ABSTRACT
OBJECTIVE:To investigate the in vitro transdermal absorption properties of galangin and effects of different pene-tration enhancers on its transdermal behaviors,and provide reference for developing skin preparations using galangin as APIs in the treatment of vitiligo. METHODS:HPLC was used to determine the galangin content. Using cumulative permeation rate (Q) and the transdermal rate(J)of galangin as indexes,the effect of absorption of receiving solution [20%,40% polyethylene glycol 400 (PEG400)solution and 30% ethanol solution] and rotating rate(200,300,400 r/min)on galangin in complete skin of mice were investigated,as well as the azone(1%,3%,5%)and propylene glycol(10%,20%,40%)alone or combination on its penetra-tion promotion. And the transdermal properties of galangin in complete skin,exfoliating skin,dermis skin of rats and mice were de-tected. RESULTS:The best permeability of complete skin of mice showed in 40% PEG400 solution at rotating speed of 300 r/min with 5% azone alone,J was 3.2570 μg/(cm2·h). Js of complete skin,exfoliating skin,dermis skin of mice were 2.7199,34.016, 33.874 μg/(cm2·h),respectively;and those of rats were 0.4996,9.5124,17.406 μg/(cm2·h). CONCLUSIONS:Galangin can penetrate the complete skin of mice and rats,however,the penetration quantity is far lower than exfoliating skin and dermis skin.
ABSTRACT
OBJECTIVE: To prepare Nimodipine hydrogel patch and to investigate the effects of different factors on the in vitro percutaneous permeability of nimodipine.METHODS: Nimodipine hydrogel patch was prepared with sodium carboxymethylcellulose as matrix.The permeation flux of nimodipine through excised mice skin in vitro was determined using Franz diffusion cell.The content of nimodipine was measured by HPLC.Accumulative transdermal delivery of nimodipine(Q) and transdermal speed constant(Js) were calculated.The loading amounts,type of transdermal enhancer(menthol,azone and oleic acid) and their content were optimized with the value of Q and Js as index.RESULTS: The best loading amount was 4 mg?cm-2.Different transdermal enhancers were found to increase the percutaneous permeability of nimodipine.5% oleic acid had the best penetration enhancing effect.The permeation of samples containing 5% oleic acid was in accordance with the zero-order kinetics.Nimodipine hydrogel transdermal patch presented high Js of 28.10 ?g?cm-2?h-1 and Q of 342.58 ?g?cm-2 in 12 h.CONCLUSION: Nimodipine hydrogel patch has good potential for transdermal delivery.
ABSTRACT
Objective To investigate the effect of different transdermal enhancers on percutaneous absorption of ephedrine in Compound Herba Ephedrae Adhesive Plaster.Methods Using modified Franz diffusion cell,the ephedrine content was determined to investigate the effect of different transdermal enhancers in promoting percutaneous absorption.Results Azone or azone used together with other transderml enhancers had a better effect in promoting percutaneous absorption,indicating that azone was the leading transderml enhancers for ephedrine.The mixed transdermal enhancer of azone and propylene glycol was the most effective combination and the rate constant of percutaneous absorption is 94.280 ?g?cm-2?h-1.Conclusion The mixture of azone and propylene glycol can enthance the percutaneous absorption of ephedrine and can be used as the transdermal enhancers for this compound plaster.