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Study of tableting materials and tablets from spray-dried mixtures of the drug and excipients
Prejdová, Magdaléna ; Mužíková, Jitka (advisor) ; Smékalová, Monika (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Mentor: doc. PharmDr. Jitka Mužíková, Ph.D. Conzultant: Mgr. Thao Tranová Student: Magdaléna Prejdová Title of Thesis: Study of tableting materials and tablets from spray-dried mixtures of the drug and excipients This work deals with the influence of three different size fractions of spray dried powders (SDP) on flow properties and on the compressibility of tablets. The aim was to obtain orodispersible tablets with a poorly soluble drug aprepitant. Different particle sizes were obtained by different nitrogen flow rates during spray drying. The SDP were composed of aprepitant and hypromellose phthalate in a 1:2 ratio. The structure of the SDP was tested by scanning electron microscopy. SPD were part of directly compressible tabletting materials or tabletting materials made from granulates. All tablets contained the co-processed dry binder Prosolv® ODT G2, the sweetener sucralose and the lubricant magnesium stearate. The tested parameters of powders and tabletting materials were particle size and flow properties. The tablets were compressed by material testing machine the Zwick/Roell with a compression force of 2.5 kN. The compression process was evaluated by using the energy profile of the compression...
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Development of material for agar-based ultrasound brain phantom
Řehořková, Petra ; Smékalová, Monika (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical technology Mentor: Mgr. Monika Smékalová, Ph.D. Consultant: MUDr. Michael Bartoš Student: Petra Řehořková Title of Thesis: Development of material for agar-based ultrasound brain phantom This thesis is concerned with the development of a material for an agar-based ultrasound phantom that would provide skill acquisition and experience in a manner approximating real surgery. The aim is to formulate and optimize the agar hydrogel preparation procedure, evaluate its acoustic properties and water loss during storage. A dependence was found between the amount of water evaporated during storage (4 weeks at 37 řC) and the glycerol content, which slows down the water loss from the samples in direct proportion. Based on the results, an agar gel (AG) formulation with 1% agar and 60% glycerol was selected for the acoustic properties measurements. During this experiment the microbial stability of AG was confirmed. The results of acoustic parameters measurements were evaluated, namely, speed of the ultrasound, attenuation coefficient and echogenicity of the samples as a function of content of scattering particles Al2O3 and SiC. It was shown that each type of particles affects grayscale value and attenuation coefficient in a...
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Development of material for agar-based ultrasound brain phantom
Řehořková, Petra ; Smékalová, Monika (advisor) ; Holas, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical technology Mentor: Mgr. Monika Smékalová, Ph.D. Consultant: MUDr. Michael Bartoš Student: Petra Řehořková Title of Thesis: Development of material for agar-based ultrasound brain phantom This thesis is concerned with the development of a material for an agar-based ultrasound phantom that would provide skill acquisition and experience in a manner approximating real surgery. The aim is to formulate and optimize the agar hydrogel preparation procedure, evaluate its acoustic properties and water loss during storage. A dependence was found between the amount of water evaporated during storage (4 weeks at 37 řC) and the glycerol content, which slows down the water loss from the samples in direct proportion. Based on the results, an agar gel (AG) formulation with 1% agar and 60% glycerol was selected for the acoustic properties measurements. During this experiment the microbial stability of AG was confirmed. The results of acoustic parameters measurements were evaluated, namely, speed of the ultrasound, attenuation coefficient and echogenicity of the samples as a function of content of scattering particles Al2O3 and SiC. It was shown that each type of particles affects grayscale value and attenuation coefficient in a...
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Dosing of veterinary eye drops 1
Marková, Jana ; Šklubalová, Zdeňka (advisor) ; Smékalová, Monika (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical technology Consultant: doc. PharmDr. Zdeňka Šklubalová, Ph.D. Student: Jana Marková Title of Thesis: Dosing of veterinary eye drops 1. The main purpose of this thesis was to find out, whether and to what extent the rate of dispensing, the dispending angle (90ř, 65ř, 45ř) and the volume of preparation (30 ml, 15 ml, 5 ml) had effected the mass of commercial eye drops for poultry vaccination. Drops were produced manually by using conventional dispensing system (plastic 30 ml dropper bottle and dropper tip) and by using a new prototype of semi-automatic device. The drop mass increased with increasing the rate of drop formation in every examined combination of factors. With decreasing of the dispensing angle, the drop mass decreased only in a case of constant rate dropping. In all other cases, especially with volume reduction to 15 ml and 5 ml, the drop size often increased due to the wetting of hemispherical dropper tip. As a result, higher variability of drop masses had occurred. With using the semi-automated prototype, the preparation volume had no impact on the final drop mass. On the other hand, higher variability of doses was noted for studied suspension eye drops.
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Development of material for gelatin-based ultrasound brain phantom
Vaclaviková, Andrea ; Smékalová, Monika (advisor) ; Šklubalová, Zdeňka (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Supervisor: Mgr. Monika Smékalová, Ph.D. Consultant: MUDr. Michael Bartoš Student: Andrea Vaclaviková Title od thesis: Development of material for gelatin-based ultrasound brain phantom There are more aspects that have an important role in selection of material for production of single-use ultrasound brain phantom: kind of material, acoustic property, price of materials and their accessibility, simplicity in preparation and its storage requirements, time stability and further. Gelatine as a hydrogel is a proper material for imitation of biological tissues since human body is mostly formed by water what is a prerequisite for acoustic and mechanical quality. Besides that, this natural biopolymer can be available for low costs. The goal was to find suitable combinations in proportion to gelatine, crosslinker, plasticiser, and preservatives in order to create material for ultrasound brain phantom with optimal time of solidification and similar acoustic property of brain in terminal stage. The emphasis was also put on temperature and microbiological stability requirements. For this purpose, there were arranged set of samples of 5%, 7,5% and 10% of gelatine with different proportion of...
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Polymeric particles for targeted anti-inflammatory therapy
Santarius, Karolina ; Holas, Ondřej (advisor) ; Smékalová, Monika (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Mentor: PharmDr. Ondřej Holas, PhD. Consultant: Mgr. Barbora Boltnarová Student: Karolina Santarius Title of thesis: Polymeric particles for targeted anti-inflammatory therapy Macrophages are heterogenous population of cells, that play crucial role in inflammatory diseases like NASH. It was found that liver macrophages polarization into phenotype M1 is major factor in NASH progression. It seems that induced conversion from proinflammatory macrophages into anti-inflammatory is one of the potencial therapeutic target. This macrophages polarization can be achieved by drug delivery system based on drug-loaded nanoparticles. The aim of this work was to prepare and optimize the preparation of nanoparticles formulation based on polymeric nanoparticles loaded dexamethasone as model substance. The nanoparticles formulation was prepared by nanoprecipitation method using three PLGA polymers with different lactic/glycolic acid ratios. Several surfactants in various concentrations were used to optimize preparation. Prepared dexamethasone-loaded nanoparticles were characterized in terms of their size and polydisperzity index using dynamic light scattering. Zeta potencial of nanoparticles was determine by...
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Preparation of spray-dried powder containing active substance, chitosan and surfactant
Kubová, Helena ; Svačinová, Petra (advisor) ; Smékalová, Monika (referee)
7 2 ABSTRACT Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: PharmDr. Petra Svačinová, Ph.D. Student: Helena Kubová Title of Thesis: Preparation of spray-dried powder containing active substance, chitosan and surfaktant The main of this work was to prepare spray-dried powder containing meloxicam, chitosan and CTAB as surfactant. Spray drying is a method used to increase the bioavailability of poorly soluble drugs. Surfactants are substances that increase the solubility of drugs by the mechanism of micellar solubilization. Samples with different concentrations of meloxicam and constant amount of CTAB and chitosan used as a carrier were prepared. Three different temperatures, 170 řC, 190 řC and 210 řC were used for spray drying. The effectiveness of CTAB on properties of prepared particles and on the drug release from the samples was evaluated. The 1,4 mm diameter nozzle was used for spray drying. Optical microscopy and SEM were used to evaluate the appearance of prepared particles and the thermal characteristics were evaluated by DSC. The amount of drug released was evaluated using dissolution test. The particles of obtained powder had an irregular plate-like shape corresponding to chitosan particles. Spherical particles of meloxicam with CTAB...
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Preparation of oxim reactivators loaded PLGA nanoparticles
Veliu, Mimoza ; Šnejdrová, Eva (advisor) ; Smékalová, Monika (referee)
5 2 ABSTRACT Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Consultant: PharmDr. Eva Šnejdrová Ph.D. Student: Mimoza Veliu Title of Thesis: Preparation of oxim reactivators loaded PLGA nanoparticles In theoretical part the main attention is paid to polymeric nanoparticles (NP) for brain targeting. The drug properties and methods of preparation of the nanoparticles with hydrophilic drugs are presented. The part is devoted to physico-chemical properties that affect the permeability of these substances across biological barriers to the target site. The polymers used for NP preparation for brain targeting are focused. The experimental part deals with the nanoparticle formulation. Nanoparticles were prepared by double emulsion method. The method of preparation was chosen based on the drug solubility. In the W/O/W system oil phase was formed by linear copolymers of poly(lactic-co-glycolic) acid (PLGA) and its derivatives branched on polyacrylic acid (A2) or tripentaerythritol (T3). Poloxamer 407 and dimethyldidodecylammonium bromide (DDAB) were chosen for NP stabilization. The effect of the polymers on particle size was studied. The effect the polymers used, and the formulation factors on the size, polydispersity and stability of NP were studied. The concentration...
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Spray drying of chitosan suspension with different content of active substance
Plotová, Lucie ; Svačinová, Petra (advisor) ; Smékalová, Monika (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: PharmDr. Petra Svačinová, Ph.D. Student: Lucie Plotová Title of Thesis: Spray drying of chitosan suspension with different content of active substance In this work, a spray-dried suspension of chitosan with different content of active substance was evaluated. By spray drying, solid particles were formed from the suspensions of various drug concentration, which were further evaluated to assess their properties. The formed suspensions contained, in addition to chitosan, 20, 30, 40 or 50 mg of meloxicam and sodium lauryl sulphate as surfactant and were subsequently dried at 170 řC, 190 řC or 210 řC. The prepared particles were evaluated using an optical microscope and a scanning electron microscope (SEM). Furthermore, the rate and amount of released active substance were evaluated by dissolution, and the thermal properties of the particles were evaluated by differential scanning calorimetry (DSC). According to the results from the optical microscope and SEM, it was shown that the particles of the spray-dried samples formed clusters of individual particles and irregular shapes can be seen in the images. Small particles of meloxicam are visible on the surface of the platelet-shaped chitosan...
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Lyophilization of polymeric nanomaterials
Švehlíková, Ingrid ; Holas, Ondřej (advisor) ; Smékalová, Monika (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Consultant: PharmDr. Ondřej Holas, PhD. Student: Ingrid Švehlíková Title od thesis: Lyophilization of polymeric nanoparticles Lyophilization is a widely used drying method with extensive application possibilities in the drug preparation. Its importance in pharmacy is growing because it is one of the important methods of stabilizing active substances, especially proteins. A detailed understanding of the properties of the drug and the physicochemical phenomena of the individual phases of lyophilization is a basic prerequisite for the preparation of a safe, effective and stable drug. Biomedical nanoparticles as drug carriers are the type of the dosage forms in which lyophilization is also used. A series of lyophilization experiments were performed using trehalose, mannitol, dextran and xylitol as cryo and lyoprotectant. The parameters assessed were particle size, PDI, appearance and lyophilisate reconstitution. The properties of nanoparticles prepared by nanoprecipitation from PLGA polymer were evaluated. Furthermore, experiments were performed to validate the deep-freezing method as an alternative method to lyophilization for long-term storage of nanoparticles. The nanoparticles were stored in...
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