Nakagawa Tomoya, Kondo Shin-ichi, Sasai Yasushi, Kuzuya Masayuki
Laboratory of Pharmaceutical Physical Chemistry, Gifu Pharmaceutical University, Japan.
Chem Pharm Bull (Tokyo). 2006 Apr;54(4):514-8. doi: 10.1248/cpb.54.514.
A novel intragastric floating drug delivery system (FDDS) has been prepared by pulsed plasma-irradiation on the double-compressed tablet of 5-Fluorouracil (5-FU) as a core material with outer layer composed of a 68/17/15 weight ratio of Povidone (PVP), Eudragit RL (E-RL) and NaHCO3. The plasma heat flux caused the thermal decomposition of NaHCO3 to generate carbon dioxide and the resultant gases were trapped in bulk phase of outer layer, so that the tablets turned to have a lower density than the gastric contents and remained buoyant in simulated gastric fluid for a prolonged period of time. In addition, the release of 5-FU from the tablet is sustained by occurrence of plasma-induced crosslink reaction on the outer layer of tablet and the release rate of 5-FU can be well controlled by plasma operational conditions.
一种新型胃内漂浮给药系统(FDDS)是通过对以5-氟尿嘧啶(5-FU)为核心材料的双层压制片进行脉冲等离子体辐照制备而成,其外层由重量比为68/17/15的聚维酮(PVP)、丙烯酸树脂RL(E-RL)和碳酸氢钠组成。等离子体热通量导致碳酸氢钠热分解产生二氧化碳,生成的气体被困在外层的主体相中,从而使片剂的密度低于胃液,在模拟胃液中长时间保持漂浮状态。此外,片剂中5-FU的释放通过片剂外层发生的等离子体诱导交联反应得以持续,并且5-FU的释放速率可以通过等离子体操作条件得到很好的控制。