Pakistan journal of pharmaceutical sciences 2011-10-01

Preparation and evaluation of 5, 9-dimethyl-2-cyclopropyl-2-decanol as a penetration enhancer for drugs through rat skin.

Gul Majid Khan, Abid Hussain, Raja Muhammad Hanif

文献索引：Pak. J. Pharm. Sci. 24(4) , 451-7, (2011)

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摘要

In the present study a new alcohol derivative of tetrahydrogeraniol (THG), an acyclic monoterpene, has been prepared by using Grignard reagent and methyl cyclopropyl ketone. Penetration enhancing effects of THG and the synthesized derivative 5,9-dimethyl-2-cyclopropyl-2-decanol (DICNOL) on the transdermal penetration of 5-fluorouracil (5-FU) and tramadol hydrochloride (tramadol HCl) across the excised rat skin were studied by an in vitro permeation technique using Franz diffusion cells. Azone was used as standard enhancer for comparison. DICNOL and THG significantly enhanced 5-FU and tramadol HCl penetration through rat skin compared with the control. DICNOL enhanced the permeability of 5-FU and tramadol HCl across full thickness skin by about 11 and 20 fold, respectively. Increased partition coefficient and diffusion coefficient values were obtained by these enhancers. The results suggest that the amount of DICNOL in the skin, especially in the stratum corneum, may be related to its penetration enhancing effects.