Study of particle rearrangement, compression behavior and dissolution properties after melt dispersion of ibuprofen, Avicel and Aerosil

Abstract

Particle rearrangements, compaction under pressure and in vitro dissolution have been evaluated after melt dispersion of ibuprofen, Avicel and Aerosil. The Cooper-Eaton and Kuno equations were utilized for the determination of particle rearrangement and compression behavior from tap density and compact data. Particle rearrangement could be divided into two stages as primary and secondary rearrangement. Transitional tapping between the stages was found to be 20-25 taps in ibuprofen crystalline powder, which was increased up to 45 taps with all formulated powders. Compaction in the rearrangement stages was increased in all the formulations with respect to pure ibuprofen. Significantly increased compaction of ibuprofen under pressure can be achieved using Avicel by melt dispersion technique, which could be beneficial in ibuprofen tablet manufacturing by direct compression. SEM, FTIR and DSC have been utilized for physicochemical characterization of the melt dispersion powder materials. Dissolution of ibuprofen from compacted tablet of physical mixture and melt dispersion particles has also been improved greatly in the following order: Ibc<Ibsmd1<Ibsmd2<Ibsmp10<Ibsmd5<Ibsmd10.

Real-time monitoring of the mechanism of ibuprofen-cationic dextran crystanule formation using crystallization process informatics system (CryPRINS)

“…11). This results are consistent with our previous reports (Abioye et al, 2014a,b) and other literature reports for pure ibuprofen (Mallick et al, 2011a).…”

“…The strong and sharp carbonyl (C¼O) band, sharp CÀ ÀO stretching, linear aliphatic CÀ ÀH stretching and aromatic ring (C¼C) vibration were noted at 1706. 66, 1229.36, 2991.26-2867.89 and 1506.64 cm À1 respectively (Mallick et al, 2011b;Nokhodchi et al, 2010). Ddex spectra exhibited characteristic broad absorption peaks at 3289.37, 1639.37, 1454.72 and 1340.80 cm À1 corresponding to polymeric À ÀOH stretching, N-H deformation vibration (NÀ ÀH bend), CÀ ÀH bend and CÀ ÀN stretching respectively (Coates, 2000;Mallick et al, 2011b).…”

“…66, 1229.36, 2991.26-2867.89 and 1506.64 cm À1 respectively (Mallick et al, 2011b;Nokhodchi et al, 2010). Ddex spectra exhibited characteristic broad absorption peaks at 3289.37, 1639.37, 1454.72 and 1340.80 cm À1 corresponding to polymeric À ÀOH stretching, N-H deformation vibration (NÀ ÀH bend), CÀ ÀH bend and CÀ ÀN stretching respectively (Coates, 2000;Mallick et al, 2011b). Spectra of the ibuprofen-Ddex conjugate crystanules shifted slightly to higher wavenumbers up to 1710.55 cm À1 as concentration of Ddex increased with relatively lower intensities.…”

Synthesis and Characterization of Novel OAT‐g‐PMMA Matrices: Its Application in Controlled and Colonic Drug Delivery

“…The major anti-inflammatory agents based upon salicylate derivatives are used to treat the chronic inflammatory conditions rheumatoid arthritis and inflammatory bowel syndrome/inflammatory bowel disease (IBS/IBD). Though 5-amino salicylic acid (5-ASA) has been applied in a prodrug form to treat UC since past 50 years, [1][2][3] the most convenient route for administration of drugs to the patient's body is oral in which drug usually dissolves and is absorbed in GI tract fluid and regions, respectively. CDDS should be capable of releasing the drug into the colon, i.e.…”

Characterization of Particle Packing and Drug Release Studies After Solvent Evaporation of Ibuprofen, Avicel, and Aerosil

“…Cooper and Eaton (1962) introduced a bi-exponential equation describing the compaction process of powders under applied pressure. An attempt has been made here to characterize the early stages of compaction behavior under the tapping process using bi-exponential equations reported recently from our laboratory (Mallick et al 2011). Physicochemical characterization of the status of the drug in the formulated powder has been carried out by analytical techniques of scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC).…”