阿卡波糖对缺血性心脏病伴糖耐量异常患者的干预作用研究

目的 探讨阿卡波糖对缺血性心脏病伴糖耐量异常患者的干预作用.方法 收集缺血性心脏病伴糖耐量异常患者共187例,分为试验组(阿卡波糖干预组)97例;对照组90例,平均随访3.5年.观察其血糖及心血管事件的发生情况.结果 187例患者,死亡6例,两组BMI、TG较治疗前均显著下降(P<0.05),试验组OGTT2h、HbA1c较治疗前均显著下降(P<0.05);急性心肌梗死发生率、新发生的心绞痛发生率及总的心血管事件发生率显著降低(P<0.05);试验组发展为DM数较对照组显著降低(P<0.05). 结论 阿卡波糖对缺血性心脏病伴糖耐量异常患者进行干预,能有效降低心血管事件的发生及减少DM的发生率.     

Influence of treatment with acarbose or glibenclamide on insulin sensitivity in type 2 diabetic patients

Aim: The aim of our double-blind, placebo-controlled study was to compare the effect of acarbose and glibenclamide on the insulin sensitivity in type 2 diabetes.
Methods: We investigated 77 patients (mean age 58.7 years, mean BMI 27.3 kg/m²), treated by diet alone for at least 4 weeks. The subjects were randomized into three treatment groups for 16 weeks: 100 mg t.i.d. acarbose ( n  = 25) or 1 mg t.i.d. glibenclamide ( n  = 27) or one t.i.d. placebo ( n  = 25). Before and after therapy, the levels of fasting plasma glucose, glycosylated haemoglobin, fasting insulin, plasma glucose and insulin 1 h after a standardized breakfast were measured and insulin sensitivity determined by euglycaemic hyperinsulinaemic clamp test.
Results: After the treatment period, BMI in the acarbose and placebo group decreased significantly, whereas in the glibenclamide group a significant increase was observed. Fasting plasma glucose was only significant reduced under glibenclamide. The postprandial glucose decreased significantly after acarbose (13.8 vs. 11.4 mmol/l, p < 0.05) and glibenclamide treatment (14.6 vs. 11.4 mmol/l, p < 0.05) and was unchanged under placebo (13.8 vs. 13.7 mmol/l). The fasting insulin levels remained unchanged in all three groups, whereas postprandial insulin values increased significantly under glibenclamide. Neither acarbose nor glibenclamide significantly changed insulin sensitivity [acarbose: glucose disposal rate before treatment 2.3 mg/kg body weight/min/insulin, after treatment 3.2; glibenclamide 2.2 vs. 2.1; placebo 2.6 vs. 3.0].
Conclusions: Our results show a more substantial improvement of glucose control under glibenclamide than under acarbose which, however, was not associated with an increase of insulin sensitivity.     

阿卡波糖联合诺和锐30治疗2型糖尿病血糖控制欠佳患者的疗效观察

目的 探讨阿卡波糖联合诺和锐30治疗2型糖尿病血糖控制欠佳者的临床疗效。方法 南京大学医院收治的52例血糖控制欠佳的2型糖尿病患者随机分为治疗组（27例）和对照组（25例）。对照组给予诺和锐30注射液,2次/d,早晚餐前皮下注射。治疗组于三餐前口服阿卡波糖片,50 mg/次,3次/d,诺和锐30注射液的用法同对照组。治疗12周后,比较两组患者治疗前后空腹血糖（FBG）、餐后2 h血糖（2 h PG）、糖化血红蛋白（HbA1c）、体质量指数（BMI）、血脂变化情况及胰岛素用量。结果 治疗后,两组患者FBG、HbA1c均较治疗前明显降低,治疗前后差异有统计学意义（P<0.05）。治疗后,治疗组患者HbA1c水平明显低于对照组,两组比较差异有统计学意义（P<0.05）。治疗后,两组全天七点血糖水平均较治疗前明显降低,同组治疗前后差异有统计学意义（P<0.05）;同时,治疗组三餐后2 h PG均显著低于对照组,两组比较差异有统计学意义（P<0.05）。治疗组血糖达标时间明显短于对照组,两组比较差异有统计学意义（P<0.05）。结论 阿卡波糖联合诺和锐30治疗血糖控制欠佳的2型糖尿病患者具有较好的临床疗效,可有效控制餐后血糖水平,具有良好的临床应用价值。     

The effect of acarbose on insulin resistance in obese hypertensive subjects with normal glucose tolerance: a randomized controlled study

Aim:  Acarbose, a glucose oxidase inhibitor, delays the absorption of glucose thus reducing post-prandial blood glucose level, haemoglobin A1c (HbA1c) and insulin resistance in patients with diabetes mellitus and in subjects with impaired glucose tolerance. The effect of acarbose in subjects with normal glucose tolerance (NGT) has hitherto not been examined. The aim of the present study was to examine the effect of acarbose in obese hypertensive subjects with NGT.
Methods:  A double-blinded, parallel group study was performed on 56 male subjects with hypertension, body mass index (BMI) 27–35 kg/m², fasting blood glucose ≤ 6 mmol/l and a normal oral glucose tolerance test. Blood pressure, HbA1c, lipid profile and insulin resistance [homeostasis model assessment (HOMA) index] were determined initially and following 24 weeks of acarbose, 150 mg/day or placebo. The primary end point was the change in insulin resistance. Anti-hypertensive treatment and diet were kept constant during the study.
Results:  Insulin resistance decreased in acarbose users but not on placebo. HOMA index declined from 5.36 ± 1.7 to 4.10 ± 1.6 (p = 0.001) on acarbose, the corresponding values on placebo were 5.44 ± 1.9 and 5.53 ± 1.7. A decrease in serum triglyceride values (2.16 ± 0.16 mmol/l to 1.76 ± 0.15 mmol/l, p = 0.02) took place on acarbose with no change on placebo. There was no change in BMI, low-density lipoprotein or high-density lipoprotein values in either group. Blood pressure declined equally in both the groups, probably due to better patient compliance.
Conclusions:  Acarbose may reduce insulin resistance and triglycerides also in obese hypertensive subjects with normal glucose tolerance.     

α-Glucosidase inhibitors and their use in clinical practice

Post-prandial hyperglycemia still remains a problem in the management of type 2 diabetes mellitus. Of all available anti-diabetic drugs, α-glucosidase inhibitors seem to be the most effective in reducing post-prandial hyperglycemia. We conducted a review analyzing the clinical efficacy and safety of α-glucosidase inhibitors, both alone and in combination with other anti-diabetic drugs, with respect to glycemic control, inflammation and atherosclerosis. α-Glucosidase inhibitors proved to be effective and safe both in monotherapy and as an add-on to other anti-diabetic drugs. Compared to miglitol and voglibose, acarbose seems to have some additive effects such as stabling carotid plaques, and reducing inflammation. Acarbose also proved to reverse impaired glucose tolerance to normal glucose tolerance.     

阿卡波糖片的亲水色谱法测定

建立了亲水色谱法测定阿卡波糖片的含量及其有关物质.采用Phenomenex氨基柱,以6 mmol/L磷酸二氢钾缓冲液(pH 6.8)-乙腈(28:72)为流动相,检测波长210nm.阿卡波糖在4～20mg/ml浓度范围内线性关系良好.平均回收率为99.2%,RSD为0.7%.     

阿卡波糖的上市后评价与风险控制研究

通过对阿卡波糖安全性相关的国内外文献报道、上市后的安全性、有效性、经济学研究状况及世界卫生组织不良反应监测中心数据库中有关安全性信息的分析,系统评价了阿卡波糖上市十余年来的安全性及有效性,提出符合疾病和药品本身特点的风险控制措施。为安全、合理使用该药提供了依据,同时明确提出了有利于维护产品生命周期及核心竞争力的研究方向。