Preparation Of Indomethacin Cream And Study On In-vitro Transdermal Properties And Pharmacodynamics

ObjectiveCream prescription was optimized by the orthogonal design method, the Indomethacin cream was prepared. The determination method of the in-vitro release of Indomethacin cream was established. The quality and stability of the homemade Indomethacin cream were investigated. The analgesic and anti-inflammatory effects of Indomethacin cream preparation and whether it had the skin irritation were investigated.MethodsWith the amounts of tween 80, glycerol monostearate, liquid paraffin, petroleum jelly as the research objects, with the appearance of the cream、centrifugal tests and heat-resistant and cold-resistant tests whether were stratified as indicators, cream prescription was optimized by the orthogonal design method. With vertical diffusion pool as experimental device, with abdominal skin of the mice as permeable barrier, with 20% ethanol-p H 7.4 buffer as acceptable liquid, the cumulative permeation amounts of the cream were determined by HPLC in the release medium. The appearance, p H, particle size, uniformity of homemade cream preparation were investigated, the drug content of cream preparation was checked, and the stability of the sample was investigated. With the mice as experimental objects, the analgesic and anti-inflammatory effects of Indomethacin cream were investigated. With the rabbits as experimental objects, respectively for skin irritation experiments of single and multiple doses.ResultsThrough the single factor and orthogonal design tests, we got the best prescription, for tween 80 was 0.45 g, monostearate was 0.9 g, liquid paraffin was 0.9 g, vaseline was 0.6 g, then according to the best prescription, three batches of Indomethacin cream were prepared, cream preparation was centrifuged in 6000 r·min-1 for 20 min, placed at 55℃ in the Incubator for 6 h, placed at-20℃ in the refrigerator for 24 h respectively, three batches of the cream had no obvious changes in appearance. Cumulative release of Indomethacin cream and time went on a linear regression, the regression equation was Q= 5.6436t+12.1370, r=0.9906, showed that cumulative permeation amounts of Indomethacin cream had a good linear relationship with the time, the cream had a good permeability. Through study on the quality and stability of the cream preparation, the results showed that various examination indicators of the cream preparation all meeted the prescribed standards. The analgesic and anti-inflammatory effects of the cream were investigated in mice, showed that cream had obvious analgesic and anti-inflammatory effects, through skin irritation experiments of single and multiple doses, the results showed that Indomethacin cream had no skin irritation.ConclusionsUsing the orthogonal design method, we optimized cream prescription, Indomethacin cream was prepared successfully, the cream’s color was uniform, texture was exquisite, easy to coating. Cumulative permeation amounts of Indomethacin cream had a good linear relationship with the time, determination method of cumulative permeation amounts was simple and reliable. The appearance, p H, particle size, uniformity, drug content and stability of homemade sample were conformed to the required standards. The Indomethacin cream had good analgesic and anti-inflammatory effects and no skin irritation, achieving the expected experimental design purposes.