Krögel I, Bodmeier R
College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169, Berlin, Germany.
J Control Release. 1999 Aug 27;61(1-2):43-50. doi: 10.1016/s0168-3659(99)00096-6.
A multifunctional drug delivery system based on hydroxypropyl methylcellulose (HPMC)-matrices (tablets) placed within an impermeable polymeric cylinder (open at both ends) was developed. Depending on the configuration of the device, extended release, floating or pulsatile drug delivery systems could be obtained. The release behaviour of the different devices was investigated as a function of HPMC viscosity grade, HPMC content, type of drug (chlorpheniramine maleate or ibuprofen), matrix weight, position of the matrix within the polymeric cylinder, addition of various fillers (lactose, dibasic calcium phosphate or microcrystalline cellulose) and agitation rate of the release medium. The drug release increased with a reduced HPMC viscosity grade, higher aqueous drug solubility, decreased HPMC content and increased surface area of the matrix. The release was fairly independent of the agitation rate, the position of the tablet within the polymeric cylinder and the length of the cylinder. With the pulsatile device, the lag time prior to the drug release could be controlled through the erosion rate of the matrix (matrix weight and composition).
开发了一种基于羟丙基甲基纤维素(HPMC)基质(片剂)的多功能药物递送系统,该基质置于两端开口的不可渗透聚合物圆筒内。根据装置的结构,可以获得缓释、漂浮或脉冲式药物递送系统。研究了不同装置的释放行为与HPMC粘度等级、HPMC含量、药物类型(马来酸氯苯那敏或布洛芬)、基质重量、基质在聚合物圆筒内的位置、各种填充剂(乳糖、磷酸氢钙或微晶纤维素)的添加以及释放介质搅拌速率的关系。药物释放随着HPMC粘度等级降低、药物在水中溶解度增加、HPMC含量降低以及基质表面积增加而增加。释放相当独立于搅拌速率、片剂在聚合物圆筒内的位置以及圆筒的长度。对于脉冲式装置,药物释放前的滞后时间可以通过基质的侵蚀速率(基质重量和组成)来控制。