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1.
Nursing (Säo Paulo) ; 22(256): 3150-3154, set.2019.
Article in Portuguese | LILACS, BDENF | ID: biblio-1026018

ABSTRACT

Introdução: A Anacardium occidentale (cajueiro), é uma árvore tropical frutífera nativa do Brasil. Suas cascas são ricas em taninos, com ação anti-inflamatória e cicatrizante. Objetivo: Desenvolver formulações semissólidas: gel de carbopol, creme e pomada de lanovaselina contendo o extrato aquoso das cascas de Anacardium occidentale nas concentrações de 2,5 %, 5 % e 7 %, e realizar estudos de estabilidade acelerada, avaliando as características organolépticas, pH, viscosidade e densidade relativa, nos tempos T(0) na data da produção, em temperatura ambiente, e T(30), T(60) e T(90) dias em estufa à 40ºC , afim de determinar a formulação mais estável. Resultados e conclusões: A formulação de creme apresentou melhor estabilidade em todas as concentrações do extrato e quanto a todos os parâmetros avaliados, no entanto, é necessário um estudo posterior para a padronização das formulações.(AU)


Introduction: The Anacardium occidentale (cashew tree) is a tropical fruit tree native to Brazil. Their peels are rich in tannins, with anti-inflammatory and healing action. Aim: To develop semi-solid formulations: carbopol gel, cream and ointment containing the aqueous extract of the barks of Anacardium occidentale at concentrations of 2.5%, 5% and 7%, and to perform accelerated stability studies, evaluating the organoleptic characteristics, pH, viscosity and relative density, at T (0) times at the production date, at room temperature, and T (30), T (60) and T (90) days at 40ºC in order to determine the most stable. Results and conclusions: The cream formulation presented better stability at all concentrations of the extract and for all the evaluated parameters, however, a further study is necessary for the standardization of the formulations.(AU)


Introducción: el Anacardium occidentale (anacardo) es un árbol frutal tropical originario de Brasil. Sus cáscaras son ricas en taninos, con acción antiinflamatoria y curativa. Objetivo: Desarrollar formulaciones semisólidas: gel de carbopol, crema y pomada que contengan el extracto acuoso de las cortezas de Anacardium occidentale en concentraciones de 2.5%, 5% y 7%, y realizar estudios de estabilidad acelerados, evaluando las características organolépticas, pH, viscosidad y densidad relativa, en T (0) veces a la fecha de producción, a temperatura ambiente, y T (30), T (60) y T (90) días a 40ºC para determinar el máximo estable Resultados y conclusiones: La formulación en crema presentó una mejor estabilidad en todas las concentraciones del extracto y para todos los parámetros evaluados, sin embargo, es necesario un estudio adicional para la estandarización de las formulaciones.(AU)


Subject(s)
Plants, Medicinal , Anacardium , Drug Stability , Drug Development
2.
Rev. ciênc. farm. básica apl ; 4001/01/2019. ilus, tab
Article in English | LILACS | ID: biblio-1100195

ABSTRACT

Fenticonazole is an antifungal drug widely used in a cream formulation including as a generic medicine. Stability studies of fenticonazole in a cream formulation are very scarce. In this research, we intent to contribute to generic medicines quality control and provide reliable data seeking for insertion of fenticonazole monograph in official compendia. Therefore, in this work it was studied the behavior of fenticonazole under several conditions and developed a stability-indicating LC method to separate the degradation products and quantify the drug in presence of them, using the Design of Experiments (DoE) as tool to achieve robust and easy transferable method. Fenticonazole stability was evaluated under aqueous, alkaline (0.1 M NaOH), acidic (0.1 M HCL) and oxidative (3% v/v, H2O2) at ambient temperature and heating at 90°C, over 6 hours. The drug shows to be unstable under all stressed test conditions. It was completely degraded under acid medium with arising of degradation products. The robust and stability indicating LC method was validated. It is able to reveal the fenticonazole instability and to separate its degradation product with accuracy and precision (CV ˂ 2%) and without any placebo interferences.(AU)


Subject(s)
Humans , Chromatography, Liquid/methods , Imidazolines/analysis , Skin Cream/metabolism , Quality Control , Drug Stability
3.
Article in Chinese | WPRIM | ID: wpr-773718

ABSTRACT

To enhance in vitro dissolution of Cur by preparing Cur solid dispersions. The ability of HPMCAS-HF,HPMCAS-MF,HPMCAS-LF and PVPK30 to maintain supersaturated solution was investigated by supersaturation test. Amorphous solid dispersions were prepared by the solvent-evaporation method. The prepared samples were characterized using infrared spectroscopy( IR) and differential scanning calorimetry( DSC),and in vitro dissolution was investigated. DSC and IR results showed that in 1 ∶3 and 1 ∶9 solid dispersions,Cur was amorphously dispersed in the carrier,and the interaction existed between drug and carrier. The supersaturation test showed that the order of the ability of polymer to inhibit crystallization of Cur was MF>HF>LF>K30. The dissolution results showed that Cur-K30 amorphous solid dispersion had the highest drug release rate; Cur-K30 and Cur-LF amorphous solid dispersions had a quicker but not stable dissolution rate,and the drug concentration decrease after 4 h; Cur-MF and Cur-HF solid dispersions had a low dissolution,which however increased steadily,attributing to the strong ability of the polymers to inhibit the crystallization of Cur. HPMCAS could inhibit the degradation of Cur better than K30,especially MF and HF. The amorphous solid dispersions of cur significantly enhanced the dissolution of Cur and improved the chemical stability of Cur. This study can provide a basis for the rational selection of the polymer used for Cur solid dispersion.


Subject(s)
Chemistry, Pharmaceutical , Curcumin , Chemistry , Drug Stability , Methylcellulose , Chemistry , Polymers , Solubility
4.
Article in English | WPRIM | ID: wpr-812427

ABSTRACT

The present study was designed to improve storage stability and oral bioavailability of Ganneng dropping pills (GNDP) by transforming lignans of Herpetospermum caudigerum (HL) composed of herpetrione (HPE) and herpetin (HPN) into nanosuspension (HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles (HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy (PCS), zeta potential measurement, and scanning electron microscopy (SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC, C and decrease in T when compared with regular GNDP. These results indicated that NS-GNDP possessed superiority with improved storage stability and increased dissolution rate and oral bioavailability.


Subject(s)
Animals , Benzofurans , Chemistry , Biological Availability , Cucurbitaceae , Chemistry , Drug Carriers , Chemistry , Drug Compounding , Drug Stability , Freeze Drying , Furans , Chemistry , Humans , Lignans , Chemistry , Pharmacokinetics , Male , Nanoparticles , Chemistry , Particle Size , Plant Extracts , Chemistry , Rats , Rats, Sprague-Dawley , Solubility
5.
Health sci. dis ; 19(2)2018.
Article in French | AIM, AIM | ID: biblio-1262799

ABSTRACT

Introduction. Le marché parallèle de la vente des médicaments s'est développé au cours des dernières décennies dans les pays en voie d'émergence et il a été établi que la commercialisation de médicaments hors du circuit officiel est une source potentielle de risques pour la santé publique. Notre étude avait pour objectif d'étudier la stabilité du Cotrimoxazole 240 mg / 5 ml suspension stocké dans les circuits formel et informel. Méthodologie : De septembre 2015 à Mai 2016, une étude expérimentale a été conduite dans la ville de Douala. Un total de 81 échantillons de Cotrimoxazole 240 mg/5 mL suspension ont été prélevés dans neuf sites. Tous les échantillons ont subi un contrôle qualité sur la base des évaluations technico-règlementaire, organoleptique, physico-chimique et microbiologique. De plus, des analyses qualitative et quantitative des composés actifs du cotrimoxazole (sulfaméthoxazole et triméthoprime) ont été réalisées. Résultats. Le Ghana et l'Inde sont apparus comme les plus grands fournisseurs du Cotrimoxazole. Les numéros de lot, la notice, les dates de fabrication et de péremption, la présentation et la forme, la classe thérapeutique, les indications, et la posologie étaient présents sur tous les échantillons (100%). Par ailleurs, 41,99% et 55,55% des échantillons étaient de couleur ponceau et avaient un goût aromatisé à la fraise respectivement (p-value < 0,0001). Le pH moyen des suspensions de Cotrimoxazole dans le secteur informel s'est révélé significativement faible par rapport à celui des suspensions du secteur formel (p-value = 0,0054). Tous les échantillons étaient exempts de microorganismes pathogènes. L'analyse spectrophotométrique UV-Vis a montré que la teneur en substances actives était en moyenne significativement plus élevée dans le secteur formel (80,16% contre 73,16%; p-value = 0,001). Conclusion. Cette étude souligne le besoin urgent de lutter activement contre la vente illicite des médicaments ainsi que la nécessité de renforcer les systèmes de contrôle qualité des médicaments dans la ville de Douala


Subject(s)
Cameroon , Drug Stability , Drug Substitution , Nonprescription Drugs , Sulfamethoxazole , Trimethoprim
6.
São Paulo; s.n; s.n; 2018. 97 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-996477

ABSTRACT

O presente estudo foi realizado com o objetivo de se desenvolver e validar uma metodologia analítica indicativa de estabilidade para separação e quantificação de anlodipino e seus produtos de degradação no medicamento besilato de anlodipino 5 mg por comprimido. Para tanto, realizou-se um estudo de degradação forçada, como forma de identificar os principais produtos de degradação, que podem vir a formar num estudo de estabilidade, bem como estabelecer possíveis rotas de degradação. Foi utilizada a técnica instrumental de separação, cromatografia a líquido (CL), com dois tipos de detectores: arranjo de diodos (DAD) e corona CAD (Detector de aerossol carregado), coluna cromatográfica Zorbax SB-Phenyl 1,8µm 4,6 x 50 mm Agilent® e fase móvel constituída por tampão pH3,0, metanol e acetonitrila sob condições de gradiente (75% de tampão pH 3,0, 15% de metanol e 10% de acetonitrila; no tempo de 10 minutos tem-se 20% de tampão pH3,0, 60% de metanol e 20% de acetonitrila; no tempo de 13 minutos tem-se 75% de tampão pH3,0, 15% de metanol e 10% de acetonitrila; e no tempo de 15 minutos tem-se 75% de tampão pH3,0, 15% de metanol e 10% de acetonitrila); fluxo de 1,0mL/min até 10 minutos; de 10,1 a 13 minutos tem-se fluxo de 0,5 mL/min; e de 13,1 a 15 minutos volta ao fluxo de 1,0 mL/min; e detecção em 238 nm. O método apresentou-se linear, preciso, exato, robusto e seletivo, e proporcionou resultados confiáveis, sem interferência de degradantes e impurezas


This study was conducted in order to develop an analytical methodology indicative of stability for separation and quantification of the antihypertensive amlodipine and its degradation products in the drug amlodipine besylate 5 mg per tablet. For this development was performed a forced degradation study, in order to identify the main degradation products that may form in a stability study, as well as establish possible degradation routes. It was used the instrumental separation technique, liquid chromatography (LC) with two types of detectors: diode array (DAD) and corona CAD (Charged Aerosol Detector), chromatographic column Zorbax SB-Phenyl 4.6 x 50 mm 1,8µm Agilent® and mobile phase of buffer pH3,0, methanol and acetonitrile under gradient conditions (75% buffer pH3,0, 15% methanol and 10% acetonitrile; 10 minutes has 20% buffer pH3,0, 60% methanol and 20% acetonitrile; 13 minutes has become 75% of buffer pH3,0, 15% methanol and 10% acetonitrile; and 15 minutes has become 75% of buffer pH3,0, 15% methanol and 10% acetonitrile); flow 1.0 mL/ min up to 10 minutes; a flow 0,5 mL/min is obtained from 10,1 to 13 minutes; and from 13,1 minutes the flows returns to 1,0 mL/min; and detection in 238 nm. The method is linear, precise, accurate, robust and selective, and provided reliable results without interference from degradation products and impurities


Subject(s)
Amlodipine/analysis , Validation Study , Analytical Methods/analysis , Drug Stability , Hypertension/diagnosis
7.
Braz. J. Pharm. Sci. (Online) ; 54(3): e00223, 2018. tab, graf
Article in English | LILACS | ID: biblio-974412

ABSTRACT

Forced degradation studies of gliquidone were conducted under different stress conditions. Three degradates were observed upon using HPLC and TLC and elucidated by LC-MS and IR. HPLC method was performed on C18 column using methanol-water (85:15 v/v) pH 3.5 as a mobile phase with isocratic mode at 1 mL.min-1 and detection at 225 nm. HPLC analysis was applied in range of 0.5-20 µg.mL-1 (r =1) with limit of detection (LOD) 0.177 µg.mL-1. TLC method was based on the separation of gliquidone from degradation products on silica gel TLC F254 plates using chloroform-cyclohexane-glacial acetic acid (6:3:1v/v) as a developing system with relative retardation 1.15±0.01. Densitometric measurements were achieved in range of 2 -20 µg /band at 254 nm (r = 0.9999) with LOD of 0.26 µg /band. Least squares regression analysis was applied to provide mathematical estimates of the degree of linearity. The analysis revealed a linear calibration for HPLC where a binomial relationship for TLC. Stability testing and methods validation have been evaluated according to International Conference on Harmonization guidelines. Moreover, the proposed methods were applied for the analysis of tablets and the results obtained were statistically compared with those of pharmacopeial method revealing no significant difference about accuracy and precision.


Subject(s)
Chromatography, High Pressure Liquid/methods , Hypoglycemic Agents/metabolism , Densitometry/methods , Diabetes Mellitus, Type 2/drug therapy , Drug Stability
8.
Braz. J. Pharm. Sci. (Online) ; 54(2): e17352, 2018. tab, graf
Article in English | LILACS | ID: biblio-951926

ABSTRACT

Abstract With the aim of controlling various symptoms, possible to use mixtures of different drugs within infusion devices. This should take into account the compatibility of the mixture. Factors influence the compatibility and stability of the mixtures are: drug type, concentration, solvent, temperature and light. When evaluating the compatibility of the mixtures for infusion for subcutaneous via is important to consider infusion devices used and the conditions of light and temperature should simulate as far as possible the conditions in practice assistance. There are diverse studies that analyze the compatibility of drug mixtures, but there are still many possible combinations of drugs for which evidence is not available. The objective of this work is to study the compatibility and stability of several mixtures of haloperidol and morphine that can be used in solution for subcutaneous infusion.


Subject(s)
Haloperidol/analysis , Morphine/analysis , Palliative Care/classification , Drug Combinations , Drug Stability
9.
Article in English | WPRIM | ID: wpr-773637

ABSTRACT

The present study was designed to improve storage stability and oral bioavailability of Ganneng dropping pills (GNDP) by transforming lignans of Herpetospermum caudigerum (HL) composed of herpetrione (HPE) and herpetin (HPN) into nanosuspension (HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles (HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy (PCS), zeta potential measurement, and scanning electron microscopy (SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC, C and decrease in T when compared with regular GNDP. These results indicated that NS-GNDP possessed superiority with improved storage stability and increased dissolution rate and oral bioavailability.


Subject(s)
Animals , Benzofurans , Chemistry , Biological Availability , Cucurbitaceae , Chemistry , Drug Carriers , Chemistry , Drug Compounding , Drug Stability , Freeze Drying , Furans , Chemistry , Humans , Lignans , Chemistry , Pharmacokinetics , Male , Nanoparticles , Chemistry , Particle Size , Plant Extracts , Chemistry , Rats , Rats, Sprague-Dawley , Solubility
10.
Medicina (B.Aires) ; 77(5): 353-357, oct. 2017. tab
Article in Spanish | LILACS | ID: biblio-894499

ABSTRACT

Candid#1 es la primera vacuna a virus vivo atenuado producida y registrada en Argentina. Se produce en el INEVH desde 2003 para prevenir la fiebre hemorrágica argentina y se obtiene mediante cosecha de sobrenadantes de cultivos de células diploides infectadas con una cepa atenuada del virus Junín, formulación y posterior liofilización. Su estabilidad es crucial para asegurar su efectividad. El objetivo de este trabajo fue evaluar la estabilidad de Candid#1 exponiéndola a distintas condiciones de temperatura y tiempo. Tres lotes producidos en 2003 fueron sometidos al siguiente esquema de almacenamiento: (a) vacuna reconstituida conservada entre 2 °C y 8 °C durante 8 días, (b) vacuna liofilizada conservada entre 2 °C y 8 °C durante 6 meses, y (c) vacuna liofilizada conservada entre -18 °C y -20 °C durante 10 años. La potencia fue evaluada en monocapa de células Vero bajo agar. Los resultados fueron: (a) Candid#1 reconstituida fue estable 8 días entre 2 °C y 8 °C, (b) Candid#1 liofilizada fue estable 2 meses entre 2 °C y 8 °C y (c) Candid#1 liofilizada fue estable 9 años entre -18 °C y -20 °C manteniendo todos sus atributos. Estos resultados permitieron establecer las siguientes condiciones de almacenamiento: reconstituida 12 horas entre 2 °C y 8 °C, liofilizada 30 días entre 2 °C y 8 °C y 9 años entre -18 °C y -20 °C. A la luz de estos resultados, se generaron cambios favorables en las condiciones de transporte, almacenamiento y distribución de la vacuna. Se implementó la instalación de freezers domésticos en centros estratégicamente distribuidos, permitiendo preservar stocks de vacuna y distribuir las dosis necesarias a vacunatorios.


Candid#1 is the first live attenuated vaccine produced and registered in Argentina. Produced since 2003 at the INEVH to prevent Argentine hemorrhagic fever, it is obtained by harvesting supernatants of diploid cells infected with an attenuated strain of Junin virus and subsequent lyophilization. The stability of this vaccine is crucial to ensure its effectiveness. This study was aimed to evaluate the stability of Candid#1 by exposing it to different time and temperature conditions. Three vaccine batches produced in 2003 were analysed according to the following storage scheme: (a) reconstituted vaccine at 2 °C to 8°C for 8 days; (b) lyophilized vaccine at 2 °C to 8 °C for 6 months; (c) lyophilized vaccine at -18 °C to -20 °C for 10 years. The potency was assessed in Vero cell monolayers under agar. The results were: (a) reconstituted vaccine was stable between 2 °C and 8 °C for 8 days, (b) lyophilized vaccine was stable between 2 °C and 8 °C for 2 months, and (c) lyophilized vaccine was stable 9 years between -18 °C and -20 °C, keeping all its properties. These results allowed us to establish the following storage conditions and expiration times for Candid#1: (a) reconstituted: 12 hours between 2 °C and 8 °C, (b) lyophilized: 30 days between 2 °C and 8 °C and (c) lyophilized: 9 years between -18 °C and -20 °C. Based on our results, favorable changes were made in the conditions of transport, storage and distribution of the vaccine. Domestic freezers in strategically located centers were installed, allowing the preservation of vaccine stocks for distribution to secondary vaccination centers.


Subject(s)
Humans , Viral Vaccines/immunology , Arenaviruses, New World/immunology , Drug Storage/methods , Hemorrhagic Fever, American/prevention & control , Antibodies, Viral/immunology , Argentina , Vaccines, Attenuated/immunology , Drug Stability
11.
An. acad. bras. ciênc ; 89(3): 1601-1613, July-Sept. 2017. tab, graf
Article in English | LILACS | ID: biblio-886732

ABSTRACT

ABSTRACT This paper describes the preparation and characterization of alginate beads coated with gelatin and containing Lactobacillus rhamnosus. Capsules were obtained by extrusion method using CaCl2 as cross linker. An experimental design was performed using alginate and gelatin concentrations as the variables investigated, while the response variable was the concentration of viable cells. Beads were characterized in terms of size, morphology, scanning electron microscopy (SEM), moisture content, Fourier Transform Infrared Spectrometry (FTIR), thermal behavior and cell viability during storage. The results showed that the highest concentration of viable cells (4.2 x 109 CFU/g) was obtained for 1 % w/v of alginate and 0.1 % w/v of gelatin. Capsules were predominantly spherical with a rough surface, a narrow size distribution ranging from 1.53 to 1.90 mm and a moisture content of 97.70 ± 0.03 %. Furthermore, FTIR and thermogravimetric analysis indicated an interaction between alginate-gelatin. Cell concentration of alginate/gelatin microcapsules was 105 CFU/g after 4 months of storage at 8 oC.


Subject(s)
Capsules/standards , Probiotics , Drug Stability , Alginates/ultrastructure , Lactobacillus rhamnosus/ultrastructure , Gelatin/ultrastructure , Microscopy, Electron, Scanning , Cell Survival , Spectroscopy, Fourier Transform Infrared , Drug Storage
12.
Arq. bras. oftalmol ; 80(2): 108-113, Mar.-Apr. 2017. tab, graf
Article in English | LILACS | ID: biblio-838784

ABSTRACT

ABSTRACT Purpose: Avastin® (bevacizumab) is an anti-vascular endothelial growth factor (VEGF) monoclonal antibody given as an off-label drug by intravitreal administration for treatment of ocular diseases. The drug's clinical application and its cost-benefit profile has generated demand for its division into single-use vials to meet the low volume and low-cost doses necessary for intraocular administration. However, the safety of compounding the drug in single-use vials is still under discussion. In this study, the stability and efficacy of Avastin® repacked in individual single-use glass vials and glass ampoules by external compounding pharmacies were evaluated. Methods: Polyacrylamide gel electrophoresis (PAGE), size-exclusion chromatography (SEC), dynamic light scattering (DLS), and turbidimetry were selected to detect the formation of aggregates of various sizes. Changes in bevacizumab biological efficacy were investigated by using an enzyme-linked immunosorbent assay (ELISA). Results: Repacked and reference bevacizumab showed similar results when analyzed by PAGE. By SEC, a slight increase in high molecular weight aggregates and a reduction in bevacizumab monomers were observed in the products of the three compounding pharmacies relative to those in the reference bevacizumab. A comparison of repacked and reference SEC chromatograms showed that the mean monomer loss was ≤1% for all compounding pharmacies. Protein aggregates in the nanometer- and micrometer-size ranges were not detected by DLS and turbidimetry. In the efficacy assay, the biological function of repacked bevacizumab was preserved, with <3% loss of VEGF binding capacity relative to that of the reference. Conclusion: The results showed that bevacizumab remained stable after compounding in ampoules and single-use glass vials; no significant aggregation, fragmentation, or loss of biological activity was observed.


RESUMO Objetivos: Avastin® (bevacizumabe) é um anticorpo monoclonal inibidor do fator de crescimento endotelial de vasos (VEGF) utilizado "off-label" por meio de administração intravítrea para o tratamento de doenças oculares. A sua aplicação clínica associada ao custo-benefício do medicamento gerou uma demanda para seu fracionamento em frascos de dose única para utilização pela via intraocular. No entanto, a segurança do fracionamento do anticorpo em frascos de dose única ainda é alvo de discussão. Neste trabalho, a estabilidade e a eficácia do Avastin® fracionado em frascos ou ampolas de vidro de dose unitária por farmácias de manipulação do mercado foram avaliadas. Métodos: As técnicas de eletroforese em gel de poliacrilamida (PAGE), cromatografia por exclusão de tamanho (SEC), espalhamento dinâmico da luz (DLS) e turbidimetria foram empregadas para avaliar a formação de agregados de diferentes tamanhos. Alterações na atividade biológica do bevacizumabe foram estudadas utilizando ELISA. Resultados: Amostras referência e do bevacizumabe fracionado apresentaram resultados semelhantes quando analisado por gel de poliacrilamida. Por cromatografia por exclusão de tamanho, um pequeno aumento na quantidade de agregados de alta massa molar seguido de uma redução nos monômeros do bevacizumabe foram observados para as amostras das três farmácias de manipulação quando comparado ao referência. A comparação dos cromatogramas mostrou uma quantidade de redução do monômero inferior a 1% para todas as amostras fracionadas. Por espalhamento dinâmico da luz e turbidimetria, não foram detectados agregados de proteína na faixa de tamanho de micrômetro e nanômetro. No ensaio de eficácia, o bevacizumabe fracionado preservou sua função biológica pois apresentou menos de 3% de perda na capacidade de ligação ao VEGF quando comparado ao referência. Conclusão: Este estudo sugere que o bevacizumabe se mantem estável após fracionamento em ampolas e frascos de vidro de dose unitária pois não foram observadas agregação e/ou fragmentação de proteínas e perda de atividade biológica em quan tidades significativas.


Subject(s)
Quality Control , Angiogenesis Inhibitors/chemistry , Drug Packaging , Bevacizumab/chemistry , Enzyme-Linked Immunosorbent Assay/methods , Chromatography, Gel/methods , Angiogenesis Inhibitors/analysis , Vascular Endothelial Growth Factor A/analysis , Drug Stability , Electrophoresis, Polyacrylamide Gel/methods , Intravitreal Injections , Bevacizumab/analysis , Dynamic Light Scattering/methods , Molecular Weight , Nephelometry and Turbidimetry/methods
13.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (1): 23-28
in English | IMEMR | ID: emr-185735

ABSTRACT

The main objective of present study was to develop a RP-HPLC method for estimation of Armodafinil in pharmaceutical dosage forms and characterization of its base hydrolytic product. The method was developed for Armodafinil estimation and base hydrolytic products were characterized. The separation was carried out on C18 column by using mobile phase as mixture of water and methanol [45:55%v/v]. Eluents were detected at 220nm at 1ml/min. Stress studies were performed with milder conditions followed by stronger conditions so as to get sufficient degradation around 20%. A total of five degradation products were detected and separated from analyte. The linearity of the proposed method was investigated in the range of 20-120 micro g/ml for Armodafinil. The detection limit and quantification limit was found to be 0.01183 micro g/ml and 0.035 micro g/ml respectively. The precision % RSD was found to be less than 2% and the recovery was between 98-102%. Armodafinil was found to be more sensitive to the base hydrolysis and yielded its carboxylic acid as degradant. The developed method was stability indicating assay, suitable to quantify Armodafinil in presence of possible degradants. The drug was sensitive to acid, base and photolytic stress and resistant to thermal and oxidation


Subject(s)
Benzhydryl Compounds/analysis , Drug Evaluation, Preclinical , Drug Stability , Chromatography, High Pressure Liquid/trends , Validation Studies as Topic
14.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (1): 143-147
in English | IMEMR | ID: emr-185751

ABSTRACT

The objective of this study was validation of a reverse phase HPLC method for the estimation of metoclopramide HCl in plasma already validated for determination of metoclopramide HCl in tablets dosage form. A reverse chromatographic method was used for estimation of metoclopramide HCl with the mobile phase of acetonitrile, 20mM potassium dihydrogen phosphate buffer solution [pH 3.0 adjusted with orthophosphoric acid] in the ratio of 40: 60. The column used was Waters C18 3.9x300mm micro Bondapak [RP]. The flow rate of the mobile phase was 2ml/ minute. The detector was set at the wavelength of 275nm. This method validated in plasma and was found to be linear, with correlation coefficient [R[2]], value of 0.9988, in the range of 48 ng/ml-0.25ng/ml. The method modified was accurate, precise, sensitive and showed good stability results. The % RSD of the retention time and peak area of metoclopramide HCl was 0.19% and 1.44% respectively. All the parameters such as specificity, linearity, range, accuracy, precision, system suitability, solution stability, detection and quantification limits were evaluated to validate this method and were found within the acceptance limits. The method can be effectively used for estimation of metoclopramide HCl in plasma


Subject(s)
Humans , Calibration , Metoclopramide/blood , Metoclopramide/pharmacokinetics , Reproducibility of Results , Drug Stability
15.
Braz. J. Pharm. Sci. (Online) ; 53(1): e15177, 2017. tab, graf
Article in English | LILACS | ID: biblio-839449

ABSTRACT

Abstract In this study, conditions were optimized for development of a simple RP-HPLC method for simultaneous analysis of gatifloxacin and dexamethasone in different matrices like pharmaceuticals, human serum and urine. Good separation of gatifloxacin and dexamethasone from the induced degradation products was accomplished using C8 as stationary phase; 0.02 M phosphate buffer (pH 3.0) and methanol (42:58 v/v) as mobile phase. The concentration was measured with DAD at 270 nm. Linearity was observed in the range of 0.000040-0.000280 mol/L for gatifloxacin (r2≥0.999) and 0.000013-0.000091 mol/L for dexamethasone (r2≥0.999). Both the analyte peaks were completely separated from the peaks of induced degradation products as indicated by the peak purity index (≥0.9999 for both analytes). The optimized method is recommended to be used for concurrent analysis of gatifloxacin and dexamethasone in different matrices.


Subject(s)
Chromatography, High Pressure Liquid/methods , Drug Stability , Chromatography, Reverse-Phase/methods , Anti-Bacterial Agents/analysis , Dexamethasone/analysis , Validation Study
16.
Braz. J. Pharm. Sci. (Online) ; 53(4): e00088, 2017. tab, graf, ilus
Article in English | LILACS | ID: biblio-889424

ABSTRACT

ABSTRACT Solid dosage forms for oral use, particularly tablets, are the most highly used dosage forms in therapy because they are easily administered, have high productivity and relatively low cost and provide a more stable drug to form a semi-solid net. Numerous parameters influence the quality of the final dosage form. In this study, the dissolution profile of 20-mg prednisone tablets bioequivalent to the reference product and three test formulations were evaluated using stability testing. During the study, prednisone tablets and the active pharmaceutical ingredient (API) prednisone from two different manufacturers were characterized with respect to their physical and physicochemical properties. The results showed that the dissolution profiles of the test batches and the reference product did not retain pharmaceutical equivalence throughout all the stability study. Notably, both samples of API prednisone were of the same crystal form, and any phase transition that occurred during the study could not be attributed to dissolution variation during stability.


Subject(s)
Prednisone/administration & dosage , Drug Stability , Dissolution/analysis , Pharmaceutical Preparations/standards , Physical and Chemical Properties , Dosage
17.
Curitiba; s.n; 20161205. 96 p. ilus, tab, graf, mapas.
Thesis in Portuguese | LILACS, BDENF | ID: biblio-1037851

ABSTRACT

Este trabalho teve como objetivo identificar a ocorrência de perdas evitáveis de imunobilógicos notificadas no período de 2011 a 2015 em um município da 2ª RS - Metropolitana do Paraná. Com esta informação o seguinte passo, foi conhecer o processo de trabalho da Enfermagem nas atividades relacionadas à rede de frio de imunobiológicos na instância local (sala de vacina) assim como as estratégias de enfrentamento à estas perdas. Trata-se de um estudo de caso do tipo exploratório documental (fase I) com abordagem quantitativa, e de campo (fase II) com abordagem qualitativa com análise do discurso para compreensão dos dados. O município de Colombo foi identificado na base de dados por ter apresentado a maior quantidade de perdas evitáveis de imunobiológicos notificados no período estudado. Porém devido a transição dos sistemas de informação em imunização a maioria dos municípios não transmitiu a informação contendo as doses de vacinas desprezadas por causas evitáveis. Das ocorrências de perdas evitáveis de imunobiológicos a que mais se destacou foi a perda por validade vencida com mais de 87 mil doses desprezadas. Em campo, os dados foram obtidos por meio de entrevistas semiestruturadas aplicadas à 54 profissionais de enfermagem que exercem atividades na sala de vacinação, sendo que destes, nove são enfermeiros, 40 são técnicos de enfermagem e 5 são auxiliares de enfermagem. A análise do discurso foi realizada em três etapas, sendo que na primeira emergiram oito figuras: organização da sala de vacinas, aplicação de vacinas, quebra de frasco, falta de energia elétrica, procedimento inadequado, falha no equipamento de refrigeração, depredação do patrimônio, validade vencida. Na segunda elaboramos as frases temáticas que geraram duas grandes categorias: Processo de Trabalho e Perdas Evitáveis de Vacinas. A partir da categorização das frases temáticas podemos identificar que a perda de vacinas por validade vencida se sobressaiu em relação às demais, com relato de 46% dos entrevistados, e que segundo os profissionais, isto acontece devido ao fato do recebimento dos imunobiológicos ser com data de validade próxima ao vencimento, fator que não está sob responsabilidade da instância local. Sendo o profissional de Enfermagem responsável pelas ações de imunização, desde a conservação até a administração das vacinas, foi extremamente relevante conhecer de que forma a prática cotidiana da equipe de Enfermagem enfrenta as perdas evitáveis de imunobiológicos, tanto para análise do processo de trabalho, como para subsidiar os gestores da rede de frio no que tange a capacitação de pessoal em sala de vacinação. Neste caso, podemos observar que o processo de trabalho da equipe de Enfermagem nas salas de vacinas do município, pode não estar relacionado com o número de doses desprezadas por validade vencida. Concluímos que são necessários novos estudos neste domínio, uma vez que o mesmo é de responsabilidade integral da equipe de Enfermagem e há escassez de literatura a respeito de perdas vacinais, o que dificultou a discussão dos achados por meio de um amplo diálogo com o estado da arte.


This study objectified to identify the occurrence of preventable losses of immunobiologicals reported in the period between 2011 and 2015 in a municipality from the 2nd Metropolitan Health Region of Paraná State, Brazil. With this information, the following step was to know Nursing work process on the related activities to the cold-chain for immunobiologicals at local level (vaccination room), as well as the strategies to cope with those losses. It is an exploratory documented (phase 1) case study with quantitative approach, and qualitative field approach (phase 2) by means of discourse analysis for data understanding. The municipality of Colombo, Paraná State (Brazil) was identified in the Sistema de Informação de Apuração de Imunobiológicos (Immunobiologicals Investigation Information System) database as the one with the largest amount of preventable vaccine losses reported during the studied period. However, due to the transition of vaccination information systems, most municipalities did not report information on discarded vaccination doses for preventable causes. From the occurrences of preventable immunobiological losses, expiration date of over 87 thousand doses stood out. Field data were gathered by means of semi-structured interviews applied to 54 Nursing professionals performing tasks in the vaccination room. Among those, 9 are nurses, 40 are nursing technicians and 5 are nursing assistants. Discourse analysis was held in three steps, with 8 figures emerging from the first one: organization of the vaccination room, vaccine administration, bottle break, power outage, inadequate procedure, cooling equipment failure, facility depredation, expiration date. In the second step, we elaborated thematic phrases, which generated two large categories: Work Process and Preventable Vaccine Losses. From the categorization of the thematic phrases, we can identify that vaccine losses for expiration date stood out of the others, reported by 46% of the participants, and according to the professionals, that is due to the fact that immunobiologicals are received near the expiration date, not being under local level responsibility. As Nursing professionals are held responsible for the immunization tasks, from vaccine storage to administration, it was extremely relevant to know the way that Nursing team's daily practice copes with preventable losses of vaccines, not only for the analysis of the work process, but also for grounding cold chain managers in relation to staff qualification for the vaccination room. In this case, we can observe that Nursing team's work process in the vaccination room of the municipality may not be associated with the number of discarded doses due to the expiration date. We concluded that further studies are deemed necessary in this realm, as the Nursing team is held totally responsible, and literature is scarce on vaccine losses, which made discussion of the findings difficult for scarcity of current studies.


Subject(s)
Humans , Male , Female , Adult , Middle Aged , Vaccines , Drug Stability , Nursing , Immunization , Refrigeration
18.
Rev. cuba. farm ; 50(1)ene.-mar. 2016. ilus, tab
Article in Spanish | LILACS, CUMED | ID: biblio-844863

ABSTRACT

Introducción: el diclofenaco sódico es un derivado del ácido fenilácetico y pertenece al grupo de los antinflamatorios no esteroideos con propiedades antinflamatorios, analgésicas y antipiréticas pronunciadas. En la Farmacopea de los Estados Unidos (USP 36, 2013) aparece reportado los métodos analíticos para el control de calidad del diclofenaco sódico en el ingrediente farmacéutico activo y en las tabletas. Objetivos: evaluar el desempeño de los métodos analíticos que se emplean en el control de la calidad de cuantificación y los estudios de estabilidad del ingrediente farmacéutico activo; así como los ensayos de disolución de las tabletas de diclofenaco sódico 100 mg retard de producción nacional. Métodos: en la evaluación del desempeño del método analítico potenciométrico para la cuantificación del ingrediente farmacéutico activo se analizaron los parámetros de linealidad y de precisión (repetibilidad y precisión intermedia). Para el método cromatográfico aplicable a la cuantificación del ingrediente farmacéutico activo en el producto terminado se analizaron los parámetros de especificidad, precisión y exactitud. En el método espectrofotométrico empleado en el ensayo de disolución se tuvo en cuenta la especificidad, la precisión, la linealidad, la influencia del filtrado y la estabilidad de las soluciones analíticas. Resultados: la evaluación del desempeño realizada a los diferentes métodos analíticos, fueron satisfactorias, demostrando que son lineales, precisos y específicos en el rango de concentraciones estudiadas. Conclusiones: se demostró la confiabilidad de los métodos empleados en el control de la calidad y los estudios de estabilidad del ingrediente farmacéutico activo y de las tabletas de diclofenaco sódico 100 mg retard de producción nacional(AU)


Introduction: sodium dicloflenac is a phenylacetic acid derivate included in the non-steroidal anti-inflammatory group, with marked analgesic and antipyretic properties. The US Pharmacopeia (USP 36, 2013) reports the analytical methods for the quality control of sodium diclofenac in the active ingredient and in tablets. Objectives: to evaluate the performance of the analytical methods used in the quality control of quantitation and the stability studies of the active ingredient as well as the dissolution tests of the Cuban-made 100 mg retard sodium diclofenac. Methods: the evaluation of the performance of the potentiometric analytical method for quantitation of the active ingredient analyzed the parameters called linearity and precision (repeatability and intermediate precision). For the chromatographic method applicable to quantitation of the active ingredient in the finished product, parameters such as specificity, precision and accuracy were analyzed. The spectrophotometric method used in the dissolution test took into account specificity, precision, linearity, filtering effect and stability of the analytical solutions. Results: the evaluation of the performance of the different analytical methods was satisfactory and they proved to be linear, precise and specific in the range of studied concentrations. Conclusions: the reliability of the methods for the quality control and of the stability studies of the active ingredient and of Cuban-made 100 mg retard sodium diclofenac was demonstrated(AU)


Subject(s)
Humans , Diclofenac/therapeutic use , Spectrophotometry/methods , Tablets , Chromatography, High Pressure Liquid/methods , Drug Stability , Validation Studies as Topic
19.
IJPR-Iranian Journal of Pharmaceutical Research. 2016; 15 (1): 119-130
in English | IMEMR | ID: emr-177542

ABSTRACT

The objective of the study was to develop a simple, specific and stability-indicating HPLC method for the simultaneous determination of creatine phosphate sodium [CPS] and its related substances in pharmaceutical formulation. Separation of creatine phosphate sodium from its major process impurities and degradation products was achieved on a Hypersil BDS C18 column [250 × 4.6 mm, 5 microm] with an aqueous mobile phase containing 0.2% [w/v] tetrabutylammonium hydroxide [TAH] and 0.2% [w/v] monopotassium phosphate adjusted to pH 6.6 with orthophosphoric acid at a flow rate of 1.0 mL min-1. The analytes were detected at 210 nm. Different chromatographic parameters were carefully optimized. The relative response factors for creatine, creatinine and creatinine phosphate disodium salt relative to CPS were determined. The method has been validated with respect to solution stability, system suitability, LOD, LOQ, linearity, accuracy, precision, specificity and robustness. The validation criteria were met in all cases. The developed method was successfully applied to determine the purity of CPS in pharmaceutical formulation


Subject(s)
Chromatography, High Pressure Liquid , Drug Stability , Chemistry, Pharmaceutical
20.
Braz. j. med. biol. res ; 49(12): e5542, 2016. tab, graf
Article in English | LILACS | ID: biblio-828179

ABSTRACT

This study aimed to estimate the absorption, distribution, metabolism and excretion (ADME) properties and safety of LDT5, a lead compound for oral treatment of benign prostatic hyperplasia that has previously been characterized as a multi-target antagonist of α1A-, α1D-adrenoceptors and 5-HT1A receptors. The preclinical characterization of this compound comprised the evaluation of its in vitro properties, including plasma, microsomal and hepatocytes stability, cytochrome P450 metabolism and inhibition, plasma protein binding, and permeability using MDCK-MDR1 cells. De-risking and preliminary safety pharmacology assays were performed through screening of 44 off-target receptors and in vivo tests in mice (rota-rod and single dose toxicity). LDT5 is stable in rat and human plasma, human liver microsomes and hepatocytes, but unstable in rat liver microsomes and hepatocytes (half-life of 11 min). LDT5 is highly permeable across the MDCK-MDR1 monolayer (Papp ∼32×10-6 cm/s), indicating good intestinal absorption and putative brain penetration. LDT5 is not extensively protein-bound and is a substrate of human CYP2D6 and CYP2C19 but not of CYP3A4 (half-life >60 min), and did not significantly influence the activities of any of the human cytochrome P450 isoforms screened. LDT5 was considered safe albeit new studies are necessary to rule out putative central adverse effects through D2, 5-HT1A and 5-HT2B receptors, after chronic use. This work highlights the drug-likeness properties of LDT5 and supports its further preclinical development.


Subject(s)
Humans , Animals , Male , Female , Mice , Rats , Drug Evaluation, Preclinical , Piperazines/pharmacology , Prostatic Hyperplasia/drug therapy , Drug Stability , Permeability , Piperazines/chemistry , Piperazines/metabolism , Time Factors
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