含去甲睾酮的聚乳酸/乙醇酸微球的制备及体外、体内评价。

Z Zhou, M Zhou, S Wang, F Lin, W Shan
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引用次数: 0

摘要

制备了含20%去甲睾酮(NET)的聚乳酸/乙醇酸(PLGA)微球,并对制备方法进行了优化。微球在27.5% wt%乙醇溶液中缓释96小时以上。微球的体内性能表明,单次肌肉注射80 mg微球可以显著延长大鼠的发情抑制时间,最长可达45天。此外,对微球稳定性的研究表明,微球储存1年后,其NET含量和体外释放率均无明显变化。
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Preparation and evaluation in vitro and vivo of copoly (lactic/glycolic) acid microspheres containing norethisterone.

Poly (lactic/glycolic) acid (PLGA) microspheres containing 20% norethisterone (NET) were prepared and the preparation methodology was optimised. The microspheres showed a slow and steady release pattern up to more than 96 hours in 27.5 wt% ethanol solution. In vivo performance of the microspheres indicated that a single intramuscular injection of 80 mg of microspheres could significantly prolong the duration of estrus suppression up to 45 days in rats. In addition, the studies on the stability of microspheres showed that there was no significant change both in the NET content of microspheres and the NET release rate in vitro after storage for one year.

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