Improved solubility and dissolution rate of piroxicam using gelucire 44/14 and labrasol.
Piroxicam is a nonsteroidal anti-inflammatory drug that is characterized by low solubility-high permeability. The present study was designed to improve the dissolution rate of piroxicam at the physiological pH's through its increased solubility by preparing semi-solid dispersions of drug using Gelucires and Labrasol. These excipients are essentially characterized by their melting points and HLB (hydrophilic-lipophilic balance) values. The dissolution tests of the preparations were performed in the media with different pH's. Differential scanning calorimetry (DSC), were used to examine the interaction between piroxicam and excipients. Gelucire 44/14 and Labrasol at the concentration of 15% w/v in water provided 20- and 50-fold increase in the solubility of piroxicam, respectively. The semi-solid dispersion containing 1/20 of drug/excipient mixture (20% Gelucire 44/14 and 80% Labrasol in w/w) produced the dissolution not less than 85% of piroxicam within 30 min in each dissolution media (simulated gastric fluid (SGF), pH 1.2; phosphate buffers, pH 4.5 and 6.8; and water). DSC analysis of this semi-solid dispersion indicated that there was no chemical reaction between the drug and excipients, and that a solid-state solution of piroxicam with excipient formed.
Karataş
Ayşegül
A
Department of Pharmaceutical Technology, School of Pharmacy, Ankara University, 06100-Tandoğan, Ankara, Turkey.
Yüksel
Nilüfer
N
Baykara
Tamer
T
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D005079:Excipients; D005989:Glycerides; D009930:Organic Chemicals / Q000737:chemistry; D010894:Piroxicam / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D005989:Glycerides; D009930:Organic Chemicals; C440220:Labrasol; C104509:gelucire 44-14; D010894:Piroxicam; D011092:Polyethylene Glycols