Soskolne W A, Chajek T, Flashner M, Landau I, Stabholtz A, Kolatch B, Lerner E I
Department of Periodontology, Hebrew University-Hadassah Faculty of Dental Medicine, Jerusalem, Israel.
J Clin Periodontol. 1998 Dec;25(12):1017-21. doi: 10.1111/j.1600-051x.1998.tb02407.x.
The release profile of chlorhexidine from the PerioChip (Chip), a biodegradable local delivery system that contains 2.5 mg of chlorhexidine gluconate (CHX) in a cross-linked hydrolyzed gelatin matrix, into the gingival crevice, was evaluated in an in vivo, open label, single-center, 10-day pharmacokinetic study conducted on 19 volunteers with chronic adult periodontitis. Each volunteer had a single chip inserted into each of 4 selected pockets, with probing pocket depths of between 5-8 mm, at time 0. Gingival crevicular fluid (GCF) samples were collected using filter paper strips prior to Chip placement and at 2 h, 4 h, 24 h and 2, 3, 4, 5, 6, 8, and 9 days post-Chip placement. The GCF volume was measured using a calibrated Periotron 6000. Blood samples were collected at times 0, 1, 4, 8, 12 h and 5 days post-dosing. Urine was collected as a total 24-h specimen immediately post-dosing and 2 single samples at time 0, prior to dosing, and 5 days. The CHX was eluted from the paper strips and the CHX levels in GCF, blood and urine quantified using HPLC. The results indicate an initial peak concentration of CHX in the GCF at 2 h post-Chip insertion (2007 microg/ml) with slightly lower concentrations of between 1300-1900 microg/ml being maintained over the next 96 h. The CHX concentration then progressively decreased until study conclusion with significant CHX concentrations (mean=57 microg/ml) still being detectable at study termination. CHX was not detectable in any of the plasma or urine samples at any time point during the study. These results indicate that the PerioChip can maintain clinically effective levels of CHX in the GCF of periodontal pockets for over 1 week with no detectable systemic absorption.
在一项针对19名慢性成人牙周炎志愿者进行的为期10天的体内开放标签单中心药代动力学研究中，评估了洗必泰从PerioChip（芯片）（一种可生物降解的局部给药系统，在交联水解明胶基质中含有2.5毫克葡萄糖酸洗必泰（CHX））释放到龈沟中的情况。在时间0时，将每片芯片插入每名志愿者4个选定的牙周袋中，这些牙周袋的探诊深度在5 - 8毫米之间。在放置芯片前以及放置芯片后2小时、4小时、24小时以及2、3、4、5、6、8和9天，使用滤纸条收集龈沟液（GCF）样本。使用校准的Periotron 6000测量GCF体积。在给药后0、1、4、8、12小时以及5天采集血样。给药后立即收集24小时总尿液样本，并在给药前0时和5天收集2个单次样本。将CHX从纸条上洗脱下来，并使用高效液相色谱法对GCF、血液和尿液中的CHX水平进行定量。结果表明，在插入芯片后2小时，GCF中CHX出现初始峰值浓度（2007微克/毫升），在接下来的96小时内维持在1300 - 1900微克/毫升之间的稍低浓度。然后CHX浓度逐渐降低，直到研究结束，在研究终止时仍可检测到显著的CHX浓度（平均 = 57微克/毫升）。在研究期间的任何时间点，血浆或尿液样本中均未检测到CHX。这些结果表明，PerioChip可以在牙周袋的GCF中维持临床有效水平的CHX超过1周，且未检测到全身吸收。
