Kommuru T R, Ashraf M, Khan M A, Reddy I K
Division of Basic Pharmaceutical Sciences, School of Pharmacy, College of Pharmacy and Health Sciences, Northeast Louisiana University, Monroe, LA-71209, USA.
Chem Pharm Bull (Tokyo). 1999 Jul;47(7):1024-8. doi: 10.1248/cpb.47.1024.
Coenzyme Q10 (CoQ10), a highly lipophilic compound present in the inner mitochondrial membrane, is essential for production of cellular energy in the form of ATP. CoQ10 is used as an antioxidant and also in the treatment of various cardiovascular disorders. The relative bioavailabilities of powder filled capsule (I) and oil-based formulation (II) of CoQ10 were compared in beagle dogs in an open, randomized, multiple dose, cross-over design. Poor and slow absorption characteristics were observed for both the formulations. The AUC, Cmax, and Tmax for formulation I and II are comparable (p < 0.05) where the values for formulation I are 22.84 +/- 6.3 micrograms ml-1 h, 0.51 +/- 0.11 microgram/ml, and 6.1 +/- 2.0 h whereas the values for formulation II are 24.32 +/- 5.6 micrograms ml-1 h, 0.55 +/- 0.16 microgram/ml, and 6.6 +/- 2.3 h, respectively. Stability of CoQ10 at various temperature and humidity conditions and its photostability were studied. Various antioxidants were evaluated to determine the type and amount of antioxidant(s) required to improve the stability of CoQ10. Large extent of degradation was observed at 45 degrees C and 55 degrees C. The effect of humidity conditions on degradation was insignificant. Among the various antioxidants studied, mixture of ascorbic acid (5%) and EDTA (0.1%) offered better protection than phenolic antioxidants such as butylated hydroxy anisole (BHA), butylated hydroxy toluene (BHT), or propyl gallate (PG). Further, increasing concentrations of phenolic antioxidants (from 0.1 to 0.3%) accelerated the degradation.
辅酶Q10（CoQ10）是一种存在于线粒体内膜的高度亲脂性化合物，对于以三磷酸腺苷（ATP）形式产生细胞能量至关重要。CoQ10用作抗氧化剂，也用于治疗各种心血管疾病。在比格犬中采用开放、随机、多剂量、交叉设计对比了CoQ10的粉末填充胶囊（I）和油基制剂（II）的相对生物利用度。两种制剂均观察到吸收不良和吸收缓慢的特性。制剂I和II的AUC、Cmax和Tmax具有可比性（p<0.05），其中制剂I的值分别为22.84±6.3微克·毫升⁻¹·小时、0.51±0.11微克/毫升和6.1±2.0小时，而制剂II的值分别为24.32±5.6微克·毫升⁻¹·小时、0.55±0.16微克/毫升和6.6±2.3小时。研究了CoQ10在不同温度和湿度条件下的稳定性及其光稳定性。评估了各种抗氧化剂，以确定提高CoQ10稳定性所需的抗氧化剂类型和用量。在45℃和55℃观察到大量降解。湿度条件对降解的影响不显著。在所研究的各种抗氧化剂中，抗坏血酸（5%）和乙二胺四乙酸（EDTA，0.1%）的混合物提供的保护优于酚类抗氧化剂，如丁基羟基茴香醚（BHA）、丁基羟基甲苯（BHT）或没食子酸丙酯（PG）。此外，酚类抗氧化剂浓度的增加（从0.1%至0.3%）加速了降解。
