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PGE<sub>1</sub>-ethyl Ester함유 발기부전 치료용 요도주입 액제의 제조 및 평가
최한곤,유봉규,이종달,김정애,권태협,우종수,용철순,Choi, Han-Gon,Yoo, Bon-Kyu,Rhee, Jong-Dal,Kim, Jung-Ae,Kwon, Tae-Hyub,Woo, Jong-Soo,Yong, Chul-Soon 한국약제학회 2006 Journal of Pharmaceutical Investigation Vol.36 No.4
[ $PGE_1$ ]-ethyl ester intraurethral solutions were prepared in ethanol/propylene glycol mixture with penetration enhancer and viscosity-enhancing agent. The stability of $PGE_1$-ethyl ester in intraurethral solution was investigated at various temperature. Simultaneous determination of $PGE_1$-ethyl ester and $PGE_1$ was performed using a validated HPLC technique. In pentobarbital anesthetized cats, increase in intracavernous pressure(ICP), increase in penile length and duration of erectile response were determined after intraurethral application of $PGE_1$-ethyl ester solutions. $PGE_1$-ethyl ester solutions, when instilled into the eyes of rabbits, produces no noticeable irritation, or slight transient conjunctival irritation. From these results, ocular irritation of this solutions was judged as practically non-irritating. The stability study indicates that the therapeutically effective content in solution is well maintained for 46 weeks or longer when they are stored at $4^{\circ}C$. After intraurethral application of $PGE_1$-ethyl ester, ICP was increased and penile erection was induced. $PGE_1$-ethyl ester intraurethral solutions for erectile dysfunction could be developed and evaluated by employing feline erection model.
최한곤(Han Gon Choi),권기철(Qi Zhe Quan),정시영(Si Young Jung),이종달(Jong Dal Rhee),용철순(Chul Soon Yong) 한국약제학회 2000 Journal of Pharmaceutical Investigation Vol.30 No.4
The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective β₂-adrenergic receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhaneer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.
건강한 지원자에 있어서 염산테르비나핀 함유 라미실정과 무조날정의 약물동력학적 비교
최한곤(Han Gon Choi),용철순(Chul Soon Yong),이종달(Jong Dhal Rhee),우종수(Jong Soo Woo),이경희(Kyung Hee Lee),유봉규(Bong Kyu Yoo) 대한약학회 2005 약학회지 Vol.49 No.4
Financial standing of National Health Insurance has been experiencing a grave deterioration during the last 4-5 years, and the yearly amount paid by the insurance for drug expense rose up to 4 trillion won recently. Furthermore, the ratio of drug expenses in the total expenditure of the insurance reached about 25%, showing the tendency to be levelled off. As a measure to improve the financial deterioration of the insurance and to encourage generic substitution among the health professionals, we compared pharmacokinetic parameters of brand name drug (Lamisil) and generic drug (Muzonal) containing terbinafine HCl in healthy volunteers. The area under the curve (AUC) of the two drugs showed 2220.4 ± 784.7 and 2143.1±861.6hr.mg/㎖ in the corresponding order and no statistically significant difference was identified. The peak concentration (Cmax) of the generic drug demonstrated 566.6±246.2 ng/㎖ compared to 550.8±204.0 of brand name drug, which was not significantly different either. Time to reach peak concentration showed about 6 minutes difference between the drugs, which has no clinical significance to the treatment of dermatomycosis and dermatophytosis.