Journal of Pharmaceutical Investigation

  • 제30권1호
  • /
  • Pages.21-26
  • /
  • 2000
  • /
  • 2093-5552(pISSN)
  • /
  • 2093-6214(eISSN)
한국약제학회 (The Korean Society of Pharmaceutical Sciences and Technology)
권호 표지

제제헝태에 따른 이프리플라본의 생체이용률 비교

Comparative Bioavailability of Ipriflavone by Pharmaceutical Preparation Types

  • 정제교 (전북대학교 고분자공학과) ;
  • 강길선 (전북대학교 고분자공학과) ;
  • 이종문 (전북대학교 고분자공학과) ;
  • 신호철 (한국화학연구소 약물독성동태팀) ;
  • 이해방 (한국화학연구소 생체의료고분자팀)
  • Jeong, Je-Kyo (Department of Polymer Science and Technology, Chonbuk National University) ;
  • Khang, Gil-Son (Department of Polymer Science and Technology, Chonbuk National University) ;
  • Rhee, John M. (Department of Polymer Science and Technology, Chonbuk National University) ;
  • Shin, Ho-Chul (Pharmacokinetics & Toxicokinetics Laboratory, Korea Research Institute of Chemical Technology) ;
  • Lee, Hai-Bang (Biomaterials Laboratory, Korea Research Institute of Chemical Technology)
  • 발행 : 2000.03.20
PDF 다운로드
⟨ 이전 논문 다음 논문 ⟩

초록

Bioavailability of ipriflavone (3-phenyl-7-isopropoxy-4H-I-benzopyran-4-one, IP), an antiosteoporotic drug with poor water-solubility, was studied for various types of pharmaceutical preparation in SD rats. The IP preparation types included (1) intact IP, (2) freezer milled IP (FIP), (3) freezer milled IP physically mixed with freezer milled poly-N-vinylpyrrolidone (PVP) (FIP+FPVP) and (4) spray-dried IP with PVP (SIP). Upon oral administration, SIP showed significantly higher absorption and elimination half-lives and the lag time $(t_{lag})$ than those of FIP+FPVP (approximately 2-fold). These results may be due to a sustained releasing effect of IP in the gastrointestinal tract by spray-drying with PVP. The $C_{max}$ of SIP was about 2 and 10 times higher than those of FIP+FPVP and FIP, respectively. The AUC of SIP was about 6 times higher than that of FIP+FPVP and 60 times that of FIP. Scanning electron microscopy (SEM) showed that SIP consisted of the finest particle size and minimal aggregation than other IP preparations. It is concluded that the IP formula prepared by the spray-drying method with PVP is the most effective approach to the improvement of bioavailability of IP.

키워드