不同结构萜类对盐酸普萘洛尔透皮活化能的影响

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Abstract Objective To investigate the effect of terpenes of different structure on the transdermal activation energy of propranolol hydrochloride. Methods The permeability coefficients of propranolol hydrochloride through the rat skin were determined in vitro at different temperatures and the transdermal activation energy was calculated from Arrhenius relationship. Results The Arrhenius equations under different conditions were calculated, in which there was good coefficient relationship （r>0.97）between the varieties. The transdermal activation energy of propranolol hydrochloride calculated from the slope of Arrhenius equations was 90.06 kJ/mol in the control solution, 69.42 kJ/mol in menthol solution, 106.14 kJ/mol in menthone solution, and 124.39 kJ/mol in bisabolol solution. Conclusions A strong transdermal activation energy of propranolol hydrochloride is required to pass through the rat skin. Terpenes except menthol cannot decrease the energy significantly. The possible mechanism might be the formation of molecular hrdrogen bonds between propranolol hydrochloride and terpenes.

Received: 05 September 2011

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http://journal08.magtechjournal.com/Jwk_wjyx/EN/ OR http://journal08.magtechjournal.com/Jwk_wjyx/EN/Y2012/V23/I2/11

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