格列齐特联合阿卡波糖治疗2型糖尿病疗效观察

目的：评价格列齐特缓释片联合阿卡波糖治疗2型糖尿病的有效性及安全性。方法：65例2型糖尿病患者根据血糖水平分为3组,分别给予格列齐特缓释片30mg、60mg、120mg,同时联合阿卡波糖片150mg治疗,观察各组血糖、糖化血红蛋白（HbAlc）水平。结果：联合治疗后,全组HbAlc从（8.8±0.75）%下降到（6.83±0.75）%,空腹血糖（FPG）从（9.7±1.86）mmol·L~（-1）下降到（6.56±0.40）mmol·L~（-1）,餐后血糖（PPG）从（15.1±2.35）mmol·L~（-1）下降到（8.87±2.1）mmol·L~（-1）。治疗前后比较,差异有统计学意义（P〈0.01）。且各剂量级患者治疗后HbAlc、FPG、PPG均较治疗前明显下降（P〈0.01）。试验期间发生低血糖事件15次,与药物剂量无关。结论：格列齐特缓释片与阿卡波糖联合治疗可有效的降低2型糖尿病患者的HbAlc、FPG、PPG水平,实现HbAlc达标。     

高效液相色谱法测定格列齐特缓释片的含量

目的 采用高效液相色谱法测定格列齐特缓释片的含量.方法 采用Diamonsil C18柱(250mm×4.6mm,5μm),流动相为乙腈-水-磷酸(70:30:0.1),流速为0.8 mL/min,检测波长为228 nm.结果 格列齐特在0.64～32 μg/mL浓度范围内呈良好线性(r=0.999 9,n=7),检测限为0.5 μg/mL,平均回收率为99.77%,RSD=1.07%(n=9).结论 本方法简便,准确,精密度好,适用于格列齐特缓释片的含量测定.     

Protective effect of gliclazide on diabetic peripheral neuropathy through Drp-1 mediated-oxidative stress and apoptosis

Objective: To investigate the protective effect of gliclazide and the role of dynamin-related protein l (Drp-1)-mediated oxidative stress and apoptosis in diabetic peripheral neuropathy (DPN). Methods: Diabetic rats developed through intra-peritoneal injection of streptozotocin were randomly assigned to treatment group receiving gliclazide or non-treatment group without gliclazide treatment. Rats in control group received intra-peritoneal injection of vehicle and no gliclazide treatment. Eight weeks later, the nerve conduction velocity (NCV) of sciatic nerve was measured and the morphological alterations, the malondialdehyde (MDA) level and superoxide-dismutase (SOD) activity, the expressions of Drp-1, caspase-3, Bax and Bcl-2 in sciatic nerve were evaluated. Results: When compared to rats in control group, rats in non-treatment group showed significantly decrease of NCV, obvious demyelinative alteration of sciatic nerve, increased expressions of Drp-1, caspase-3, Bax, Bcl-2 and MDA, and decreased SOD activity. Compared to rats in non-treatment group, rats in treatment group showed significantly increase of NCV, less demyelination of sciatic nerve, decreased expressions of Drp-1, caspase-3, Bax and MDA, and increased activity of SOD. The expression of Bcl-2 was not significantly different between treatment and non-treatment groups. Conclusion: Gliclazide showed protective effect on DPN through modulating Drp-1-mediated oxidative stress and apoptosis.     

格列齐特缓释剂治疗2型糖尿病的疗效研究

目的观察格列齐特缓释片治疗2型糖尿病的疗效。方法选取2011年9月—2012年6月在我院接受治疗的2型糖尿病患者100例,分成干预组和对照组,每组各50例。干预组在刚开始治疗时使用单纯的格列齐特普通制剂,在开始观察时改为使用格列齐特缓释片;对照组采用常规型制剂格列齐特。观察两组疗效。结果经过12周的治疗后,两组治疗效果差异无统计学意义(P>0.05)。干预组患者依从性明显优于对照组,差异有统计学意义(P<0.05)。结论格列齐特缓释片与常规剂型的治疗效果比较相似,并且安全性更佳。     

地特胰岛素联合格列齐特缓释片治疗2型糖尿病观察

目的：评价地特胰岛素联合格列齐特缓释片治疗继发性磺脲类降糖药失效（SFS）2型糖尿病患者的疗效及安全性.方法：48例SFS 2型糖尿病患者随机分为地特胰岛素联合格列齐特缓释片（D）组和门冬胰岛素30（R）组进行治疗.观察治疗前后两组体质指数（BMI）和糖化血红蛋白（HbAlc）水平,24h血糖达标时段、24 h平均血糖（MBG）、血糖波动幅度（MAGE）及以及低血糖发生频率及程度等.结果：与治疗前比较,治疗后两组血糖达标时段均明显延长,MBG及HbA1c均明显下降（P＜0.05）;治疗后两组间低血糖发生率差异无统计学意义（P＞0.05）,但D组MAGE及低血糖程度均低于R组（P＜0.05）.结论：地特胰岛素联合格列齐特缓释片能有效控制SFS的2型糖尿病患者血糖,安全性高.     

格列奇特中残留溶媒甲醇、乙酸乙酯的测定

目的：建立一种气相色谱法测定原料药格列奇特中甲醇和乙酸乙酯有机溶剂残留量的方法。方法：选正丙醇作内标物．以N,N-二甲基甲酰胺为溶剂在极性弹性石英毛细柱上进行各组分分离,效果良好。(采用程序升温)柱温100℃保留3分钟,以25℃／min的速率升160C保留5分钟。进样口温度200℃,检测器温度250℃,分流比70：1,载气：高纯氮气,流速：2．0ml／min。结果：平均回收率甲醇105．1％乙酸乙酯101．5％。结论：该方法克服了进样量不准确的缺点,重现性好,精度高。     

Formulation and characterization of extruded and spheronized pellets using pectin and crosslinking agents

The aim of this study was to prepare pellets of gliclazide by extrusion spheronization process by use of two methods in situ cross linking method and interracial complexation method and to study the effect of different cross linking agents on the formed pellets. Extrusion/spheronization being an established technique for producing spherical pellets so this technique was used to prepare pellets. The gliclazide pellets prepared by extrusion-spheronization techniques and then the formed pellets were coated with pectin solution by interfacial complexation method. The effect of cross-linkers calcium chloride and aluminium chloride concentration, by in situ cross linking on properties of gliclazide pellets like swelling and drug release were studied. The formed pellets were subjected to swelling, analysis of morphology, in dissolution and vivo studies. Most of the pellets were of acceptable shape. From the results calcium chloride when coated with pectin, retarded drug release. As the concentration of calcium chloride increased, it led to slow release of the drug. This may be due to the water solubility of calcium salt, which induced cross linking with pectin. Thus pellets with calcium chloride cross linked with pectin were beneficial, because it retarded the release of the drug. Though the release from interfacial coated pellets was retarded, it was less as compared to the in situ formed pellets. The in vivo studies on alloxan-induced diabetic rats indicated the significant hypoglycemic effect that was observed 24 h after oral administration of optimized pellets. Thus, the developed and optimized pellets were suitable for prolonged systemic absorption of gliclazide to maintain lower blood glucose level and improved patient compliance. The results suggested that the in situ cross linking pellets were able to retard the release of gliclazide greater than the interfacial complexation method. Therefore, this approach has been effectively achieved.