辅酶Q10的纯化

应用大孔吸附树脂和硅胶柱色谱制备高纯度辅酶Q10.检测了7种大孔树脂对辅酶Q10的吸附及解吸性能,确定HZ816为最佳吸附剂.工艺条件为:以无水乙醇为溶剂,上样浓度1.6～1.8 mg/ml,吸附流速3 BV/h,上样体积14 BV;分步洗脱:先用5 BV无水乙醇洗脱,流速3 BV/h;然后用丙酮洗脱.经初步纯化,辅酶Q10纯度从56.5％提高到93.4％,回收率78.4％.利用硅胶柱色谱进一步纯化,获得纯度99％的辅酶Q10.     

辅酶Q10片与辅酶Q10胶囊溶出度试验方法的探讨

辅酶Q1 0 是一种脂溶性药物 ,临床主要用于慢性缺血性心脏病及高血压性心脏病的治疗。辅酶Q1 0 片和胶囊是 2 0 0 1年国家重点考察品种之一 ,作者在崩解时限检查时发现 ,辅酶Q1 0 胶囊样品囊壳虽已崩解 ,但胶囊内容物聚结成小颗粒通过筛网后仍悬浮在水面。因此 ,作者对辅酶Q1 0 片与辅酶Q1 0胶囊的溶出度方法进行了探讨。1　仪器与试药D - 80 0LS智能药物溶出仪 (天津大学无线电厂) ,UV - 2 2 0 1型分光光度计 (日本岛津公司 ) ,辅酶Q1 0 对照品 (中国药品生物制品检定所 ) ,辅酶Q1 0 片 [卫材 (苏州 )制药有限公司 ] ,辅酶Q1 0 胶囊 …     

发酵法生产辅酶Q10的研究进展

微生物发酵法生产辅酶Q10因其具有生物活性高、没有原材料的限制并实现了产业化等优点而受到国内外学者的关注。该文概述菌株选育及代谢调节工艺优化等方面的研究进展。     

Protective effects of Coenzyme Q10 against acute pancreatitis

Acute pancreatitis (AP) refers to inflammation in the pancreas, which may lead to death in severe cases. Coenzyme Q10 (Q10), generally known to generate energy, plays an important role as an anti-oxidant and anti-inflammatory effector. Here, we showed the effect of Q10 on inflammatory response in murine AP model. For this study, we induced AP by injection of cerulein intraperitoneally or pancreatic duct ligation (PDL) in mice. The level of cytokines and digestive enzymes were measured in pancreas, and blood. All pancreatic tissues were excised for investigation such as histological changes, infiltration of immune cells. Administration of Q10 attenuated the severity of AP and its associated pulmonary complication as shown by reduction of acinar cell death, parenchymal edema, inflammatory cell infiltration and alveolar thickening in both cerulein-induced AP and PDL-induced AP. Moreover, reduction of the cytokines such as interleukin (IL)-1β, IL-6 and tumor necrosis factor (TNF)-α were observed in pancreas and pancreatic acinar cells by Q10. Furthermore, Q10 reduced the infiltration of immune cells such as monocytes and neutrophils and augmentation of chemokines such as CC chemokine-2 (CCL2) and C-X-C chemokine-2 (CXCL2) in pancreas of AP mice. In addition, Q10 deactivates the phosphorylation of extracellular signal-regulated kinase (ERK) and c-jun NH₂-terminal kinase (JNK) in pancreas. In conclusion, these observations suggest that Q10 could attenuate the pancreatic damage and its associated pulmonary complications via inhibition of inflammatory cytokines and inflammatory cell infiltration and that the deactivation of ERK and JNK by Q10 might contribute to the attenuation of AP.     

辅酶Q10眼用微乳的研制

目的研制适合眼部用药的辅酶Q10微乳制剂。方法以溶解度、乳化效率及伪三元相图法筛选最佳油相、乳化剂及助乳化剂;以星点设计-效应面法及制备工艺的单因素考察,优化处方和工艺;并进行了辅酶Q10微乳制剂在角膜的滞留时间,辅酶Q10眼用微乳的稳定性初步评价以及家兔眼部刺激性实验的考察。结果经处方筛选和星点效应面法优化得出最佳处方为:MCT,Cremophor EL,Capmul MCM C8 EP分别为油相,乳化剂和助乳化剂,比例为3∶5∶2,药用浓度为10 mg·mL 1;乳化温度和时间对粒径没有明显影响;高温、强光考察10 d,粒径、pH值和含量均有明显变化,低温保存各指标没有变化明显;辅酶Q10微乳在家兔角膜滞留可达2 h;刺激性实验显示该制剂对家兔眼部无刺激性。结论该处方及工艺筛选、优化法简便可行,容易控制,制备的眼用微乳可延长在角膜的滞留时间,安全无刺激,低温避光保存稳定,适合眼部用药。     

辅酶Q10包合物的制备及其稳定性

目的 提高辅酶Q<,10>胶囊含量的稳定性.方法 将辅酶Q<,10>与β-环糊精混合,制成辅酶Q<,10>环糊精包合物,并通过正交试验优化包合工艺.结果 用包合工艺生产的辅酶Q<,10>胶囊在2年内含量稳定.结论 辅酶Q<,10>-环糊精包合物的制备工艺可用于辅酶Q<,10>胶囊的生产.     

辅酶Q10氯化钠注射液的制备工艺

目的：制备优良的辅酶Q10氯化钠注射液。方法：采用正交设计试验对处方工艺进行研究,对关键生产技术进行控制,保证产品质量,按照确定的处方工艺中试3批样品,并将样品进行影响因素考察。结果：最佳配制温度、聚山梨酯80的加入量、抗氧剂和络合剂分别为4550℃、0.1%、0.01%亚硫酸氢钠和0.01%依地酸钙钠。结论：按该方法制备的辅酶Q10氯化钠注射液,完全符合自拟质量标准。     

辅酶Q_(10)亚微乳的制备及理化性质考察

目的:制备辅酶Q10亚微乳,并考察其稳定性及理化性质。方法:设计正交试验优选辅酶Q10亚微乳的处方及制备工艺并制备乳剂,以高效液相色谱法测定其含量及包封率,考察其粒径、ζ电位、pH值及稳定性等。结果:辅酶Q10亚微乳的最佳处方工艺为大豆油∶中碳链甘油三酸酯=1∶2,大豆磷脂∶泊洛沙姆188=3∶1,高速剪切乳化时间10min,制备温度60℃。所制备的乳剂包封率3批样品平均值为98.07%,ζ电位为—28.4mV,平均粒径为168nm。该制剂贮存时应避免光照和冻融,在4℃条件下稳定性较好。结论:所制备的辅酶Q10亚微乳满足静脉注射用制剂要求。     

辅酶Q10黄芪注射液治疗病毒性心肌炎

目的探讨辅酶Q10,黄芪注射液治疗病毒性心肌炎的临床效果.方法治疗组在常规治疗的基础上加辅酶Q10和黄芪注射液.结果治疗组显效率为91.65%,对照组显效率为79.5%两组有显著性差异,P＜0.05.结论辅酶Q10黄芪注射液具有抗病毒、调节免疫、保护心肌,改善心功能作用.     

Coenzyme Q10 oral bioavailability: effect of formulation type

Coenzyme Q10 (Q10) has a poor bioavailability due to its very low aqueous solubility and high molecular weight. The purpose of this review is to discuss the different types of Q10 drug delivery systems (DDS) ranging from the simple oily dispersions to the nanotechnology-oriented systems such as nanocrystals, self-nanoemulsified drug delivery systems, etc. to overcome the solubility issue. The basics of these approaches were discussed in relationship to the effect of Q10 absorption. For that purpose, the percentage of the drug absorbed to the blood stream out of the administered dose was calculated as the fraction absorbed (Fa%). The Fa% for the nanoemulsions discussed in this article did not correlate with droplet size. In human studies most of the delivery systems had a low Fa% being in the range from 1.53 to 12.48 %. The highest Fa% value was found to be for the self-emulsified drug delivery systems (SEDDS). In dogs studies, the Fa% values ranged between 0.28 (cyclodextrin complex) and 4.8 %. In rat studies, some other DDS like emulsions and solubilized formulations showed Fa% of around 0.22 %. The relationship between the average Fa% in rats, dogs and humans was found to be 1:15:20. One recent study applied both oral and intravenous delivery of Q10; the orally tested SEDDS formulation had an absolute bioavailability of 2.2 % corresponding to Fa% = 0.04 %. The studies with Q10 formulations based only on in vitro data were also discussed and assessed regarding the influence of formulation on solubility, release and/or uptake.     

产辅酶Q10细菌CPU0402的初步研究

为了实现用微生物发酵法生产辅酶Q10，筛选出一株辅酶Q10高产菌株，并对其从C源、N源、最适温度、最适pH值、通氧量、添加前体等方面进行了优化。筛选出的菌株用不同的碳源、氮源在37℃培养24h，检测其CoQ10含量；以富马酸为碳源、玉米浆为氮源、35℃、pH7．2发酵24h辅酶Q10含量达87mg／L；通氧量对该菌生长及辅酶Q10合成有促进作用；添加前体对羟基苯甲酸、异戊二烯、β-胡萝卜素均可有效提高辅酶Q10产量，其中异戊二烯可提高产率178．4％。该菌辅酶Q10产量较高，经TLC-UV法定量，HPLC法进行纯度检测，红外、质谱分析进行成品鉴定，其纯度达99．5％。     

辅酶Q10制剂新技术研究进展

目的介绍辅酶Q10制剂新技术研究最新进展。方法检索近年来国内外相关文献并整理、分析。结果与结论通过固体分散体技术、环糊精包合技术、乳化技术、自微乳化技术、脂质体技术等物理改性方式可显著提高其生物利用度，丰富辅酶Q10的使用途径。     

辅酶Q10静脉注射乳的制备及其体外释放研究

目的制备辅酶Q10静脉注射乳,并研究其体外释放行为。方法对处方组成进行响应面优化,确定最佳处方。用激光粒度仪测定乳剂粒径、Zeta电位,透射电镜观察乳滴形态,初步考察乳剂稳定性及体外释放行为。结果油水比与磷脂用量对其稳定性系数Ke的影响较大,采用最佳处方制备的乳剂平均粒径为172±19.2 nm,Zeta电位为-33.1±2.9 m V。体外药物的释放试验中,反透析法比透析法稍快。结论所制备的辅酶Q10静脉注射乳质量可控,稳定性良好,具一定缓释作用。     

Coenzyme Q10 counteracts testicular injury induced by sodium arsenite in rats

The protective effect of coenzyme Q10 against testicular toxicity induced by sodium arsenite (10mg/kg/day, orally for two consecutive days) was investigated in rats. Coenzyme Q10 treatment (10mg/kg/day, i.p.) was applied for five consecutive days, starting three days before arsenite administration. Coenzyme Q10 significantly increased serum testosterone level which was reduced by sodium arsenite. Coenzyme Q10 significantly suppressed lipid peroxidation, restored the depleted antioxidant defenses, and attenuated the increases of tumor necrosis factor-α and nitric oxide resulted from arsenic administration. Also, the elevation of arsenic ion, and the reductions of selenium and zinc ions in testicular tissue were mitigated by coenzyme Q10. Histopathological examination showed that testicular injury mediated by arsenic was ameliorated by coenzyme Q10 treatment. Immunohistochemical analysis revealed that coenzyme Q10 significantly decreased the arsenic-induced expression of inducible nitric oxide synthase, nuclear factor-κB, Fas ligand and caspase-3 in testicular tissue. It was concluded that coenzyme Q10 represents a potential therapeutic option to protect the testicular tissue from the detrimental effects of arsenic intoxication.     

CoQ10软胶囊在Beagle犬体内的相对生物利用度评价

目的:比较在 Beagle 犬体内3种辅酶 Q_(10)(CoQ_(10))制剂的相对生物利用度。方法:采用三制剂三周期(3×3拉丁方)自身对照交叉多剂量口服给药方式,周期间清洗1周。用高效液相色谱法测定6条健康 Beagle 犬口服 CoQ_(10)软胶囊(受试制剂A)、CoQ_(10)普通胶囊(参比制剂 B)和进口 CoQ_(10)软胶囊(参比制剂 C)后不同时间点血浆中 CoQ_(10)的浓度,扣除内源性 CoQ_(10)本底,绘制血药浓度-时间曲线,计算相对生物利用度。结果:受试犬口服 CoQ_(10)60mg 的受试制剂(A)和参比制剂(B,C)后,血浆中 CoQ_(10)AUC_(0-t)(μg·h·mL~(-1))分别为69.31±40.49,62.38±59.05,104.90±64.32。与参比制剂 B 与 C 相比,受试制剂中的相对生物利用度平均为(144.07±79.48)%和(78.60±54.28)%。结论:CoQ_(10)受试制剂 A 生物利用度高于参比制剂 B 而低于参比制剂 C。     

辅酶Q10防晒霜成分的紫外光谱研究

目的：研究辅酶Q10防晒霜成分的紫外光谱特性,评价其防晒效果。方法测定辅酶Q10防晒霜成分吸光度值,计算防晒指数。结果辅酶Q10吸光度值与防晒指数比甘草次酸、硫辛酸值高,同时配方三防晒指数比配方一、二值高。结论辅酶 Q10、甘草次酸、硫辛酸具有不同防晒效果;这3种配方可产生不同效果的防晒霜,发挥不同的防晒效果。