甲磺酸罗哌卡因缓释微球的制备及加速释放度试验研究

发布时间：2018-06-11 13:31

本文选题：甲磺酸罗哌卡因 + 微球　；参考：《中国新药杂志》2015年10期

【摘要】：目的:制备甲磺酸罗哌卡因微球,建立甲磺酸罗哌卡因微球的加速释放度试验方法。方法:采用S/O/W法制备甲磺酸罗哌卡因微球,通过考察振摇频率、温度和释放介质p H对甲磺酸罗哌卡因微球释药速度的影响,确定体外加速释放的条件,通过评价加速与长期释放度的相关性,建立甲磺酸罗哌卡因微球的体外加速释放方法。结果:微球外观圆整,表面光滑,无黏连。F1批及F2批的平均粒径分别为(12.06±0.45)和(15.11±0.79)μm,载药量分别为(17.86±0.38)%和(23.62±0.15)%;包封率分别为(50.46±0.63)%和(66.74±0.31)%。振摇频率和释放介质的p H对微球的释药速率影响不大,温度的提高可显著加快药物的释放。结果表明,以p H 7.4磷酸盐缓冲液为释放介质,在100 r·min-1和程序升温条件下,加速释放度与长期释放度数据之间具有良好的非线性相关(r=0.988 0)。结论:加速释放度试验可用于快速评价甲磺酸罗哌卡因微球的释药特性。
[Abstract]:Objective: to prepare the microspheres of Ropivacaine Mesylate and establish the test method for the accelerated release of Ropivacaine Mesylate microspheres. Methods: Ropivacaine Mesylate microspheres were prepared by S/O/W method. The effects of the vibration frequency, temperature and the release medium P H on the release rate of ropivacaine microspheres were determined, and the conditions for the accelerated release in vitro were determined. The accelerated release method of Ropivacaine Mesylate microspheres was established. Results: the surface of microspheres was round and smooth, the average particle size of.F1 batch and F2 batch was (12.06 + 0.45) and (15.11 + 0.79) mu m respectively, the drug loading was (17.86 + 0.38)% and (23.62 + 0.15)% respectively, and the encapsulation efficiency was 50.4. 6 + 0.63% and (66.74 + 0.31)%. The vibration frequency and P H of the release medium have little effect on the release rate of the microspheres. The increase of temperature can significantly accelerate the release of the drug. The results show that the P H 7.4 phosphate buffer solution is the release medium, and the accelerated release and the long-term release data are good between the 100 R / min-1 and the programmed temperature. Nonlinear correlation (r=0.988 0). Conclusion: the accelerated release test can be used to rapidly evaluate the release characteristics of Ropivacaine Mesylate.
【作者单位】：湖北科技学院药学院;军事医学科学院毒物药物研究所;
【基金】：国家“重大新药创制”科技重大专项(2012ZX09301003-001-009)
【分类号】：R943

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