骨髓炎治疗用缓释制剂的制备及体外抑菌活性研究

骨髓炎的定点缓释给药治疗是重要的生物医学问题,关键是要制备高效的缓释药棒。我们采用热熔法,以聚(二聚酸(十四烷二酸)共聚物P(DA-TA),WDA:WTA=50:50]为药物缓释材料,硫酸庆大霉素为模型药物,制备了硫酸庆大霉素-聚酸酐缓释药棒,以期最终用于骨髓炎的定点缓释给药治疗。初步的制剂稳定性研究表明,在室温干燥条件下,该缓释药棒具有良好的制剂稳定性。体外释药结果表明,37℃时,该缓释药棒在蒸馏水中、0．9％生理盐水中和0．1 mol／L pH7．4 PBS中具有明显缓释作用,其体外释药动力学均符合一级动力学方程和Peppas方程。抑菌活性实验表明,该缓释药棒对骨髓炎常见致病菌:金黄色葡萄球菌及大肠杆菌有长达60 d的抑制作用。该类硫酸庆大霉素-聚酸酐缓释药棒具有良好的制剂稳定性和长达60 d的抑菌活性,可望用于骨髓炎治疗领域。

Preparation of Gentamicin Sulfate-polyanhydride Sustained-releas Beads and In Vitro Bacteriostatic Activity Studies

Drug slow release in osteomyelitis treatment is an important biomedical problem, to prepare the high effect drug sustained-release bead is the sticking point. A sustained-release bead system consisting of gentamicin sulfate in biodegradable poly(dimer acid-tetradecandioic acid) copolymer P(DA-TA), WDA: WTA= 50: 50] is prepared by melt casting which may be useful in osteomyelitis treatment. The stability at room temperature and the in vitro release profile in distilling water, in 0.9% saline buffer and in 0.1 mol/LpH7.4 PBS at 37 degrees C of the bead are determined, the drug release behavior in vitro follows the first order release kinetics and Peppas release kinetics equation. In vitro bacteriostatic activity studies demonstrated that the beads possessed desired bacteriostatic activity and lasted for 50 days for Staphylococcus aureus and Escherichia coli, which are common bacteria for infections in bone. All the above suggest that the biodegradable sustained-release beads may be a new treatment device for osteomyelitis treatment.