the side chain rotates over a certain angle to accommodate the drug in site I. We propose that the protonated BPA is also bound in site I, where the Y150 residue stabilizes the presence of this compound in the binding pocket. No spectroscopic evidence was found for conformational changes of the protein affecting the spectroscopic properties of W and Y in this pH range.
[Mh] Termos MeSH primário: Antagonistas dos Receptores Histamínicos H1/química
Receptores Histamínicos H1/química
Albumina Sérica/química
Espectrofotometria Ultravioleta
Análise Espectral Raman
[Mh] Termos MeSH secundário: Sítios de Ligação
Bromofeniramina/química
Antagonistas dos Receptores Histamínicos H1/metabolismo
Seres Humanos
Ligações de Hidrogênio
Concentração de Íons de Hidrogênio
Pirilamina/química
Receptores Histamínicos H1/metabolismo
Albumina Sérica/metabolismo
Tripelenamina/química
Triptofano/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Receptors, Histamine H1); 0 (Serum Albumin); 3C5ORO99TY (Tripelennamine); 8DUH1N11BX (Tryptophan); H57G17P2FN (Brompheniramine); HPE317O9TL (Pyrilamine)
[Em] Mês de entrada:1207
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120301
[St] Status:MEDLINE
[do] DOI:10.1021/jp206409d


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[PMID]:22337782
[Au] Autor:Rodrigues WC; Castro C; Catbagan P; Moore C; Wang G
[Ad] Endereço:Immunalysis Corporation, Pomona, CA 91767, USA. wrodrigues@immunalysis.com
[Ti] Título:Immunoassay screening of diphenhydramine (Benadryl®) in urine and blood using a newly developed assay.
[So] Source:J Anal Toxicol;36(2):123-9, 2012 Mar.
[Is] ISSN:1945-2403
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Diphenhydramine (DPH) is a common over the counter antihistamine that produces drowsiness and has the potential to cause driving under the influence of drugs-related accidents. To date there are no commercially available immunoassay screening kits for its detection in biological fluids such as urine and/or blood. We describe a newly developed enzyme-linked immunosorbent assay (ELISA) screen and report on its utility in the analysis of authentic specimens taken from volunteers. The assay is specific for detection of DPH and does not detect closely related antihistamines like brompheniramine, chlorpheniramine, and doxylamine. There is a varying amount of cross-reactivity seen with certain tricyclic compounds, due to similarities in side chain structure with DPH. Intra- and interday precision of the assay were determined to be less than 10%. The assay is highly sensitive and has a working range from 1 to 500 ng/mL for urine and 1 to 250 ng/mL for blood. The assay was further validated with authentic urine and blood specimens obtained from volunteers and coroner's laboratories.
[Mh] Termos MeSH primário: Difenidramina/sangue
Difenidramina/urina
Ensaio de Imunoadsorção Enzimática/métodos
[Mh] Termos MeSH secundário: Bromofeniramina/sangue
Clorfeniramina/sangue
Doxilamina/sangue
Antagonistas dos Receptores Histamínicos
Seres Humanos
Reprodutibilidade dos Testes
Manejo de Espécimes
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine Antagonists); 3U6IO1965U (Chlorpheniramine); 8GTS82S83M (Diphenhydramine); 95QB77JKPL (Doxylamine); H57G17P2FN (Brompheniramine)
[Em] Mês de entrada:1206
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120217
[St] Status:MEDLINE
[do] DOI:10.1093/jat/bkr015


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[PMID]:22213440
[Au] Autor:Zidan AS; Rahman Z; Khan MA
[Ad] Endereço:Division of Product Quality and Research, Center for Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, Maryland, USA.
[Ti] Título:Chemometric evaluation of brompheniramine-tannate complexes.
[So] Source:J Pharm Sci;101(4):1450-61, 2012 Apr.
[Is] ISSN:1520-6017
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The objective of the current study was to evaluate the performance of Raman and near-infrared (NIR) techniques combined with chemometrics in characterizing the critical quality attributes of brompheniramine (BP)-tannate complexes. Seven complexes were prepared and evaluated for chemical interactions, solubilities, dissolutions, and spatial distributions by NIR chemical imaging (CI). Principal component analysis (PCA) was applied before either partial least squares regression (PLSR) or principal component regression (PCR) models were developed. Complexation was confirmed by Fourier transform IR analysis to yield complexes of lower drug solubilities and sustained-release characteristics in alkaline media. PCA results showed better discrimination ability by NIR than by Raman spectroscopy. Compared with PCR, the PLSR predictions errors, calculated from the Raman and NIR data with second-derivative pretreatment, showed lesser values of 2.68, 0.37, 1.79, and 5.60 and 0.58, 0.25, 0.93, and 0.58 for complex solubilities in acidic and alkaline media and percentages dissolved after 1 and 20 h, respectively. In addition, good correlation (>0.95) was obtained for predicting the drug concentration using PLSR score images explaining the validity of the NIR-CI model for spatial quantitation of BP within its tannate complexes. In conclusion, the chemometric analysis of NIR and/or Raman spectra represented an innovative approach to determine the tannate complexation variability.
[Mh] Termos MeSH primário: Bromofeniramina/química
Antagonistas dos Receptores Histamínicos H1/química
Taninos/química
[Mh] Termos MeSH secundário: Análise dos Mínimos Quadrados
Análise de Componente Principal
Análise de Regressão
Espectroscopia de Luz Próxima ao Infravermelho
Análise Espectral Raman
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Tannins); H57G17P2FN (Brompheniramine)
[Em] Mês de entrada:1206
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120104
[St] Status:MEDLINE
[do] DOI:10.1002/jps.23030


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[PMID]:22037447
[Au] Autor:Rahman Z; Zidan AS; Berendt RT; Khan MA
[Ad] Endereço:Division of Product Quality and Research, Center of Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD 20993-002, USA.
[Ti] Título:Tannate complexes of antihistaminic drug: sustained release and taste masking approaches.
[So] Source:Int J Pharm;422(1-2):91-100, 2012 Jan 17.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The aim of this investigation was to evaluate the complexation potential of brompheniramine maleate (BPM) and tannic acid (TA) for sustained release and taste masking effects. The complexes (1:1-1:7 TA to BPM ratio) were prepared by the solvent evaporation method using methanol, phosphate buffer pH 6.8 or 0.1N HCl as common solvents. The complexes were characterized microscopically by scanning electron microscopy (SEM), chemically by Fourier transform infrared (FTIR) and solid-state NMR (SSNMR), thermally by differential scanning calorimetry (DSC), for crystallinity by powder X-ray powder diffraction (PXRD), for organoleptic evaluation by electronic tongue (e-tongue), and for solubility in 0.1N HCl and phosphate buffer pH 6.8. The dissolution studies were carried out using the USP II method at 50 rpm in 500 ml of dissolution media (0.1N HCl or phosphate buffer pH 6.8). SEM images revealed that the morphology of complexes were completely different from the individual components, and all complexes had the same morphological characteristics, irrespective of the solvent used for their preparation, pH or ratio of BPM and TA. The FTIR spectra showed the presence of chemical interactions between the TA and BPM. DSC, PXRD and SSNMR indicated that the drug lost its crystalline nature by formation of the complex. Complexation has significantly reduced the solubility of BPM and sustained the drug release up to 24h in phosphate buffer pH 6.8 media. The bitter taste of the BPM was completely masked which was indicated by Euclidean distance values which was far from the drug but near to its placebo in the complexes in all ratios studied. The taste masked complexes can be potentially developed as suitable dosage forms for pediatric use. In summary, complexation of BPM and TA effectively sustained the dissolution and masked the bitter taste of drug for the development of suitable dosage forms for pediatric use.
[Mh] Termos MeSH primário: Bromofeniramina/química
Antagonistas dos Receptores Histamínicos H1/química
Mascaramento Perceptivo
Taninos/química
Paladar/efeitos dos fármacos
[Mh] Termos MeSH secundário: Tampões (Química)
Varredura Diferencial de Calorimetria
Química Farmacêutica
Cristalografia por Raios X
Preparações de Ação Retardada
Composição de Medicamentos
Ácido Clorídrico/química
Cinética
Espectroscopia de Ressonância Magnética
Metanol/química
Microscopia Eletrônica de Varredura
Fosfatos/química
Potenciometria
Difração de Pó
Solubilidade
Solventes/química
Espectroscopia de Infravermelho com Transformada de Fourier
Propriedades de Superfície
Tecnologia Farmacêutica/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Buffers); 0 (Delayed-Action Preparations); 0 (Histamine H1 Antagonists); 0 (Phosphates); 0 (Solvents); 0 (Tannins); H57G17P2FN (Brompheniramine); QTT17582CB (Hydrochloric Acid); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1204
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:111101
[St] Status:MEDLINE
[do] DOI:10.1016/j.ijpharm.2011.10.033



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