케토프로펜 로오숀의 약물동력학적 특성과 항염증작용

단현광,배준호,박은석,지상철 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5㎎/㎏, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market, was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, C_max were 316±22.3ng/㎖ and 163±12.2ng/㎖, respectively, at the same T_max of 2 hours postdose, while C_max and T_max after oral administration of the drug were 1,030±89.1ng/㎖ and 0.25 hours, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageenen-induced edema method after 50㎎ of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while E-lotion showed 34.7%. The calculated ED_50 after transdermal application of ID-lotion was 2.5㎎/㎏, while that after oral administration was 7.0 ㎎/㎏. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.

케토프로펜 로오숀의 약물동력학적 특성과 항염증작용

단현광(Hyun Kwang Tan),배준호(Joon Ho Bae),박은석(Eun Seok Park),지상철(Sang Cheol Chi) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.1

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and Elotion, which is a 3% ketoprofen lotion in the Japanese market, was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, C_(max) were 316±22.3 ng/ml and 163 ±12.2 ng/ml, respectively, at the same T_(max) of 2 hours postdose, while C_(max) and T_(max) after oral administration of the drug were 1,030 ±89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and E-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageenen-induced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while E-lotion showed 34.7%. The calculated EDT after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.

케토프로펜 겔제제로부터 약물의 경피흡수

전흥원,단현광,지상철 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.1

In order to reduce the systemic side effects and gastrointestinal irritation of ketoprofen after its oral administration, it was formulated as a 3% ketoprofen gel (ID-GEL) with Pluronic F-127. The pharmacokinetic characteristics of ID-GEL was evaluated following its transdermal application on the dorsal skin of rats at the dose of 9 ㎎/㎏ in reference to those of existing 3% ketoprofen gels. Even though the maximum concentration of 810 ng/㎖ was reached at 6 hrs postdose, the plasma concentration was kept almost constant until 24 hrs postdose, which suggested that ketoprofen was released continuously from the gel during this period. The bioavailability of ID-GEL was two times higher than those of existing 3% ketoprofen gels, based on the calculated area under the plasma concentration-time curves after the percutaneous administration.

케토프로펜 겔의 궤양형성작용 평가

전흥원,지상철,단현광 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.2

The ulcerogenic activity of a 3% ketoprofen gel (ID-GEL) after its transdermal application in rats was determined with the Litchfield and Wilcoxon method in reference to the oral administration of ketoprofen in a suspension. The UD_(50) (dose producing ulcers in 50% of the rats tested) of ID-GEL after its transdermal application was approximately 4 times greater than that after the oral administration of the drug, indicating that the ulcerogenic activity of ketoprofen was much lowered with its transdermal application.

세파클러 서방정의 제조

손영택,박미영,김상린,단현광 德成女子大學校 藥學硏究所 2003 藥學論文誌 Vol.14 No.1

Cefaclor is a semisynthetic cephalosporin for oral administration. It is absorbed 50∼75% after oral administration and having a biological half life of 0.6∼0.9hours. To maintain therapeutic range, the drug should be administrated 3∼4 times a day, which leads to the saw both kinetic of the absorption and resulting in ineffective therapy. Hence many authors attempted to develop sustained/extended release dosage forms for cefaclor in order to achieve effective administrated regimens. In this study we attempted to formulate cefaclor sustained release tablet by using HPMC(hydroxypropyl methylcellulose) and vinyl pyrrolidone vinyl acetate complex, which can provide convenient administration and are economic and the drug release from HPMC matrix is uniform irrespective of the pH. The cefaclor sustained release tablets were prepared by wet granulation techinique. The wet granules were dried at 50℃ for 5 hours in a tray drier. The dried granules were passed through sieve #20, lubricated with magnesium stearate by mixing in rapid mixer granulator and compressed using 7kgf/cm² punch to get tablets. In vitro release of cefaclor form formulated tablets was carried out in 0.1N HCl for 30 minute at 37±0.5℃ and 100rpm. The formulated cefaclor tablets were kept for a short term accelerated stability study in high temperature at 20℃, 50℃ for 4 weeks. And the formulation 16 18 carried out long term stability study for 24 months.

케토프로펜 로오숀으로부터 약물의 피부투과

지상철(Sang Cheol Chi),박은석(Eun Seok Park),단현광(Hyun Kwang Tan),이윤석(Yun Seok Rhee) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.4

The effects of formulation variables of topical lotion on the skin permeation of ketoprofen were evaluated using excised rat skins. The formulation variables were the amounts of poloxamer 407, drug and ethanol, and penetration enhancers. The Keshary-Chien diffusion cells were used for the diffusion study. The flux of ketoprofen linearly decreased as the concentration of poloxamer increased from 5% to 15% in the preparation, and linearly increased as the amount of drug increased. Penetration enhancers such as fatty acids and fatty alcohols showed markedly enhancing effects at the level of 5%. Among them, the highest flux was shown in linolenic acid. From these results, optimum formula containing 3% ketoprofen, 5% poloxamer 407, 40% ethanol and 5% linolenic acid having the flux of 537.6 ㎍/㎠/hr were noted.

말산클레보프리드 서방성 제제의 제조 및 약물동태학적 평가

류해원(Hae Won Ryou),이주한(Joo Han Lee),지용하(Yong Ha Chi),한양희(Yang Hee Hahn),단현광(Hyun Kwang Tan),이규흥(Kyu Heung Lee),김상린(Sang Lin Kim),전승윤(Seung Yoon Jeon),최영욱(Young Wook Choi) 한국약제학회 2000 Journal of Pharmaceutical Investigation Vol.30 No.3

Clebopride malate(Cm) is a new benzamide drug which has a potent central antidopaminergic activity possessing antiemetic and anxiolytic properties. A purpose of this study was to assess the feasibility of formulating sustained release preparation by dispersing a drug in hydrophilic polymeric matrices and double layered tablets(DLT), using HPMC, carbopol, PEO, PVP/VA and other polymers as a rate controlling barrier. The matrix and DLT showed optimum dissolution pattern up to 8 hours and the contents of polymer were optimized at 30% level in this preparation. After an oral administration in beagle dog, Cm concentration was determined by use of GC-ECD and pharmacokinetic parameters were calculated by Vallner`s method. The AUC of DLT showed similar results and the duration of action was increased 55% compared to that of regular release dosage form. The calculated absorption rate effectiveness(ARE) and controlled release effectiveness(CRE) for DLT increased 50% compared to that of matrix, the overall effectiveness(E) of this product appears to be about 70%. in vivo effectiveness test, DLT showed significant differences from control on antiemetic action of Cm. In consequence, it was possible to conclude that double layered tablet might be a good candidate for the sustained release dosage forms.