1. Effect of the surfactant on the availability of piroxicam as a poorly hydrosoluble drug from suppositories.
- Author
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Dal Zorro M, Franceschinis E, Punchina A, and Realdon N
- Subjects
- Absorption, Anti-Inflammatory Agents, Non-Steroidal chemistry, Biological Availability, Excipients, Hydrophobic and Hydrophilic Interactions, Intestinal Mucosa metabolism, Membranes, Artificial, Particle Size, Piroxicam chemistry, Polyethylene Glycols, Rectum metabolism, Rheology, Solubility, Suppositories, Triglycerides, Anti-Inflammatory Agents, Non-Steroidal administration & dosage, Anti-Inflammatory Agents, Non-Steroidal pharmacokinetics, Piroxicam administration & dosage, Piroxicam pharmacokinetics, Surface-Active Agents chemistry
- Abstract
The use of surfactants in suppository formulations has been suggested to improve availability of poorly soluble drugs. In the present study, different kinds of surfactants have been investigated to clarify the influence on piroxicam release from suppositories formulated with both lipophilic and hydrophilic bases. Two hydrophilic glucose-derivate surfactants, and a polyoxylglyceride amphiphilic surfactant, all with high HLB values, were investigated for their use in improving drug availability. The two glucose derivate surfactants reduced drug availability from both lipophilic suppositories and hydrophilic formulations, according to longer disintegration times and drug micellization. The more complex surfactant, a lauroyl macrogolglyceride, showed an increase in piroxicam availability from lipophilic suppositories at the higher tested concentrations (15% and 20%). Otherwise, when used in hydrophilic formulations, it was less effective in promoting drug release and even reduced drug availability.
- Published
- 2012