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Development of Coated Nifedipine Dry Elixir as a Long Acting Oral Delivery with Bioavailability Enhancement
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  • Development of Coated Nifedipine Dry Elixir as a Long Acting Oral Delivery with Bioavailability Enhancement
  • Development of Coated Nifedipine Dry Elixir as a Long Acting Oral Delivery with Bioavailability Enhancement
저자명
Choi. Jae-Yoon,Jin. Su-Eon,Park. You-Mie,Lee. Hyo-Jong,Park. Yo-Han,Maeng. Han-Joo,Kim. Chong-Kook
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2011년|34권 10호|pp.1711-1717 (7 pages)
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대한약학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

To develop the long acting nifedipine oral delivery with bioavailability enhancement, a nifedipine dry elixir (NDE) containing nifedipine ethanol solution in dextrin shell was prepared using a spray-dryer, and then coated nifedipine dry elixir (CNDE) was prepared by coating NDE with Eudragit acrylic resin. The physical characteristics and bioavailability of NDE and CNDE were evaluated, and then compared to those of nifedipine powder. NDE and CNDE, which were spherical in shape, had about 6.64 and $8.68-8.75{mu}m$ of geometric mean diameters, respectively. The amount of nifedipine dissolved from NDE for 60 min increased about 7- and 40-fold compared to nifedipine powder in pH 1.2 simulated gastric fluid and pH 6.8 simulated intestinal fluid, respectively. Nifedipine released from CNDE was retarded in both dissolution media compared with that from NDE. After oral administration of NDE, the $C_{max}$ and $AUC_{0{ ightarrow}8h}$ of nifedipine in rat increased about 13- and 7-fold, respectively, and the $T_{max}$ of nifedipine was reduced significantly compared with those after oral administration of nifedipine powder alone. The $AUC_{0{ ightarrow}8h}$ and $T_{max}$ of nifedipine in CNDE increased markedly and the $C_{max}$ of nifedipine in CNDE was significantly reduced compared to those in NDE. It is concluded that CNDE, which could lower the initial burst-out plasma concentration and maintain the plasma level of nifedipine over a longer period with bioavailability enhancement, might be one of potential alternatives to the marketed long acting oral delivery system for nifedipine.