Coenzyme Q <sub> 10 </ Sub> Liposome Injections

The validated HPLC analytical method for Coenzyme Q₁₀ liposome was developed. The solubilities of Coenzyme Q₁₀ liposome in water, ethanol, methanol, propylene glycol and apparent partition coefficients in n-octyl alcohol: water was determined at ambient temperature by HPLC. The HPLC method for the content of Coenzyme Q₁₀ in liposomes was established. The entrapment efficiency of Coenzyme Q₁₀ liposome was determinated by filtrate-HPLC method.The Coenzyme Q₁₀ liposome was prepared by ethanol injection- filtrate method. The single factor investigation and the orthogonal design was adopted to obtain the optimized prescription, the index were entrapment efficiency and stability.The physicochemical properties of Coenzyme Q₁₀ liposome were studied. The CoenzymeQ₁₀ liposome was spheroidal and uniform, the number diameter is 155±22 nm, the volume diameter is 165±24 nm, the surface area diameter was 162±23 nm, the Zeta potential was—31.2 mV, pH value is 7.02±0.30, the entrapment efficiency was 99.5±0.42%.The stability of Coenzyme Q₁₀ liposome was reviewed with the index of appearance, drug content, POV, pH value and entrapment efficiency. The results of stability tests indicated that the Coenzyme Q₁₀ liposome should be preserved from light and stored at low temperature.The security investigation indicated that the CoenzymeQ₁₀ liposome injection is non-irritant, pyrogen-free and non- hematolytic, the preparation met the regulations of the IV administration.The HPLC method of CoenzymeQ₁₀ liposome in blood plasma and tissues was established. After IV administrated Coenzyme Q₁₀ solutions and liposomes to mice, respectively, the drug concentrations in different tissues were monitored by HPLC. The pharmacokinetic processes in mice for the two preparations were both accorded with two compartmental models. Compare with Coenzyme Q₁₀ solutions, the liposome had longer half-life and higher bioavailability. The levels of Coenzyme Q₁₀ liposome in heart, spleen, lung were slightly higher than that of Injection group.