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1.
Pharmaceutics ; 16(9)2024 Sep 22.
Artículo en Inglés | MEDLINE | ID: mdl-39339269

RESUMEN

Background/Objectives: This study developed and characterized hydrogels (HG-CGG) and films (F-CGG) based on cationic guar gum (CGG) for application in wound healing. Methods: HG-CGG (2% w/v) was prepared by gum thickening and evaluated for pH, stability, spreadability, and viscosity. F-CGG was obtained using an aqueous dispersion of CGG (6% w/v) and the solvent casting method. F-CGG was characterized for thickness, weight uniformity, morphology, mechanical properties, hydrophilicity, and swelling potential. Both formulations were evaluated for bioadhesive potential on intact and injured porcine skin, as well as antioxidant activity. F-CGG was further studied for biocompatibility using hemolysis and cell viability assays (L929 fibroblasts), and its wound-healing potential by the scratch assay. Results: HG-CGG showed adequate viscosity and spreadability profiles for wound coverage, but its bioadhesive strength was reduced on injured skin. In contrast, F-CGG maintained consistent bioadhesive strength regardless of skin condition (6554.14 ± 540.57 dyne/cm2 on injured skin), presenting appropriate mechanical properties (flexible, transparent, thin, and resistant) and a high swelling capacity (2032 ± 211% after 6 h). F-CGG demonstrated superior antioxidant potential compared to HG-CGG (20.50 mg/mL ABTS+ radical scavenging activity), in addition to exhibiting low hemolytic potential and no cytotoxicity to fibroblasts. F-CGG promoted the proliferation of L929 cells in vitro, supporting wound healing. Conclusions: Therefore, CGG proved to be a promising material for developing formulations with properties suitable for cutaneous use. F-CGG combines bioadhesion, antioxidant activity, biocompatibility, cell proliferation, and potential wound healing, making it promising for advanced wound treatment.

2.
J Adv Nurs ; 80(4): 1335-1354, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37908152

RESUMEN

AIM: To appraise and synthesize research investigating optimizing the administration of solid oral dosage forms (SODFs) to adults with swallowing difficulties. DESIGN: An integrative review. METHODS: An electronic search was conducted on Medical Literature Analysis and Retrieval System Online (Public Medline interface), Elsevier SciVerse Scopus and Scientific Electronic Library Online (updated February 2023). Restriction regarding the publication date was not considered for the inclusion of records. Studies addressing risks, general aspects, recommendations about patient postural adjustments, swallowing techniques, swallowing aids and aspects of concealment of SODFs were included. RESULTS: Fifty-three records published between 2002 and 2021 were included. The main administration risks were aspiration, asphyxia and solid oral dosage form-induced oral/oesophageal mucosal lesions. The most frequent general aspect reported was administering one oral dosage form at a time. The sitting position was the most patient postural adjustment mentioned. The most frequently reported solid oral dosage form swallowing technique was the lean-forward method for capsules. Solid oral dosage form swallowing aids cited: tongue and throat lubricant and solid oral dosage form coating device, swallowing cup and swallowing straw. CONCLUSION: The literature data on administering SODFs for adults with swallowing difficulties were appraised and synthesized. Some aspects, for example, not administering SODFs simultaneously, can make swallowing safer. Postural adjustments and solid oral dosage form swallowing aids are important to avoid administration risks. Swallowing SODFs can be easier if learned by techniques. Liquid and food are helpful as vehicles, and several of these have been listed. IMPLICATIONS FOR THE PROFESSION AND/OR PATIENT CARE: By optimizing the contributing factors of administering oral pharmacotherapy, the nurse can use appropriate practices to improve patient safety. Additionally, knowing and establishing the administration aspects are reasonable steps for standardizing care for patients with swallowing oral dosage form difficulties. IMPACT: This study addressed administering SODFs to adult patients with swallowing difficulties. The administration of SODFs to adult patients with swallowing difficulties can be optimized if only one oral dosage form at a time is administrated and if patient postural adjustments, swallowing techniques and swallowing aids are used. This investigation will impact the care of patients with swallowing difficulties. REPORTING METHOD: The authors declare they adhered to the relevant EQUATOR guidelines and report following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 Statement. PATIENT OR PUBLIC CONTRIBUTION: No patient or public contribution.


Asunto(s)
Administración Oral , Trastornos de Deglución , Deglución , Humanos , Cápsulas
3.
Braz. J. Pharm. Sci. (Online) ; 60: e23272, 2024. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1533988

RESUMEN

Abstract The last decade provided significant advances in the understanding of microbiota and its role in human health. Probiotics are live microorganisms with proven benefits for the host and were mostly studied in the context of gut health, but they can also confer significant benefits for oral health, mainly in the treatment of gingivitis. Postbiotics are cell-free extracts and metabolites of microorganisms which can provide additional preventive and therapeutic value for human health. This opens opportunities for new preventive or therapeutic formulations for oral administration. The microorganisms that colonize the oral cavity, their role in oral health and disease, as well as the probiotics and postbiotics which could have beneficial effects in this complex environment were discussed. The aim of this study was to review, analyse and discuss novel probiotic and postbiotic formulations intended for oral administration that could be of great preventive and therapeutic importance. A special attention has been put on the formulation of the pharmaceutical dosage forms that are expected to provide new benefits for the patients and technological advantages relevant for industry. An adequate dosage form could significantly enhance the efficiency of these products.


Asunto(s)
Salud Bucal/clasificación , Probióticos/análisis , Microbiota/inmunología , Preparaciones Farmacéuticas/administración & dosificación , Ligilactobacillus salivarius/clasificación , Boca/lesiones
4.
Curr Med Chem ; 30(12): 1351-1367, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-35796458

RESUMEN

The anti-inflammatory 5-aminosalicylic acid (5-ASA) is the main therapeutic option used to prevent and treat inflammatory bowel diseases. The upper intestinal tract performs rapid and almost complete absorption of this drug when administered orally, making local therapeutic levels of the molecule in the inflamed colonic mucosa difficult to achieve. Micro and nanoparticle systems are promising for 5-ASA incorporation because the reduced dimensions of these structures can improve the drug's pharmacodynamics and contribute to more efficient and localized therapy. Together, the association of these systems with polymers will allow the release of 5-ASA through specific targeting mechanisms to the colon, as demonstrated in the mesalazine modified-release dosage form. This review will summarize and discuss the challenges for the oral administration of 5-ASA and the different colon-specific delivery strategies using polymers.


Asunto(s)
Antiinflamatorios no Esteroideos , Mesalamina , Humanos , Mesalamina/uso terapéutico , Mesalamina/metabolismo , Antiinflamatorios no Esteroideos/uso terapéutico , Sistemas de Liberación de Medicamentos/métodos , Colon/metabolismo , Polímeros , Administración Oral
5.
Dysphagia ; 37(4): 909-922, 2022 08.
Artículo en Inglés | MEDLINE | ID: mdl-34652512

RESUMEN

Swallowing difficulties affects the deglutition of solid oral dosage forms (SODFs) and it is a common problem among neurological disorders. Interventions may improve the use of SODFs in healthcare settings. The aim of this study was to map the available research about the interventions aiming the effective and safe use of SODFs in adults with neurological disorders and swallowing difficulties and to identify potential literature gaps in this scientific field. A scoping review was carried out based on Joanna Briggs Institute guidelines and reported according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses Extension for Scoping Reviews, in PubMed, Scopus, and SciELO databases (March 2021). Peer-reviewed observational studies assessed the effectiveness and safety of SODFs in adults with neurological disorders and swallowing difficulties in the healthcare organizations setting were included. 11 studies were included (three case reports, two mixed-methods intervention studies, and six analytic studies). The frequency of women ranged from 49 to 67%, and the age from 57 to 91 years. Most studies (n = 7) included elderly patients, Parkinson (n = 6) and dementia (n = 3). Medication review was the most frequently reported intervention, 35% (9/26). In most studies, interventions were targeted to patients during hospitalization (n = 7) and performed by physicians (n = 8). At least 20 different outcomes were evaluated in the studies. Implementing specific protocols for using SODFs aimed at the swallowing difficulties of this population is not a common practice. Additional studies on interventions aimed at optimizing SODFs are needed to support the safety and efficacy of oral therapy in this patient group.


Asunto(s)
Trastornos de Deglución , Enfermedades del Sistema Nervioso , Adulto , Anciano , Anciano de 80 o más Años , Deglución , Trastornos de Deglución/epidemiología , Femenino , Humanos , Persona de Mediana Edad , Enfermedades del Sistema Nervioso/complicaciones
6.
Braz. J. Pharm. Sci. (Online) ; 58: e18630, 2022. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1364418

RESUMEN

Abstract The objective of the present investigation was to design, optimize and characterize the gastro retentive floating levofloxacin tablets and perform in-vivo evaluation using radiographic imaging. The floating tablets were prepared by using polymers i.e hydroxy propyl methyl cellulose (HPMC-K4M) and carbopol-940 individually and in combination by nonaquous granulation method. All the Formulations were evaluated for swelling index (S.I), floating behavior and in-vitro drug release kinetics. The compatibility study of levofloxacin with other polymers was investigated by FTIR, DSC, TGA and XRD. Results from FTIR and DSC revealed no chemical interaction amongst the formulation components. The optimized formulation (F11) showed floating lag time (FLT), total floating time (TFT) swelling index (S.I) of 60 sec, >16h and approximately 75 %, respectively. Moreover, F11 showed zero order levofloxacin release in simulated gastric fluid over the period of 6 h. X-ray studies showed that total buoyancy time was able to delay the gastric emptying of levofloxacin floating tablets in rabbits for more than 4 hours. In conclusion the optimized formulation (F11) can be used for the sustained delivery of levofloxacin for the treatment of peptic ulcer.


Asunto(s)
Liberación de Fármacos , Úlcera Péptica/clasificación , Comprimidos/farmacología , Rayos X/efectos adversos , Técnicas In Vitro/instrumentación , Espectroscopía Infrarroja por Transformada de Fourier , Composición de Medicamentos/instrumentación , Optimización de Procesos/análisis , Levofloxacino/análisis , Vaciamiento Gástrico/efectos de los fármacos
7.
Pharmaceutics ; 13(8)2021 Aug 19.
Artículo en Inglés | MEDLINE | ID: mdl-34452258

RESUMEN

We present a data-driven approach to unveil the pharmaceutical technologies of cyclodextrins (CDs) by analyzing a dataset of CD pharmaceutical patents. First, we implemented network science techniques to represent CD patents as a single structure and provide a framework for unsupervised detection of keywords in the patent dataset. Guided by those keywords, we further mined the dataset to examine the patenting trends according to CD-based dosage forms. CD patents formed complex networks, evidencing the supremacy of CDs for solubility enhancement and how this has triggered cutting-edge applications based on or beyond the solubility improvement. The networks exposed the significance of CDs to formulate aqueous solutions, tablets, and powders. Additionally, they highlighted the role of CDs in formulations of anti-inflammatory drugs, cancer therapies, and antiviral strategies. Text-mining showed that the trends in CDs for aqueous solutions, tablets, and powders are going upward. Gels seem to be promising, while patches and fibers are emerging. Cyclodextrins' potential in suspensions and emulsions is yet to be recognized and can become an opportunity area. This is the first unsupervised/supervised data-mining approach aimed at depicting a landscape of CDs to identify trending and emerging technologies and uncover opportunity areas in CD pharmaceutical research.

8.
Int J Pharm ; 606: 120886, 2021 Sep 05.
Artículo en Inglés | MEDLINE | ID: mdl-34298107

RESUMEN

This study investigates the use of twin-screw binder-free melt granulation (BFMG) in the development of high-dose solid dose formulations for low melting point thermally stable drugs. Both ibuprofen and guaifenesin are examined. By granulating pure API powder, it is shown that BFMG can successfully be used to produce granules that contain 100% API. A design of experiments (DoE) response surface methodology was used to establish the design space for the end-product. The effects of the most relevant process variables (barrel operating temperature, powder feed rate, screw speed and screw configuration) on granule properties (outlet temperature, size distribution, morphology, flowability, compressibility, porosity) and tablet attributes (tensile strength and in-vitro dissolution) were thoroughly studied. Barrel temperature (alone or in interactions with the other variables) represented the most significant variable for both drugs since it governs the formation of granules by partial melting and subsequent agglomeration of the fed powder. Interestingly, the shear action originated by screw speed and screw configuration resulted in various significant responses depending on the drug substance, indicating that it can also be affected by the nature of the processed molecule. Flow properties were improved (i.e., lower Hausner ratio) for both drugs after formation of granules. Tabletability was also tested by preparing 600 mg tablets for all samples. Surprisingly, the resulting granules were highly compactible, requiring only 1% lubricant to form strong tablets containing 96% API and 3% disintegrant. The results also showed that tablets become harder as the granule size increased, especially for guaifenesin. As expected, in-vitro dissolution results indicated that tablets and capsules showed slightly slower dissolution rates than the granules.


Asunto(s)
Excipientes , Tecnología Farmacéutica , Composición de Medicamentos , Tamaño de la Partícula , Polvos , Comprimidos
9.
Pharm Dev Technol ; 26(2): 119-137, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33274664

RESUMEN

The palatability of medications is an essential factor for children's adherence to drug treatment. Several methods for drug taste assessment have been developed. The aim of this review is to explore the literature reports of the main methods for the evaluation of medicines taste, named electronic tongue (e-tongue, in vitro) and human sensory panel. A systematic search was performed up to March 2020 and a total of 88 articles were selected. The e-tongue (57.5%) has been more frequently described than the sensory panel (10.3%), while some articles (32.2%) used both techniques. 74.7% of the articles mentioned 'pediatric', 'paediatric' or 'children' in the text, but only 19.5% developed formulations targeting pediatric audience and sensory testing in children is rarely seen. The e-tongue has predominance of use in the taste evaluation of pediatric medicines probably since it is fast, easy to perform and risk free, besides presenting less imprecise data and no fatigue. The human panel is more realistic, despite its intrinsic variability. In this sense, it is proposed the use of e-tongue as a fast way to select the most promising sample(s) and, after that, the sensory panel should be applied in order to confirm the taste masking.


Asunto(s)
Nariz Electrónica , Preparaciones Farmacéuticas/administración & dosificación , Percepción del Gusto , Niño , Humanos , Preparaciones Farmacéuticas/química , Gusto , Lengua
10.
Pharm Dev Technol ; 25(10): 1188-1191, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32746682

RESUMEN

The pediatric adherence to antiretroviral therapy is critical to therapeutic success. Ritonavir, a protease inhibitor drug, is commercially available as an oral solution containing a high amount of ethanol and propylene glycol, contraindicated in children younger than 4 years. Moreover, this medicine presents a bitter taste, which is limiting for the adherence to treatment. This study aims to develop ritonavir nanoparticles followed by polymeric coating for sensory characteristics improvement. The nanoparticles were coated with Eudragit® L 100-55 and characterized. A human sensory panel evaluated the proposed formulations regarding its bitter taste. The formulation showed nanotechnological features, with 130 and 134 nm for ritonavir nanoparticles and ritonavir coated nanoparticles, respectively. The pH, zeta potential, drug content and encapsulation efficiency results were suitable for oral administration. The coated nanoparticles were capable of decreasing the drug bitter taste as shown in the sensory analysis. The ritonavir incorporation in nanoparticles, followed by polymer coating can be a reasonable strategy to obtain alcohol free taste-masked medicines, which are promising for pediatric therapy.


Asunto(s)
Inhibidores de la Proteasa del VIH/administración & dosificación , Nanopartículas , Ritonavir/administración & dosificación , Gusto , Resinas Acrílicas/química , Administración Oral , Adulto , Química Farmacéutica , Preescolar , Portadores de Fármacos/química , Inhibidores de la Proteasa del VIH/química , Humanos , Concentración de Iones de Hidrógeno , Tamaño de la Partícula , Ritonavir/química , Suspensiones , Adulto Joven
11.
Pharm Dev Technol ; 25(7): 892-898, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32321344

RESUMEN

Praziquantel (PZQ), a broad spectrum anthelmintic drug, cannot be found in acceptable dosage forms for elderly patients, paediatric patients, and for veterinary use. In fact, very little has been done up to now in the formulation of liquid dosage forms, being they always formulated for parenteral administration. To beat this important challenge, it was accomplished a comprehensive analysis of the influence of two elementary physicochemical aspects, i.e. surface thermodynamic and electrokinetic properties, on the colloidal stability of PZQ nanosuspensions. The hydrophobic character of the drug, intensely determining the flocculation curves, was confirmed by the thermodynamic characterization. The electrophoretic characterization, in combination with the sedimentation and relative absorbance versus time curves, highlighted that the electrical double layer thickness and the surface charge can play an essential role in the stability of the pharmaceutical colloid. Finally, it was demonstrated that controlling the pH values and the incorporation of electrolytes can help in formulating PZQ aqueous nanosuspensions with appropriate stability and redispersibility behaviours for pharmaceutical use.


Asunto(s)
Antihelmínticos/síntesis química , Composición de Medicamentos/métodos , Nanosferas/química , Praziquantel/síntesis química , Antihelmínticos/farmacocinética , Química Farmacéutica/métodos , Electrólitos/síntesis química , Electrólitos/farmacocinética , Concentración de Iones de Hidrógeno , Interacciones Hidrofóbicas e Hidrofílicas , Nanosferas/metabolismo , Praziquantel/farmacocinética , Agua/química , Agua/metabolismo
12.
Curr Drug Deliv ; 17(4): 348-360, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32183668

RESUMEN

BACKGROUND: Orodispersible Tablets (ODTs) are an option to facilitate the intake of pharmaceutical solid dosage forms, which dissolve in the mouth within 30 seconds releasing the drug immediately with no need for water intake or chewing. OBJECTIVE: The main goal of our study is the technological development of lactose-free orodispersible tablets that contain ketoprofen. METHODS: We assessed different variables during the pharmaceutical development of ODTs: compression techniques conducted after a wet granulation process, aiming to optimize the flow properties of the formulation, and a suspension freeze-drying molded in blisters. We developed three formulations for each method, each containing one of the superdisintegrants: croscarmellose, crospovidone, or starch glycolate. RESULTS: During the production of ODTs, we performed quality control of the granulation process, since the production of pellets contributed to the enhancement of the disintegration time and content homogeneity. Quality control tests for ODTs produced by freeze-drying were also satisfactory, despite significant changes in the final physical aspect of these products when compared to that of ODTs produced by compression. In addition, the disintegration times of ODTs produced by freeze-drying were substantially higher. Furthermore, these tablets displayed greater friability and pose a challenge to the control of a standard individual weight. CONCLUSION: Among the superdisintegrants, croscarmellose contributed most significantly to reduce the disintegration time and to dissolve KTP effectively in 20 minutes.


Asunto(s)
Desarrollo de Medicamentos , Cetoprofeno/síntesis química , Administración Oral , Composición de Medicamentos , Humanos , Cetoprofeno/administración & dosificación , Cetoprofeno/química , Tamaño de la Partícula , Control de Calidad , Solubilidad , Propiedades de Superficie , Comprimidos , Factores de Tiempo
13.
Eur J Pharm Sci ; 142: 105081, 2020 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-31669384

RESUMEN

Bromopride is a prokinetic and antiemetic drug used to treat nausea and vomiting. Although its prescription is common in Brazil, there is a lack of studies about bromopride pharmacokinetics. Therefore, the aims of this study were to investigate the population pharmacokinetics of bromopride and to evaluate the influence of covariates on its absorption. This study is a retrospective analysis of data collected from bioequivalence studies. The data was modeled using MONOLIX 2018R2. Assuming one-compartment and linear elimination, the absorption phase was evaluated with different structural models. The model of sequential first- and zero-order with combined error and exponential inter-individual variability in all parameters best described the atypical absorption profile of bromopride. Population estimates were first-order absorption rate (ka) of 0.08 h - 1, fraction of dose absorbed by first-order (Fr) of 32.60%, duration of the zero-order absorption (Tk0) of 0.88 h with latency time (Tlag) of 0.47 h, volume of distribution of 230 l and clearance of 46.80 l h - 1. Bodyweight affects Tk0, dosage form was found to correlate with Tk0 and Tlag, while gender affects Tlag. However, simulations evaluating the clinical importance of these covariates on steady-state indicated minimal changes on bromopride exposure. The mixed absorption model was reasonable to describe the absorption process of bromopride because it had the flexibility to fit multiple-peaks profile and shows good agreement with physicochemical properties of drug.


Asunto(s)
Antieméticos/farmacocinética , Absorción Gastrointestinal/fisiología , Metoclopramida/análogos & derivados , Administración Oral , Adulto , Disponibilidad Biológica , Brasil , Femenino , Humanos , Cinética , Masculino , Metoclopramida/farmacocinética , Estudios Retrospectivos
14.
Einstein (São Paulo, Online) ; 18: eAO5023, 2020. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1056064

RESUMEN

ABSTRACT Objective To adapt an antibiotic dose adjustment software initially developed in English, to Portuguese and to the Brazilian context. Methods This was an observational, descriptive study in which the Delphi method was used to establish consensus among specialists from different health areas, with questions addressing the visual and operational aspects of the software. In a second stage, a pilot experimental study was performed with the random comparison of patients for evaluation and adaptation of the software in the real environment of an intensive care unit, where it was compared between patients who used the standardized dose of piperacillin/tazobactam, and those who used an individualized dose adjusted through the software Individually Designed and Optimized Dosing Strategies. Results Twelve professionals participated in the first round, whose suggestions were forwarded to the software developer for adjustments, and subsequently submitted to the second round. Eight specialists participated in the second round. Indexes of 80% and 90% of concordance were obtained between the judges, characterizing uniformity in the suggestions. Thus, there was modification in the layout of the software for linguistic and cultural adequacy, minimizing errors of understanding and contradictions. In the second stage, 21 patients were included, and there were no differences between doses of piperacillin in the standard dose and adjusted dose Groups. Conclusion The adapted version of the software is safe and reliable for its use in Brazil.


RESUMO Objetivo Adaptar um software de ajuste de dose de antibióticos inicialmente elaborado em língua inglesa para o português e a conjuntura brasileira. Métodos Trata-se de estudo observacional, descritivo, em que foi utilizado o método Delphi para estabelecer consenso entre especialistas de diferentes áreas da saúde, com perguntas que abordaram os aspectos visuais e operacionais do software. Em uma segunda etapa, foi realizado um estudo piloto, experimental, com alocação aleatória dos pacientes, para avaliação e adaptação do software em ambiente real de uma unidade de tratamento intensivo, onde foram comparadas diferenças entre pacientes que utilizaram dose padronizada usual de piperacilina/tazobactam, e os que utilizaram a dose individualizada ajustada por meio do software Individually Designed Optimum Dosing Strategies. Resultados Participaram da primeira rodada 12 profissionais cujas sugestões foram encaminhadas ao desenvolvedor do software para adequação e ajustes, e posteriormente submetidas à segunda rodada. Oito especialistas participaram da segunda rodada. Foram obtidos índices de 80% e 90% de concordância entre os juízes, caracterizando uniformidade nas sugestões. Dessa forma, houve modificação no layout do software para adequação linguística e cultural, minimizando erros de entendimento e contradições. Na segunda etapa, foram incluídos 21 pacientes, e não houve diferenças entre doses de piperacilina nos grupos dose padronizada e dose ajustada. Conclusão A versão adaptada do software é segura e confiável para seu uso no Brasil.


Asunto(s)
Humanos , Masculino , Femenino , Anciano , Anciano de 80 o más Años , Piperacilina/administración & dosificación , Diseño de Software , Tazobactam/administración & dosificación , Lingüística/normas , Antiinfecciosos/administración & dosificación , Estándares de Referencia , Brasil , Antropometría , Comparación Transcultural , Encuestas y Cuestionarios , Reproducibilidad de los Resultados , Técnica Delphi , Estadísticas no Paramétricas , Unidades de Cuidados Intensivos , Persona de Mediana Edad
15.
AAPS PharmSciTech ; 21(1): 9, 2019 Dec 03.
Artículo en Inglés | MEDLINE | ID: mdl-31797083

RESUMEN

Increased human-pet interactions have led to concerns related to the prevention and treatment of ectoparasite infestations. Fipronil (FIP) is a widely used ectoparasiticide in veterinary medicine available for topical administration; however, its use may cause damage to the owners and the environment. The aim of the study was to develop immediate-release tablets of FIP, as well as to determine its pharmacokinetic properties after oral administration in beagle dogs. The prepared FIP tablets were evaluated for pre-compression (angle of repose, speed flow, and Carr's index) and post-compression (weight variation, friability, thickness, hardness, disintegration time, and dissolution rate) parameters. Orally administered FIP at a dose of 2 mg/kg was rapidly absorbed with Cmáx of 3.13 ± 1.39 µg/mL at 1.83 ± 0.40 h post treatment (P.T.) and metabolized with 1.27 ± 1.04 µg/mL at 2.33 ± 0.82 h P.T. for fipronil sulfone (SULF) (the primary metabolite). The elimination of FIP and SULF occurred slowly and had maintained quantifiable plasma levels in the blood for up to 28 days P.T. The goal of the study is aligned with the concept of One Health, which aims to collaboratively achieve the best health for people, animals, and the environment. Therefore, the use of FIP tablets for the control of ectoparasites in dogs may be a safer alternative for owners and the environment.


Asunto(s)
Antiparasitarios/química , Antiparasitarios/farmacocinética , Pirazoles/química , Pirazoles/farmacocinética , Administración Oral , Animales , Antiparasitarios/administración & dosificación , Perros , Dureza , Pirazoles/administración & dosificación , Comprimidos , Contaminación del Agua/prevención & control
16.
Arch Pediatr ; 26(7): 431-436, 2019 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31611144

RESUMEN

Taste is a crucial factor that determines the palatability of the oral dosage form and patient compliance. OBJECTIVE: The aim of this work was to evaluate the organoleptic excipients in oral antibiotics for pediatric use marketed in Brazil. METHODS: The information was obtained from the GuidetoPharmacy, a reference for the pharmaceutical trade. The analysis included dosage forms for oral administration and drugs and their combination with antibacterial action. After this survey, we identified the constitution of the flavoring, sweetening, and coloring agents of each medicine. The results are presented in a descriptive form. RESULTS: Twelve drugs or associations are distributed in 70medicines. Oral suspension was the most common pharmaceutical dosage form. Sweeteners were sucrose, sodium saccharin, and sodium cyclamate. All the coloring agents observed are synthetic and the most frequent ones were yellow twilight no. 6, yellow tartrazine no. 5, and red ponceau 4R. The presence of two or more types of flavorings per medicine was observed. CONCLUSION: Antibacterials use coloring agents, flavorings, and sweeteners to facilitate the administration of medicines for children, using up to six different substances per formulation. No natural coloring agent was observed, demonstrating an issue to be explored in the future. It is important to note that, although necessary, these excipients are responsible for a high incidence of allergic reactions in children.


Asunto(s)
Antibacterianos/química , Colorantes , Excipientes , Aromatizantes , Edulcorantes , Administración Oral , Antibacterianos/administración & dosificación , Brasil , Niño , Humanos , Pediatría
17.
J Pharm Anal ; 9(1): 40-48, 2019 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-30740256

RESUMEN

Tioconazole (TCZ), a broad-spectrum antifungal agent, has significant activity against Candida albicans and other Candida species, and therefore, it is indicated for the topical treatment of superficial mycoses. The main goal of this work is to report an exhaustive identification and characterization procedure to improve and facilitate the online quality control and continuous process monitoring of TCZ in bulk material and loaded in two different dosage forms: ovules and nail lacquer. The methodologies were based on thermal (differential scanning calorimetry (DSC), melting point, and thermogravimetry (TG)), spectroscopic (ultraviolet (UV), Raman, near infrared (NIR), infrared spectroscopy coupled to attenuated total reflectance (FTIR-ATR), and nuclear magnetic resonance (NMR)), microscopic and X-ray diffraction (XRD). The TCZ bulk powder showed a high crystallinity, as observed by XRD, with a particles size distribution (3-95 µm) resolved by microscopic measurements. TCZ melting point (82.8 °C) and a degradation peak centered at 297.8 °C were obtained by DSC and DTG, respectively. An unambiguous structure elucidation of TCZ was obtained by mono- and two- dimensional 1H and 13C NMR spectral data analysis. The FTIR-ATR, Raman and NIR spectra of both the raw material and the commercial products were analyzed and their characteristic bands were tabulated. The best methods for TCZ identification in ovules were DSC, TG, XRD, NIR and Raman, while NIR and FTIR-ATR were the most appropriate techniques to analyze it in the nail lacquer. DSC, TG, DRX, Raman, FTIR-ATR and NIR spectroscopy are effective techniques to be used in online process analysis, because they do not require sample preparation, and they are considerably sensitive to analyze complex samples.

18.
Braz. J. Pharm. Sci. (Online) ; 55: e18129, 2019. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1039036

RESUMEN

A simple, sensitive, precise, accurate and robust high performance liquid chromatographic method has been developed for simultaneous estimation of saxagliptin (SAXA) and dapagliflozin (DAPA) in pharmaceutical formulation. Design of experiments (DoE) was applied for multivariate optimization of the experimental conditions of RP-HPLC method. Risk assessment was performed to identify the critical method parameters. Three independent factors; mobile phase composition, flow rate and column temperature were used to design mathematical models. Central composite design (CCD) was used to study the response surface methodology and to study in depth the effects of these independent factors. Desirability function was used to simultaneously optimize the retention time and resolution of SAXA and DAPA. The optimized and predicted data from contour diagram consisted of acetonitrile and ortho phosphoric acid (0.1%) in the ratio of 50:50 respectively, at a flow rate of 0.98 ml/min and column temperature 31.4 °C. Using these optimum conditions baseline separation of both drugs with good resolution and run time of less than 6 min were achieved. The optimized assay conditions were validated according to ICH guidelines. Hence, the results clearly showed that Quality by design approach could be successfully applied to optimize RP-HPLC method for simultaneous estimation of SAXA and DAPA.


Asunto(s)
Preparaciones Farmacéuticas/clasificación , Cromatografía Líquida de Alta Presión/métodos , Diabetes Mellitus Tipo 2/clasificación , Comprimidos/administración & dosificación , Formas de Dosificación , Optimización de Procesos/métodos
19.
Braz. J. Pharm. Sci. (Online) ; 55: e18015, 2019. tab, graf
Artículo en Inglés | LILACS-Express | LILACS | ID: biblio-1055313

RESUMEN

Currently, medications used in children are typically modified from pharmaceutical dosage forms designed for adults. Captopril is widely adapted to liquid formulations for use in hospitals. Its stability in the aqueous medium is reduced since it undergoes oxidation producing captopril disulfide (its main metabolite). The aim of this formulation study was to suggest favorable conditions for the development of a stable captopril formulation. The compatibility between the drug and excipients was evaluated by differential scanning calorimetry analysis (DSC). For studies in solution, different formulations were prepared according to a factorial design varying EDTA concentration, water purity and pH. The resultant formulations were stored at 60°C and analyzed over a twelve-day period using HPLC. The DSC curves obtained suggested, although not conclusive to elucidation, interactions of captopril with citric acid and sucralose. The stability study of these solutions revealed that the variables significantly influenced captopril content, which degraded at zero order kinetics and rates differing by a factor of up to 7 times, where pH proved the most influential factor. Interactions between variables were observed. Therefore, development of a stable captopril formulation is feasible provided EDTA and a buffering agent is used at suitable concentrations (0.08% and pH 3.85).

20.
Iatreia ; Iatreia;31(4): 412-418, oct.-dic. 2018. tab, graf
Artículo en Español | LILACS | ID: biblio-975492

RESUMEN

RESUMEN Ante la alta resistencia a los antibióticos por infecciones bacterianas multirresistentes a nivel intrahospitalario, se debe pensar en alternativas terapéuticas que requieren el uso de antibióticos potentes y dosis mayores. Presentamos el caso de un paciente de 56 años con múltiples intervenciones quirúrgicas quien había recibido manejo antibiótico previo. Al presentar deterioro clínico se aísla en hemocultivos Pseudomonas aeruginosa resistente a carbapenémicos, se inicia manejo con colistina intravenosa y doripenem, con el posterior desarrollo de una falla renal que se revierte al disminuir la dosis de colistina. Finalmente el paciente culmina el tratamiento con un ajuste de antibiótico de 10 días, con la respuesta clínica favorable.


SUMMARY Given the high resistance to antibiotics due to multiresistant bacterial infections at the hospital level, therapeutic alternatives that require the use of more potent antibiotics and higher doses should be considered. We presented the case of a 56-year-old patient with multiple surgeries and several previous antibiotic treatments. After clinical deterioration, a blood culture yield Pseudomonas aeruginosa resistant to carbapenems, treated with intravenous colistin and doripenem. The patient then developed acute renal failure, which reverts when the colistin dose decreases. Finally, the patient finishes the treatment with 10-day antibiotic adjustment and favorable clinical response.


Asunto(s)
Humanos , Colistina , Dosificación
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