Larsen Susan Weng, Østergaard Jesper, Friberg-Johansen Henrik, Jessen Marit N B, Larsen Claus
Department of Pharmaceutics and Analytical Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Eur J Pharm Sci. 2006 Dec;29(5):348-54. doi: 10.1016/j.ejps.2006.07.002. Epub 2006 Jul 14.
In vitro drug release rates from oil depot formulations intended for intra-articular injection have been investigated by using the rotating dialysis cell. The rate of drug appearance in the acceptor phase after instillation of sesame oil solutions of naproxen and lidocaine into the small aqueous donor compartment applied to first-order kinetics. In the present three-compartment model oil-aqueous phase distribution equilibrium was maintained at all times in the donor phase and thus drug efflux from the donor compartment was dictated by the distribution coefficient. A mathematical description of the rate of drug release into the acceptor phase and the interdependence of the observed apparent first-order rate constants and the drug oil-water distribution coefficients is provided. The in vitro model may constitute a valuable tool in formulation design and development allowing comparison of drug release rates originating from alteration of the oil vehicle composition, the drug compound or the composition of the release media to be performed.
通过使用旋转透析池，对用于关节内注射的油库制剂的体外药物释放速率进行了研究。将萘普生和利多卡因的芝麻油溶液滴入小型水相供体隔室后，受体相中药物出现的速率符合一级动力学。在当前的三室模型中，供体相中始终保持油-水相分配平衡，因此供体隔室中的药物流出由分配系数决定。本文提供了药物释放到受体相的速率以及观察到的表观一级速率常数与药物油水分配系数之间相互关系的数学描述。该体外模型可能是制剂设计和开发中的一个有价值的工具，可用于比较因油载体组成、药物化合物或释放介质组成改变而产生的药物释放速率。
