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리포좀에 봉입된 5-플루오로우라실 프로드럭의 약물 동태 및 장기 분포
이계원(Gye Won Lee),지웅길(Ung Kil Jee) 대한약학회 1996 약학회지 Vol.40 No.5
In cancer chemotherapy, it is necessary to control the phamacokinetic behavior of an antitumor drug for effective treatment. Therefore, two 5-fluorouracil derivatives synthesized with N-a-cyloxycarbonyl derivatives {1-(N-t-butyloxycarbonyl)leucyloxymethyl-5-FU(BLFU) and 1-(N-t-carbobenzyloxymethyl)leucyloxymethyl-5-FU(CLFU)}. prodrugs of 5-fluorouracil, antitumor agent, were loaded into liposome of different lipid compositions. After liposomal drugs were injected intramuscularly, their pharmacokinetics and tissue distribution were assessed. The AUC0->infinity values were 1.29, 72.50, 85.57, 66.40 and 103.60mcg.hr/ml for 5-FU, BLFU, CLFU, BLFU- and CLFU-loaded liposome, respectively. 5-FU was distributed to spleen and liver with a maximal concentration after 1 hr and eliminated after 24 hr. But both prodrugs and dimyristoylphosphatidylcholine liposome entrapped prodrugs were distributed to spleen and liver at a lower concentration but maintained for a long time with a relatively high concentration in lung. Especially, liposome-entrapped CLFU was distributed to lung with a maximal concentration after 1 hr and redistributed to spleen increasingly, while the concentration of liposome-entrapped BLFU in lung reached a maximal level after 12 hr.
이계원(Gye Won Lee),이주연(Ju Yeon Lee),조영호(Young Ho Cho) 한국생물공학회 2010 KSBB Journal Vol.25 No.1
본 연구에서는 가래나무 추출물의 항산화 효과와 티로시나제 활성 저해, 멜라닌 생성 및 티로시나제 합성 억제 효과를 측정하고 이 추출물을 함유하는 제품의 임상시험을 실시하여 미백 화장품 소재로서의 개발 가능성을 관찰하였다. 가래나무 추출물은 농도 의존적으로 DPPH radical 과 초산소 음이온 라디칼을 소거하였고, SC50 값은 각각 20 μg/mL 및 25 μg/mL 이었다. B16/BL6 멜라노마 세포를 이용하여 세포내 티로시나제 활성, 멜라닌 생성 및 티로시나제 합성 억제 효과를 측정한 결과 농도 의존적으로 티로시나제의 활성 및 멜라닌생성을 억제하였으며, 티로시나제 단백질의 합성도 감소시켰다. 또한, 임상시험을 통하여 가래나무 추출물을 함유한 화장품이 대조 제품에 비해 통계적으로 유의한 피부 미백 효과가 있음을 확인하였다. 이상의 결과를 종합해 볼 때 가래나무 추출물은 색소침착 방지와 개선에 효과있는 새로운 미백 원료로 개발할 수 있을 것으로 사료된다. Juglans mandshurica belongs to the family Juglandaceae is known to contain a wide range of pharmacological activities including anti-cancer, anti-inflammation, astringent, and anti-human immunodeficiency virus-type 1 (HIV-1). Melanogenesis refers to the biosynthesis of melanin pigment in melanocytes. In this study, to investigate the whitening activity of the extracts from Juglans mandshurica, we measured effects on a tyrosinase activity, a melanogenesis, and a tyrosinase synthesis in the B16/BL6 melanoma cells and an antioxidant activity. The extracts significantly scavenged a 1,1-diphenyl-2-picrylhydrazyl (DPPH) and a superoxide anion radicals in a dose-dependent manner with a SC50 value of 20 μg/mL and 25 μg/mL, respectively. Also, the tyrosinase activity and melanogenesis were significantly inhibited by the extracts. Furthermore, the synthesis of tyrosinase protein was ignificantly decreased by the extracts in enzyme-linked immunosorbent assay. Double blind study on the clinical efficacy of a cream containing 2% of the extracts showed that the extracts have a significant skin whitening effect. Therefore, this study demonstrates that the extracts from Juglans mandshurica may be useful as a potential agent for skin whitening.
경피제제로서 수종의 플루비프로펜 Vehicle 과 O/W 마이크로에멀젼의 평가
이계원(Gye Won Lee),지웅길(Ung Kil Jee) 한국약제학회 1998 Journal of Pharmaceutical Investigation Vol.28 No.3
N/A In order to reduce systemic side effects following administration, flurbiprofen was formulated as O/W microemulsion consisting of the surfactant, oil phase and aqueous phase. Particle size distribution, apparent viscosity, solubility and skin permeation of flurbiprofen in various vehicles and microemulsion were evaluated. The domain of O/W microemulsion`s phase diagram had difference between oil types and the area of O/W microemulsion was wide distributed by adding to PG and cosurfactant than that of water alone. As increasing 10, 15 and 20% of Brij 97 content and 1, 2.5, 5% of oil content, the solubility of flurbiprofen in O/W microemulsions and various vehicles was 400∼1,000 and 10∼500 times higher than that of control. Also, apparent viscosity of soybean oil microemulsions was higher than that of IPM microemulsions and that of vehicle were increased as increasing vehicle content. Since skin permeation of flurbiprofen decreased as increasing viscosity, in each vehicle, it was not affected 2% β-CD and decreased as increasing PG content and to 2, 5 and 10% of HP-β-CD. In O/W microemulsion, 5% soybean oil, 20% Brij 97 and 75% water(A-1) with high viscosity showed low skin penetration.
김계원 ( Gye Won Kim ),이진호 ( Jin Ho Lee ),이슬애 ( Seul Ae Lee ),심재용 ( Jae Yong Shim ) 한국산업식품공학회 2012 산업 식품공학 Vol.16 No.3
This study was conducted to develop the optimum processing conditions for grape-makgeolli to improve its sensory characteristics. Quality characteristics of grape-makgeolli were also evaluated. Fermivin was selected as suitable yeast for fermentation because it provided a proper acid level and desirable fruit flavor, which was to enhance the stability of fermentation and maintain the acidity level for anthocyanin. The optimum adding period of grape was at the second mashing period by the fermentation profiles. Addition at second mashing period revealed that it had a richer flavor, a higher alcohol content, and a lower reducing sugar than addition at formulation. As addition of 20% grape could not produce a satisfying color in grape-makgeolli, addition of black rice as anthocyanin pigment could enable to enhance the natural color and flavor of grape-makgeolli. As a result, the usage of Fermivin as yeast, the addition of 20% grape at second mashing period and the addition of 2.5% black rice were the optimum conditions for manufacturing the grape-makgeolli.