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Sublingual in vitro permeation of folic acid as a vitamin.
Špiritová, Martina ; Doležal, Pavel (advisor) ; Musilová, Marie (referee)
Diploma thesis deals with information about sublingual administration of drugs in the first part. In the context with the tested permeant briefly describes individual vitamins groups. In the second part more specifically describes folic acid in the vitamin function and possible use in prevention of the congenital evolution defects and its protective effect on the cardiovascular system. Experimental part is aimed at caffeine permeation as a marker and folic acid as model drug over sublingual membrane non-trypsinized-frozen or trypsinized. As one of the main results it can be considered measuring of the values of folic acid permeation and the effect of used type of sublingual membrane. It is possible to consider measuring of the value folic acid flux values from dispersion vehicles EM1 and EM2 to be one the second main results. In dispersion vehicle EM1 was value for sublingual non-trypsinized membrane J= 0,6 [µg /cm2 . h-1 ] ± 0,4 and for sublingual trypsinized membrane was J= 0,5 [µg /cm2 . h-1 ] ± 0,2. For dispersion vehicle EM2 sublingual non-trypsinized membrane has value J= 0,3 [µg /cm2 . h-1 ] ± 0,2 and for sublingual trypsinized membrane the same. This flux value compared with simple liquid vehicle (e.g. IPM) is low. This implies significant retardation effect of the dispersion systems. This...
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Thermal analysis of interaction of epidermal lipids V
Kaloušová, Petra ; Musilová, Marie (advisor) ; Doležal, Pavel (referee)
Thermal analysis of interaction of epidermal lipids V Petra Kaloušová, degree work , June 2009 Abstract Natural function of human skin is to protect the body from adverse influences of the surrounding. In 1950's and 70's it was discovered, that the skin barrier is situated in stratum corneum and is determined by lipids in intercellular space of that layer. Transdermal application of medicaments has many advantages compared to peroral one. On the other hand stratum corneum is a certain barrier for penetration of the medicaments. Thus we have focused on this lipid layer and its interaction with water. We have used samples prepared in vitro consisting of cholesterol, pseudoceramid and modulators of transdermal penetration. We have tried to hydrate the samples and tracked their characteristics and interactions by differential scanning calorimetry. At the same time we have evaluated the individual groups of drugs and proper experimental conditions for that particular measurement.
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Cleaning Validation Procedures in Manufacturing of Liquid Dosage Forms
Koníková, Veronika ; Doležal, Pavel (advisor) ; Vachek, Josef (referee)
The thesis preamble introduces validations of analytical methods, as an important process during pharmaceutical development and quality control in pharmaceutical manufacturing. Method validation has essential influence on pharmacoeconomics and greatly shortens the time of placing the medicament to the market. The IMS principle greatly shortens analysis time, thus ensuring economic and innovation growth for pharmaceutical companies. Experimental part of this thesis was performed on the device IONSCAN - LS Smiths- Detection, USA in the branch of the Teva company in Opava, which introduces IMS to analytical procedures validation for cleaning validation in pharmaceutical manufacturing. For measuring, the Naphazolini nitras standard was used and the Teflon dry method was applied. During the method development itself, in which I participated, the method usability range was found in the interval of mass concentrations from 0,06 - 0,80 mg / ml. The detection limit at the level of 0.02 ppm and the quantification limit at the level of 0.08 ppm were determined and linearity was verified. In the second part, I validated the analytical method for cleaning process validation. Sampling was performed by means of polyurethane swabs "Large Swab" from a metal plate of surface size 5 x 5 cm2. From this equipment, a...
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Nanofiber membranes as carriers of drugs 2. Polyvinylalcohol, chitosan, (D,L) polylactic acid.
Bidmonová, Hana ; Doležal, Pavel (advisor) ; Dittrich, Milan (referee)
1. ABSTRACT Diploma thesis concerns with the evaluation of the basic properties of the nanofibre membranes that are made of polyvinylalcohol, chitosan and (D,L) polylactic acid in connection with their possible use as carriers of drugs. Thesis characterizes electrospinning as a method of production of nonwoven textiles and nanofibre materials, polymers that were used in preparation of the nanofibre membranes under experiments, and testing methods that were used. Transdermal pharmaceuticals declared in the AISLP database were summarized in the connection with their possible use in drug administration. The selected physical characteristics of three chemical types of the nonwoven nanofibre membranes made in laboratories ELMARCO Liberec were investigated. The tensile stress properties, hydrophile-lipophile character of surface and absorption-release properties of the membranes were studied at a permeation in vitro study using caffein as a model drug in the experimental part of my work. Tensile properties of membranes are affected by previous radiation sterilization and direction of testing. General characterization of all membranes was not found. Chitosan membrane becomes firmer material after sterilization and it is also tougher in transverse tensile force. PLA membrane is weak after sterilization and also...
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Thermal analysis of interaction of epidermal lipids IV
Komárková, Radka ; Musilová, Marie (advisor) ; Doležal, Pavel (referee)
Thermal analysis of interaction of epidermal lipids IV Radka Komárková, diploma paper, June 2009 Abstract Main function of skin is protect organism in face of chemical and mechanical damage. Skin is composed of several layers, and most considerable barrier of which forges most upper part stratum corneum. Stratum corneum contains cells fill in with keratin, which are surrounded lipid matrix. Main components of lipid matrix are ceramides (50%), cholesterol (25%) and fatty acids (10%). At present are many experimental works specialized up to preperation in vitro lipid membrane and aim of our work is find out, whether concentration of water can influence hydration lipophilic components of lipid membrane. We used samples, which had constant composition lipid mixture (cholesterol : ceramid 14S24, 1:5) and they differentiated content of water (75%, 50% and 25%). This samples were remit to several cycles of cool down and warming up by the help of DSC, where was establishment only one mixed peak of lipid mixture. All samples showed out interaction with water, however sample with 25% substantiality, it was rather on limits of analytic mistake.
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Evaluation of transdermal permeability of folic acid using methylparaben as marker.
Kubíková, Kateřina ; Berka, Pavel (advisor) ; Doležal, Pavel (referee)
In the theoretical part, there is briefly described the problematic of skin in the connection with transdermal permeability of substances. This part is followed by a general summary about transdermal permeability testing. Further on there were described the basic features of methylparaben and folic acid as substances used for permeability tests. Experimental part of the diploma thesis describes the testing conditions for in vitro testing of permeability of methylparaben and folic acid from the TRIS buffer, the TRIS buffer with propylene glycol (PG) (3:2), isopropyl myristate (IPM) and isopropyl myristate (IPM) with parafin oil (PO) (2:3) through the full thickness pig ear skin. Measured values of normalized fluxes of folic acid JKLn were as follows: from TRIS buffer: 1,00 ± 0,47, RSD 46,5%; from TRIS buffer with PG: 0,28 ± 0,11, RSD 40,1%; from IPM: 0,86 ± 0,72, RSD 83,4%; from IPM and PO: 2,08 ± 3,91, RSD 188,2%. The following average ratios of folic acid normalized fluxes and methylparaben normalized fluxes JKLn/JMPn from separate donors (and their standard devations and relative standard deviations) were obtained: from TRIS buffer: 0,98 ± 0,46, RSD 46,3%; from TRIS buffer with PG: 0,18 ± 0,09, RSD 52,2%; from IPM: 0,78 ± 0,77, RSD 98,9%; from IPM and PO: 1,76 ± 2,86, RSD 162,4%. The conclusion...
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Srovnávací in vitro studie permeace vybraných léčiv z lipofilních roztoků přes lidskou kůži
Koláčková, Lenka ; Doležal, Pavel (advisor) ; Zbytovská, Jarmila (referee)
A COMPARISON IN VITRO STUDY OF PERMEATION OF SELECTED DRUGS FROM LIPOPHILIC SOLUTIONS TROUGH HUMAN SKIN ABSTRACT The aim of the study was to compare the permeation of testosterone (TST), caffeine (CAF), flufenamic acid (FA) and benzoic acid (BA) from highly liquid paraffin through human heat-separated epidermis (HSE). For evaluation of saturation concentration of the drugs in the vehicle(csat), an excess of BA, CAF, FA or TST was suspended in 5 ml of highly liquid paraffin in a screw top scintillation vial (500 rpm, 32 řC; 24 h). After sedimentation of non- dissolved substance, samples were drawn from the supernatant, diluted 1:10 with dichloromethane and analyzed via UV/VIS-spectroscopy: (Lambda 35; Perkin Elmer, BA 228 nm; CAF 277 nm; FA 287 nm; TST 238 nm). Permeation experiments over human HSE of two donors (6 pieces of each) were performed in Franz diffusion cells at 32 řC. The donor was composed of TST, FA, BA (0.4 mg/ml), CAF (0.1 mg/ml) dissolved in paraffin. Samples of 0.4 ml were collected over the time, replaced by fresh acceptor solution (Soerensen phosphate buffer pH 7.4) and quantified by validated HPLC methods. The steady state flux (J) was evaluated from the linear part of cumulative amount versus time plots and dividing it by donor concentration (cdon), the apparent permeability coefficient...
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The effect of addition of thickening agents on nanoemulsion properties.
Kovaříková, Alžběta Dorota ; Berka, Pavel (advisor) ; Doležal, Pavel (referee)
Nanoemulsions are o/w emulsions with the particle size of discontinuous phase in the range of 1 - 500 nm. They are not transparent and thermodynamically stable as microemulsions. Although nanoemulsions are usually more stable than macroemulsions, creaming, flocculation or Ostwald ripening may occur. One of possibilities to avoid such destabilizing processes is the addition of a thickening agent. The thickening agent increases the viscosity of the external phase, thus reducing the movement of the internal phase and stabilizing the entire system. The aim of this work was to evaluate the effect of an addition of the thickening agents to nanoemulsions. Cellulose derivatives (specifically: hydroxypropylmethyl- (HPMC), hydroxyethyl- (HEC) and hydroxypropylcellulose (HPC)) were used as the thickening agents. They were added at concentrations of 0.00, 0.15, 0.33, 1.33, 2.00 and 3.33 ‰. The samples with thickening agent concentration lower than 1.33 ‰ seemed relatively stable from macroscopic point of view. Centrifugation was chosen as a method for accelerated stability testing. It was performed with 3000 revolutions per second for 10 minutes, which was sufficient to establish the balance in the system. Samples with lower concentrations of the thickening agent (up to 1.33 ‰) had particle size in the range...
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