The Investigation Of Aceclofenac Transdermal Patches

In this paper, aceclofenac(ACF), a new kind of NSAIDs was selected as the model drug and acrylic pressure sensitive adhesives were used as vehicles to prepare Aceclofenac Transdermal Patches(ATPs).Ultraviolet(UV) spectrophotometry method was developed for the in vitro release study of ATPs and the assay of ATPs; High-performance liquid chromatography (HPLC) method with UV detection was applied to in vitro permeation and in vivo distribution study.Some physico-chemical characteristics of ACF were investigated before formulation design.The results showed that the solubility of ACF in PBS with pH7.4 at 32℃ was 697.81μg/mL;logP of ACF in n-octanol/water system at 32℃ was 0.99. The permeability of ACF underdifferent pH and ionic strength were determined, Jss showed a rise with the increase of pH and a decline with the increase of ionic strength.The effect of several type of permeation enhancers in common concentration were evaluated, Azone, oleic acid and turpentine can be selected as the effective enhancers.On the basis of the studies mentioned above, the formulation of ATPs was optimized by single factor experiments. The stability study of ATPs showed that the appearance and drug content had no obvious changes in accelerated and long-term testing.In this thesis, drug distribution in local tissues (skin, muscle) after topical administration of the ATPs was investigated with HPLC technique, concentration of ACF in skin and muscle remained high during 12hours. Pharmacodynamic of ATPs was evaluated with diclofenac gel as a control, and it was found that ATPs had stronger anti-inflammatory activity than diclofenac gel.The results of rabbit skin irritation test and Guinea pig skin allergia test make it certain that ATPs is safe for topical administration.