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1.
Int J Pharm Compd ; 22(6): 516-526, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30384353

RESUMO

Compounded liquid medication is frequently required in children to allow easy dose adjustment and overcome swallowing difficulties. The objective of this study was to evaluate the stability of oral suspensions compounded with SyrSpend SF PH4 and the commonly used active pharmaceutical ingredients baclofen 2.0 mg/mL, carvedilol 5.0 mg/mL, hydrochlorothiazide 2.0 mg/mL, mercaptopurine 10.0 mg/mL, methadone hydrochloride 10.0 mg/mL, oseltamivir phosphate 6.0 mg/mL, phenobarbital 9.0 mg/mL and 15.0 mg/mL, propranolol hydrochloride 0.5 mg/mL and 5.0 mg/mL, pyrazinamide 100.0 mg/mL, spironolactone 2.0 mg/mL and 2.5 mg/mL, sotalol hydrochloride 5.0 mg/mL, tacrolimus monohydrate 0.5 mg/mL, ursodeoxycholic acid 20.0 mg/mL, and vancomycin hydrochloride 25.0 mg/mL. Suspensions were compounded with raw powders, except for mercaptopurine, pyrazinamide, and sotalol hydrochloride, which were made from commercial tablets. Stability was assessed by measuring the percentage recovery at 0 (baseline), 60 days, and 90 days after compounding for suspensions made with raw powders, which were stored at 2ÅãC to 8ÅãC. The stability of tablets, which were stored at 2ÅãC to 8ÅãC and 20ÅãC to 25ÅãC, was assessed by measuring the percentage recovery at 0 (baseline), 7 days, 14 days, 30 days, 60 days, and 90 days. Active pharmaceutical ingredients quantification was performed by ultraviolet high-performance liquid chromatography via a stability-indicating method. Given the percentage of recovery of the active pharmaceutical ingredients within the suspensions, the beyond-use date of the final products (active pharmaceutical ingredients + vehicle) was at least 90 days for all suspensions in the conditions tested. This suggests that SyrSpend SF PH4 is suitable for compounding active pharmaceutical ingredients from different pharmacological classes.


Assuntos
Baclofeno/química , Carvedilol/química , Hidroclorotiazida/química , Mercaptopurina/química , Metadona/química , Oseltamivir/química , Veículos Farmacêuticos/química , Fenobarbital/química , Propranolol/química , Sotalol/química , Espironolactona/química , Amido/química , Tacrolimo/química , Ácido Ursodesoxicólico/química , Vancomicina/química , Administração Oral , Baclofeno/administração & dosagem , Carvedilol/administração & dosagem , Composição de Medicamentos , Estabilidade de Medicamentos , Hidroclorotiazida/administração & dosagem , Concentração de Íons de Hidrogênio , Mercaptopurina/administração & dosagem , Metadona/administração & dosagem , Oseltamivir/administração & dosagem , Soluções Farmacêuticas , Fenobarbital/administração & dosagem , Propranolol/administração & dosagem , Pirazinamida/administração & dosagem , Sotalol/administração & dosagem , Espironolactona/administração & dosagem , Suspensões , Tacrolimo/administração & dosagem , Temperatura , Fatores de Tempo , Ácido Ursodesoxicólico/administração & dosagem , Vancomicina/administração & dosagem
2.
Photochem Photobiol Sci ; 17(10): 1355-1364, 2018 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-30183793

RESUMO

Methylene Blue (MB) has been widely used in antimicrobial Photodynamic Therapy (aPDT), however, the mechanisms of action (Type I or Type II) are defined by its state of aggregation. In this sense, the identification of the relationships between aggregation, the mechanisms of action and the effectiveness against microorganisms, as well as the establishment of the means and the formulations that may favor the most effective mechanisms, are essential. Thus, the objective of this study was to assess the in vitro aPDT efficacies against Candida albicans, by using MB in vehicles which may influence the aggregation and present an oral formulation (OF) containing MB, to be used in clinical aPDT procedures. The efficacy of MB at 20 mg L-1 was tested in a range of vehicles (water, physiological solution - NaCl 0.9%, phosphate saline buffer - PBS, sodium dodecyl sulfate 0.25% - SDS and urea 1 mol L-1) in a C. albicans planktonic culture, when using 4.68 J cm-2 of 640 ± 12 nm LED for the irradiations, as well as 5 minutes of pre-irradiation time, together with measuring the UFC mL-1. Based upon these analyses, an OF containing MB in the most effective vehicle was tested in the biofilms, as a proposal for clinical applications. When comparing some of the vehicles, sodium dodecyl sulfate was the only one that enhanced an MB aPDT efficacy in a planktonic C. albicans culture. This OF was tested in the biofilms and 50 mg L-1 MB was necessary, in order to achieve some reduction in the cell viabilities after the various treatments. The light dosimetries still need further adaptations, in order for this formulation to be used in clinical applications. The present research has indicated that the development of this formulation for the control of MB aggregations may result in more effective clinical protocols.


Assuntos
Candida albicans/efeitos dos fármacos , Candidíase/tratamento farmacológico , Dimerização , Azul de Metileno/administração & dosagem , Veículos Farmacêuticos/química , Fármacos Fotossensibilizantes/administração & dosagem , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/farmacologia , Biofilmes/efeitos dos fármacos , Candida albicans/fisiologia , Candidíase/microbiologia , Humanos , Azul de Metileno/química , Azul de Metileno/farmacologia , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/farmacologia , Dodecilsulfato de Sódio/química
3.
J AOAC Int ; 101(5): 1461-1465, 2018 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-29895343

RESUMO

BACKGROUND: The fruits acerola and red plum are known to be good sources of antioxidants, particularly vitamin C. Antioxidants are compounds that protect organisms from biomolecular damage, such as accelerated aging, caused by free radicals. OBJECTIVE: The objective of this study was to extract vitamin C from acerola and red plum, incorporate these extracts into different topical formulations, and evaluate the physicochemical stabilities of these formulations under stress conditions. METHODS: Vitamin C was extracted from acerola and red plum via dynamic maceration for 2 h at 50 ± 2°C and was quantified via HPLC. In vitro antioxidant activities were evaluated using DPPH assays. The extracts were then incorporated into emulsion and gel formulations in two types of packaging, and stability studies were carried out. RESULTS: Red plum and acerola extracts were orange and red and contained vitamin C concentrations of 2732.70 ± 93.01 mg/100 g and 2.60 ± 1.2 mg/100 g, respectively. In vitro antioxidant activity resulted in over 90.0% inhibition of free radicals at 0.01 mL/mL acerola extract and 0.1 mL/mL red plum extract. In the stability study, pH values decreased for both acerola formulations when stored in the oven or in transparent glass containers. Formulations containing red plum extract were stable under all conditions. Acerola extracts contained a higher concentration of vitamin C than red plum extracts. Both extracts possessed antioxidant activity, although the acerola-based formulation was unstable when stored at high temperatures or in transparent glass containers. HIGHLIGHTS: Extracts from red plum and acerola contained vitamin C; antioxidant activity of the extracts resulted in over 90.0% inhibition of free radicals. Formulations containing red plum were stable under all tested conditions, and formulations containing acerola were unstable when stored in the oven or in transparent glass containers.


Assuntos
Antioxidantes/análise , Ácido Ascórbico/análise , Cromatografia Líquida de Alta Pressão/métodos , Malpighiaceae/química , Extratos Vegetais/análise , Prunus domestica/química , Administração Tópica , Antioxidantes/administração & dosagem , Antioxidantes/farmacologia , Ácido Ascórbico/administração & dosagem , Ácido Ascórbico/farmacologia , Composição de Medicamentos , Estabilidade de Medicamentos , Emulsões/química , Radicais Livres/química , Frutas/química , Géis/química , Veículos Farmacêuticos/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia
4.
Braz Oral Res ; 31: e43, 2017 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-28678965

RESUMO

The aim of this study was to evaluate edemogenic activity and subcutaneous inflammatory reaction induced by Psidium cattleianum leaf extracts associated with Ca(OH)2. Thirty male Wistar rats, split equally into three groups [aqueous extract + Ca(OH)2; ethanolic extract + Ca(OH)2; and propylene glycol + Ca(OH)2], were assessed every 3 h or 6 h (five animals in each period). Under general anesthesia, 0.2 mL of 1% Evans blue per 100 g of body weight was injected into the penile vein and each combination to be evaluated was subcutaneously injected into the dorsal region 30 min thereafter. Edemogenic activity was analyzed by spectrophotometry (λ=630 nm). For inflammatory reaction analysis, 50 rats received four polyethylene tubes (three experimental groups) and an empty tube (control group). The assessments were made at 7, 15, 30, 60, and 90 days, followed by hematoxylin-eosin staining and by the assignment of scores for evaluation of tissue response intensity. Ethanolic extract + Ca(OH)2 yielded the largest edemogenic activity at 3 h. Intergroup differences at 6 h were not significant. The histological analysis showed progressive repair over time (p<0.05) and aqueous and ethanolic extracts produced similar responses to those of the control and Ca(OH)2 + propylene glycol groups. Psidium cattleianum leaf extracts used as Ca(OH)2 vehicles evoked similar tissue response when compared to Ca(OH)2 associated with propylene glycol.


Assuntos
Hidróxido de Cálcio/farmacologia , Extratos Vegetais/farmacologia , Psidium/química , Tela Subcutânea/efeitos dos fármacos , Animais , Anti-Infecciosos/farmacologia , Portadores de Fármacos , Avaliação Pré-Clínica de Medicamentos , Etanol/farmacologia , Inflamação/tratamento farmacológico , Inflamação/patologia , Masculino , Teste de Materiais , Veículos Farmacêuticos/química , Veículos Farmacêuticos/farmacologia , Folhas de Planta/química , Propilenoglicol/farmacologia , Ratos Wistar , Reprodutibilidade dos Testes , Tela Subcutânea/patologia , Fatores de Tempo , Água/química
5.
Braz. oral res. (Online) ; 31: e43, 2017. graf
Artigo em Inglês | LILACS | ID: biblio-952091

RESUMO

Abstract The aim of this study was to evaluate edemogenic activity and subcutaneous inflammatory reaction induced by Psidium cattleianum leaf extracts associated with Ca(OH)2. Thirty male Wistar rats, split equally into three groups [aqueous extract + Ca(OH)2; ethanolic extract + Ca(OH)2; and propylene glycol + Ca(OH)2], were assessed every 3 h or 6 h (five animals in each period). Under general anesthesia, 0.2 mL of 1% Evans blue per 100 g of body weight was injected into the penile vein and each combination to be evaluated was subcutaneously injected into the dorsal region 30 min thereafter. Edemogenic activity was analyzed by spectrophotometry (λ=630 nm). For inflammatory reaction analysis, 50 rats received four polyethylene tubes (three experimental groups) and an empty tube (control group). The assessments were made at 7, 15, 30, 60, and 90 days, followed by hematoxylin-eosin staining and by the assignment of scores for evaluation of tissue response intensity. Ethanolic extract + Ca(OH)2 yielded the largest edemogenic activity at 3 h. Intergroup differences at 6 h were not significant. The histological analysis showed progressive repair over time (p<0.05) and aqueous and ethanolic extracts produced similar responses to those of the control and Ca(OH)2 + propylene glycol groups. Psidium cattleianum leaf extracts used as Ca(OH)2 vehicles evoked similar tissue response when compared to Ca(OH)2 associated with propylene glycol.


Assuntos
Animais , Masculino , Hidróxido de Cálcio/farmacologia , Extratos Vegetais/farmacologia , Tela Subcutânea/efeitos dos fármacos , Psidium/química , Fatores de Tempo , Veículos Farmacêuticos/farmacologia , Veículos Farmacêuticos/química , Teste de Materiais , Portadores de Fármacos , Água/química , Reprodutibilidade dos Testes , Ratos Wistar , Folhas de Planta/química , Propilenoglicol/farmacologia , Tela Subcutânea/patologia , Etanol/farmacologia , Avaliação Pré-Clínica de Medicamentos , Inflamação/patologia , Inflamação/tratamento farmacológico , Anti-Infecciosos/farmacologia
6.
J. appl. oral sci ; J. appl. oral sci;23(5): 508-514, Sept.-Oct. 2015. tab, graf
Artigo em Inglês | LILACS, BBO - Odontologia | ID: lil-764164

RESUMO

The aim of this study was to evaluate the subcutaneous tissue response in rats and the antimicrobial activity of intracanal calcium hydroxide dressings mixed with different substances against E. faecalis. Fifty four rats were divided into three experimental groups according to the vehicle in the calcium hydroxide treatment: 0.4% chlorohexidine in propylene glycol (PG),Casearia sylvestris Sw in PG and calcium hydroxide+PG (control group). The pastes were placed into polyethylene tubes and implanted into the subcutaneous tissue. After 7, 14 and 30 days, the samples were processed and histologically evaluated (hematoxylin and eosin). The tissue surface in contact with the material was analyzed, and the quantitative analysis determined the volume density occupied by the inflammatory infiltrate (giant cells, polymorphonuclear cells and mononuclear cells), fibroblasts, collagen fibers and blood vessels. For the antimicrobial analysis, 20 dentin blocks infected with E. faecalis were treated with calcium hydroxide pastes in different vehicles; 0.4% chlorhexidine in PG, PG, extract fromCasearia sylvestris Sw in PG and a positive control (infection and without medication) for 7 days. The efficiency of the pastes was evaluated by the live/dead technique and confocal microscopy. The results showed that 0.4% chlorhexidine induced a higher inflammatory response than the other groups. The Casearia sylvestris Sw extract showed satisfactory results in relation to the intensity of the inflammatory response. In the microbiological test, there were no statistical differences between the evaluated intracanal dressings and the percentage of bacterial viability was between 33 and 42%. The control group showed an 86% viability. Antimicrobial components such as chlorhexidine or Casearia sylvestris Sw did not improve the antimicrobial activity against E. faecalis in comparison to the calcium hydroxide+PG treatment. In addition, the incorporation of chlorhexidine in the calcium hydroxide paste promoted the highest inflammatory response.


Assuntos
Animais , Bovinos , Anti-Infecciosos/farmacologia , Hidróxido de Cálcio/farmacologia , Casearia/química , Clorexidina/farmacologia , Tela Subcutânea/efeitos dos fármacos , Anti-Infecciosos/química , Hidróxido de Cálcio/química , Células Cultivadas , Clorexidina/química , Colágeno/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Teste de Materiais , Viabilidade Microbiana/efeitos dos fármacos , Pomadas , Veículos Farmacêuticos/química , Veículos Farmacêuticos/farmacologia , Propilenoglicol/química , Propilenoglicol/farmacologia , Ratos Wistar , Tela Subcutânea/patologia , Fatores de Tempo
7.
J Appl Oral Sci ; 23(5): 508-14, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26200527

RESUMO

The aim of this study was to evaluate the subcutaneous tissue response in rats and the antimicrobial activity of intracanal calcium hydroxide dressings mixed with different substances against E. faecalis. Fifty four rats were divided into three experimental groups according to the vehicle in the calcium hydroxide treatment: 0.4% chlorohexidine in propylene glycol (PG),Casearia sylvestris Sw in PG and calcium hydroxide+PG (control group). The pastes were placed into polyethylene tubes and implanted into the subcutaneous tissue. After 7, 14 and 30 days, the samples were processed and histologically evaluated (hematoxylin and eosin). The tissue surface in contact with the material was analyzed, and the quantitative analysis determined the volume density occupied by the inflammatory infiltrate (giant cells, polymorphonuclear cells and mononuclear cells), fibroblasts, collagen fibers and blood vessels. For the antimicrobial analysis, 20 dentin blocks infected with E. faecalis were treated with calcium hydroxide pastes in different vehicles; 0.4% chlorhexidine in PG, PG, extract from Casearia sylvestris Sw in PG and a positive control (infection and without medication) for 7 days. The efficiency of the pastes was evaluated by the live/dead technique and confocal microscopy. The results showed that 0.4% chlorhexidine induced a higher inflammatory response than the other groups. The Casearia sylvestris Sw extract showed satisfactory results in relation to the intensity of the inflammatory response. In the microbiological test, there were no statistical differences between the evaluated intracanal dressings and the percentage of bacterial viability was between 33 and 42%. The control group showed an 86% viability. Antimicrobial components such as chlorhexidine or Casearia sylvestris Sw did not improve the antimicrobial activity against E. faecalis in comparison to the calcium hydroxide+PG treatment. In addition, the incorporation of chlorhexidine in the calcium hydroxide paste promoted the highest inflammatory response.


Assuntos
Anti-Infecciosos/farmacologia , Hidróxido de Cálcio/farmacologia , Casearia/química , Clorexidina/farmacologia , Tela Subcutânea/efeitos dos fármacos , Animais , Anti-Infecciosos/química , Hidróxido de Cálcio/química , Bovinos , Células Cultivadas , Clorexidina/química , Colágeno/efeitos dos fármacos , Enterococcus faecalis/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Teste de Materiais , Viabilidade Microbiana/efeitos dos fármacos , Pomadas , Veículos Farmacêuticos/química , Veículos Farmacêuticos/farmacologia , Propilenoglicol/química , Propilenoglicol/farmacologia , Ratos Wistar , Tela Subcutânea/patologia , Fatores de Tempo
8.
Carbohydr Polym ; 104: 166-74, 2014 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-24607174

RESUMO

Efavirenz (EFV) used as a part of the treatment of first choice in antiretroviral therapy for AIDS has low aqueous solubility and presents problems of absorption. We thus initially present a phase solubility diagram with carriers of different classes. With a view to obtaining a solid dispersion (SD) with suitable consistency to that of a solid formulation, we chose to use PVP K-30, since polymers present some of the best results. The kneading (KN) and solvent evaporation (EV) methods were thus used at different rates. These were characterized by the way of DSC, FT-IR, SEM, DR-X and dissolution. SD EV proved unsatisfactory, resulting in a decreased dissolution rate, despite the amorphous state of the samples, while the SD KN 4:1 (EFV:polymer) and physical mixtures (PM) had a higher rate of dissolution. SD KN and PM 4:1 were also evaluated for stability after storage, with benefits being observed in relation to EFV.


Assuntos
Benzoxazinas/química , Veículos Farmacêuticos/química , Povidona/química , Inibidores da Transcriptase Reversa/química , Alcinos , Ciclopropanos , Solubilidade
9.
Hum Exp Toxicol ; 33(1): 54-63, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23536518

RESUMO

It has been hypothesized that oils containing high levels of omega-3 polyunsaturated fatty acids, such as canola and fish oil, could counteract some of the adverse effects induced by phthalates. In the present study, the influence of different oily vehicles on di-butyl phthalate (DBP)-induced testicular toxicity and lipid profile was investigated. Pregnant Wistar rats were treated by oral gavage from gestation days 13 to 20 with DBP (500 mg/kg/day) diluted in three different vehicles: corn, canola or fish oil. Male fetuses were analyzed on gestation day 20. DBP exposure lowered intratesticular testosterone levels and anogenital distance, regardless of the vehicle used. The percentage of seminiferous cords containing multinucleated gonocytes and cord diameter was increased in DBP-exposed groups, compared with vehicle controls, with no difference between the three DBP-exposed groups. Clustering of Leydig cells was seen in all DBP groups. Lipid profile indicated that administration of canola and fish oil can increase the content of omega-3 fatty acids in rat testis. However, content of omega-3 was diminished in DBP-treated groups. Overall, our results indicate that different oily vehicles did not alter fetal rat testicular toxicity induced by a high DBP dose.


Assuntos
Dibutilftalato/toxicidade , Disruptores Endócrinos/toxicidade , Ácidos Graxos Ômega-3/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Exposição Materna/efeitos adversos , Veículos Farmacêuticos/metabolismo , Testículo/efeitos dos fármacos , Animais , Óleo de Milho/química , Óleo de Milho/metabolismo , Dibutilftalato/administração & dosagem , Disruptores Endócrinos/administração & dosagem , Poluentes Ambientais/administração & dosagem , Poluentes Ambientais/toxicidade , Ácidos Graxos Monoinsaturados/química , Ácidos Graxos Monoinsaturados/metabolismo , Ácidos Graxos Ômega-3/química , Feminino , Desenvolvimento Fetal/efeitos dos fármacos , Óleos de Peixe/química , Óleos de Peixe/metabolismo , Masculino , Veículos Farmacêuticos/química , Plastificantes/administração & dosagem , Plastificantes/toxicidade , Gravidez , Óleo de Brassica napus , Ratos , Processos de Determinação Sexual/efeitos dos fármacos , Testículo/embriologia , Testículo/metabolismo , Testosterona/metabolismo
10.
J Appl Oral Sci ; 21(4): 327-34, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24037071

RESUMO

OBJECTIVE: The aim of this study was to evaluate the antimicrobial and fluoride releasing capacity of 3 bonding materials. MATERIAL AND METHODS: Thirty nine specimens with standardized surface smoothness and dimensions were prepared. The antimicrobial capacity of the materials against S. mutans, L. casei and C. albicans was evaluated by determining the percentage of growth inhibition of these microorganisms in an inoculated medium, obtained by optical density readouts on a spectrophotometer. The potential to interfere in microbial growth on the surface of the studied materials was observed by means of scanning electron microscopy (SEM). The fluoride release capacity in ultrapure water for 14 days was analyzed by means of ion chromatography. RESULTS: The PLUS group presented the highest percentage of microbial inhibition and the most contamination-free surface. The FUJI group presented the best fluoride release capacity. CONCLUSIONS: The TransbondTM Plus Color Change was the one that presented the best general behavior considering the evaluated aspects.


Assuntos
Anti-Infecciosos/administração & dosagem , Colagem Dentária , Materiais Dentários/química , Fluoretos/administração & dosagem , Resinas Acrílicas/química , Silicatos de Alumínio/química , Candida albicans/efeitos dos fármacos , Resinas Compostas/química , Lacticaseibacillus casei/efeitos dos fármacos , Teste de Materiais , Microscopia Eletrônica de Varredura , Veículos Farmacêuticos/química , Cimentos de Resina/química , Streptococcus mutans/efeitos dos fármacos , Propriedades de Superfície , Fatores de Tempo
11.
J. appl. oral sci ; J. appl. oral sci;21(4): 327-334, Jul-Aug/2013. tab, graf
Artigo em Inglês | LILACS | ID: lil-684561

RESUMO

OBJECTIVE: The aim of this study was to evaluate the antimicrobial and fluoride releasing capacity of 3 bonding materials. MATERIAL AND METHODS: Thirty nine specimens with standardized surface smoothness and dimensions were prepared. The antimicrobial capacity of the materials against S. mutans, L. casei and C. albicans was evaluated by determining the percentage of growth inhibition of these microorganisms in an inoculated medium, obtained by optical density readouts on a spectrophotometer. The potential to interfere in microbial growth on the surface of the studied materials was observed by means of scanning electron microscopy (SEM). The fluoride release capacity in ultrapure water for 14 days was analyzed by means of ion chromatography. RESULTS: The PLUS group presented the highest percentage of microbial inhibition and the most contamination-free surface. The FUJI group presented the best fluoride release capacity. CONCLUSIONS: The TransbondTM Plus Color Change was the one that presented the best general behavior considering the evaluated aspects. .


Assuntos
Anti-Infecciosos/administração & dosagem , Colagem Dentária , Materiais Dentários/química , Fluoretos/administração & dosagem , Resinas Acrílicas/química , Silicatos de Alumínio/química , Candida albicans/efeitos dos fármacos , Resinas Compostas/química , Lacticaseibacillus casei/efeitos dos fármacos , Teste de Materiais , Microscopia Eletrônica de Varredura , Veículos Farmacêuticos/química , Cimentos de Resina/química , Propriedades de Superfície , Streptococcus mutans/efeitos dos fármacos , Fatores de Tempo
12.
Drug Dev Ind Pharm ; 39(11): 1750-7, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23216218

RESUMO

BACKGROUND: Hydrogels are widely used for cutaneous formulations; thereby comparing the bioadhesive properties of polymers with a view to prolong the residence time of topical drugs on the skin would be very useful to design novel topical drug delivery systems. AIM: The objective of this study was to correlate data from rheological studies and texture profile analysis, with bioadhesion on the skin. METHODS: Polyacrylic acid polymers used were carbomer homopolymer type A (C971) and type B (C974), and polycarbophil (PP) dispersed in water at various concentrations (0.1, 0.5, 1.0, 1.5, 2.0, 3.0, 5.0%, w/v). Rheological, texture, and bioadhesive properties were determined to compare the hydrogels. RESULTS: Rheological analysis showed that all samples exhibited pseudoplastic behavior with thixotropy. Texture profile analysis showed that compressibility, hardness, and adhesiveness of the hydrogels were dependent on the polymer concentration, and the cohesion values were high. Bioadhesion of C974 and PP at 0.5 and 2% was of the same magnitude, while all samples of C971 had lower values. The bioadhesion of 5% C974 was the highest, while that 5% PP was lower, possibly because PP showed the greatest hardness and this rigidity may decrease the interaction of the polymer with the skin. CONCLUSION: A comprehensive comparative rheological and textural analyses of several polymers for topical systems were undertaken in terms of their bioadhesion. Therefore, it is possible to conclude that these polymers can be used for optimization of drug delivery systems on the skin.


Assuntos
Resinas Acrílicas/química , Fármacos Dermatológicos/química , Sistemas de Liberação de Medicamentos , Veículos Farmacêuticos/química , Pele/química , Acrilatos/química , Adesividade , Administração Cutânea , Animais , Fenômenos Químicos , Fármacos Dermatológicos/administração & dosagem , Orelha , Módulo de Elasticidade , Dureza , Hidrogéis , Fenômenos Mecânicos , Sus scrofa , Viscosidade
13.
Int Endod J ; 45(6): 565-70, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22720325

RESUMO

AIM: To evaluate the influence of propylene glycol (PG) on the flowability, setting time, pH and calcium ion release of mineral trioxide aggregate (MTA). METHODOLOGY: Mineral trioxide aggregate was mixed with different proportions of PG, as follows: group 1: MTA + 100% distilled water (DW); group 2: MTA + 80% DW and 20% PG; group 3: MTA + 50% DW and 50% PG; group 4: MTA + 20% DW and 80% PG; group 5: MTA + 100% PG. The ANSI/ADA No. 57 was followed for evaluating the flowability and the setting time was measured by using ASTM C266-08. For pH and calcium release analyses, 50 acrylic teeth with root-end cavities were filled with the materials (n = 10) and individually immersed in flasks containing 10 mL deionized water. After 3 h, 24 h, 72 h and 168 h, teeth were placed in new flasks and the water in which each specimen was immersed had its pH determined by a pH metre and the calcium release measured by an atomic absorption spectrophotometer with a calcium-specific hollow cathode lamp. Data were analysed by using one way anova test for global comparison and by using Tukey's test for individual comparisons. RESULTS: The highest value of flowability was observed with MTA + 20% DW and 80% PG and the lowest values were found with MTA + 100% DW. They were significantly different compared to the other groups (P < 0.05). The presence of PG did not affect the pH and calcium release. The MTA + 100% PG favoured the highest (P < 0.05) pH and calcium release after 3 h. Increasing the PG proportion interfered (P < 0.05) with the setting time; when used at the volume of 100% setting did not occur. CONCLUSION: The addition of PG to MTA-Angelus increased its setting time, improved flowability and increased the pH and calcium ion release during the initial post-mixing periods. The ratio of 80% DW­20% PG is recommended.


Assuntos
Compostos de Alumínio/química , Compostos de Cálcio/química , Óxidos/química , Veículos Farmacêuticos/química , Propilenoglicol/química , Silicatos/química , Cálcio/química , Fenômenos Químicos , Combinação de Medicamentos , Dureza , Humanos , Concentração de Íons de Hidrogênio , Eletrodos Seletivos de Íons , Teste de Materiais , Reologia , Espectrofotometria Atômica , Fatores de Tempo , Viscosidade , Água/química
14.
Dent Traumatol ; 28(4): 320-3, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22273011

RESUMO

The release and diffusion of hydroxyl ions (OH(-)) of calcium hydroxide (Ca(OH)(2))-based intracanal medications may be affected by the association with other substances. The aim of this study was to evaluate the diffusion of OH- ions through root dentin by the medications: G1, Ca(OH)(2)/saline; G2, Calen; G3, Calen/camphorated p-monochlorophenol (CMCP); and G4, Calen/0.4% chlorhexidine (CHX). Root canals from bovine teeth were prepared in a standardized manner. A cavity until dentin was prepared in the middle third of the root surface of each specimen. The external surface of the root was made impermeable using a layer of adhesive, except the prepared cavity. The root canals were filled with different medications, and teeth were individually stored in flasks containing 10 ml distilled water at 37°C. The water pH was measured at 1, 3, 7, 14, 21, 30, and 60 days. Data obtained were subjected to anova and Tukey's tests. Increase in pH was observed at 3 days for Calen/CHX and from 7 to 14 days for the other mixtures. Calen paste promoted pH increase up to 21 days. Calen/CMCP had the highest pH up to 21 days, and all groups had similar results at 30 days. At 60 days, the greatest pH values were observed for Calen/CMCP and Calen alone. All different formulations of Ca(OH)(2)-based medications tested release hydroxyl ion that can diffuse through the dentin.


Assuntos
Anti-Infecciosos/farmacologia , Hidróxido de Cálcio/farmacologia , Permeabilidade da Dentina/efeitos dos fármacos , Dentina/efeitos dos fármacos , Hidróxidos/farmacologia , Irrigantes do Canal Radicular/farmacologia , Análise de Variância , Animais , Anti-Infecciosos/uso terapêutico , Hidróxido de Cálcio/uso terapêutico , Bovinos , Difusão/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Veículos Farmacêuticos/química , Irrigantes do Canal Radicular/uso terapêutico , Raiz Dentária/efeitos dos fármacos , Raiz Dentária/metabolismo
15.
Int J Nanomedicine ; 6: 1193-200, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21822381

RESUMO

BACKGROUND: We report herein a novel strategy for the preparation of protein-based nanodelivery vehicles for hydrophobic active pharmaceutical ingredients. METHODS: The procedure consisted of three steps, ie, exposure of hydrophobic residues of a protein to a pH-induced partial unfolding: interaction between hydrophobic residues on the protein and the hydrophobic active pharmaceutical ingredient, and a final step where the structure of the protein was reversed to a native-like state by returning to neutral pH. As proof of concept, the interaction of paclitaxel with partially unfolded states of human serum albumin was evaluated as a potential method for the preparation of water-soluble complexes of the taxane with albumin. RESULTS: We found that paclitaxel readily binds to pH-induced partially unfolded albumin, leading to the formation of optically clear water-soluble complexes. The complexes thus formed were more stable in solution when the albumin native state was at least partially restored by neutralization of the solution to a pH around 7. It was also observed that the hydrodynamic radius of human serum albumin was only slightly increased after the cycle of pH changes, remaining in a monomeric state with a size according to paclitaxel binding. Furthermore, paclitaxel binding did not affect the overall exposure of charged groups of human serum albumin, as evaluated by its interaction with an ionic exchange resin. CONCLUSION: The in vitro biological activity of the complexes formed was qualitatively equivalent to that of a Cremophor(®)-based formulation.


Assuntos
Paclitaxel/administração & dosagem , Paclitaxel/química , Albumina Sérica/química , Linhagem Celular Tumoral , Cromatografia por Troca Iônica , Estabilidade de Medicamentos , Humanos , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Nanopartículas/química , Nanopartículas/ultraestrutura , Concentração Osmolar , Tamanho da Partícula , Veículos Farmacêuticos/administração & dosagem , Veículos Farmacêuticos/química , Polietilenoglicóis/química , Desdobramento de Proteína , Albumina Sérica/administração & dosagem , Solubilidade , Temperatura
16.
Int Endod J ; 43(9): 763-8, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-20546045

RESUMO

AIM: To compare the ability of two irrigant regimens to remove calcium hydroxide (CH) mixed with different vehicles from root canal walls. METHODOLOGY: The root canals of 92 freshly extracted bovine incisor teeth were prepared with a step-back technique and randomly assigned into two experimental groups (n = 40), whilst the remaining teeth (n = 12) served as positive and negative controls. In each experimental group, ten teeth were assigned to each CH preparation: G1 - CH powder; G2 - CH + saline solution; G3 - CH + polyethylene glycol (PEG); G4 - CH + PEG + camphorated paramonochlorophenol (CPMC). The negative control did not receive CH placement, and the positive control received the intracanal dressing, but no subsequent removal. After 7 days, the CH was retrieved using manual or passive ultrasonic irrigation (PUI). The roots were grooved longitudinally and split into halves. Images of each half of the canal were acquired by a digital camera, and the percentage of CH coated surface area in relation to the surface area of each third of the canal was calculated. The results were statistically analysed with anova with post hoc Tukey test with the null hypothesis set as 5%. RESULTS: Remnants of medicament were found in all experimental groups. The positive control group had complete coverage of the canal walls with CH in contrast to the negative control (P < 0.001). Considering the cervical and middle thirds, the percentage of CH retention in G1 was significantly lower using PUI (26.6% and 32.2%, respectively) than the manual (38.7% and 46.1%, respectively) technique (P < 0.05). No significant differences were observed between G2, G3 and G4 in all thirds and the experimental groups at the apical third (P > 0.05). CONCLUSIONS: Neither syringe injection nor PUI methods were efficient in removing the inter-appointment root canal medicaments. Remnants of medicament were found in all experimental groups regardless of the vehicle used.


Assuntos
Hidróxido de Cálcio/química , Cavidade Pulpar/patologia , Irrigantes do Canal Radicular/química , Preparo de Canal Radicular/métodos , Animais , Cânfora/química , Bovinos , Clorofenóis/química , Combinação de Medicamentos , Incisivo , Injeções/instrumentação , Teste de Materiais , Veículos Farmacêuticos/química , Polietilenoglicóis/química , Distribuição Aleatória , Preparo de Canal Radicular/instrumentação , Cloreto de Sódio , Propriedades de Superfície , Seringas , Irrigação Terapêutica/instrumentação , Irrigação Terapêutica/métodos , Fatores de Tempo , Ultrassom/instrumentação
17.
Braz Dent J ; 20(5): 382-8, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-20126906

RESUMO

The purpose of this in vitro study was to measure the concentration of hydrogen ions (pH) of calcium hydroxide [(Ca(OH)2] pastes combined with different vehicles over 7 periods of time. The Ca(OH)2 was manipulated with the following vehicles: i: sterile water; ii: iodoform plus sterile water; iii: local anesthetics (Lydocaine 2% with 1: 100,000 epinephrine); iv: polyethyleneglycol; v: glycerin; vi: 2.0% chlorhexidine gel; vii: camphorated paramonochlorophenol (CMCP); viii: (CMCP) + glycerin; and ix: polyethyleneglycol plus CMCP. The pastes were made on a glass plate to toothpaste consistency and the pH was measured at the following times: 5 min, 1, 24, 48 h; 7, 14 and 28 days. The data were statistically analyzed (Kruskal-Wallis at p<0.05). At 5 min, 1 and 24 h, the pH of all tested pastes ranged from 13.05 to 11.16. At 48 h and 7 days the pH of all tested pastes ranged from 11.66 to 8.92. At 14 and 28 days almost all pastes had pH means lower than 10. In conclusion, the mean pH of all tested calcium hydroxide pastes decreased with the time. Pastes made with aqueous vehicles (especially with sterile water), followed by oily vehicles (especially with CMCP + glycerin), held the highest pH means over the periods of time tested.


Assuntos
Hidróxido de Cálcio/química , Irrigantes do Canal Radicular/química , Anestésicos Locais/farmacologia , Anti-Infecciosos Locais/química , Anti-Infecciosos Locais/farmacologia , Hidróxido de Cálcio/farmacologia , Cânfora/farmacologia , Clorexidina/farmacologia , Clorofenóis/farmacologia , Combinação de Medicamentos , Glicerol/farmacologia , Concentração de Íons de Hidrogênio , Lidocaína/farmacologia , Teste de Materiais , Veículos Farmacêuticos/química , Polietilenoglicóis/farmacologia , Irrigantes do Canal Radicular/farmacologia , Reabsorção da Raiz/prevenção & controle , Fatores de Tempo , Remineralização Dentária/métodos , Viscosidade , Água
18.
Rev. clín. pesq. odontol. (Impr.) ; 4(3): 169-173, set.-dez. 2008. tab
Artigo em Português | LILACS, BBO - Odontologia | ID: lil-617355

RESUMO

OBJETIVO: O objetivo deste estudo foi avaliar o pH e difusão de íons cálcio da pasta de hidróxidode cálcio e propilenoglicol, a partir de três marcas comerciais. Foram utilizados quatro grupos, cada umcom dez dentes humanos (G1=Inodon®, G2=Biodinâmica®, G3=Farmadoctor, G4=controle).MATERIAL E MÉTODO: Os dentes foram preparados e os grupos 1, 2 e 3 preenchidos com asrespectivas pastas; o grupo controle sem pasta. A análise do pH foi feita por medidor de pH e amedição da difusão dos íons cálcio pelo método colorimétrico, com tempos de 0 e 48 horas, 7, 14, 21e 28 dias. A análise estatística foi realizada utilizando os testes ANOVA a dois critérios com medidasrepetidas, modelo fatorial completo, comparações múltiplas de Tukey HSD, teste de normalidade deKolmogorov-Smirnov, coeficiente de correlação de Pearson. O nível de significância foi de 5% com ouso do software SPSS 15.0. RESULTADOS: Os resultados mostraram que, independentemente dostempos analisados, para a média dos valores do pH houve diferença estatística entre os grupos (P<0,05),sendo que o grupo controle apresentou a menor média de pH diferindo dos outros três. Na difusão deíons cálcio observou-se diferenças significativas na média do G4 e demais grupos (p<0.05). Em 48horas a maior média ocorreu no grupo G1, em 7, 14 e 21 dias no G2 e em 28 dias no G1.CONCLUSÕES: Não houve diferença no pH dos grupos experimentais; a difusão de íons de cálciofoi maior no G1 e G2, com tendência crescente somente no G1.


OBJECTIVE: The purpose of this study was to evaluate the pH and dissemination of calciumions in the folder of calcium hydroxide and propylene from three trademarks (Inodon, Biodinâmicaand Farmadoctor). Four groups of specimens were used, each containing ten human teeth (GI –Inodon; G2 – Biodinâmica; G3 –Farmadoctor; G4 - control). The teeth were prepared and groups1, 2 and 3 satisfied with their portfolios and the control group without portfolio. pH was measuredby a pH meter and the diffusion of calcium ions was measured by the colorimetric method (0 and48 hours, 7, 14, 21 and 28 days). The statistical analysis was performed using the tests on twocriteria ANOVA with repeated measures, full factorial design, multiple comparisons of Tukey’sHSD, test of normality of Kolmogorov-Smirnov, Pearson’s correlation coefficient. The level ofsignificance was 5% with the use of the software SPSS 15.0. RESULTS: The results showedthat, regardless of time tested, for the average values of pH was no statistical difference betweenthe groups (P <0.05), while the control group had the lowest average Ph. In the disseminationof calcium ions there was significant differences in average for the G4 and other groups (P<0.05). In 48 hours at higher average occurred in the group G1, 7, 14 and 21 days in G2 and28 days in G1. CONCLUSION: There was no difference in the pH of experimental groups, thediffusion of ions of calcium was higher in G1 and G2, with only growing trend in G1.


Assuntos
Humanos , Hidróxido de Cálcio/química , Cálcio/química , Técnicas In Vitro , Análise de Variância , Concentração de Íons de Hidrogênio , Veículos Farmacêuticos/química , Propilenoglicol/química , Irrigantes do Canal Radicular/química , Fatores de Tempo
19.
Clin Exp Ophthalmol ; 36(4): 335-8, 2008 May.
Artigo em Inglês | MEDLINE | ID: mdl-18700920

RESUMO

BACKGROUND: The clinical behaviour of mycotic keratitis is aggressive, and the options for treating it are limited. This poses a need to explore new options for efficacious, low-cost treatment. Recent evidence suggests that topical itraconazole may be useful for treating this entity and that it may be possible to improve its efficacy using a suitable vehicle. METHODS: We included 12 New Zealand white (NZW) rabbits (24 eyes). The rabbits were infected with pathogenic strains of Aspergillus fumigatus and subsequently randomized to receive every 2 h for 5 weeks two different preparations of topical itraconazole 1%. In group 1 (12 eyes), ricinus oil and in group 2 (12 eyes), Systane were used as vehicle. Rabbits were evaluated every week by a masked ophthalmologist to determine the treatment response. RESULTS: The size of the ulcers was similar in the two groups at the baseline: group 1: 12.7 +/- 2.7 mm (median 12.8, range 9.8-15.5 mm); and group 2: 12.3 +/- 3.1 mm (median 12.1, range 9.8-20.8; P = 0.67). Although both groups responded well to the treatment, the response was better in the group 2, especially in weeks 2 and 3: week 1: 12.7 +/- 2.7 vs. 9.3 +/- 4.61 mm (P = 0.1); week 2: 9.4 +/- 3.4 vs. 4.1 +/- 2.9 mm (P = 0.004); week 3: 5.0 +/- 3.4 vs. 1.7 +/- 1.0 mm (P = 0.004); week 4: 1.9 +/- 1.9 vs. 1.0 +/- 1.2 mm (P = 0.1); and week 5: 0.68 +/- 1.2 vs. 0.0 +/- 0.0 mm (P = 0.3). CONCLUSION: Topical itraconazole may be useful for treating corneal ulcers caused by Aspergillus fumigatus, and its efficacy seems to be related with the vehicle solubility.


Assuntos
Antifúngicos/uso terapêutico , Aspergilose/tratamento farmacológico , Aspergillus fumigatus , Úlcera da Córnea/microbiologia , Infecções Oculares Fúngicas/tratamento farmacológico , Itraconazol/uso terapêutico , Veículos Farmacêuticos/química , Administração Tópica , Animais , Antifúngicos/administração & dosagem , Úlcera da Córnea/patologia , Itraconazol/administração & dosagem , Soluções Oftálmicas/química , Óleos de Plantas/química , Coelhos , Ricinus , Solubilidade , Resultado do Tratamento
20.
Community Dent Health ; 22(3): 180-3, 2005 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16161883

RESUMO

OBJECTIVE: This study aimed to determine free sugar concentration and pH of paediatric syrup medicines. Setting Ten paediatric syrup medicines most frequently prescribed in urban centres in Brazil were randomly chosen to be tested. OUTCOME MEASURES: Three different bottles from each type of syrup medicine were analysed (n = 30). Analysis of free sugars was performed using normal phase High-Performance Liquid Cromatography (HPLC). Quantification of free sugars was achieved by peak height comparison with standards of sucrose, fructose, glucose and sorbitol (Merck). The results were average of replicates from three bottles of each medicine. The pH of the three different bottles of each medicine was determined using a digital pHmeter (Analion - PM 600). RESULTS: Sucrose and glucose were detected in seven of the ten types of paediatric syrup medicines, with concentrations varying from 3.7 to 49.4% (w/w) (Median 32.7%) and 2.1 to 23.2% (w/w) (Median = 6.1%), respectively. Only two medicines contained fructose, and three, sorbitol, with respective medians of 12.8% (3.1-22.4%) and 24.6% (22.8-27.4%). The median of pH values was 4.9 (2.6-6.1). CONCLUSIONS: Most paediatric syrup medicines showed high concentration of free sugars and pH below the critical value (5.5), which can increase their cariogenic and erosive potentials.


Assuntos
Carboidratos/análise , Cariogênicos/análise , Preparações Farmacêuticas/química , Edulcorantes/análise , Brasil , Criança , Cromatografia Líquida de Alta Pressão , Humanos , Concentração de Íons de Hidrogênio , Veículos Farmacêuticos/química
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