Laboratoire d'Ingénierie Ostéo-Articulaire et Dentaire, LIOAD, Faculté de Chirurgie Dentaire, INSERM, U 791, 1 Place A. Ricordeau, 44042, Nantes, France.
J Mater Sci Mater Med. 2010 Dec;21(12):3141-50. doi: 10.1007/s10856-010-4172-8. Epub 2010 Nov 3.
Calcium phosphate substitutes drug delivery systems are well known substances used in minor bone void-filling to release their therapeutic agent in situ. Few studies associating anaesthetics and analgesics have been performed to date. The aim of this work was to study the association of the analgesic, morphine, and the local anaesthetic, lidocaine, with a calcium deficient apatite matrix. Three types of biomaterials i.e. powders, granules and blocks, were prepared by isostatic compression, wet granulation and a combination of the two, evaluated and compared. The chemical structure of the associated therapeutic agent was studied and the characteristics of the drug delivery systems were appraised in terms of drug release. The integrity of the lidocaine hydrochloride structure, as determined by RMN (1)H, was confirmed regardless of the formulation technique used (isostatic compression or wet granulation). However, analyses of morphine hydrochloride by RMN (1)H revealed slight structural modifications. The association and formulation techniques that were used made it possible to obtain an in vitro release time varying from 1 to 4 days for lidocaine hydrochloride and from 1 to 3 days for morphine hydrochloride.
钙磷酸盐替代药物输送系统是众所周知的用于小骨空隙填充的物质，可就地释放其治疗剂。迄今为止，很少有研究将麻醉剂和镇痛药与之相关联。本工作的目的是研究镇痛剂吗啡和局部麻醉剂利多卡因与缺钙磷灰石基质的关联。通过等静压压缩、湿法制粒和两者的组合制备了三种类型的生物材料，即粉末、颗粒和块状物，对其进行了评估和比较。研究了相关治疗剂的化学结构，并根据药物释放评价了药物输送系统的特性。通过（1）H RMN 确定了盐酸利多卡因结构的完整性，无论使用何种制剂技术（等静压压缩或湿法制粒）都是如此。然而，通过（1）H RMN 分析盐酸吗啡显示出轻微的结构修饰。所使用的联合和配方技术使得可以获得盐酸利多卡因的体外释放时间从 1 天到 4 天不等，盐酸吗啡的释放时间从 1 天到 3 天不等。
