세팔렉신 함유 생체막점착성 마이크로캅셀의 생체이용율 평가

지웅길,한건,정연복,김정환 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.4

Bioadhesive microcapsules of cephalexin, using Eudragit RS/RL coated with polycarbophil or carbopol, were evaluated biopharmaceutically. The GI transit of microcapsules in rats was studied. Bioadhesive microcapsules coated with polycarbophil or carbopol were shown to have substantially longer GI transit time than Eudragit RS/RL microcapsule. The delay in transit time was due to bioadhesion of the polymer to the mucin-epithelial cell surface which was clearly observable on animal autopsy. Plasma drug levels in rabbits showed that bioadhesive microcapsules resulted in a longer duration of action and greater bioavailability than other microcapsule or drug powder. Thus, the principle of bioadhesion can significantly improve therapy, due to a reduced rate of gastric emptying, an increase in contact time, and the intimacy of contact of the drug with the absorbing membrane.

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.

초록집 ( 1992 . 5 . 6 ) : 제 3 분과 ( 임상 , 안전성 평가 , 제제 ) ; 마이크로캅셀화에 의한 조절방출제제 개발 1 ; 유드라짓 마이크로캅셀화에 의한 β-락탐계 항생제의 방출제어

지웅길,한건,정연복 한국응용약물학회 1992 학술대회 Vol.1992 No.1

O-Ethoxybenzamide의 安定性에 關한 硏究

智雄吉 보건장학회 1976 보건장학회보연구논문집 Vol.5 No.-

어린이의 疾患과 治療

智雄吉 藥業新聞社 1976 醫藥情報 Vol.1976 No.12

중이염 치료용 암피실린 - 폴리락트산 필름의 약물방출조건

지웅길,나성범,정서영,박기동,전성균,구현철,양승은 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.1

A new local drug delivery device to treat otitis media (OM) has been developed. This device consists of a biodegradable poly(L-lactic acid) (PLLA) film containing antibiotic (ampicillin, AMP), which can be placed into the middle ear cavity and release the therapeutic concentration of AMP for prolonged period. Biodegradable films containing AMP (10 w/w%) were prepared by solution casting method using a suspension of the drug in a PLLA/CH₂Cl₂ solution (molecular weight of PLLA, 100,000 (100 K) and 300,000 (300 K), respectively). PLLA-AMP films were characterized by FTIR, DSC, and SEM. In vitro release of AMP from AMP-PLLA films were examined. The release pattern of AMP from AMP-PLLA films remained consistent from 1 day to 14 days, and the release rates of AMP from AMP-l00K-PLLA film and AMP-300K-PLLA film were 0.7384 ㎍/㎖/day, 0.4107 ㎍/㎖/day, respectively.

비이온성 미셀용액과 수중유형 마이크로에멀젼계의 특성 및 수단 IV의 가용화

지웅길,황성주,장은옥,현종목 대한약학회 1995 약학회지 Vol.39 No.5

The O/W microemulsion systems were made from 2 or 4% (w/w) oil (soybean oil, olive oil or isopropyl myristate) and 10, 15 or 20% (w/w) Brij 96. They were compared with micellar solution of equivalent surfactant concentration m therms of physicochemical properties, and the solubilization of sudan IV. They were characterized by dynamic light scattering, stability, surface tension, viscosity and rheogram. The mean diameters of O/W microemulsion systems were 10-15nm, and those of Brij 96 micellar solutions were 18-19 nm. Both of them were monodisperse systems. The O/W microemulsion systems showed Newtonian flow and their apparent viscosities were lower than those of micellar solutions. The surface tensions of O/W microemulsion systems were increased or decreased depending on the types of oil used, when compared with those of micellar solutions. The O/W microemulsion systems were very stable, and did not show any flocculation or aggregation. Their mean diameters were not changed after three months. But oxidation was observed in microemulsions without nitrogen gas at high temperature. There was a significant improvement in the sudan IV solubffimtion in micromulsion compared with that m the micellar solution containing equivalent concentration of surfactant. The size distribution and mean diameters of O/W micromulsions were not changed when sudan IV was solubilized.

병풀(Centella asiatica)엑스 - 베타시클로덱스트린 고체 분산체를 함유한 폴록사머 407 히드로겔 제조 및 피부투과

지웅길,박목순,이계원,박진규,김경국,곽은선 한국약제학회 1998 Journal of Pharmaceutical Investigation Vol.28 No.1

Extract of Centella asiatica(ECA), which is poorly water-soluble extract from the Centella asiatica is known to express excellent wound healing properties. ECA-β-cyclodextrin (asiaticoside-β-cyclodextrin and genin-β-cyclodextrin) solid dispersion system, which was prepared by freeze-drying method, was formulated as gels containing poloxamer 407 and propylene glycol, and evaluated with respect to their viscosity, stability, skin permeation and drug amount in the skin of hairless mouse. The average molar ratio asiaticoside-β-CD and genin-β-CD was 1:1.7 and 1:22. respectively. When the molar ratio of genin and β-CD was 1:5, madecassic acid made 100% solid dispersion system and asiatic acid about 65%. In dissolution study. >99% of asiaticoside from asiaticoside-β-CD was dissolved in 5 minutes, and >99% madecassic acid and >64% asiatic acid from genin-β-CD. The apparent viscosity of poloxamer 407 gels with ECA-β-CD solid dispersion system increased in proportion to poloxamer 407 and propylene glycol concentration. In the accelerated stability test, all ECA-β-CD poloxamer 407 gels showed that asiaticoside was most stable and madecassic acid stable and asiatic acid similar to stability of gel with free ECA. The permeation amount of asiaticoside in poloxamer gels through hairless mouse skin decreased as the concentration of poloxamer 407 increased. When propylene glycol was added at the level of 10%, the permeation amount of asiaticoside at poloxamer gels through hairless mouse skin increased but from 15% it decreased. The permeation of asiaticoside into the skin of hairless mouse was estimated to be about 0.10㎍/㎠.

무스콘의 β-시클로덱스트린 포접 복합체의 제조 및 평가

지웅길,이계원,곽은선,조인숙,박대규 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.4

An inclusion complex of muscone with β-cyclodextrin (CD), as a solid form of muscone, was prepared to increase the solubility of muscone. The molar ratio of muscone to β-CD in complex was in the range of 1:1∼1:5 when prepared by freeze-drying method: The interaction of muscone with β-CD in solid state was investigated by Infrared (IR) spectroscopy and differential scanning calorimetry (DSC). IR and DSC studies between muscone-β-CD inclusion complex and physical mixture showed that muscone-β-CD inclusion complex was prepared stably. From the amount of muscone incorporated in the inclusion complex, it was found that the molar ratio of muscone : β-CD was 1:1. Relative spatial position of muscone and β-CD was observed by Hyperchem molecular modelling program.

케토프로펜을 함유하는 고형 지질 나노파티클의 제조 및 평가

지웅길,백명기,이상영 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.4

Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage: low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile. SLN as a new drug delivery system is known to entrap drugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods. ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about 0.1 ㎛, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative. -9∼13mV and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. T_(max) was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.