Siekmann B, Westesen K
Institute of Pharmaceutical Technology, Technical University of Braunschweig, Federal Republic of Germany.
Pharm Res. 1995 Feb;12(2):201-8. doi: 10.1023/a:1016270724413.
The present study describes a novel pharmaceutical formulation of coenzyme Q10, viz. submicron-sized dispersions of the substance prepared by emulsification of molten coenzyme Q10 in an aqueous phase. Photon correlation spectroscopy reveals mean diameters of 60 to 300 nm depending on process parameters. Coenzyme Q10 nanoparticles remain stable on storage for more than 30 months. Lipophilic drugs can be incorporated into the nanoparticles demonstrating their potential use as a drug carrier system. Transmission electron micrographs of freeze-fractured replica show spherical particles with an amorphous core. Cryo-electron microscopy reveals the coexistence of small unilamellar vesicles in phospholipid stabilized dispersions. Thermoanalysis and X-ray studies indicate that the dispersed and emulsified coenzyme Q10 does not recrystallize even at 4 degrees C over 30 months. These agree with 1H NMR data which demonstrate that coenzyme Q10 molecules have a high mobility when formulated as nanoparticles and that colloidally dispersed coenzyme Q10 remains in the state of a supercooled melt. Despite the high melting point of the bulk material, coenzyme Q10 dispersions represent no suspensions but O/W emulsions according to the IUPAC definition (1).
本研究描述了辅酶Q10的一种新型药物制剂，即通过将熔融的辅酶Q10在水相中乳化制备的亚微米级分散体。光子相关光谱显示，根据工艺参数，平均直径为60至300纳米。辅酶Q10纳米颗粒在储存30多个月后仍保持稳定。亲脂性药物可掺入纳米颗粒中，表明其作为药物载体系统的潜在用途。冷冻断裂复制品的透射电子显微镜照片显示具有无定形核心的球形颗粒。冷冻电子显微镜揭示了在磷脂稳定的分散体中存在小单层囊泡。热分析和X射线研究表明，分散和乳化的辅酶Q10即使在4℃下30个月也不会重结晶。这些与1H NMR数据一致，该数据表明当配制成纳米颗粒时辅酶Q10分子具有高迁移率，并且胶体分散的辅酶Q10保持过冷熔体状态。尽管块状材料熔点高，但根据IUPAC定义(1)，辅酶Q10分散体不是悬浮液而是O/W乳液。
