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1.
Mol Pharm ; 21(2): 916-931, 2024 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-38235686

RESUMO

Electrospinning has become a widely used and efficient method for manufacturing nanofibers from diverse polymers. This study introduces an advanced electrospinning technique, Xspin - a multi-functional 3D printing platform coupled with electrospinning system, integrating a customised 3D printhead, MaGIC - Multi-channeled and Guided Inner Controlling printheads. The Xspin system represents a cutting-edge fusion of electrospinning and 3D printing technologies within the realm of pharmaceutical sciences and biomaterials. This innovative platform excels in the production of novel fiber with various materials and allows for the creation of highly customized fiber structures, a capability hitherto unattainable through conventional electrospinning methodologies. By integrating the benefits of electrospinning with the precision of 3D printing, the Xspin system offers enhanced control over the scaffold morphology and drug release kinetics. Herein, we fabricated a model floating pharmaceutical dosage for the dual delivery of curcumin and ritonavir and thoroughly characterized the product. Fourier transform infrared (FTIR) spectroscopy demonstrated that curcumin chemically reacted with the polymer during the Xspin process. Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) confirmed the solid-state properties of the active pharmaceutical ingredient after Xspin processing. Scanning electron microscopy (SEM) revealed the surface morphology of the Xspin-produced fibers, confirming the presence of the bifiber structure. To optimize the quality and diameter control of the electrospun fibers, a design of experiment (DoE) approach based on quality by design (QbD) principles was utilized. The bifibers expanded to approximately 10-11 times their original size after freeze-drying and effectively entrapped 87% curcumin and 84% ritonavir. In vitro release studies demonstrated that the Xspin system released 35% more ritonavir than traditional pharmaceutical pills in 2 h, with curcumin showing complete release in pH 1.2 in 5 min, simulating stomach media. Furthermore, the absorption rate of curcumin was controlled by the characteristics of the linked polymer, which enables both drugs to be absorbed at the desired time. Additionally, multivariate statistical analyses (ANOVA, pareto chart, etc.) were conducted to gain better insights and understanding of the results such as discern statistical differences among the studied groups. Overall, the Xspin system shows significant potential for manufacturing nanofiber pharmaceutical dosages with precise drug release capabilities, offering new opportunities for controlled drug delivery applications.


Assuntos
Curcumina , Nanofibras , Preparações Farmacêuticas , Curcumina/química , Ritonavir , Sistemas de Liberação de Medicamentos , Polímeros/química , Liberação Controlada de Fármacos , Nanofibras/química
2.
Chem Pharm Bull (Tokyo) ; 72(3): 298-302, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38479857

RESUMO

The current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra® as the reference formulation, and generic formulations A and B as the test formulations. Allegra®, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit® E, EUD-E), a basic polymer commonly used to mask the bitter taste of drugs. Both generic A and generic B have been known to be bioequivalent to Allegra®. The dissolution tests were conducted using a compendial paddle, with either bicarbonate (10 mM, pH 6.8) or phosphate buffer (25 mM, pH 6.8) as the dissolution media. A floating lid was employed to cover the surface of the bicarbonate buffer to prevent volatilization. Results indicated that in phosphate buffer, the dissolution profiles of Allegra and generic B significantly varied from that of generic A, whereas in the bicarbonate buffer, the dissolution profiles of Allegra, generic A, and generic B were comparable. These findings suggest that the use of bicarbonate buffer may offer a more precise prediction of human bioequivalence compared to phosphate buffer.


Assuntos
Bicarbonatos , Paladar , Terfenadina/análogos & derivados , Humanos , Polímeros , Solubilidade , Comprimidos , Fosfatos , Administração Oral , Composição de Medicamentos/métodos
3.
Nano Lett ; 23(1): 319-325, 2023 01 11.
Artigo em Inglês | MEDLINE | ID: mdl-36580275

RESUMO

Logic-in-memory (LIM) has emerged as an energy-efficient computing technology, as it integrates logic and memory operations in a single device architecture. Herein, a concept of ternary LIM is established. First, a p-type 2,7-dioctyl[1]benzothieno[3,2-b][1]benzothiophene (C8-BTBT) transistor is combined with an n-type PhC2H4-benzo[de]isoquinolino[1,8-gh]quinolone diimide (PhC2-BQQDI) transistor to obtain a binary memory inverter, in which a zinc phthalocyanine-cored polystyrene (ZnPc-PS4) layer serves as a floating gate. The contrasting photoresponse of the transistors toward visible and ultraviolet light and the efficient hole-trapping ability of ZnPc-PS4 enable us to achieve an optically controllable memory operation with a high memory window of 18 V. Then, a ternary memory inverter is developed using an anti-ambipolar transistor to achieve a three-level data processing and storage system for more advanced LIM applications. Finally, low-voltage operation of the devices is achieved by employing a high-k dielectric layer, which highlights the potential of the developed LIM units for next-generation low-power electronics.


Assuntos
Eletrônica , Indóis , Poliestirenos , Raios Ultravioleta
4.
Pharm Dev Technol ; 29(5): 517-529, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38721970

RESUMO

The present study aims to investigate the potential of the 3D printing technique to design gastroretentive floating tablets (GFTs) for modifying the drug release profile of an immediate-release tablet. A 3D-printed floating shell enclosing a captopril tablet was designed having varying number of drug-release windows. The impact of geometrical changes in the design of delivery system and thermal cross-linking of polymers were evaluated to observe the influence on floating ability and drug release. Water uptake, water insolubilization, Differential Scanning Calorimetry (DSC), and Attenuated Total Reflection-Fourier Transform Infrared Spectroscopy (ATR-FTIR) were performed to assess the degree of thermal cross-linking of polyvinyl alcohol (PVA) filament. The 3D-printed GFT9 was considered the optimized gastric floating tablet that exhibited >12 h of total floating time with zero floating lag time and successfully accomplished modified-drug release by exhibiting >80% of drug release in 8 h. The zero-order release model, with an r2 value of 0.9923, best fitted the drug release kinetic data of the GFT9, which followed a super case II drug transport mechanism with an n value of 0.95. The optimized gastric floating device (GFT9) also exhibited the highest MDT values (238.55), representing slow drug release from the system due to thermal crosslinking and the presence of a single drug-releasing window in the device.


Assuntos
Captopril , Liberação Controlada de Fármacos , Impressão Tridimensional , Comprimidos , Captopril/química , Captopril/administração & dosagem , Captopril/farmacocinética , Polímeros/química , Solubilidade , Álcool de Polivinil/química , Preparações de Ação Retardada/química , Sistemas de Liberação de Medicamentos/métodos , Varredura Diferencial de Calorimetria
5.
J Environ Manage ; 329: 117057, 2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36549056

RESUMO

In this work, spherical photocatalytic floaters were fabricated by depositing TiO2:Bi (TBi) particles on polypropylene (PP) spheres (recycled from beer cans). These particles were deposited on the sphere (TBi-sphere) by the spray coating technique and evaluated their performance for the photocatalytic degradation of 2,4,6-trichlorophenol (2,4,6-TCP) herbicide. SEM images demonstrated that the BTi powders consisted in conglomerated grains with sizes of 20-80 nm and the analysis by X-ray diffraction confirmed the presence of rutile and anatase phases in the BTi. The photocatalytic experiments showed that the TBi and TBi-sphere produced maximum degradation of 90 and 97% for 2,4,6-TCP, respectively, after 4 h under UV-Vis light. The photocatalytic powders/composites were reused 3 times and the loss of degradation efficiency was 3 and 16% for the TBi powder and TBi-sphere, respectively. This means that the TBi-sphere is more stable for the continuous degradation of the 2,4,6-TCP contaminant. The TiO2:Bi powder was compared with the commercial TiO2 (P25) and found that the TiO2:Bi powder had higher light absorption (≈42%) and higher surface area (≈105%) than the P25. Therefore, the degradation percentage for the 2,4,6-TCP was 52% higher in the sample doped with Bi. Also, scavenger experiments were carried out and found that the main oxidizing agents produced for the degradation of 2,4,6-TCP were •OH- radicals and •O2- anions. Other species such as h+ were also produced at lower amount. Hence, our results demonstrated that spherical/floatable photocatalytic composites are a viable option to remove herbicide residuals from the water, which is of interest in water-treatment-plants.


Assuntos
Herbicidas , Luz , Pós , Polipropilenos , Titânio , Água , Catálise
6.
Environ Monit Assess ; 195(10): 1251, 2023 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-37768383

RESUMO

The first study related to the characteristics of the riverine litter was carried out at the mouth of the Cimandiri River in the southern West Java to provide a national database, as mandated in the Indonesian Presidential Regulation 83/2018 concerning the handling of marine debris. We examined floating riverine litter entering the South Java Sea at Cimandiri River outlets four times between December 2020 and October 2021 using a Thomsea 1 T trawl-net. The amount of litter collected tended to rise throughout the sampling period. Daily floating riverine litter released into the South Java Sea was estimated to be 285,931 ± 133.70 items or 307 ± 192.69 kg. Our monitoring data revealed no sampling period differences in litter release into the South Java Sea with no correlation with rainfall. Our data indicate that plastics are the most single abundant type of floating riverine litter entering the South Java Sea from the Cimandiri River, accounting for 99.92% of abundance (285,701 ± 133,464.75 items per day) or 97.78% in terms of weight (300 ± 181.99 kg per day) of the total litter collected. As the Cimandiri River is one of the major rivers with an outlet in the south of Java, this land-derived litter information could be an archetype for riverine ecosystems in the nation and region.


Assuntos
Ecossistema , Rios , Indonésia , Oceano Índico , Monitoramento Ambiental , Resíduos/análise , Plásticos
7.
Pharm Res ; 39(9): 2277-2290, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35851629

RESUMO

PURPOSE: 3D printing (3DP) makes it possible to obtain systems that are not achievable with current conventional methods, one of them, sustained release floating systems. Floating systems using ricobendazole (RBZ) as a model drug and a combination of polymers were designed and obtained by melt solidification printing technique (MESO-PP). METHODS: Four different MESO-PP inks were formulated based on combinations of the polymers Gelucire 43/01 and Gelucire 50/13 in different ratios. For each of the formulated inks, physicochemical characterization was performed by thermal analysis (thermogravimetric analysis [TGA] and differential scanning calorimetry [DSC]), fourier transform infrared spectrophotometer (FTIR) and X-ray diffraction (XRD). Pharmaceutical characterization was performed by in vitro assays to determine pharmaceutically relevant parameters. These parameters were calculated by applying mathematical models developed to evaluate in vitro drug release profiles. On the other hand, a physiologically based pharmacokinetic (PBPK) model was developed to predict the in vivo performance of RBZ loaded in the different inks by determining the Cmax, and the AUC0-∞. RESULTS: By increasing the proportion of Gelucire 50/13 co-surfactant in the mixtures (the proportion in Ink 1 was 33%, while the proportion in Ink 4 was 80%), the dissolution capacity of RBZ increases substantially, decreasing flotation times. CONCLUSION: MESO-PP produced ink 1 (50% Gelucire 43/01, 25% Gelucire 50/13 and 25% RBZ), which has a zero-order release (RR = 0.180%/min) and the longest flotation time (545 ± 23 min), and in turn would produce a significant increase in oral absorption of the drug, with an AUC0-∞ 2.16-fold higher than that obtained in animals treated with RBZ loaded in conventional tablets.


Assuntos
Excipientes , Tinta , Albendazol/análogos & derivados , Animais , Preparações de Ação Retardada/química , Excipientes/química , Polímeros , Impressão Tridimensional , Tensoativos , Comprimidos
8.
Environ Res ; 215(Pt 1): 114216, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36057334

RESUMO

In this work, a floating photocatalyst was constructed by loading g-C3N4@Bi2MoO6@AgI (GBA) nanocomposite on a modified polyurethane sponge via a simple dip-coating method and applied for the inactivation of Microcystis aeruginosa under visible light. GBA ternary photocatalyst was fabricated successfully and the morphology, structure, chemical state, and optical properties were characterized systematically. The floating catalyst achieved near 100% removal efficiency of algae cells under 6 h visible light irradiation and also could be retrieved and used at least three times repeatedly. The influences of various conditions on photocatalytic performance such as loading content of nanoparticles, algae density, and concentration of natural organic matters were also studied, which revealed that the GBA floating catalyst exhibited excellent photocatalytic performance of algae removal under different conditions. Furthermore, the physiological characteristics of algae cells during the photocatalytic process, including cell morphology, membrane permeability, Zeta potential, photosynthetic system, antioxidant system, and the metabolic activity were investigated. Results confirmed that the algae cells were severely damaged during the photocatalytic inactivation and the normal physiological functions were significantly affected, which resulted in the death of algae cells at last. Finally, a possible photocatalytic inactivation mechanism of algae cells was proposed. In summary, GBA floating catalyst can effectively inactivate Microcystis aeruginosa under visible light, which confirmed the high efficiency of the novel photocatalytic algae removal technology. Meanwhile, the recyclable floating material also makes the practical application in eutrophic waters of the algae removal technology possible.


Assuntos
Microcystis , Antioxidantes , Bismuto , Catálise , Luz , Microcystis/química , Molibdênio , Poliuretanos
9.
Pharm Res ; 38(12): 2119-2127, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34931285

RESUMO

PURPOSE: The intestinal fluid pH is maintained by the bicarbonate buffer system that shows unique properties regarding drug dissolution. Nevertheless, current compendial dissolution tests use phosphate buffers. The purpose of the present study was to investigate the effect of bicarbonate and phosphate buffers on the dissolution profiles of amorphous solid dispersions (ASD) composed of ionizable polymers. METHODS: Hydroxypropylmethylcellulose acetate succinate (HPMCAS), amino methacrylate copolymer (AMC), and hydroxypropylmethylcellulose (HPMC) were employed as acidic, basic, and neutral polymers, respectively. Nifedipine (NIF) was used as a model drug. Dissolution profiles were measured in pH 6.5 bicarbonate and phosphate buffers by a mini-scale paddle dissolution test. The pH of bicarbonate buffers was maintained by the floating lid method. RESULTS: The pH change of the bicarbonate buffer was suppressed to less than + 0.25 pH for 3 h by the floating lid method. In all cases, the NIF concentration was supersaturated against the solubility of crystalline NIF. The dissolution rates of HPMCAS and AMC ASDs were 1.5 to 2.0-fold slower in the bicarbonate buffer than in the phosphate buffer when compared at the same buffer capacity. The dissolution profile of HPMC ASD was not affected by the buffer species. The higher the buffer capacity and ionic strength, the faster the dissolution rate of HPMCAS ASD. CONCLUSION: The dissolution rate of ASDs with ionizable polymers would be overestimated by using unphysiological phosphate buffer solutions. It is important to use a biorelevant bicarbonate buffer solution for dissolution testing.


Assuntos
Portadores de Fármacos/química , Nifedipino/farmacocinética , Bicarbonatos/química , Soluções Tampão , Química Farmacêutica , Liberação Controlada de Fármacos , Concentração de Íons de Hidrogênio , Metilcelulose/análogos & derivados , Metilcelulose/química , Nifedipino/administração & dosagem , Fosfatos/química , Polímeros/química , Solubilidade
10.
Environ Res ; 198: 111257, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33974837

RESUMO

Paper-TiO2-Ag2O floating photocatalysts were produced under mild condition and their photocatalytic activity for the degradation of aromatic amine under sunlight stimulant was investigated. Characterizations by Raman, XRD, XPS, DRS and PL confirmed the presence of TiO2 and Ag2O, and the morphology of the appended TiO2/Ag2O layer was probed by FE-SEM. The photocatalytic activity of the prepared samples was investigated by the degradation of aniline (AN) in water under simulated sun-light illumination and constrained conditions, i.e. non-stirring and non-oxygenation. The presence of Ag2O combined with TiO2 was shown to improve the resistance of paper to bacteria attack, thus increasing the durability of the photocatalyst. Thanks to its hydrophobic character, the paper-TiO2-Ag2O NPs can be employed as useful floating photocatalyst and can be reused in continuous cycles.


Assuntos
Celulose , Prata , Antibacterianos/farmacologia , Catálise , Titânio
11.
Sensors (Basel) ; 21(16)2021 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-34450812

RESUMO

High-density polyethylene geomembranes are employed as covers for the sewage treatment lagoons at Melbourne Water Corporation's Western Treatment Plant, to harvest the biogas produced during anaerobic degradation, which is then used to generate electricity. Due to its size, inspecting the cover for defects, particularly subsurface defects, can be challenging, as well as the potential for the underside of the membrane to come into contact with different substrates, viz. liquid sewage, scum (consolidated solid matter), and biogas. This paper presents the application of a novel quasi-active thermography inspection method for subsurface defect detection in the geomembrane. The proposed approach utilises ambient sunlight as the input thermal energy and cloud shading as the trigger for thermal transients. Outdoor laboratory-scale experiments were conducted to study the proposed inspection technique. A pyranometer was used to measure the intensity of solar radiation, and an infrared thermal camera was used to measure the surface temperature of the geomembrane. The measured temperature profile was analysed using three different algorithms for thermal transient analysis, based on (i) the cooling constant from Newton's law of cooling, (ii) the peak value of the logarithmic second derivative, and (iii) a frame subtraction method. The outcomes from each algorithm were examined and compared. The results show that, while each algorithm has some limitations, when used in combination the three algorithms could be used to distinguish between different substrates and to determine the presence of subsurface defects.


Assuntos
Polietileno , Termografia , Algoritmos , Temperatura Alta , Temperatura
12.
BMC Oral Health ; 21(1): 582, 2021 11 17.
Artigo em Inglês | MEDLINE | ID: mdl-34789214

RESUMO

BACKGROUND: The aim of our study was to evaluate the allocation of dental resources and explore access to dental care in Taiwan. In addition, we tried to understand the spatiotemporal characteristics of dental care quality and analyze the relationship between dental care quality and areas with deficiencies in dental resources. METHODS: The study used a two-step floating catchment area to calculate the dental resources accessibility and explore the spatiotemporal distributions of dental care quality. The association between dental care quality and spatial accessibility was analyzed using a spatial error model. RESULTS: Most areas with deficient dental resources and lower dental care quality were remote townships, agricultural towns, or aging towns with spatial clustering. The quality of children's preventive dental care had increased over time. Most highly urbanized areas had higher dental care quality. The quality of some dental care types such as children's preventive care and full-mouth calculous removal was associated with higher accessibility. CONCLUSIONS: Understanding the spatiotemporal distribution of both dental care accessibility and quality can assist in allocation of dental care resources. Adequate dental resources may elevate dental care quality. Suggestions include policies to balance dental resources and routinely monitor improvement in areas with deficient dental care.


Assuntos
Assistência Odontológica , Acessibilidade aos Serviços de Saúde , Área Programática de Saúde , Criança , Humanos , Análise Espacial , Taiwan
13.
Anal Biochem ; 591: 113545, 2020 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-31846620

RESUMO

Plastic waste has become a major environmental problem. An increasing number of studies investigate microplastic particles with regard to their uptake and effects in cell culture systems. Individual plastic materials vary in their molecular structure, composition, size distribution, material density, and may also differ with respect to their toxicological effects. Plastic particles with lower densities than the cell culture medium, for example polyethylene (PE), pose a particular problem for in vitro assays as they float up during the incubation and thus do not contact the cells located on the bottom of the culture dish. We thus developed a practical and easy-to-use in vitro inverse cell culture model for investigating cellular effects of floating plastic particles. Cytotoxicity tests with floating PE particles were performed to demonstrate the utility of the inverted cell model. PE particles incubated in overhead culture were cytotoxic to HepG2 cells, while under the same cultivation conditions, except for inversion, no cytotoxicity occurred. These positive results demonstrate that inverted cell culture was required to detect the effects of PE particles and underlines the necessity to adapt cell culture conditions to the physicochemical properties of particles in order to obtain a more accurate estimate of the effects of floating particles on cells.


Assuntos
Técnicas de Cultura de Células/métodos , Monitoramento Ambiental/métodos , Microplásticos/toxicidade , Poluentes Químicos da Água/toxicidade , Células Hep G2 , Humanos , Tamanho da Partícula
14.
Pharm Dev Technol ; 25(9): 1081-1089, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32654568

RESUMO

Silymarin has a short half-life (4-6 hours) which leads to necessity of frequent administration. Besides, it suffers from intestinal degradation. Thus, our study aims to formulate encapsulated floating microspheres using different polymers as HPMC, EC and a blend of them. Emulsion solvent evaporation technique was applied for preparation of microspheres. Parameters considered during preparation are drug: polymer ratio and emulsifier concentration. Selected formulations were characterized by SEM and subjected for assessment by drug entrapment efficiency, buoyancy for 12 hr, in- vitro drug release, kinetics of release and stability. In-vivo bio-equivalence study was performed using albino rabbits. Formula F24 (treatment II) exhibited high % buoyancy (73.4), higher t90 (190.7 day), high Cmax (1021.3 ng/ml) and Tmax (6 h) with a significant difference between it and treatment I (Silymarin plus) after carrying out ANOVA study. Also formula F24 exhibited MRT (hr) equal 9.44 ± 0.03 and high relative bioavailability RB% (227%), which indicates promising microspheres that could be used for effective management of liver disease.


Assuntos
Polímeros/química , Silimarina/química , Animais , Química Farmacêutica/métodos , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Emulsões/química , Microesferas , Coelhos
15.
AAPS PharmSciTech ; 21(2): 66, 2020 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-31932983

RESUMO

The purpose of this study was to investigate the potential of Bletilla striata polysaccharide (BSP, a natural glucomannan material) for the development of a gastroretentive drug delivery system for the first time. Novel BSP-based porous wafer was prepared for levofloxacin hydrochloride (LFH) delivery by combining floating, swelling, and mucoadhesion mechanisms. The influences of BSP and ethyl cellulose (EC) on drug release and mucoadhesive strength were studied by 32 factorial design. The optimized matrix was coated with polycaprolactone (PCL) electrospun membrane by electrospinning and heat treatment technology. The optimized formula (F6, coated) exhibited Q4 h of 41.20 ± 1.90%, Q8 h of 76.49 ± 1.69%, and mucoadhesive strength of 86.11 ± 1.33 gf, and its drug release profile most closely resembled the Korsmeyer-Peppas model with anomalous diffusion driving mechanism. F6 (coated) also presented excellent buoyancy, preferred swelling characteristic due to the porous structure formed by freeze-drying. Meanwhile, the internal morphology, physical state, drug-excipient compatibility, and thermal behavior were recorded. The negligible cytotoxicity of F6 (coated) was observed in human gastric epithelial cell cultures. In the in vitro antimicrobial experiment, the prepared wafer exhibited obvious bacterial inhibition zone, and due to its longer gastric retention, the wafer also performed a more effective Helicobacter pylori clearance than free LFH in vivo. Graphical abstract.


Assuntos
Sistemas de Liberação de Medicamentos , Mucosa Gástrica/metabolismo , Mananas/química , Orchidaceae/química , Poliésteres/química , Células Cultivadas , Celulose/análogos & derivados , Celulose/química , Composição de Medicamentos , Liberação Controlada de Fármacos , Humanos
16.
Chem Pharm Bull (Tokyo) ; 67(9): 992-999, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31474738

RESUMO

A three-dimensional (3D) printer is a powerful tool that can be used to enhance personalized medicine. A fused deposition modeling (FDM) 3D printer can fabricate 3D objects with different internal structures that provides the opportunity to introduce one or more specific functionalities. In this study, zero-order sustained-release floating tablet was fabricated using FDM 3D printer. Filaments comprising poorly water-soluble weak base drug, itraconazole (ITZ) and polymers (hydroxypropyl cellulose and polyvinylpyrrolidone) were prepared, and tablets with a hollow structure and different outside shell thicknesses were fabricated. In the 3D printed tablets, ITZ existed as an amorphous state and its solubility improved markedly. As the outside shell thickness of the tablet increased, drug release was delayed and floating time was prolonged. In the tablets with 0.5 mm of the upper and bottom layer thickness and 1.5 mm of the side layer thickness, holes were not formed in the tablets during the dissolution test, and the tablets floated for a long period (540 min) and showed nearly zero-order drug release for 720 min. These findings may be useful for improving the bioavailability of several drugs by effective absorption from the upper small intestine, with floating gastric retention system.


Assuntos
Itraconazol/química , Impressão Tridimensional , Comprimidos/química , Varredura Diferencial de Calorimetria , Composição de Medicamentos , Liberação Controlada de Fármacos , Cinética , Polímeros/química , Solubilidade , Difração de Raios X
17.
Cogn Process ; 20(3): 359-362, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30810927

RESUMO

The novel object recognition (NOR) tasks can be used to quantify memory function in zebrafish similarly to rodents. The development of zebrafish learning and memory tests provides a means for testing the effects of pharmacological manipulations of memory. Several authors reported on the successful application of different objects in NOR tests placed either at the bottom of test tanks or submerged into the tank water of zebrafish. This pilot study was designed to test the suitability of floating objects in NOR tests using adult zebrafish. Floating objects such as crumpled aluminum balls and pink plastic hollow pearls were found to be suitable for NOR tests when small groups of zebrafish are used as experimental animals. Adult zebrafish of both sexes were capable of distinguishing between the different colors and surface consistencies of certain floating objects. A significantly higher number of mouth-object contacts were recorded when either floating aluminum balls or floating plastic pearls were used as novel object during NOR tests.


Assuntos
Reconhecimento Psicológico , Peixe-Zebra , Animais , Feminino , Humanos , Masculino , Projetos Piloto , Percepção Visual
18.
AAPS PharmSciTech ; 21(1): 6, 2019 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-31754916

RESUMO

The aim of the study is to investigate the feasibility of fabricating FDM 3D-printed gastric floating tablets with low infill percentages and the effect of infill percentage on the properties of gastric floating tablets in vitro. Propranolol hydrochloride was selected as a model drug, and drug-loaded polyvinyl alcohol (PVA) filaments were produced by hot melt extrusion (HME). Ellipsoid-shaped gastric floating tablets with low infill percentage of 15% and 25% (namely E-15 and E-25) were then prepared respectively by feeding the extruded filaments to FDM 3D printer. Thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), and scanning electron microscopy (SEM) were employed to characterize the filaments and 3D-printed tablets, and a series of evaluations were performed to the 3D-printed tablets, including the weight variation, drug content, hardness, in vitro floating behavior, and drug release of the tablets. The SEM results showed that the drug-loaded filaments and 3D-printed tablets appeared intact without defects, and the printed tablets were composed of filaments deposited uniformly layer by layer. The model drug and the excipients were thermally stable under the process temperature of extruding and printing, with a small amount of drug crystals dispersing in the drug-loaded filaments and 3D-printed tablets. Both E-15 and E-25 could float on artificial gastric fluids without any lag time and released in a sustained manner. Compared with E-15, the E-25 presented less weight variation, higher tablet hardness, shorter floating time, and longer drug release time.


Assuntos
Portadores de Fármacos/síntese química , Excipientes/síntese química , Impressão Tridimensional , Comprimidos/síntese química , Tecnologia Farmacêutica/métodos , Varredura Diferencial de Calorimetria/métodos , Portadores de Fármacos/farmacocinética , Liberação Controlada de Fármacos , Excipientes/farmacocinética , Álcool de Polivinil/síntese química , Álcool de Polivinil/farmacocinética , Propranolol/síntese química , Propranolol/farmacocinética , Comprimidos/farmacocinética , Difração de Raios X/métodos
19.
AAPS PharmSciTech ; 20(1): 35, 2019 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-30604045

RESUMO

The main purpose of the study was to develop valsartan floating tablets (VFT) via non-effervescent technique using low density polypropylene foam powder, carbopol, and xanthan gum by direct compression. Before compression, the particulate powdered mixture was evaluated for pre-compression parameters. The prepared valsartan tablets were evaluated for post-compression parameters, swelling index, floating lag time, in vitro buoyancy studies, and in vitro and in vivo X-ray imaging studies in albino rabbits. The result of all formulations for pre- and post-compression parameters were within the limits of USP. FTIR and DSC studies revealed no interaction between the drug and polymers used. The prepared floating tablets had good swelling and floating capabilities for more than 12 h with zero floating lag time. The release of valsartan from optimized formulation NF-2 showed sustained release up to 12 h; which was found to be non-Fickian release. Moreover, the X-ray imaging of optimized formulation (NF-2) revealed that tablet was constantly floating in the stomach region of the rabbit, thereby indicating improved gastric retention time for more than 12 h. Consequently, all the findings and outcomes have showed that developed valsartan matrix tablets could be effectively used for floating drug delivery system.


Assuntos
Química Farmacêutica/métodos , Polipropilenos/síntese química , Polipropilenos/metabolismo , Valsartana/síntese química , Valsartana/metabolismo , Animais , Anti-Hipertensivos/síntese química , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/síntese química , Preparações de Ação Retardada/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos/métodos , Liberação Controlada de Fármacos , Polipropilenos/administração & dosagem , Pós , Coelhos , Estômago/diagnóstico por imagem , Estômago/efeitos dos fármacos , Estômago/fisiologia , Comprimidos , Valsartana/administração & dosagem
20.
Ceska Slov Farm ; 68(5): 183-197, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31896262

RESUMO

This review focuses on the characterization of (meth)acrylate copolymers - Eudragit®, describing their thermal treatment behaviour, possible interactions between cationic and anionic polymers, incompatibilities related to Eudragits® and their use in the pharmaceutical technology of oral tablets. In summary, Eudragit® copolymers are divided into soluble ones, insoluble ones and a combination of these two types. The combination of soluble and insoluble poly(meth)acrylate gave a new type of polymer, Eudragit® FL. In oral tablet technology, Eudragits® are widely used in matrix tablets, either alone or in combination, where they mainly provide sustained drug release. To a lesser extent, Eudragits® are used in gastroretentive systems. Moreover, Eudragits® are also of great importance in coated tablets technology, where these enteric polymers provide specific drug targeting to certain parts of the digestive tract, mainly to the small intestine or colon. Important systems such as CODESTM and MMX® technology are mentioned. Last but not least an overview table of currently available oral medicinal products on the Czech market, where at least one of the Eudragits® was used as a film-forming agent, is included.


Assuntos
Química Farmacêutica , Ácidos Polimetacrílicos/química , Comprimidos , Preparações de Ação Retardada , Solubilidade
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