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1.
Braz. J. Pharm. Sci. (Online) ; 59: e22505, 2023. tab, graf
Article in English | LILACS | ID: biblio-1439507

ABSTRACT

Abstract Natural products are considered an important source of the therapeutic arsenal currently available. Among these alternatives are the seeds of Ambrosia peruviana (altamisa), whose extract has shown an anti-inflammatory effect. The main objective of this work was to perform a preformulation study of Ambrosia peruviana seeds ethanolic extract, where the main factors that affect the physical, chemical, and pharmacological stability of the extract were evaluated, as well as a compatibility study by differential scanning calorimetry (DSC) analysis against different excipients. A dry extract was obtained by rotary evaporation of the seeds macerated with 96% ethanol. The anti-inflammatory activity was determined by measuring its effect on NO production in RAW 264.7 macrophages, stimulated with LPS. The results showed that the dry extract maintained its stability over time when stored at a temperature of 4 and 25ºC, demonstrating its biological activity, the content of phenolic compounds, and its physicochemical parameters remain practically invariable. However, when exposed to high temperatures (60 ºC) it was affected. The thermal analysis revelated that the behavior of most of the selected excipients and the dry extract was maintained, which indicates that it did not present incompatibilities, therefore they can be candidates for formulating a microemulsion.


Subject(s)
Seeds/metabolism , Asteraceae/classification , Ambrosia/adverse effects , Biological Products , Calorimetry, Differential Scanning/methods , Excipients/administration & dosage
2.
Braz. J. Pharm. Sci. (Online) ; 59: e21217, 2023. tab, graf
Article in English | LILACS | ID: biblio-1429971

ABSTRACT

Abstract Solid dispersions (SDs) of ursolic acid (UA) were developed using polyvinylpyrrolidone K30 (PVP K30) in combination with non-ionic surfactants, such as D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) or poloxamer 407 (P407) with the aim of enhancing solubility and in vitro release of the UA. SDs were investigated using a 24 full factorial design, subsequently the selected formulations were characterized for water solubility, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), particle diameter, scanning electron microscopy, drug content, physical-chemical stability and in vitro release profile. SDs showed higher UA water-solubility than physical mixtures (PMs), which was attributed by transition of the drug from crystalline to amorphous or molecular state in the SDs, as indicated by XRD and DSC analyses. SD1 (with P407) and SD2 (with TPGS) were chosen for further investigation because they had higher drug load. SD1 proved to be more stable than SD2, revealing that P407 contributed to ensure the stability of the UA. Furthermore, SD1 and SD2 increased UA release by diffusion and swelling-controlled transport, following the Weibull model. Thus, solid dispersions obtained with PVP k-30 and P407 proved to be advantageous to enhance aqueous solubility and stability of UA.


Subject(s)
Polyethylene Glycols/administration & dosage , Solubility , Poloxamer/adverse effects , Diffusion , X-Rays/adverse effects , In Vitro Techniques , Calorimetry, Differential Scanning/methods , Pharmaceutical Preparations/analysis , Microscopy, Electron, Scanning/methods
3.
Braz. J. Pharm. Sci. (Online) ; 58: e21131, 2022. tab, graf
Article in English | LILACS | ID: biblio-1420447

ABSTRACT

Abstract The study is aimed to develop a monolithic controlled matrix transdermal patches containing Metoclopramide as a model drug by solvent casting method. Eudragit L100, Polyvinylpyrrolidone K-30, and Methylcellulose were used in different ratios and Polyethylene glycol 400 added as a plasticizer. Resulting patches were evaluated for their physicochemical characters like organoleptic characters, weight variation, folding endurance, thickness, swelling index, flatness, drug content, swelling index, percentage erosion, moisture content, water vapor transmission rate and moisture uptake. Formed patches were also evaluated through Fourier transform spectroscopy (FT-IR), X-ray diffraction (XRD), Differential Scanning calorimetry (DSC) and Scanning Electron Microscopy (SEM). Results of SEM unveiled smooth surface of drug-loaded patches. In-vitro dissolution studies were conducted by using dissolution medium phosphate buffer saline pH 7.4. Effect of natural permeation enhancers was elucidated on two optimized formulations (Z4 and Z9). Different concentrations (5%-10 %) of permeation enhancers i.e. Olive oil, Castor oil and Eucalyptus oil were evaluated on Franz diffusion cell using excised abdominal rat skin. Z4-O2 (Olive oil 10%) had enhanced sustain effect and flux value (310.72) close to the desired flux value. Z4-O2 followed Higuchi release model (R2= 0.9833) with non-fickian diffusion release mechanism (n=0.612)


Subject(s)
Spectrum Analysis/methods , Oils, Volatile/analysis , Metoclopramide/agonists , X-Ray Diffraction/instrumentation , Calorimetry, Differential Scanning/methods , Microscopy, Electron, Scanning/methods
4.
São Paulo; s.n; s.n; 2022. 80 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-1415544

ABSTRACT

O objetivo deste trabalho foi preparar e caracterizar nanocarreadores via auto-organização a partir da pectina de citros e lisozima para o encapsulamento da ß-lactose. Foram estudadas três condições de interação entre os biopolímeros variando a razão molar pectina/lisozima (3:1, 2:1, 1:1, 1:2 e 1:3), o pH e o tempo de aquecimento. A confirmação da interação foi determinada por espectroscopia no infravermelho por transformada de Fourier (FTIR) e por calorimetria de varredura diferencial (DSC). Os espectros de infravermelho evidenciaram que ligações de hidrogênio foram as principais forças envolvidas na formação dos nanocarreadores e sugeriram a ausência de ß-lactose livre na superfície das nanopartículas. Os termogramas evidenciaram que as nanopartículas formadas na presença de ß-lactose têm maior estabilidade térmica do que as nanopartículas sem ß-lactose. Para ambas as formulações estudadas, na presença e na ausência de ß-lactose, a formação das nanopartículas ocorreu entre os valores de pKa e ponto isoelétrico (pI) da pectina e lisozima, respectivamente, sendo a melhor razão de interação pectina/lisozima 1:2, em pH 10, a 80 ºC por 30 min. As nanopartículas foram formadas via auto-organização e todos as partículas apresentaram distribuição de tamanho homogênea, formato esférico, diâmetro inferior a 100 nm e carga superficial negativa. A morfologia e o tamanho das partículas pouco alteraram com a incorporação da -lactose. A eficiência de encapsulação (EE) da ß-lactose foi superior a 96% para as concentrações estudadas. Ensaios preliminares in vitro, em células epiteliais de câncer de cólon (HCT-116), evidenciaram que as nanopartículas formadas são capazes de adentrar no meio intracelular, possivelmente, por via endocitose


This work aimed to prepare and characterize nanocarriers via self-assembly using citrus pectin and lysozyme for ß-lactose encapsulation. Three interaction conditions between the biopolymers were studied, varying the pectin/lysozyme molar ratio (3:1, 2:1, 1:1, 1:2 and 1:3), pH and heating time. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) determined the interaction's confirmation. The infrared spectra showed that hydrogen bonds were the main forces involved in the formation of nanocarriers and suggested the absence of free ß-lactose on the surface of the nanoparticles. The thermograms showed that nanoparticles formed in the presence of ß-lactose have greater thermal stability than nanoparticles without ß-lactose. For both formulations studied, in the presence and absence of lactose, the formation of nanoparticles occurred between the pKa and isoelectric point (pI) values of pectin and lysozyme, respectively, with the best pectin/lysozyme interaction molar ratio 1:2, at pH 10, at 80 °C for 30 min. Nanoparticles were formed via self-assembly, and all particles presented homogeneous size distribution, spherical shape, diameter less than 100 nm, and negative surface charge. The morphology and size of the particles changed little with the incorporation of ß-lactose. The encapsulation efficiency (EE) of ß-lactose was higher than 96% for the concentrations studied. Preliminary in vitro assays in colon cancer epithelial cells (HCT-116) showed that the nanoparticles formed are capable of entering the intracellular medium, possibly via endocytosis


Subject(s)
Muramidase/analysis , Pectins/analysis , Biopolymers/adverse effects , Calorimetry , Calorimetry, Differential Scanning/methods , Spectroscopy, Fourier Transform Infrared/methods , Colonic Neoplasms , Nanoparticles , Hydrogen-Ion Concentration , Lactose
5.
Braz. J. Pharm. Sci. (Online) ; 58: e18946, 2022. tab, graf
Article in English | LILACS | ID: biblio-1364411

ABSTRACT

Abstract To investigate structure-property relationship of polymer-based curcumin solid dispersion (SD), three acrylic polymers were used to formulate curcumin SD by solvent evaporation method. Curcumin Eudragit EPO SD (cur@EPO), curcumin Eudragit RS PO SD (cur@RSPO) and curcumin Eudragit RL PO SD (cur@RLPO) showed deep red, golden orange and reddish orange color, respectively. Cur@RSPO entrapped 15.42 wt% of curcumin followed by cur@RL PO and cur@EPO. FTIR spectra indicated that in cur@EPO, curcumin may transfer hydrogen to the dimethylaminoethyl methacrylate group and thus change its color to red. In contrast, curcumin may form hydrogen bonding with Eudragit RS PO and Eudragit RL. Curcumin exists in amorphous state in three SDs as proved by differential scanning calorimetry and X-Ray diffraction measurement. In vitro digestion presented that lower pH value in simulated gastric fluid (SGF) stimulates the curcumin release from cur@EPO while permeability influences the release profile in other two SDs. When in simulated intestinal fluid (SIF), first order release model governs the release behaviors of all three SDs which showed sustained release pattern. Our results are helpful to elucidate how structure of polymer may impact on the major properties of curcumin contained SD and will be promising to broaden its therapeutic applications.


Subject(s)
Polymers , Curcumin/analysis , Methods , Solvents/administration & dosage , X-Ray Diffraction/instrumentation , In Vitro Techniques/methods , Calorimetry, Differential Scanning/methods , Evaporation/classification , Spectroscopy, Fourier Transform Infrared , Color , Citrus sinensis/classification , Hydrogen-Ion Concentration
6.
Braz. J. Pharm. Sci. (Online) ; 58: e19723, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394035

ABSTRACT

Abstract Passiflora nitida Kunth, an Amazonian Passiflora species, is little studied, although the specie's high biological potential. Herein the plant's pharmacognostic characterization, extract production, antioxidant potential evaluation, and application of this extract in cosmetic products is reported. The physical chemical parameters analyzed were particle size by sieve analysis, loss through drying, extractive yield, total ash content, laser granulometry, specific surface area and pore diameter (SBET), differential scanning calorimetry, thermogravimetry (TG), and wave dispersive X-Ray fluorescence (WDXRF). Total phenol/flavonoid content, LC-MS/MS analysis, DPPH and ABTS antioxidant radical assays, cytotoxicity, melanin, and tyrosinase inhibition in melanocytes test provided evidence to determine the content of the major constituent. P. nitida dry extract provided a fine powder with mesopores determined by SBET, with the TG curve showing five stages of mass loss. The antioxidant potential ranged between 23.5-31.5 mg∙mL-1 and tyrosinase inhibition between 400-654 µg∙mL-1. The species presented an antimelanogenic effect and an inhibitory activity of cellular tyrosinase (26.6%) at 25 µg/mL. The LC-MS/MS analysis of the spray-dried extract displayed the main and minor phenolic compounds constituting this sample. The results indicate that P. nitida extract has promising features for the development of cosmetic formulations


Subject(s)
Plant Extracts/analysis , Plant Leaves/adverse effects , Cosmetics/classification , Passiflora/classification , Thermogravimetry/methods , X-Rays/adverse effects , Calorimetry, Differential Scanning/methods , Monophenol Monooxygenase/antagonists & inhibitors , Phenolic Compounds , Melanins , Antioxidants/adverse effects
7.
São Paulo; s.n; s.n; 2021. 123 p. tab, graf, ilus.
Thesis in Portuguese | LILACS | ID: biblio-1380006

ABSTRACT

Diante das exigências crescentes das agências regulatórias do mundo todo quanto à redução/eliminação de ácidos graxos trans nos alimentos industrializados, bem como da conscientização do consumidor sobre a relação entre alimentação e saúde, o desenvolvimento de alternativas mais saudáveis aos óleos parcialmente hidrogenados e a outras fontes lipídicas com alto grau de saturaçã o se faz necessário. O oleogel, um sistema composto por um óleo preso em uma rede tridimensional formada por um agente estruturante, se apresenta como uma solução promissora. Dentre os diversos agentes estruturantes, as ceras vegetais se destacam por sua excelente capacidade de gelificação de óleos. Contudo, apresentam uma desvantagem sob o aspecto sensorial, pois podem conferir cerosidade e sabor residual desagradável aos alimentos. Com o objetivo de viabilizar o uso das ceras como agentes estruturantes em oleogéis face ao seu excelente desempenho tecnológico, este projeto propõe o estudo e a aplicação de oleogéis à base de óleo de soja (SBO) estruturado com ceras de farelo de arroz (RBW) a 2 e 4 % (m/m) ou carnaúba (CBW) a 3 e 6% (m/m), isoladamente. As matérias-primas foram caracterizadas e o comportamento de gelificação de cada cera foi avaliado por análises de textura por penetração de cone, estabilidade à perda de óleo por centrifugação, energia coesiva por parâmetro de solubilidade de Hansen (HSP) e comportamento de cristalização e fusão por calorimetria exploratória diferencial (DSC). Os resultados mostraram que ambas as ceras são capazes de formar oleogéis estruturalmente estáveis, contudo, o oleogel com 2% de RBW apresentou maior firmeza a 20 °C (190,4 gf/cm2) do que o oleogel com 6% de CBW a 5 °C (186,1 gf/cm2). Ao final de 5 dias, a capacidade de retenção de óleo do oleogel preparado com RBW foi de 100% às concentrações de 2 e 4% (m/m), contra 61 e 99,3% do oleogel elaborado com CBW às concentrações de 3 e 6% (m/m), respectivamente. Esses resultados podem ser explicados pela diferença entre as energias coesivas, ou seja, do grau de interação molecular entre o solvente e o soluto de cada oleogel. De acordo com os resultados de distância, que prevê se o gel formado será forte, fraco ou se não haverá formação de gel, o soluto CBW apresentou menor interação com o óleo (3,3 MPa1/2) do que o soluto RBW (3,7 MPa1/2). Os oleogéis foram aplicados como ingredientes em diferentes formulações de cream cheese, que foram analisados quanto a diferentes parâmetros de textura e esses resultados foram comparados a uma referência comercial. Nenhuma das amostras produzidas obteve resultados de textura estatisticamente iguais aos do cream cheese comercial (CC), o que pode ser explicado pelas diferenças de formulação e processamento dos produtos. Face aos resultados para textura e estabilidade à perda de óleo dos oleogéis de RBW, este agente estruturante apresenta ria maior potencial de aplicação, porém o oleogel CBW6 obteve alta capacidade de retenção de óleo (99,3%) e quando aplicado na formulação de cream cheese (CCBW6) apresentou resultados de firmeza e espalhabilidade mais próximos da amostra de referência, feita com gordura do leite (CMF)


Given the growing demands of regulatory agencies around the world regarding the reduction/elimination of trans fatty acids in processed foods, as well as consumer awareness about the relationship between food and health, the development of healthier alternatives to partially hydrogenated oils and others lipid sources with a high degree of saturation are necessary. Oleogel, a system composed of an oil trapped in a three-dimensional network formed by a structuring agent, presents itself as a promising solution. Among the various structuring agents, vegetable waxes stand out for their excellent oil gelling capacity. However, they have a sensory disadvantage, as they can give waxy and unpleasant aftertaste to foods. Aiming at enabling the use of waxes as structuring agents in oleogels in view of their excellent technological performance, this study proposes the evaluation and application of oleogels based on soybean oil (SBO) structured with rice bran wax (RBW) at 2 and 4% (m/m) or carnauba (CBW) at 3 and 6% (m/m). The raw materials were characterized and the gelling behavior of each wax was evaluated by analysis of texture by cone penetration, stability to oil loss by centrifugation, cohesive energy by Hansen solubility parameter (HSP) and crystallization and melting behavior. by differential scanning calorimetry (DSC). The results showed that both waxes are able to form structurally stable oleogels, however, oleogel with 2% RBW showed greater firmness at 20 °C (190.4 gf/cm2) than oleogel with 6% CBW at 5° C (186.1 gf/cm2). At the end of 5 days, the oil retention capacity of oleogel prepared with RBW was 100% at concentrations of 2 and 4% (m/m), against 61 and 99.3% of oleogel prepared with CBW at concentrations of 3 and 6% (m/m), respectively. These results can be explained by the difference between the cohesive energies, that is, the degree of molecular interaction between the solvent and the solute of each oleogel. According to the distance results, which predicts if the formed gel will be strong, weak or if there will be no gel formation, the CBW solute showed less interaction with the oil (3.3 MPa1/2) than the RBW solute (3 ,7 MPa1/2). Oleogels were applied as ingredients in different cream cheese formulations, which were analyzed for different texture parameters and these results were compared to a commercial reference. None of the samples produced had texture results statistically equal to those of commercial cream cheese (CC), which can be explained by the differences in formulation and processing of the products. Given the results for texture and oil binding capacity of RBW oleogels, this structuring agent would present greater application potential, but CBW6 oleogel obtained high oil biding capacity (99.3%) and when applied in cream cheese formulation (CCBW6) showed firmness and spreadability results closer to the reference sample, made with milk fat (CMF)


Subject(s)
Chemistry, Pharmaceutical , Industrialized Foods , Food/adverse effects , Vegetables , Waxes/pharmacology , Soybean Oil/classification , Calorimetry/methods , Calorimetry, Differential Scanning/methods
8.
São Paulo; s.n; s.n; 2021. 176 p. tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-1396454

ABSTRACT

A baixa solubilidade aquosa dos insumos farmacêuticos ativos (IFA) é um grande desafio no desenvolvimento de formulações farmacêuticas, pois pode resultar em biodisponibilidade insuficiente e variável. Diversas estratégias de modificação do estado sólido dos compostos ativos, têm sido propostas para incrementar a solubilidade de fármacos pouco solúveis em água. Dentre as estratégias abordadas a ispersão sólida (DS) é uma das formas mais promissoras de aumentar a solubilidade, dissolução e a biodisponibilidade de IFAs com baixa solubilidade aquosa. O efavirenz (EFV) é um inibidor não nucleosídeo da transcriptase reversa (NNRTI) e um dos componentes da terapia antirretroviral de alta atividade (HAART), sendo parte da primeira linha de tratamento de infecções do vírus HIV tipo 1. O antirretroviral está classificado como pertencente à classe II do SCB, e exibe baixa solubilidade aquosa (solubilidade menor que 10 µg/mL) e alta permeabilidade com absorção dependente da taxa de dissolução, resultando em biodisponibilidade oral baixa e variável. A administração de fármacos pouco solúveis na forma de DS é um método atraente para aumentar a biodisponibilidade in vivo. Neste estudo, um método de triagem rápida por evaporação de solvente foi empregado para preparar DS de EFV, variando-se proporções em misturas compostas pelos carreadores, polivinilpirrolidona K-28/32 (PVP K-28/32), copovidona (CoPVP), hidroxipropilmetilcelulose ftalato (HPMCP-50, HPMCP-55 e HPMCP-55s), poloxâmero 188 (P188) e poloxâmero 407 (P407). A solubilidade das DS foi avaliada por meio do método do equilíbrio (shake-flask), onde selecionou-se os polímeros P188 e P407 que conduziram a uma elevada capacidade de saturação em meio aquoso, superior a 1.000 vezes ao fármaco puro. As propriedades físico-químicas e do estado sólido das amostras foram avaliadas por meio de calorimetria exploratória diferencial (DSC); termogravimetria (TG); espectroscopia do infravermelho com transformada de Fourier (FTIR), difratometria de raios X pelo método do pó (DRXP) e ensaios de dissolução com emprego do aparato IV USP. Os resultados de DRXP demonstraram que os carreadores P188 e P407 foram capazes de estabilizar o EFV na forma amorfa nas DS, fato esse evidenciado pela ausência de picos característicos do antirretroviral


he low aqueous solubility of the active pharmaceutical ingredient (API) is a major challenge in the development of pharmaceutical formulations as it may result in insufficient and variable bioavailability. Several strategies for modifying the solid-state of the active compounds have been proposed to increase solubility of drugs that are poorly soluble in water. Among the strategies approaches, solid dispersion (SD) is one of the most promising ways to increase solubility, dissolution and bioavailability of APIs with low aqueous solubility. Efavirenz (EFV) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and one of the components of highly active antiretroviral therapy (HAART), being part of the first line of treatment of type 1 HIV virus infections. The antiretroviral is classified as belonging to BCS class II, and exhibits low aqueous solubility (solubility less than 10 µg / mL) and high permeability with dissolution ratedependent absorption, resulting in low and variable oral bioavailability. Drug delivery of poorly aqueous soluble drugs in form SD is an appealing method to increase in vivo bioavailability. In this study, a fast screening method of solvent evaporation method was used to prepare EFV SD, varying the proportions in mixtures composed by the carriers polyvinylpyrrolidone K-28/32 (PVP K-28/32), copovidone (CoPVP), hydroxypropylmethylcellulose phthalate (HPMCP-50, HPMCP-55 e HPMCP-55s), poloxamer 188 (P188) e poloxamer 407 (P407). The solubility of the samples was evaluated by the method of equilibrium (shake-flask), wherein the polymers P188 and P407 were selected due to the capacity to promote high saturation in aqueous medium, 1,000 times superior to the pure drug. The physicochemical and solid-state properties of the samples were evaluated by differential scanning calorimetry (DSC); thermogravimetry (TG); Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD) and dissolution assays using the IV USP apparatus. The results of XRPD demonstrated that the carriers P188 and P407 were able to stabilize the EFV in amorphous form in the SD, a fact evidenced by the absence of characteristic peaks of the antiretroviral


Subject(s)
Pharmaceutical Preparations/administration & dosage , Pharmaceutical Raw Material , Dissolution , Spectrum Analysis/instrumentation , Calorimetry, Differential Scanning/methods , RNA-Directed DNA Polymerase/adverse effects , Spectroscopy, Fourier Transform Infrared , Poloxamer/analogs & derivatives , Antiretroviral Therapy, Highly Active/instrumentation , Hypromellose Derivatives/metabolism , Fourier Analysis
9.
Braz. J. Pharm. Sci. (Online) ; 56: e18575, 2020. tab, graf
Article in English | LILACS | ID: biblio-1285517

ABSTRACT

Buccal route of administration has many advantages such as improving patient compliance, bypassing the GIT and hepatic first pass effect. The objectives are to formulate mucoadhesive buccal tablet using Mefenamic acid and compatible excipients, and to evaluate the product using quality control tests and in vitro tests. The ingredients were subjected to Differential Scanning Calorimetry and Fourier Transform Infrared Spectroscopy studies for compatibility test and the results showed no interaction. Two batches of mefenamic buccal tablet were prepared. The tablet thickness and diameter are 3.75 mm and 12 mm respectively. All tablets are within the specification of +/- 5%. The in-house tablet hardness is 6.8-15kg and percent friabilation is not more than 0.8%. The disintegration test showed that all tablets disintegrated within 4 hours. The content uniformity showed that tablets are within the range of 85%-115%. The tablet weight is within the 5% range. The percent swelling is 53.83% to 58.86% and moisture absorption is 14.79% to 15.56%. The surface pH of the tablet is close to the salivary pH, which means that it would not irritate the buccal mucosa. The buccal tablet has a mucoadhesiveness of 0.196 to 0.200. There was no change in pH and size after subjecting it to stability studies in human saliva. Drug release studies showed 80.7% to 83.4% after 3 hours. Even after 3 months of subjecting the tablets to 40 ºC and 75% RH, results are within acceptable range. The results show the potential of the formulation as a mucoadhesive buccal tablet.


Subject(s)
Mefenamic Acid/analysis , Mouthwashes/analysis , Quality Control , Tablets/pharmacology , Calorimetry, Differential Scanning/methods , Spectroscopy, Fourier Transform Infrared/methods
10.
Braz. J. Pharm. Sci. (Online) ; 56: e18562, 2020. tab, graf
Article in English | LILACS | ID: biblio-1285519

ABSTRACT

The aim of present work was to investigate blends of Eudragit® NE 30D with Aquacoat® ECD using different ratios to eliminate curing effect associated with individual polymers. Propranolol HCl 10% w/w was layered onto sugar cores using 5% w/w HPMC as a binder. Drug-layered-cores were coated either with pure or blends of Aquacoat® ECD: Eudragit® NE 30D in a fluidized bed coater to obtain 20% w/w coating level. Talc 35% w/w was used as anti-tacking agent. The pellets were characterized for in vitro dissolution studies, morphology, water uptake-weight loss, osmolality and adhesion of coating after curing at 60 °C or 60 °C/75% RH for 24 h. The findings revealed that Aquacoat® ECD coated pellets showed curing effect due to further gradual coalescence of polymeric particles which resulted into better film formation upon curing. In contrast, the curing effect of Eudragit® NE 30D coated pellets was caused by decrease in adhesion of coatings after curing which provided entirely different swelling behavior of uncured (localized swelling) and cured (uniform swelling) pellets. The undesired curing effect of individual polymers was eliminated by using their blends in appropriate ratio.


Subject(s)
Polymers/analysis , /classification , Calorimetry, Differential Scanning/methods , Drug Delivery Systems/adverse effects
11.
Braz. J. Pharm. Sci. (Online) ; 56: e18414, 2020. tab, graf
Article in English | LILACS | ID: biblio-1249155

ABSTRACT

Tolmetin sodium (TS) is a powerful non-steroidal mitigating drug for the treatment of rheumatoid joint inflammation, osteoarthritis, and adolescent rheumatoid joint pain. In addition to its gastrointestinal (GIT) problems, TS has a short biological half-life (1 hr). In a trial to overcome these side effects and control the rate of (TS) release, chitosan coated alginate microspheres are recommended. A Box-Behnken experimental design was employed to produce controlled release microspheres of TS in the sodium alginate and chitosan copolymers (Alg-Ch) by emulsification internal gelation methodology. The effect of critical formulation variables namely, drug to polymer ratio (D:P ratio), speed of rotation and span 80% on drug encapsulation efficiency (% EE), drug release at the end of 2 hours (Rel2) and drug release at the end of 8 hours (Rel8) were analyzed using response surface modeling. The parameters were assessed using the F test and mathematical models containing only the significant terms were generated for each parameter using multiple linear regression analysis. The produced microspheres were spherical in shape with extensive pores at D:P ratio 1:1 and small pores at a drug to polymer ratio (D:P ratio) 1:3. Differential scanning calorimetry (DSC) affirmed the steady character of TS in microspheres and revealed their crystalline form. All formulation variables examined exerted a significant influence on the drug release, whereas the speed emerged as a lone factor significantly influencing % EE. Increasing the D: P ratio decreases the release of the drug after two and 8 hours. The increase in speed results in an increase in drug release after two and eight hours. The drug release from the microspheres followed zero order kinetics. TS Alg-Ch microspheres exhibited a significant anti-inflammatory effect on incited rat paw edema after eight hours. These results revealed that the internal gelation technique is a promising method to control TS release and eradicate GIT side effects using Alg-Ch copolymers.


Subject(s)
Tolmetin/analysis , Chitosan/analysis , Alginates/analysis , Microspheres , Calorimetry, Differential Scanning/methods , Pharmaceutical Preparations , Arthralgia/pathology , Drug Liberation , Inflammation/pathology , Joints/pathology
12.
Braz. J. Pharm. Sci. (Online) ; 54(2): e17295, 2018. tab, graf, ilus
Article in English | LILACS | ID: biblio-951945

ABSTRACT

ABSTRACT The aim of the present study was to characterize biotin-decorated docetaxel-loaded bovine serum albumin nanoparticles (DTX-BIO-BSA-NPs) and evaluate their antiproliferative activity in vitro. The particle size of prepared DTX-BIO-BSA-NPs was found to be always lower than 200 nm, with sizes of 166.9, 160.3, 159.0, 176.1 and 184.8 nm and the zeta potential was -29.51, -28.54, -36.54, -36.08 and -27.56 mV after redissolution with water for 0, 1, 2, 4 and 8 hours, respectively. The polydispersity index (PDI) was stable in the range of 0.170 - 0.178. In the in vitro drug-release study, the DTX-BIO-BSA-NPs targeted a human breast cancer cell line MCF-7 effectively. The x-ray diffraction spectrum and DSC curve of DTX-BIO-BSA-NPs suggested that docetaxel was in an amorphous or disordered crystalline phase in DTX-BIO-BSA-NPs. In vitro cytotoxicity results showed that DTX-BIO-BSA-NPs inhibits proliferation of MCF-7, SGC7901, LS-174T and A549 cells in a concentration-dependent manner after exposure to DTX-BIO-BSA-NPs for 48 hours. Taken together, these results indicate that DTX-BIO-BSA-NPs may have potential as an alternative delivery system for parenteral administration of docetaxel.


Subject(s)
Biotin , Serum Albumin, Bovine/analysis , Particle Size , In Vitro Techniques/instrumentation , Calorimetry, Differential Scanning/methods , Neoplasms/drug therapy
13.
São Paulo; s.n; s.n; 2016. 211 p. ilus, tab, graf.
Thesis in Portuguese | LILACS | ID: biblio-883757

ABSTRACT

A nistatina (NYS) é o fármaco de primeira escolha no tratamento da candidíase oral, que frequentemente acomete mais os indivíduos imunocomprometidos e pacientes com outras desordens (diabetes não tratada, neoplasias, imunodeficiências). No mercado brasileiro, a NYS é encontrada na forma de suspensão oral aquosa, onde o procedimento para sua administração consiste em bochechar o medicamento. Apesar de haver a indicação de que se mantenha o contato direto entre fármaco e a mucosa oral, na qual se encontra a Candida spp., o que aumentaria expressivamente o sucesso terapêutico, a suspensão não apresenta tal propriedade. Assim, a NYS que é fármaco com ação efetiva contra a candidíase oral, é considerada pertencente à Classe IV do Sistema de Classificação Biofarmacêutica, ou seja, apresenta baixa solubilidade e baixa permeabilidade. A baixa solubilidade pode comprometer sua disponibilidade na cavidade oral, e consequentemente, sua ação farmacológica. Diante desse quadro, o objetivo do presente trabalho foi o desenvolvimento de dispersões sólidas de NYS para o tratamento da candidíase oral, e sua posterior incorporação em gel mucoadesivo oral, favorecendo a formulação no local de ação. As dispersões sólidas são sistemas farmacêuticos, onde um fármaco pouco solúvel em água encontra-se dispersado em um carreador, no estado sólido. Os carreadores normalmente são hidrofílicos, o que permite que esses sistemas sejam empregados para aumentar a solubilidade aquosa do fármaco. Assim, foram desenvolvidas as dispersões sólidas de NYS, pelo método de eliminação do solvente, empregando como carreadores, lactose, HPMC, poloxamer 407 e poloxamer 188. Essas foram submetidas à caracterização por análise térmica, usando os ensaios de calorimetria exploratória diferencial (DSC) e termogravimetria/termogravimetria derivada (TG/DTG). Dentre essas dispersões sólidas, aquelas que se mostraram com comportamento térmico sugerindo a formação de um novo "sistema", foram analisadas por meio de ensaio de solubilidade. Dessa forma, a formulação NYS DS G2 (49) se destacou, pois apresentou maior solubilidade em água (4,484 mg/mL); em pH 5,5 (4,249 mg/mL) e em pH 7,0 (4,293 mg/mL), ou seja, houve um aumento de 1,426 vezes em água; 4,227 vezes em pH 5,5; e 2,743 vezes em pH 7,0. Essa formulação foi, por fim avaliada por difração de raio-X e espectroscopia de infravermelho com transformada de Fourier, técnicas que corroboraram com a análise térmica quanto à indicação de formação da dispersão sólida. Por sua vez, essa dispersão sólida foi incorporada em 4 bases de géis mucoadesivos de carbopol ® 934 PNF, alterando apenas a concentração do polímero (0,5; 1,0; 1,5; 2,0 %p/p). Foi observado que a liberação de NYS DS G2 (49) foi superior, quando comparada à liberação de NYS MP a partir do gel, e através do ensaio de mucoadesão, percebeu-se que os géis desenvolvidos apresentaram propriedades mucoadesivas compatíveis com relatos na literatura, independentemente da quantidade de carbopol ® empregada. As características reológicas foram distintas, e foi observado que as formulações Gel A e Gel B, que possuem menor quantidade de polímero, tiverem um indicativo de comportamento de fluido newtoniano, diferente dos demais, o que pode não ser desejado para esse tipo de forma farmacêutica tópica e semi-sólida. Ao final desse trabalho, pode-se concluir que foi possível desenvolver um sistema farmacêutico na forma de dispersão sólida com maior solubilidade que a NYS pura, e sua incorporação em uma forma farmacêutica mucoadesiva, e que a liberação da NYS na forma DS foi muito superior que o fármaco na forma "convencional", o que permite que a NYS esteja mais disponível na cavidade oral, e também junto à mucosa bucal, o que levaria a efeito farmacológico mais efetivo do antifúngico


Nystatin (NYS) is the drug of first choice in the treatment of oral candidiasis that most often affect immunocompromised individuals, and patients with other disorders. In the Brazilian market, NYS is found in the form of aqueous oral suspension, a medication used in the form of mouthwash. Although there is an indication to maintain direct contact between the drug and the oral mucosa, where Candida spp. is found, as well as where therapeutic success would significantly be increased, the suspension has no such property. Thus, the NYS is an effective drug against oral candidiasis, and belongs to Class IV of the Biopharmaceutical Classification System, it has low solubility and low permeability. The low solubility can compromise its availability in the oral cavity, and consequently, its pharmacological action. Given this situation, the objective of this work was the development of solid dispersions of NYS for the treatment of oral candidiasis, and its subsequent incorporation into oral mucoadhesive gel, in order to facilitate its action. Solid dispersions are pharmaceutical systems, in which a solid drug poorly soluble in water is dispersed in a carrier. These carriers are usually hydrophilic, and this allows the systems to be employed in order to increase the aqueous solubility of the drug. Thus, the solid NYS dispersions were developed by the solvent evaporation method, employing lactose, HPMC, poloxamer 407 and poloxamer 188 as carrier. These samples were subjected to characterization by thermal analysis, using differential scanning calorimetry (DSC) and thermogravimetry / derivative thermogravimetry (TG / DTG). Among these solid dispersions, those samples which showed a specific thermal behavior suggesting the formation of new "system" were analyzed by solubility test. Thus, the NYS DS G2 formulation (49) stood out, once it showed greater solubility in water (4.484 mg/mL); at pH 5.5 (4.249 mg/mL) and pH 7.0 (4.293 mg/mL), in other words, an increase of 1,426 times in water; 4,227 times at pH 5.5; and 2,743 times at pH 7.0. This formulation was finally evaluated by X-ray diffraction, infrared spectroscopy with Fourier transform, techniques that corroborate the thermal analysis, indicating the formation of the solid dispersion. On the other hand, this solid dispersion was incorporated into 4 Carbopol ® 934 PNF mucoadhesive gels, with a variation of the polymer concentration. It was observed that NYS is improved of delivery from the gels, employing mucoadhesion test, and was also observed that the gels have mucoadhesive properties consistent with reports in the literature. However, the rheological characteristics are different, and it was observed that the Gel A and Gel B formulations, which has a lower amount of polymer behaved as a Newtonian fluid, which may not be desired for this type of topical gel. As conclusion, it was possible to develop a pharmaceutical system in the form of solid dispersion with greater solubility than the pure NYS, and their incorporation in a mucoadhesive dosage form and the release of NYS as DS was far superior wherein the drug in the "conventional" manner, which allows the NYS is longer available in the oral cavity, and also adjacent to the buccal mucosa, leading to more effective pharmacological effect of the antifungal agent


Subject(s)
Candidiasis, Oral/drug therapy , Nystatin/analysis , Solubility , Thermogravimetry/methods , Calorimetry, Differential Scanning/methods , Spectroscopy, Fourier Transform Infrared/instrumentation , Differential Thermal Analysis/instrumentation
14.
Braz. j. pharm. sci ; 52(2): 239-250, Apr.-June 2016. tab, graf
Article in English | LILACS | ID: lil-795002

ABSTRACT

ABSTRACT The objective of this research was to design a new colon-targeted drug delivery system based on chitosan. The properties of the films were studied to obtain useful information about the possible applications of composite films. The composite films were used in a bilayer system to investigate their feasibility as coating materials. Tensile strength, swelling degree, solubility, biodegradation degree, Fourier transform infrared spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning electron microscope (SEM) investigations showed that the composite film was formed when chitosan and gelatin were jointly reacted jointly. The results showed that a 6:4 blend ratio was the optimal chitosan/gelatin blend ratio. In vitro drug release results indicated that the Eudragit- and chitosan/gelatin-bilayer coating system prevented drug release in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF). However, the drug release from a bilayer-coated tablet in SCF increased over time, and the drug was almost completely released after 24 h. Overall, colon-targeted drug delivery was achieved by using a chitosan/gelatin complex film and a multilayer coating system.


RESUMO O objetivo desta pesquisa foi planejar um novo sistema de liberação de fármacos direcionado ao cólon, utilizando quitosana. Estudaram-se as propriedades dos filmes a fim de obter informações úteis sobre a aplicação desses filmes compósitos. Utilizaram-se os filmes compósitos em sistema de bicamada para investigar a sua viabilidade como materiais de revestimento. Estudos de resistência à tração, grau de intumescimento, solubilidade, grau de biodegradação, no infravermelho por transformada de Fourier (FTIR), de calorimetria diferencial de varredura (DSC) e de microscopia eletrônica de varredura (SEM) mostraram que o filme compósito se formou quando a quitosana e a gelatina reagiram entre si. Os resultados mostraram que a mistura de proporção ótima foi de 6:4 de quitosana:gelatina. Resultados da liberação do fármaco in vitro indicaram que o sistema de revestimento de Eudragit e bicamada de quitosana/gelatina impediu a liberação de fármaco em fluido intestinal simulado (SIF) e em fluido gástrico simulado (SGF). Entretanto, a liberação de fármaco do comprimido revestido em bicamada no SCF aumentou ao longo do tempo e o fármaco foi quase completamente liberado após 24 h. Em geral, se obteve a forma de liberação dirigida ao cólon, utilizando filme complexo de quitosana/gelatina e sistema de revestimento multicamada.


Subject(s)
Hydrocortisone/pharmacokinetics , Colon/drug effects , Tablets/pharmacokinetics , Calorimetry, Differential Scanning/methods , Microscopy, Electron, Scanning/methods , Spectroscopy, Fourier Transform Infrared/methods , Chitosan/pharmacokinetics
15.
Rev. cuba. farm ; 49(1)ene.-mar. 2015. ilus, tab
Article in Spanish | LILACS, CUMED | ID: lil-770992

ABSTRACT

Introducción: el desarrollo de medicamentos transdérmicos manifiesta gran interés en los últimos años debido a las ventajas que ofrece; sin embargo, muchos de los sistemas desarrollados utilizan componentes solubles lo cual podría llevar a una ineficacia terapéutica si la matriz polimérica del sistema se solubiliza muy rápido, por ello se ensayan polímeros insolubles que permitan modular la liberación de un ingrediente farmacéuticamente activo. Objetivo: evaluar la liberación de pravastatina sódica en matrices poliméricas insolubles de quitosan/PF-127 con el método de paleta sobre disco para obtener su perfil cinético de liberación, con la finalidad de proponerse como matrices viables para la elaboración de parches transdérmicos. Métodos: se realizaron estudios de contenido químico, diámetro y espesor de las películas, calorimetrías de barrido diferencial y estudios de liberación. La cuantificación del principio activo se realizó mediante espectrofotometría UV-Vis a 238 nm. Resultados: se obtuvieron parches transdérmicos con buena uniformidad de contenido, espesor, diámetro, con una buena estabilidad en base a los estudios de calorimetría. El uso de PF-127 incrementó o retardó la liberación de pravastatina de la matriz polimérica dependiendo de su concentración y al realizarse los perfiles cinéticos de liberación las formulaciones se ajustaron a una cinética de orden 0 que describe el comportamiento de algunos sistemas transdérmicos. Conclusiones: los resultados manifiestan la posibilidad de usar esta matriz polimérica insoluble de quitosana con PF-127 para modular la liberación de pravastatina sódica y de fármacos con estructura similar a la misma por vía transdérmica, lo que generará de esta manera nuevas alternativas a las formas farmacéuticas orales para el tratamiento de padecimientos y enfermedades(AU)


Introduction: the development of transdermal drugs has aroused great interest in recent years due to their advantages, however many of the drug delivery systems use soluble matrix components which could trigger therapeutic problems due to a rapid release of the active ingredient. Therefore, insoluble polymers are being tested that can modulate the release of a pharmaceutically active ingredient. Objective: to evaluate the release of pravastatin sodium in insoluble polymer chitosan/PF-127 matrices by VER to obtain kinetic profile of release in order to submit them as viable systems for the manufacture of transdermal patches. Methods: studies on the chemical content, diameter and thickness of films, differential scanning calorimetry and release studies were performed. The UV-Vis spectrophotometry at 238 nm allowed quantitating the active principle. Results: transdermal patches with adequate uniform drug content, suitable thickness and diameter with good stability, based on calorimetric studies, were obtained. The use of PF-127 increased or delayed the release of pravastatin sodium from the polymeric matrix depending on concentration. When performing the kinetic profiles of release, the formulations were regulated to zero kinetic that describes the behavior of some transdernal systems. Conclusions: the results demonstrated the possibility of using these insoluble polymer chitosan/PF-127 matrices to modulate the release of pravastin sodium and of other structurally similar drugs, thus creating new alternatives to existing pharmaceutical oral forms for treatment of diseases(AU)


Subject(s)
Humans , Male , Female , Pravastatin/therapeutic use , Drug Delivery Systems/methods , Chitosan , Chitosan/therapeutic use , Transdermal Patch , Calorimetry, Differential Scanning/methods , Mexico
16.
Rev. cuba. farm ; 47(1): 51-56, ene.-mar. 2013.
Article in Spanish | LILACS | ID: lil-674110

ABSTRACT

Introducción: en la primera etapa de preformulación de un medicamento se seleccionan los excipientes y es importante la realización de los estudios de compatibilidad química entre el ingrediente activo farmacéutico (IFA) y excipientes. Una de las técnicas más rápidas para realizar dichos estudios es la Calorimetría diferencial de barrido (DSC), y como técnica complementaria la Termogravimetría (TG). Objetivo: empleando DSC y TG, se realiza un estudio de compatibilidad química entre IFA y excipientes preseleccionados, para comprobar la existencia o no de interacción química. Métodos: el equipo empleado fue el TA3000Mettler, aco­plado a la celda DSC20 y al horno TG50. El IFA utilizado fue Piracetam, y los excipientes: Kollidon VA 64, Estearato de magnesio, Celulosa microcristalina, Polietilenglicol 20 000 y Aerosil. Dichos excipientes se caracterizaron por DSC al igual que el IFA, al cual se le detectó la transición física de fusión. Para el estudio de compatibilidad se prepararon mezclas físicas binarias en una relación de concentración 1:1 Resultados: la figura 1 muestra la detección del punto de fusión por DSC del IFA. Se obtuvieron dos transiciones endotérmicas, comprobándose por TG cuál era la de fusión. La figura 2 muestra los termogramas de las mezclas formadas entre IFA y excipientes. Conclusiones: no se detectó aparición de nuevos picos, por lo que se infiere que no hay incompatibilidad química entre las sustancias estudiadas y se recomienda el uso de los excipientes para el desarrollo de la formulación farmacéutica


Introduction: the first phase of the drug preformulation comprises the selection of excipients and the conduction of studies on chemical compatibility between pharmacologically active ingredient and the excipients. One of the quickest techniques is the differential scanning calorimetry and the supplementary technique called thermogravimetic analysis. Objective: to conduct a chemical compatibility study of the pharmacologically active ingredient and of the preselected excipients by using differential scanning calorimentry (DSC) and thermogravimetric analysis (TG), in order to confirm the chemical interaction between them. Methods: this study used the thermal analysis equipment TA 3000 Mettler, coupled with the DSC 20 cell and the TG50 oven. The pharmacologically active ingredient was Piracetam and the excipients were Aerosil Kollidon VA64, magnesium stearate, microcrystalline cellulose, Polyethylene glycol 20 000. The differential scanning calorimetry characterized the excipients and the pharmacologically active ingredient as well, whose physical fusion transition was determined. Some binary physical mixtures with a concentration ratio of 1:1 were prepared to study compatibility. Results: figure 1 showed the pharmacologically active ingredient´s fusion point detection. Two endothermal transitions were determined as well as the fusion transition by the TG equipment. Figure 2 showed the thermograms of mixtures between pharmacologically active ingredient and excipients. Conclusions: the occurrence of new peaks was bit detected, so it was inferred from this study that there was no chemical incompatibility between the studied substances, and the excipients are recommended for the development of the final pharmaceutical formulation


Subject(s)
Drug Incompatibility , Piracetam , Calorimetry, Differential Scanning/methods
17.
Rev. cuba. farm ; 45(1): 43-49, ene.-mar. 2011.
Article in Spanish | LILACS | ID: lil-584564

ABSTRACT

Como parte de la pre-estabilidad de la preformulación de auranofin tabletas, se realizó un estudio de compatibilidad química, para lo cual se emplearon técnicas de análisis térmico como la calorimetría diferencial de barrido y la termogravimetría. Previo a dichos estudios se caracterizó térmicamente por calorimetría diferencial de barrido el principio activo y cada uno de los excipientes. Posteriormente se procedió a la realización del estudio de compatibilidad química, mediante la preparación de mezclas físicas binarias entre el principio activo y cada uno de los excipientes. Se detectó por ambos métodos que el principio activo tuvo una transición física de fusión, no reportada en la literatura, lo que permitió poder calcular su pureza por calorimetría diferencial de barrido. Mediante la técnica calorimétrica fue posible inferir la ausencia de incompatibilidad química entre el principio activo y los excipientes estudiados. Además, mediante el cálculo de la energía de activación se estableció el siguiente orden de estabilidad térmica: auranofin:PVP> auranofin:lactosa> auranofin:explotab> auranofin:estearato> auranofin:aerosil> auranofin:celulosa, por lo que se recomienda el uso de estos excipientes en la elaboración de la formulación farmacéutica


As part of the pre-stability study of the Auranofin tablet pre-formulation, a chemical compatibility study was conducted using thermal analysis techniques such as the differential scanning calorimetry and the thermogravimetry. Prior to these studies, the active principle and each of the excipients were thermally characterized with the aid of the differential scanning calorimetry. Then, there proceeded to carry out the chemical compatibility study by preparing binary physical mixtures between the active principle and each of the excipients. Both methods showed that the active principle had a melting physical transition, not reported in the literature, which allowed calculating its purity aided by the differential scanning calorimetry. It was possible to infer from the calorimetry technique that there was not chemical incompatibility between the active principle and the studied excipients. By means of the activation energy estimation, the following order of thermal stability was set: Auranofin:PVP> Auranofin: lactose> Auranofin:explotab> Auranofin:estearate> Auranofin:aerosil> Auranofin:celullose. The use of these excipients was recommended for the preparation of the pharmaceutical formulation


Subject(s)
Auranofin/analysis , Auranofin/therapeutic use , Drug Stability , Thermogravimetry/methods , Calorimetry, Differential Scanning/methods
18.
Rev. cuba. farm ; 44(4): 512-518, oct.-dic. 2010.
Article in Spanish | LILACS | ID: lil-584555

ABSTRACT

En el presente trabajo se aplicó una de las técnicas más representativas que conforman el análisis térmico, la calorimetría diferencial de barrido, para estudiar la compatibilidad entre el extracto seco de Rhizophora mangle L y distintos excipientes preseleccionados para la obtención de formulaciones a partir de esta especie vegetal. Se obtuvo como resultado la no interacción química entre el extracto vegetal seco y los excipientes


In present paper authors applied one of the more representative techniques conforming the thermal analysis, the differential scanning clometry to study the compatibility among the Rhizophora mangle L dry extract and different excipients selected to obtain the formulae from this vegetal species. As result, it was possible to obtain the non-chemical interaction between the dry vegeral extract and the excipients ones


Subject(s)
Rhizophoraceae/chemistry , Technology, Pharmaceutical/methods , Calorimetry, Differential Scanning/methods , Differential Thermal Analysis
19.
Rev. cuba. farm ; 44(3): 354-359, jul.-sep. 2010.
Article in Spanish | LILACS | ID: lil-584535

ABSTRACT

El D-002, ingrediente activo antioxidante extraído de la cera de abejas Apis mellifera, fue caracterizado desde el punto de vista físicoquímico, de igual forma se analizó su interacción con excipientes de interés farmacéutico. El D-002 es un polvo fluido inodoro de color blanco a crema, con pérdidas por secado £ 1 por ciento; es insoluble en agua y etanol, y muy ligeramente soluble en otros disolventes orgánicos. Su composición, determinada por cromatografía de gases, fue: 1-tetracosanol (6-15 por ciento), 1-hexacosanol (7-20 por ciento), 1-octacosanol (12-20 por ciento), 1-triacontanol (25-35 por ciento) 1-dotriacontanol (18-25 por ciento) y 1-tetratriacontanol (£ 7,5 por ciento), para una pureza ³ 85 por ciento. Fue estable durante 5 años en la zona climática IV y su análisis por calorimetría diferencial de barrido mostró 2 transiciones de fusión a 59,0 y 81,1 ºC sin descomposición, una alta estabilidad térmica hasta 200 ºC, así como la ausencia de interacciones con lactosa, almidón, croscarmelosa sódica, polivinil pirrolidona, celulosa microcristalina y estearato de magnesio, lo que posibilita el empleo de estos excipientes en la formulación de las tabletas


The D002, an antioxidant active ingredient extracted from the Apis mellifera bees wax was characterized from the physicochemical point of view analyzing its interaction with excipients of pharmaceutical interest. The D-002 is a creamy white odourless fluid powder with losses by £ 1 percent dry; it is water and ethanol insoluble and very slightly soluble in other organic solvents. Its composition, determined by gas chromatography was: 1-tetracosanol (6-15 percent), 1-hexacosanol (7-20 percent), 1-octacosanol (12-20 percent), 1-triacontanol (25-35 percent, 1-dotriacontanol (18-25 percent) and 1-tetratriacontaol (£ 7,5 percent) for ³ 85 percent of purity. It remained stable during 5 years in the IV climatic zone and its analysis by differential scanning calorimetry showed 2 fusion transitions at 59,0 and 81,1 ºC. without decomposition, a high thermal stability up to 200 ºC, as well as a lack of interactions with lactose, starch, sodium croscarmelosa, polyvinylpyrrolidone, microcrystalline cellulose, and magnesium stearate allowing the use of these excipients in tablets formula


Subject(s)
Bees/analysis , Thermogravimetry/methods , Calorimetry, Differential Scanning/methods
20.
Rev. biol. trop ; 57(3): 567-588, sep. 2009. ilus, graf, tab
Article in Spanish | LILACS | ID: lil-637893

ABSTRACT

Velvet worm taxonomy from Santander, Colombia and thermogravimetry, differential scanning calorimetry and infrared spectroscopy of the adhesive secretion (Onychophora: Peripatidae). Onychophoran worms are terrestrial organisms that have changed relatively little since the mid-Cambrian. We collected Macroperipatus geagy in coffee plantations at "Hacienda El Roble", Santander, Colombia, and here redescribe the species based on 15 individuals. A digital three-dimensional reconstruction of the ventral side of the body indicates that the primary and accessory papillae lack a defined distribution pattern. Diagnostic characters: one main tooth and one accessory tooth in the outer jaw, and one main tooth, one accessory tooth and seven denticles in the internal jaw. Measurements: length (X=45.66 mm; SD=26.10), weight (X= 0.95 g; SD= 2.21) and number of lobopods (X= 28.13 pairs; SD= 1.30). We present a taxonomic key for six species of Macroperipatus. The liquid adhesive secretion lost 60% of the initial weight at 70 oC (solid: 13% close to 90 oC). The stability phase of the liquid secretion was within 90-280 oC (100 oC -205 oC in the solid secretion). The starting degradation temperature of the sample was 355 oC. Heat flow changes in the solid and liquid secretions were confirmed by the sample behavior during thermogravimetric analysis. The percentage of β sheets calculated by infrared spectrum was 59%. In comparison with Nephila spiders, the onychophoran secretion lost more weight and entered the phase of degradation at lower temperatures. This secondary structure of proteins gives the onychophoran adhesive secretion a tensile strength and extensibility similar to those of the silk produced by spiders for prey-capture. Rev. Biol. Trop. 57 (3): 567-588. Epub 2009 September 30.


Redescribimos taxonómicamente el gusano Macroperipatus geagy Bouvier 1899, a partir de 15 especímenes recolectados en los cafetales de hacienda El Roble, Santander, Colombia. De acuerdo con la reconstrucción en tres dimensiones de la superficie dorsal del cuerpo, las papilas primarias y accesorias de M. geagy se distribuyen sin formar un patrón determinado. Características diagnósticas: un diente accesorio y un diente principal en la mandíbula externa; y un diente principal, un diente accesorio y siete dentículos en la sierra de la mandíbula interna. Cuerpo: longitud (X=45.66; S=26.10 mm), peso (X= 0.95; S= 2.21) y pares de lobopodos (X= 28.13; S= 1.30). Se elaboró una clave para seis especies de Macroperipatus. La secreción adhesiva en estado líquido perdió 60% del peso inicial al alcanzar los 70 ºC, la muestra sólida perdió el 13% del peso cerca de los 90 ºC, la fase de estabilidad térmica de la secreción estuvo entre los 90 y 280 ºC en la secreción líquida y entre los 100 y 205 ºC en la sólida. La temperatura de inicio de la degradación de las muestras se registró a los 355 ºC. En comparación con la araña Nephila sp., el onicóforo perdió mayor porcentaje de peso y alcanzó la fase de degradación a temperaturas más bajas. Los cambios en el flujo de calor en la secreción adhesiva sólida y líquida de M. geagy fueron confirmados con el comportamiento de las muestras en el análisis de termogravimetría. La proporción de láminas beta calculado en el espectro infrarrojo de la secreción adhesiva fue del 59%. La presencia de este tipo de conformación de la estructura secundaria de las proteínas en la secreción adhesiva de M. geagy conferiría extensibilidad y resistencia a la tracción, en similitud con las fibras de seda tejidas por las arañas para depredación.


Subject(s)
Animals , Bodily Secretions/chemistry , Invertebrates/classification , Colombia , Calorimetry, Differential Scanning/methods , Invertebrates/anatomy & histology , Invertebrates/physiology , Spectrophotometry, Infrared/methods , Thermogravimetry/methods
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