TY - THES AU - Szabados-Nacsa, Ágnes TI - Improvement of the solubility and bioavailability of loratadine by pharmaceutical technological mtehods PB - Szegedi Tudományegyetem (SZTE) PY - 2012 SP - 65 DO - 10.14232/phd.1413 UR - https://m2.mtmt.hu/api/publication/2241558 ID - 2241558 LA - English DB - MTMT ER - TY - JOUR AU - Szabados-Nacsa, Ágnes AU - Sipos, Péter AU - Martinek, Tamás AU - Mándity, István AU - Blazsó, Gábor AU - Balogh, A AU - Révész, Piroska AU - Aigner, Zoltán TI - Physico-chemical characterization and in vitro/in vivo evaluation of loratadine: dimethyl-β-cyclodextrin inclusion complexes JF - JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS J2 - J PHARMACEUT BIOMED ANAL VL - 55 PY - 2011 IS - 2 SP - 294 EP - 300 PG - 7 SN - 0731-7085 DO - 10.1016/j.jpba.2011.01.024 UR - https://m2.mtmt.hu/api/publication/1696527 ID - 1696527 N1 - Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720, Szeged, Hungary Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Szeged, H-6720, Szeged, Hungary Department of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, H-6720, Szeged, Hungary Cited By :16 Export Date: 18 November 2022 CODEN: JPBAD Correspondence Address: Aigner, Z.; Department of Pharmaceutical Technology, Eötvös u. 6, H-6720, Szeged, Hungary; email: aigner@pharm.u-szeged.hu AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Szabados-Nacsa, Ágnes AU - Berkesi, Ottó AU - Révész, Piroska AU - Aigner, Zoltán TI - Achievement of pH-independence of poorly-soluble, ionizable loratadine by inclusion complex formation with dimethyl-β-cyclodextrin JF - JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY J2 - J INCL PHENOM MACRO CHEM VL - 64 PY - 2009 IS - 3-4 SP - 249 EP - 254 PG - 6 SN - 1388-3127 DO - 10.1007/s10847-009-9558-1 UR - https://m2.mtmt.hu/api/publication/1872118 ID - 1872118 N1 - Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, 6720 Szeged, Hungary Department of Physical Chemistry, University of Szeged, Rerrich B. tér 1, 6720 Szeged, Hungary Cited By :21 Export Date: 1 December 2022 Correspondence Address: Aigner, Z.; Department of Pharmaceutical Technology, Eötvös u. 6, 6720 Szeged, Hungary; email: aigner@pharm.u-szeged.hu AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Ambrus, Rita AU - Szabados-Nacsa, Ágnes AU - Révész, Piroska AU - Aigner, Zoltán AU - S, Cinta-Panzaru TI - Polyvinylpyrolidone as Carrier to Prepare Solid Disperssion - pros and Cons JF - REVISTA DE CHIMIE J2 - REV CHIM-BUCHAREST VL - 60 PY - 2009 IS - 6 SP - 539 EP - 543 PG - 5 SN - 0034-7752 UR - https://m2.mtmt.hu/api/publication/1872098 ID - 1872098 AB - 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 LA - English DB - MTMT ER - TY - JOUR AU - Szabados-Nacsa, Ágnes AU - Ambrus, Rita AU - Berkesi, Ottó AU - Révész, Piroska AU - Aigner, Zoltán TI - Water-soluble loratadine inclusion complex: analytical control of the preparation by microwave irradiation JF - JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS J2 - J PHARMACEUT BIOMED ANAL VL - 48 PY - 2008 IS - 3 SP - 1020 EP - 1023 PG - 4 SN - 0731-7085 DO - 10.1016/j.jpba.2008.07.001 UR - https://m2.mtmt.hu/api/publication/1872095 ID - 1872095 AB - 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. LA - English DB - MTMT ER - TY - JOUR AU - Szabados-Nacsa, Ágnes AU - Aigner, Zoltán AU - Révész, Piroska TI - Loratadine oldékonyságának és biohasznosíthatóságának növelése gyógyszertechnológiai módszerekkel JF - BULLETIN OF MEDICAL SCIENCES / ORVOSTUDOMÁNYI ÉRTESÍTŐ J2 - ORVOSTUDOMÁNYI ÉRTESÍTŐ VL - 79 PY - 2006 IS - 2 SP - 257 EP - 260 PG - 4 SN - 1453-0953 UR - https://m2.mtmt.hu/api/publication/1872123 ID - 1872123 LA - Hungarian DB - MTMT ER -