Improvement of Dissolution Property of Poorly Water-Soluble Drug by Novel Dry Coating Method Using Planetary Ball Mill

Abstract

The dissolution property of a poorly water-soluble drug, flurbiprofen (FP), was improved by a novel dry coating method using a planetary ball mill. Several mixtures composed of water-soluble additives (D-mannitol, lactose, and erythritol), light anhydrous silicic acid, and flurbiprofen were prepared. These mixtures and several starches were co-ground in a planetary ball mill, and the surface of the starches was dry coated with the mixtures. The size, appearance, yield, and drug dissolution property of the dry coated preparations were evaluated, and the optimal formulation which improved the dissolution property of poorly water-soluble flurbiprofen was determined. The dissolution rate of FP was increased by dry coating of the surface of starches with microparticulated FP. It was further increased by co-grinding of FP, starch, and a water-soluble additive, or dry coating of the starch surface with microparticulated FP and light anhydrous silicic acid, as a glidant. These co-ground and dry coated preparations could be recovered from the pot of the planetary ball mill readily without adhesion to the inside wall of the pot. These are considered to be novel, industrially applicable methods for improving the dissolution rate of poorly water-soluble drugs.

Preparation and physicochemical characterizations of tanshinone IIA solid dispersion

“…Thus, stabilization of an amorphous form of drug is particularly desirable for pharmaceutical products. Co-grinding of drugs with water-soluble polymers has been recently studied and is prone to preparation of stable amorphous materials (Sonoda et al, 2008;Balani et al, 2010). In the present study, a novel solid dispersion of tanshinone IIA was prepared by planetary ball mill technology to improve the solubility and dissolution rate of this poorly water soluble drug.…”

Prospective Application of Response Surface Methodology for Predicting High-Energy Mixing Process Conditions towards Fine Powders Flow Improvement

“…A planetary ball mill, applied so far mainly for milling and carrying out mechanochemical processes, has recently been proven to be an effective device to perform high-energy mixing. It was firstly used as a high-energy mixer by Sonoda et al [4] to obtain better dissolution of flurbiprofen via dry coating. Moreover, this type of mill can be used on an industrial scale [5].…”

Characterization of surface properties of dry-coated anhydrous borax powders

“…As an alternative tool for dry coating, a laboratoryscale planetary milling device was used by Sonoda et al [23]. This device operates in the centrifugal mode, which leads to a more gentle size reduction process with fewer abrasions.…”