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Ibuprofen이 함유된 Microemulsion의 제조 및 떵가
양재헌(Jae Heon Yang),김영일(Young Il Kim),김현주(Hyun Ju Kim),정규호(Kyu Ho Chung) 대한약학회 2001 약학회지 Vol.45 No.6
Ibuprofen is one of the nonsteroidal anti-inflammatory drugs (NSAID) and has shown anti-inflammatory antipyretic, and analgesic activity in both animals and humans. But it causes gastric mucosal abnormalities including edema, erythema, and submucosal petechial hemorrhages and erosin in human. In addition, based on the pharmaceutical point of views the compression and dissolution ability of ibuprofen is known as poor Therefore we studied to develop novel formulation containing water-insoluble drug, ibu- profen, using microemulsion consisting of surfactant, oil phase, and water phase was prepared for the purpose of increasing its bioavilability The physicochemical properties such as particle sixte, dissolution rate, solubility of ibuprofen in the system were determined. After oral administration of ibuprofen containing the microemulsion system, to Sprague-Dawley rats, pharmacokinetic parameters were also obtained. For the formulation in the study; oleic acid, linoleic acid, and several kinds of glycerides and triglycerides were used as an oil phase with several surfactants. Diethylene glycol monoethyl ether (Transcutof?? ) or saturated polyglycolized glycerides (Labrasol??) as surfactant was used, the domain of microemulsion was wide. The diameter of o/w microemulsion was ranged from 90 to 220 nm. Microemulsion, prepared with unsaturated polyglycolized glycerides (Labrafil??) and the 2 : 1 molar mixture of diethylene glycol monoethyl ether (Transcutol??)/polyoxyethylene(4) lauryl ether (Brij?? 30), is expected to be promising system that increased the bioavilability of ibuprofen.
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정규호,김영일,양재헌 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.4
Piroxicam is one of the NSAID, which is used in the systemic and topical treatment of a variety of inflammatory conditions. Conventionally, for topical use, the drug is formulated in gel. We designed an phonophoretic drug delivery system to investigate the piroxicam permeability and the influence of ultrasound application (continuous mode, pulsed mode), frequency (1.0 MHz, 3.0 MHz) and intensity (1.0 w/㎠, 1.5 w/㎠, 2.0 w/㎠) with 0.5% piroxicam gel. Percutaneous absorption studies were performed in vitro models to determine the rate of drug absorption via the skin. Permeation study using hairless mouse skin was performed at 37℃ using buffered saline (pH 7.4, 10% propylene glycol solution) as the receptor solution. Anti-inflammatory activity was determined using carrageenan-induced foot edema model in rat. A pronounced effect of ultrasound on the skin absorption of the piroxicam was observed at all ultrasound energy level studied. Ultrasound was carried out for 10 hr. The highest permeation was observed at intensity of 2.0 w/㎠, frequency of 1.0 MHz and continuous output. The inclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory activity in vivo.
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독시사이클린 나노입자가 함유된 치주용 키토산 스트럽의 제조 및 특성
송경숙,양재헌,김영일,정규호 한국약제학회 2001 Journal of Pharmaceutical Investigation Vol.31 No.4
Local drug delivery by using biocompatible polymers has been developed in the treatment of periodontitis for many years. In the field of dental therapy, doxycycline is usually a first choice because of its broad-spectrum antibiotic activity. The strip releases antibiotics for a week, and the polymer should be degradable after a week. In this study, we prepared and evaluated the chitosan strips and nanoparticle strips containing doxycycline hydrochloride, and studied their antiacterial activity, dissoultion, and degrability in vitro. The weight of cast strip containing a 5 mg of doxycycline hydrochloride and a 45 mg of chitosan polymer was 57.67±0.17 mg. The release rate of doxycycline hydrochloride from the strip was measured by HPLC. The drug released from chitosan strip and nanoparticle strip was shown to be 50 ㎍/ml, in first 24 hours. In antibacterial test showed growth inhibitory activity after 24 hrs anaerobic incubation. In vitro degradability showed demolished weight of 93.74±0.08% chitosan strip, 82.48±1.29% chitosan nanoparticle strip, 2.47±1.99% polycarprolactione strip (control). These results showed that, with this doxycycline hydrochloride strip, it is feasible to obtain a sustained release of the drug within the periodontal pocket for seven days which may be improve for local drug delivery system for treatment of periodontal disease.
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