• 제목/요약/키워드: acebutolol

검색결과 18건 처리시간 0.03초

토끼에서 체내담즙이 아세부톨롤의 생체이용률 및 체내동태에 미치는 영향 (Effect of Bile juice on the Bioavailability and Pharmacokinetics of Acebutolol in Rabbits)

  • 최준식
    • 약학회지
    • /
    • 제46권1호
    • /
    • pp.47-51
    • /
    • 2002
  • Although acebutolol (ABT) is almost completely absorbed in the gastrointestinal (Gl) tract, oral bioavailability of the drug is low due to extensive first-pass metabolism in the Gl tract and liver. In the present study, bioavailability and pharmacokinetics of ABT was studied in bile duct-bypassed rabbits after oral administration. For ABT the time to reach the plasma peak (T$_{max}$) and mean resident time (MRT) were increased by the treatment. For diacetolol (DAT), a metabolite of ABT area under the plasma concentration-time curve (AUC), T$_{max}$ and plasma half-life were increased by the treatment. These results indicate that oral bioavailability of ABT is associated with the enterohepatic recycling of bile juice components.nts.

Determination of Stability Constants of the Inclusion Complexes of ${\beta}$-Blockers in Heptakis (2,3-Dimethyl-6-Sulfato)- ${\beta}$-Cyclodextrin

  • Phuong, Nuyen Thi;Lee, Kyung-Ah;Kim, Kyung-Ho;Choi, Jung-Kap;Kim, Jong-Moon;Kang , Jong-Seong
    • Archives of Pharmacal Research
    • /
    • 제27권12호
    • /
    • pp.1290-1294
    • /
    • 2004
  • The ${\beta}$-blockers possess at least one chiral center and the S(-)-enantiomer shows higher affinity for binding to the ${\beta}$-adrenergic receptors than antipode. The stability constants of acebutolol, celiprolol, propranolol and terbutaline in the inclusion complexes with single-isomer heptakis (2,3-dimethyl-6-sulfato)- ${\beta}$-cyclodextrin (HDMS-${\beta}$-CD) were determined by capillary electrophoresis. The approximation and linear double reciprocal methods were adapted with comparable results. Among the ${\beta}$-blockers studied, propranolol had the lowest stability constant but the highest enantioselectivity, indicating that the magnitudes of the stability constants carried little information about enantioseparation. The magnitudes of enantioselectivities between the enantiomer pair were in the order of propranolol > celiprolol > terbutaline > acebutolol.

Chiral Separation of $\beta$-Blockers after Derivatization with (-)-Menthyl chloroformate by Reversed-Phase High Performance Liquid Chromatography

  • Kim, Kyeong-Ho;Choi, Pok-Wha;Hong, Seon-Pyo;Kim, Hyun-Ju
    • Archives of Pharmacal Research
    • /
    • 제22권6호
    • /
    • pp.608-613
    • /
    • 1999
  • Optimum conditions of chiral derivatization reaction of $\beta$-blockers (acebutolol, arotinolol, betaxolol, bisoprolol, celiprolol, metoprolol and pindolol) with (-)-menthyl chloroformate were investigated for the resolution by HPLC. With more than 30 times molar excess of (-)-methyl chloroformate chiral derivatization reactions were completed within one hour at room temperature except arotinolol and celiprolol. Diastereomeric derivatives of $\beta$-blockers were well resolved on the ODS column using acetonitrile-methanol-water as a mobile phase.

  • PDF

Carbamazepine으로 유발된 Bronchiolitis Obliterans Organizing Pneumonia 1예 (A Case of Carbamazepine Induced Bronchiolitis Obliterans Organizing Pneumonia)

  • 옥경선;박봉건;김희숙;이혜경;진성림;진재용;이혁표;김주인;최수전;염호기
    • Tuberculosis and Respiratory Diseases
    • /
    • 제48권5호
    • /
    • pp.794-801
    • /
    • 2000
  • 약제 유발성 BOOP의 경우는 약을 중단하여도 증상과 방사선학적 소견이 호전되지 않을 수 있고 부신피질스테로이드를 사용한 후 뚜렷한 호전을 보일 수 있기 때문에 BOOP를 일으킬 수 있는 약제에 대한 인지가 진단과 치료에 중요하다. 저자들은 carbamazepine에 의한 BOOP 1예를 경험하였기에 보고하는 바이다.

  • PDF