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http://dx.doi.org/10.4333/KPS.2004.34.2.107

External Lyogel Formulation of Prostaglandin E1 Ethyl Ester  

Yang, Sung-Woon (Formulation Lab. Guju Pharmaceutical Co. Ltd.)
Lee, Jin-Kyo (Formulation Lab. Guju Pharmaceutical Co. Ltd.)
Lee, Ji-Eun (Formulation Lab. Guju Pharmaceutical Co. Ltd.)
Kim, Hee-Kyu (College of Pharmacy, Chung-Ang University)
Park, Hye-Sook (College of Pharmacy, Chung-Ang University)
Kim, Jong-Seok (College of Pharmacy, Chung-Ang University)
Choi, Han-Gon (College of Pharmacy, Yeungnam University)
Yong, Chul-Soon (College of Pharmacy, Yeungnam University)
Choi, Young-Wook (College of Pharmacy, Chung-Ang University)
Publication Information
Journal of Pharmaceutical Investigation / v.34, no.2, 2004 , pp. 107-114 More about this Journal
Abstract
External lyogels containing prostaglandin $E_1$ ethyl ester $(PGE_1-EE)$, a prodrug of prostaglandin $E_1\;(PGE_1)$ as a therapeutic agent for erectile dysfunction, were formulated to overcome the aqueous instability and enhance the percutaneous absorption. Lyogels of $PGE_1-EE$ were prepared with ethanol (EtOH)/proplyene glycol (PG) cosolvent system as a vehicle, cineol as an enhancer, and hydroxypropylcellusose as a gelling agent. In vitro percutaneous absorption studies were performed to determine the rate of $PGE_1$ absorption through rat or hairless mouse skin. The permeability of $PGE_1-EE$ lyogel with enhancer was 16-fold greater than that of lyogel without enhancer. Cosolvent produced 9-fold increase in percutaneous absorption. Pharmacodynamic effects of lyogels were evaluated in mature male cats in terms of intracavernosal pressure (ICP). Lyogels containing 0.1 % of $PGE_1-EE$ showed higher ICP compared to intraurethral preparation of $PGE_1$ (1 %) and enhancer-free control lyogel. The shelf-life $(t_{10%})$ of lyogel at refrigerated condition $(4^{\circ}C)$ was calculated as 928 days, which is 4.2 times longer than that of control hydrogel. As a result, $PGE_1-EE$ was formulated successfully to a lyogel system with a selective enhancer and cosolvent system for the topical delivery of $PGE_1$.
Keywords
Erectile dysfunction; Prostaglandin $E_1$ ethyl ester; Prodrug; Lyogel; Percutaneous absorption;
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