• The Effect of Bead Size and Drug Solubility on Drug Release from Osmotic Granule Delivery System for Nifedipine
  • Jeong SC, Chon SK, Jo YH, Kim MS, Lee B, Khang G, Lee HB
  • 니페디핀의 삼투정 과립 시스템에서 과립의 크기와 약물의 용해도가 약물의 방출에 미치는 영향
  • 정성찬, 전세강, 조영호, 김문석, 이봉, 강길선, 이해방
Abstract
Osmotic granule system which is one of the drug delivery systems has been developed to improve manufacturing process and other problems of tablet osmotic systems. It consists of water swellable seed layer, nifedipine drug layer, and drug release controlled membrane layer and manufactured by fluidized bed coater. The granule size and membrane thickness can be controlled by various amounts of seed and coating solution, respectively. It could be observed that the morphology of osmotic granule was different at each coating step as well as type of coating solution. The bigger the size of granule, the slower the release rate was observed due to decreasing the total specific surface area of granule. Also, it was observed that the increase of membrane thickness was caused to retard the dissolution of nifedipine due to decreasing the water absorption rate. The drug solubility for dissolution media is greatly affected to nifedipine release. From these results, we assured that osmotic granule can be fabricated by fluidized bed coating methods, and the appropriate release profile could be controlled by the controlling of bead size, membrane thickness and dissolution media.

약물을 전달하기 위한 많은 방법들 중의 하나인 삼투압을 이용한 과립화는 타블렛 체형의 단점인 제조공정의 복잡함과 여러 문제점을 보완하기 위해 시도되었다. 유동층 코팅기로 제조된 삼투압을 이용한 과립은 물을 흡수하면 팽윤하는 시드층과 모델 약물인 니페디핀을 포함하는 약물층, 그리고 약물의 방출을 조절할 수 있는 반투막으로 구성되었다. 서로 다른 크기와 반투막의 두께는 각기 다른 양의 시드와 반투막 코팅액을 사용하여 얻을 수 잇었다. 얻어진 과립은 각코팅 단계에 따라서 서로 다른 모폴로지는 코팅되는 용액의 형태에 따라 다르게 나타났다. 과립의 크기가 클수록 방출은 지연되며, 이는 과립이 가지는 비표면적의 차이로 인한 것이라 사료된다. 또한 반투막의 두께가 두꺼울수록 약물의 방출이 지연되는데 이는 반투막이 두꺼울수록 물의 흡수가 늦어지는 것으로 추정된다. 용출액의 약물 용해도는 약물의 방출에 큰 영향을 미쳐 용출액 선택의 중요성을 알 수 있었다 .이 실험을 통해 삼투압을 이용한 과립은 유동층 코팅을 이용하여 제조할 수 있었으며, 과립의 크기와 반투막의 두께, 용출액에 따라 약물의 방출을 조절할 수 있음을 확인하였다.

Keywords: osmotic drug delivery system; granulation; fluidized bed coating

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    ISSN 0379-153X(Print)
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This Article

  • 2005; 29(3): 288-293

    Published online May 25, 2005