BK21 Project Team, College of Pharmacy, Chosun University, Dong-gu, Gwangju 501-759, South Korea.
Int J Pharm. 2010 Jan 4;383(1-2):147-53. doi: 10.1016/j.ijpharm.2009.09.031. Epub 2009 Sep 23.
This study aimed to develop a stable solid dispersion of Coenzyme Q(10) (CoQ(10)) with high aqueous solubility and dissolution rate. Among various carriers screened, poloxamer 407 was most effective to form a superior solid dispersion of CoQ(10) having significantly enhanced solubility. Particularly, solid dispersion of CoQ(10) with poloxamer 407 in the weight ratio of 1:5 prepared by melting method enhanced the solubility of CoQ(10) to the greatest extent. However, it exhibited poor stability and hence Aerosil 200 (colloidal silicon dioxide) was incorporated into the solid dispersion as an adsorbent to inhibit the recrystallization process. The solid dispersion of CoQ(10), poloxamer 407 and Aerosil 200 in the weight ratio of 1:5:6 exhibited improved stability with no significant change in solubility during the 1-month stability test. Moreover, the solid dispersion formulation containing Aerosil 200 significantly enhanced the extent of drug release (approx. 75% release) as well as the dissolution rate of CoQ(10). In conclusion, the present study has developed the stable solid dispersion formulation of CoQ(10) with poloxamer 407 and Aerosil 200 for the enhanced solubility and dissolution of CoQ(10), which could also offer some additional advantages including ease of preparation, good flowability and cost-effectiveness.
本研究旨在开发具有高水溶性和高溶解速率的稳定辅酶 Q(10)（CoQ(10)）固体分散体。在筛选的各种载体中，聚氧乙烯 407 对形成具有显著增强的溶解度的 CoQ(10)的优越固体分散体最有效。特别是通过熔融法制备的 CoQ(10)与聚氧乙烯 407 的重量比为 1:5 的 CoQ(10)固体分散体最大限度地提高了 CoQ(10)的溶解度。然而，它表现出较差的稳定性，因此将胶体二氧化硅（Aerosil 200）掺入固体分散体中作为吸附剂以抑制重结晶过程。CoQ(10)、聚氧乙烯 407 和 Aerosil 200 的重量比为 1:5:6 的固体分散体在 1 个月的稳定性测试中表现出改善的稳定性，而溶解度没有显著变化。此外，含有 Aerosil 200 的固体分散体配方显著提高了药物释放程度（约 75%的释放）和 CoQ(10)的溶解速率。总之，本研究开发了具有聚氧乙烯 407 和 Aerosil 200 的稳定 CoQ(10)固体分散体配方，以提高 CoQ(10)的溶解度和溶解速率，这还可能提供一些额外的优势，包括易于制备、良好的流动性和成本效益。
