Study On The Percutaneous Penetration Properties Of Antihistamine And Its Hydrogel

Transdermal drug delivery system (TDDS) attracts the attentions from the pharmaceutical industry for its advantages. However, the skin barrier limits the development of TDDS. Safe and effective transdermal enhancers were employed to overcome this barrier. This thesis was focused on transdermal properties of Diphenhydramine Hydrochloride and Cetirizine Hydrochloride, and both chitosan oligomer and normal transdermal enhancers were evaluated in the transdermal delivery system of both drugs.In this dissertation, the methods of HPLC were set up to determine Diphenhydramine Hydrochloride and Cetirizine Hydrochloride quantitatively. Then the effects of chitosan oligomer and normal transdermal enhancers on Diphenhydramine Hydrochloride and Cetirizine Hydrochloride transdermal delivery were studied in vitro. The results showed that for Diphenhydramine Hydrochloride, the enhancement effect of normal transdermal enhancers and chitosan oligomer were in : Chitosan oligomer> Oleic acid>1,3- Propylene glycol>Azone>Glycerol. In which, 0.5% chitosan oligomer performed the best enhancing effect under pH7.5. The Q24 of Diphenhydramine Hydrochloride was 981.13μg/cm~2 and the EFQ was raised to 4.21(P<0.05). For Cetirizine Hydrochloride the enhancement effect of normal transdermal enhancers and chitosan oligomer were in: Azone>Glycerol>Oleic acid>Chitosan oligomer. Chitosan oligomer had no enhancing effect on Cetirizine Hydrochloride. In these enhancers 0.06% Azone resulted in the best effect, which leaded Q24 of Cetirizine Hydrochloride to 227.94μg/cm~2, EFQ raised to 2.95.Meanwhile the hydrogel of Diphenhydramine Hydrochloride and Cetirizine Hydrochloride were designed and prepared, and in vitro transdermal delivery experiments were conducted separately. The results showed that Diphenhydramine Hydrochloride gel had good permeation character with Q24 285.58μg/cm~2. When 1% Chitosan oligomer was added, the Q24 was raised to 418.53μg/cm~2, and EFQ was raised to 1.47. The Q24 of Cetirizine Hydrochloride gel without any enhancers was 35.95μg/cm~2. 0.06% Azone had the best enhancing effect on Cetirizine Hydrochloride gel, under whose function, the Q24 was raised to 43.29μg/cm~2, and EFQ was raised to 1.20.