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논문 기본 정보

자료유형
학술저널
저자정보
Kim, Iksoo (College of Pharmacy, Chung-Ang University) Kim, Hyeongmin (College of Pharmacy, Chung-Ang University) Ro, Jieun (College of Pharmacy, Chung-Ang University) Jo, Kanghee (College of Pharmacy, Chung-Ang University) Karki, Sandeep (College of Pharmacy, Chung-Ang University) Khadka, Prakash (College of Pharmacy, Chung-Ang University) Yun, Gyiae (Department of Food Science and Technology, Chung-Ang University) Lee, Jaehwi (College of Pharmacy, Chung-Ang University)
저널정보
한국응용약물학회 Biomolecules & Therapeutics(구 응용약물학회지) Biomolecules & therapeutics 제23권 제3호
발행연도
2015.1
수록면
296 - 300 (5page)

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${\beta}$-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of ${\beta}$-lapachone as well as its first-pass metabolism in the liver, and small and large intestines after oral administration to measure the absolute bioavailability in rats. A sensitive HPLC method was developed to evaluate levels of ${\beta}$-lapachone in plasma and organ homogenates. The drug degradation profiles were examined in plasma to assess the stability of the drug and in liver and intestinal homogenates to evaluate first-pass metabolism. Pharmacokinetic profiles were obtained after oral and intravenous administration of ${\beta}$-lapachone at doses of 40 mg/kg and 1.5 mg/kg, respectively. The measured oral bioavailability of ${\beta}$-lapachone was 15.5%. The considerable degradation of ${\beta}$-lapachone was seen in the organ homogenates but the drug was quite stable in plasma. In conclusion, we suggest that the fairly low oral bioavailability of ${\beta}$-lapachone may be resulted from the first-pass metabolic degradation of ${\beta}$-lapachone in the liver, small and large intestinal tracts and its low aqueous solubility.

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