Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Effect of Molecular Weights and Mixture Ratios of Polyvinylpyrrolidone on the Bioavailability of Ipriflavone Solid Dispersion

이프리플라본 고체분산체의 생체이용률에 미치는 폴리비닐피롤리돈의 분자량 및 혼합비율의 영향

  • 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 Institutes of Chemical Technology)
  • 정제교 (전북대학교 고분자공학과) ;
  • 강길선 (전북대학교 고분자공학과) ;
  • 이종문 (전북대학교 고분자공학과) ;
  • 신호철 (한국화학연구소 약물독성동태팀) ;
  • 이해방 (한국화학연구소 생체의료고분자팀)
  • Published : 2000.12.20
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Abstract

Ipriflavone (3-phenyl-7-isopropoxy-4H-1-benzopyran-4-one, IP) is a well-known antiosteoporotic drug with poor bioavailability. In the previous study, we reported that the IP formulation prepared by spray-drying method with polyvinylpyrrolidone (PVP) (SIP) was very effective in improving the bioavailability of IP. In this study, we examined the effects of molecular weight and mixture ratios of PVP to IP on the systemic absorption of IP following oral administration of SIP at a dose of 50 mg/kg to rats. In the effect of molecular weight, the Cmax of spray-dried IP with PVP K30 (SIP-K30) was significantly higher than those of spray-dried IP with PVP 360 (SIP-360), spray-dried IP with PVP K90 (SIP-K90), and spray-dried IP with PVP K17 (SIP-K17) (p<0.05). The AUC of SIP-K30 was about 2, 3, and 5.5 times higher than those of SIP-360, SIP-K90, and SIP-K17, respectively. The AUC value of SIP-K30 was significantly greater than those of SIP-K17 and SIP-K90 (p<0.05) except for SIP-360. In the ratio of PVP K30 to drug, the $C_{max}$ and the AUC value of 3 : 7 IP-PVP solid dispersion were similar to those of 5 : 5 IP-PVP and significantly higher than those of the other solid dispersions (p<0.05). It was concluded that the spray-dried IP with PVP K30 at the ratio of 3:7 (w/w) was the best formulation for improving the bioavailability of IP.

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