Fluidity and Tableting Characteristics of a Powder Solid Dispersion of the Low Melting Drugs Ketoprofen and Ibuprofen with Crospovidone

Abstract

A powder solid dispersion system (SD) of ketoprofen (KP) or ibuprofen (IP), which possess low melting points, plus crospovidone (CrosPVP), have good fluidity characteristics and can be used to formulate tablets. Tablets of KP or IP in the SD of adequate hardness within a narrow weight range can be prepared by direct compression. Addition of microcrystalline cellulose (MCC) resulted in greater hardness characteristics and less variation in tablet weight. Forces during the tableting process were measured with a tableting process analyzer (TabAll) equipped with a single-punch for determining capping and sticking properties during the tableting process. Pressure transmission ratio from the upper to the lower punch and die wall force were increased by adding 1% magnesium stearate (MS) to the SD. Ejection force decreased when MS was added to the SD. When tablets of the IP SD were prepared without excipient, scraper pressure (SP) was large, resulting in sticking. However, addition of 1% MS, lowered the SP value and eliminated sticking. Thus, an SD of compounds with a low melting point such as KP or IP is suitable for tablet manufacture by direct compression with the addition of 1% MS.

Preparation and Evaluation of Ibuprofen Solid Dispersion Systems with Kollidon Particles Using a Pulse Combustion Dryer System

“…17) Pignatello et al 18) reported that SDs of IBU were prepared with Eudragit RL100 as carriers using a coevaporative method. Shibata et al 19) also reported that solid dispersions of ibuprofen were prepared with PVP by a solvent method. Khan and Jiabi 20) reported that solid dispersions of ibuprofen were prepared by a solvent evaporation method using polyethylene glycol 10000 (PEG), talc, and PEG-talc as dispersion carriers.…”

Characterization of Tableting using the OSDRC System

“…Ejection force of microcelac was smaller than that of ascorbic acid independent of the compression method indicating the weak interaction between the die wall and microcelac tablet. An increase in compression force tended to result on an increase in ejection force and crushing strength (24). Despite the high crushing strength of the tablets compressed by method (OSDRC), the interaction was weak the same as when the other methods were used.…”

“…The data are from three experiments. PTR is useful for evaluating, compression during tableting (22)(23)(24)(25). PTR for method (1-1), (1-3), , and (OSDRC) was 96.8, 96.7, 96.8, and 96.7%, respectively.…”

Sustained release of diltiazem HCl tableted after co-spray drying and physical mixing with PVAc and PVP

“…The sticking of the compacted powders to the die wall was estimated on the basis of the maximum ejection force (F ej ) 23,24 .…”