AAPS PharmSci

Journal Information
ISSN / EISSN : 1522-1059 / 1522-1059
Published by: Springer Nature (10.1208)
Total articles ≅ 192
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, Kathrin F. Wunder, Andrea Okoloekwe
Published: 1 June 2004
AAPS PharmSci, Volume 6, pp 17-26; https://doi.org/10.1208/ps060215

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Ranjit Madhukar Bidhe,
Published: 1 June 2004
AAPS PharmSci, Volume 6, pp 7-16; https://doi.org/10.1208/ps060214

The publisher has not yet granted permission to display this abstract.
Published: 1 June 2004
AAPS PharmSci, Volume 6, pp 1-6; https://doi.org/10.1208/ps060213

Abstract:
This study was undertaken to categorize representative fluoroquinolone drug substance permeability based on the methods outlined in the Food and Drug Administration's biopharmaceutic classification system (BCS) Guidance for Industry. The permeability of ciprofloxacin, levofloxacin, lomefloxacin, and ofloxacin was measured in an in vitro Caco-2 assay with previously demonstrated method suitability. The permeability class and efflux potential were ascertained by comparing test drug results with standard compounds (metoprolol, atenolol, labetalol, and rhodamine-123). All 4 quinolones drugs demonstrated concentration-dependent permeability, indicating active drug transport. In comparing absorptive versus secretive in vitro transport, the tested fluoroquinolones were found to be subject to efflux in varying degrees (ciprofloxacin > lomefloxacin > rhodamine 123 > levofloxacin > ofloxacin). Based on comparison to labetalol, the high permeability internal standard, ciprofloxacin was classified as a low permeability drug, whereas lomefloxacin, levofloxacin, and ofloxacin were classified as high permeability drugs. The in vitro permeability results matched human in vivo data based on absolute bioavailabilities. This laboratory exercise demonstrated the applicability of an in vitro permeability method for classifying drugs as outlined in the BCS Guidance.
Ranjit Madhukar Bidhe, Sangita Ghosh
Published: 7 April 2004
AAPS PharmSci, Volume 6

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M. Narender Reddy, Tasneem Rehana, S. Ramakrishna, K. P. R. Chowdary,
Published: 1 March 2004
AAPS PharmSci, Volume 6, pp 68-76; https://doi.org/10.1208/ps060107

Abstract:
Celecoxib, a specific inhibitor of cycloxygenase-2 (COX-2) is a poorly water-soluble nonsteroidal anti-inflammatory drug with relatively low bioavailability. The effect of β-cyclodextrin on the aqueous solubility and dissolution rate of celecoxib was investigated. The possibility of molecular arrangement of inclusion complexes of celecoxib and β-cyclodextrin were studied using molecular modeling and structural designing. The results offer a better correlation in terms of orientation of celecoxib inside the cyclodextrin cavity. Phase-solubility profile indicated that the solubility of celecoxib was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1∶1 stoichiometric inclusion complexes. Solid complexes prepared by freeze drying, evaporation, and kneading methods were characterized using differential scanning calorimetry, powder x-ray diffractometry, and scanning electron microscopy. In vitro studies showed that the solubility and dissolution rate of celecoxib were significantly improved by complexation with β-cyclodextrin with respect to the drug alone. In contrast, freeze-dried complexes showed higher dissolution rate than the other complexes.
Anas Saadeddin, Francisca Torres-Molina, Jaime Cárcel-Trullols, Amparo Araico,
Published: 1 March 2004
AAPS PharmSci, Volume 6, pp 1-9; https://doi.org/10.1208/ps060101

The publisher has not yet granted permission to display this abstract.
, Carlo Mischiati, Monica Borgatti, Laura Breda, , , Carlo Pedone, ,
Published: 1 March 2004
AAPS PharmSci, Volume 6, pp 10-21; https://doi.org/10.1208/ps060102

Abstract:
This article describes the production and characterization of cationic submicron particles constituted with Eudragit RS 100, plus different cationic surfactants, such as dioctadecyl-dimethyl-ammonium bromide (DDAB18) and diisobutyphenoxyethyl-dimethylbenzyl ammonium chloride (DEBDA), as a transport and delivery system for DNA/DNA and DNA/peptide nucleic acid (PNA) hybrids and PNA-DNA chimeras. Submicron particles could offer advantages over other delivery systems because they maintain unaltered physicochemical properties for long time periods, allowing long-term storage, and are suitable for industrial production. Submicron particles were characterized in terms of size, size distribution, morphology, and zeta potential. Moreover, the in vitro activity and ability of submicron particles to complex different types of nucleic acids were described. Finally, the ability of submicron particles to deliver functional genes to cells cultured in vitro was determined by a luciferase activity assay, demonstrating that submicron particles possess superior transfection efficiency with respect to commercially available, liposome-based transfection kits.
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