TY - JOUR AU - Diós, Péter AU - Szigeti, Krisztián AU - Budán, Ferenc Csaba AU - Pocsik, M AU - Veres, Dániel AU - Máthé, Domokos AU - Pál, Szilárd AU - Dévay, Attila AU - Nagy, Sándor TI - Influence of barium sulfate X-ray imaging contrast material on properties of floating drug delivery tablets. JF - EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES J2 - EUR J PHARM SCI VL - 95 PY - 2016 SP - 46 EP - 53 PG - 8 SN - 0928-0987 DO - 10.1016/j.ejps.2016.09.034 UR - https://m2.mtmt.hu/api/publication/3119939 ID - 3119939 N1 - Institute of Pharmaceutical Technology and Biopharmacy, University of Pécs, Rókus str. 2, Pécs, H-7624, Hungary Department of Biophysics and Radiation Biology, Semmelweis University, Tűzoltó utca 37-47, Budapest, H-1094, Hungary CROmed Translational Research Centers, Baross str. 91-95, Budapest, H-1047, Hungary Department of Public Health Medicine, University of Pécs, Szigeti str. 12, Pécs, H-7624, Hungary Cited By :10 Export Date: 31 October 2023 CODEN: EPSCE Correspondence Address: Diós, P.; Institute of Pharmaceutical Technology and Biopharmacy, Rókus str. 2, Hungary; email: peter.dios@aok.pte.hu AB - The objective of the study was to reveal the influence of necessarily added barium sulfate (BaSO4) X-ray contrast material on floating drug delivery tablets. Based on literature survey, a chosen floating tablet composition was determined containing HPMC and carbopol 943P as matrix polymers. One-factor factorial design with five levels was created for evaluation of BaSO4 (X1) effects on experimental parameters of tablets including: floating lag time, total floating time, swelling-, erosion-, dissolution-, release kinetics parameters and X-ray detected volume changes of tablets. Applied concentrations of BaSO4 were between 0 and 20.0% resulting in remarkable alteration of experimental parameters related especially to flotation. Drastic deterioration of floating lag time and total floating time could be observed above 15.0% BaSO4. Furthermore, BaSO4 showed to increase the integrity of tablet matrix by reducing eroding properties. A novel evaluation of dissolutions from floating drug delivery systems was introduced, which could assess the quantity of drug dissolved from dosage form in floating state. In the cases of tablets containing 20.0% BaSO4, only the 40% of total API amount could be dissolved in floating state. In vitro fine resolution X-ray CT imagings were performed to study the volume change and the voxel distributions as a function of HU attenuations by histogram analysis of the images. X-ray detected relative volume change results did not show significant difference between samples. After 24h, all tablets containing BaSO4 could be segmented, which highlighted the fact that enough BaSO4 remained in the tablets for their identification. LA - English DB - MTMT ER - TY - THES AU - Diós, Péter TI - Preformulation studies and optimization of floating drug delivery systems based on pharmaceutical technological and biopharmaceutical parameters. Design of modified drug delivery systems TS - Design of modified drug delivery systems PB - Pécsi Tudományegyetem PY - 2016 SP - 95 UR - https://m2.mtmt.hu/api/publication/3071247 ID - 3071247 LA - English DB - MTMT ER - TY - JOUR AU - Máthé, Domokos AU - Budan, F AU - Pál, Szilárd AU - Kiss, I AU - Diós, Péter AU - Szigeti, Krisztián TI - X-Ray CT Imaging of Stomach Passage of Contrast-Enhanced Floating Tablets in a New Rat Model JF - EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING J2 - EUR J NUCL MED MOL I VL - 42 PY - 2015 IS - Suppl. 1 SP - S412 EP - S413 SN - 1619-7070 UR - https://m2.mtmt.hu/api/publication/3033954 ID - 3033954 LA - English DB - MTMT ER - TY - GEN AU - Máthé, Domokos AU - Budán, Ferenc AU - Pál, Szilárd AU - Kiss, István AU - Diós, Péter AU - Szigeti, Krisztián TI - X-Ray CT Imaging of Stomach Passage of Contrast-Enhanced Floating Tablets in a New Rat Model PY - 2015 UR - https://m2.mtmt.hu/api/publication/3025450 ID - 3025450 AB - Introduction. Cost-effective in vivo animal models are warranted to be developed to test modified drug delivery systems with the purpose to optimize those medical agent carriers. In this study, a novel rat model was evaluated to gain information about attributions of floating drug delivery systems (FDDS) practically in form of small sized tablets. X- ray computed tomography (CT) was performed.Materials and Methods. Sodium alginate as a biodegradable swelling polymer to create coherent frame of the tablets, sodium bicarbonate as carbon dioxide (CO2) creating agent and barium sulfate (BaSO4) contrast material to enhance X-ray CT. Partly anaesthetized rats were made to swallow tablets. In vivo imaging was performed at the following sampling times: 15 min, 1 h, 2 h, 3 h, 4 h, 6 h, 24 h and 48 h. Additionally, a maximum intensity projection (MIP) was rendered at 30 min after administration to provide fine resolution of spatial and temporal details about FDDSs in situ behavior using an adequate selected lookup table (LUT).Results. tablets with 10% BaSO4 content enabled quantitative in vivo imaging. These pharmaceutical agent carriers formed CO2 bubbles 15 minutes after the administration and remained floating in the stomach for at least 24 hours. 48 hours after administration tablets were observed to be disintegrated mostly in the small intestine. Thus, the tablet?s putative obstruction in stomach can be excluded. So the model can be considered as cheap, representative and capable to interpret results better.Conclusions.We can suppose that this newly developed rat model will be useful to provide comprehensive data about certain factors (e.g. food effect, posture, etc.) influencing gastrointestinal behavior of FDDS in future experiments by tracking their properties. LA - English DB - MTMT ER - TY - GEN AU - Diós, Péter AU - Budán, Ferenc AU - Szigeti, Krisztián AU - Horváth, Ildikó AU - Nagy, Sándor AU - Pernecker, Tivadar AU - Dévay, Attila AU - Gerencsér, Gellért AU - Gyöngyi, Zoltán AU - Kiss, István AU - Pál, Szilárd AU - Máthé, Domokos TI - Parameters of floating drug delivery systems - tracked in animal model utilizing in vivo X-ray CT imaging PY - 2015 UR - https://m2.mtmt.hu/api/publication/3025443 ID - 3025443 AB - Attribution of floating drug delivery systems (FDDSs) can be studied utilizing in vivo animal models recently including X- ray imaging. High resolution X-ray computed tomography (CT) (1) approach could be cost-effective in respect to the information possessed in comparison to costs. Comprehensive data can be provided about specific factors (e.g. quantity of distinct excipients, food effect, anaesthetics, posture) influencing gastrointestinal behavior of specific tested drug delivery systems (2). In this study, a novel in vivo Wistar rat model was evaluated to gain information about spatial and temporal patterns of structure, position and behavior of floating drug delivery systems, practically in form of small sized tablets. Different concentrations (5, 10 and 20%) of barium sulfate contrast material enhanced X-ray imaging. For in vivo X-ray CT evaluation, suitable concentration of barium sulfate was determined. Flotation of tablets could be achieved for 24 hours in stomach and after 48 hours tablets were present in the intestinal system. During the examination, structural changes of floating tablets could be tracked such as disintegration or swelling. LA - English DB - MTMT ER - TY - GEN AU - Diós, Péter AU - Budán, Ferenc AU - Nagy, Sándor AU - Horváth, Ildikó AU - Szigeti, Krisztián AU - Máthé, Domokos AU - Pál, Szilárd AU - Dévay, Attila TI - Achievement of very high floating force and rapid dissolution of sodium alginate based floating drug delivery systems: in vitro, in vivo study PY - 2015 UR - https://m2.mtmt.hu/api/publication/3025435 ID - 3025435 AB - Floating force values as examination parameters have one of the most significant influence on the buoyancy of floating drug delivery systems (FDDSs) beyond floating lag time and total floating time (1-3). Gastric retention and consequently location of drug release may be significantly affected by how FDDSs float, however in most of the cases floating force values are not measured. The aim of this study is to examine sodium alginate (X1), low-substituted hydroxypropyl cellulose (L-HPC B1, X2), and sodium bicarbonate (X3) concentrations in floating tablets to achieve very high value of floating force. Face-centered central composite design was used with three numerical factors in three levels. X1 and X2 were used in unusual concentration intervals: sodium alginate in 2.5-5% and L-HPC B1 40-50%. Studied examination parameters were: floating lag time (tlag), maximal floating force (Fmax), and time for maximal floating force (tFmax), dissolution. Formulation with the highest floating force was studied in vivo using X-ray CT for 24 hours. Result showed very high values of maximal floating force at several formulation. Optimal tablets for our further fine-optimization aims were studied in rats, where 24 hours of gastric retention was observed. LA - English DB - MTMT ER - TY - GEN AU - Diós, Péter AU - Nagy, Sándor AU - Pernecker, Tivadar AU - Pál, Szilárd AU - Dévay, Attila TI - Influence of sodium alginate and low-substituted hydroxylpropyl cellulose quantity in floating behavior and drug release in floating drug delivery systems PY - 2015 UR - https://m2.mtmt.hu/api/publication/3025432 ID - 3025432 AB - The aim of this research is to evaluate the influence of low- substituted hydroxypropyl cellulose (L-HPC) and sodium alginate concentrations on floating behavior and drug release of floating drug delivery systems. Face-centered central composite design was used with two numerical factors (sodium alginate %, X1; L-HPC B1 %, X2) and three levels. Sodium alginate amount between 0.5% and 35.15%, L-HPC amount between 0.5 and 25% were used (1). Studied parameters (dependent variables) were the following: floating lag time (tlag), maximal floating forces (Fmax) and dissolution of paracetamol. On floating lag time data, only sodium alginate was significant factor, while both factors and their interactions were significant in the case of maximal floating force. Significance of factors on dissolution data was depended on the sampling time. Results of floating lag time, floating force and paracetamol release studies revealed various behavior of floating tablets depending on L-HPC and sodium alginate quantity. Low level of sodium alginate (0.5%) resulted in shorter floating lag times and rapid dissolution in comparison with the other formulations. Results highlight the possible wide range applicability of sodium alginate as swelling polymer and L- HPC as disintegrant. LA - English DB - MTMT ER - TY - CONF AU - Diós, Péter AU - Nagy, Sándor AU - Bognár, Vivien AU - Pál, Szilárd AU - Dévay, Attila TI - Hidrofil mátrixképző polimerek alkalmazhatósága efferveszcens úszó készítményekben T2 - I. Cholnoky László Szakkollégiumi Szimpózium C1 - Pécs PY - 2015 SP - x UR - https://m2.mtmt.hu/api/publication/2929738 ID - 2929738 AB - Módosított hatóanyag-leadású készítmények alapos megtervezésével különböző biofarmáciai igényeknek megfelelő hatóanyag-felszabadulású rendszerek készíthetők. Ezen készítmények előállítása során a hatóanyag-leadás módosítását speciális segédanyagok és/vagy különleges technológiai eljárások segítségével érhetjük el. A gasztroretentív rendszerek alkalmazásának célja a készítmények gyomorban való tartózkodási idejének meghosszabbítása. A gasztroretentív rendszerek leggyakrabban alkalmazott technológiai megvalósítása az úszó hatóanyag- leadó rendszerek (FDDSs). Ezen úszó rendszerek gyomor retenciós idejének megnövelését azok lecsökkent átlagsűrűsége révén érhető el. A szakirodalom az úszó készítményeken belül élesen elkülöníti az efferveszcens és nem-efferveszcens úszó rendszereket. Az előadás célja, hogy bemutassa a gyógyszertechnológiai gyakorlatban, az iparban és magisztrálisan egyaránt leggyakrabban használt hét hidrofil mátrixképző polimer efferveszcens úszótablettákban való alkalmazhatóságát. Az elkészített tabletták összetételei csak az alkalmazott polimerekben különböznek. Alkalmazott hidrofil mátrixképzők: hidroxipropil- metilcellulóz (HPMC), metilcellulóz (MC), hidroxietil- cellulóz (HEC), karmellóz-nátrium (CMC-Na), kismértékben szubsztituált hidroxipropilcellulóz (L-HPC), nátrium-alginát, karbomer (Carbopol 934P). A kísérlet során elvégzett vizsgálatok: az úszás eléréséhez szükséges idő (tlag) meghatározása és a hatóanyag 24 órás kioldódás vizsgálata. A vizsgálati minták eredményei között jelentős különbségek mutatkoztak. Egyes minták teljes hatóanyagtartalma 24 órás vizsgálat során sem tudott felszabadulni, míg több esetben már akár egy órát követően teljes hatóanyag kioldódás és gyors duzzadás volt tapasztalható. LA - Hungarian DB - MTMT ER - TY - JOUR AU - Diós, Péter AU - Nagy, Sándor AU - Pál, Szilárd AU - Pernecker, Tivadar AU - Kocsis, Béla AU - Budán, Ferenc Csaba AU - Horváth, Ildikó AU - Szigeti, Krisztián AU - Bölcskei, Kata AU - Máthé, Domokos AU - Dévay, Attila TI - Preformulation studies and optimization of sodium alginate based floating drug delivery system for eradication of Helicobacter pylori JF - EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS J2 - EUR J PHARM BIOPHARM VL - 96 PY - 2015 SP - 196 EP - 206 PG - 11 SN - 0939-6411 DO - 10.1016/j.ejpb.2015.07.020 UR - https://m2.mtmt.hu/api/publication/2924040 ID - 2924040 N1 - Institute of Pharmaceutical Technology and Biopharmacy, University of Pécs, Rókus Str. 2, Pécs, H-7624, Hungary Department of Microbiology, University of Pécs, Szigeti Str. 12, Pécs, H-7624, Hungary CROmed Translational Research Centers, Baross Str. 91-95Budapest H-1047, Hungary Department of Public Health Medicine, University of Pécs, Szigeti Str. 12, Pécs, H-7624, Hungary Department of Pharmacology and Pharmacotherapy, University of Pécs, Szigeti Str. 12, Pécs, H-7624, Hungary Cited By :38 Export Date: 6 September 2023 CODEN: EJPBE Correspondence Address: Diós, P.; Institute of Pharmaceutical Technology and Biopharmacy, University of Pécs, Rókus Str. 2, Hungary AB - The aim of this study was to design a local, floating, mucoadhesive drug delivery system containing metronidazole for Helicobacter pylori eradication. Face-centered central composite design (with three factors, in three levels) was used for evaluation and optimization of in vitro floating and dissolution studies. Sodium alginate (X1), low substituted hydroxypropyl cellulose (L-HPC B1, X2) and sodium bicarbonate (X3) concentrations were the independent variables in the development of effervescent floating tablets. All tablets showed acceptable physicochemical properties. Statistical analysis revealed that tablets with 5.00 % sodium alginate, 38.63 % L-HPC B1 and 8.45 % sodium bicarbonate content showed promising in vitro floating and dissolution properties for further examinations. Optimized floating tablets expressed remarkable floating force. Their in vitro dissolution studies were compared with two commercially available non-floating metronidazole products and then microbiologically detected dissolution, ex vivo detachment force, rheological mucoadhesion studies and compatibility studies were carried out. Remarkable similarity (f1, f2) between in vitro spectrophotometrically and microbiologically detected dissolutions was found. Studies revealed significant ex vivo mucoadhesion of optimized tablets, which was considerably increased by L-HPC. In vivo X-ray CT studies of optimized tablets showed 8 h gastroretention in rats represented by an animation prepared by special CT technique. LA - English DB - MTMT ER - TY - JOUR AU - Diós, Péter AU - Pernecker, Tivadar AU - Nagy, Sándor AU - Pál, Szilárd AU - Dévay, Attila TI - Influence of different types of low substituted hydroxypropyl cellulose on tableting, disintegration, and floating behaviour of floating drug delivery systems JF - SAUDI PHARMACEUTICAL JOURNAL J2 - SAUDI PHARM J VL - 23 PY - 2015 IS - 6 SP - 658 EP - 666 PG - 9 SN - 1319-0164 DO - 10.1016/j.jsps.2014.09.001 UR - https://m2.mtmt.hu/api/publication/2807473 ID - 2807473 N1 - Export Date: 27 January 2024; CODEN: SPJOE AB - Abstract The object of the present study is to evaluate the effect of application of low-substituted hydroxypropyl cellulose (L-HPC) 11 and B1 as excipients promoting floating in gastroretentive tablets. Directly compressed tablets were formed based on experimental design. Face-centred central composite design was applied with two factors and 3 levels, where amount of sodium alginate (X1) and L-HPC (X2) were the numerical factors. Applied types of L-HPCs and their 1:1 mixture were included in a categorical factor (X3). Studied parameters were floating lag time, floating time, floating force, swelling behaviour of tablets and dissolution of paracetamol, which was used as a model active substance. Due to their physical character, L-HPCs had different water uptake and flowability. Lower flowability was observed and lower water uptake after 60 minutes at L-HPC 11 compared to L-HPC B1. Shorter floating times were detected at L-HPC 11 and L-HPC mixtures with 0.5% content of sodium alginate, whereas alginate was the only significant factor. Evaluating results of drug release and swelling studies on floating tablets revealed correlation, which can serve to help to understand the mechanism of action of L-HPCs in the field development of gastroretentive dosage forms. LA - English DB - MTMT ER -