野生与家种大花红景天的质量评价研究

大花红景天(Rhodiola crenulata)系景天科红景天属植物,以根及根茎入药,是珍贵的滋补品.     

大花红景天的化学成分研究

目的研究景天科大花红景天的根和根茎中的化学成分。方法采用柱色谱法分离纯化,通过光谱数据鉴定其结构。结果从大花红景天的根和根茎乙醇提取物的石油醚部位、乙酸乙酯部位和正丁醇部位中分离得到12个化合物,分别鉴定为大花红天素(Ⅰ)、胡萝卜甾醇(Ⅱ)、草质素-7-氧-α-L-吡喃鼠李糖苷(Ⅲ)、阿魏酸二十八烷醇酯(Ⅳ)、酪醇(Ⅴ)、红景天苷(Ⅵ)、没食子酸(Ⅶ)、β-谷甾醇(Ⅷ)、正二十六烷酸(Ⅸ)、正二十六烷醇(Ⅹ)、正十八烷酸(Ⅺ)和十九烷(Ⅻ)。结论化合物Ⅱ、Ⅳ、Ⅸ、Ⅹ、Ⅺ、Ⅻ为首次从该植物中分离得到。     

比较大花红景天、红景天提取物药理作用的差异

目的:研究比较大花红景天、红景天提取物对小鼠抗疲劳、耐缺氧作用的差异.方法:采用小鼠常压耐缺氧和游泳法实验.实验组分为红景天提取物A组(含3%红景天苷和3%rosavin)、大花红景天提取物B组(含3%红景夭苷)和C组(舍12%红景天苷)3个提取物组,各提取物组以3.0、2.0、1.0 g·(kg·d)-1的剂量灌胃给予小鼠,对照组灌胃等量的蒸馏水.结果:与对照组比较,各提取物组的高、中、低剂量均能延长小鼠耐缺氧、抗疲劳的时间,且大花红景天提取物C组的高剂量有极显著的差异(P＜0.01).同等剂量下,红景天提取物A组与大花红景天提取物B组比较,没有显著差异(P＞0.05);大花红景天提取物C组与红景天提取物A组、大花红景天提取物B组比较,有显著差异(P＜0.05).在同一提取物组中,高剂量与低剂量比较,有显著差异(P＜0.05).结论:两种红景天的提取物都具有增强小鼠耐缺氧和抗疲劳的作用;大花红景天提取物对小鼠耐缺氧、抗疲劳作用更明显,且与红景天苷呈剂量关系.     

生活方式干预对糖尿病治疗的影响

目的:对糖尿病患者进行生活方式干预来观察治疗效果.方法:对60 例糖尿病5年以上的患者除药物治疗外,另加生活方式的干预,干预2个月后检测三餐前后血糖及糖化血红蛋白、血脂、体重的变化,及慢性并发症发展的检测.结果:在药物治疗的前提下,健康生活方式依从性好的糖尿病患者血糖稳定,糖化血红蛋白、血脂、体重均达标,大血管并发症无明显加重,未发现新的并发症.结论:生活方式的干预是提高糖尿病治疗效果的重要有效措施,它将对糖尿病并发症的发生发展起到积极的预防作用.     

RP-HPLC法测定大花红景天和长鞭红景天中红景天苷的含量

目的:建立测定大花红景天和长鞭红景天中红景天苷含量的方法。方法:采用反相高效液相色谱法。色谱柱为OPH RP-ODS C18(250mm×4.6mm,5μm),流动相为50mmol·L-1磷酸盐缓冲液(以氢氧化钠调pH值在7.0左右)-甲醇(90∶10),流速为1.0mL·min-1,柱温为室温,检测波长为253nm,进样量为10μL。结果:红景天苷的检测浓度在62.5～1000.0μg·mL-1范围内与峰面积积分值呈良好线性关系(r=0.9997);平均加样回收率为97.59%,RSD=1.71(n=6)。大花红景天中含有红景天苷,含量与等级呈线性关系;长鞭红景天含红景天苷较少或没有,不可作为其替代品。结论:本方法准确、灵敏、专属性强,可作为红景天药材中红景天苷的含量测定方法。     

红景天治疗糖尿病研究进展

红景天是珍贵的药用植物,大量研究表明该药对糖尿病及其并发症具有治疗作用,其机制可能与调节炎症反应、氧化应激和糖脂代谢等有关.该文通过检索文献,综述红景天治疗糖尿病及其并发症的作用与机制,以期为促进红景天药用植物资源利用提供参考.     

HPLC法测定大花红景天中红景天苷及没食子酸的含量

目的:建立大花红景天中红景天苷、没食子酸的含量测定方法。方法:采用YWG-C_(18)柱分离测定;甲醇-四氢呋喃-冰乙酸-水(0.1∶0.5∶2:97.4)为流动相;检测波长:270nm;流速:0.8mL·min~(-1)。结果:红景天苷在0.30-1.50μg,没食子酸在0.22-1.10μg范围内呈良好的线性关系,r=0.9994,r=0.9996,平均回收率分别为97.3%,RSD=2.0%;98.7%,RSD=2.3%.结论:本方法快捷、简便,结果准确、可靠,可做为红景天类药材有效成分的测定方法。     

社区优质护理对2型糖尿病患者生活方式的影响

目的探讨社区优质护理在患有2型糖尿病患者中的应用价值。方法随机选取160例患有2型糖尿病的患者,将其分成研究组（80例）与对照组（80例）,研究组实施社区优质护理,对照组运用常规护理。比较两组患者之生活方式的改善情况以及患者血糖的控制情况。结果研究组患者的运动规律、控盐情况、运动时间大于150min／周分别所占的比例为92．5％、87．5％、90％,均优于对照组（P〈0．05）。研究组的空腹血糖值（4．78±0．75）mmol／L、糖化血红蛋白5．4％分别低于对照组（P〈0．05）。结论社区优质护理在患有2型糖尿病老患者中的应用价值比较高,有益于改善患者的生活方式以及提升患者的生存质量。     

藏药大花红景天根茎的形态组织学研究

目的 鉴别大花红景天根茎的内部结构,并进行解剖学研究.方法 采用性状和显微鉴定方法.结果 其内部结构除具有双子叶植物的一般特征外,根的薄壁组织还具有发达的空腔隙,并且含有大量着色很深的异细胞.结论 通过对大花红景天的显微特征描述,可防止药材品种混淆.     

反相高效液相色谱法测定大花红景天及其混淆品中红景天苷的含量

目的建立RP-HPLC测定市场上大花红景天及其混淆品中红景天苷含量的方法。方法色谱柱为Phe-nomenex C18（250 mm×4.60 mm,5μm）,流动相为甲醇-水（15∶85）,等度洗脱,流速为1.0 mL.min-1,检测波长为223 nm,柱温为25℃。结果红景天苷在62.5～1 000μg.mL-1与峰面积线性关系良好（r=0.999 7,n=5）,平均加样回收率为100.1%,RSD为0.40%（n=6）。结论本方法简便、准确、重复性强,可用于市面上大花红景天及其混淆品中红景天苷的含量测定。     

Mitiglinide for type 2 diabetes treatment

Introduction: Mitiglinide, a rapid-acting insulin secretion-stimulating agent, is approved in Japan for the treatment of type 2 diabetes (T2DM). Rapid-acting insulin secretion-stimulating agents, also known as meglitinides, are not recommended as monotherapy, however, may be added to metformin therapy for those patients with continued postprandial hyperglycemia. Currently, repaglinide (Prandin®) and nateglinide (Starlix®) are the only US Food and Drug Administration-approved agents in this class of drugs.

Areas covered: This review describes the pharmacology, pharmacokinetics, efficacy, safety, and potential role in therapy of mitiglinide therapy. Phase II and III clinical studies have demonstrated that A1C levels should be expected to decrease by 0.17 – 1.1% with mitiglinide therapy. The most common adverse effects in these studies were hypoglycemia related.

Expert opinion: Meglitinides are limited by their cost, frequency of administration, and minimal available data assessing clinical impact; however, mitiglinide shows selective action on the pancreatic β-cells, has greater affinity for β-cells, and limited metabolism when compared to other meglitinides. These properties may allow more utility in patients with chronic kidney disease or at high risk of hypoglycemia. The primary role in therapy for mitiglinide is the treatment of elevated postprandial glucose in patients with T2DM.     

2型糖尿病的药物治疗

2型糖尿病的治疗已取得巨大进展。随着人们对2型糖尿病机制的不断探索,针对不同机制的新药层出不穷,最大限度地满足着患者的需求。笔者简述了当前2型糖尿病治疗药物的发展史,重点描述当前以胰高血糖素样肽-1(glucagon-likepeptide1,GLP-1)受体激动剂,DPP-4抑制剂和钠葡萄糖共转运蛋白-2(SGLT-2)抑制剂为代表的新型降糖药物的发现和研究热点。     

Pharmacokinetic drug evaluation of exenatide for the treatment of type 2 diabetes

Introduction: Glucagon-like peptide-1 (GLP-1) receptor analogs are a group of therapeutic agents which mimic endogenous GLP-1, exerting their effect by the stimulation of the GLP-1 receptor with a wide distribution. Its activation increases insulin releasing dependent on blood glucose levels, suppression of glucagon secretion and a reduction of hepatic glucose output. It delays gastric emptying and increases satiety. Exenatide is the synthetic version of exendin-4, a natural peptide with similar properties to human GLP-1. There are two pharmaceutical forms, for subcutaneous injection: twice daily and once weekly.

Clinical practice guidelines recommend them because of a high efficacy reducing hyperglycemia, low risk of hypoglycemia and a significative weight loss effect. Gastrointestinal adverse events are the most common beside injection site-related. Their cost is the main limitation to use.

Areas covered: We review the recent literature investigating the pharmacokinetics and pharmacodynamics and efficacy-safety studies of exenatide twice daily and once weekly in type 2 diabetes

Expert opinion: GLP-1 receptor analogs are now positioned as an effective and safe drug for the treatment of type 2 diabetes. Exenatide significally reduces HbA1c and fasting plasma glucose. Additionally, it produces moderate weight loss and decreases blood pressure. One weekly formulation may improve compliance while cost is still a limitation. EXSCEL trial has shown that, despite cardiovascular safety, exenatide do not exhibits cardiovascular benefits.     

Linagliptin for the treatment of type 2 diabetes (pharmacokinetic evaluation)

INTRODUCTION: Dipeptidyl peptidase-4 (DPP-4) inhibitors offer new options for the management of type 2 diabetes (T2DM). The novel compound linagliptin has important different pharmacokinetic (PK) properties, when compared with previously commercialized DPP-4 inhibitors, which may offer some advantages in clinical practice. Linagliptin has a unique PK/pharmacodynamic (PD) profile and is the first DPP-4 inhibitor with a nonrenal elimination route. Therefore, it can be administered in patients with renal impairment without dose adjustment or monitoring of renal function. The drug has a low potential for drug-drug interactions (DDIs) and no clinically relevant ones were reported so far. AREAS COVERED: An extensive literature search was performed to analyse primarily PK and secondarily PD characteristics of linagliptin in both healthy volunteers and patients with T2DM (treated with linagliptin as monotherapy or combined therapy). Updated information about linagliptin PK either after single administration (large dose range) or after chronic administration (steady state) were also included. A special focus has been put on DDIs and on PK/PD of linagliptin in patients with renal impairment. EXPERT OPINION: Head-to-head comparative studies and/or increased clinical experience with DPP-4 inhibitors will determine the clinical advantage, if any, of one agent over another.     

The treatment of type 1 diabetes mellitus with agents approved for type 2 diabetes mellitus

Introduction: The management of type 1 diabetes remains a challenge for clinicians. Current practice is to administer insulin analogues to best mimic normal physiological insulin profiles. However, despite our best efforts the majority of individuals with type 1 diabetes continue to suffer from suboptimal glucose control, significant hypoglycemia and microvascular tissue complications of the disease. There is thus a significant unmet need in the treatment of T1DM to obtain better glycemic control.

Areas covered: We discuss the use of α-glucosidase inhibitors, dipeptidyl-peptidase inhibitors, glucagon-like peptide 1 agonists, biguanides, thiazolidinediones and sodium glucose co-transporter 2 inhibitors in individuals with T1DM.

Expert opinion: Non-insulin therapies present a unique and exciting adjunctive treatment for individuals with type 1 diabetes. Although data are scarce, the classes of medications discussed help to lower glucose, decrease glycemic excursions and in some cases improve body weight, along with allowing dose reductions in total daily insulin. Glucagon-like peptide 1 agonists and sodium glucose co-transporter 2 inhibitors, in particular, have been demonstrated to provide clinical improvements in individuals with T1DM and we feel their use can be explored in obese, insulin-resistant patients with T1DM, those with frequent and significant glycemic excursions or individuals with persistently elevated hemoglobin A1c.     

An up-to-date evaluation of alogliptin benzoate for the treatment of type 2 diabetes

ABSTRACT

Introduction: A growth in the market for anti-diabetic drugs, along with an ever-increasing population suffering from type 2 diabetes mellitus (T2DM), requires a critical re-evaluation of anti-diabetic drugs used for a long time, in order to provide up-to-date practical prescribing information for clinicians. Alogliptin benzoate was firstly approved in 2010 in Japan for T2DM, both as a monotherapy or in combination with other anti-diabetic drugs.

Areas covered: This article provides a comprehensive review of the latest data on alogliptin benzoate, including hypoglycemic activity and safety.

Expert opinion: The cumulative evidence for alogliptin benzoate is robust with regards to glycemic efficacy and safety. Low hypoglycemia risks and weight changes support its consideration as a first-line medication for T2DM, either as a monotherapy or in combination therapy with other anti-diabetic drugs such as metformin. Ongoing trials will look to better analyze and address its safety and efficacy in pediatric patients and expand our clinical knowledge of this medication.     

A safety evaluation of canagliflozin: a first-in-class treatment for type 2 diabetes

Introduction: Numerous treatments are available for type 2 diabetes mellitus (T2DM), which can improve insulin sensitivity or stimulate its secretion. These are usually unable to halt progression. Inhibition of glucose reabsorption from the renal filtrate was proposed as a novel therapeutic target. Sodium/glucose co-transporter 2 (SGLT2) inhibitors were developed accordingly, with canagliflozin the first to launch in the US in 2013.

Areas covered: The mechanism of action of canagliflozin, its pharmacokinetic data and its clinical applications and efficacy data from clinical studies of both subjects with T2DM controlled on diet and exercise, and those on glucose-lowering agents and insulin. The evaluation focuses primarily on the safety of canagliflozin in clinical trials conducted for initial registration due to limited post-marketing data, discusses safety in special populations, before comparing its safety with existing therapies.

Expert opinion: Canagliflozin offers a novel therapeutic approach to T2DM; advantages include weight loss and blood pressure lowering with a low intrinsic risk of hypoglycaemia. The main adverse effects likely to be seen are a very small increase in risk of urinary tract infections and a modest risk of developing genital fungal infections. Studies suggest no increased risk of cardiovascular (CV) disease, but longer duration outcome studies are essential.     

Alogliptin for the treatment of type 2 diabetes: a drug safety evaluation

ABSTRACT

Introduction: Dipeptidyl peptidase-4 (DPP-4) inhibitors such as alogliptin are becoming more widely established as treatment options for patients with type 2 diabetes (T2DM) because of their ability to improve glycemic control without increasing the risk of hypoglycemia or weight gain. New therapies with improved safety profiles are needed, especially because of the chronic and progressive nature of T2DM.

Areas covered: In this article, the overall safety and tolerability of alogliptin are evaluated based upon a review of the literature. In particular, adverse events (AEs) that have been of interest for the DPP-4 class of drugs, such as the risk of major cardiovascular (CV) events and acute pancreatitis, will be investigated in detail.

Expert opinion: Alogliptin is generally well-tolerated in a broad range of patient populations including different ethnic groups and the elderly. In the pivotal EXAMINE clinical trial, alogliptin was found not to be associated with an increased risk of major CV events or acute pancreatitis/pancreatic cancer.     

Emerging treatment options for type 2 diabetes

Type 2 diabetes mellitus (T2DM) is rapidly increasing in prevalence and is a major public health problem. It is a progressive disease which commonly requires multiple pharmacotherapy. Current options for treatment may have undesirable side effects (particularly weight gain and hypoglycaemia) and contraindications, and little effect on disease progression. Incretin based therapy is one of several newer therapies to improve glycaemia and is available in two different forms, dipeptidyl peptidase-4 (DPP-4) inhibitors and glucagon-like peptide-1 (GLP-1) agonists. Use of these agents results in a ‘glucose-dependant’ increase in insulin secretion and glucagon suppression resulting in improved glycaemia with low incidence of hypoglycaemia. DPP-4 inhibitors are oral drugs which are weight neutral, while GLP-1 agonists are injected subcutaneously and help promote weight loss while improving glycaemia. GLP-1 agonists have also been shown to increase beta cell mass in rat models. Bariatric surgery is another option for the obese patient with T2DM, with blood glucose normalizing in over half of the patients following surgery. Other therapies in development for the treatment of T2DM include sodium-glucose transporter 2 (SGLT-2) inhibitors, glucagon receptor antagonists, glucokinase activators and sirtuins. In this article, we will review the various existing and emerging treatment options for T2DM.