Higashi K, Morisaki K, Hayashi S, Kitamura M, Fujimoto N, Kimura S, Ebisu S, Okada H
Research and Development Divn., Rohto Pharmaceutical Co., Osaka, Japan.
J Periodontal Res. 1990 Jan;25(1):1-5. doi: 10.1111/j.1600-0765.1990.tb01201.x.
PT-01, a controlled-release insert, was developed for topical chemotherapy in periodontal disease. It is a soluble insert that consists of fast-release and sustained-release parts containing ofloxacin (OFLX) as an antibacterial agent. In this study, the release profile of OFLX from PT-01 was investigated in vitro. Twelve adult volunteers were administered OFLX as PT-01 or as an aqueous solution into their periodontal pockets, OFLX concentrations in gingival crevicular fluid (GCF) were evaluated from the viewpoint of pharmacokinetics. The in vitro release profile of OFLX from PT-01 showed a biphasic pattern. The release rate of OFLX was relatively rapid in the early phase and slow thereafter. When OFLX aqueous solution was administered into periodontal pockets, the OFLX level in GCF rapidly decreased to be about 1/100 after 30 minutes. When PT-01 was inserted into the pockets, the OFLX level in GCF immediately reached a peak (about 12 mg/ml), and gradually decreased until the 3rd day, and maintained a constant level above 2 micrograms/ml, the effective minimum antibacterial concentration for periodontopathic microorganisms, from the 3rd to 7th day after insertion. No side-effects were observed in the volunteers who received the PT-01 insert. The above results suggest that PT-01 is a suitable pharmaceutical preparation for periodontal chemotherapy.
PT-01是一种控释植入剂，专为牙周疾病的局部化疗而研发。它是一种可溶性植入剂，由含有抗菌剂氧氟沙星（OFLX）的速释部分和缓释部分组成。在本研究中，对PT-01中OFLX的体外释放特性进行了研究。12名成年志愿者接受了PT-01形式或水溶液形式的OFLX并将其注入牙周袋，从药代动力学角度评估龈沟液（GCF）中的OFLX浓度。PT-01中OFLX的体外释放特性呈双相模式。OFLX的释放速率在早期相对较快，之后变慢。当将OFLX水溶液注入牙周袋时，30分钟后GCF中的OFLX水平迅速降至约1/100。当将PT-01植入袋中时，GCF中的OFLX水平立即达到峰值（约12毫克/毫升），并逐渐下降直至第3天，且从植入后的第3天到第7天维持在高于2微克/毫升的恒定水平，这是牙周病原微生物的有效最低抗菌浓度。接受PT-01植入剂的志愿者未观察到副作用。上述结果表明，PT-01是一种适用于牙周化疗的药物制剂。
