辅酶Q10乳剂的处方工艺改进与质量评价

The improvement of formulation process and quality evaluation of coenzyme Q10 emulsion

目的对处方工艺改进的辅酶Q10乳剂进行质量评价,并建立其含量测定方法。方法制备高油量辅酶Q10乳剂,利用HPLC建立其含量测定与有关分析方法,并进行理化性质表征,测定包封率,考察灭菌、冻融和稀释稳定性,进行强光降解试验以及影响因素、加速和长期试验。结果辅酶Q10乳剂粒径、Zeta电位、pH值、含量和包封率分别为(239.5±0.8)nm、(−32.28±2.04)mV、(5.86±0.02)、(100.59±1.24)%和(98.5±1.1)%,灭菌、冻融和稀释稳定性均良好。乳剂光解速率与稀释倍数呈正比,与载药量呈反比。辅酶Q10乳剂需避光制备、低温储存;(40±2)℃避光放置10天,pH值下降0.61;加速和长期试验稳定性良好。结论高油量辅酶Q10乳剂符合静脉注射液的质量要求,稳定性良好。

Objective To evaluate the quality of coenzyme Q10 emulsion with improved formulation and technology and establish an assay method.Methods Coenzyme Q10 emulsion with a high oil concentration was prepared and analyzed by HPLC.The physical and chemical properties of the emulsion were characterized,and the entrapment efficiency was determined.The stability of sterilization,freeze-thaw and dilution was investigated.The photodegradation test as well as the influencing factors,acceleration and long-term stability tests were carried out.Results The particle size,Zeta potential,pH value,content and entrapment efficiency of coenzyme Q10 emulsion were(239.5±0.8)nm、(−32.28±2.04)mV、(5.86±0.02)、(100.59±1.24)%and(98.5±1.1)%,respectively.The stability of sterilization,freeze-thaw and dilution was good.The photolysis rate was directly proportional to the dilution ratio and inversely proportional to the drug loading.Coenzyme Q10 emulsion should be prepared in light free environment and stored at a low temperature.The pH value dropped 0.61 when it was kept in darkness at(40±2)℃for 10 days.It exhibited good stability both in the accelerated and long-term test.Conclusion The physicochemical properties of coenzyme Q10 emulsion with a high oil concentration meet the quality requirements for intravenous injection with good stability.