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프로스타글란딘 E<sub>1</sub> 에칠에스테르의 외용 리오겔 제제 설계
양성운,이진교,이지은,김희규,박혜숙,김종석,최한곤,용철순,최영욱,Yang, Sung-Woon,Lee, Jin-Kyo,Lee, Ji-Eun,Kim, Hee-Kyu,Park, Hye-Sook,Kim, Jong-Seok,Choi, Han-Gon,Yong, Chul-Soon,Choi, Young-Wook 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.2
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 $PGE_1$.
경피용 프로드럭인 에칠 글리콜레이트의 국소자극 및 피부투과성
양성운(Sung Woon Yang),하용호(Yong Ho Ha),김종갑(Johng Kap Kim),최영욱(Young Wook Choi) 대한약학회 1996 약학회지 Vol.40 No.2
Hyperkeratinization is a dermatologic disorder, which is due to the increase of corneocyte cohesion force. Glycolic acid, an alpha hydroxy acid(AHA), has been used to breakdown the hyperkeratinization processes. However, it has a problem of skin irritation when applied topically, due to the strong acidity especially in high concentration. A molecular optimization of glycolic acid has been tried to reduce the skin irritation by the way of prodrug formation. Ethyl glycolate was synthesized by the esterification of glycolic acid with ethanol in acidic conditions in the presence of sulfuric acid, and examined under the spectroscopic trials, such as UV, IR, 1H-NMR, and GC-MS. The physicochemical and biopharmaceutical properties of the prodrug were also evaluated. Through the toxicological tests of both skin irritation and eye mucous irritation, it has been proved that ethyl glycolate was less irritant than glycolic acid, since the pH value of synthetic prodrug was higher than that of glycolic acid. In the penetration test through nude mouse skin by diffusion cell, ethyl glycolate was continuously hydrolyzed to glycolic acid, which was assayed form the receptor compartment. It was obtained that the penetrated amount of ethyl glycolate was five times higher than that of glycolic acid. These results suggest that ethyl glycolate might be a successful prodrug of glycolic acid to reduce the skin irritation and to increase the skin penetration as well.
Ill - Conditioned 정방행렬의 단측 역행렬 산출용 유사 인공신경망 알고리듬
문병수(Byung Soo Moon),양성운(Sung Woon Yang),김영택(Young Taek Kim) 한국정보과학회 1998 한국정보과학회 학술발표논문집 Vol.25 No.2Ⅱ
이 논문에서는 크기가 큰 Ill-Conditioned 정방행렬의 좌측 또는 우측 역행렬 계산시 계산상의 정확도를 향상시키는 알고리듬에 대하여 기술한다. 이 알고리듬은 대상 행렬의 행벡터들을 Input으로 하고 해당 Input 벡터가 몇번째 행 벡터인지를 나타내는 단위 벡터를 Target 벡터로 하며 초기 Weight 값으로 Pivoting을 겸한 Gauss소거법을 적용하여 얻은 역행렬을 사용하는 Single Layer 인공신경망에 적용하는 역전파 알고리듬과 흡사한 것이다. 각각의 Input 행 벡터에 대하여 역행렬의 열 벡터들이 점진적을 직교가 되거나 평행이 되도록 근접시키므로써 모든 Input 행 벡터들이 열벡터들에 비교적 균일하게 직교 또는 평행이 되도록 학습시키는 알고리듬이다.
프로스타글란딘 E₁에칠에스테르의 외용 리오겔 제제 설계
양성운,이진교,이지은,김희규,박혜숙,김종석,최한곤,용철순,최영욱 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.2
External lyogels containing prostaglandin E₁ethyl ester(PGE₁-EE), a produrg of prostaglandin E₁(PGE₁) as a therapeutic agent for erectile dysfunction, were formulated to overcome the aqueous instability and enhance the percutaneous absorption. Lyogels of PGE₁-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 PGE₁ absorption through rat or hairless mouse skin. The permeability of PGE₁-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). Lyogles containing 0.01% of PGE₁-EE showed higher ICP compared to intraurethral preparation of PGE₁(1%) and enhancer-free control lyogel. The shelf-life (t_(10%) of lyogel at refrigerated condition (4℃) was calculated as 928 days, which is 4.2 times longer than that of control hydrogel. As a result, PGE₁-EE was formulated successfully to a lyogel system with a selective enhancer and cosolvent system for the topical delivery of PGE₁.