Comparative study of oxaprozin complexation with natural and chemically-modified cyclodextrins in solution and in the solid state

Hybrid systems based on “drug – in cyclodextrin – in nanoclays” for improving oxaprozin dissolution properties

“…Table 3 Bulk density (g/cm3) Carr index (CI) (%) and Hauner Ratio (HR) of sepiolite (SV) alone or as physical mixture (PM) or cofused products (COF) with oxaprozin (OXA)); physical mixture (PM) and co-ground product (GR) of OXA with RAMEB; ternary (OXA-RAMEB GR)-SV physical mixture (PM) or cofused products (COF). Percent dissolved at 15 min (P.D.15) and Dissolution Efficiency at 60 min (D.E.60) of oxaprozin (OXA), alone and from its physical mixtures (PM), or co-ground products (GR) with RAMEB or physical mixtures (PM) or cofused products (COF), with SV or from ternary (OXA-RAMEBGR)-SV (physical mixtures (PM) or cofused products (COF RAMEB was selected for OXA complexation, since it was the most effective CD in enhancing the drug solubility and dissolution properties (Maestrelli et al, 2009). Among the different clays tested, SV was chosen for preparation of (OXA-RAMEB)-clay ternary systems in virtue of its greater ability to effectively adsorb the drug.…”

“…Drug-RAMEB co-ground systems (GR) were obtained by ballmilling PM in a high-energy vibrational micro-mill (Mixer Mill MM 200,Retsch GmbH,Dusseldorf,Germany) at 24 Hz for 30 min (Maestrelli et al, 2009). …”

“…Recent studies performed to investigate the ability of several natural and derivative CDs in improving OXA dissolution properties indicated the randomlymethylated ß-CD (RAMEB) as the best carrier, and the equimolar OXA-RAMEB product obtained by co-grinding as the most effective in improving drug solubility and dissolution rate (Maestrelli et al, 2009). However, it is known that the amount of CDs that can be used in pharmaceutical dosage forms is limited by various problems, including, in particularly for the methylated derivatives, their potential toxicity (Kiss et al, 2010).…”

“…With this objective, we evaluated and compared the adsorption properties towards OXA of three different aluminum-magnesium containing clays, namely sepiolite, attapulgite and bentonite, in order to select the most effective one for preparing the ternary "drug-in CD-in clay" systems. On the other hand, based on the results of our previous studies (Maestrelli et al, 2009), RAMEB was selected as the most effective CD for OXA complexation. The solid state characterization of binary (drug-CD and drug-clay), and ternary (drug-in CD-in clay) systems was carried out by differential scanning calorimetry, thermogravimetric analysis and powder Xray diffractometry, while the dissolution properties of the different products were evaluated by the dispersed amount method.…”

Cyclodextrin-Based Nanofibers and Membranes: Fabrication, Properties and Applications

“…In fact, inclusion complexation can result in hypsochromic or bathochromic shift and/or increase or decrease in the intensity of the absorption maxima. However, this technique does not provide conclusive results on complexation or functionalization [116,118].…”