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마이크로플루다이저를 이용한 아클라루비신 리포좀의 제조 및 평가
박목순(Mork Soon Park),박진규(Jin Kyu Park),이계원(Gye Won Lee),백명기(Myoung Ki Baek),지웅길(Ung Kil Lee) 대한약학회 1998 약학회지 Vol.42 No.3
In order to attain a sustained release at targeted organs in a prolonged time which can reduce the side effects and maximize the therapeutic effect, aclarubicin (ACL) was entrapped into liposomes of different lipid compositions using Microfluidizer, and dry liposomes were prepared by lyophilization. The dry aclarubicin-entrapped liposomes were evaluated in terms of mean particle size and size distribution, entrapment efficiency and in vitro drug release profile. The Entrapment efficiency of liposome, when the concentration of aclarubicin and lipid were 0.5 to 1.0mg/ml and 200mcmol/ml,respectively, was over 80% using Microfluidizer, in contrast to 70% of entrapment efficiency using hand-shaking method. Mean particle size and size distribution of aclarubicin-entrapped liposomes of various lipid compositions did not change considerably by the freeze drying. The range of particle size was between 80 and 200nm. Among aclarubicin-entrapped liposomes, ACL-liposome of PC/DPPC/CH0L/TA displayed the most significant sustained release. The addition of DPPC appeared to be favorable for the control of release. In general, aclarubicin entrapped in liposomes was less stable than free aclarubicin either in pH 7.4 phosphate buffer or in human plasma. Formulation I(t1/2, 20.3 hr) devoid of lipid additive was the most unstable in the phosphate-buffer solution while formulation II(t1/2, 40.7 hr) with cardiolipin was the most stable. Half lives of aclarubicin-entrapped liposomes in human plasma were 43.2, 50.7, 35.9 and 35.3 hr for formulation I. II, III and IV, respectively, in contrast to 57.8 hr for free aclarubicin.
리포좀에 봉입된 아클라루비신의 약물동태, 세포독성, 항암효과 및 비장/혈구 세포독성
박목순(Mork Soon Park),박진규(Jin Kyu Park),이계원(Gye Won Lee),명평근(Pyung Keun Myung),석대은(Dai Eun Sok),황성주(Sung Joo Hwang),지웅길(Ung Kil Lee) 大韓藥學會 1998 약학회지 Vol.42 No.3
Aclarubicin(ACL)-entrapped freeze dried liposomes were prepared using Microfludizer to attain a sustained release at targeted organs in a prolonged time so that it can reduce the side effect and maximize the therapeutic effect. The freeze-dried liposomes were evaluated for pharmacokinetics, antitumor activity against Sarcoma 180, cytotoxicity against L1210 and A549 tumor cells, spleen toxicity and myelosuppressive action. The AUC0->8hr values were 122+/-42, 382+/-140, 419+/-171, 835+/-206 and 443+/-309mcg min/ml for free ACL. ACL-liposome formulation I, II, III and IV, respectively. Cytotoidcity of ACL-entrapped liposomes against L1210 and A549 tumor cells was 2-4 times higher than that of free aclarubicin. ACL-liposome formulation I(PC/CHOL/TA) showed the most potent antitumor activity against Sarcoma 180 in mice. The loss of body weight was much smaller with ACL-entrapped liposomes than free ACL after I.p. injection at a dose of 2 mg/kg/day. Compared to free ACL, ACL-entrapped liposomes expressed a lower and delayed spleen toxicity up to 5th day after I.v. administration. Myelosupperssion seemed to be lower with ACL-entrapped liposome of PC/PC-hydrate/CHOL/TA (formulation III) than free aclarubicin.
Norfloxacin과 ${\beta}-Cyclodextrin$간의 Inclusion Complex에 관한 약제학적 연구
지웅길,박목순,권중무,Jee, Ung-Kil,Park, Mork-Soon,Kwon, Joong-Moo 한국약제학회 1987 Journal of Pharmaceutical Investigation Vol.17 No.1
To increase the bioavailability of norfloxacin, inclusion complex of antimicrobial agent norfloxacin with ${\beta}-Cyclodextrin$ was prepared and studied by the solubility method, spectrophotometric methods(UV, IR, $^1H-NMR$), differential thermal analysis, powder X-ray diffractometry, the physical properties, the antimicrobial activity, DNA binding and in situ recirculation technique. The conclusions are summerized as following; 1) The inclusion complexation was identified by means of solubility, spectrophotometry(UV, IR, NMR), DTA and X-ray diffraction. 2) The molar ratio of $norfloxacin-{\beta}-cyclodextrin$ complex was 1 : 1. 3) The stability constant of $norfloxacin-{\beta}-cyclodextrin$ complex was $21.5\;M^{-1}$, and both true and apparent partition coefficients of the inclusion complex were larger than those of norfloxacin. 4) The time required to dissolve 60% $(T_{60}%)$ of the inclusion complex was 120 min. in distilled water and in the artificial intestinal juice, while norfloxacin did not reach to 60% dissolution within 120 min. 5) The antimicrobial activity of the inclusion complex against Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus showed no significant difference compared to that of norfloxacin alone. 6) Studies on binding properties between the inclusion complex and norfloxacin alone to DNA according to equilibrium dialysis showed no significant differency. 7) In situ absorption rates (Ka) of inclusion complex and norfloxacin alone were 0.229 and $0.102hr^{-1}$, respectively.
마이크로에멀젼을 이용한 프로포폴 주사제의 개발 및 평가
이종화(Jong Hwa Lee),박선영(Sun Young Park),김동우(Dong Woo Kim),조미현(Mi Hyun Cho),조인숙(In Suk Cho),이계원(Gye Won Lee),박목순(Mork Soon Park),지웅길(Ung Kil Jee) 대한약학회 2002 약학회지 Vol.46 No.5
Propofol(2,6-diisopropyl phenol) is a phenol derivative that is chemically distinct from other intravenous serdative hypnotics. It has been extensively used as a short term anesthetic agent, because of the rapid onset and short duration of action. Propofol microemulsion system was prepared with different concentrations of ethyl oleate, Solutol(R) HS 15 and Kollidon(R) 17 PF Propofol microemulsions were studied by transmittance, viscosity, Particle size, in vitro release and Pharmacokinetics. The range of transmittance of A group with 4% ethyl oleate and that of B group with 5% ethyl oleate were 2.6-95.1 and 91.3∼94.2%, respective17: Transmittance 1∼2% decreased as concentration of Kollidon(R)17 PF was increased and increased 0.8∼3.3% when 10 times diluted with normal saline. The viscosity of A and B group were in the range of 3.9∼ 4.1 mPa ·sec and 4.4∼5.3 mPa ·sec, respectively: The particle sizes of A and B group increased as amount of Kollidon(R) 17 PF Also, release of propofol was slowly increased as the amount of Kollidon (R) 17 PF was increased. Propofol plasma concentration by 1.v injection showed 2-compartment model. Pharmacokinetics of A-5 was similar to that of commercial emulsion(POFOL).
조한진(Han Jin Jo),나성범(Sung Bum La),남상철(Sang Cheol Nam),박목순(Mork Soon Park),지웅길(Ung Kil Jee) 대한약학회 1990 약학회지 Vol.34 No.2
To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, lbu-P.A., and lbu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The LD50 was 495mg/kg for ibuprofen, 187mg/kg for Ibu-M.P., and over 1250mg/kg for Ibu-P.A.. 6) The absorption rate constants(k) and half-life(t1/2) were 0.74(hr-1) and 0.94(hr) for ibuprofen, and 0.72 (hr-1) and 0.96 (hr) respectively for Ibu-M.P..