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论文类型：期刊论文

发表时间：2017-04-01

发表刊物：AAPS PHARMSCITECH

收录刊物：SCIE、PubMed、Scopus

卷号：18

期号：3

页面范围：738-748

ISSN号：1530-9932

关键字：Parkinson's disease; pharmacokinetics; pramipexole; prolonged-release; transdermal patch

摘要：The current study aimed to develop a prolonged-release pramipexole (PPX) transdermal patch for the treatment of Parkinson's disease. Permeation parameters of PPX were investigated using human cadaver skin. Pramipexole patches were prepared using DURO-TAK (R) pressure-sensitive-adhesive (PSA) and evaluated for drug stability, drug loading, in vitro drug release, and in vitro permeation through mouse skin. The results indicated that blends of DURO-TAK (R) 87-2852 and DURO-TAK (R) 87-2510 were suitable for creating a prolonged-release PPX patch due to their advantages in drug release, drug loading, and stability. The final formulation consisted of 87-2852/87-2510 (70: 30), 10% PG, and 15% PPX and showed a cumulative permeation amount of 1497.19 +/- 102.90 mu g/cm(2) with a continuous flux over 6.0 mu g/(cm(2).h) across human cadaver skin for 7 days. In vivo studies in rats indicated that PPX patch produced a significantly longer (p<0.001) half-life (t(1/2), 75.16 +/- 17.37 h) and mean residence time (MRT, 135.89 +/- 24.12 h) relative to oral tablets (Sifrol (R)) and had a relative bioavailability of 51.64 +/- 21.32%. Therefore, this study demonstrated the feasibility of developing a prolonged-release PPX patch, which proposed the potential to serve as an alternate to conventional oral tablets and may therefore improve patient compliance.