니페디핀을 함유한 생분해성 PLGA 웨이퍼의 제조와 특성분석

Characteristics of Nifedipine Loaded PLGA Wafer

  • 서선아 (전북대학교 고분자공학과) ;
  • 최학수 (전북대학교 고분자공학과) ;
  • 이동헌 (전북대학교 고분자공학과) ;
  • 강길선 (전북대학교 고분자공학과) ;
  • 이해방 (한국화학연구원 생체의료고분자연구팀)
  • 발행 : 2001.11.01

초록

고혈압 치료제로 사용되는 니페디핀을 지속적으로 방출하는 제형을 제조하기 위하여 poly(L-lactide-co-glycolide) 글리코리드와 랙티드의 몰비 50: 50, 분자량:5000 g/mole)를 이용하여 직접 압축성형 방법으로 생분해성 웨이퍼를 제조하였다. 약물과 고분자의 함량비, 웨이퍼의 두께, 하이드록실 메틸셀룰로오스 (HPMC) 함유량 등을 조절하여 PLGA 웨이퍼를 제조하였고, 이들의 형태학적 특성과 방출거동 및 분해거동을 조사하였다. 제조된 웨이퍼는 11일동안 영차의 안정한 방출거동을 보였고, HPMC를 첨가함으로써 초기 방출거동을 제어하는 등 조건을 달리함으로써 방출거동을 조절할 수 있었다. 수분흡수율과 무게변화를 조사한 결과, 방출 실험 4일부터 웨이퍼의 무게 감소가 현저하게 발생하였고, 방출이 완료된 후에는 무게가 약 40% 감소하였다. 이러한 약물전달 시스템은 압축성형방법에 의해 제조하므로 제조가 간단하고, 약물방출 속도를 정확하게 제어할 수 있으므로 이식을 위한 제형으로 제조시 유용하게 쓰일 것으로 예상되었다.

Biodegradable wafers were prepared with poly (L-lactide-co-glycolide) (50 : 50 mole ratio of lactide to glycolide, molecular weight:5000 g/mole) by direct compression method for the sustained release of nifedipine to investigate the possibility of the treatment of hypertension. PLGA wafers were prepared by altering initial drug/polymer loading ratio, wafer thickness, and hydroxypropyl methylcellulose (HPMC) content. These wafers showed new zero-order release patterns for 11 days, and various biphasic release patterns could be obtained by altering the composition of wafers such as addition of matrix binder as HPMC to the PLGA wafer to reduce release rate of initial phase. The onset of polymer mass loss only occured after 4 days and about 40% of mass loss was observed after 11 days nifedipine release. This system had advantages in terms of simplicity in design and obviousness of drug release rate and may be useful as an implantable dosage form.

키워드

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