케토프로펜 로오숀의 약물동력학적 특성과 항염증작용

박은석,지상철,단현광,배준호 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.

랫드에서 fluoroquinolone 항균제 DW-116 의 단회 경구투여에 의한 태반통과와 약물동태연구

김종춘,윤효인,신호철,허정두,이종화,정문구 한국응용약물학회 2002 Biomolecules & Therapeutics(구 응용약물학회지) Vol.10 No.4

마이크로에멀젼으로 제제 설계된 피록시캄 외용제의 약물동력학적 특성 및 약효 평가

박은석,지상철,윤범진 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.1

The pharmacological activities and pharmacokinetic aspects of a topical microemulsion (KDPM) containing 0.5% piroxicam were evaluated after its topical application compared with a commercially available 0.5% piroxicam gel (R gel). When the pharmacological activities were evaluated with the carrageenaninduced paw edema model, KDPM showed 55.6% edema inhibition, while R gel resulted in 37.1%. With the adjuvant-induced arthritis model, KDPM also resulted in the better pharmacological activities than R gel. The relative bioavailability of KDPM based on R gel was 176% in rabbits.

CJ-50001 (recombinant human granulocyte-colony stimulating factor)의 흰쥐와 개에서의 약물동태학적 연구

김성남,신재규,이수정,정용환,하석훈,김기완,고형곤,김제학 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.4

The pharmacokinetics of CJ-50001 (recombinant human granulocyte-colony stimulating factor, developed by R&D center of Cheil Jedang Corp.) were investigated in rats and dogs. The serum concentrations of CJ-50001 were measured by a sandwich enzyme immunoassay. After single intravenous (iv) administration of Cf-50001 to rats at a dose of 5 $\mu$g/kg, the mean terminal half-life and area under the concentration-time curve (AUC) were 0.96 h and 124.497g . h/ml, respectively. After single subcutaneous (sc) administration at the same dose, maximum serum concentration was observed at about 2 hours after administration, and the mean terminal half-life, AUC and the bioavailability were 1.11 h,63.58$\mu$g . h/ml and 51.07%, respectively. In repeated dosing studies, CJ-50001 was administered iv and sc to rats at a daily dose of 5$\mu$g/kg for 7 days. The pharmacokinetic parameters, such as mean AUC and terminal half-life, were no significantly different from those of single administration. Following single iv and sc administration of CJ-50001 to dogs at a dose of 5 $\mu$g/kg, mean AUCs were much higher than those of rats, due to the decreased clearence (CL). After sc administration to dogs, maximum serum concentration was observed at 2~4 hours after administration and the bioavailability was 54.60%.

랫트에서 한국형유산균인 Bifidobacterium breve K-110, K-111 및 infantis K-525 균주제제의 경구투여 급성독성

이영경,한명주,최응칠,김동현 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.4

Acute oral toxicity of Bifidobacterium breve K-110, Bifidobacterium breve K-111, Bifidobacterium infantis K-525 were studied in Sprague-Dawley rats of both sexes. In this study, we examined number of deaths, clinical signs, bod weight and gross findings for 14 day after single oral administration of B. breve K-110,B. breve K-111 or B. infantis K-525 with different levels. They did not show any toxic effect in rats and oral LD$_{50}$ value was over 5 g/kg in rats.s.

랫트에서 한국형유산균인 Bifidobacterium breve K-110,K-111 및 B. infantis K-525 균주제제의 경구투여 급성독성

김동현,최응칠,한명주,이영경 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.4

Acute oral toxicity of Bifidobacterium breve K-110, Bifidobacterium breve K-111, Bifidobacterium infantis K-525 were studied in Sprague-Dawley rats of both sexes. In this study, we examined number of deaths, clinical signs, body weight and gross findings for 14 days after single oral administration of B. breve K-110, B. breve K-111 or B. infantis K-525 with different levels. They did not show any toxic effect in rats and oral LD_(50) value was over 5 g/㎏ in rats.

김학성 박사 연보 ( 응용약물학회지 제 10 권 제 1 호 : 2002 년 )

학회자료 한국응용약물학회 2002 Biomolecules & Therapeutics(구 응용약물학회지) Vol.10 No.1

한국 Streptomyces sp. 로 부터 분리한 방향족 화합물과 지질 화합물의 세포독성 연구

염곤,신석우 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2

In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Streptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388D1 and L1210. While the IC_(50) values of compound 2 against P388D1 and L1210 were 0.073 ㎍/㎖ and 0.07 ㎍/㎖, respectively, and the IC_(50) value of Compound 3 was 0.17 ㎍/㎖ against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.

한국 독사독으로부터의 혈전 용해제 개발에 관한 연구 II. 살모사(A. bromhoffi brevicaudus) 사독 Protease의 특성과 혈전 용해능에 관한 연구

김병재,이문한,임종섭,이항,이혜숙,김종호,채창수,Kim, Byoung-Jae,Lee, Mun-Han,Rim, Jong-Seop,Lee, Hang,Lee, Hye-Suk,Kim, Jong-Ho,Chai, Chang-Su 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.2

The biochemical properties of the fibrinolytic protease of 50,800 Da isolated from the venom of Kgdistrodon blomhoffi brevicaudus were characterized. The enzyme hydrolyzed the carboxyl side of arginine in the synthetic chromogenic peptides, N-Benzoyl-Phe-Val-Arg-pNA and N-p-Tosyl-Gly-Pro-Arg-pNA, and the enzyme activity was inhibited by phenylmethylsulfonylfluoride indicating that the enzyme belongs to the serine protease family. The pretense showed maximum activity at pH 7.5 and inhibited by ZnCl$_2$, CuSO$_4$, but not by soybean trypsin inhibitor, pepstatin A, 2-mercaptoethanol and EDTA. The fm value determined with N-p-Tosyl-Gly-Pro-Arg-pNA was 0.2 mM. The thrombolytic activity of the purified enzyme was evaluated by platelet aggregation test in rabbits. While the platelet count ratio in blood of the rabbits injected with thrombin alone declined from 1.0 to 0.6 within 7 min and maintained around 0.6 for 24 hours thereafter, the ratio rapidly recovered from around 0.6 to 0.8 in 1 hr, to 1.0 in 24 hrs when the rabbits were sequentially treated with thrombin and the purified enzyme. The result showed that the serine protease from A. blomhoffi brevicoudus of 50,800 Da had a thrombolytic activity in vivo and the enzyme might be developed as a therapuetic agent for the treatment of thrombic disease.

간장내 허혈 및 재관류시 약물대사 효소계의 지질 과산화에 관한 연구

이상호,조태순,이선미,박미정,박두순 한국응용약물학회 1994 Biomolecules & Therapeutics(구 응용약물학회지) Vol.2 No.2

This study was done to determine whether specific alterations exist in hepatic microsomal function after varying periods of ischemia (IS) and reperfusion (RP) during microsomal lipid peroxidation occurs. Rats were pretreated with α-tocopherol to inhibit lipid peroxidation or with vehicle (soybean oil). Control animals were time-matched sham-ischemic animals. Four groups of animals were studied: Group 1 (sham), group 2 (30 mins IS), group 3 (60 mins IS) and group 4 (90 mins IS). After 1, 5 or 24 hr of reperfusion, liver microsomes were isolated and cytochrome P-450s were studied. In all vehicle-treated ischemic rats, serum ALT levels peaked at 5 hr and were significantly reduced by α-tocopherol pretreatment. Similarly, microsomal lipid peroxidation was elevated in all vehicle-treated ischemic animal groups, but this elevation was prevented by α-tocopherol pretreatment. Cytochrome P-450 content was significantly decreased in both group 3 and group 4. In all vehicle-treated ischemic animal groups, aminopyrine N-demethylase activity was significantly decreased for the entire reperfusion period. α-Tocopherol inhibited reductions of cytochrome P-450 content and aminopyrine N-demethylase activity at both 1 hr and 5 hr of reperfusion but did not affect the reduced levels of cytochrome P-450 content and aminopyrine N-demethylase activity at 24 hr of reperfusion. Aniline p-hydroxylase activity was significantly decreased in group 4, whereas it was increased in group 3. These decreases and increases were prevented by α-tocopherol pretreatment. Our finding suggests that abnormalities in microsomal drug metabolizing function occur during hepatic ischemia and reperfusion in vivo and this is attributed to microsomal lipid peroxidation.