• Title/Summary/Keyword: ${\beta}$-Cyclodextrin-piroxicam

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Comparison of Absorption Rate Between Piroxicam-$\beta$-Cyclodextrin and Piroxicam in Korean Healthy Subjects After A Single Dose Administration (정상 성인 한국인에서 Piroxicam-$\beta$-cyclodextrin 정과 Piroxicam 확산정의 1회 투여시의 흡수속도 비교)

  • Jeon, Seong Sill;Cha, Hye Ri;Park, Yun Ju;Lee, Byung Chul;Kim, Nam Deuk
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.95-100
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    • 1998
  • Piroxicam-$\beta$-cyclodextrin은 piroxicam을 $\beta$-cyclodextrin으로 포접시킨 비스테로이드성 항염증약물이다. 이러한 포접형 약물은 위장관에서의 흡수속도가 증가하는 것으로 외국자료에서 보고되고 있으며 이는 이 약물의 위장관 내성에 보다 나은 영향을 끼칠 수 있음을 시사하고 있다. 본 연구는 정상성인 한국인을 대상으로 randomized, crossover design에 의해 piroxicam-$\beta-cyclodextrin(Brexin^{(R)})$과 piroxicam 확산정$(Feldene^{(R)})$ 흡수속도를 비교하고자 하였다. 건강한 성인 8명의 피험자를 2군으로 나누어 시험약 또는 대조약을 각각 20 mg씩 20일의 휴약 기간을 두고 이중 맹검으로 교차 투여하였다. 시험약 또는 대조약의 투여 후 24시간 동안 일정 간격으로 채혈하여 HPLC 방법으로 혈장 내 piroxicam 농도를 측정하였다. $AUC_{0-24}\;({\mu}g/mL)$는 piroxicam-$\beta$-cyclodextrin군에서 $56.1\pm4.9$, piroxicam군에서 $57.3\pm5.6$으로 통계적인 유의성이 없었으나, 투여 후 0.5시간에서의 혈중농도는 piroxicam-$\beta$-cyclodextrin군 $2.9\pm0.4\;{\mu}g/mL$, piroxicam군 $1.6\pm0.3\;{\mu}g/mL$으로 통계적인 유의성을 보였다(p<0.05). 또한 최고혈중농도는 piroxicam-$\beta$-cyclodextrin$(4.3\pm0.5\;{\mu} g/mL)\;piroxicam(3.5\pm0.3\l{\mu}g/mL)$,으로 유의성이 있었으며(p<0.05), 흡수 속도상수는 piroxicam-$\beta$-cyclodextrin$(3.00\pm0.49\;h^{-1}), \;piroxicam(1.80\pm0.21\;h^{-1})$이었다(p<0.1). 이상의 결과에서, piroxicam-$\beta$-cyclodextrin정은 piroxicam 확산정과 비교하여 흡수되는 정도는 서로 비슷하지만 흡수 초기의 혈장농도 및 흡수속도상수에서 보다 빠른 약동학적 특성을 나타내었다.

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Bioavailability Studies on Suspension of Inclusion Complexes of Piroxicam with Cyclodextrins (Piroxicam-Cyclodextrin 포접화합물의 현탁제에 대한 생체내 이용율의 연구)

  • Park, Sun Hee;Lee, Chang Hoon;Choi, Young Wook;Park, Gee Bae;Kim, Johng Kap
    • Korean Journal of Clinical Pharmacy
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    • v.1 no.1
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    • pp.9-14
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    • 1991
  • Inclusion complexes of piroxicam with $\alpha,\;\beta\;and\;\gamma- cyclodextrins$ were prepared and suspended to enhance the bioavailability of piroxicam. A quantitative analysis was employed HPLC for the determination of piroxicam in the rabbit serum after a single oral dose in suspension of piroxicam and each of inclusion complexes of piroxicam with $\alpha,\;\beta\;and\;\gamma- cyclodextrins$, respectively. The bioavailability and serum level of piroxicam exhibited the highest in piroxicam clathrated $\beta-cyclodextrin$ than both piroxicam and the other complexes administered. and the total area under the curve of serum concentration versus time for their inclusion complexes were larger than that of piroxicam.

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Complexation of Piroxicam and Tenoxicam with $Hydroxypropyl-{\beta}-cyclodextrin$ (히드록시프로필-베타-시클로덱스트린과 피록시캄 및 테녹시캄 간의 복합체 형성)

  • Kim, Ju-Hyun;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.30 no.1
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    • pp.33-37
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    • 2000
  • One of the methods to increase the solubility of a drug is to use complexation with a cyclodextrin. Due to the hydrophobic nature of the interior cavity of the cyclodextrin, it has been known that undissociated lipophilic drugs can be included within the cyclodextrin by hydrophobic interaction. Recently, inclusion of hydrophilic or dissociated form of a drug has been investigated. In this study, the synergism of pH and complexation with $hydroxypropy-{\beta}-cyclodextrin\;(HP\;{\beta}\;CD)$ to increase the solubility of two oxicam derivatives was investigated. In addition, the effect of partition coefficient of dissociated and undissociated form of the drug on the extent of complexation with HP ${\beta}$ CD was studied. The solubility was measured by equilibrium solubility method. The solubility of tenoxicam and piroxicam increased exponentially with an increase in solution pH above the pKa of the drug in the presence and absence of HP ${\beta}$ CD. The solubility of the drugs increased linearly as a function of HP ${\beta}CD$ concentration at fixed pH. Although the stability constant of ionized species is less than that of the unionized species, the concentration of the ionized drug complex is greater than that of the unionized drug complex due to higher concentration of ionized species at pH 7.3.

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The objective and quantitative analysis of malocclusion : Part 1. Objective malocclusion severity and subjective treatment difficulty (부정교합의 객관적 정량분석: Part 1. 객관적 부정교합 경중도와 주관적인 치료난이도의 상관관계)

  • Joo, Bo-Hoon;Lee, Ki-Soo
    • The korean journal of orthodontics
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    • v.35 no.1 s.108
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    • pp.60-68
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    • 2005
  • The evaluation of malocclusion has to be done quantitatively and qualitatively. This will be lead toward an analysis of malocclusion severity as well as treatment difficulty. The method of proper evaluation of malocclusion severity and treatment difficulty is necessary to assess treatment effect and efficiency for the orthodontists and to establish fundamentals for planning and executing the health-related policies in private and public institutions. The purposes of this study as the first part of the objective and quantitative analysis of malocclusion were 1) to measure treatment difficulty based on the opinions of several orthodontists. and 2) to investigate the relationships between objective malocclusion severity and subjective treatment difficulty 100 pairs of dental casts that had various types and severity of malocclusion were selected from the orthodontic departments of Kyurghee University and Samsung Medical Center The objective malocclusion severity was measured with the PAR (Peer Assessment Rating) index and the subjective treatment difficulty was evaluated by 8 experienced orthodontists. The relationships between objective malocclusion severity and subjective treatment difficulty were statistically evaluated. There were significant relationships between objective malocclusion severity and subjective treatment difficulty especially in the measurements of the upper anterior alignment, the buccal occlusion. the overjet, the overbite and the midline discrepancy en the malocclusion components. The results of this study can provide the background knowledge to develop a new occlusal index. which contains both the malocclusion severity and treatment difficulty for Korean orthodontists.