ω-피리딜 알켄산의 형태와 활성간의 상관관계

이종달,도성탁 영남대학교 약품개발연구소 1998 영남대학교 약품개발연구소 연구업적집 Vol.8 No.-

Molecular mechanics and conformation search methods were carried out to investigate the relationship between conformations and thromboxane synthetase inhibitory activities of w-pyridylalkenoic acids. The initial geometries of w-pyridylalkenoic acids and heme part of cytochrome P-450 were obtained from MM+ geometry optimization. The bond lengths and angles were not varied by step during the conformation searching. Stable conformers of some w-pyridylalkenoic acids were obtained by conformational search method. The distances were 8.5~10.8Å between N atom at 3-position of pyridine ring and C atom at carboxylic group of stable w-pyridylalkenoic acids. The conformations of w-pyridylalkenoic acids and heme part complex were determined by same method. In these structures, benzene ring and ethylene group in w-pyridylalkenoic acids are making the structure more rigid and increase inhibitory activity. The electron donating groups in C atom which is connected to pyridine ring also increase activity.

레티노익 산의 형태와 구조-활성 관계 : 레티노벤조익 산 Retinobenzoic Acid

이종달,이인자 영남대학교 약품개발연구소 1994 영남대학교 약품개발연구소 연구업적집 Vol.4 No.-

The structure-activity relationships of (E)-chalcone-4-carboxylic acids, flavone-4'-carbo-xylic acids, two types of aromatic amides, terephthalic monoanilides, and (arylcarboxamido)benzoic acids, which were made by Shudo group, are discussed by conformation analysis(AM1) of retinoic acid and those compounds. Conformer of each compound is superimposed on the conformationally restricted compound, 4-(6, 7, 8, 9-tetrahydro-6, 6, 9, 9-tetramethyl-4H-4-oxonaphto[2, 3-b]pyran-2-yl)benzoic acid(Fv80), possessing the strongest differentiation-inducing activity on human promyelocytic leukemia cells HL-60. The results indicated that the lengths between the carboxylic carbon and the two 6, 9 carbons binding to dimethyl, 1.20 nm and 1.09 nm, as well as the planarity of molecule are very important factors for the activity, especially 1.20 nm. In the case of the recently synthesized azulenic retinoic acids by Sato, et al. in 1993, the distance probably is also important, resulted from superimposing them on a Ch55 conformer and Fv80. The distance 1.0 nm is also important in Ch55. Several conformers of all-trans retinoic acid (RA) are well superimposed on the almost non-flexible Fv80, RA, 9-cis RA, and, specifically s-10, 12 cis RA. And a simple hexangular model of RA is suggested to draw RA conformers easily without computer drawing model or molecular model.

色差의 三屬性 分解 (Ⅱ)

李鍾文,신영진,李達雨 全北大學校 1979 論文集 Vol.21 No.-

The fading behaviour of sorghum pigment may be expressed by the equation F(H_NBS)―~4.00(1-e^-0.2055^t) F(V_NBS)―~24.00(1-e^-0.2055^t) F(C_NBS)―~19.00(1-e^-0.2055^t) F(ΔE)―~30.87 (1-e^-0.2055^t) ―~√(F(H_NBS)^2+F(V_NBS)^2+F(C_NBS)^2) where t is the fading time(hr), and F(H_NBS), F(V_NBS), F(C_NBS), and F(ΔE) are the changes of color difference of Hue, Value, Chroma and ΔE due to light fading.

프로스타글란딘 E₁ 요도좌제의 제조 및 평가

김종오,권기철,이종달,최한곤,용철순 영남대학교 약품개발연구소 2000 영남대학교 약품개발연구소 연구업적집 Vol.10 No.-

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 intracavemous pressure(ICP), penile length and duration of erectile response were determined after transurethral administration of PGE₁ suppository and compared with those after intracavemosal 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 pro-portional 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 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 injuctable PGE₁ solution. However, it gave 2.5-fold increased dura-tion 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.

大規摸 染色工業團地 廢水의 綜合處理에 關하여

曺秉樂,李種達,朴永圭,李哲熙,李武康 嶺南大學校 環境問題硏究所 1981 環境硏究 Vol.1 No.1

In this study, a method of treating waste water from the Bisan Dyeing Industry complex has been developed. This process will be used as a model for treating waste water from the future large-scale dyeing industy complex. If the concentrated dyeing waste water may be seperated from the scouring waste water the C-2 process is the most economical to treat the concentrated dyeing waste water first by the coagulation precipitation process and the scouring waste water mixed with the effluent of coagulation precipitaion next by the activated sludge process. When it is impossible to seperate the concentrated dyeing waste water from scouring water for the Biasn Dyeing Industry complex, the B-2 process treating by the activated sludge process following coagulation precipitation with alum can be applied.

클렌부테롤의 피부투과에 미치는 경피흡수촉진제의 영향

최한곤,이종달,유봉규,용철순 한국약제학회 2003 Journal of Pharmaceutical Investigation Vol.33 No.1

Clenbuterol, a selective β_2-adrenergic receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease, chronic bronchitis and pulmonary emphysema. The percutaneous permeation of clenbuterol was investigate in hairless mouse skin after application of 50/50 buffer(pH 10)/propylene glycol solvent mixture. The enhancing effects of various penetration enhancers such as terpenes, non-ionic surfactants, pyrrolidones, fatty acids and some other enhancers on the permeation of clenbuterol were evaluated using Franz diffusion cell. Among terpenes studied, 1,8-cineole was the most effective enhancer, which increase the permeability of clenbuterol approximately 39.33-fold compared with the control without penetration enhancer, followed by menthone with enhancement ratio of 23.57. Nonionic surfactants did not have significant enhancing effects. N-Lauryl-2-pyrrolidone increased the permeability of clenbuterol approximately 4.51-fold compared with the control. Lauric acid increased the permeability of clenbuterol approximately 35.57-fold with decreasing the lag time from 2.64 to 0.52 hr. Oleic acid, linoleic acid, the permeability of clenbuterol 9.24-fold compared with that without enhancer.

고구배자기 분리기를 이용한 폐수처리와 자원 재활용에 관한 연구

오상오,김창수,이종달 慶北大學校 1979 論文集 Vol.27 No.-

In the application of magnetic separation procedures, ferrite and δ-FeOOH particles are proposed as magnetic seeding materials to remove many metal ions from waste water. New style of high gradient magnetic separation apparatus were prepared and obtained with good efficiency for removing the heavy metal ion from waste water. A mechanism for removing the heavy metal from the waste water has heen proposed to substitute iron ion of ferrite or δ-FeOOH for the other metal ion.

지방산, 지방 알코올 및 프로필렌글리콜이 클렌부테롤의 경피투과에 미치는 영향

이영대,권기철,정시영,이종달,용철순 영남대학교 약품개발연구소 2000 영남대학교 약품개발연구소 연구업적집 Vol.10 No.-

Clenbuterol, a selective β_(2)-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(pH10) 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 alcobol(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.

근린약국에서 산제로 조제된 아테놀올정의 안정성

용철순,최한곤,이종달,유봉규 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.4

Prescription filling in powder form is performed in community pharmacy practice to adjust dose for children and patients who cannot swallow whole tablet. However, there are few reports regarding the stability of the active ingredient and possible microbial growth after the medication is dispensed to powder form. This study examined the stability of atenolol, an antihypertensive agent, and microbial growth in the unit dose pouches dispensed at twenty-one community pharmacies located in Taegu area. Randomly chosen first unit dose pouch contained 77.4% of the prescribed dose of the drug and there were only four community pharmacies that dispensed the drug within 10% deviation from the dose prescribed by physician. Surprisingly, there were three community pharmacies that dispensed the drug with greater than 40% deviation, which may pose a major concern regarding the efficacy and safety of the drug prescribed for the treatment of hypertension. Atenolol content during a month did not indicate significant change, showing 5.4%, 4.3%, and 3.3% of decrease in 50%, 80%, and 90% relative humidity conditions, respectively. Microbiological examination during a month showed less than 0.5 microorganism in high power field (hpf) in all the relative humidity conditions tested. Based on this study, pharmacy practice in community pharmacy needs to be rigorously regulated to ensure that the dose of the prescribed drug is properly incorporated into the unit dose pouch dispensed as powder form.

클렌부테롤 경피흡수제제의 개발

최한곤,권기철,정시영,이종달,용철순 영남대학교 약품개발연구소 2001 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-

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 B_(2)-adrenergic receptor stimulant, has been introduced as a polent bronchodilator for patients with bronchial asthma, asthma, chronic obstructive bronchial disease. For the development of transdennal systems containing clenbuterol, two limiting factors ? long lag time and low flux - must be overcome. In this studym we altempted 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 enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of elenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Futhermore, 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 levelsin 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.