@mastersthesis{MTMT:2241558, title = {Improvement of the solubility and bioavailability of loratadine by pharmaceutical technological mtehods}, url = {https://m2.mtmt.hu/api/publication/2241558}, author = {Szabados-Nacsa, Ágnes}, doi = {10.14232/phd.1413}, publisher = {SZTE}, unique-id = {2241558}, year = {2012} } @article{MTMT:1696527, title = {Physico-chemical characterization and in vitro/in vivo evaluation of loratadine: dimethyl-β-cyclodextrin inclusion complexes}, url = {https://m2.mtmt.hu/api/publication/1696527}, author = {Szabados-Nacsa, Ágnes and Sipos, Péter and Martinek, Tamás and Mándity, István and Blazsó, Gábor and Balogh, A and Révész, Piroska and Aigner, Zoltán}, doi = {10.1016/j.jpba.2011.01.024}, journal-iso = {J PHARMACEUT BIOMED ANAL}, journal = {JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS}, volume = {55}, unique-id = {1696527}, issn = {0731-7085}, abstract = {A tricyclic, piperidine derivative of antihistamines, loratadine, which belongs in class II of the Biopharmaceutical Classification System, was investigated. It is an ionizable drug, whose solubility depends on the gastrointestinal pH, and the bioavailability is therefore very variable. Inclusion complexes were prepared by kneading method, containing loratadine (LOR) and dimethyl-beta-cyclodextrin (DIMEB) in two different molar ratios in an attempt to achieve better dissolution and therefore the better bioavailability of loratadine. The formation and physicochemical properties of the inclusion complexes were investigated by means of dissolution tests, pH-dependent solubility studies, electrospray ionization mass spectrometry and diffusion-ordered (1)H NMR spectroscopy. The in vivo efficiency of the complexes was examined in rat animal experiments to confirm the better in vitro dissolution. The instrumental examinations proved the presence of total complexes in 1:1 ratio in both compositions. However, the in vitro pH-dependent solubility results, the in vivo blood levels and the greater pharmacological effect prove that excess DIMEB is needed to achieve the pH-independent and complete solubility of LOR, and therefore better and more consistent bioavailability. (C) 2011 Elsevier B.V. All rights reserved.}, keywords = {CLASSIFICATION; NMR; Solubility; DISSOLUTION; BIOAVAILABILITY; ESI-MS; H-1-RECEPTOR ANTAGONISTS; loratadine; ORAL-DRUG ABSORPTION; In vivo examination; DOSY; pH-independent solubility; DIMEB inclusion complex}, year = {2011}, eissn = {1873-264X}, pages = {294-300}, orcid-numbers = {Martinek, Tamás/0000-0003-3168-8066; Mándity, István/0000-0003-2865-6143; Révész, Piroska/0000-0002-5336-6052} } @article{MTMT:1872118, title = {Achievement of pH-independence of poorly-soluble, ionizable loratadine by inclusion complex formation with dimethyl-β-cyclodextrin}, url = {https://m2.mtmt.hu/api/publication/1872118}, author = {Szabados-Nacsa, Ágnes and Berkesi, Ottó and Révész, Piroska and Aigner, Zoltán}, doi = {10.1007/s10847-009-9558-1}, journal-iso = {J INCL PHENOM MACRO CHEM}, journal = {JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY}, volume = {64}, unique-id = {1872118}, issn = {1388-3127}, abstract = {A tricyclic, piperidine derivative of antihistamines, loratadine, which belongs in class II of the Biopharmaceutical Classification System, was investigated. It is an ionizable drug, whose solubility depends on the gastrointestinal pH, and the bioavailability is therefore very variable. The aim of this work was to enhance the dissolution and make the solubility of loratadine independent of pH. Inclusion complexes were prepared between loratadine and dimethyl-β-cyclodextrin in two different molar ratios by three techniques (physical mixing, kneading and spray-drying). The formation and physicochemical properties of the inclusion complexes were investigated by means of dissolution tests, thermal analysis and Fourier Transform Infrared spectroscopy. The instrumental examinations proved the presence of partial or total complexes depending on the preparation method and molar ratio, which resulted in better dissolution. For some compositions and preparation methods, the application of this cyclodextrin made the solubility of loratadine independent of pH.}, keywords = {Release; ABSORPTION; AGENTS; CRYSTAL; Solubility; thermal analysis; DISSOLUTION; Formulation; BIOAVAILABILITY; FT-IR; loratadine; pH-independent solubility; DIMEB; drug classification; Co-crystal}, year = {2009}, eissn = {1573-1111}, pages = {249-254}, orcid-numbers = {Berkesi, Ottó/0000-0001-6184-1768; Révész, Piroska/0000-0002-5336-6052} } @article{MTMT:1872098, title = {Polyvinylpyrolidone as Carrier to Prepare Solid Disperssion - pros and Cons}, url = {https://m2.mtmt.hu/api/publication/1872098}, author = {Ambrus, Rita and Szabados-Nacsa, Ágnes and Révész, Piroska and Aigner, Zoltán and S, Cinta-Panzaru}, journal-iso = {REV CHIM-BUCHAREST}, journal = {REVISTA DE CHIMIE}, volume = {60}, unique-id = {1872098}, issn = {0034-7752}, abstract = {Enhancement of the solubility of poorly-soluble drug substances is one of the most important tasks in pharmaceutical technology. It is possible to solve this problem with new drug carrier systems and/or with new technological processes. The solid dispersion technology is generally accepted technique which is able to enhance the dissolution characteristics of drugs with poor water solubility. For this purpose, the drug substance is dispersed in a water-soluble inert polymer matrix; at the higher surface area, due to the presence of the polymer, sometimes the drug solubility and dissolution rate may increase. This work summarizes the theoretical basics of solid dispersion technology and introduces pros and cons of studies using polyvinylpyrrolidone (PVP) as a carrier in the cases of two chosen active pharmaceutical ingredients (APIs), nifluminic acid (NIF) and loratadine (LOR). Wettability properties and dissolution were characterized. The drug-polymer interaction was investigated by using differential scanning calorimetry, and powder X-ray diffraction. Even though the instrumental examinations show similar results for both drugs, the dissolution rate improved only by NIF significantly. The explanation for this phenomena could be sought in the different chemical structure and the strength of the connection between the PVP and the drugs}, keywords = {BEHAVIOR; X-RAY; DSC; Solubility; DISSOLUTION; Dispersions; Dissolution kinetics; Solid dispersion; loratadine; POLYVINYLPYRROLIDONE; Nifluminic acid; drug classification}, year = {2009}, pages = {539-543}, orcid-numbers = {Révész, Piroska/0000-0002-5336-6052} } @article{MTMT:1872095, title = {Water-soluble loratadine inclusion complex: analytical control of the preparation by microwave irradiation}, url = {https://m2.mtmt.hu/api/publication/1872095}, author = {Szabados-Nacsa, Ágnes and Ambrus, Rita and Berkesi, Ottó and Révész, Piroska and Aigner, Zoltán}, doi = {10.1016/j.jpba.2008.07.001}, journal-iso = {J PHARMACEUT BIOMED ANAL}, journal = {JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS}, volume = {48}, unique-id = {1872095}, issn = {0731-7085}, abstract = {The majority of active pharmaceutical ingredients are poorly soluble in water. The rate-determining step of absorption is the dissolution of these drugs. Inclusion complexation with cyclodextrin derivatives can lead to improved aqueous solubility and bioavailability of pharmacons due to the formation of co-crystals through hydrogen-bonding between the components. Inclusion complexes of loratadine were prepared by a convenient new method involving microwave irradiation and the products were compared with those of a conventional preparation method. Dissolution studies demonstrated that the solubility and rate of dissolution of loratadine increased in both of the methods used. The interactions between the components were investigated by thermal analysis and Fourier Transform Infrared studies. The microwave treatment did not cause any chemical changes in the loratadine molecule.}, keywords = {MICROWAVE IRRADIATION; cyclodextrin; Structural analysis; Co-crystals; loratadine; HYDROCHLORIDE; HYDROXYPROPYL-BETA-CYCLODEXTRIN}, year = {2008}, eissn = {1873-264X}, pages = {1020-1023}, orcid-numbers = {Berkesi, Ottó/0000-0001-6184-1768; Révész, Piroska/0000-0002-5336-6052} } @article{MTMT:1872123, title = {Loratadine oldékonyságának és biohasznosíthatóságának növelése gyógyszertechnológiai módszerekkel}, url = {https://m2.mtmt.hu/api/publication/1872123}, author = {Szabados-Nacsa, Ágnes and Aigner, Zoltán and Révész, Piroska}, journal-iso = {ORVOSTUDOMÁNYI ÉRTESÍTŐ}, journal = {BULLETIN OF MEDICAL SCIENCES / ORVOSTUDOMÁNYI ÉRTESÍTŐ}, volume = {79}, unique-id = {1872123}, issn = {1453-0953}, year = {2006}, eissn = {2537-5059}, pages = {257-260}, orcid-numbers = {Révész, Piroska/0000-0002-5336-6052} }