Coviello T, Dentini M, Rambone G, Desideri P, Carafa M, Murtas E, Riccieri F M, Alhaique F
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive. Università di Roma 'La Sapienza', 00185 Rome, Italy.
J Control Release. 1998 Oct 30;55(1):57-66. doi: 10.1016/s0168-3659(98)00028-5.
The formulation of a new controlled delivery system, based on a novel type of matrix obtained by the chemical reaction carried out in an aqueous medium on a mixed physical gel of gellan and scleroglucan, is described in this paper. The preparation yielded a new co-crosslinked polysaccharide (CCP) hydrogel, bearing carboxylic groups, that showed a sustained release behaviour that can be modulated by means of calcium ions. For the characterization of CCP, diffusion experiments through the swelled hydrogel were carried out in different environmental conditions and the release from tablets prepared with CCP and a model drug was evaluated. The addition of CaCl2 in the formulation of the dosage forms allowed a further marked reduction in delivery rate to be obtained; this effect is to be related to the free ionized carboxylic groups still present in the gellan moiety of CCP. The different behaviour of Ca+2 and Na+ ions is discussed.
本文描述了一种新型控释系统的配方,该系统基于一种新型基质,这种基质是通过在水介质中对结冷胶和硬葡聚糖的混合物理凝胶进行化学反应而获得的。制备过程产生了一种带有羧基的新型共交联多糖(CCP)水凝胶,它表现出可持续释放行为,且这种行为可通过钙离子进行调节。为了对CCP进行表征,在不同环境条件下进行了通过溶胀水凝胶的扩散实验,并评估了用CCP和一种模型药物制备的片剂的释放情况。在剂型配方中添加CaCl2可使释放速率进一步显著降低;这种效应与CCP的结冷胶部分中仍存在的游离离子化羧基有关。文中讨论了Ca+2和Na+离子的不同行为。