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지방산 , 지방 알코올 및 프로필렌글리콜이 클렌부테롤의 경피투과에 미치는 영향
이영대(Yeong Dae Lee),권기철(Qi Zhe Quan),정시영(Si Young Jung),이종달(Jong Dal Rhee),용철순(Chul Soon Yong) 한국약제학회 1999 Journal of Pharmaceutical Investigation Vol.29 No.4
Clenbuterol, a selective β₂-adrenergic receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic bronchitis and pulmonary emphysema. For the purpose of developing a transdermal preparation for clenbuterol, we attempted to select an optimal solvent system and permeation enhancer among fatty acids and fatty alcohols which are known to accelerate the penetration of various drugs in permeation experiments using hairless mouse skin and Franz diffusion cell. Apparent partition coefficient of clenbuterol was increased as pH of buffer solution was increased and solubility of clenbuterol was increased as the percent of propylene glycol(PG) in buffer solution(pH 10) was increased. Permeability of clenbuterol from different buffer(pH 10)/PG solvent mixtures was decreased as the percent of PG in pH 10 buffer solution was increased and among the various enhancers studied, lauryl alcohol was found to be the most effective enhancer, increasing the permeability of clenbuterol approximately 76-fold compared with control. Lauryl alcohol(0∼2%) enhanced the permeability of clenbuterol concentration-dependently. In this study, the optimal solvent system for the penetration of clenbuterol was found to be 50/50 buffer(pH 10)/PG solvent mixture containing 2% lauryl alcohol.
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.
헬리코박터 파이로리 균 진단용 <sup>13</sup>C-요소 캅셀의 개발
용철순,김용일,김지만,강성훈,권기철,이종달,김종국,사홍기,최한곤,Yong, Chul-Soon,Kim, Yong-Il,Kim, Chi-Man,Kang, Sung-Hoon,Quan, Qi-Zhe,Rhee, Jong-Dal,Kim, Chong-Kook,Sah, Hong-Kee,Choi, Han-Gon 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.1
The purpose of this study was to develop a new $^{l3}C-urea-containing$ capsule for diagnosis of H. pylori. The urea-containing capsules were prepared with various diluents such as polyethylene glycol (PEG), microcrystalline cellulose, sodium lauryl sulfate and citric acid. The dissolution test, $^{l3}C-urea$ breath test and stability test were then performed on the capsules. Microcrystalline cellulose and sodium lauryl sulfate retarded the initial dissolution rates of urea. However, PEG increased the initial dissolution rates of urea. Furthermore, two formulae composed of PEG, [$^{l3}C-urea/PEG$ (38/1.9 mg/cap)] and [$^{l3}C-urea/PEG/citric$ acid (38/1.9/1.9 mg/cap)] had the maximum DOB value, about 16 at 20 mim, while the formula composed of only 38 mg $^{l3}C-urea$ had the maximum DOB value at 30 min. The results indicated that PEG improved the, sensitivity of $^{l3}C-urea$ in the human volunteers. The capsule [$^{l3}C-urea/PEG$ (38/1.9 mg/cap)] was stable for at least six months in 25 and $37^{\circ}C$. Thus, a PEG-containing capsule, [$^{l3}C-urea/PEG$ (38/1.9 mg/cap)] would be a more economical, sensitive and stable preparation for diagnosis of H. pylori.
김종오(Jong Oh Kim),권기철(Qi Zhe Quan),이종달(Jong Dal Rhee),최한곤(Han Gon Choi),용철순(Chul Soon Yong) 한국약제학회 2000 Journal of Pharmaceutical Investigation Vol.30 No.3
The purpose of this work is to develop a transurethral suppository containing prostaglandin E₁ (PGE₁), which stabilizes the drug, gives no irritation to physiological body and enhances the erectile response of PGE₁. PGE₁ transurethral suppositories were prepared with various amounts of compositions such as saturated polyglycolysed glyceride (Suppocire^ⓡ AP, SAP), polyoxyethylene hydrogenated castor oil (HCO-50) and ethanol. The melting points, viscosities and PGE₁ release of the suppositories were investigated. Ocular irritation test was carried out after application of PGE₁ suppository to rabbit`s eye. The intracavernous pressure (ICP), penile length and duration of erectile response were determined after transurethral administration of PGE₁ suppository and compared with those after intracavernosal injection of PGE₁ solution to cats. HCO-50 hardly affected the melting points and viscosities of PGE₁ suppositories. Additionally, PGE₁ transurethral suppositories, whose melting point ranges was 34-35℃, was speedily melted in physiological body. HCO-50 significantly decreased the dissolution rates of PGE₁ from the suppositories. Dissolution mechanism analysis showed the release of PGE₁ was proportional to the square root of time, indicating that PGE₁ might be released from the suppositories by Fickian diffusion. The release rate of PGE₁ from PGE₁ suppository [PGE1/SAP/HCO-50/ethanol (1/94.5/2.5/2%)] was about 80% within 2h. This PGE₁ suppository gave no significant irritation to the ocular tissue, expecting that it gave no irritation to the urethral tissue less sensive than ocular tissue. Furthermore, PGE₁ in this suppository was stable at 4℃ for 2 years. This suppository increased the ICP and penile erection similar to those of injectable PGE₁ solution. However, it gave 2.5-fold increased duration of erectile response than injectable PGE₁ solution. Our results suggested that it gave more effective erectile response than injectable PGE₁ solution in cats. It is concluded that this PGE₁ suppository with good safety, excellent stability and enhanced erectile response, could be a more effective and convenient transurethal delivery system of PGE₁.