中国组织工程研究
中國組織工程研究
중국조직공정연구
Journal of Clinical Rehabilitative Tissue Engineering Research
2013年
29期
5351-5356
,共6页
生物材料%生物材料与药物控释%加替沙星-聚癸二酸酐缓释制剂%骨感染%加替沙星%生物相容性%生物降解%聚酸酐
生物材料%生物材料與藥物控釋%加替沙星-聚癸二痠酐緩釋製劑%骨感染%加替沙星%生物相容性%生物降解%聚痠酐
생물재료%생물재료여약물공석%가체사성-취계이산항완석제제%골감염%가체사성%생물상용성%생물강해%취산항
biomaterials%biomaterials and controlled drug release%gatifloxacin-poly sebacic anhydride sustained release preparations%bone infection%gatifloxacin%biocompatibility%biodegradation%poly anhydride
背景：全身大剂量应用抗生素治疗骨感染的不良反应较多，效果不是十分理想，因此探索一种以可降解材料为载体预防骨感染的方法具有很好的应用价值。目的：分析加替沙星-聚癸二酸酐局部缓释系统的体内释药特性。方法：在新西兰大耳白兔右侧膝关节制作3 mm×6 mm大小的骨窗，植入加替沙星-聚癸二酸酐缓释制剂，术后1，2，3，6，9，12，15，18，25，30 d取心脏血、骨组织及骨髓组织标本，以高效液相色谱法测定各组织内加替沙星浓度；扫描电镜观察加替沙星-聚癸二酸酐缓释制剂植入前后的结构变化。结果与结论：加替沙星-聚癸二酸酐缓释制剂植入后，骨髓组织内药物浓度逐渐降低，在第1天出现了一个较高的高峰，第3-15天药棒释放较平稳，15-30 d逐渐降低，但在30 d末时的药物浓度仍大于对金黄色葡萄球菌的最小抑菌浓度0.1 mg/L；骨组织内的药物浓度高峰出现于第3天，其余时间的浓度较平稳，并且均大于0.1 mg/L；在同一时间点，血标本中药物浓度小于骨髓组织和骨组织内药物浓度。加替沙星-聚癸二酸酐缓释制剂是表面溶蚀降解，降解残留物为小球状，其内部结构未发生变化，在药物持续释放过程中药棒未发生崩解和碎片化。表明加替沙星-聚癸二酸酐局部缓释制剂具有良好的载药及药物缓释能力。
揹景：全身大劑量應用抗生素治療骨感染的不良反應較多，效果不是十分理想，因此探索一種以可降解材料為載體預防骨感染的方法具有很好的應用價值。目的：分析加替沙星-聚癸二痠酐跼部緩釋繫統的體內釋藥特性。方法：在新西蘭大耳白兔右側膝關節製作3 mm×6 mm大小的骨窗，植入加替沙星-聚癸二痠酐緩釋製劑，術後1，2，3，6，9，12，15，18，25，30 d取心髒血、骨組織及骨髓組織標本，以高效液相色譜法測定各組織內加替沙星濃度；掃描電鏡觀察加替沙星-聚癸二痠酐緩釋製劑植入前後的結構變化。結果與結論：加替沙星-聚癸二痠酐緩釋製劑植入後，骨髓組織內藥物濃度逐漸降低，在第1天齣現瞭一箇較高的高峰，第3-15天藥棒釋放較平穩，15-30 d逐漸降低，但在30 d末時的藥物濃度仍大于對金黃色葡萄毬菌的最小抑菌濃度0.1 mg/L；骨組織內的藥物濃度高峰齣現于第3天，其餘時間的濃度較平穩，併且均大于0.1 mg/L；在同一時間點，血標本中藥物濃度小于骨髓組織和骨組織內藥物濃度。加替沙星-聚癸二痠酐緩釋製劑是錶麵溶蝕降解，降解殘留物為小毬狀，其內部結構未髮生變化，在藥物持續釋放過程中藥棒未髮生崩解和碎片化。錶明加替沙星-聚癸二痠酐跼部緩釋製劑具有良好的載藥及藥物緩釋能力。
배경：전신대제량응용항생소치료골감염적불량반응교다，효과불시십분이상，인차탐색일충이가강해재료위재체예방골감염적방법구유흔호적응용개치。목적：분석가체사성-취계이산항국부완석계통적체내석약특성。방법：재신서란대이백토우측슬관절제작3 mm×6 mm대소적골창，식입가체사성-취계이산항완석제제，술후1，2，3，6，9，12，15，18，25，30 d취심장혈、골조직급골수조직표본，이고효액상색보법측정각조직내가체사성농도；소묘전경관찰가체사성-취계이산항완석제제식입전후적결구변화。결과여결론：가체사성-취계이산항완석제제식입후，골수조직내약물농도축점강저，재제1천출현료일개교고적고봉，제3-15천약봉석방교평은，15-30 d축점강저，단재30 d말시적약물농도잉대우대금황색포도구균적최소억균농도0.1 mg/L；골조직내적약물농도고봉출현우제3천，기여시간적농도교평은，병차균대우0.1 mg/L；재동일시간점，혈표본중약물농도소우골수조직화골조직내약물농도。가체사성-취계이산항완석제제시표면용식강해，강해잔류물위소구상，기내부결구미발생변화，재약물지속석방과정중약봉미발생붕해화쇄편화。표명가체사성-취계이산항국부완석제제구유량호적재약급약물완석능력。
BACKGROUND:High-dose antibiotics for bone infection have many adverse reactions, and its outcomes are not perfect. Thus, to explore a degradable material as a vector to prevent bone infection is valuable. OBJECTIVE:To study drug release characteristics of gatifloxa-poly sebacic anhydride local control ed release system in vivo. METHODS:A 3 mm × 6 mm bone window was made at right knee joint of New Zealand rabbits. The gatifloxacin-poly sebacic anhydride sustained release preparation was implanted. Heart blood, bone tissue and myeloid tissue specimens were obtained at 1, 2, 3, 6, 9, 12, 15, 18, 25 and 30 days after surgery. High-performance liquid chromatography was utilized to determine gatifloxacin concentration. Scanning electron microscope was employed to observe the structural changes before and after implantation of gatifloxacin-poly sebacic anhydride sustained release preparation. RESULTS AND CONCLUSION:After implantation of gatifloxacin-poly sebacic anhydride sustained release preparation, drug concentration gradual y decreased in the myeloid tissue, peaked at 1 day, stabilized at 3-15 days, gradual y reduced at 15-30 days. However, the drug concentration was stil higher than the minimal inhibitory concentration 0.1 mg/L against Staphylococcus aureus at 30 days. The peak of drug concentration in the bone tissue occurred at 3 days, and stabilized at other days, which was higher than 0.1 mg/L. At the same time point, drug concentration in the blood specimen was lower than that in the myeloid tissue and bone tissue. The degradation of gatifloxacin-poly sebacic anhydride sustained release preparation was surface erosion, and the shape of the degradation residue is smal globular. The change of the internal structure of gatifloxacin-poly sebacic anhydride sustained release preparation was not found. In the drug release procedure, gatifloxacin-poly sebacic anhydride sustained release preparation did not show disintegration or fragmentation. These results indicated that <br> gatifloxacin-poly sebacic anhydride local sustained release preparation has good abilities of drug load and drug release.
