| 摘要: |
| 目的考察注射型植入剂体外释放方法的可行性。方法建立模型药物诺氟沙星的反相高效液相色谱测定方法,以直接注射法、单向圆筒法、透析袋法及自制圆筒法考察注射型植入剂的体外释药特性,并与大鼠皮下注射的释放结果作比较。结果注射型植入剂体内释药速率明显快于体外,体内持续释药阶段(1~20 d)接近零级释药(r=0.993 5),而体外持续释药阶段以15 d为界分为缓慢释药、快速释药两个阶段。4种体外释放方法中,自制圆筒法的突释阶段较为接近体内释药。结论注射型植入剂的4种体外释放方法均有一定的缺陷,不能完全模拟药物在体内的释放情况,注射型植入剂的体外释放方法有待于进一步探索。 |
| 关键词: 注射型植入剂 体内研究 体外研究 释放模型 |
| DOI：10.3724/SP.J.1008.2010.0374 |
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| 基金项目: |
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| Investigation of in vitro release model of injectable implants |
| LIU Qing-feng, LU Ying, ZHOU Gui-chen, XUAN Ji-ming, XIE Shao-bo,,ZHONG Yan-qiang* |
| (Department of Pharmaceutical Science, School of Pharmacy, Second Military Medical University,Shanghai 200433, China) |
| Abstract: |
| ObjectiveTo investigate the feasibility of in vitro release models of injectable implants. MethodsAn RP-HPLC method was established for determination of norfloxacin (NF). The in vitro release profiles of injectable implants in four release models, including direct injection model, one-way cylinder, dialysis tube and home-made cylinder, were studied and compared with the in vivo release profiles. ResultsThe in vivo release of NF from injectable implants was much faster than the in vitro release of NF. The in vivo release was close to the zero-order release kinetics in the sustained release phase (1-20 d, r=0.993 5), while the in vitro release could be divided into slow phase and fast phase with 15 d as the turning point. Of the four in vitro release models, home-made cylinder showed the closest initial release to the initial release of NF in vivo. ConclusionAll the above four release models have limitations; they can not well reflect the in vivo release profiles of injectable implants; and further studies are needed for the in vitro release model of injectable implants. |
| Key words: injectable implant in vivo in vitro release model |
