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Study of Topical Ceramide Application
Kulhánková, Roksolana ; Kováčik, Andrej (advisor) ; Vraníková, Barbora (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Author: Roksolana Kulhánková Supervisor: doc. PharmDr. Andrej Kováčik, Ph.D. Title of diploma thesis: Study of topically administred ceramides The human stratum corneum (SC) is the uppermost layer of the epidermis, which is made up of several layers of corneocytes. The space between the corneocytes is filled with barrier lipids, i.e., ceramides, cholesterol, and fatty acids, which are represented in an equimolar ratio. The arrangement of intercellular lipids has a significant effect on the barrier properties of the skin. Damaged skin barrier (e.g., in atopic dermatitis) is associated with a lack of lipids in the SC lipid matrix, which is reflected in increased trans-epidermal water loss and deterioration of skin quality (e.g., severe dryness, flaking, and cracks). One of the potential ways to restore the skin barrier is the topical administration of barrier lipids, especially ceramides (Cer). The goal of this work was to study the effect of topically administered Cer (very long-chain Cer AP alone or in combination with ultra-long-chain Cer EOS) on model-damaged SC and their effect in the process of restoring barrier function. Several topically administered formulations (creams) were prepared, which...
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Effect of mesoporous carrier on the properties of hydrophilic matrix based on guar gum.
Šnajdrová, Lucie ; Vraníková, Barbora (advisor) ; Šklubalová, Zdeňka (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Mentor: doc. PharmDr. Barbora Vraníková, PhD. Consultant: Mgr. Chiazor Ugo Ogadah Student: Lucie Šnajdrová Title of Thesis: Effect of mesoporous carrier on the properties of hydrophilic matrix based on guar gum The treatment effectiveness can be significantly increased by targeting the drug delivery on a specific tissue. Therefore, colon targeting is desirable for the treatment of a range of local diseases (e.g., Crohn's disease). The drug can be delivered to the colon by various strategies while the oral route is preferred due to the patient compliance.1 The combination of several formulation strategies represents one of the most promising approaches in colon targeting. For this reason, the presented study aims at preformulation studies of liquisolid systems combined with mucoadhesive matrix systems. The presence of the silicate carrier Neusilin® US2 (NUS2) with a great absorption capacity can affect the performance of mucoadhesive polymers. Especially, mucoadhesion and swelling ability connected to the dissolution of the drug may be influenced upon preparation of these novel colon targeted drug delivery systems. Accordingly, tablets containing guar gum and NUS2 in different ratios were subjected to...
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Determination of the flowable liquid retention potential of silicates for polyethylene glycol 400 and propylene glycol
Jandáčková, Adriana ; Vraníková, Barbora (advisor) ; Svačinová, Petra (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Consultant: PharmDr. Barbora Vraníková, Ph.D. Student: Adriana Jandáčková Title of Thesis: Determination of the flowable liquid retention potential of silicates for polyethylene glycol 400 and propylene glycol Liquisolid systems are modern dosage form used to increase the bioavailability of poorly water-soluble drugs. The basic principle of liquisolid systems formulation lies in sorption of a drug in a liquid state onto a highly porous carrier which is subsequently coated with a material possessing a large surface area. This process leads to the forming of dry non- adhesive powder with properties suitable for further processing After oral administration, these systems allows elimination of dissolving as the drug is in already dissolved state. However, the ability of the powder to retain liquid while maintaining acceptable flow properties is limited. The aim of this diploma thesis was to determine the maximum amount of liquid (polyethylene glycol 400 and propylene glycol) that the powder (Veegum® HS, Veegum® F and Syloid® 244 FP) can absorb while maintaining suitable flow properties (flowable liquid retention potential). The value of flowable retention potential was established to 0.14 for Veegum® HS...
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Effect of combination of mucoadhesive polymers on the behaviour of matrix tablets in the small intestine
Janoušek, Miroslav ; Vraníková, Barbora (advisor) ; Svačinová, Petra (referee)
Charles University, Faculty of Pharmacy in Hradci Králové Department of: Pharmaceutical Technology Mentor: PharmDr. Barbora Vraníková, Ph.D. Consultant: Mgr. Chiazor Ugo Ogadah Student: Miroslav Janoušek Title of Thesis: Effect of combination of mucoadhesive polymers on the behaviour of matrix tablets in the small intestine Colon-targeted drug delivery is highly desirable due to the direct treatment of local intestinal diseases, drug dose reduction, and minimization of systemic adverse effects. This effect can be achieved by several specific drug delivery systems based on different mechanisms. Generally, the most preferred are orally administrated formulations due to the relatively easy manufacturing and high adherence of patients to treatment. These include matrix systems based on mucoadhesive polymers that allow both targeting to the desired site (e.g. colon) and controlled drug release. For the above-mentioned reasons, the aim of the presented study was to evaluate the behavior of two mucoadhesive polymers, namely guar gum (GK), hypromellose K15M (HPMC K15M) and their combinations in biorelevant media simulating small intestine fluids (FaSSIF). The viscosity of the polymer dispersions was measured using a rotational rheometer. Polymer formulations (compacts) containing the model drug...
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Study of influence of hydrophilic carriers on the solubility of a poorly soluble drug
Veselá, Eliška ; Šklubalová, Zdeňka (advisor) ; Vraníková, Barbora (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Department of Pharmaceutical Technology Supervisor: Doc. PharmDr. Zdeňka Šklubalová, Ph.D. Consultant: Mgr. Jana Brokešová Student: Eliška Veselá Title of Thesis: Study of influence of hydrophilic carriers on the solubility of a poorly soluble drug The aim of this thesis was to enhance the solubility of a poorly soluble model drug meloxicam (MLX) by preparing binary interactive mixtures with hydrophilic carriers by simple mixing and co-milling. The mixtures were characterized for granulometric properties. The dissolution studies were carried out using the USP-4 apparatus assembled with a flow-through powder cell in an open-loop system. The dissolution rate rrel (min-1 ) and the amount of released drug mrel (%) were evaluated. The observable positive effect of carriers was registerred in terms of increasing the dissolution rate and the amount of released drug for both mixed and co-milled mixtures comparing to the raw drug. Mixtures with hypromellose were the exception; the improvement of the monitored parameters was not detected.
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Study of Topical Ceramide Application
Kulhánková, Roksolana ; Kováčik, Andrej (advisor) ; Vraníková, Barbora (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Technology Author: Roksolana Kulhánková Supervisor: doc. PharmDr. Andrej Kováčik, Ph.D. Title of diploma thesis: Study of topically administred ceramides The human stratum corneum (SC) is the uppermost layer of the epidermis, which is made up of several layers of corneocytes. The space between the corneocytes is filled with barrier lipids, i.e., ceramides, cholesterol, and fatty acids, which are represented in an equimolar ratio. The arrangement of intercellular lipids has a significant effect on the barrier properties of the skin. Damaged skin barrier (e.g., in atopic dermatitis) is associated with a lack of lipids in the SC lipid matrix, which is reflected in increased trans-epidermal water loss and deterioration of skin quality (e.g., severe dryness, flaking, and cracks). One of the potential ways to restore the skin barrier is the topical administration of barrier lipids, especially ceramides (Cer). The goal of this work was to study the effect of topically administered Cer (very long-chain Cer AP alone or in combination with ultra-long-chain Cer EOS) on model-damaged SC and their effect in the process of restoring barrier function. Several topically administered formulations (creams) were prepared, which...
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Effect of mesoporous carrier on the properties of hydrophilic matrix based on hydroxypropyl methylcellulose.
Milá, Jana ; Vraníková, Barbora (advisor) ; Kováčik, Andrej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Technology Mentor: doc. PharmDr. Barbora Vraníková, Ph.D. Consultant: Mgr. Chiazor Ugo Ogadah Student: Jana Milá Title of Thesis: Effect of mesoporous carrier on the properties of hydrophilic matrix based on hydroxypropyl methylcellulose Colon targeted drug delivery has an essential role in treating local colon diseases. Various specific drug delivery systems resistant to the acidic environment of the upper gastrointestinal tract are used in the controlled drug release. In addition, higher efficacy, especially of poorly soluble drugs, can also be achieved by using mucoadhesive matrix systems in combination with liquisolid systems. Within these systems, the drug is usually dissolved and, therefore, it does not need to dissolve during release from the dosage form. The aim of the presented work was to study the effect of the mesoporous carrier Neusilin® US2 on the mucoadhesive properties and swelling rate of tablets based on hypromellose. Formulations containing the model drug theophylline, Neusilin® US2, hypromellose K15M (HPMC K15M) or their mixtures were subjected to determination of swelling and mucoadhesion strength in the environment of three biorelevant media simulating the fasted state of the stomach...
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Formulation and characterization of hydrogels for local treatment of musculoskeletal infections
Drdová, Pavlína ; Šnejdrová, Eva (advisor) ; Vraníková, Barbora (referee)
Charles University Faculty of Pharmacy in Hradec Kralove Department of Pharmaceutical Technology Author: Pavlína Drdová Title of thesis: Formulation and characterization of hydrogels for local treatement of musculoskeletal infection Supervisor: PharmDr. Eva Šnejdrová, Ph.D. Local anti-infective therapy for musculoskeletal infections eliminates systemic drug toxicity. By selecting a suitable drug delivery system, higher drug concentrations at the site of infection and sustained release can be achieved. Such a system may be gels, formulated and tested in the submitted diploma thesis. The theoretical part of the work was devoted to the description of musculoskeletal infections and their treatment, characterization of gels and their use in parenteral administration. Hydrophilic gels based on hypromellose, carrageenan, gelatin and fish gelatin containing vamcomycin hydrochloride and gentamicin sulfate were formulated. Flow and viscoelastic properties were tested on a rotational rheometer. The analysis of flow curves by the Power law model proved a non-Newtonian type of flow. The most sensitive to applied stress is a 3 % hypromellose gel, the least a dispersion of iota-carrageenan with povidone 25. Viscoelastic properties were evaluated based on elastic, viscous and complex modulus, phase angle and yield...
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Fractal aspects of sorbitol flow.
Dvořáková, Klára ; Šklubalová, Zdeňka (advisor) ; Vraníková, Barbora (referee)
The size and shape of bulk solid particles is an important factor which affects its flow and consolidation behaviour. In this thesis, the properties of sorbitol size fractions ranging from 80 to 500 µm were studied by using helium pycnometry, optical microscopy and changes in the volume of the powder bed during the initial phase of consolidation. A significant influence (p ≤ 0.01) of the sample drying on the density of solid sorbitol was detected. Porosity of sorbitol size fractions ranged from 56.6 to 62.3%; with the increasing in the particle size the porosity decreased. For the consolidation of the powder bed, the first 10 taps were critical when the volume decreased most dramatically. This is particularly evident for the size fraction of 100 µm and 158 µm.
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Evaluation of co-processed excipients intended for orodispersible tablets formulation
Vondrušková, Hana ; Svačinová, Petra (advisor) ; Vraníková, Barbora (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Co-processed excipients (CPE) can be defined as a combination of two or more substances, which are physically modified by an appropriate process (e.g. spray-drying). These excipients are currently increasingly used for production of tablets by direct compression. Due to the availability of a wide range of initial materials for their production, it is possible to obtain a large number of combinations with required characteristics and better properties than simple physical mixtures. Although the composition of these CPE may be similar, the small changes in the component's characteristics can make them behave differently after tableting. The aim of this work was a comparison of compressibility (using force- displacement record) of CPE (Starlac®, Combilac®, Cellactose 80®, DisintequikTM ODT® containing lactose and Ludiflash®, SmartEx QD 50®, SmartEx QD 100® containing mannitol) and properties of obtained tablets (tensile strength, friability, disintegration and water absorption ratio) prepared using compression pressures of 78, 130, 182 MPa. CPE containing lactose had lower values of plasticity compared with CPE containing mannitol but higher values of released elastic energy. This observation is also reflected in values of tensile strength...
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