D'Cruz Osmond J, Uckun Fatih M
Drug Discovery Program, Parker Hughes Institute, St Paul, MN 55113, USA.
AAPS PharmSciTech. 2006 Sep 1;7(3):73. doi: 10.1208/pt070373.
The objective of this study was to evaluate the long-term stability of the antiretroviral spermicide WHI-07 (5-bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-bromophenyl)-methoxyalaninyl phosphate) in a polymer-based microemulsion. The recovery and stability of WHI-07 in gel-microemulsion was examined by a validated high-performance liquid chromatography (HPLC) method. The stability was examined over a period of 24 weeks at 3 controlled temperatures (4 degrees C, 25 degrees C, and 40 degrees C). The recovery of the prodrug from 0.5% to 2.0% WHI-07-loaded gel-microemulsion was 99.8%. HPLC analysis revealed that a 2% WHI-07-loaded gel-microemulsion stored at room temperature and cold temperatures for 24 weeks retained >90% of the prodrug, whereas those stored at 40 degrees C maintained 90% of initial WHI-07 for at least 10 weeks. The observed stability of WHI-07 in gel-microemulsion is of great importance for its widespread utility in various climatological conditions.
本研究的目的是评估抗逆转录病毒杀精剂WHI-07（5-溴-6-甲氧基-5,6-二氢-3'-叠氮胸苷-5'-(对溴苯基)-甲氧基丙氨酰磷酸酯）在基于聚合物的微乳液中的长期稳定性。采用经过验证的高效液相色谱（HPLC）法检测了WHI-07在凝胶微乳液中的回收率和稳定性。在3个受控温度（4℃、25℃和40℃）下，对其稳定性进行了为期24周的检测。从含0.5%至2.0% WHI-07的凝胶微乳液中回收前药的回收率为99.8%。HPLC分析显示，含2% WHI-07的凝胶微乳液在室温和低温下储存24周后，前药保留率>90%，而在40℃下储存的样品在至少10周内保持了初始WHI-07的90%。观察到的WHI-07在凝胶微乳液中的稳定性对其在各种气候条件下的广泛应用具有重要意义。
