To enhance dissolution rate of meloxicam (MX), a poorly soluble model drug, a natural polysaccharide excipient chitosan (CH) is employed in this work as a carrier to prepare binary interactive mixtures by either mixing or co-milling techniques. The MX-CH mixtures of three different drug loads were characterized for morphological, granulometric, and thermal properties as well as drug crystallinity. The relative dissolution rate of MX was determined in phosphate buffer of pH 6.8 using the USP-4 apparatus; a significant increase in MX dissolution rate was observed for both mixed and co-milled mixtures comparing to the raw drug. Higher dissolution rate of MX was evidently connected to surface activation by mixing or milling, which was pronounced by the higher specific surface energy as detected by inverse gas chromatography. In addition to the particle size reduction, the carrier effect of the CH was confirmed for co-milling by linear regression between the MX maximum relative dissolution rate and the total surface area of the mixture (R2 = 0.863). No MX amorphization or crystalline structure change were detected. The work of adhesion/cohesion ratio of 0.9 supports the existence of preferential adherence of MX to the coarse particles of CH to form stable interactive mixtures.

Department of Organic Technology UCT Prague Faculty of Chemical Technology Technická 5 Dejvice Prague 6 166 28 Czech Republic

Department of Pharmaceutical Technology Charles University Faculty of Pharmacy Akademika Heyrovského 1203 8 Hradec Králové 500 05 Czech Republic

University of Applied Sciences and Arts Northwestern Switzerland Institute of Pharma Technology Hofackerstrasse 30 Muttenz CH 4132 Switzerland

Zentiva K S U Kabelovny 130 Prague 10 102 37 Czech Republic

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