통합 검색 | Korea Science

Zanamivir Oral Delivery: Enhanced Plasma and Lung Bioavailability in Rats

Shanmugam, Srinivasan;Im, Ho Taek;Sohn, Young Taek;Kim, Kyung Soo;Kim, Yong-Il;Yong, Chul Soon;Kim, Jong Oh;Choi, Han-Gon;Woo, Jong Soo
- Biomolecules & Therapeutics
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- 제21권2호
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- pp.161-169
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- 2013
The objective of this study was to enhance the oral bioavailability (BA) of zanamivir (ZMR) by increasing its intestinal permeability using permeation enhancers (PE). Four different classes of PEs (Labrasol$^{(R)}$, sodium cholate, sodium caprate, hydroxypropyl ${\beta}$-cyclodextrin) were investigated for their ability to enhance the permeation of ZMR across Caco-2 cell monolayers. The flux and $P_{app}$ of ZMR in the presence of sodium caprate (SC) was significantly higher than other PEs in comparison to control, and was selected for further investigation. All concentrations of SC (10-200 mM) demonstrated enhanced flux of ZMR in comparison to control. The highest flux (13 folds higher than control) was achieved for the formulation with highest SC concentration (200 mM). The relative BA of ZMR formulation containing SC (PO-SC) in plasma at a dose of 10 mg/kg following oral administration in rats was 317.65% in comparison to control formulation (PO-C). Besides, the $AUC_{0-24\;h}$ of ZMR in the lungs following oral administration of PO-SC was $125.22{\pm}27.25$ ng hr $ml^{-1}$ with a $C_{max}$ of $156.00{\pm}24.00$ ng/ml reached at $0.50{\pm}0.00$ h. But, there was no ZMR detected in the lungs following administration of control formulation (PO-C). The findings of this study indicated that the oral formulation PO-SC containing ZMR and SC was able to enhance the BA of ZMR in plasma to an appropriate amount that would make ZMR available in lungs at a concentration higher (>10 ng/ml) than the $IC_{50}$ concentration of influenza virus (0.64-7.9 ng/ml) to exert its therapeutic effect.
https://doi.org/10.4062/biomolther.2013.010 인용 PDF KSCI

한국산(韓國産) Juniperus rigida의 두 산지(産地)의 핵형분석(核型分析) (Karyotype Analysis of Juniperus rigida Sieb. et Zucc. of Two Different Provenances in Korea)

김정석;정우규;안중극;정미정;한창숙
- 한국산림과학회지
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- 제73권1호
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- pp.9-13
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- 1986
Juniperus rigida의 경남(慶南)과 충북(忠北)의 두 산지종(産地種)에 대하여 핵형분석(核型分析)을 하였다. 염색체수(梁色體數)는 두 산지종(産地種) 공(共)히 2n=22이다. 두 산지종(産地種)에 있어 가장 공통적(共通的)인 특징(特徵)을 나타낸 염색체(染色體)는 두완(短腕)에 secondary constriction을 지닌 No.7 이고, 가장 특이적(特異的) 특징(特徵)을 한 염색체(染色體)는 secondary constriction을 지닌 경남산(慶南産)의 No.9와 충북산(忠北産)의 No.5 염색체(染色體)이다. 핵형식(核型式)은 다음과 같다. 경남산지종(慶南山地種) $$K(2n)=22=2A^m+2B^m+2C^m+2D^{sm}+2E^{st}+2F^m+2^{sc}G^m+2H^m+2^{sc}I^t+2J^{st}+2K^m$$ 충북산지종(忠北山地種) $$K(2n)=22=2A^m+2B^m+2C^m+2D^{st}+2^{sc}E^{sm}+2F^m+2^{sc}G^m+2H^m+2I^m+2J^{st}+2K^{sm}$$.
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