| α -Asarone is one of the important ingredients of acorus gramineous soland.It has antitussive, apophlegmatic, antiasthmatic,sedative and anticonvulsantic roles.It is used for the treatment of chronicus bronchitis, obstructive pneumonitis and epilepsy.It is one of the first selective drugs for epileptic.There are several kinds of dosage marketed such as injection.tablets and capsules.But It is easy to bring up gastrointestinal tract relapses when orally and intravenously administrated.If It was used for a long time ,It could cause serious adverse effects.It also has the special properties of good lipophilic.low melting point,molecular weight.So It can be prepared to be a transdermal form of dosage.Because its load is high and moist-proof quality is very good without hypersensitivity reaction.Therefore,the cataplasma of α -Asarone was formulated and studied.First,basic physical-chemical properties of α -Asarone were investigated.The results showed that α -Asarone belonged to lipophilic drug and was suitable for topical application.The solubility of α -Asarone in 20 % alcohol physiological saline was 0.47 mg/ml.Horizontal diffusion cell and 20 % alcohol physiological saline were used to screen the permeation promoters in order to improve the drug permeation. Vitro permeation experiments showed that the permeation kinetics of α-Asarone across the rat skin was zero order with a steady-state flux(Js) of 0.0603 μ gcm-2V-1 and permeability coefficient of 1.37 cms-1, The lag time was 3.86 h.The co-application of enhancers could...
|
PDF Full Text Request