Studies On A Transdermal Patch Of Loxoprofen

Objective: To prepare a transdermal patch of loxoprofen, and toevaluate properties of the patch.Methods: With Loxoprofen as a model drug and emulsion-type acrylicpressure-sensitive adhesive as the carrier, prepared a transdermal patch ofloxoprofen. With release parameters in vitro of the patche with Franzdiffusion cell,selected the group of organic amine which had the biggestimprovement. With propylene glycol, Azone and menthol accelerator astransdermal enhancer, cumulative release per unit area as the indictor,designed an orthogonal experiment to select the optimum formulation. Madea preliminary investigation of the content uniformity and the stability of thepreparations. Established an HPLC analytical method for the determinationof loxoprofen content, and investigated the safety and preliminarypharmacodynamics of the preparation.Results: The optimum formulation: loxoprofen content700±5μg·cm-2,n (diethanolamine): n (loxoprofen)=1:1, the amounts of propylene glycol,azone and menthol respectively were2%,3%,3%(W/V). The results of thepreliminary stability test and the content uniformity test showed that thepatch had a promising stability and content uniformity. The results of the safety and preliminary pharmacodynamic test showed that the patch had noobvious skin irritation, and could significantly inhibit the egg white-inducedrat paw swelling.Conclusion: The preparation process of the patch of loxoprofen isreasonable and practicable. The results of in vitro release test showed thatdrug release property of the patch was stable. The content uniformity andstability and safety of the patch complied with pharmacopoeial requirements.The patch had has significant anti-inflammatory effects.