口服降糖药治疗新诊断的2型糖尿病疗效观察

目的观察口服降糖药对新诊断的2型糖尿病的疗效。方法 35例新诊断的2型糖尿病患者,给予格列美脲及阿卡波糖口服,观察服药后血糖达标时间。结果治疗1周后血糖明显下降,2周血糖达标,1个月降糖药物开始减量,3个月后有6例患者停服所有降糖药物。结论格列美脲(亚莫利)与阿卡波糖(拜糖平)联合应用可明显改善高血糖状态。     

预混人胰岛素联合格列美脲治疗老年2型糖尿病疗效观察

目的对单用预混人胰岛素（30%短效与70%中效）血糖控制不佳的老年2型糖尿病患者联合应用格列美脲,观察其疗效及安全性。方法选取2006年1月至2008年3月符合纳入标准的共21名门诊就诊老年2型糖尿病患者,继续原有预混胰岛素治疗方案（均为每日早晚两次注射）,加用格列美脲2mg/d,门诊随访（加药后第1周第一次,以后每2周一次,至第13周）,采用t检验,对比分析基线及治疗后1周、13周后空腹及餐后血糖,基线及治疗13周后糖化血红蛋白（HbA1c）、尿微量白蛋白、胰岛素用量、肝功、肾功。结果 （1）加用格列美脲前患者平均空腹血糖（9.1±2.7）mmol/L,早餐后血糖（13.6±2.3）mmol/L,平均HbA1c（7.7±1.4）%;加药后13周平均空腹血糖（6.7±2.3）mmol/L,早餐后血糖（10.5±1.9）mmol/L,HbA1c（6.8±1.2）%,血糖、HbA1c明显下降,差异有统计学意义（P〈0.05）。（2）加用格列美脲前及加药后13周预混胰岛素用量分别为（53±4.5）U/d、（45±2.9）U/d,胰岛素用量下降,差异有统计学意义（P〈0.05）。结论每日两次注射预混人胰岛素联用格列美脲对老年2型糖尿病患者能改善血糖控制,安全性较好,方法简单,经济花费亦不高,依从性好,对符合条件的门诊老年2型糖尿病患者是一种较好的选择。     

格列美脲治疗2型糖尿病有效性及安全性系统评价

目的本研究旨在探讨格列美脲治疗2型糖尿病降糖的疗效,并对其安全性进行评价。方法选择我院2008年1月～2010年2月收治的100例2型糖尿病患者作为研究对象,随机分为观察组和对照组各50例,观察组给予格列美脲治疗,对照组采用格列本脲治疗,疗程3个月,观察比较两组治疗前后空腹血糖(FBG)、餐后2h血糖(2hPPG)、BIM、血脂、血压的变化以及不良反应情况。结果治疗组50例采用格列美脲治疗的总有效率为94.0%(47/50),明显高于对照组有效率70.0%,两组总有效率比较差异有统计学意义(P0.05)。两组治疗3个月后,FBG、2hPBG、BMI均明显降低(P0.05),且治疗组下降更明显,但两组间治疗前后分别比较,差异无统计学意义(P0.05)。两组经3个月治疗后,两组的血脂TC、TG、HDL-C、LDL-C指标及血压指标SBP、DBP均变化不明显,两组组内及组间比较,差异均无统计学意义(P0.05)。治疗组共计出现低血糖、头痛、腹痛、腹部不适2例,经对症处理后明显好转,不良反应的发生率为4.0%(2/50),对照组出现头晕、胃部不适等共8例,不良反应的发生率为16.0%(8/50),经对症治疗后均缓解或消失。两组不良反应发生率比较,差异有统计学意义(P0.05)。结论格列美脲治疗2型糖尿病疗效较好,不良反应发生率较低,且可明显降低FBG、2hPBG,是一种值得临床推荐的安全、有效、理想的降糖药物。     

2型糖尿病患者在磺脲类药物疗效不佳改用胰岛素疗法后续用格列美脲的作用

目的 探讨2型糖尿病患者在磺脲类药物用至足量后血糖控制不佳而改用胰岛素疗法后续用格列美脲的作用.方法 80例口服足量磺脲类药物血糖控制不佳的2型糖尿病患者先均改用格列美脲（3 mg,1次/d）8周,如血糖仍不达标者再改用胰岛素疗法（皮下注射门冬胰岛素30 U,2次/d）.随机分为续用格列美脲组和不续用格列美脲组,观察两组空腹血糖（FPG）及餐后2 h血糖（2hPG）、糖化血红蛋白（HbA1c）、体重指数（BMI）、胰岛素用量、低血糖发生次数等变化.结果 治疗28周及48周时,两组FPG、2hPG均较用胰岛素前明显下降.从第8周到28周,续用格列美脲组HbA1c从（9.2±1.1）%降至（7.9±1.0）%,并于48周进一步降至（7.1±0.6）%,不续用格列美脲组HbA1c从（9.1±1.0）%降至（8.3±0.9）%,但48周时HbA1c为（8.4±1.1）%.结束观察时续用格列美脲组日用胰岛素量比不续用格列美脲组少,分别为（0.21±0.12）U/（kg·d）和（0.34±0.13）U/（kg·d）.治疗过程中出现低血糖的患者,续用格列美脲组9例,不续用格列美脲组7例,差异无统计学意义（P〉0.05）.两组均无严重低血糖事件发生.结论 在改为胰岛素治疗时,续用格列美脲药物可以减少胰岛素用量,更有效地控制血糖,而不增加低血糖风险.     

Microparticle size control and glimepiride microencapsulation using spray congealing technology

Drug-free microparticles were prepared using a spray congealing process with the intention of studying the influence of processing parameters. By varying the atomizing pressure and liquid feed rate, microparticles with median sizes (d_(0.5)) from 58 to 278 μm were produced, with total process yields ranging from 81% to 96%. An increased liquid feed rate was found to increase microparticle size, and higher atomizing pressures were found to decrease microparticle size. Greater change in microparticle size was achieved by varying atomizing pressure, which can be considered a dominant process parameter regarding microparticle size. In addition, microparticles with glimepiride, a model poorly water-soluble drug, were prepared by spray congealing using three different hydrophilic meltable carriers: Gelucire^® 50/13, poloxamer 188, and PEG 6000. Spherical microparticles with relatively smooth surfaces were obtained, with no drug crystals evident on the surfaces of drug-loaded microparticles. XRPD showed no change in crystallinity of the drug due to the technological process of microparticle production. All glimepiride-loaded microparticles showed enhanced solubility compared to pure drug; however, Gelucire^® 50/13 as a carrier represents the most promising approach to the dissolution rate enhancement of glimepiride. The influence of storage (30 °C/65% RH for 30 days) on the morphology of glimepiride/Gelucire^® 50/13 microparticles was studied, and the formation of leaf-like structures was observed (a “blooming” effect).     

格列美脲治疗2型糖尿病的系统评价

目的对公开发表的格列美脲治疗2型糖尿病的文献进行系统评价,评价格列美脲对2型糖尿病的疗效。方法检索中文期刊全文数据库(CNKI),收集格列美脲治疗2型糖尿病的随机对照试验(RCT),采用Revman 5.0软件做Meta分析。结果纳入14篇中文RCT,0篇英文文献,共累计病例1 604例。其中,治疗组816例,对照组788例。Meta分析结果显示,两组差异有统计学意义。格列美脲可减少2型糖尿病患者的三酰甘油(TG)、总胆固醇(TC)、空腹血糖(FBG)、低密度脂蛋白(LDL-C),同时,升高高密度脂蛋白(HDL-C)、C肽,其中,格列美脲对TG、TC、FBG及HDL-C的改善优于常用降糖药。敏感性分析结果也与以上研究结果一致。结论格列美脲治疗2型糖尿病明显优于对照组。但由于高质量的文献较少,样本量有限,需做深入研究。     

格列美脲片剂与滴丸体外溶出度比较

目的:比较格列美脲片剂和滴丸体外溶出度。方法:按2005年版《中国药典》中相关方法进行体外溶出度试验,以紫外分光光度法测定格列美脲的含量,分别计算累积溶出百分率;以Weibull方程拟合溶出参数T50、Td、m、r,再对溶出百分率数据进行分析。结果:溶出时间5min时片剂与滴丸溶出百分率分别约为18.70%、40.25%,45min时,片剂与滴丸的累积溶出百分率分别约为90.32%、99.96%,片剂与滴丸T50、Td、m、r结果分别为14.55、6.14,20.35、8.45,1.091、1.146,0.9968、0.9884,片剂与滴丸体外溶出度比较具有显著性差异(P<0.05)。结论:格列美脲滴丸比片剂溶出速度快。     

格列美脲与格列吡嗪治疗初诊超重的2型糖尿病疗效比较

目的：比较格列美脲与格列吡嗪对初诊超重的2型糖尿病（T2DM）的临床疗效。方法：T2DM患者64例,随机分为2组,格列美脲组31例,格列吡嗪组33例,疗程均为12周。观察2组血糖、胰岛素、血脂、体重指数（BMI）等的变化及不良反应。结果：2组降空腹血糖、餐后2小时血糖及糖化血红蛋白作用相似,对空腹胰岛素水平影响2组无差异。治疗12周后2组餐后2h胰岛素水平均升高,升高程度格列美脲组低于格列吡嗪组,差异有显著性（P〈0．01）。格列美脲组病人BMI下降,二组之间比较差异有显著性（P〈0．05）。低血糖反应发生率格列美脲组（3．2％）低于格列吡嗪组（12．1％）,二组间差异有显著性（P〈0．05）。结论：格列美脲对初诊超重T2DM不仅能有效降低血糖且能降低BMI,较少的升高胰岛素水平。     

Synthesized nano particles of glimepiride via spray freezing into cryogenic liquid: characterization,antidiabetic activity,and bioavailability

The aim of this work was to formulate glimepiride (class II drug) which is characterized by low solubility and high permeability as nanostructured particles using a cryogenic technique with an aid of water-soluble polymer to improve its aqueous solubility and hence its bioavailability. 27 formula of glimepiride nano size particles were prepared by a spray freezing into cryogenic liquid (SCFL) using poly vinyl pyrrolidone K-30 (PVP K-30); that three drug polymer ratio (1:1, 1:2, and 1:3), with three different volumes of feeding solution (50, 100, 150 mL), at three flow rates (10, 20, and 30 mL/min). The prepared formulations were evaluated for production yield, particle size, zeta potential, drug content, release rate, in vivo hypoglycemic activity, and bioavailability. All prepared formulations showed high production yield and drug content ranged between 91.1 ± 3.4% and 94.3 ± 1.8% and 95.1 ± 2.8% and 97.1 ± 2.5%, respectively. The mean particles size was ranged between 280 ± 62 nm and 520 ± 30 nm. The results of in vitro release study revealed significant enhancement in the solubility of prepared formulations compared with the pure drug. It was found that optimal formula showed a significant reduction in blood glucose levels in diabetic rats, and 1.79-fold enhancements in oral bioavailability compared with market tablets. Nanoparticle prepared by SCFL method is an encouraging formula for improving the solubility and the bioavailability of glimepiride.