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1.
Ceska Slov Farm ; 71(5): 190-199, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36443024

RESUMEN

Films are thin, flexible, and transparent wound dressings. They can be prepared from both synthetic and natural materials. In practice, synthetic polyurethane dominates, but research is mainly focused on substances of natural origin. An endogenous substance with excellent filmforming properties, which is involved in the wound healing process, is collagen. However, collagen films themselves have weak mechanical properties, which can be improved by, among other things, combining collagen with other materials. Such material could be carboxymethylcellulose, which has been shown to affect wound healing positively. Films consisting only of CMC also have weak mechanical properties, so combining both materials seems to be a suitable solution to the given problems, and a wound dressing with many beneficial properties for wound healing could be created. Therefore, our experiment aimed to prepare composite films for wound therapy consisting of a combination of collagen and CMC. The films were prepared by the solvent evaporation method, and their properties were compared with those formed only by CMC. In both cases, films with suitable organoleptic, physicochemical, and application properties for wound therapy were produced. The composite films showed lower absorption capacity and better mechanical resistance compared to those formed only by CMC. The combination of collagen and CMC in composite films intended for wound therapy has thus resulted in improved properties of the resulting dressing and holds potential for further research.


Asunto(s)
Vendajes , Carboximetilcelulosa de Sodio , Colágeno , Cicatrización de Heridas , Poliuretanos
2.
AAPS PharmSciTech ; 21(6): 230, 2020 Aug 10.
Artículo en Inglés | MEDLINE | ID: mdl-32779033

RESUMEN

The vaginal rings research is almost exclusively focused on rings for human medicine, although the dosage form offers improvement of therapeutic effect in other mammals as well. This contribution studied an effect of varying dimension parameters (diameter 20, 30 or 40 mm; height 3, 4 or 5 mm; width of annulus 5, 7.5 or 10 mm) on mechanical properties and dissolution behaviour of silicone vaginal rings with constant drug amount, intended for use in dogs. Results showed that altering dimensions influenced mechanical properties (compressive force, tensile strength and resistance of removal thread), in vitro drug release and water uptake. The removal thread resistance was increasing with increasing height and width. Compression force was higher for the rings with smaller diameter. The total drug release was increasing with decreasing height and rising diameter, surface area and water uptake during dissolution test. The initial dissolution rate was slower for the rings with higher width. As the best candidate for use in model dog subjects, the ring with 30 mm diameter, 3 mm height and 7.5 mm width was found. These drug-free vaginal rings were further tested in in vivo safety study. The results did not show any major deviation from the physiological conditions. Graphical abstract.


Asunto(s)
Dispositivos Anticonceptivos Femeninos , Animales , Perros , Liberación de Fármacos , Femenino , Fenómenos Mecánicos , Solubilidad , Resistencia a la Tracción , Pruebas de Toxicidad
3.
Ceska Slov Farm ; 69(1): 24-32, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32460507

RESUMEN

Currently, nerve agents are often used in terrorist attacks or assassinations. In such cases, it is necessary to detect them quickly, accurately and easily right in the field. Detection tubes, which are small devices containing pellets with immobilized cholinesterase and detection reagents, meet these conditions. Their detection mechanism is based on a highly sensitive enzymatic Ellman reaction, when in the absence of cholinesterase inhibitors the pellets develop a visible yellow color, whereas in their presence the carriers retain the original color. The rate of reaction, its sensitivity and the distinct color transition are the key points of the research. In this experiment, double-coated pellets were prepared. The first coating contained the butyrylcholinesterase immobilized in hypromellose, while the second coating consisted of ethylcellulose and triethyl citrate. Based on the properties of such carriers, samples containing lactose dispersed in the ethylcellulose coating were also prepared, which was expected to have an effect on increasing the permeability of the coating and hence the detection rate and color intensity. In addition to selected physicochemical properties, carriers were evaluated for enzyme activity, sensitivity and color transition intensity. Samples showing the best properties were subjected to a 24-months stability test at three different temperatures and humidity.


Asunto(s)
Butirilcolinesterasa/química , Celulosa/análogos & derivados , Inhibidores de la Colinesterasa/aislamiento & purificación , Enzimas Inmovilizadas/química
4.
Ceska Slov Farm ; 68(2): 69-77, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31331176

RESUMEN

Currently, the method of external ionic gelation for the preparation of alginate particles is successfully used not only in the field of pharmacy and medicine, but also especially in the field of biotechnology. Therefore, the preparation of alginate particles and their subsequent evaluation using principal component analysis was the key task of our experiment. To optimize this method, we focused on the evaluation of the effect of formulation (the polymer concentration, the hardening solution concentration) and process parameters (the outer diameter of the injection needle) on the properties of the resulting beads (yield, sphericity factor, equivalent diameter and swelling capacity at pH 6). Using multivariate data analysis, the major influence on the resulting properties of the prepared particles was confirmed only in sodium alginate concentration. Obtained results verified the reliable and safe potential of the external ionic gelation for preparation alginate-based particulate dosage forms.


Asunto(s)
Alginatos/química , Cobre/química , Polímeros , Análisis de Componente Principal
5.
Biopharm Drug Dispos ; 38(8): 458-463, 2017 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-28670738

RESUMEN

Maintaining a stable glycaemia in diabetes mellitus type 1 requires flexible insulin administration and carbohydrate intake to affected individuals. In real life, there might be some situations limiting the insulin-sugar balance control, e.g. night sleep or prolonged sporting activities. Glucose pellets with a pre-determined time lag between the pellet administration and glucose release were developed to mimic a 'snack eaten in advance'. In this article, a 13 C-glucose breath test was introduced to translate laboratory dissolution testing to clinical confirmation of the glucose release pattern using 5% δ abundance to differentiate the appearance of in 13 C exhaled breath. An independent two-sample t-test (p = 0.20) confirmed an average clinical lag time of 300 min and an in vitro time of 338 min to be identical at a level of significance of α = 0.05. Moreover, using the same statistical method, the clinical tmax (564 min) and the in vitro t50 (594 min) were also considered identical (p = 0.34). It was concluded that dissolution testing is a relevant method to determine the time lags of dosage forms with controlled release of glucose and that the 13 C-glucose breath test is a suitable clinical tool for lag time verification in clinical studies.


Asunto(s)
Pruebas Respiratorias , Glucosa/química , Glucosa/farmacocinética , Adulto , Cápsulas , Isótopos de Carbono/farmacocinética , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Liberación de Fármacos , Femenino , Glucosa/administración & dosificación , Humanos , Masculino , Persona de Mediana Edad
6.
Molecules ; 22(12)2017 Nov 23.
Artículo en Inglés | MEDLINE | ID: mdl-29168747

RESUMEN

Biorelevant dissolution instruments represent an important tool for pharmaceutical research and development. These instruments are designed to simulate the dissolution of drug formulations in conditions most closely mimicking the gastrointestinal tract. In this work, we focused on the optimization of dissolution compartments/vessels for an updated version of the biorelevant dissolution apparatus-Golem v2. We designed eight compartments of uniform size but different inner geometry. The dissolution performance of the compartments was tested using immediate release caffeine tablets and evaluated by standard statistical methods and principal component analysis. Based on two phases of dissolution testing (using 250 and 100 mL of dissolution medium), we selected two compartment types yielding the highest measurement reproducibility. We also confirmed a statistically ssignificant effect of agitation rate and dissolution volume on the extent of drug dissolved and measurement reproducibility.


Asunto(s)
Química Farmacéutica , Modelos Biológicos , Farmacocinética , Solubilidad , Simulación por Computador , Diseño de Equipo , Absorción Gastrointestinal , Tracto Gastrointestinal/metabolismo , Análisis Multivariante
7.
Pharm Dev Technol ; 22(2): 229-236, 2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-27291554

RESUMEN

CONTEXT: Mucoadhesive oral films, with their prolonged residence time at the site of application, offer a promising approach for protection of the oral lesion surface. The addition of sodium hyaluronate of different molecular weights as a second mucoadhesive polymer into the film matrix could positively influence the physico-mechanical and mucoadhesive properties of films. OBJECTIVE: The aim of this study was to investigate the formulation of a monolayered film matrix containing varying amounts of sodium hyaluronate and to test the properties of such matrices by applying different characterization methods. MATERIALS AND METHODS: Film matrix was composed of two mucoadhesive polymers, carmellose sodium and sodium hyaluronate, plasticized with glycerol. Resulting films were characterized with regard to their viscosity and physico-mechanical properties. RESULTS AND DISCUSSION: Multivariate data analysis was employed to evaluate the influence of varying amounts of mucoadhesive polymers on the main mucoadhesive oral films' properties. The lower content of sodium hyaluronate caused improvements in mechanical properties and residence time on the artificial oral mucosa, both of which are the main characteristics that determine the quality of the final product. CONCLUSIONS: The best results were obtained by samples containing carmellose sodium with a small amount of sodium hyaluronate (about 0.5% in casting dispersion).


Asunto(s)
Adhesivos/química , Carboximetilcelulosa de Sodio/química , Sistemas de Liberación de Medicamentos/métodos , Ácido Hialurónico/química , Adhesividad , Adhesivos/metabolismo , Carboximetilcelulosa de Sodio/metabolismo , Liberación de Fármacos , Glicerol/química , Glicerol/metabolismo , Humanos , Ácido Hialurónico/metabolismo , Mucosa Bucal/metabolismo , Análisis Multivariante , Absorción por la Mucosa Oral , Plastificantes/química , Plastificantes/metabolismo , Polímeros , Resistencia a la Tracción , Viscosidad
8.
AAPS PharmSciTech ; 18(4): 1242-1253, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-27474035

RESUMEN

The solubility of weakly basic drugs in passage through gastrointestinal tract leads to their pH-dependent release from extended release formulations and to lower drug absorption and bioavailability. The aim of this study was to modulate the micro-environmental pH of hypromellose/montanglycol wax matrices and to observe its influence on the release of weakly basic drug verapamil hydrochloride (VH) with a pH-dependent solubility with respect to gel layer formation and its dynamics. For this study, malic and succinic acids differing in their solubility and pKa were selected as pH modifiers. The dissolution studies were performed by the method of changing pH. Within the same conditions, pH, thickness, and penetration force of the gel layer were measured as well. From the PCA sub-model, it is evident that a higher acid concentration ensured lower gel pH and conditions for higher drug solubility, thus creating larger gel layer with smaller rigidity, resulting in higher VH release during the dissolution test. Incorporation of stronger and more soluble malic acid (100 mg/tablet) created the most acidic and the thickest gel layer through which a total of 74% of VH was released. Despite having lower strength and solubility, matrices containing succinic acid (100 mg/tablet) released a comparable 71% of VH in a manner close to zero-order kinetics. The thinner and less rigid gel layers of the succinic acid matrices allowed an even slightly faster VH release at pH 6.8 than from matrices containing malic acid. Thus acid solubility is more parametrically significant than acid pKa for drug release at pH 6.8.


Asunto(s)
Preparaciones de Acción Retardada/química , Derivados de la Hipromelosa , Ceras , Liberación de Fármacos , Geles , Concentración de Iones de Hidrógeno , Cinética , Malatos/química , Análisis Multivariante , Solubilidad , Succinatos/química , Comprimidos , Verapamilo/administración & dosificación , Verapamilo/química , Verapamilo/metabolismo
9.
Pharm Dev Technol ; 21(7): 867-874, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-26334252

RESUMEN

Patients tend to evade the occurrence of hypoglycemic episodes by excessive carbohydrate intake. Glucose pellets with delayed release in the time of the maximum effect of insulin can not only prevent hypoglycemia but also eliminate the preventive carbohydrate intake. The pellets can be administered in a mixture with semisolid food. The cores containing glucose in combination with osmotically active agents (croscarmellose sodium, carmellose sodium, polyethylene glycol, or carboxymethyl starch) were prepared by extrusion-spheronization and coated with 15% water ethylcellulose dispersion (Surelease® B NF) in Wurster column (Medipo, Havlíckuv Brod, Czech Republic) into four coating levels (12.5, 25, 35, and 50%). Mean particle size is 0.63-0.73 for cores and 0.82-0.98 for coated pellets. Cores and coated pellets have excellent or good flow properties according to Hausner ratio and Carr index. Aspect ratio ranges from 1.78 to 2.17 for cores and from 1.73 to 2.31 for coated pellets. Dissolution was performed using pH-independent method and method with continual change of pH. The suitable pH-independent release was achieved in the samples containing carboxymethyl starch or polyethylene glycol. Glucose release is enabled by a membrane rupture caused by core swelling. It can be, therefore, assumed that the glucose release profile will not be affected by food or transit time.


Asunto(s)
Preparaciones de Acción Retardada/administración & dosificación , Diabetes Mellitus/tratamiento farmacológico , Glucosa/administración & dosificación , Hipoglucemia/tratamiento farmacológico , Hipoglucemiantes/administración & dosificación , Celulosa/análogos & derivados , Celulosa/química , Química Farmacéutica/métodos , Niño , Preparaciones de Acción Retardada/química , Formas de Dosificación , Sistemas de Liberación de Medicamentos/métodos , Implantes de Medicamentos/administración & dosificación , Excipientes/química , Humanos , Tamaño de la Partícula , Polietilenglicoles/química , Solubilidad , Almidón/análogos & derivados , Almidón/química
10.
Ceska Slov Farm ; 65(1): 22-7, 2016.
Artículo en Checo | MEDLINE | ID: mdl-27118501

RESUMEN

UNLABELLED: Diabetes mellitus and its compensation are accompanied by serious complications. One of them is hypoglycaemia, which occurs in patients treated with insulin and/or certain peroral antidiabetics. Hypoglycaemic episodes can be prevented by a dosage form with controlled release of glucose. The pellet cores of four compositions and three different sizes corresponding to the diameter of extrusion screen mesh (0.6, 0.8, and 1.0 mm) were prepared for this purpose. The cores contain 75-80% of glucose combined with one of the following osmotically or swellable active agents: croscarmellose sodium (ADS), a mixture of microcrystalline cellulose and carmellose sodium Avicel RC 591 (RC), polyethylene glycol 6000 (PEG), and carboxymethyl starch (CMS). The cores were prepared by extrusion-spheronization and are intended for subsequent coating by a semipermeable membrane based on ethylcellulose. The aim of the work was to statistically evaluate the results of the physical evaluation of the pellets which were prepared and evaluated in previously published papers. The results are processed in the form of a meta-analysis using principle component analysis. The physical characteristics of the individual pellet sizes were different among themselves. Although the same compositions and manufacturing methods were used for all the pellets sizes, the cores produced through a 0.6 and 0.8 mm mesh screens showed similar properties while the properties of cores produced through a 1.0 mm mesh screen were rather different. KEY WORDS: hypoglycemia delayed release glucose principal component analysis PCA meta-analysis of data.


Asunto(s)
Composición de Medicamentos/instrumentación , Excipientes/química , Glucosa/química , Celulosa/análogos & derivados , Celulosa/química , Preparaciones de Acción Retardada/química , Tamaño de la Partícula , Polietilenglicoles/química , Análisis de Componente Principal , Almidón/análogos & derivados , Almidón/química
11.
Int J Pharm X ; 7: 100229, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38292298

RESUMEN

The technological process of production of biosimilars determines the degree of biosimilarity to the original biological drug. In particular, the focus is on the similarity of immunogenic responses. The primary endpoint of our retrospective study was to find the differences in SARS-CoV-2 antibody amount between patients treated with original adalimumab and biosimilar adalimumab MSB11022 (Idacio) and the differences in the SARS-CoV-2 antibody amount between patients treated with and without biological treatment. We collected the gender, autoimmune disease type, age, and treatment data of the patients in the outpatient clinic MEDICAL PLUS, s.r.o., Uherske Hradiste. These patients suffer from autoimmune rheumatic diseases. All patients received the mRNA vaccine (Pfizer/BioNTech - BNT162b2), with a 21-day (interquartile range, 21-24) gap between the two vaccinations. Patients receiving adalimumab were able to develop cellular immune responses after the second vaccination dose, as well as the individuals without adalimumab. In the period of 6-23 weeks after the second vaccination dose (D63 - D182), the SARS-CoV-2 antibody levels did not change significantly in the patients receiving the original adalimumab, while in the patients receiving biosimilar adalimumab a significant decrease was revealed. A statistically significant difference in the SARS-CoV-2 antibody amount between the patients without biological treatment (median: 504.3 U/mL) and with biological treatment (Original and Biosimilar - median: 47.2 and 28.2 U/mL, respectively) was confirmed on day 182. According to our observation, the effect of the treatment type on the increase/decrease of antibodies over time is dominant, while the impact of other variables (gender, methotrexate treatment, autoimmune disease type, and age) was confirmed as insignificant or minor.

12.
Eur J Pharm Sci ; 193: 106683, 2024 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-38142949

RESUMEN

Treating oral diseases remains challenging as API is quickly washed out of the application site by saliva turnover and mouth movements. In situ gels are a class of application forms that present sol-gel transition's ability as a response to stimuli. Their tunable properties are provided using smart polymers responsible for stimuli sensitivity, often providing mucoadhesivity. In this study, antimicrobial in situ gels of thermosensitive and pH-sensitive polymers loaded with silver nanoparticles were prepared and evaluated. The nanoparticles were prepared by green synthesis using Agrimonia eupatoria L. extract. According to the data analysis, the in situ gel with the most promising profile contained 15 % of Pluronic® F-127, 0.25 % of methylcellulose, and 0.1 % of Noveon® AA-1. Pluronic® F-127 and methylcellulose significantly increased the viscosity of in situ gels at 37 °C and shear rates similar to speaking and swallowing. At 20 °C, a behavior close to a Newtonian fluid was observed while being easily injectable (injection force 13.455 ±â€¯1.973 N). The viscosity of the formulation increased with temperature and reached 2962.77 ±â€¯63.37 mPa·s (37 °C). A temperature increase led to increased adhesiveness and rigidity of the formulation. The critical sol-gel transition temperature at physiological pH was 32.65 ±â€¯0.35 °C. 96.77 ±â€¯3.26 % of Ag NPs were released by erosion and dissolution of the gel after 40 min. The determination of MIC showed effect against E. coli and S. aureus (0.0625 mM and 0.5000 mM, respectively). The relative inhibition zone diameter of the in situ gel was 73.32 ±â€¯11.06 % compared to gentamicin sulfate. This work discusses the optimization of the formulation of novel antibacterial in situ gel for oromucosal delivery, analyses the impact of the concentration of excipients on the dependent variables, and suggests appropriate evaluation of the formulation in terms of its indication. This study offers a promising dosage form for local treatment of oral diseases.


Asunto(s)
Nanopartículas del Metal , Poloxámero , Poloxámero/química , Plata , Escherichia coli , Staphylococcus aureus , Temperatura , Geles/química , Metilcelulosa
13.
Pharmaceutics ; 15(2)2023 Feb 02.
Artículo en Inglés | MEDLINE | ID: mdl-36839819

RESUMEN

Inhalation is used for local therapy of the lungs and as an alternative route for systemic drug delivery. Modern powder inhalation systems try to target the required site of action/absorption in the respiratory tract. Large porous particles (LPPs) with a size >5 µm and a low mass density (usually measured as bulk or tapped) of <0.4 g/cm3 can avoid protective lung mechanisms. Their suitable aerodynamic properties make them perspective formulations for deep lung deposition. This experiment studied the effect of spray-drying process parameters on LPP properties. An experimental design of twelve experiments with a central point was realized using the Box-Behnken method. Three process parameters (drying temperature, pump speed, and air speed) were combined on three levels. Particles were formed from a D-mannitol solution, representing a perspective material for lung microparticles. The microparticles were characterized in terms of physical size (laser diffraction), aerodynamic diameter (aerodynamic particle sizer), morphology (SEM), and densities. The novelty and main goal of this research were to describe how the complex parameters of the spray-drying process affect the properties of mannitol LPPs. New findings can provide valuable data to other researchers, leading to the easy tuning of the properties of spray-dried particles by changing the process setup.

14.
Pharmaceutics ; 15(3)2023 Mar 10.
Artículo en Inglés | MEDLINE | ID: mdl-36986771

RESUMEN

Probiotics have been used in human and veterinary medicine to increase resistance to pathogens and provide protection against external impacts for many years. Pathogens are often transmitted to humans through animal product consumption. Therefore, it is assumed that probiotics protecting animals may also protect the humans who consume them. Many tested strains of probiotic bacteria can be used for individualized therapy. The recently isolated Lactobacillus plantarum R2 Biocenol™ has proven to be preferential in aquaculture, and potential benefits in humans are expected. A simple oral dosage form should be developed to test this hypothesis by a suitable preparation method, i.e., lyophilization, allowing the bacteria to survive longer. Lyophilizates were formed from silicates (Neusilin® NS2N; US2), cellulose derivates (Avicel® PH-101), and saccharides (inulin; saccharose; modified starch® 1500). They were evaluated for their physicochemical properties (pH leachate, moisture content, water absorption, wetting time, DSC tests, densities, and flow properties); their bacterial viability was determined in conditions including relevant studies over 6 months at 4 °C and scanned under an electron microscope. Lyophilizate composed of Neusilin® NS2N and saccharose appeared to be the most advantageous in terms of viability without any significant decrease. Its physicochemical properties are also suitable for capsule encapsulation, subsequent clinical evaluation, and individualized therapy.

15.
Front Vet Sci ; 10: 1196884, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37377950

RESUMEN

Introduction: Due to the intensification of fish farming and the associated spread of antimicrobial resistance among animals and humans, it is necessary to discover new alternatives in the therapy and prophylaxis of diseases. Probiotics appear to be promising candidates because of their ability to stimulate immune responses and suppress the growth of pathogens. Methods: The aim of this study was to prepare fish feed mixtures with various compositions and, based on their physical characteristics (sphericity, flow rate, density, hardness, friability, and loss on drying), choose the most suitable one for coating with the selected probiotic strain Lactobacillus plantarum R2 Biocenol™ CCM 8674 (new nom. Lactiplantibacillus plantarum). The probiotic strain was examined through sequence analysis for the presence of plantaricin- related genes. An invented coating technology based on a dry coating with colloidal silica followed by starch hydrogel containing L. plantarum was applied to pellets and tested for the viability of probiotics during an 11-month period at different temperatures (4°C and 22°C). The release kinetics of probiotics in artificial gastric juice and in water (pH = 2 and pH = 7) were also determined. Chemical and nutritional analyses were conducted for comparison of the quality of the control and coated pellets. Results and discussion: The results showed a gradual and sufficient release of probiotics for a 24-hour period, from 104 CFU at 10 mi up to 106 at the end of measurement in both environments. The number of living probiotic bacteria was stable during the whole storage period at 4°C (108), and no significant decrease in living probiotic bacteria was observed. Sanger sequencing revealed the presence of plantaricin A and plantaricin EF. Chemical analysis revealed an increase in multiple nutrients compared to the uncoated cores. These findings disclose that the invented coating method with a selected probiotic strain improved nutrient composition and did not worsen any of the physical characteristics of pellets. Applied probiotics are also gradually released into the environment and have a high survival rate when stored at 4°C for a long period of time. The outputs of this study confirm the potential of prepared and tested probiotic fish mixtures for future use in in vivo experiments and in fish farms for the prevention of infectious diseases.

16.
Pharmaceutics ; 14(2)2022 Jan 21.
Artículo en Inglés | MEDLINE | ID: mdl-35213983

RESUMEN

Orodispersible films are an innovative dosage form. Their main advantages are the application comfort and the possibility of personalization. This work aimed to evaluate the influence of different drying times on the properties of orodispersible films of various thicknesses, prepared in two different semisolid extrusion 3D printing setups. In the first experiment, drying times were dependent on the overall print time of each batch. In the second setup, the drying time was set equal according to the longest one. The evaluated parameters were films' weight uniformity, thickness, moisture content, surface pH, disintegration time, hardness, and tensile strength. Upon statistical comparison, significant differences in the moisture content were found, subsequently affecting the disintegration time. Moreover, statistically significant differences in films' mechanical properties (hardness, tensile strength) were also described, proving that moisture content simultaneously affects film plasticity and related properties. In conclusion, a mutual comparison of the manufactured orodispersible films showed that the drying time affects their physical and mechanical properties. The in-process drying setup was proved to be sufficient while allowing quicker manufacturing.

17.
Pharmaceutics ; 14(8)2022 Jul 29.
Artículo en Inglés | MEDLINE | ID: mdl-36015203

RESUMEN

Pharmaceutical technology offers several options for protecting substances from acidic environments, such as encapsulation in enteric capsules or dosage form with enteric coating. However, commercial enteric capsules do not always meet limits for pharmacopeial delayed release, and the coating process is generally challenging. Preparing small enteric batches suitable for clinical use is, therefore, an unsolved problem. This experiment offers a simple coating process of DRcapsTM capsules based on hypromellose (HPMC) and gellan gum to achieve small intestine administration. In addition, DRcapsTM capsules were compared to hard gelatin capsules to evaluate the suitability of the coating method. Both capsules were immersed in dispersions of Eudragit® S 100, Acryl-EZE®, and Cellacefate at concentrations of 10.0, 15.0, and 20.0% and dried. Coated capsules were evaluated by electron microscopy, disintegration, and dissolution test with a two-step pH change (from 1.2 to 6.8, then to 7.5) to simulate passage through the digestive tract. DRcapsTM capsules coated with Eudragit® S and Cellacefate achieved acid resistance. While samples coated with Eudragit® S released their contents within 360 min at pH 6.8 (small intestine), regardless of polymer concentration, capsules with 15.0 and 20.0% coatings of Cellacefate released content at pH 7.5 (colon) within 435 and 495 min, respectively.

18.
Pharmaceutics ; 14(4)2022 Apr 03.
Artículo en Inglés | MEDLINE | ID: mdl-35456616

RESUMEN

Collagen is essential as a physiological material in wound healing, so it is often used in wound management, mainly as a lyophilisate. Collagen also has excellent film-forming properties; unfortunately, however, its utilisation as a film wound dressing is limited because of its weak mechanical properties, especially in its wet state. For this reason, modifications or combinations with different materials are investigated. The combination of collagen with partially modified microfibrillar carboxymethylcellulose (CMC), which has not previously been described, provided a new possibility for strengthening collagen films and was the aim of this work. The collagen-CMC films based on three types of collagens, two plasticizers and two collagen. Plasticiser ratios were prepared using the solvent casting method; partially modified CMC served here as both a film-forming agent and a filler, without compromising the transparency of the films. The presence of microfibrils was confirmed microscopically by SEM. Organoleptic and physicochemical evaluation, especially in terms of practical application on wounds, demonstrated that all the samples had satisfactory properties for this purpose even after wetting. All the films retained acidic pH values even after 24 h, with a maximum of 6.27 ± 0.17, and showed a mild degree of swelling, with a maximum of about 6 after 24 h.

19.
Pharmaceutics ; 14(2)2022 Jan 21.
Artículo en Inglés | MEDLINE | ID: mdl-35213981

RESUMEN

A method of preparing tablets called liquisolid technique is currently emerging. In these formulations, an important role is played by porous carriers, which are the basic building blocks of liquisolid systems (LSSs). The most common are microcrystalline cellulose (MCC), magnesium aluminometasilicates, silica aerogels, mesoporous silicates, clays, etc. In this study, magnesium aluminometasilicate is used to prepare modified LSS formulations with plant extracts as model drugs dissolved in water (W) or ethanol (E). The modification involves drying tablets in a microwave (MW) and hot air dryer (HA) for a specified period. Powder blends and tablets were evaluated for physical properties, and their antioxidant activity (AA) was measured in a modified dissolution by ferric reducing antioxidant power assay (FRAP). PLS and ANOVA were used to compare tablets properties depending on the composition and technology. The experiment is based on a previous one, in which the plant extracts were processed into tablets using a similar method. Therefore, extending the study to include more plants and the robust statistical evaluation and comparison of the products was a procedure to justify the suitability of the presented method for a wide range of liquid plant extracts. As a result, we obtained tablets with excellent physical properties, including a short disintegration and dissolution, which is problematic in tableted extracts.

20.
Pharmaceutics ; 13(11)2021 Nov 04.
Artículo en Inglés | MEDLINE | ID: mdl-34834274

RESUMEN

Pharmaceutical technology offers various dosage forms that can be applied interdisciplinary. One of them are spherical pellets which could be utilized as a carrier in emerging second-generation detection tubes. This detection system requires carriers with high specific surface area (SSA), which should allow better adsorption of toxic substances and detection reagents. In this study, a magnesium aluminometasilicate with high SSA was utilized along with various concentrations of volatile substances (menthol, camphor and ammonium bicarbonate) to increase further the carrier SSA after their sublimation. The samples were evaluated in terms of physicochemical parameters, their morphology was assessed by scanning electron microscopy, and the Brunauer-Emmett-Teller (BET) method was utilized to measure SSA. The samples were then impregnated with a detection reagent o-phenylenediamine-pyronine and tested with diphosgene. Only samples prepared using menthol or camphor were found to show red fluorescence under the UV light in addition to the eye-visible red-violet color. This allowed the detection of diphosgene/phosgene at a concentration of only 0.1 mg/m3 in the air for samples M20.0 and C20.0 with their SSA higher than 115 m2/g, thus exceeding the sensitivity of the first-generation DT-12 detection tube.

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