Beijing Institute of Pharmacology and Toxicology , Beijing , P.R. China .
Drug Deliv. 2014 Feb;21(1):1-7. doi: 10.3109/10717544.2013.838718. Epub 2013 Oct 9.
An economical, convenient portable drug delivery system combining osmotic pump with subcutaneous infusion was developed, which was composed of three primary components: water chamber, osmotic pump chamber and support base. Ceftriaxone sodium (CRO) was selected as the model drug and osmotic pump tablets were prepared. The influence of osmotic agents on drug release profiles was evaluated. As the adjustment made by the osmotic agents was limited, the compositions of semipermeable membrane were investigated to determine significant associations of factors based on orthogonal design. The in vitro release profiles of the optimum formulation achieved to the predetermined value (15 ± 3 min for the initial release time T(i) and 5.75 ± 0.25 h for the extent release time T(e)). The pharmacokinetic profiles of this drug delivery system were evaluated in Beagle dogs. In vivo results demonstrated that the osmotic pump subcutaneous infusion administration was equivalent to intravenous injection administration in terms of bioavailability. Moreover, constant drug plasma levels with minimized fluctuations could be achieved with this osmotic pump subcutaneous infusion system, compared with intravenous injection.
研制了一种经济、方便的可携式药物输送系统，将渗透泵与皮下输注相结合，该系统由三个主要部分组成：水腔、渗透泵腔和支撑底座。选择头孢曲松钠（CRO）作为模型药物并制备渗透泵片。评估了渗透剂对药物释放曲线的影响。由于渗透剂的调整有限，因此研究了半透膜的组成，根据正交设计确定了因素的显著相关性。最佳配方的体外释放曲线达到预定值（初始释放时间 T(i)为 15 ± 3 分钟，释放时间 T(e)为 5.75 ± 0.25 小时）。在比格犬中评价了该药物输送系统的药代动力学特征。体内结果表明，渗透泵皮下输注给药在生物利用度方面相当于静脉注射给药。此外，与静脉注射相比，这种渗透泵皮下输注系统可实现药物血浆水平的稳定且波动最小。
