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1.
Arq. ciências saúde UNIPAR ; 26(3): 643-656, set-dez. 2022.
Article in Portuguese | LILACS | ID: biblio-1399314

ABSTRACT

O Diabetes Mellitus (DM) é uma doença crônica, que tem elevada prevalência na sociedade e representa um problema de saúde pública devido à natureza de suas complicações, acredita-se que a dificuldade na manutenção do tratamento, pode estar relacionada a deficiência ou falta de adesão. O estudo teve como objetivo relatar à adesão ao tratamento do Diabetes Mellitus na Atenção Primária a Saúde. Trata-se de um estudo descritivo, com abordagem qualitativa, realizado com 30 pacientes diabéticos de uma Unidade de Atenção Primária à Saúde de Guaiúba-CE, no período de agosto a outubro de 2021. A coleta de dados deu-se por entrevista semiestruturada utilizando questões norteadoras sobre adesão ao tratamento, adoção de práticas promotoras de saúde e posteriormente sujeita a análise de conteúdo. Observou-se que a adesão ao tratamento do diabetes envolve inúmeros desafios, relacionados principalmente ao usuário e sistemas de saúde/profissionais. Os maiores desafios encontrados foram em relação a supervalorização do tratamento medicamentoso frente a adoção de hábitos saudáveis e de ações promotoras de autocuidado. Nesse cenário, nota-se a importância de conhecer os fatores que influenciam na adesão ao tratamento com o intuito de se lançar estratégias para aperfeiçoar o planejamento de ações e intervenções a esses pacientes.


Diabetes Mellitus (DM) is a chronic disease that is highly prevalent in society and represents a public health problem due to the nature of its complications. The study aimed to report on the adherence to treatment of Diabetes Mellitus in Primary Health Care. This is a descriptive study, with a qualitative approach, conducted with 30 diabetic patients from a Primary Health Care Unit in Guaiúba-CE, in the period from August to October 2021. Data were collected through semi-structured interviews using guiding questions about adherence to treatment, adoption of health-promoting practices and later subjected to content analysis. It was observed that diabetes treatment adherence involves numerous challenges, mainly related to the user and health systems/professionals. The biggest challenges found were related to the overvaluation of drug treatment against the adoption of healthy habits and self-care promoting actions. In this scenario, it is important to know the factors that influence treatment adherence in order to develop strategies to improve the planning of actions and interventions for these patients.


La diabetes mellitus (DM) es una enfermedad crónica, que tiene una alta prevalencia en la sociedad y representa un problema de salud pública debido a la naturaleza de sus complicaciones, se cree que la dificultad para mantener el tratamiento puede estar relacionada con la deficiencia o falta de adherencia. El estudio tenía como objetivo informar sobre la adherencia al tratamiento de la Diabetes Mellitus en Atención Primaria. Se trata de un estudio descriptivo con enfoque cualitativo, realizado con 30 pacientes diabéticos de una Unidad de Atención Primaria de Salud de Guaiúba-CE, en el período de agosto a octubre de 2021. La recogida de datos se llevó a cabo mediante entrevistas semiestructuradas en las que se utilizaron preguntas orientativas sobre la adherencia al tratamiento y la adopción de prácticas de promoción de la salud, y posteriormente se sometieron a un análisis de contenido. Se ha observado que el acceso al tratamiento de la diabetes conlleva numerosos desafíos, relacionados principalmente con el usuario y los sistemas de salud/profesionales. Los mayores retos encontrados estaban relacionados con la sobrevaloración del tratamiento farmacológico frente a la adopción de hábitos saludables y acciones de promoción del autocuidado. En este escenario, se constata la importancia de conocer los factores que influyen en la adherencia al tratamiento para poner en marcha estrategias que mejoren la planificación de las acciones e intervenciones para estos pacientes.


Subject(s)
Male , Female , Adult , Middle Aged , Aged , Aged, 80 and over , Patients , Primary Health Care/organization & administration , Diabetes Mellitus/drug therapy , Treatment Adherence and Compliance , Self Care/instrumentation , Unified Health System , Pharmaceutical Preparations/analysis , Exercise/physiology , Public Health , Chronic Disease/drug therapy , Diabetes Mellitus/diagnosis , Drug Therapy , Diet, Healthy , Health Promotion , Health Services Accessibility , Nursing Care/methods
2.
Arq. ciências saúde UNIPAR ; 26(3): 681-692, set-dez. 2022.
Article in Portuguese | LILACS | ID: biblio-1399322

ABSTRACT

Com o avanço da medicina e o aumento do uso de antimicrobianos, a resistência microbiana vem se tornando um problema sério na saúde pública. Para que uma bactéria se torne resistente, são necessários vários fatores, entre eles, o uso indiscriminado e prolongado de antimicrobianos e as resistências intrínsecas e adquiridas. Nesse contexto, o objetivo do trabalho foi explorar os mecanismos de ação dos antimicrobianos, de resistência e a sua importância na saúde pública. Foram utilizadas para a presente pesquisa, as bases de dados Pubmed, Google acadêmico e Scielo. Segundo a Organização Mundial da Saúde define-se resistência ao antibiótico quando o mesmo não produz mais efeito. A inserção cada vez mais frequente de antimicrobianos favorece a resistência, onde provocam uma pressão seletiva sobre os microrganismos, tornando-os resistentes a diversas drogas. O uso indiscriminado de antimicrobianos é o principal fator de resistência microbiana, assim como o uso de antimicrobianos sem exame de cultura e teste de sensibilidade. Neste sentido, conclui-se que é de suma importância a atualização de protocolos que contenham os mecanismos de resistência bacteriana a fim de minimizar o uso indiscriminado de antimicrobianos, assim como capacitar os profissionais da saúde para este problema na saúde pública.


With the advance of medicine and the increase in the use of antimicrobials, microbial resistance has become a serious problem in public health. For a bacterium to become resistant, several factors are necessary, among them, the indiscriminate and prolonged use of antimicrobials and the intrinsic and acquired resistance. In this context, the objective of the work was to explore the mechanisms of action of antimicrobials, resistance and their importance in public health. Pubmed, Google academic and Scielo databases were used for this research. According to the World Health Organization, resistance to antibiotics is defined when it no longer has an effect. The increasingly frequent insertion of antimicrobials favors resistance, where they put selective pressure on microorganisms, making them resistant to various drugs. The indiscriminate use of antimicrobials is the main factor of microbial resistance, as well as the use of antimicrobials without culture examination and sensitivity test. In this sense, it is concluded that it is extremely important to update protocols that contain the mechanisms of bacterial resistance in order to minimize the indiscriminate use of antimicrobials, as well as to train health professionals for this problem in public health.


Con los avances de la medicina y el mayor uso de antimicrobianos, la resistencia microbiana se ha convertido en un grave problema de salud pública. Para que una bacteria se vuelva resistente son necesarios varios factores, entre ellos, el uso indiscriminado y prolongado de antimicrobianos y la resistencia intrínseca y adquirida. En este contexto, el objetivo de este trabajo fue explorar los mecanismos de acción de los antimicrobianos, la resistencia y su importancia en la salud pública. Para esta investigación se utilizaron las bases de datos Pubmed, Google Scholar y Scielo. Según la Organización Mundial de la Salud, la resistencia a un antibiótico se define cuando deja de producir efecto. El uso cada vez más frecuente de antimicrobianos favorece la resistencia, ya que provocan una presión selectiva sobre los microorganismos, haciéndolos resistentes a varios fármacos. El uso indiscriminado de antimicrobianos es el principal factor de resistencia microbiana, así como el uso de antimicrobianos sin pruebas de cultivo y sensibilidad. En este sentido, se concluye que es de suma importancia actualizar los protocolos que contienen los mecanismos de resistencia bacteriana para minimizar el uso indiscriminado de antimicrobianos, así como capacitar a los profesionales de la salud para este problema en la salud pública.


Subject(s)
Public Health , Drug Resistance, Bacterial/drug effects , Bacteria/drug effects , Drug Resistance/drug effects , Drug Resistance, Microbial/drug effects , Pharmaceutical Preparations/analysis , Cell Wall/drug effects , Review , Biofilms/drug effects , Libraries, Digital , Anti-Infective Agents/analysis , Anti-Bacterial Agents/pharmacology
3.
São Paulo; s.n; s.n; 2022. 270 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-1379116

ABSTRACT

A leishmaniose é uma zoonose de ampla distribuição mundial, causada pelos parasitas tripanossomatídeos do gênero Leishmania. Infelizmente, o arsenal terapêutico disponível é precário, mas vê-se crescente o interesse científico pela busca do potencial de derivados nitroheterocíclicos como alternativas terapêuticas. Nesse contexto, este trabalho analisou o potencial de derivados 5-nitro-2-furfurilidênicos contra diferentes cepas de Leishmania, assim como investigou um possível modo de ação para esta classe de nitrocompostos. Para tal, a quimioteca foi sintetizada de acordo com publicações prévias do grupo. O potencial de inibição de crescimento das culturas de promastigotas de L. (L.) infantum (Linf) e L. (L.) major (Lmaj) foi determinado, utilizando miltefosina (MILT) (Linf - IC50: 8,28±0,33 µM), anfotericina B (AMB) (Linf - IC50: 0,02±0,002 µM) e nifurtimox (NFX) (Lmaj - IC50: 3,5±0,09 µM) como referência. A maioria dos compostos apresentaram maior potencial que as referênias, destacando o composto 40 (Linf - IC50: 0,2±0,019 µM/ Lmaj - IC50: 0,087 ± 0,001 µM) como mais eficaz. Contra as formas amastigotas intracelulares, para Linf os compostos 40, 13 e 15 foram mais eficazes em reduzir a carga parasitária dos macrófagos infectados que fármacos de referência. Para Lmajor, o composto 40 (IC50: 0,006 ± 0,0003 µM) foi mais ativo que o NFX (IC50: 2,15 ± 0,01 µM). Também foi determinada a atividade da quimioteca frente a enzima nitrorredutase (NTR1), utilizando cepas de T. brucei superexpressantes de NTR1, e os compostos analisados foram até 18 vezes mais eficazes que à cepa wild-type. Ademais, a partir da análise exploratória de dados por análise de componentes principais (PCA) e de grupamentos hierárquicos (HCA), foi reconhecida a influência das propriedades relacionadas com o equilíbrio hidrófilo-lipófilo e da natureza estérica/geométrica das moléculas para atividade anti-Leishmania


Leishmaniasis is a worldwide zoonosis caused by trypanosomatid parasites of the genus Leishmania. Unfortunately, the available therapeutic arsenal is precarious, but there is growing scientific interest in searching the potential of nitroheterocyclic derivatives as therapeutic alternatives. In this context, this work analyzed the potential of 5-nitro-2-furfurylidene derivatives against different Leishmania strains, as well as investigated the potential mode of action for this nitro compounds class. To this end, the chemolibrary was synthesized according to our group's previous publications. The growth inhibitory potential potential for promastigote cultures of L. (L.) infantum (Linf) and L. (L.) major (Lmaj) was determined using miltefosine (MILT) (Linf - IC50: 8.28±0.33 µM), amphotericin B (AMB) (Linf - IC50: 0.02±0.002 µM) and nifurtimox (NFX) (Lmaj - IC50: 3.5±0.09 µM) as reference. Most of the compounds were more potent than the references, highlighting compound 40 (Linf - IC50: 0.2±0.019 µM/ Lmaj - IC50: 0.087 ± 0.001 µM) as the most effective. Against intracellular amastigote, for Linf, compounds 40, 13 and 15 were more effective in reducing the parasite load of infected macrophages than reference drugs. For Lmajor, compound 40 (IC50: 0.006 ± 0.0003 µM) was more active than NFX (IC50: 2.15 ± 0.01 µM). The activity against nitroreductase (NTR1) enzyme was determined using overexpressing NTR1 mutant T. brucei strains, and the analyzed compounds were up to 18 times more effective than wild-type. Furthermore, exploratory data analysis using principal component analysis (PCA) and hierarchical clustering (HCA) methods were used. The influence of properties related to the hydrophiliclipophilic balance and the steric/geometric nature of the molecules was associated with the anti-Leishmanial activity


Subject(s)
Complementary Therapies/instrumentation , Leishmaniasis/pathology , Principal Component Analysis/classification , Leishmania/metabolism , Nitroreductases/analysis , Pharmaceutical Preparations/analysis , Data Analysis , Nitro Compounds/agonists
4.
São Paulo; s.n; s.n; 2022. 79 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-1380631

ABSTRACT

A contaminação microbiana pode comprometer a eficácia e a segurança dos produtos farmacêuticos. Os testes de contagem microbiana são utilizados para avaliar a qualidade microbiológica de produtos farmacêuticos não estéreis, exigidos pela maioria dos compêndios farmacopeicos. Apesar disso, raramente é considerada a avaliação da incerteza de medição para testes de contagem microbiana, o que pode levar a falsas decisões quanto à conformidade/nãoconformidade. Neste trabalho avaliamos os efeitos de matriz nos testes de contagem microbiana e sua avaliação de incerteza top-down, e avaliamos a incerteza da medição utilizando a abordagem bottom-up, além de que estimamos os riscos do consumidor ou do produtor devido à incerteza da medição. As incertezas combinada e expandida são calculadas empregando-se a abordagem topdown consideraram a exatidão (recuperação) e a precisão como os principais componentes de incerteza. O componente de incerteza da exatidão foi o mais relevante em 59% das amostras estudadas, enquanto a precisão foi a principal fonte de incerteza em apenas 41% das amostras, sendo observado que quanto maior a interferência da matriz, maior o fator de incerteza e, consequentemente, maior a assimetria para o intervalo em torno da medida. A partir da abordagem bottom-up, foram identificadas e quantificadas três principais fontes de incerteza: fator de diluição, volume plaqueado e contagem das placas. A contribuição dessas fontes de incerteza depende do valor medido da carga microbiana em produtos farmacêuticos, a contribuição do fator de diluição e das incertezas do volume plaqueado aumentam com o aumento do valor medido, enquanto a contribuição da contagem das placas diminui com o aumento do valor medido. Foi possível avaliar o risco de decisões falsas devido à incerteza de medição, por meio das estimativas dos riscos do consumidor ou do produtor. Os riscos foram avaliados utilizando-se o método Monte Carlo. Portanto, foi demonstrado a relevância da avaliação da incerteza de medição para garantir a confiabilidade dos resultados dos testes de contagem microbiana e a apoiar a tomada de decisões quando a avaliação da conformidade/não-conformidade dos produtos farmacêuticos não estéreis


Microbial contamination can compromise the efficacy and safety of pharmaceutical products. Microbial counting tests are used to assess the microbiological quality of non-sterile pharmaceutical products required by most pharmacopoeia compendiums. Despite this, measurement uncertainty assessment for microbial count tests is rarely considered, which can lead to false compliance/non-compliance decisions. In this work we evaluated the matrix effects on microbial counting tests and their top-down uncertainty assessment, and evaluated measurement uncertainty using the bottom-up approach, inaddition to estimating the consumer's or producer's risks due to measurement uncertainty. The combined and expanded uncertainties calculated using the top-down approach considered accuracy (recovery) and accuracy as the main components of uncertainty. The uncertainty component of accuracy was the most relevant in 59% of the samples studied, while accuracy was the main source of uncertainty in only 41% of the samples, being observed that the greater the interference of the matrix, the greater the uncertainty factor and, consequently, the greater the asymmetry for the interval around the measurement. From the bottom-up approach, three main sources of uncertainty were identified and quantified: dilution factor, platelet volume and plaque count. The contribution of these sources of uncertainty depends on the measured value of microbial load in pharmaceutical products, the contribution of the dilution factor and uncertainties of the plated volume increase with the increase in the measured value, while the contribution of plate counting decreases with the increase of the measured value. It was possible to assess the risk of false decisions due to measurement uncertainty by estimating consumer or producer risks. The risks were evaluated using the Monte Carlo method. Therefore, the relevance of measuring uncertainty assessment has been demonstrated to ensure the reliability of microbial count test results and to support decision-making when assessing non-sterile pharmaceutical conformity/non-compliance


Subject(s)
Pharmaceutical Preparations/analysis , Efficacy , Uncertainty , Reproducibility of Results , Total Quality Management/methods , Compliance
5.
São Paulo; s.n; s.n; 2022. 70 p. tab, graf.
Thesis in English | LILACS | ID: biblio-1392313

ABSTRACT

The purpose of this work was to elaborate a diagnosis of the dissolution test in Africa in comparison with Brazil, evaluating the dissolution profile of low solubility drugs such as albendazole, ibuprofen, furosemide, glibenclamide, hydrochlorothiazide and carvedilol to ascertain their quality. The dissolution profiles were evaluated by utilizing the United States Pharmacopeia (USP). The glibenclamide medicine was evaluated according to the Food and Drug Administration (FDA), while a dissolution method was developed for the carvedilol medicine. A filter selection test for all the drugs showed that cannula is suitable for all, except for carvedilol, which is centrifuged. The various brands of Nigerian and Brazilian medicines tested showed some statistical differences. The suitable conditions that allowed the dissolution of carvedilol to be determined were the USP type II apparatus at 75 rpm containing 900 mL of acetate buffer, pH 4.5. The results of the dissolution test showed that out of the 17 different brands of Brazilian medicines and 17 different products from Nigeria, 94.12% and 58.82% passed respectively


O objetivo deste trabalho foi elaborar um diagnóstico do teste de dissolução na África em comparação ao Brasil, avaliando o perfil de dissolução de medicamentos de baixa solubilidade como albendazol, ibuprofeno, furosemida, glibenclamida, hidroclorotiazida e carvedilol para verificar sua qualidade.Os perfis de dissolução foram avaliados utilizando a Farmacopeia dos Estados Unidos (USP). O medicamento glibenclamida foi avaliado de acordo com a Food and Drug Administration (FDA), enquanto um método de dissolução foi desenvolvido para o medicamento carvedilol.Um teste de seleção de filtro para todos os medicamentos mostrou que a cânula é adequada para todos, exceto para o carvedilol, que é centrifugado. As diversas marcas de medicamentos Nigerianos e Brasileiros testadas apresentaram algumas diferenças estatísticas. As condições adequadas que permitiram a determinação da dissolução do carvedilol foram o aparelho USP tipo II a 75 rpm contendo 900 mL de tampão acetato, pH 4,5. Os resultados do teste de dissolução mostraram que das 17 diferentes marcas de medicamentos brasileiros e 17 diferentes produtos da Nigéria, 94,12% e 58,82% foram aprovados, respectivamente


Subject(s)
Solubility , Brazil/ethnology , Pharmaceutical Preparations/analysis , Africa/ethnology , Dissolution , United States Food and Drug Administration , Albendazole/pharmacology , Ibuprofen , Carvedilol/pharmacology , Furosemide/pharmacology , Methods , Acetates/adverse effects
6.
Braz. J. Pharm. Sci. (Online) ; 58: e20180, 2022. tab, graf
Article in English | LILACS | ID: biblio-1403759

ABSTRACT

Abstract Conjunctivitis is an inflammation of the conjunctiva, which covers the white part of the eyeball. It can be caused by allergies, bacterial or viral infection. In situ hydrogels are three-dimensional hydrophilic cross-linked network of polymers. In situ hydrogel provided better therapeutic index when compared to conventional treatment. The present work describes the formulation and evaluation of ofloxacin and dexamethasone based on the concept of pH triggered in situ gelation. Carbopol 934p was used as the gelling agent in combination with HPMC, as a viscosity-enhancing agent, benzalkonium chloride as preservative, sodium chloride as tonicity adjusting agent. The prepared formulations were liquid at the low pH and underwent rapid transition into viscous gel at the pH of the tear fluid. Formulations were evaluated for various rheological, in vitro and in vivo release characteristics. Infrared spectroscopy studies showed that there were no interactions between the drug and polymers. Viscosity of the prepared hydrogels lies in the optimum range and drug was released up to 85 % as the end of 13 h. The prepared in situ hydrogel was sterile, non-irritant to the eye. The present study indicated that it is possible to develop safe and physiologically effective in situ hydrogel which is patient compliant.


Subject(s)
Dexamethasone/agonists , Conjunctivitis/drug therapy , Hydrogels/analysis , Spectrum Analysis , In Vitro Techniques/methods , Pharmaceutical Preparations/analysis , Spectroscopy, Fourier Transform Infrared/methods
7.
Braz. J. Pharm. Sci. (Online) ; 58: e18688, 2022. tab, graf
Article in English | LILACS | ID: biblio-1364425

ABSTRACT

Abstract Hydrogels are interesting for use in the treatment of topical wounds due to their virtually zero toxicity, and capacity for extended release of pharmaceuticals. Silver sulfadiazine (SSDZ) is the drug of choice in the treatment of skin burns. The aim of the study was to determine cytotoxicity, antimicrobial activity and stability of a PVA hydrogel with integrated silver sulfadiazine. SSDZ-hydrogels were prepared using 10% (w/w) PVA (either 89% or 99% hydrolyzed) and 1% (w/w) silver sulfadiazine. Cellular viability was assessed via MTS assays, antimicrobial activity via disk-diffusion and accelerated stability tests were carried out with analysis at 0, 30, 60, 90 and 180 days of storage at 40 ± 2 °C and a relative humidity of 75 ± 5%. The parameters evaluated included organoleptic characteristics, moisture, swelling ability, mechanical strength, FTIR, XRD, TGA and DSC, and silver release patterns via XRD and potentiometry. Cell viability tests indicated some cytotoxicity, although within acceptable levels. After 90 days of storage, SSDZ hydrogel samples exhibited a brown coloration, probably due to the formation of Ag or Ag2O nanoparticles. The SSDZ-loaded hydrogels suffered visual and physical changes; however, these changes did not compromise its use as occlusive wound dressings or its antimicrobial properties.


Subject(s)
Silver Sulfadiazine/pharmacology , Pharmaceutical Preparations/analysis , Hydrogels/analysis , Skin/injuries , Wounds and Injuries/classification , Spectroscopy, Fourier Transform Infrared , Reference Standards/classification
8.
Braz. J. Pharm. Sci. (Online) ; 58: e18637, 2022. tab, graf
Article in English | LILACS | ID: biblio-1364416

ABSTRACT

Abstract The therapeutic drugs to treat Herpes simplex virus (HSV) infections have toxic side effects and there has been an emergence of drug-resistant strains. Therefore, the search for new treatments for HSV infections is mounting. In the present study, semi-solid formulations containing a crude hydroethanolic extract (CHE) from Schinus terebinthifolia were developed. Skin irritation, cutaneous permeation, and in vivo therapeutic efficacy of the formulations were investigated. Treatment with the ointment formulations did not result in any signs of skin irritation while the emulsions increased the thickness of the epidermis in Swiss mice. The cutaneous permeation test indicated that the CHE incorporated in the formulations permeated through the skin layers and was present in the epidermis and dermis even 3 h after topical application. In vivo antiviral activity in BALB/c mice treated with the CHE ointments was better than those treated with the CHE emulsions and did not significantly differ from an acyclovir-treated group. Taken together, this suggests that the incorporation of CHE in the ointment may be a potential candidate for the alternative topical treatment of herpetic lesions.


Subject(s)
Pharmaceutical Preparations/analysis , Simplexvirus/classification , Herpesvirus 1, Human/classification , Anacardiaceae/adverse effects , Antiviral Agents/adverse effects , Acyclovir/antagonists & inhibitors , Efficacy , Emulsions/adverse effects
9.
Braz. J. Pharm. Sci. (Online) ; 58: e191134, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394031

ABSTRACT

Abstract Existing medications i.e. the antipsychotic drugs are known to be effective in treating only the positive symptoms of schizophrenia, while being ineffective on negative and cognitive symptoms of the disease. In addition, these medications cause extrapyramidal symptoms, forcing many patients towards natural medicine in the hope of minimizing the unwanted adverse effects. Nardostachys jatamansi is a medicinal plant that has been traditionally prescribed for various types of brain disorders. The active constituents of the plant have beneficial effects on the negative and cognitive symptoms of schizophrenia. This study was designed to identify the active constituents of Nardostachys jatamansi with the highest binding affinities for the key macromolecular drug targets involved in the pathophysiology of schizophrenia and thereby elucidate the possible mechanism of action. These targets are dopamine receptors, Gamma-aminobutyric acid receptors, N-methyl-D-aspartate receptors and Phosphodiesterase 10A. The results of molecular docking showed that, β-sitosterol, chlorogenic acid, oleanic acid and ursolic acid, displayed high binding affinity toward all the macromolecular drug targets. Ligands with steroid backbone and pentacyclic triterpene structure have been found to possess high binding affinity toward the dopamine receptor and phosphodiesterase 10A. While ligands with carbonyl group form stronger binding interactions with the N-methyl-D-aspartate receptor.


Subject(s)
Plants, Medicinal/adverse effects , Research/classification , Pharmaceutical Preparations/analysis , Valerianaceae/classification , Nardostachys/adverse effects , Schizophrenia , Antipsychotic Agents
10.
Braz. J. Pharm. Sci. (Online) ; 58: e19608, 2022. tab, graf
Article in English | LILACS | ID: biblio-1383987

ABSTRACT

Abstract Nanobubbles are nanometer size bubbles having different constituents of varying physicochemical characteristic for the inner core and outer shell. Nanobubbles are mainly fabricated to improve the stability, bioavailability and improve the biodistribution of the delivered drug to the specific targeted site. Their small sizes bubbles allow the possibility of extravasation from blood vessels into the surrounding tissues and ultrasound-targeted site-specific release with minimal invasiveness. Nanobubbles are developing as important contrast agents for imaging and carriers for drug delivery at targeted region. Sonication is the primary method for preparation of nanobubbles followed by thin-layer evaporation, high shear emulsification, mechanical agitation and coacervation or coalescence. With exposure to ultrasound/extracorporeal shock waves, the drug is liberated from the nanobubbles into the target cells. This review paper is an effort to reveal the different formulation development techniques briefly and varying shell and core content for developing nanobubbles.


Subject(s)
Pharmaceutical Preparations/analysis , Drug Delivery Systems/adverse effects , Blood Vessels , Genetic Therapy/adverse effects , Contrast Media/pharmacology , Methods
11.
Braz. J. Pharm. Sci. (Online) ; 58: e19426, 2022. tab, graf
Article in English | LILACS | ID: biblio-1383978

ABSTRACT

Abstract Bioequivalence (BE) assessment of topical drug products is a long-standing challenge. Agencies such as the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have published several drafts in recent years suggesting different approaches as alternative to evaluate the BE. A proposed Topical Classification System (TCS) has even been discussed. Given the above, the objective of this research was to use in vitro and in vivo BE approaches to evaluate Brazilian marketed mupirocin (MPC) ointments, previously classified as TCS class The in vitro permeation test (IVPT) was performed by applying formulations to pig skin by Franz cells. The in vivo methodology was dermatopharmacokinetic (DPK). These approaches (in vivo tape stripping and IVPT) demonstrated capability of distinguishing among different formulations, thus making them useful methodologies for BE evaluation.


Subject(s)
Ointments/analysis , In Vitro Techniques/methods , Therapeutic Equivalency , Mupirocin/analysis , Research/instrumentation , Skin , United States Food and Drug Administration , Pharmaceutical Preparations/analysis , Methodology as a Subject
12.
Braz. J. Pharm. Sci. (Online) ; 58: e19759, 2022. tab
Article in English | LILACS | ID: biblio-1383977

ABSTRACT

Abstract Dissolution is a key step in the uptake of oral drugs. In order to compare the behaviour of the dissolution of two formulations, the dissolution profile test was used. This assay must be discriminative and should mimic in vivo conditions. Many dissolution media described in pharmacopoeias are not predictive of bioavailability. Due to this, biorelevant media are used as an alternative to solve this problem. The objective of this work is to evaluate the relevance of biorelevant dissolution media to predict in vivo drug dissolution. For this, a bibliographic search was carried out in scientific databases. The search was first performed for articles verifying the physicochemical properties of human gastrointestinal fluids. Subsequently, a comparison was made between the properties of gastrointestinal fluids and those of biorelevant and pharmacopoeial media. Finally, the results of bioequivalence studies and dissolution profile tests in biorelevant media described in the literature were compared. The results revealed that there are a few publications that have analysed some physicochemical properties of gastrointestinal fluids. In addition, high variability was observed for some properties. Regarding the comparison of these properties with pharmacopoeial media and biorelevant media, the analysis showed that the biorelevant media are more similar to gastrointestinal fluids than the pharmacopoeial media. Finally, the in vitro dissolution profile results were similar to the results obtained in vivo. Thus, biorelevant media may be useful for analysing dissolution profiles.


Subject(s)
Therapeutic Equivalency , Dissolution , Drug Liberation , Publications/classification , In Vitro Techniques/instrumentation , Pharmaceutical Preparations/analysis
13.
Braz. J. Pharm. Sci. (Online) ; 58: e19989, 2022. tab, graf
Article in English | LILACS | ID: biblio-1383997

ABSTRACT

Abstract Proton pump inhibitors (PPI) are drugs that suppress gastric acid secretion. Its use, without support from scientific evidence, can contribute to polypharmacy, lead to drug interactions and, in the long term, cause serious adverse reactions. Studies advise physicians to deprescribe PPI. A quick review of scientific evidence, also called a rapid systematic review, on the deprescribing of PPI was performed. Evidence searches were performed in the LILACS, Embase, PubMed and NICE evidence databases with the terms "omeprazole", "proton pump inhibitors", "deprescription", "deprescribing". At LILACS these descriptors were also used in Portuguese and Spanish. Of 118 studies identified, four systematic reviews were selected for analysis. Abrupt deprescribing was associated with an increased risk of symptom recurrence. Fear of symptom recurrence is one of the major barriers to patient-related deprescribing. Educational interventions directed at prescribers, pharmacists, and patients are effective strategies in the deprescribing of PPI. Deprescribing process showed to be feasible in different contexts, with different strategies. The process is most effective through actions with educational and guidance materials directed to health professionals and patients, and with the involvement or leadership of the pharmacist.


Subject(s)
Proton Pump Inhibitors/adverse effects , Deprescriptions , Pharmaceutical Preparations/analysis , Polypharmacy , Drug Interactions , Drug-Related Side Effects and Adverse Reactions
14.
Braz. J. Pharm. Sci. (Online) ; 58: e19859, 2022. tab, graf
Article in English | LILACS | ID: biblio-1383996

ABSTRACT

To overcome the problems associated with bioavailability and systemic side effects of the drug by oral administration, monolithic matrix type transdermal patches containing cinnarizine (CNZ) were developed. For this purpose, films based on hydroxypropyl methylcellulose and polyvinylpyrrolidone as matrix-forming polymers were designed. Physical characteristics of transdermal films and drug-excipient compatibility were investigated. Factors affecting in vitro drug release and ex vivo skin penetration and permeation of the drug were studied. It was confirmed that films displayed sufficient flexibility and mechanical strength for application onto the skin for a long time period. Ex vivo penetration experiments gave satisfactory results for transdermal drug delivery through rat skin. The parameters determining good skin penetration were also evaluated. The highest drug permeation rate was obtained with incorporation of Transcutol® (0.102 mg/cm2/h) into the base CNZ formulation, followed by propylene glycol (0.063 mg/cm2/h), menthol (0.045 mg/cm2/h), and glycerin (0.021 mg/cm2/h) as penetration enhancers (p < 0.05). As a result, the developed transdermal patches of CNZ may introduce an alternative treatment for various conditions and diseases such as idiopathic urticarial vasculitis, Ménière's disease, motion sickness, nausea, and vertigo. Thus, the risk of systemic side effects caused by the drug can be reduced or eliminated


Subject(s)
Administration, Oral , Cinnarizine , Histamine Agonists/adverse effects , Cholinergic Antagonists , Anesthetics/classification , Skin , In Vitro Techniques/methods , Pharmaceutical Preparations/analysis , Hypromellose Derivatives/adverse effects , Drug Liberation
15.
Braz. J. Pharm. Sci. (Online) ; 58: e18553, 2022. tab, graf
Article in English | LILACS | ID: biblio-1360166

ABSTRACT

Abstract The aqueous solubility of cefixime trihydrate (a water insoluble drug) using different hydrotropic agents was determined and solid dispersions of cefixime trihydrate were prepared by hydrotropic solubilization technique. The drugs content were determined. The aqueous solubility of v was increased many fold in presence of sodium acetate trihydrate as hydrotropic agent. This hydrotropic agent was used to prepare solid dispersion of cefixime trihydrate. Cefixime trihydrate and sodium acetate trihydrate were accurately weighed and taken in a 200 mL beaker. Distilled water 10-15 mL was taken to dissolve hydrotropic agent using heat (48-50 °C). The drug was then added to it and magnetically stirred till whole mass get viscous. The solid dispersions of cefixime trihydrate were characterized by XRD, DSC and IR studies. DSC thermogram, XRD and Infra-Red spectra were studied. Solid dispersions, thus prepared, showed faster release of the drug as compared to pure drug and physical mixture.


Subject(s)
Solubility/drug effects , Pharmaceutical Preparations/analysis , Methods , Water , Sodium Acetate/administration & dosage , Cefixime/adverse effects
16.
Braz. J. Pharm. Sci. (Online) ; 58: e20079, 2022. tab, graf
Article in English | LILACS | ID: biblio-1403747

ABSTRACT

Abstract Sustained release matrix tablets of 100 mg losartan potassium HCl were fabricated with two release retarding polymers namely HPMC K100 M and affinisol by direct compression method. Nine trial formulations were prepared by varying content of these polymers, each from 50 mg to 100 mg; keeping the total weight of the tablet 310 mg. The best formulation was selected based on in vitro drug release profile for 12 hours conducted in Type II dissolution apparatus at 50 rpm and water as dissolution medium. Pre-compression parameters such as bulk density, tap density, Carr's index and Hausner ratio were evaluated for the selected tablet. The tablets were subjected to thickness, weight variation test, drug content, hardness and friability. Drug release kinetics, surface morphology and accelerated stability study were investigated for that selected formulation. Formulation F4 with the composition of 75 mg HPMC K100M and 100 mg affinisol was selected as the best formulation that extended the drug release up to 12 hours. Pre-compression parameters and other tableting properties were within the Pharmacopoeia limit. Release kinetics analysis proved non-fickian zero-order drug release and that was further confirmed by surface morphology of the tablets before and after dissolution study visualized by SEM. The developed formulation was found to be stable for one month stored at 60 ○C.


Subject(s)
Tablets/analysis , In Vitro Techniques/methods , Pharmaceutical Preparations/analysis , Losartan/agonists , Drug Compounding/methods , Dissolution , Drug Liberation/drug effects , Methods
17.
Braz. J. Pharm. Sci. (Online) ; 58: e19710, 2022. tab, graf
Article in English | LILACS | ID: biblio-1384010

ABSTRACT

The aim of this work was to assess if the commercially available Fluconazole drug products (Reference, Generic and Similar) would meet the biowaiver criteria from Food and Drug Administration (FDA) and Brazilian Agency for Health Surveillance (ANVISA) agencies. All formulations were evaluated considering the dissolution profile carried out in Simulated Gastric Fluid (SGF) pH 1.2, Acetate Buffer (AB) pH 4.5 and Simulated Intestinal Fluid (SIF) pH 6.8. The results demonstrated that all formulations fulfilled the 85% of drug dissolved at 30 min criterion in SGF pH 1.2. However, in AB pH 4.5 and SIF pH 6.8, some formulations, including the comparator, did not achieve this dissolution percentage. The discrepant dissolution profiles also failed the ƒ2 similarity factor analysis, since none of the formulations showed values between 50 and 100 in the three dissolution media. Comparative dissolution profiles were not similar, considering that the main issues concerning the dissolution were evidenced for the comparator product. Hence, a revision in the regulatory norms in order to establish criteria to switch the comparator could result in an increased application of drugs based on biowaiver criteria


Subject(s)
Fluconazole/analysis , United States Food and Drug Administration/classification , Pharmaceutical Preparations/analysis , Similar/classification , Factor Analysis, Statistical , Brazilian Health Surveillance Agency , Dissolution , Acetates/agonists
18.
Braz. J. Pharm. Sci. (Online) ; 58: e191123, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394050

ABSTRACT

Chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) is a problem, often occurs in patient. Inspite of high bioavailability, the demerits such as: hepatic first pass metabolism and invasive nature of oral and parenteral dosage forms can be avoided with anti-emetic therapy of transdermal device. The major objective of the present study is to modify the hydrochloride (HCl) form of Ondansetron (OND) to the base form followed by improvement of solubility and permeability of OND by employing solid dispersion (SD) loaded patches. Preformulation study, as observed, begins with an approach to enthuse solubility of OND by SD technique choosing different carriers. The choice of carriers was rationalized by phase solubility study. Several combinations of transdermal films were prepared with pure drug, carriers and SDs with plasticizer Ka values of OND-HPßCD binary system were found lower (54.43 to 187.57 M-1) than that of OND-PVP K-30 binary system (1156.77 to 12203.6 M-1). The drug content of SDs and patches were found satisfactory. Better permeation rate (236.48±3.66 µg/3.935 cm2) with promising flux enhancement (8.30 fold) was found with DBP loaded SD patch (P6*). Hence, enhancement of solubility and permeability of P6* ensures that it can successfully enhance the bioavailability


Subject(s)
Plasticizers/adverse effects , Solubility , Ondansetron/antagonists & inhibitors , Patients/classification , Vomiting , Pharmaceutical Preparations/analysis , Postoperative Nausea and Vomiting , Dosage Forms , Drug Therapy/instrumentation , Methods , Motion Pictures/classification
19.
Braz. J. Pharm. Sci. (Online) ; 58: e19538, 2022. tab, graf
Article in English | LILACS | ID: biblio-1383993

ABSTRACT

Abstract The globalization of the pharmaceutical market has enabled access to a considerable number of new medicinal products. Consequently, the circulation of substandard medicinal products has also increased. To minimize this problem, post-marketing quality sampling and testing programs are performed to monitor and confirm that the medicinal products available in the market meet appropriate quality requirements. In this review, the post-approval sampling and testing procedures of six regulatory authorities were compared with the goal of strengthening these market surveillance systems. Similarities were observed between the procedures adopted by different regulatory authorities. However, the agencies were not always transparent about the results of these monitoring procedures. A probable mismatch between the registration procedures and the quality requirements listed in official compendiums was observed, which resulted in dissonance and contradiction between the specifications approved by the regulatory authorities and those required in the pharmacopeias. Therefore, strengthening harmonization projects related to these activities can help minimize such difficulties.


Subject(s)
Pharmaceutical Preparations/analysis , Pharmaceutical Preparations/standards , Sampling Studies , Quality Control , Total Quality Management , Marketing
20.
Braz. J. Pharm. Sci. (Online) ; 58: e191055, 2022. graf
Article in English | LILACS | ID: biblio-1384017

ABSTRACT

Abstract In recent years, nanocarriers have been studied as promising pharmaceutical tools for controlled drug-delivery, treatment-efficacy follow-up and disease imaging. Among them, X-shaped amphiphilic polymeric micelles (Tetronic®, poloxamines) display great potential due to their biocompatibility and non-toxic effects, among others. In the present work, polymeric micelles based on the T1307 copolymer were initially decorated with a 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY)-fluorophore in order to determinate its in vivo biodistribution on 4T1 tumor-bearing mice. However, unfavorable results with this probe led to two different strategies. On the one hand, the BODIPY-micelle-loaded, L-T1307-BODIPY, and on the other hand, the 99mTc-micelle-radiolabeled, L-T1307- 99m Tc, were analyzed separately in vivo. The results indicated that T1307 accumulates mainly in the stomach, the kidneys, the lungs and the tumor, reaching the maximum organ-accumulation 2 hours after intravenous injection. Additionally, and according to the results obtained for L-T1307- 99m Tc, the capture of the polymeric micelles in organs could be observed up to 24 hours after injection. The results obtained in this work were promising towards the development of new radiotracer agents for breast cancer based on X-shaped polymeric micelles.


Subject(s)
Animals , Female , Mice , Efficacy , Diagnosis , Injections, Intravenous/classification , Micelles , Neoplasms/diagnosis , Stomach/abnormalities , Pharmaceutical Preparations/analysis , Health Strategies , Lung/abnormalities
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