[Development of minocycline containing polycaprolactone film as a local drug delivery].

Taehan Ch'ikkwa Uisa Hyophoe chi Pub Date : 1990-03-01
K D Kyun, K S Yun, J S Young, C C Pyoung, S S Heui
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Abstract

Local drug delivery by using biocompatible polymers has been developed in the treatment of periodontitis for many years. The purpose of this study was to examine the release kinetics of minocycline from monolithic film prepared from polycaprolactone and polyethylene glycol and to examine the antimicrobial activity in vitro. Polycaprolactone (Mwt 60,000), polyethylene glycol and minocyline was dissolved by chloroform, which was vigorously stirred for 24 hours and it was dried in vacuum chamber. The thickness of cast films containing 20%, 30% and 40% minocycline was 200 +/- 10 microns. Release rate of minocycline from the film was measured by means of a UV spectrophotometer. In vitro releasing test, each film showed a large burst effect within first two and three hours and a steady state release kinetic at the rate of 4-8 micrograms/cm/hour for 7 days. In antimicrobial test, each sample (one fourth inch in diameter) sunk in the broth that had been innoculated with periodontopathic bacteria showed growth inhibitory activity after 48 hr anaerobic incubation. In cytotoxicity test, there was no significant cytotoxic effect in casting film to human gingival fibroblast. This study showed that, by embedding minocycline in polycaprolactone, it is feasible to obtain substained release of the drug within the periodontal pocket for seven days and should be useful tool for elimination of pathogenic microflora from periodontal pocket or reducing inflammation in periodontal disease.

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[含聚己内酯膜的米诺环素局部给药的发展]。
利用生物相容性聚合物局部给药治疗牙周炎已发展多年。本研究考察了米诺环素从聚己内酯和聚乙二醇制备的单片膜中的释放动力学,并考察了其体外抗菌活性。聚己内酯(Mwt 60000)、聚乙二醇、二甲胺四环素用氯仿溶解,强力搅拌24h,真空室干燥。含20%、30%和40%米诺环素的铸膜厚度为200 +/- 10 μ m。用紫外分光光度计测定了二甲胺四环素的释放率。在体外释放试验中,每片在前2、3小时内均表现出较大的爆裂效应,并以4 ~ 8微克/厘米/小时的速度稳定释放,持续7天。在抗菌试验中,每个样品(直径四分之一英寸)浸泡在接种了牙周病菌的肉汤中,在厌氧培养48小时后显示出生长抑制活性。在细胞毒试验中,铸膜对人牙龈成纤维细胞无明显的细胞毒作用。本研究表明,将米诺环素包埋在聚己内酯中,可以使药物在牙周袋内持续释放7天,是消除牙周袋内病原菌群或减轻牙周病炎症的有效工具。
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